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303 Cards in this Set
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Acamprosate 1. Brand? 2. Class? 3. Indications? 4. Dose? |
Acamprosate 1. Campral 2. Alcohol dependence treatment 3. Maintenance of alcohol abstinence 4. 666mg TDS |
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Acamprosate 5. MOA? 6. Pharmacokinetics? |
Acamprosate 5. Reduces excitatory glutamate neurotransmission and increases GABA neurotransmission. Because withdrawal can lead to excessive glutamate activity and deficient GABA, alcamprosate can act as "artificial alcohol" to mitigate these effects. 6. Terminal half-life 20 - 33 hours Excreted unchanged via the kidneys |
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Acamprosate 7. Adverse effects? 8. Pearls? |
Acamprosate 7. GI effects (nausea, diarrhea) and Behavioural effects (depression and anxiety). 8. Preferred treatment if goal is complete abstinence but may not be preferred if the goal is reduced-risk drinking |
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Alprazolam 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. Xanax 2. Benzodiazepine 3. Generalised anxiety disorder, panic disorder 4. Anxiety: 1 to 4mg daily; Panic: 5 to 6mg daily |
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Alprazolam 5. MOA? 6. Pharmacokinetics? |
5. Binds to benzodiazepine receptor at GABA-A ligand-gated chrolide channel complex => enhances inhibitory effect of GABA => inhibits neuronal activity in amygdala-centred fear circuits to provide therapeutic benefits 6. - Metabolised by CYP450 3A4 --Inhibitors of CYP450 3A (fluvoxamine, fluoxetine, grape juice) may decrease alprazolam clearance => raise plasma levels --Inducers of CYP450 3A (carbamazapine) may increase alprazolam clearance => lower plasma levels - Inactive metabolites - Elimination half-life is 12-15 hrs |
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Alprazolam 7. Adverse effects? 8. Pearls? |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion 8. - Rapid onset of action - Less sedation than some other benzos - Euphoria may lead to abuse |
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Amisulpride 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. Solian 2. Atypical antipsychotic (benzamide) 3. Schizophrenia 4. 400mg - 800mg daily in 2 doses |
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Amisulpride 5. MOA? 6. Pharmacokinetics? |
5. - Theoretically blocks pre-synaptic dopamine 2 receptors at low doses and post-synaptic dopamine 2 receptors at high doses - Unlike other atypical antipsychotics, does not have potent actions at serotonin receptors 6. - Elimination half-life approx 12 hours - Excreted largely unchanged - Can decrease effects of levodopa - Can increase effects of antihypertensives |
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Amisulpride 7. Adverse effects? 8. Pearls? |
7. - Extra-pyramidal symptoms - Galactorrhea, amenorrhea - Increased risk of DM and high cholesterol - Insomnia, sedation, agitation, anxiety - Weight gain, constipation 8. - Efficacy has been particularly well demonstrated in patients with predominantly negative symptoms |
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Amitriptyline 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. Elavil 2. TCA (serotonin and norepinephrine reuptake inhibitor) 3. - Depression - Neuropathic pain/ chronic pain - Fibromyalgia - Insomnia 4. 50 to 150mg daily |
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Amitriptyline 5. MOA? 6. Pharmacokinetics? |
5. - Blocks serotonin reuptake pump => increases serotonergic neurotransmission - Blocks norepinephrine reuptake pump => increases noradrenergic neurotransmission 6. - Substrate of CYP450 2D6 and 1A2 - Plasma half-life 10 to 28 hours - Tramadol increases risk of seizures in patients taking TCAs - Use of TCAs with anticholinergic drugs may result in paralytic ileus or hyperthermia - Fluoxetine/paroxetine/duloxetine and other CYP450 2D6 inhibitors can decrease conversion of amitriptyline => increase amitriptyline concentrations |
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Amitriptyline 7. Adverse effects? 8. Pearls? |
7. - Anticholinergic effects: sedation, dry mouth, constipation, blurred vision - Antihistamine effects: weight gain, sedation - Alpha adrenergic receptor blockade: dizziness, hypotension, sedation - Sexual dysfunction, unusual taste in mouth, rash 8. - Advantageous for insomnia 8. |
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Amoxapine 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. Asendin 2. TCA 3. - Neurotic or reactive depressive disorder - Endogenous and psychotic depression - Depression accompanied by anxiety or agitation 4. 200 to 300mg daily |
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Amoxapine 5. MOA? 6. Pharmacokinetics? |
5. - Blocks norepinephrine reuptake pump => increases noradrenergic neurotransmission - Boosts neurotransmitter serotonin at high doses - Blocks dopamine 2 receptors 6. - Substrate for CYP450 2D6 - Half life of active metabolites is approx 24 hrs - Tramadol increases risk of seizures in patients taking TCAs - Use of TCAs with anticholinergic drugs may result in paralytic ileus or hyperthermia - Fluoxetine/paroxetine/duloxetine and other CYP450 2D6 inhibitors can decrease conversion of amitriptyline => increase amitriptyline concentrations |
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Amoxapine 7. Adverse effects? 8. Pearls? |
7. - Anticholinergic effects: sedation, dry mouth, constipation,blurred vision - Antihistamine effects: weight gain, sedation - Alpha adrenergic receptor blockade:dizziness, hypotension, sedation - Sexual dysfunction, unusual taste in mouth,rash - Can cause extrapyramidal symptoms due to D2 blockade 8. - Despite not being 1st line, continues to be useful for severe or treatment-resistant depression |
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Amphetamine 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. - Dexedrine (d-amphetamine) - Adderall (d, l-amphetamine) 2. Stimulant 3. - ADHD (ages 3 to 16) - Narcolepsy 4. 5 to 40mg daily (divided doses for tablets) |
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Amphetamine 5. MOA? 6. Pharmacokinetics? |
5. -Increases norepinephrine and especially dopamine actions by blocking their reuptake and facilitating their release 6. - Half life approx 10 to 12 hours - Haloperidol, chlorpromazine, and lithium may inhibit stimulatory effects of amphetamine - Amphetamines inhibit the antipsychotic and mood-stabilising effects of atypical antipsychotics |
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Amphetamine 7. Adverse effects? 8. Pearls? |
7. - Norepinephrine peripherally causes autonomic side effects: tremor, tachycardia, hypertension, cardiac arrhythmias - Norepinephrine and dopamine in CNS: insomnia, agitation, psychosis substance abuse - Anorexia, nausea, dry mouth, constipation, weight loss 8. - May be useful for treatment of depressive symptoms in medically ill elderly patients |
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Aripiprazole 1. Brand? 2. Class? 3. Indications? 4. Dose? |
1. Abilify 2. Atypical antipsychotic (dopamine partial agonist) 3. - Schizophrenia - Bipolar maintenance - Depression (adjunct) 4. 15 to 30mg daily |
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Aripiprazole 5. MOA? 6. Pharmacokinetics? |
5. - Partial agonism at dopamine 2 receptors => reduces D output when D concentrations are high and increases D output when D concentrations are low - Actions at D3 receptors could contribute to efficacy - Also partial agonism of 5HT1A receptors 6. - Metabolised primarily by CYP450 2D6 and 3A4 enzymes - Mean elimination half life is 75 hrs |
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Aripiprazole 7. Adverse effects? 8. Pearls? |
7. - Blocks alpha 1 adrenergic receptors: dizziness, sedation, hypotension - D2 receptor: extrapyramidal effects, mostly akathisia (occasionally) - Weight gain reported in a few patients, especially those with low BMIs, but not expected (less frequent and less severe than for most other antipsychotics) - Insomnia, constipation 8. - Favorable tolerability profile - One of only two antipsychotics with an indication in children |
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Atomoxetine 1. Brand 2. Class 3. Indications 4. Dose |
1. Strattera 2. SNRI 3. - ADHD in children > 6 yrs old and adults - Treatment-resistant depression 4. - 0.5 to 1.2mg/kg daily for children up to 70kg - 40 to 100mg daily in adults |
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Atomoxetine 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine reuptake transporters => increases noradrenergic neurotransmission + may increase dopamine in prefrontal cortex 6. - Metabolised by CYP450 2D6 - Half life approx 5 hours |
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Atomoxetine 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue - Decreased appetite - Increased heart rate, increased BP - Insomnia, dizziness, anxiety, irritability - Dry mouth, constipation, nausea, abdominal pain - Urinary retention - Sexual dysfunction 8. - Unlike other agents approved for ADHD, atomoxetine does not have abuse potential - Despite being an SNRI, atomoxetine enhances both dopamine and norepinephrine in frontal cortex => accounts for therapeutic actions on attention and concentration |
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Bupropion 1. Brand 2. Class 3. Indications 4. Dose |
1. Wellbutrin, Zyban, Aplenzin 2. Nurepinephrine dopamine reuptake inhibitor (NDRI) 3. - Major depressive disorder - Seasonal affective disorder - Nicotine addiction 4. 225 to 450mg in 3 divided doses (max single dose of 150mg) |
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Bupropion 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine and dopamine transporters => increases norepinephrine and dopamine neurotransmission - Increases dopamine neurotransmission in the frontal cortex 6. - Inhibits CYP450 2D6 - Metabolite half life of 20 to 27 hrs |
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Bupropion 7. Adverse effects 8. Pearls |
7. - Norepinephrine effects: dry mouth, constipation, nausea, anorexia, sweating, hypertension - Insomnia, headache, agitation, anxiety, rash - Seizures, hypomania 8. - May be effective if SSRIs have failed or for SSRI "poop-out" - May improve cognitive slowing/pseudo-dementia - Reduces hypersomnia and fatigue |
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Buspirone 1. Brand 2. Class 3. Indication 4. Dose |
1. BuSpar 2. Anxiolytic (azapirone; serotonin 1A partial agonist) 3. - Management of anxiety disorders - Short term treatment of symptoms of anxiety 4. 20 to 30mg/daily |
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Buspirone 5. MOA 6. Pharmacokinetics |
5. - Binds to serotonin 1A receptors => partial agonist actions postsynaptically diminish serotonergic activity and contribute to anxiolytic actions 6. - Metabolised primarily by CYP 450 3A4 - Elimination half life approx 2-3 hrs |
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Buspirone 7. Adverse effects 8. Pearls |
7. - Serotonin partial agonist: dizziness, headache, nervousness, sedation, nausea, restlessness 8. - Advantages: safety profile, lack of dependence/withdrawal - Disadvantages: takes 4 weeks for results, whereas benzodiazepines have immediate effect |
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Carbamazepine 1. Brand 2. Class 3. Indications 4. Dose |
1. Tegretol, Carbatrol, Equetro 2. Anticonvulsant (voltage-sensitive sodium channel antagonist) 3. - Seizures - Pain associated with true trigeminal neuralgia - Acute mania/ mixed mania 4. 400 to 1200mg daily |
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Carbamazepine 5. MOA 6. Pharmacokinetics |
5. - Acts as a use-dependent blocker of voltage-sensitive sodium channels - Inhibits release of glumamate 6. - Metabolised by the liver; primarily by CYP450 3A4 - Renally excreted - Initial half life of 26 t to 65 hrs; half life of 12 to 17 hrs after repeated dose - Not only a substrate of CYP450 3A4 but also an inducer => thus carbamazepine induces its own metabolism, often requiring an upward dosage adjustment |
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Carbamazepine 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, confusion, unsteadiness, headache - Nausea, vomiting, diarrhea - Blurred vision, benign leukopenia - Rare aplastic anaemia, stevens johnson syndrome, SIADH 8. - Advantages: treatment-resistant bipolar and psychotic disorders - Disadvantages: patients who do not wish to or cannot comply with blood testing and close monitoring |
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Chlordiazepoxide 1. Brand 2. Class 3. Indications 4. Dose |
1. Limbitrol, Librium, Librax 2. Benzodiazepine 3. - Anxiety disorders - Symptoms of anxiety - Withdrawal symptoms of acute alcoholism 4. 15 to 100mg daily in 3-4 doses |
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Chlordiazepoxide 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half life is 24 to 48 hours |
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Chlordiazepoxide 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, nervousness, hyperexcitability 8. - Available in injectable form - Rapid onset of action but habit-forming |
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Chlorpromazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Thorazine 2. Typical antipsychotic (phenothiazine; antiemetic) 3. - Schizophrenia - Nausea, vomiting - Combativeness and/or explosive hyperexcitable behaviour in children 4. 200 to 800mg daily |
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Chlorpromazine 5. MOA 6. Pharmacokinetics |
5. - Blocks dopamine 2 receptors => reduces positive symptoms of psychosis and improving other behaviours - Combination of D2, histamine H1, cholinergic MI blockade in the vomiting centre => reduces vomiting 6. - Half life approx 8 to 33 hrs |
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Chlorpromazine 7. Adverse effects 8. Pearls |
7. - D2 block: extrapyramidal symptoms, galactorrhea, amenorrhea, neuroleptic-induced deficit syndrome - Anticholinergic: sedation, blurred vision, constipation, dry mouth - Antihistaminic: sedation, weight gain 8. - One of the earliest typical antipsychotics - Risk of tardive dyskinesia and availability of alternative treatments makes in 2nd line treatment |
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Citalopram 1. Brand 2. Class 3. Indications 4. Dose |
1. Celexa 2. SSRI 3. - Depression - Anxiety disorders 4. 20 to 60mg daily |
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Citalopram 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin transporter => boosts neurotransmitter serotonin => increases serotonergic transmission - Also has mild antagonist actions at H1 histamine receptors 6. - Half life of 23 to 45 hrs - Weak inhibitor of CYP450 2D6 |
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Citalopram 7. Adverse effects 8. Pearls |
7. - Increase serotonin: insomnia, diarrhea - Diminished dopamine d.t increased serotonin: emotional flattening, cognitive slowing, apathy - Sexual dysfunction - GI: decreased appetite, nausea, diarrhea, constipation, dry mouth - CNS: insomnia, sedation, agitation, tremors, headache, dizziness - SIADH 8. - May be more tolerable than some other antidepressants, especially in the elderly |
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Clomipramine 1. Brand 2. Class 3. Indications 4. Dose |
1. Anafranil 2. TCA 3. - OCD - Severe and treatment-resistant depression - Cataplexy syndrome 4. 100 to 200mg daily |
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Clomipramine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => boosts serotonergic and noradrenergic neurotransmission 6. - Substrate for CYP450 2D6 and 1A2 - Half life approx 17 to 28 hrs |
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Clomipramine 7. Adverse effects 8. Pearls |
7. - Anticholinergic: sedation, dry mouth, constipation, blurred vision, urinary retention - Antihistamine: weight gain, sedation - Block of alpha adrenergic 1 receptors: dizziness, hypotension - Unusual taste in mouth, sexual dysfunction, headache 8. - The only TCA with proven efficacy in OCD - One of the most favored TCA for treating treatment-resistant depression |
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Clonazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Klonopin 2. Benzodiazepine 3. - Panic disorder - Lennox-Gastaut syndrome - Seizures 4. 0.5 to 2mg daily |
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Clonazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half life approx 30 to 40 hrs - Long half life compared to other benzos |
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Clonazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, nervousness, hyperexcitability 8. - Rapid onset of action - Less sedation than other benzos - One of the most popular benzos for anxiety |
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Clonidine 1. Brand 2. Class 3. Indications 4. Dose |
1. Duraclon, Catapres 2. Antihypertensive (centrallyacting alpha 2 agonist hypotensive agent) 3. - Hypertension - ADHD - Tourette’s syndrome 4. 0.2 to 0.6mg/day in divided doses |
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Clonidine 5. MOA 6. Pharmacokinetics |
5. - Has central actions on either pre- orpostsynaptic alpha 2 receptors - Actions at imidazoline receptors maycause behavioural changes in numerous conditions 6. - Half life 12 to 16 hours - Metabolized by the liver - Excreted renally |
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Clonidine 7. Adverse effects 8. Pearls |
7. - Dry mouth, dizziness, constipation,sedation - Weakness, fatigue, impotence, loss oflibido, insomnia, headache 8. - Although not approved for ADHD, clonidinehas been shown to be effective treatment for this disorder in several publishedstudies - As Monotherapy for ADHD, may be inferiorto other options, including stimulants and desipramine |
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Clorazepate 1. Brand 2. Class 3. Indications 4. Dose |
1. Azene, Tranxene 2. Benzodiazepine 3. - Anxiety disorder - Symptoms of anxiety - Acute alcohol withdrawal 4. 15 to 60mg/day in divided doses |
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Clorazepate 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at theGABA-A ligand-gated chloride channel complex => boosts chloride conductancethrough GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half-life of 40 to 50 hrs |
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Clorazepate 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech,weakness - Forgetfulness, confusion,hyperexcitability, nervousness 8. - More commonly used than some otherbenzodiazepines for treating alcohol withdrawal |
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Clozapine 1. Brand 2. Class 3. Indications 4. Dose |
1. Clozaril, Leponex 2. Atypical antipsychotic(serotonin-dopamine antagonist)
3. - Treatment-resistant schizophrenia - Reduction in risk of recurrent suicidalbehaviour in patients with schizophrenia or schizoaffective disorder 4. 300 to 450mg/day |
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Clozapine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reducespositive symptoms- Blocks serotonin 2A receptors =>causes enhancement of dopamine release in certain brain regions => improvescognitive and affective symptoms - Specifically, interactions at 5HT2C and5HT1A receptors may contribute to efficacy for cognitive and affective symptoms 6. - Half-life 5 to 16 hrs - Metabolised by CYP450 enzymes (including1A2, 2D6, and 3A4) |
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Clozapine 7. Adverse effects 8. Pearls |
7. - Histamine 1 receptor: sedation, weightgain - Alpha 1 adrenergic receptor: dizziness,sedation, and hypotension - Muscarinic 1 receptor: dry mouth,constipation, sedation - Increased risk of diabetes and dyslipidaemia- Increased salivation, sweating - Agranulocytosis - Seizures, myocarditis, increased risk ofdeath and cardiovascular events in elderly patients 8. - Most efficacious but most dangerousantipsychotic - Reduces suicide in schizophrenia - Not a 1st line treatment inmost countries |
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Cyamemazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Tercian 2. Typical antipsychotic (phenothiazine) 3. - Schizophrenia- Anxiety associated with psychosis 4. 300 to 600mg/day |
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Cyamemazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors - Although classified as a typicalantipsychotic, cyamemazine is a potent serotonin 2A antagonist - Specifically, antagonist actions at 5HT2Creceptors may contribute to notable anxiolytic effects in many patients 6. - Half life approx. 10 hrs |
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Cyamemazine 7. Adverse effects 8. Pearls |
7. - Extrapyramidal symptoms- Neuroleptic-induced deficit syndrome - Galactorrhea, amenorrhea - Hypotension, tachycardia- Dry mouth, constipation, visiondisturbance, urinary retention - Sedation, weight gain, sexual dysfunction 8. - Appears to have unique anxiolytic actionsat low doses without rebound anxiety following discontinuation |
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Desipramine 1. Brand 2. Class 3. Indications 4. Dose |
1. Norpramin 2. TCA 3. - Depression - Anxiety - Insomnia Neuropathic pain/chronic pain 4. 100 to 200mg/day |
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Desipramine 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporters => increases noradrenergic neurotransmission - Dopamine in frontal cortex is also increased due to blockade of norepinephrine reuptake pump - At high doses may also boost neurotransmitter serotonin 6. - Substrate for CYP450 2D6 and 1A2 - Half life approx 24 hrs |
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Desipramine 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinary retention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusual taste in mouth - Fatigue, weakness, dizziness, sedation, headache, anxiety - Sexual dysfunction, sweating 8. - Desipramine is one of the few TCAs where monitoring of plasma drug levels has been well studied - Fewer anticholinergic side effects than some other TCAs |
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Desvenlafaxine 1. Brand 2. Class 3. Indications 4. Dose |
1. Pristiq 2. SNRI (dual serotonin and norepinephrine reuptake inhibitor) 3. - Major depressive disorder - Vasomotor symptoms - Fibromyalgia - GAD, PTSD, social phobia 4. 50mg daily |
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Desvenlafaxine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => increases serotonergic and noradrenergic neurotransmission - Dopamine is also increased in frontal cortex secondary to blockade of norepinephrine reuptake 6. - Active metabolite of venlafaxine - Half life of 9 to 13 hours - Minimally metabolised by CYP450 3A4 |
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Desvenlafaxine 7. Adverse effects 8. Pearls |
7. - Insomnia, sedation, anxiety, dizziness - Nausea, vomiting, constipation, decreased appetite - Sexual dysfunction, sweating, SIADH, hyponatraemia 8. - Because desvenlafaxine is only minimally metabolised by CYP450 3A4 and is not metabolised at all by CYP450 2D6, as venlafaxine is, it should have a more consistent plasma level than venlafaxine |
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Diazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Valium, Diastat 2. Benzodiazepine 3. - Anxiety disorder - Symptoms of anxiety (short-term) - Delirium tremens and acute alcohol withdrawal 4. 4 to 40mg/day in divided doses |
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Diazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half-life of 20 to 50 hours |
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Diazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression, dizziness, weakness, ataxia, slurred speech - Forgetfulness, confusion - Hyperexcitability, nervousness 8. - Multiple dosage formulations (oral tablet, oral liquid, rectal gel, injectable) allow for more flexibility of administration compared to most other benzodiazepines |
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Donepezil 1. Brand 2. Class 3. Indications 4. Dose |
1. Aricept, Memac 2. Cholinesterase inhibitor (selective acetylcholinesterase inhibitor) 3. - Alzheimer disease 4. 5 to 10mg nocte |
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Donepezil 5. MOA 6. Pharmacokinetics |
5. - Reversibly but non-competitively inhibits centrally active acetylcholinesterase (AChE) => makes more acetylcholine available => compensates in part for degenerating cholinergic neurons in neocortex that regulate memory 6. - Metabolised by CYP450 2D6 and CYP450 3A4 - Elimination half-life approx 70 hrs |
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Donepezil 7. Adverse effects 8. Pearls |
7. - Peripheral inhibition of AChE: GI effects, such as nausea, vomiting, appetite loss, weight loss - Central inhibition of AChE: nausea, vomiting, weight loss, sleep disturbances 8. - One of only two drugs indicated for moderate to severe Alzheimer disease |
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Dothiepin 1. Brand 2. Class 3. Indications 4. Dose |
1. Prothiaden 2. TCA 3. - Major depressive disorder - Anxiety - Insomnia - Neuropathic pain/chronic pain 4. 75 to 150mg/day |
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Dothiepin 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine and serotonin transporters => increases noradrenergic andserotonergic neurotransmission - Dopamine in frontal cortex is also increased due to blockade of norepinephrine reuptake pump 6. - Substrate for CYP450 2D6 - Half-life approx 14 to 40 hours |
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Dothiepin 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinary retention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusual taste in mouth - Fatigue, weakness, dizziness, sedation, headache, anxiety - Sexual dysfunction, sweating 8. - Close structural similarity to Amitriptyline |
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Doxepin 1. Brand 2. Class 3. Indications 4. Dose |
1. Sinequan 2. TCA 3. - Psychoneurotic patient with depression and/or anxiety - Depression and/or anxiety associated with alcoholism 4. 75 to 150mg daily |
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Doxepin 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine and serotonin transporters => increases noradrenergic andserotonergic neurotransmission - Dopamine in frontal cortex is also increased due to blockade of norepinephrine reuptake pump 6. - Substrate for CYP450 2D6 - Half-life approx. 8 to 24 hrs |
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Doxepin 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinary retention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusual taste in mouth - Fatigue, weakness, dizziness, sedation, headache, anxiety - Sexual dysfunction, sweating 8. - Only TCA available in topical formulation - Topical administration may reduce symptoms in patients with various neurodermatitis syndromes, especially itching |
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Duloxetine 1. Brand 2. Class 3. Indications 4. Dose |
1. Cymbalta 2. SNRI 3. - Major depressive disorder - Diabetic peripheral neuropathic pain - Fibromyalgia - GAD 4. 40 to 60mg daily |
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Duloxetine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => increases serotonergic and noradrenergic neurotransmission - Increases dopamine in the frontal cortex by blocking norepinephrine transporters 6. - Elimination half-life approx. 12 hours - Metabolised mainly by CYP450 2D6 and CYP450 1A2 - Inhibitor of CYP450 2D6 and CYP450 1A2 -Absorption may be delayed by up to 3 hrs and clearance may be increased by by 33% after an nocte dose as compared to a mane dose |
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Duloxetine 7. Adverse effects 8. Pearls |
7. - Nausea, vomiting, decreased appetite, dry mouth, constipation - Insomnia, sedation, dizziness - Sexual dysfunction, sweating, urinary retention 8. - Duloxetine has well-documented efficacy for the painful physical symptoms of depression |
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Escitalopram 1. Brand 2. Class 3. Indications 4. Dose |
1. Lexapro 2. SSRI 3. - Major depressive disorder - GAD - Panic disorder, OCD, PTSD, social phobia 4. 10 to 20mg daily |
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Escitalopram 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin transporters => boosts neurotransmitter serotonin => increases serotonergic neurotransmission 6. - Mean terminal half-life of 27 to 32 hours - Steady state plasma concentrations achieved within 1 week - No significant actions on CYP450 enzymes |
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Escitalopram 7. Adverse effects 8. Pearls |
7. - Sexual dysfunction (delayed ejaculation, erectile dysfunction, decreased sexual desire) - GI effects (decreased appetite, nausea, diarrhea, constipation, dry mouth) - Insomnia, sedation, agitation, tremors, headache, dizziness 8. - May be among the best-tolerated antidepressant - Escitalopram is commonly used with augmenting agents, as it is the SSRI with the least interaction at either CYP450 2D6 or 3A4, therefore causing fewer pharmacokinetically mediated drug interactions with augmenting agents than other SSRIs |
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Estazolam 1. Brand 2. Class 3. Indications 4. Dose |
1. ProSom 2. Benzodiazepine 3. - Insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings 4. 1 to 2mg nocte |
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Estazolam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Half-life of 10 to 24 hours - Inactive metabolites |
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Estazolam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, hyperexcitability, nervousness 8. - Useful for transient insomnia - Best short-term use is for less than 10 consecutive days, and for less than half of the nights in a month |
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Eszopiclone 1. Brand 2. Class 3. Indications 4. Dose |
1. Lunesta 2. - Non-benzodiazepine hypnotic - Alpha-1 isoform selective agonist of GABA-A/benzodiazepine receptor 3. - Insomnia 4. 2 to 3mg nocte |
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Eszopiclone 5. MOA 6. Pharmacokinetics |
5. - Binds to alpha-1 isoform, a subtype of the benzodiazepine receptor => boosts chloride conductance through GABA-regulated channels => enhances GABA inhibitory actions 6. - Metabolised by CYP450 3A4 and 2E1 - Terminal elimination half-life approx. 6 hrs |
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Eszopiclone 7. Adverse effects 8. Pearls |
7. - Unpleasant taste - Sedation, dizziness, dose-dependent amnesia - Nervousness, dry mouth, headache 8. - Chronic studies of eszopiclone suggest lack of notable tolerance or dependence developing over time |
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Flumazenil 1. Brand 2. Class 3. Indications 4. Dose |
1. Romazicon, Anexate, Lanexat 2. Benzodiazepine receptor antagonist 3. - Reversal of sedative effects of benzodiazepines - Management of benzodiazepine overdose 4. 0.4 to 1mg usually causes complete antagonism of therapeutic doses of benzodia |
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Flumazenil 5. MOA 6. Pharmacokinetics |
5. - Blocks benzodiazepine receptors at GABA-A ligand-gated chloride channel complex => prevents benzodiazepine from binding there 6. - Terminal half-life of 41 to 79 minutes - Onset of action is 1 to 2 minutes; peak action in 6 to 10 minutes |
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Flumazenil 7. Adverse effects 8. Pearls |
7. - May precipitate benzodiazepine withdrawal in patients dependent upon or tolerant to benzodiazepines - Dizziness, injection site pain, sweating, headache, blurred vision - Seizures, cardiac dysrythmia 8. - Can precipitate benzodiazepine withdrawal seizures - Can wear off before the benzodiazepine is reversing - Can precipitate anxiety or panic in conscious patients with anxiety disorder |
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Flunitrazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Rohypnol 2. Benzodiazepine 3. - Short-term treatment of insomnia (severe, disabling) 4. 0.5 to 1mg nocte |
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Flunitrazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half-life of 16 to 35 hours - Half-life of active metabolite is 23 to 33 hours |
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Flunitrazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, hyperexcitability, nervousness 8. - Paradoxical reactions and psychiatric symptoms may be quite severe with flunitrazepam and may be more frequent than with other benzodiazepines - Has earned a reputation as a "date rape drug"; in combination with alcohol is claimed to reduce inhibition, judgement, and physical ability to resist sexual advances - Until 1999 was colourless, but a compound was added so that now the drug turns blue when added to liquid |
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Fluoxetine 1. Brand 2. Class 3. Indications 4. Dose |
1. Prozac, Sarafem 2. SSRI 3. - Major depressive disorder - OCD - Bulimia nervosa, Panic disorder, PTSD, social phobia 4. 20 to 80mg daily |
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Fluoxetine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin transporter => boosts neurotransmitter serotonin => increases serotonergic neurotransmission - Also has antagonist properties at 5HT2C receptors, which could increase norepinephrine and dopamine neurotransmission 6. - Active metabolite (norfluoxetine) has 2 week half-life - Parent drug has 2-3 day half-life - Inhibits CYP450 2D6 and CYP450 3A4 |
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Fluoxetine 7. Adverse effects 8. Pearls |
7. - Sexual dysfunction (delayed ejaculation, erectile dysfunction, decreased sexual desire) - GI symptoms (decreased appetite, nausea, diarrhea, constipation, dry mouth) - Insomnia, sedation, agitation, tremors, headache, dizziness - Increasing serotonin can cause diminished dopamine release and might contribute to emotional flattening, cognitive slowing, and apathy in some patients - Most side effects are immediate but often go away with time 8. - May be a 1st line choice for atypical depression (eg. hypersomnia, hyperphagia, low energy, mood reactivity) - Actions at 5HT2C receptors may explain its activating properties - Evidence of efficacy in children |
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Flupenthixol 1. Brand 2. Class 3. Indications 4. Dose |
1. Depixol 2. Typical antipsychotic (thioxanthene) 3. - Schizophrenia - Depression (low dose) - Bipolar disorder 4. - Oral: 3 to 6mg/day in divided doses - IM: 40 to 120mg every 1 to 4 weeks |
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Flupenthixol 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reducing positive symptoms of psychosis 6. - Oral: maximum plasma concentrations within 3 to 8 hours - IM: rate-limiting half-life approx. 8 days with single dose, approx. 17 days within multiple doses |
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Flupenthixol 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome - Extra-pyramidal symptoms - Insomnia, restlessness, agitation, sedation - Galactorrhea, amenorrhea - Weight gain, tachycardia, hypomania, rarely causes eosinophilia 8. - Less sedation and orthostatic hypotension but more extra-pyramidal symptoms than some other typical antipsychotics - Long-term poly-pharmacy with a combination of a typical antipsychotic and atypical antipsychotic may combine their side effects without clearly augmenting their side effects |
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Fluphenazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Prolixin 2. Typical antipsychotic (phenothiazine) 3. - Psychotic disorders - Bipolar disorder 4. - Oral: 1 to 20mg/day maintenance - IM: generally 1/3 or 1/2 the oral dose |
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Fluphenazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Mean half-life of oral formulation is approx. 15 hours - Mean half-life of IM formulation approx. 6 to 9 days |
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Fluphenazine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome - Extra-pyramidal symptoms - Galactorrhea, amenorrhea - Dizziness, sedation, dry mouth, constipation, urinary retention, blurred vision, decreased sweating, sexual dysfunction - Hypotension, tachycardia, syncope, weight gain 8. - Potential advantages is IM formulation for emergency use - Not shown to be effective for behavioural problems in mental retardation |
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Flurazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Dalmane 2. Benzodiazepine 3. - Insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakening - Recurring insomnia or poor sleeping habits 4. 15 to 30mg nocte for 7 to 10 days |
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Flurazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half-life approx. 24 to 100 hrs - Active metabolites |
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Flurazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, hyperexcitability, nervousness 8. - Flurazepam has a longer half-life than some other sedative hypnotics, so it may be less likely to cause rebound insomnia on discontinuation - Long-term accumulation of flurazepam and its active metabolites may cause insidious confusion or falls, especially in the elderly |
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Fluvoxamine 1. Brand 2. Class 3. Indications 4. Dose |
1. Luvox 2. SSRI 3. - OCD - Social anxiety disorder - Depression - Panic disorder, GAD, PTSD 4. 100 to 300mg daily |
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Fluvoxamine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin transporter => boosts neurotransmitter serotonin => increases serotonergic neurotransmission - Has antagonist properties at sigma 1 receptors 6. - Parent drug has 9 to 28 hour half-life - Inhibits CYP450 3A4 and 1A2 and 2C9 and 2C19 |
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Fluvoxamine 7. Adverse effects 8. Pearls |
7. - Sexual dysfunction (delayed ejaculation, erectile dysfunction, decreased sexual desire) - GI symptoms (decreased appetite, nausea, diarrhea, constipation, dry mouth) - Insomnia but also has sedation, agitation, tremors, headache, dizziness 8. - Often a preferred treatment of anxious depression as well as major depressive disorder comorbid with anxiety disorders |
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Gabapentin 1. Brand 2. Class 3. Indications 4. Dose |
1. Neurontin 2. - Anticonvulsant - Alpha 2 delta ligand at voltage-sensitive calcium channel 3. - Partial seizures - Postherpetic neuralgia (shingles) - Neuropathic pain/chronic pain - Anxiety (adjunctive) 4. 900 to 1800mg/day in 3 divided doses |
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Gabapentin 5. MOA 6. Pharmacokinetics |
5. - Binds to the alpha 2 delta subunit of voltage-sensitive calcium channels => this closes N and P/Q presynaptic calcium channels => diminishes excessive neuronal activity and neurotransmitter activity - No known direct actions on GABA or its receptors 6. - Gabapentin is not metabolised but excreted intact renally - Not protein bound - Elimination half-life approx. 5 to 7 hours |
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Gabapentin 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, ataxia, fatigue, nystagmus, tremor - Vomiting, dyspepsia, diarrhea, dry mouth, constipation, weight gain - Blurred vision - Peripheral edema 8. - Gabapentin is generally well tolerated, with only mild adverse effects - Most use is off label; off-label use for 1st line treatment of neuropathic pain may be justified |
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Galantamine 1. Brand 2. Class 3. Indications 4. Dose |
1. Razadyne 2. Cholinesterase inhibitor (acetylcholinesterase inhibitor 3. - Alzheimer disease (mild to moderate) 4. |
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Galantamine 5. MOA 6. Pharmacokinetics |
5. - Reversibly and competitively inhibits centrally-active acetylcholinesterase (AChE) => makes more acetylcholine available => increased availability of acetylcholine compensates in part for degenerating cholinergic neurons in neocortex that regulate memory - Modulates nicotinic receptors, which enhances actions of acetylcholine 6. - Terminal elimination half-life approx. 7 hours - Metabolized by CYP450 2D6 and 3A4 |
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Galantamine 7. Adverse effects 8. Pearls |
7. - Nausea, diarrhea, vomiting, appetite loss, increased gastric acid secretion, weight loss - Headache, dizziness - Fatigue, depression 8. - Treats behavioural and psychological symptoms of Alzheimer dementia as well as cognitive symptoms (i.e. especially apathy, disinhibition, delusions, anxiety, cooperation, pacing) |
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Guanfacine 1. Brand 2. Class 3. Indications 4. Dose |
1. Intuniv, Tenex 2. - Centrally acting alpha 2A agonist - Antihypertensive 3. - Hypertension - ADHD - ODD 4. 1 to 2mg/day |
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Guanfacine 5. MOA 6. Pharmacokinetics |
5. - For hypertension, stimulates alpha 2 adrenergic receptors in the brain stem => reduces sympathetic outflow from the CNS => decreases peripheral resistance/renal vascular resistance/heart rate/BP - For ADHD, has central actions on postsynaptic alpha 2A receptors in the prefrontal cortex 6. - Elimination half-life approx. 17 hours |
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Guanfacine 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, dry mouth, constipation - Fatigue, weakness 8. - No known abuse potential - Less sedation than clonidine |
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Haloperidol 1. Brand 2. Class 3. Indications 4. Dose |
1. Haldol 2. Typical antipsychotic (butyrophenone) 3. - Psychotic disorders - Tics and vocal utterances in Tourette's syndrome - 2nd line treatment for severe behaviour problems in children of combative, explosive behaviour 4. - 1 to 40mg/day orally - Immediate release injection 2 to 5mg each dose - Decanoate injection is 10 to 20 times the previous dose of oral Haloperidol |
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Haloperidol 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis and possibly combative, explosive behaviour - Blocks D2 receptors in the nigrostriatal pathway => improves tics and other symptoms of Tourette's syndrome 6. - Decanoate half-life approx. 3 weeks - Oral half-life approx. 12 to 38 hours |
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Haloperidol 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome - Extra-pyramidal symptoms - Galactorrhea, amenorrhea - Dizziness, sedation, dry mouth, constipation, urinary retention, blurred vision - Hypotension, tachycardia, hypertension - Weight gain 8. - Prior to introduction of atypical antipyschotics, Haloperidol was one of the preferred antipsychotics |
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Hydroxyzine 1. Brand 2. Class 3. Indications 4. Dose |
1. Atarax, Marax, Vistaril 2. Anti-histamine (anxiolytic, hypnotic, antiemetic) 3. - Anxiety and tension associated with psychoneurosis - Pruritis due to allergic conditions - Sedation following general anaesthesia 4. - Anxiety: 50 to 100mg QID |
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Hydroxyzine 5. MOA 6. Pharmacokinetics |
5. - Blocks histamine 1 receptors 6. - Rapidly absorbed from GI tract - Mean elimination half-life approx. 20 hours |
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Hydroxyzine 7. Adverse effects 8. Pearls |
7. - Blocking histamine 1 receptors can cause sedation - Dry mouth, tremor 8. - No abuse liability, dependence, or withdrawal - A preferred anxiolytic for patients with dermatitis or skin symptoms such as pruritis |
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Imipramine 1. Brand 2. Class 3. Indications 4. Dose |
1. Tofranil 2. TCA 3. - Depression - Enuresis - Anxiety - Neuropathic pain/chronic pain 4. 50 to 150mg/day |
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Imipramine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => boosts neurotransmitters serotonin and norepinephrine => increases serotonergic and noradrenergic neurotransmission - Imipramine can also increase dopamine neurotransmission in frontal cortex via blocking norepinephrine reuptake 6. - Substrate for CYP450 2D6 and 1A2 - Metabolised to an active metabolite, desipramine, a perdominantly norepinephrine reuptake inhibitor, by demethylation via CYP450 1A2 |
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Imipramine 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinary retention, increased appetite, dry mouth, nausea, diarrhea - Heartburn, unusual taste in mouth, weight gain - Fatigue, weakness, dizziness, sedation - Sexual dysfunction, sweating 8. - Probably the most preferred TCA for treating enuresis in children - Preference of some prescribers for imipramine over other TCAs for the treatment of enuresis is based more upon are and acedote than comparative clinical trials with other TCAs |
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Isocarboxazid 1. Brand 2. Class 3. Indications 4. Dose |
1. Marplan 2. MAOI (monoamine oxidase inhibitor) 3. - Depression - Treatment-resistant panic disorder or social phobia 4. 40 to 60mg daily |
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Isocarboxazid 5. MOA 6. Pharmacokinetics |
5. - Irreversibly blocks monoamine oxidase (MAO) from breaking down norepinephrine, serotonin, and dopamine => this boosts noradrenergic, serotonergic, and dopaminergic neurotransmission 6. - Clinical duration of action may be up to 21 days due to irreversible enzyme inhibition - Hypertensive crisis may result from combining MAOIs with sympathomimetic drugs (eg. amphetamines, cocaine etc.) |
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Isocarboxazid 7. Adverse effects 8. Pearls |
7. - Dizziness, sedation, headache, sleep disturbances, fatigue, weakness, tremor, movement problems, blurred vision, increased sweating - Constipation, dry mouth, nausea, change in appetite, weight gain - Sexual dysfunction - Orthostatic hypotension - Hypertensive crisis (when MAOIs are used with certain tyramine-containing foods) 8. - Food to generally avoid as they are usually high in tyramine content: dry sausage, pickled herring, liver, broad bean pods, cheese, yogurt, alcoholic beverages, chocolate, caffeine, meat, fish |
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Lamotrigine 1. Brand 2. Class 3. Indications 4. Dose |
1. Lamictal, Labileno, Lamictin 2. Anticonvulsant, mood stabilizer 3. - Maintenance of bipolar 1 - Partial seizures 4. 100 to 200mg/day for monotherapy of bipolar 1 |
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Lamotrigine 5. MOA 6. Pharmacokinetics |
5. - Acts as a use-dependent blocker of voltage-sensitive sodium channels => interacts with the open channel conformation of voltage-sensitive sodium channels => inhibits release of glutamate and asparate 6. - Valproate increases plasma concentrations and half-life of lamotrigine, requiring lower doses of lamotrigine - Metabolised in the liver through glucorunidation but through the CYP450 enzyme system - Inactive metabolite - Renally excreted - Elimination half-life in healthy volunteers approx. 33 hrs after a single dose of lamotrigine |
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Lamotrigine 7. Adverse effects 8. Pearls |
7. - Benign rash (10%) - Sedation, blurred or double vision, dizziness, ataxia, headache, tremor, insomnia, poor coordination, fatigue - Nausea, vomiting, dyspepsia, abdominal pain, constipation, rhinitis - Rare serious rash 8. - Seems to be more effective in treating depressive episodes than manic episodes in bipolar 1 - Seems to be effective in preventing both manic relapses as well as depressive relapses - May actually be one of the best tolerated mood stabilizers with little weight gain or sedation; low levels of use may be based upon exaggerated fears of skin rashes |
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Levetiracetam 1. Brand 2. Class 3. Indications 4. Dose |
1. Keppra 2. Anticonvulsant 3. - Adjunct therapy for partial seizures - Neuropathic pain/chronic pain - Mania 4. 1,000 to 3,000mg/day |
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Levetiracetam 5. MOA 6. Pharmacokinetics |
5. - Binds to synaptic vesicle protein SV2A, which is involved in synaptic vesicle exocytosis - Opposes the activity of negative modulators of GABA- and glycine-gated currents and partially inhibits N-type calcium currents in neuronal cells 6. - Elimination half-life approx. 6 to 8 hrs - Inactive metabolites - Not metabolised by CYP450 enzymes - Does not inhibit/induce CYP450 enzymes - Renally excreted |
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Levetiracetam 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, ataxia, asthenia - Hematologic abnormalities (decrease in RBCs and hemoglobin) 8. - Off-label use 2nd line and as an augmenting agent may be justified for bipolar disorder and neuropathic pain unresponsive to other treatments |
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Lisdexamfetamine 1. Brand 2. Class 3. Indications 4. Dose |
1. Vyvanse 2. Stimulant 3. - ADHD - Narcolepsy - Treatment-resistant depression 4. 30mg/day |
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Lisdexamfetamine 5. MOA 6. Pharmacokinetics |
5. - Is absorbed by the intestinal tract and converted to dextroamphetamine and l-lysine => increases norepinephrine and dopamine actions by blocking their reuptake and facilitating their release 6. - 1 hour to maximum concentration of lisdexamfetamine, 3.5 hours to maximum concentration of dextroamphetamine - Duration of clinical action is 10 to 12 hours |
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Lisdexamfetamine 7. Adverse effects 8. Pearls |
7. - Insomnia, headache, nervousness, irritability, overstimulation, tremor, dizziness - Anorexia, nausea, dry mouth, diarrhea, weight loss 8. - May have less propensity for abuse, intoxication, or dependence than other stimulants - Can reverse sexual dysfunction caused by psychiatric illness and by some other drugs such as SSRIs |
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Lithium 1. Brand 2. Class 3. Indications 4. Dose |
1. Eskalith, Lithobid 2. Mood stabiliser 3. - Manic episodes - Maintenance treatment for bipolar disorder - Major depressive disorder (adjunct) 4. - Acute: 1,800mg/day in divided doses - Maintenance: 900 to 1,200mg/day in divided doses |
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Lithium 5. MOA 6. Pharmacokinetics |
5. - Unknown and complex - May alter intracellular signalling through actions on second messenger systems 6. - Half life 18 to 30 hrs - NSAIDs, diuretics (especially thiazides), ACEi can increase plasma levels of lithium - can increase plasma levels of lithium |
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Lithium 7. Adverse effects 8. Pearls |
7. - Ataxia, dysarthria, delirium, tremor, memory problems - Polyuria, polydipsia - Diarrhea, nausea, weight gain, sedation - Acne, rash, alopecia - Euthyroid or hypothyroid goitre 8. - 1st line treatment option - Seems to be more effective treating manic episodes than depressive episodes - May decrease suicide and suicide attempts in bipolar disorder - Has a narrow therapeutic index; toxic side effects occur at doses close to its therapeutic effects |
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Lofepramine 1. Brand 2. Class 3. Indications 4. Dose |
1. Deprimyl, Gamanil 2. TCA 3. - Major depressive disorder - Anxiety - Insomnia - Neuropathic pain/chronic pain 4. |
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Lofepramine 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporter => boosts neurotransmitter norepinephrine => increases norepinephrine neurotransmission - Increases dopamine in frontal cortex due to blocking norepinephrine reuptake 6. - Substrate for CYP450 2D6 - Half-life of parent compound approx. 1.5 to 6 hours - Major metabolite is the antidepressant desipramine, with a half-life of approx. 24 hours |
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Lifepramine 7. Adverse effects 8. Pearls |
7. - Dry mouth, constipation, blurred vision - Sedation, weight gain, dizziness, hypotension - Cardiac arrhythmias, seizures, increased appetite, unusual taste in mouth 8. - Lofepramine is a short-acting prodrug of the TCA desipramine - Fewer anticholinergic side effects, particularly sedation, than some other TCAs |
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Loflazepate 1. Brand 2. Class 3. Indications 4. Dose |
1. Meilax 2. Benzodiazepine 3. - Anxiety, tension, depression, sleep disorders in patients with neurosis or pscyhosomatic disease 4. 1mg daily or BD |
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Loflazepate 5. MOA 6. Pharmacokinetics |
5. -Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - Elimination half-life approx. 122 hours (ultra-long half-life) |
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Loflazepate 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression - Dizziness, ataxia, slurred speech, weakness - Forgetfulness, confusion, hyperexcitability, nervousness 8. - Is the only "ultra-long half-life" benzodiazepine with a half-life much longer than 24 hours - Less interdose anxiety than other benzodiazepines - Long half-life could theoretically reduce abuse and withdrawal symptoms |
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Lorazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Ativan 2. Benzodiazepine 3. - Anxiety disorder - Status epilepticus - Insomnia - Alcohol withdrawal psychosis 4. 2 to 6mg/day in divided doses; largest dose at bedtime |
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Lorazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepinereceptors at the GABA-A ligand-gated chloride channel complex => boostschloride conductance through GABA-regulated channels - Inhibits neuronal activity inthe amygdala-centered fear circuits 6. - Elimination half-life 10 to 20 hours - No active metabolites |
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Lorazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression, - Dizziness,ataxia, slurred speech, weakness, - Forgetfulness, confusion, hyperexcitability,nervousness 8. - One of the most popular and useful benzos in inpatient setting; this is due in part to useful sedative properties and flexibility of administration - Rapid onset of action |
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Loxapine 1. Brand 2. Class 3. Indications 4. Dose |
1. Loxitane 2. Typical antipsychotic 3. - Schizophrenia - Other psychotic disorders 4. 60 to 100mg/day in divided doses |
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Loxapine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positivepsychotic symptoms - Loxapine is also a potent serotonin 2A antagonist; may be relevant at low doses but generally overwhelmed by high dosing 6. - Oral: half-life approx. 4 hours - IM: half-life approx. 12 hours - Multiple active metabolites with longer half-lives than parent drug - N-desmethyl loxapine is amoxapine, an antidepressant |
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Loxapine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome,extra-pyramidal symptoms - Galactorrhea, amenorrhea - Sedation, dry mouth,constipation, vision disturbance 8. - Causes less weight gain than other typical antipsychotics, and may even be associated with weight loss |
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Maprotiline 1. Brand 2. Class 3. Indications 4. Dose |
1. Ludiomil 2. TCA 3. - Depression - Anxiety - Insomnia - Neuropathic pain/chronic pain 4. 50 to 150mg/day |
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Maprotiline 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporter => boostsneurotransmitter norepinephrine => increases noradrenergic neurotransmission - Increase in dopamine neurotransmissionsecondary to norepinephrine reuptake inhibition 6. - Substrate for CYP450 2D6 - Mean half-life approx. 51 hours - Peak plasma concentration 8 to 24 hours |
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Maprotiline 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinaryretention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusualtaste in mouth - Weight gain, fatigue, weakness, dizziness, sedation, anxiety - Sexual dysfunction, Sweating, rash, itching 8. - May have somewhat increased risk of seizures compared to some other TCAs, especially at higher doses - May have a more rapid onset of action than some other TCAs |
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Memantine 1. Brand 2. Class 3. Indications 4. Dose |
1. Namenda 2. NMDA receptor antagonist; cognitive enhancer 3. - Alzheimer disease - Chronic pain 4. 10mg BD |
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Memantine 5. MOA 6. Pharmacokinetics |
5. - Is a low to moderate affinity noncompetitive (open-channel) NMDA receptor antagonist, which binds preferentially to the NMDA receptor-operated cation channels - Presumably interferes with the postulated persistent activation of NMDA receptors by excessive glutamate release in Alzheimer disease 6. - Little metabolism; mostly excreted unchanged in the urine - Terminal elimination half-life approx. 60 to 80 hours - Minimal inhibition of CYP450 enzymes |
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Memantine 7. Adverse effects 8. Pearls |
7. - Dizziness, headache, constipation 8. - One of only two drugs indicated for moderate to severe Alzheimer disease - Well-tolerated with a low incidence of adverse effects |
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Mesoridazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Serentil, Lidanil 2. Typical antipsychotic 3. - Schizophrenia 4. - Oral: 100 to 400mg/day - Injection: 25 to 200mg/day |
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Mesoridazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positivepsychotic symptoms 6. - Half-life approx. 2 to 9 hours |
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Mesoridazine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome,extra-pyramidal symptoms - Galactorrhea, amenorrhea - Sedation, dry mouth,constipation, vision disturbance - Pigmentary retinopathy at high doses 8. - Generally, the benefits of mesoridazine do not outweigh its risks for most patients - Because of its effects on the QTc interval, mesoridazine is not intended for use unless other options have failed |
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Methylphenidate 1. Brand 2. Class 3. Indications 4. Dose |
1. Focalin 2. Stimulant 3. - ADHD - Narcolepsy - Treatment-resistant depression 4. |
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Methylphenidate 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine and dopamine reuptake => increases norepinephrine and dopamine action 6. - Mean plasma elimination half-life approx. 2.2 hours - Does not inhibit CYP450 enzymes |
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Methylphenidate 7. Adverse effects 8. Pearls |
7. - Insomnia, headache, exacerbation of tics, nervousness, irritability, overstimulation - Tremor, dizziness, anorexia, nausea, abdominal pain, weight loss - Blurred vision, temporarily slow growth in children 8. - The active s enantiomer of methylphenidate may be more than twice as efficacious as racemic d,l-methylphenidate - Disadvantageous for patients with current or past substance abuse, bipolar disorder, or psychosis |
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Methylphenidate (D,L) 1. Brand 2. Class 3. Indications 4. Dose |
1. Concerta, Ritalin, Daytrana 2. Stimulant 3. - ADHD in children and adults - Narcolepsy - Treatment-resistant depression 4. - Up to 2mg/kg per day in children 6 years and older, with a max of 60mg/day - In adults usually 20-30mg/day but may use up to 40 - 60mg/day |
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Methylphenidate (D,L) 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine and dopamine reuptake => increases norepinephrine and dopamine action 6. - Average half-life in adults is 3.5 hours - Average half-life in children is 2.5 hours |
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Methylphenidate (D,L) 7. Adverse effects 8. Pearls |
7. - Insomnia, headache, exacerbation of tics, nervousness, irritability, overstimulation - Tremor, dizziness, anorexia, nausea, abdominal pain, weight loss - Blurred vision, temporarily slow growth in children 8. - Established long-term efficacy as a 1st line treatment for ADHD - A classical augmentation strategy for treatment-refractory depression |
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Midazolam 1. Brand 2. Class 3. Indications 4. Dose |
1. Versed 2. Benzodiazepine 3. - Sedation in pediatric patients - Sedation - Preoperative anxiolytic 4. - Adults: IV dose is 1 to 2.5mg - Children: liquid dose is 0.25-1mg/kg, max. 20mg |
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Midazolam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex => boosts chloride conductance through GABA-regulated channels => enhances the inhibitory effects of GABA 6. - IV onset of action is 3 to 5 minutes - IM onset of action is 15 minutes; peak 30 minutes - Elimination half-life 2 to 6 hours - Active metabolite |
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Midazolam 7. Adverse effects 8. Pearls |
7. - Oversedation, impaired recall, agitation, involuntary movements, headache, nausea, vomiting - Hiccups, hypotension 8. - Fast onset but can be oversedating |
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Milnacipran 1. Brand 2. Class 3. Indications 4. Dose |
1. Toledomin, Ixel, Savella 2. SNRI 3. - Fibromyalgia - Major depressive disorder - Neuropathic pain/chronic pain 4. 30 to 200mg/day in 2 doses |
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Milnacipran 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => boosts neurotransmitter serotonin and norepinephrine => increases serotonergic and noradrenergic neurotransmission - Increases dopamine neurotransmission via norepinephrine blockade - Weak noncompetitive NMDA-receptor antagonist, which may contribute to actions in chronic pain 6. - Half-life 8 hours - No active metabolite |
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Milnacipran 7. Adverse effects 8. Pearls |
7. - Headache, nervousness, insomnia, sedation - Nausea, diarrhea, decreased appetite - Sexual dysfunction - SIADH - Dry mouth, constipation, dysuria, urinary retention - Tachycardia, palpitations 8. - Has a greater potency for norepinephrine reuptake blockade than for serotonin reuptake blockade, but this is of unclear clinical significance |
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Mirtazapine 1. Brand 2. Class 3. Indications 4. Dose |
1. Remeron 2. - Alpha 2 antagonist - Noradrenaline and specific serotonergic agent 3. - Major depressive disorder - Panic disorder - GAD, PTSD 4. 15 to 45mg nocte |
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Mirtazapine 5. MOA 6. Pharmacokinetics |
5. - Blocks alpha 2 adrenergic presynaptic receptor + on serotonin neurons => boosts serotonin and norepinephrine neurotransmitters => increases serotonin and norepinephrine neurotransmission - Also blocks 5HT2A, 5HT2C, and 5HT3 serotonin receptors - Also blocks H1 histamine receptors 6. - Half-life is 20 to 40 hours |
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Mirtazapine 7. Adverse effects 8. Pearls |
7. - Dry mouth, constipation, increased appetite, weight gain - Sedation, dizziness, abnormal dreams, confusion - Change in urinary function - Hypotension 8. - Useful for patients particularly concerned with sexual dysfunction, as it only causes this infrequently - Does not affect the CYP450 system, and so may be preferable in patients requiring concomitant medications |
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Moclobemide 1. Brand 2. Class 3. Indications 4. Dose |
1. Aurorix, Arima, Manerix 2. Reversible inhibitor of monoamine oxidase A (RIMA) 3. - Depression - Social anxiety disorder 4. 300 to 600mg/day |
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Moclobemide 5. MOA 6. Pharmacokinetics |
5. - Reversibly blocks MAO-A from breaking down norepinephrine, dopamine, and serotonin => boosts noradrenergic, serotonergic, and dopaminergic neurotransmission - MAO-A inhibition predominates unless significant concentrations of monoamines build up (eg. due to dietary tyramine), in which case MAO-A inhibition is theoretically reversed 6. - Partially metabolised by CYP450 2C19 and 2D6 - Inactive metabolites - Elimination half-life approximately 1 to 4 hours - Clinical duration of action at least 24 hours |
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Moclobemide 7. Adverse effects 8. Pearls |
7. - Insomnia, dizziness, agitation, anxiety, restlessness - Dry mouth, diarrhea, constipation, nausea, vomiting - Galactorrhea - Rare hypotension - Hypertensive crisis (especially when MAOIs are used with certain tyramine-containing foods; however, reduced risk compared to irreversible MAOIs) 8. - Potential advantages for atypical depression and severe depression - May be a safer alternative to classical irreversible nonselective MAO-A and MAO-B inhibitors with less propensity for tyramine and drug interactions and hepatotoxicity |
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Modafinil 1. Brand 2. Class 3. Indications 4. Dose |
1. Provigil, Alertec, Modiodal 2. Wake-promoting drug 3. - Reducing excessive sleepiness in patients with narcolepsy - Reducing excessive sleepiness in patients with obstructive sleep apnea 4. 200mg mane |
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Modafinil 5. MOA 6. Pharmacokinetics |
5. - Unknown but clearly different from classical stimulants such as methylphenidate and amphetamine - Preseumably enhances activity in hypothalamic wakefulness center within the hypothalamic sleep-wake switch by an unknown mechanism 6. - Metabolised by the liver - Excreted renally - Elimination half-life of 10 hours - Inhibits CYP450 2C19 - Induces CYP450 3A4 |
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Modafinil 7. Adverse effects 8. Pearls |
7. - Headache, anxiety, nervousness, insomnia - Dry mouth, diarrhea, nausea, anorexia - Pharyngitis, rhinitis, infection, hypertension 8. - Only agent approved for sleepiness associated with OSA - Only agent approved for treating sleepiness associated with shift work sleep disorder |
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Molindone 1. Brand 2. Class 3. Indications 4. Dose |
1. Moban 2. Typical antipsychotic 3. - Schizophrenia - Other psychotic disorders 4. 40 to 100mg/day in divided doses |
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Molindone 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Half-life approx. 1.5 hours |
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Molindone 7. Adverse effects 8. Pearls |
7. - D2 block: extrapyramidal symptoms, galactorrhea, amenorrhea, neuroleptic-induced deficit syndrome - Anticholinergic: sedation, blurred vision, constipation, dry mouth - Antihistaminic: sedation, weight gain 8. - May cause less weight gain than some antipsychotics - Some patients benefit from molindone's sedative properties |
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Naltrexone 1. Brand 2. Class 3. Indications 4. Dose |
1. Revia, Vivitrol 2. Alcohol dependence treatment; muopioid receptor antagonist 3. - Alcohol dependence - Blockade of effects of exogenously administered opioids 4. - Oral: 50mg/day - Injection: 380mg monthly |
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Naltrexone 5. MOA 6. Pharmacokinetics |
5. - Blocks mu opioid receptors => prevents alcohol or exogenous opioids from binding there => prevents the pleasurable effects of alcohol or opioid consumption 6. - Elimination half-life of oral naltrexone is approx. 13 hours - Elimination half-life of naltrexone via injection is 5 to 10 days |
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Naltrexone 7. Adverse effects 8. Pearls |
7. - Nausea, vomiting, decreased appetite - Dizziness - Rarely eosinophilic pneumonia 8. - Advantageous in patients who are not ready to abstain from alcohol completely and for binge drinkers - Some patients complain of apathy or loss of pleasure with chronic treatment |
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Nefazodone 1. Brand 2. Class 3. Indications 4. Dose |
1. Dutonin 2. SARI (serotonin 2 antagonist/reuptake inhibitor) 3. - Depression - Relapse prevention in MDD - Panic disorder 4. 300 to 600mg/day |
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Nefazodone 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin 2A receptors potently - Blocks serotonin and norepinephrine transporters => increases serotonergic and noradrenergic neurotransmission 6. - Half-life of parent compound is 2 to 4 hours - Half-life of active metabolites up to 12 hours - Inhibits CYP450 3A4 |
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Nefazodone 7. Adverse effects 8. Pearls |
7. - Nausea, dry mouth, constipation, dyspepsia, increased appetite - Headache, dizziness, vision changes, sedation, insomnia, agitation, confusion, memory impairment - Risk of hepatotoxicity 8. - Risk of hepatotoxicity makes this agent a 2nd line choice and has led to its withdrawal in some markets |
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Nortriptyline 1. Brand 2. Class 3. Indications 4. Dose |
1. Pamelor 2. TCA 3. - Depression - Anxiety - Insomnia - Neuropathic pain/chronic pain 4. 75 to 150mg/day once daily or in up to 4 divided doses |
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Nortriptyline 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporter => boostsneurotransmitter norepinephrine => increases noradrenergic neurotransmission - Increase in dopamine neurotransmissionsecondary to norepinephrine reuptake inhibition - Substrate for CYP450 2D6 - Nortriptyline is the active metabolite of amityriptyline, formed by demethylation via CYP450 1A2 - Half-life approx. 36 hours |
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Nortriptyline 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinaryretention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusualtaste in mouth - Weight gain, fatigue, weakness, dizziness, sedation, anxiety - Sexual dysfunction, Sweating, rash, itching 8. - Nortriptyline is one of the few TCAs where monitoring of plasma drug levels has been well studied |
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Phenelzine 1. Brand 2. Class 3. Indications 4. Dose |
1. Nardil, Nardelzine 2. MAOI 3. - Depressed patients characterized as “atypical”,“nonendogenous”, or “neurotic” 4. 45 to 75mg/day |
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Phenelzine 5. MOA 6. Pharmacokinetics |
5. - Irreversibly blocks monamine oxidase frombreaking down norepinephrine, serotonin, and dopamine => boostsnoradrenergic, serotonergic, and dopaminergic neurotransmission 6. - Clinical duration of action may be up to 21 days due to irreversible enzyme inhibition |
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Phenelzine 7. Adverse effects 8. Pearls |
7. - Dizziness, sedation, headache, sleep disturbances, fatigue, weakness, tremor, movement problems, blurred vision, increased sweating - Constipation, dry mouth, nausea, change in appetite, weight gain - Sexual dysfunction - Hypertensive crisis (especially when MAOIs are used with certain tyramine-containing foods or prohibited drugs) 8. - MAOIs should not be neglected as therapeutic agents for the treatment-resistant |
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Pimozide 1. Brand 2. Class 3. Indications 4. Dose |
1. Orap 2. Typical antipsychotic, tic suppressant 3. - Suppression of motor and phonic tics in patients with Tourette syndrome who have failed to respond satisfactorily to standard treatment - Psychotic disorders in patients who have failed to respond satisfactorily to standard treatment 4. Less than 10mg/day |
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Pimozide 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors in the nigrostriatal dopamine pathway => reduces tics in Tourette's syndrome 6. - Metabolized by CYP450 3A and to a lesser extent by CYP450 1A2 - Mean elimination half-life approx. 55 hours |
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Pimozide 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome,extra-pyramidal symptoms - Galactorrhea, amenorrhea - Sedation, dry mouth,constipation, vision disturbance - Dose dependent QTc prolongation 8. - In the past it was a 1st line choice for Tourette's syndrome; however, it is now recognized that the benefits of pimozide generally do not outweigh its risks |
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Pipothiazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Piportil 2. Typical antipsychotic (phenothiazine) 3. - Maintenance of Schizophrenia - Bipolar disorder 4. IM: 50 to 100mg monthly |
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Pipothiazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positivepsychotic symptoms 6. - Onset of action of palmitic ester formulation is within 2 to 3 days - Duration of action of palmitic ester formulation is 3 to 6 weeks |
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Pipothiazine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome,extra-pyramidal symptoms - Galactorrhea, amenorrhea - Insomnia, excitement, restlessness, dry mouth,constipation, vision disturbance - Weight gain, hypotension, arrhythmia 8. - Only available in long-acting parenteral formulation |
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Pregabalin 1. Brand 2. Class 3. Indications 4. Dose |
1. Lyrica 2. Anticonvulsant 3. - Diabetic peripheral neuropathy - Postherpetic neuralgia - Fibromyalgia - Partial seizures - GAD, social phobia, panic disorder - Peripheral neuropathic pain 4. 150 to 600mg/day in 2-3 doses |
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Pregabalin 5. MOA 6. Pharmacokinetics |
5. - Binds to the alpha 2 delta subunit of voltage-sensitive calcium channels => this closes N and P/Q presynaptic calcium channels => diminishes excessive neuronal activity and neurotransmitter release - Although structurally related to GABA, no known direct actions on GABA or its receptors 6. - Pregabalin is not metabolized but excreted intact renally - Elimination half-life approx. 5 to 7 hours |
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Pregabalin 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness - Ataxia, fatigue, tremor, dysarthria, memory impairment, paraesthesia, impaired attention, confusion, euphoric mood, irritability - Vomiting, dry mouth, constipation, weight gain, increased appetite, flatulence - Blurred vision, diplopia, decreased libido, erectile dysfunction 8. - 1st treatment approved for fibromyalgia - One of the few agents that enhances slow-wave delta sleep, which may be helpful in chronic neuropathic pain syndrome |
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Protriptyline 1. Brand 2. Class 3. Indications 4. Dose |
1. Triptil, Vivactil 2. TCA 3. - Mental depression 4. 15 to 40mg/day in 3-4 divided doses |
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Protriptyline 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporter => boostsneurotransmitter norepinephrine => increases noradrenergic neurotransmission - Increase in dopamine neurotransmissionsecondary to norepinephrine reuptake inhibition - Substrate for CYP450 2D6 - Half-life approx. 74 hours |
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Protriptyline 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinaryretention, increased appetite, dry mouth, nausea, diarrhea, heartburn, unusualtaste in mouth - Weight gain, fatigue, weakness, dizziness, sedation, anxiety - Sexual dysfunction, Sweating, rash, itching 8. - Has some potential advantages for withdrawn, anergic patients - May have a more rapid onset of action than some other TCAs |
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Quazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Doral 2. Benzodiazepine 3. - Short-term treatment for insomnia 4. 15mg nocte |
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Quazepam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-Aligand-gated chloride channel complex => boosts chloride conductance throughGABA-regulated channels - Inhibits neuronal activity in the amygdala-centeredfear circuits 6. - Half-life 25 to 41 hours - Active metabolite - Metabolized in part by CYP450 3A4 |
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Quazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression, dizziness,ataxia - Slurred speech, weakness, forgetfulness - Confusion, hyperexcitability,nervousness 8. - Because quazepam tends to accumulate over time, perhaps not the best hypnotic for chronic nightly use - Long-term accumulation of quazepam and its active metabolites may cause insidious onset of confusion or falls, especially in the elderly |
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Quetiapine 1. Brand 2. Class 3. Indications 4. Dose |
1. Seroquel 2. Atypical antipsychotic 3. - Acute schizophrenia - Schizophrenia maintenance - Acute mania - Bipolar maintenance 4. 400 to 800mg/day in 1 or 2 doses |
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Quetiapine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis - Blocks serotonin 2A receptors => causes enhancement of dopamine release in certain areas of the brain thus reducing cognitive and affective symptoms - Interactions at a myriad of other neurotransmitters (specifically, 5HT1A receptors) may contribute to efficacy for cognitive and affective symptoms in some patients 6. - Metabolites are inactive - Parent drug has 6 to 7 hour half-life |
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Quetiapine 7. Adverse effects 8. Pearls |
7. - May increase risk of diabetes and dyslipidaemia - Dizziness, sedation, dry mouth, constipation, dyspepsia, abdominal pain - Weight gain, tachycardia, orthostatic hypotension 8. - Efficacy may be underestimated for psychosis and mania since Quetiapine is often under-dosed in clinical practice - Essentially no motor side effects or prolactin elevation - Anecdotal reports of efficacy in PTSD, including symptoms of sleep disturbance and anxiety |
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Ramelteon 1. Brand 2. Class 3. Indications 4. Dose |
1. Rozerem 2. Melatonin 1 and 2 receptor antagonist 3. - Insomnia (difficulty with sleep onset) - Primary insomnia 4. 8mg nocte |
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Ramelteon 5. MOA 6. Pharmacokinetics |
5. - Binds selectively to melatonin 1 and 2 receptors as a full antagonist 6. - Metabolised predominantly by CYP450 1A2 - CYP450 3A4 and 2C are also involved in metabolism of ramelteon - Mean elimination half-life of major metabolite, M-II, is 2 to 5 hours |
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Ramelteon 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, fatigue, headache - Respiratory depression 8. - May be preferred over benzodiazepines because of its rapid onset of action, short duration of effect, and safety profile - Rebound insomnia does not appear to be common |
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Reboxetine 1. Brand 2. Class 3. Indications 4. Dose |
1. Norebox, Edronax 2. Selective norepinephrine reuptake inhibitor (NRI) 3. - Major depressive disorder - Dysthymia - Panic disorder 4. 8mg/day in 2 doses |
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Reboxetine 5. MOA 6. Pharmacokinetics |
5. - Blocks norepinephrine transporters => boosts neurotransmitter norepinephrine => increases noradrenergic neurotransmission - Blocking norepinephrine reuptake in frontal cortex => increases dopamine neurotransmission 6. - Metabolised by CYP450 3A4 - Inhibits CYP450 2D6 and 3A4 at high doses - Elimination half-life approx. 13 hours |
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Reboxetine 7. Adverse effects 8. Pearls |
7. - Insomnia, dizziness, anxiety, agitation - Dry mouth, constipation, urinary hesitancy, urinary retention - Sexual dysfunction 8. - May be effective if SSRIs have failed or for SSRI "poop-out" - May be more likely than SSRI to improve social and work functioning |
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Risperidone 1. Brand 2. Class 3. Indications 4. Dose |
1. Risperdal, CONSTA 2. Atypical antipsychotic 3. - Schizophrenia - Other psychotic disorders - Acute mania - Autism-related irritability in children ages 5 to 16 4. 2 to 8mg/day orally for acute psychosis or bipolar disorder |
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Risperidone 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis - Blocks serotonin 2A receptors => causes enhancement of dopamine release in certain areas of the brain thus reducing cognitive and affective symptoms - Interactions at a myriad of other neurotransmitters may contribute to efficacy for cognitive and affective symptoms in some patients 6. - Metabolites are active - Metabolized by CYP450 2D6 - Parent drug of oral formulation has 20 to 24 hour half-life - Long-acting rsiperidone has 3 to 6 day half-life - Long-acting risperidone has elimination phase of approx. 7 to 8 weeks after last injection |
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Risperidone 7. Adverse effects 8. Pearls |
7. - May increase risk of diabetes and dyslipidaemia - Dizziness, sedation, dry mouth, constipation, dyspepsia, abdominal pain - Weight gain, tachycardia, orthostatic hypotension 8. - Often a preferred treatment for dementia with aggressive features - Often a preferred atypical antipsychotic for children with behavioural disturbances of multiple causations - Only atypical antipsychotic with a long-acting depot formulation |
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Rivastigmine 1. Brand 2. Class 3. Indications 4. Dose |
1. Exelon 2. Cholinesterase inhibitor; cognitive enhancer 3. - Alzheimer disease - Parkinson's disease dementia 4. 6 to 12mg in 2 doses |
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Rivastigmine 5. MOA 6. Pharmacokinetics |
5. - Pseudoirreversibly inhibits centrally acting acetylcholinesterase (AChE) => makes more acetylcholine available => compensates in part for degenerating cholinergic neurons in neocortex that regulate memory 6. - Elimination half-life 1 to 2 hours - Not hepatically metabolized; no CYP450 mediated pharmacokinetic drug interactions |
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Rivastigmine 7. Adverse effects 8. Pearls |
7. - Nausea, diarrhea, vomiting, appetite loss, weight loss, dyspepsia, increased gastric acid secretion - Headache, dizziness - Fatigue, asthenia, sweating 8. - Treats behavioural and psychological symptoms of Alzheimer dementia as well as cognitive symptoms - May be more useful for later stages or for more rapidly progressive forms of Alzheimer disease, when gliosis increases butyrylcholinesterase |
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Selegiline 1. Brand 2. Class 3. Indications 4. Dose |
1. EMSAM, Eldepryl 2. - Oral: Selective MAO-B inhibitor - Transdermal: tissue selective MAOI (MAO-B and MAO-A in brain) 3. - Major depressive disorder - Parkinson's disease (adjunct) 4. - Oral: 30 to 60mg/day - Transdermal: 6mg/24hrs to 12mg/24hrs |
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Selegiline 5. MOA 6. Pharmacokinetics |
5. - Oral: selectively and irreversibly blocks MAO-B - Transdermal: irreversibly inhibits MAO-A and MAO-B 6. - Clinical duration of action may be up to 21 days due to irreversible enzyme inhibition - Mean half-life of transdermal is approx. 18 to 25 hours - Steady-state mean elimination half-life of oral is approx. 10 hours |
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Selegiline 7. Adverse effects 8. Pearls |
7. - Transdermal: application site reactions, headache, insomnia, diarrhea, dry mouth - Oral: exacerbation of levodopa side effects, especially nausea, dizziness, abdominal pain, dry mouth, headache, dyskinesia, confusion, hallucinations, vivid dreams 8. - Transdermal administration may allow freedom from dietary restrictions - Enhancement of levodopa action can occur for Parkinson's patients at low oral doses, but antidepressant actions probably require high oral doses that do not have the potential tissue selectivity and lack dietary restrictions of the low dose transdermal formulation |
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Sertraline 1. Brand 2. Class 3. Indications 4. Dose |
1. Zoloft 2. SSRI 3. - Major depressive disorder - Panic disorder - PTSD - Social phobia - OCD, GAD 4. 50 to 200mg/day |
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Sertraline 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin transporters => boosts neurotransmitter serotonin => increases serotonergic neurotransmission - Also has some ability to block dopamine transporter => increases dopamine => contributes to therapeutic action 6. - Parent drug has 22 to 36 hour half-life - Metabolite half-life of 62 to 104 hours - Inhibits CYP450 2D6 - Inhibits CYP450 3A4 |
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Sertraline 7. Adverse effects 8. Pearls |
7. - Sexual dysfunction (delayed ejaculation, erectile dysfunction, decreased sexual desire) - GI symptoms (decreased appetite, nausea, diarrhea, constipation, dry mouth) - Insomnia, agitation, tremors, headache, dizziness - Sedation is reported but not expected; possibly activating in some patients 8. - Cognitive and affective "flattening" may theoretically be diminished in some patients by sertraline's dopamine reuptake blocking properties - May be a 1st line choice for atypical depression due to activation in some patients |
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Sulpiride 1. Brand 2. Class 3. Indications 4. Dose |
1. Dolmatil 2. Typical antipsychotic 3. - Schizophrenia - Depression 4. 400 to 800mg/day in 2 doses |
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Sulpiride 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis - Also blocks D3 and D4 receptors 6. - Elimination half-life approx. 6 to 8 hours - Excreted largely unchanged |
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Sulpiride 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome, extra-pyramidal symptoms - Galactorrhea, amenorrhea - Insomnia, excitement, restlessness, dry mouth, constipation, vision disturbance - Weight gain, hypotension 8. - Controversy over whether sulpride is more effective than older typical antipsychotics at treating negative symptoms - Some patients with inadequate response to clozapine may benefit from augmentation with sulpride |
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Temazepam 1. Brand 2. Class 3. Indications 4. Dose |
1. Restoril 2. Benzodiazepines 3. Short-term treatment of insomnia 4. 15mg nocte |
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Temazepam 5. MOA 6. Pharmacokinetics |
5. - Binds tobenzodiazepine receptors at the GABA-A ligand-gated chloride channel complex=> boosts chloride conductance through GABA-regulated channels - Inhibits neuronal activity inthe amygdala-centered fear circuits 6. - No active metabolites - Half-life approx. 8 to 15 hours |
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Temazepam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression, dizziness, ataxia - Slurred speech, weakness, forgetfulness - Confusion, hyperexcitability, nervousness 8. - Notable for delayed onset of action compared to some other sedative hypnotics - Slow gastrointestinal absorption compared to other sedative benzodiazepines, so may be more effective for nocturnal awakening than for initial insomnia unless dosed 1-2 hours prior to bedtime |
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Thioridazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Mellaril 2. Typical antipsychotic (phenothiazine) 3. - Schizophrenic patients who fail to respond to treatment with other antipsychotic drugs 4. 200 to 800mg/day in divided doses |
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Thioridazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Metabolised by CYP450 2D6 |
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Thioridazine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induceddeficit syndrome, extra-pyramidal symptoms - Galactorrhea, amenorrhea - Insomnia, excitement,restlessness, dry mouth, constipation, vision disturbance - Weight gain, hypotension 8. - Generally, the benefits of Thioridazine do not outweigh its risks for most patients - Because of its QTc prolongation, it is not intended for use unless other options have failed |
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Thiothixene 1. Brand 2. Class 3. Indications 4. Dose |
1. Navane 2. Typical antipsychotic (thioxanthene) 3. - Schizophrenia - Other psychotic disorders 4. 15 to 30mg/day |
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Thiothixene 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Initial elimination half-life approx. 3.4 hours - Terminal elimination half-life approx. 34 hours |
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Thiothixene 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome, extra-pyramidal symptoms - Galactorrhea, amenorrhea - Insomnia, excitement, restlessness, dry mouth, constipation, vision disturbance - Weight gain, hypotension 8. - Although not systematically studied, may cause less weight gain than other antipsychotics - Patients have very similar antipsychotic responses to any typical antipsychotic, which is different from atypical antipsychotics that can occasionally vary greatly |
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Tiagabine 1. Brand 2. Class 3. Indications 4. Dose |
1. Gabitril 2. Anticonvulsant 3. - Partial seizures - Anxiety disorders - Neuropathic pain/chronic pain 4. - 32 to 56mg/day in 2-4 divided doses for epilepsy - 2 to 12mg/day for adjunctive treatment of chronic pain and anxiety disorder |
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Tiagabine 5. MOA 6. Pharmacokinetics |
5. - Selectively blocks reuptake of GABA by presynaptic and glial GABA transporters 6. - Primarily metabolised by CYP450 3A4 - Steady state concentrations tend to be lower in the evening than in the morning - Half-life approx. 7 to 9 hours - Renally excreted |
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Tiagabine 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, asthenia, nervousness, difficulty concentrating, speech/language problems - Confusion, tremor 8. - Much use is off-label; 2nd line and as an augmenting agentmay be justified for treatment resistant anxiety disordes and neuropathic pain and also for fibromyalgia - One of the few agents that enhances slow-wave delta sleep, which may be helpful in chronic pain syndromes |
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Tianeptine 1. Brand 2. Class 3. Indications 4. Dose |
1. Coaxil, Stablon, Tatinol 2. Glutamergic modulator; often classified as a TCA but pharmacologically distinct 3. - Major depressive disorder - Dysthymia 4. |
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Tianeptine 5. MOA 6. Pharmacokinetics |
5. - Modulates glutamatergic neurotransmission, perhaps through potentiation of AMPA receptor function - Possibly increases serotonin uptake, but could also act similarly to agents that block serotonin reuptake 6. - Not primarily metabolised by CYP450 enzyme system - Tianeptine is rapidly eliminated - Half-life approx. 2.5 hours |
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Tianeptine 7. Adverse effects 8. Pearls |
7. - Headache, dizziness, insomnia, sedation, nausea, constipation, abdominal pain, dry mouth - Abnormal dreams - Tachycardia 8. - Mechanism of action not well understood - Not marketed widely throughout the world but mostly in France |
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Topiramate 1. Brand 2. Class 3. Indications 4. Dose |
1. Topamax, Epitomax, Topamac, Topimax 2. Anticonvulsant 3. - Partial seizures - Migraine prophylaxis - Bipolar disorder (adjunct) 4. 200 to 400mg/day in 2 divided doses |
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Topiramate 5. MOA 6. Pharmacokinetics |
5. - Blocks voltage-sensitive sodium channels by an unknown mechanism - Inhibits release of glutamate - Potentiates activity of GABA 6. - Elimination half-life approx. 21 hours - Renally excreted |
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Topiramate 7. Adverse effects 8. Pearls |
7. - Sedation, asthenia, dizziness, ataxia, parasthesia, nervousness, nystagmus, tremor - Nausea, appetite loss, weight loss - Blurred vision, mood problems, confusion, memory problems, psychomotor retardation 8. - Some anecdotes, cases series, and open-label studies have been published and are widely known suggesting efficacy in bipolar disorder - However, randomised clinical trials do not suggest efficacy in bipolar disorder |
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Tranylcypromine 1. Brand 2. Class 3. Indications 4. Dose |
1. Parnate 2. MAOI 3. - Major depressive episode without melancholia 4. 30mg/day in divided doses |
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Tranylcypromine 5. MOA 6. Pharmacokinetics |
5. - Irreversibly blocks MAO from breaking down norepinephrine, serotonin, and dopamine => boosts noradrenergic, serotonergic, and dopaminergic neurotransmission - As the drug is structurally related to amphetamine, it may have some stimulant-like actions due to monoamine release and reuptake inhibition 6. - Clinical duration of action may be up to 21 days due to irreversible enzyme inhibition |
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Tranylcypromine 7. Adverse effects 8. Pearls |
7. - Agitation, anxiety, insomnia, weakness, sedation, dizziness - Constipation, dry mouth, nausea, diarrhea, change in appetite, weight gain - Sexual dysfunction 8. - MAOIs are generally reserved for 2nd line use after SSRIs, SNRIs, and combination of newer antidepressants have failed |
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Trazodone 1. Brand 2. Class 3. Indications 4. Dose |
1. Desyrel 2. SARI (serotonin 2 antagonist/reuptake inhibitor) 3. - Depression - Insomnia 4. |
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Trazodone 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin 2A receptors potently - Blocks serotonin reuptake pump (serotonin transporter) less potently 6. - Metabolised by CYP450 3A4 - Half-life is biphasic; 1st phase is approx. 3 to 6 hours long; 2nd phase is approx. 5 to 9 hours |
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Trazodone 7. Adverse effects 8. Pearls |
7. - Nausea, vomiting, edema, blurred vision, constipation, dry mouth - Dizziness, sedation, fatigue, headache, incoordination, tremor - Hypotension, syncope 8. - For insomnia when it is preferred to avoid the use of dependence-forming agents - As an adjunct to the treatment of residual anxiety and insomnia with other antidepressants |
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Triazolam 1.Brand 2. Class 3. Indications 4. Dose |
1. Halcion 2. Benzodiazepine 3. - Short-term treatment of insomnia 4. 0.125 to 0.25mg nocte |
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Triazolam 5. MOA 6. Pharmacokinetics |
5. - Binds to benzodiazepine receptors at the GABA-A ligand-gatedchloride channel complex=> boosts chloride conductance throughGABA-regulated channels - Inhibits neuronal activity in the amygdala-centered fear circuits 6. - Half-life 1.5 to 5.5 hours - Inactive metabolites |
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Triazolam 7. Adverse effects 8. Pearls |
7. - Sedation, fatigue, depression, dizziness, ataxia - Slurred speech, weakness, forgetfulness - Confusion, hyperexcitability, nervousness 8. - Shorter half-life should prevent impairments in cognitive and motor performance during the day as well as daytime sedation - The risk of unusual behaviours or hallucinations may be greater with triazolam than with other sedative benzodiazepines |
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Trifluoperazine 1. Brand 2. Class 3. Indications 4. Dose |
1. Stelazine 2. Typical antipsychotic (phenothiazine) 3. - Schizophrenia - Nonpsychotic anxiety - Other psychotic disorders 4. 15 to 20mg/day |
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Trifluoperazine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Mean elimination half-life approx. 12.5 hours |
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Trifluoperazine 7. Adverse effects 8. Pearls |
7. - Neuroleptic-induced deficit syndrome, extra-pyramidal symptoms - Galactorrhea, amenorrhea - Insomnia, excitement, restlessness, dry mouth, constipation,vision disturbance - Weight gain, hypotension 8. - Although not systematically studied, may cause less weight gain than other antipsychotics - Less risk of sedation and orthostatic hypotension but greater extrapyramidal symptoms than with low potency phenothiazines |
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Trimipramine 1. Brand 2. Class 3. Indications 4. Dose |
1. Surmontil 2. TCA 3. - Depression - Endogenous depression - Anxiety - Insomnia - Neuropathic pain/chronic pain 4. 50 to 150mg/day |
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Trimipramine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters => boostsneurotransmitters serotonin and norepinephrine => increases serotonergic andnoradrenergic neurotransmission - Trimipramine can also increase dopamine neurotransmission infrontal cortex via blocking norepinephrine reuptake 6. - Substrate for CYP450 2D6, 2C19, and 2C9 - Half-life approx. 7 to 23 hours |
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Trimipramine 7. Adverse effects 8. Pearls |
7. - Blurred vision, constipation, urinary retention, increasedappetite, dry mouth, nausea, diarrhea- Heartburn, unusual taste in mouth, weight gain- Fatigue, weakness, dizziness, sedation - Sexual dysfunction, sweating 8. - May be more sedating than some other TCAs - May be more useful than some other TCAs for patients with anxiety, sleep disturbance, and depression with physical illness |
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Valproate 1. Brand 2. Class 3. Indications 4. Dose |
1. Depakene, Depacon, Stavzor, Depakote 2. Anticonvulsant 3. - Acute mania - Complex partial seizures - Migraine prophylaxis - Maintenance treatment of bipolar disorder 4. 1,200 to 1,500mg/day |
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Valproate 5. MOA 6. Pharmacokinetics |
5. - Blocks voltage-sensitive sodium channels by an unknown mechanism - Increases brain concentrations of GABA by an unknown mechanism 6. - Mean terminal half-life is 9 to 16 hours - Metabolised primarily by the liver, approx. 25% dependent upon CYP450 system |
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Valproate 7. Adverse effects 8. Pearls |
7. - Sedation, tremor, dizziness, ataxia, headache - Abdominal pain, nausea, vomiting, diarrhea, reduced appetite, constipation, dyspepsia, weight gain - Alopecia 8. - Valproate is a 1st line treatment option that may be best for patients with mixed states of bipolar disorder or for patients with rapid cycling bipolar disorder - Used to treat aggression, agitation, and impulsivity not only in bipolar disorder and schizophrenia but also in many other disorders, including dementia, personality disorders, and brain injury |
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Varenicline 1. Brand 2. Class 3. Indications 4. Dose |
1. Chantix, Champix 2. Alpha 4 beta 2 partial agonist of nicotinic acetylcholine receptors 3. - Nicotine addiction/dependence 4. 1mg BD |
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Varenicline 5. MOA 6. Pharmacokinetics |
5. - Causes sustained but small amounts of dopamine release (less than with nicotine) - Specifically, as a partial agonist at alpha 4 beta 2 nicotinic acetylcholine receptors, varenicline activates these receptors to a lesser extent than the full agonist nicotine and also prevents nicotine from binding to these receptors - Most prominent actions are on mesolimbic dopaminergic neurons in the ventral tegmental area 6. - Elimination half-life of 24 hours |
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Varenicline 7. Adverse effects 8. Pearls |
7. - Dose-dependent nausea, vomiting, constipation, flatulence - Insomnia, headache, abnormal dreams 8. - More effective than nicotine or bupropion - Unlike nicotine or bupropion, the patient cannot "smoke over" varenicline since varenicline, but not the others, will block the effects of additional smoked nicotine if the patient decides to smoke during treatment |
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Venlafaxine 1. Brand 2. Class 3. Indications 4. Dose |
1. Effexor 2. SNRI 3. - Depression - GAD, social phobia, panic disorder, PTSD 4. 75 to 225mg/day divided into 2-3 doses |
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Venlafaxine 5. MOA 6. Pharmacokinetics |
5. - Blocks serotonin and norepinephrine transporters =>increases serotonergic and noradrenergic neurotransmission - Dopamine is also increased in frontal cortex secondary toblockade of norepinephrine reuptake 6. - Parent drug has 3 to 7 hour half-life - Active metabolite has 9 to 13 hour half-life |
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Venlafaxine 7. Adverse effects 8. Pearls |
7. - Insomnia, sedation, anxiety, dizziness - Nausea, vomiting, constipation, decreased appetite - Sexual dysfunction, sweating, SIADH, hyponatraemia 8. - May be effective in patients who fail to respond to SSRIs, and may be one of the preferred treatments for treatment-resistant depression |
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Zaleplon 1. Brand 2. Class 3. Indications 4. Dose |
1. Sonata 2. - Non-benzodiazepine hypnotic - Alpha 1 isoform agonist of GABA-A/benzodiazepine receptors 3. - Short-term treatment of insomnia 4. 10mg nocte |
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Zaleplon 5. MOA 6. Pharmacokinetics |
5. - Binds selectively to a subtype of the benzodiazepine receptor, the alpha 1 isoform => boosts chloride conductance through GABA-regulated channels => may enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA 6. - Terminal phase elimination half-life approx. 1 hour |
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Zaleplon 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, ataxia, dose-dependent amnesia - Hyper-excitability, nervousness - Headache, decreased appetite 8. - May be preferred over benzodiazepines because of its rapid onset of action, short duration of effect, and safety profile - Popular for uses requiring short half-life (eg. dosing in the middle of the night, sleeping on airplanes, jet lag) |
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Ziprasidone 1. Brand 2. Class 3. Indications 4. Dose |
1. Geodon 2. Atypical antipsychotic 3. - Schizophrenia - Acute agitation in Schizophrenia - Acute mania - Behavioural disturbances 4. 40 to 200mg/day in divided doses |
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Ziprasidone 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms ofpsychosis - Blocks serotonin 2A receptors => causes enhancement of dopaminerelease in certain areas of the brain thus reducing cognitive and affectivesymptoms - Interactions at a myriad of other neurotransmitters(specifically, 5HT1A and 5HT2C receptors) may contribute to efficacy for cognitive andaffective symptoms in some patients 6. - Mean half-life of 6.6 hours - Protein binding > 99% - Metabolized by CYP450 3A4 |
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Ziprasidone 7. Adverse effects 8. Pearls |
7. - Dizziness, sedation, dry mouth, constipation, dyspepsia,abdominal pain - Weight gain, tachycardia, orthostatic hypotension - Extrapyramidal symptoms 8. - Well-accepted in clinical practice when wanting to avoid weight gain because less weight gain than most other atypical antipsychotics |
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Zolpidem 1. Brand 2. Class 3. Indications 4. Dose |
1. Ambien 2. - Non-benzodiazepine hypnotic - Alpha 1 isoform selective agonist of GABA-A/benzodiazepine receptors 3. - Short-term treatment of insomnia 4. 10mg nocte |
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Zolpidem 5. MOA 6. Pharmacokinetics |
5. - Binds selectively to a subtype of the benzodiazepine receptor, the alpha 1 isoform => boosts chloride conductance through GABA-regulated channels => may enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA 6. - Short elimination half-life of approx. 2.5 hours |
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Zolpidem 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, ataxia, dose-dependent amnesia - Hyper-excitability, nervousness - Headache 8. - One of the most popular sedative hypnotic agents in psychopharmacology - May be preferred over benzodiazepines because of its rapid onset of action, short duration of effect, and safety profile - Has been shown to increase the total time asleep and to reduce the amount of nighttime awakenings |
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Zonisamide 1. Brand 2. Class 3. Indications 4. Dose |
1. Zonegran, Excegran 2. Anticonvulsant 3. - Adjunct therapy for partial seizures - Bipolar disorder 4. 100 to 600mg/day in 1-2 doses |
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Zonisamide 5. MOA 6. Pharmacokinetics |
5. - Unknown - Modulates voltage-sensitive sodium channels by an unknown mechanism - Facilitates dopamine and serotonin release 6. - Plasma elimination half-life approx. 63 hours - Metabolized in part by CYP450 3A4 - Partially eliminated renally |
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Zonisamide 7. Adverse effects 8. Pearls |
7. - Sedation, depression, difficulty concentrating, agitation, irritability - Psychomotor slowing, dizziness, ataxia - Headache, nausea, anorexia, abdominal pain, vomiting - Kidney stones 8. - Much off-label use is based upon theoretical considerations rather than clinical experience or compelling efficacy studies |
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Zopiclone 1. Brand 2. Class 3. Indications 4. Dose |
1. Imovane 2. - Non-benzodiazepine hypnotic - Alpha 1 isoform selective agonist of GABA-A/benzodiazepine receptors 3. - Short-term treatment of insomnia 4. 7.5mg nocte |
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Zopiclone 5. MOA 6. Pharmacokinetics |
5. - Binds selectively to a subtype of the benzodiazepine receptor, the alpha 1 isoform => boosts chloride conductance through GABA-regulated channels => may enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA 6. - Metabolized by CYP450 3A4 - Terminal elimination half-life approx. 3.5 to 6.5 hours |
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Zopiclone 7. Adverse effects 8. Pearls |
7. - Sedation, dizziness, ataxia, dose-dependent amnesia - Hyper-excitability, nervousness - Headache, dry mouth, loss of appetite, constipation, bitter taste 8. - May be preferred over benzodiazepines because of its rapid onset of action, short duration of effect, and safety profile |
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Zotepine 1. Brand 2. Class 3. Indications 4. Dose |
1. Lodopin, Zoleptil 2. Atypical antipsychotic 3. - Schizophrenia 4. 75 to 300mg/day in 3 divided doses |
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Zotepine 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis - Blocks serotonin 2A receptors => causes enhancement of dopamine release in certain areas of the brain thus reducing cognitive and affective symptoms - Interactions at a myriad of other neurotransmitters may contribute to efficacy for cognitive and affective symptoms in some patients 6. - Metabolized by CYP450 3A4 and CYP450 1A2 - Active metabolite norzotepine |
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Zotepine 7. Adverse effects 8. Pearls |
7. - May increase the risk of diabetes and dyslipidaemia - Dizziness, sedation, dry mouth, constipation, dyspepsia, abdominal pain - Weight gain, tachycardia, orthostatic hypotension - Extrapyramidal symptoms 8. - Zotepine inhibits norepinephrine reuptake, which may have implications for treatment of depression, as well as cognitive symptoms of schizophrenia |
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Zuclopenthixol 1. Brand 2. Class 3. Indications 4. Dose |
1. Clopixol 2. Typical antipsychotic 3. - Schizophrenia 4. 20 to 60mg/day |
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Zuclopenthixol 5. MOA 6. Pharmacokinetics |
5. - Blocks D2 receptors => reduces positive symptoms of psychosis 6. - Metabolized by CYP450 2D6 - For oral formulation: elimination half-life approx. 20 hours - For acetate: rate-limiting half-life approx. 32 hours - For decanoate: rate-limiting half-life approx. 17 to 21 days with multiple doses |
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Zuclopenthixol 7. Adverse effects 8. Pearls |
7. - D2 block: extrapyramidal symptoms, galactorrhea, amenorrhea, neuroleptic-induced deficit syndrome - Anticholinergic: sedation, blurred vision, constipation, dry mouth - Antihistaminic: sedation, weight gain 8. - Potential advantages with non-compliant patients |
