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72 Cards in this Set
- Front
- Back
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Amitripyline (Elavil)
Nortriptyline (Pamelor) |
TCA
- Inhibit the reuptake (NE, 5-HT) - Also block muscarinic cholinergic, alpha1 adrenergic, histamine (H1) receptors - Use: Depression, Enuresis (imipramine most commonly used), Chronic pain (amitriptyline) -- Behavioral effect: inhibition of reuptake occurs immediately, but it may take 2 - 3 weeks to begin to see antidepressant activity, and 8-10 weeks for maximal effect ? adaptive changes in the process of neurotransmission (down- or up-regulation of receptors, changes in second messenger systems, etc.) ---> produce resolution of symptoms - Side effects -- Sedationn, normal subjects do not show mood elevation (may feel unpleasant or dysphoric), seizures in high doses -- weight gain -- withdrawal can occur if stopped abruptly -- nausea, dizziness, headache, increased perspiration, salivation patients should be slowly tapered off drug -- Autnomic Nervous system Anticholinergic (antimuscarinis activity): Dry mouth, blurred vision, constipation, urinary retention -- CV : Tachycardia, arrhythmias, Orthostatic hypotension, bundle branch block and impaired conduction -- OD can be fatal - potential to exacerbate CNS depressants, sympathetic amines, antimuscarinics, Alzheimer's...can be problematic to give with MAOis! |
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Imipramine (Tofranil)
Desipramine (Norpramin) Clomipramine (Anafranil) |
TCA
- Inhibit the reuptake (NE, 5-HT) - Also block muscarinic cholinergic, alpha1 adrenergic, histamine (H1) receptors - Use: Depression, Enuresis (imipramine most commonly used), Chronic pain (amitriptyline) -- Behavioral effect: inhibition of reuptake occurs immediately, but it may take 2 - 3 weeks to begin to see antidepressant activity, and 8-10 weeks for maximal effect ? adaptive changes in the process of neurotransmission (down- or up-regulation of receptors, changes in second messenger systems, etc.) ---> produce resolution of symptoms - Side effects -- Sedationn, normal subjects do not show mood elevation (may feel unpleasant or dysphoric), seizures in high doses -- weight gain -- withdrawal can occur if stopped abruptly -- nausea, dizziness, headache, increased perspiration, salivation patients should be slowly tapered off drug -- Autnomic Nervous system Anticholinergic (antimuscarinis activity): Dry mouth, blurred vision, constipation, urinary retention -- CV : Tachycardia, arrhythmias, Orthostatic hypotension, bundle branch block and impaired conduction -- OD can be fatal - potential to exacerbate CNS depressants, sympathetic amines, antimuscarinics, Alzheimer's...can be problematic to give with MAOis! |
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Miratazapine (Remeron)
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2nd gen antidepressant
- Blocks 5-HT2 and alpha2 adrenergic receptors - Doesn’t inhibit reuptake - Very sedative and associated with weight gain |
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Bupropion
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2nd gen antidepressant
- A weak inhibitor of reuptake of NE, DA - nAChR antagonist - uses: depression, smoking cessation - Side effect profile -- Can cause seizures esp in patients with eating disorders -- Doesn’t cause weight gain or sexual dysfunction |
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Trazodone (desyrel)
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2nd gen antidepressant
- Inhibits serotonin reuptake and block 5-HT2 receptors - Little antimuscarinic and autonomic activity - Side effect -- Very sedative; frequently used to promote sleep in nondepressed patients -- Can produce priapism |
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St. John's Wort
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Herbal tx for depression
- CYP450 inducer; be wary if patients are taking this, as it will mae other drugs less effective |
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Fluoxetine (prozac)
Paroxetine (Paxil) |
SSRi
NOTE ROOT SIMILARITY TO DULOXETINE (an SNRI) - Block reuptake of 5-HT - Little effect on NE and muscarinic of alpha1 receptors - Side Effect profile -- Produce few CV, antimuscarinic side effects -- Nausea (mild and transient), GI upset, Headache, Insomnia, Nervousness, Sexual dysfunction (decrease libido, anorgasmia) -- Sexual dysfunction is normally why people stop using these |
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Fluvoxamine (luvox)
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SSRi
- Block reuptake of 5-HT - Little effect on NE and muscarinic of alpha1 receptors - Side Effect profile -- Produce few CV, antimuscarinic side effects -- Nausea (mild and transient), GI upset, Headache, Insomnia, Nervousness, Sexual dysfunction (decrease libido, anorgasmia) -- Sexual dysfunction is normally why people stop using these |
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Sertaline (zoloft)
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SSRi
- Block reuptake of 5-HT - Little effect on NE and muscarinic of alpha1 receptors - Side Effect profile -- Produce few CV, antimuscarinic side effects -- Nausea (mild and transient), GI upset, Headache, Insomnia, Nervousness, Sexual dysfunction (decrease libido, anorgasmia) -- Sexual dysfunction is normally why people stop using these |
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Citalopram (celexa)
Escitalopram (lexapro) |
SSRi
- Block reuptake of 5-HT - Little effect on NE and muscarinic of alpha1 receptors - Side Effect profile -- Produce few CV, antimuscarinic side effects -- Nausea (mild and transient), GI upset, Headache, Insomnia, Nervousness, Sexual dysfunction (decrease libido, anorgasmia) -- Sexual dysfunction is normally why people stop using these |
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Duloxetine (cymbalta)
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SNRI
NOTE ROOT SIMILARITY TO SSRis - Blocks both 5-HT and NE reuptake |
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Venlafaxine (Effexor)
Desvenlafaxine (Pritiq) |
SNRI
- Primarily block 5-HT reuptake at lower does, and both 5-HT and NE reuptake at higher doses -May cause more restlessness and insomnia that SSRIs |
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Isocarboxazid (marplan)
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Hydrazides, MAOi
- Inhibit MAO A and B |
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Phenelzine (Nardil)
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Hydrazides, MAOi
- Inhibit MAO A and B - increases concentration of biogenic amines - Uses: 2nd line for depression, narcolepsy - mood elevation takes 2-3 wks. - Side effects -- CV: orthostatic hypotension and decrease blood pressure in hypertensives -- CNS stimulation (dizziness, headache, inability to sleep) Inhibits ejaculation -- Hepatotoxicity (hypersensitivity rxn, serious) -- OD: tachycardia, coma, convulsions, hyperthermia, hypo and hypertension, watch for 1 wk - Drug interactions: -- Wait 10-14 days before giving another drug -- Hypertensive crisis if used with sympathomimetic amine or in tyramine ingested. Can lead to stroke or death -- Potentiate tricyclic antidepressents leading to hypertensive crisis -- Potentiate effects of CNS depressents and drugs that are oxidatively deaminated -- Potential fatal adverse rxn with opiates, esp meperidine |
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Tranylcypromine (Parnate)
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Non-hydrazide structurally similar to d-Amphetamine, MAOi
- inhibits MAO A and B |
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Selegiline
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Selective MAO B inhibitor
- Primary use= parkinsons - Also available in transdermal patch |
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Lithium
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mood stabilizer
- Administered as lithium carbonate - Mech: unknown. May change electrolyte conductance (close Na+ in periodic table). - Interferes with phosphatidylinositol signaling cascade in brain - Pharmacokinectics: -- Absorption: rapidly and well absorbed -- Metabolism: not metabolized -- Excretion: only by renal -- T1/2= 24hr, reduced in renal disease, reduced by diuretics so lithium dose must be reduced - Side effects - low therapeutic index -- CNS: little effect in nLs, calms manics and dampen mood swings in patients with bipolar -- Nausea, vomiting, diarrhea -- Fine tremor common- treat with propranol -- Fatigue, muscle weakness, confusion, slurred speech, ataxia. Seizures. -- Polyuria, polydipsia: Li+ inhibits action of ADH on distal tubule (blocks cAMP production) -- Decrease thyroid function, can lead to thyroid enlargement -- Cardiac arrhythmias -- Weight gain, fluid retention (NA retention) |
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Valproic acid
lamotrigine carbamazepine |
mood stabilizers, Na+ channel blocking activity
- All have Na+ channel inhibiting activity +/- other effects - VPA is teratogenic - Carb can cause a number of varied side effects, including SJS and aplastic anemia. It's a teratogen also |
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Disulfiram (antabuse)
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anti-abuse treatment, AHD inhibitor
- nhibits aldehyde dehydrogenase, increasing acetaldehyde and causing headache, nausea, vomiting. (so-so evidence) - Effects can last 72 hours after last dose - Most likely to benefit: highly motivated patients, directly observed patients - Side effects:Nausea, metallic taste,dysphoria, fatigue, hepatitis, psychosis (dopamine) |
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Naltrexone (oral - Revia, IM - vivitrol)
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anti-abuse treatment, opiate antagonist
- Opiate Antagonist - decrease positive or reinforcing effects, increase negative aspects of drinking, decrease craving from first dose (prime), decrease craving from cues - modest effect yet expensive - SE: dysphoria, nausea, increased LFTs |
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Acamprosate (campral)
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anti-abuse treatment
- NMDA receptor antagonist, GABA agonist - SE: Diarrhea, rash. |
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Methadone (Dolophine; Symoron)
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anti-abuse treatment
- u-opiod agonist - Can still overdose and withdrawal - Decreased withdrawal, suppress urges and craving |
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Burpenorphine (Subutex and Suboxone)
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anti-abuse treatment
- partial u-opiod agonist; long dissociatio but partial agonism - Reported to reduce pleasure from opiates - Doesn’t seem to reduce cravings in opiate dependent. Some evidence for “highly motivated” patients or directly observed - Overdose risk increased after d/c |
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Thiopental (Pentothal)
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barbituate
- ultra-short acting; highly lipohillic - positive allosteric modulator of GABAa - Uses: anxiety, induction of anesthesia, anticonvulsant - Side effects -- low therapeutic window -- induces porphyrin synythesis by induving aminolevulinic acid synthetase) -- Induces hepatic microsomal enzymes and their own metabolism -- death from overdose due to respiratory depression,cardiovascular collapse, pulmonary edema, pneumonia --causes dependence |
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Pentobarbital (Nembutal)
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barbituate
- medium duration of action - positive allosteric modulator of GABAa - Uses: anxiety, induction of anesthesia, anticonvulsant - Side effects -- low therapeutic window -- induces porphyrin synythesis by induving aminolevulinic acid synthetase) -- Induces hepatic microsomal enzymes and their own metabolism -- death from overdose due to respiratory depression,cardiovascular collapse, pulmonary edema, pneumonia --causes dependence |
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Phenobarbital (Luminal)
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barbituate
- long duration of action - positive allosteric modulator of GABAa, - Uses: anxiety, induction of anesthesia, anticonvulsant - Side effects -- low therapeutic window -- induces porphyrin synythesis by induving aminolevulinic acid synthetase) -- Induces hepatic microsomal enzymes and their own metabolism -- death from overdose due to respiratory depression,cardiovascular collapse, pulmonary edema, pneumonia --causes dependence |
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Ethanol
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BOOZE!
- positive regulator of GABA - Use: disinfectant, topical coolant for hyperthermia - Side effects -- CNS depressant -- CV: vasodilation, depress myocardial contractility -- GI: stimulatre gastric secretions, inhibits intestinal brush border enzymes involved in absorption of nutrients -- Blood: mild anemia, due to folic acid def -- Endocrine: decreases testosterone, inhibits ADH causing diuresis, sexual dysfunction Adverse reactions: Acute: not potent BAC 50-150: moderate intoxication: impaired sense of time and space, poor coordination, reduced reaction times, poor concentration, memory difficulties, impaired judgment -- Chronic use: peripheral neuropathy (paresthesias, tingling), cerebellar cortical degeneration, motor dysfunction, mammillary body atrophy, prevent REM and delta sleep, Amnesia for recent events (alcoholic blackouts) -- Wernicke-Korsakoff syndrome -- Fetal alcohol syndrome -- dependence - AMDE -- Well absorbed throughout GI (food just slows), will cross placenta -- primarily metabolized by the liver -- two enzyme systems involved in ethanol metabolism (alcohol dehydrogenase and aldehyde dehydrogenase); some microsomal mixes-function oxidase (CYP2E1) -- additive effects with other CNS depressants. --- effects on drug metabolism acute: decreases rate of metabolism of other drugs (enzyme competition) --- chronic: increases rate of drug metabolism (enzyme induction). increases aspirin-induced GI bleeding |
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Oxazepam
lorazepam |
Benzodiazepines
- do not form active metabolites - benzo of choice for those with liver disease (alcoholics) - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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Triazolam
midazolam |
Benzodiazepines
- short-acting benzo, anesthetics - use: insomina...less hangover or rebound anxiety - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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Diazepam
clonazepam |
Benzodiazepines
- active metabolites, long half-lives, accumulate when given - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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chloriazepoxide
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Benzodiazepines
- active metabolites, long half-lives, accumulate when given - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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Temazepam
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Benzodiazepines
- intermediate acting benzo - use: insomina, but sleep onset can be delayed due to absorption profile - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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Alprazolam
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Benzodiazepines
- intermediate acting benzo - Clinical effects: anxiolytic, sedative, hypnotic (but not normal sleep), anesthetic (not analgesic), anticonvulsant, muscle relaxant - Side effects -- Relatively safe but variability between patients but tendency for increased sensitivity in elderly, liver disease -- CNS: cognitive depression, sedation, antreretrograde amnesia, psychomotor impairment, withdrawal seizure -- OD is rare but can be fatal if combined with EtOh or other CNS depressant -- Can develop dependence and tolerance to sedative effects (but not others, including anxiolytic) - ADME: -- well absorbed -- lipid soluble -- hepatic metabolism -- many off the class accumulate, have long half lives |
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Flumazenil (Romazicon)
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Benzo ANTAGONIST
- competitive antagonist at the benzo binding site - used to treat benzo overdose |
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Buspirone
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non-benzo anxiolytic
- doesnt interact with GABA rec, partial agonist at 5HT 1a rec (decrease cAMP) - uses: general anxiety (long term!, minimal acute affects), drug of choice for long-term CNS depressant users - pharm profile -- response occurs only after several weeks of treatment -- produces little or no sedation; ("anxioselective”) - no anticonvulsant or muscle-relaxant properties -- little impairment of cognitive or psychomotor skills -- no tolerance or withdrawal upon cessation -- little or no abuse potential -- not additive with ethanol -- no cross-tolerance with benzos - side effects: some headaches, dizziness (mild) |
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Zolpidem (Ambien)
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non-benzo hypnotic
- GABA-A interaction - relatively short half-life (1.5 – 4.5h) - no active metabolites |
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Zaleplon (Sonata)
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non-benzo hypnotic
- GABA-A interaction - very short duration of action; useful for patients who have difficulty falling asleep or awaken in the middle of the night |
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Eszopiclone (Lunesta)
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non-benzo hypnotic
- GABA-A interaction - intermediate duration of action |
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Ramelteon (Rozerem)
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melatonin receptor agonist
- Non- Gaba mediated sedative hypnotics - Targets MT1 and MT2 melatonin receptors (expressed in SCN and thoughout brain) - Not been shown to produce dependence not potential for abuse - Use 1 to 2 days, not longer than 1 to 2 weeks |
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Caffeine
theophylline theobromine |
Methylxanthines
Natural alkaloids in plants, purine base - adenosine receptor antagonist (adenosine would decrease cAMPthrough GalphaI, so caffeine increases cAMP) - PDE activity at high doses not normally acheived in vivo - Potencies: theophylline>caffeine>theobromine - Effects -- CNS stimulatory effects: increases alertness and defers drowsiness and fatigue -- cardiovascular - increases heart rate, increases coronary blood flow -- respiratory smooth muscle - relaxes the smooth muscle of the bronchioles at high dosages -- gastric mucosa - stimulates secretion of HCl from the gastric mucosa (ulcers!) -- Diuretic - Side effects: anxiety, insomnia, precipitation of panic attacks, tachycardia, tremors, increase in urination frequency |
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Amphetamine (Benzedrine)
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amphetamine
- indirectly acting sympathomimetics - release catecholamines, (NE, DA) and 5-HT - block their reuptake - at high doses, MAO activity is also inhibited - Uses : narcolepsy, attention deficit disorder, not recommended for weight loss - Side effects -- Psychiatric: dizziness, tremor, hyperirritability, insomnia, hyperthermia; chronic use can produce paranoid psychosis, addiction -- Neurological: cerebral edema, hemorrhage; chronic use is associated with neurotoxicity (long-term dopaminergic deficits) -- Cardiovascular: effects include tachycardia, palpitations, arrhythmias, hypertension, headache, and stroke -- Gastrointestinal: anorexia, nausea, vomiting - hypertensive crisis with MAO inhibitors |
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Methamphetamine
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amphetamine
- long half-life - indirectly acting sympathomimetics - release catecholamines, (NE, DA) and 5-HT - block their reuptake - at high doses, MAO activity is also inhibited - Effects -- Central Nervous System - stimulant actions: causes wakefulness, mood elevation, and improves performance on dull repetitive tasks (does not facilitate learning); produces appetite suppression -- Cardiovascular stimulation -- Tolerance - occurs rapidly (tachyphylaxis) -- Psychological and physical dependence - the withdrawal syndrome (the crash) includes prolonged sleep, lassitude, fatigue, depression and intense hunger (hyperphagia) |
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Methylphenidate (ritalin or concerta ( long acting formulation))
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amphetamine
– blocks the reuptake of DA and NE but DOES NOT CAUSE RELEASE LIKE OTHERS - Pharmacologic Effects - similar to amphetamine but less potent, fewer peripheral and cardiovascular effects - Side effects - insomnia, restlessness, talkativeness, behavioral disturbances |
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Ephedrine, pseudoephedrine*
not on drug list |
Indirectly acting sympathomimetic
- ephedrine has alpha and beta adrenergic agonist activity; also blocks reuptake of norepinephrine; - so does pseudoephedrine but less potent |
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Atomoxetine*
not on drug list |
Selective norepinephrine reuptake inhibitor (NRI)
- approved for the treatment of ADHD - less abuse potential than stimulants, not scheduled as a controlled substance - "black box warning” from the FDA due to reports of increased suicidal thoughts and behaviors |
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Modefinil
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Unclear, "wakefulness promoting agent"
- mechanisms of action remain unclear; increases the release of DA; may also involve hypocretin, histamine, GABA, and glutamate that results in activation of NE neurons in locus ceruleus, leading to a more “wakeful state” considered a "wakefulness promoting agent" rather than a classic amphetamine-like stimulant - uses: narcolepsy and other sleep disorders; ADHD, and Alzheimer’s disease |
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Cocaine
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indirect sympathomimetic, Na+ channel blocker
- blocks the reuptake of DA, NE - Blocks Na+ channels (anesthesia) - Uses: only legitimate use is as a local anesthetic - Side effect -- CNS: similar to meth (seizures, hyperthermia and respiratory arrest) , physical and intense psychological dependence -- Peripheral Effects - local anesthetic activity, vasoconstriction of blood vessels; -- CV: can stimulate or stop the heart, stroke, ischemia (bowel, brain, heart, etc) -- Tolerance - rapidly develops to the CNS effects. Tolerance to other effects of cocaine develop at different rates and to different degrees -- OD can be fatal - ADME: can be smoked, infected, eaten, or snorted. Short half-life (only a few minute "high" |
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MDMA
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indirect sympathomimetic
- potent releaser and/or reuptake inhibitor of presynaptic 5-HT, DA, and NE - releases oxytocin and vasopressin - clinical effects: increased energy, euphoria, emotional warmth and empathy toward others, and distortions in sensory and time perception - Side effects -- increases in hr, bp -- Intoxication can cause something similar to symptoms of Serotonin Syndrome: neuromuscular effects (hyperreflexia, clonus, tremor), autonomic effects (hyperthermia, tachycardia) and mental effects (agitation, confusion, anxiety) -- negative aftereffects from seratonin surge include confusion, depression, sleep problems, drug craving, anxiety - may occur soon after taking the drug or during the days or weeks thereafter |
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LSD
psilocybin ('shrooms) mescaline Mescaline Peyote |
hallucinogens
- acts on 5-ht somehow, but mechanism is unknown - Sensory alterations (visual, auditory, taste, olfactory, kinaesthetic) - Pseudo-hallucination - Alteration in affectviity- eotional, euphora, dyseuphoria -LSD is EXTREMELY potent - dilated pupils; closed/open eye visual experiences, hallucinations - synesthesia - Acute tolerance develops after several days of administration |
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Synthetic Cathinones (Bath salts)
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indirect sympathomimetic
- MDMA like, stimulatory and hallucinogen - Adverse effects: cardiac, psychiatric, neuro signs and sxs most common like serotonin syndrome |
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Haloperidol
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butyorophenone, typical antipsychotic
- TCA-like backbone -> think TCA side effects but switch D antagonism for re-uptake activity - Block dopamine, muscarinic cholinergic, alpha1 adrenergic receptors, H1 histamine receptors - Uses: -- Acute pschosis, Schizophrenia, Schizoaffective Disorder, Schizophreniform Disorder and Brief Psychotic Disorder, manic episode, psychotic depression, depression, demential, rapid control of violence -- Tourette's, Nausea and vomiting, intractable hiccup - Side effects: --initial psychomotor slowing, emotional quieting (sedation and tranquilization), sleepiness, restlessness, and emotional indifference (called the neuroleptic syndrome) -- Neurologic (Extrapyramidal Syndrome (EPS): Parkinsonian Syndrome, Akathisia, Acute Dystonic Reactions, Tardive Dyskinesia -- Neuroleptic Malignant Syndrome (NMS) : fever, muscle rigidity, autonomic instability, and altered mental status --Brain electrical activity is slowed with increased synchronization. Decrease seizure threshold and can elicit seizures in susceptible individuals -- Endocrine - gynecomastia, galactorrhea, amenorrhea -- CV - orthostatic hypotension and fainting with reflex tachycardia, Cardiac tox -- ANS - Antimuscarinic effects (dry mouth, blurred vision, constipation, urinary retention). Inhibition of ejaculation -- Weight Gain -- Pigmentary Retinopathy – especially with thioridazine -- Allergic Reactions - agranulocytosis, cholestatic (obstructive) jaundice, dermatitis and photosensitivity reactions - Distribution Highly lipid soluble and extensively protein bound (>90%)Vd Metabolism |
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Chlorpromazine (Thorazine)
Fluphenazine (Prolixin) Thioridazine (Mellaril) |
Phenothiazides, typical antipsychotics
- think TCA side effects but switch D antagonism for re-uptake activity - Phenothiazines have very complicated metabolic pathways with active metabolites - Block dopamine, muscarinic cholinergic, alpha1 adrenergic receptors, H1 histamine receptors - Uses: -- Acute pschosis, Schizophrenia, Schizoaffective Disorder, Schizophreniform Disorder and Brief Psychotic Disorder, manic episode, psychotic depression, depression, demential, rapid control of violence -- Tourette's, Nausea and vomitting, intractable hiccup - Side effects: --initial psychomotor slowing, emotional quieting (sedation and tranquilization), sleepiness, restlessness, and emotional indifference (called the neuroleptic syndrome) -- Neurologic (Extrapyramidal Syndrome (EPS): Parkinsonian Syndrome, Akathisia, Acute Dystonic Reactions, Tardive Dyskinesia -- Neuroleptic Malignant Syndrome (NMS) : fever, muscle rigidity, autonomic instability, and altered mental status --Brain electrical activity is slowed with increased synchronization. Decrease seizure threshold and can elicit seizures in susceptible individuals -- Endocrine - gynecomastia, galactorrhea, amenorrhea -- CV - orthostatic hypotension and fainting with reflex tachycardia, Cardiac tox -- ANS - Antimuscarinic effects (dry mouth, blurred vision, constipation, urinary retention). Inhibition of ejaculation -- Weight Gain -- Pigmentary Retinopathy – especially with thioridazine -- Allergic Reactions - agranulocytosis, cholestatic (obstructive) jaundice, dermatitis and photosensitivity reactions - Distribution Highly lipid soluble and extensively protein bound (>90%)Vd Metabolism |
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Clozapine
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Atypical antipsychotic
- highly non-selective - DA and 5-HT Interactions - Uses: Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- CLOZAPiNE - agranulocytosis -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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rispiridone
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atypical antipsychotic
- highly non-selective - DA and 5-HT Interactions - Uses: -- UNIQUE FOR AUTISM IRRITATION -- Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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Aripiprazole
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Atypical antipsychotics
- a partial agonist at dopamine (and thus a net antagonist, particularly D4) and serotonin receptors - Uses: -- Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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olanzapine(zyprexa)
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Atypical antipsychotics
- highly non-selective - DA and 5-HT Interactions - Uses: -- Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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quetiapine (seroquel),
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Atypical antipsychotics
- highly non-selective - DA and 5-HT Interactions - Uses: -- Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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ziprasidone (Geodon)
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Atypical antipsychotics
- highly non-selective - DA and 5-HT Interactions - Uses: -- Sometimes effective in patients who have not responded to typical antipsychotics, more efficacious in treating the negative symptoms of schizophrenia - Side effects -- EPS and endocrine symptoms of typicals less likely -- weight gain, associated with the development of type II diabetes -- Lengthening of the Q-T interval -- dizziness, palpitations and syncope |
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Benztropine (Cogentin)
Trihexyphenidyl (Artane) Diphenhydramine (Benadryl) |
All have antimuscarinic activity
- Used to treat EPS |
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Pemoline (Cylert)
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dopamimetic
- Treatment of ADHD and narcolepsy |
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Nicotine
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nicotinic ACh agonist
seriously, one should know this |
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Methanol
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The reason that I don't make my own moonshine
- Can be broken down by ADH into formaldehyde or formic acid, which are toxic - Treat with ethanol or fomepizole |
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Propranolol (Inderal)
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non-selective beta blocker
- To prevent sympathetic reaction in panic attack |
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Naloxone (Narcan)
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opioid inverse agonist
- used for treating overdose |
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Heroin
Codeine (Tylenol w/Codeine; Codate; Codephos; Codamol) Opium Morphine (MS Contin; Oramorph; Roxanol; Avinza) Oxycodone (Percocet; Percodan; Oxycontin) |
opiod agonists, drugs of abuse
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Ketamine
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anesthetics
we didn't talk about these...but they exist and are on the drug list |
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Phencyclidine (PCP)
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anesthetics
we didn't talk about these...but they exist and are on the drug list |
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Merperidine (Demerol)
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opiod agonists, drugs of abuse
fast-acting |
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Flunitrazepam (Rohypnol)
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anesthetics
we didn't talk about these...but they exist and are on the drug list |
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Gamma-Hydroxybutyrate (GHB)
|
anesthetics
we didn't talk about these...but they exist and are on the drug list |
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Donezepil (Aricept)
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acetylcholine esterase inhibitor
- AChE inhibitor - Uses: treatment of mild to moderate alzheimer's - Side effects: bradycardia, nausea, diarrhea, anorexia, abdominal pain - Don't use in those with CV counterindications or COPD |
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Memantine (Namenda)
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NDMA receptor antagonist
- NMDA antagonist, competes with Mg site - Believed to prevent excitotoxicity oof overstimulation by NMDA - Uses: treatment of moderate to severe Alzheimer's (+/- Donezepil) - Side effects: confusion, dizziness, drowsiness, headache, insomnia, agitation, and/or hallucinations. Less common adverse effects include vomiting, anxiety, hypertonia, cystitis, and increased libido |
