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72 Cards in this Set
- Front
- Back
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HAM side effects found in which drugs?
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(anti-Histamine, anti-Adrenergic, anti-Muscarinic)
Found in TCAs and low-potency antipsychotics |
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Serotonin Syndrome occurs when…
Tx? |
Occurs when there is too much serotonin, classically when SSRIs and MAOIs are combined
Tx: stop drugs |
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Hypertensive crisis caused by...
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Caused by a buildup of stored catecholamines, MAOIs plus foods with tyramine (red wine, cheese, chicken liver, cured meats) or plus sympathomimetics.
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Extrapyramidal side effects (EPS) occurs with...
Reversible? Time course? Choice of drug to Tx EPS produced by neuroleptics? |
Occurs with high-potency traditional antipsychotics (can be life threatening)
Yes, reversible Occurs within days of starting med Tx: Benztropine |
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Hyperprolactinemia occurs with...
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Occurs with high-potency traditional antipsychotics and risperidone
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Tardive Dyskinesia occurs with...
Reversible? |
Occurs after years of antipsychotic (particularly high-potency typical antipsychotics)
Can be irreversible |
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Neuroleptic Malignant Syndrome can be caused by…
Px? |
Can be caused by all antipsychotics after short or long time (increased risk with high-potency traditional antipsychotics)
Px: A medical emergency with 20% mortality rate |
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Examples of CYP450 Inducers (4)
Examples of CYP450 Inhibitors (5) |
-Smoking (1A2)
-Carbamazepine (1A2, 2C9, 3A4) -Barbiturates (2C9) -St. John's wort (2C19, 3A4) -Fluvoxamine (1A2, 2D6, 3A4) -Fluoxetine (2C19, 2C9, 2D6) -Paroxetine (2D6) -Duloxetine (2D6) -Sertraline (2C19) |
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_____ are known to exacerbate Alzheimer's disease
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Anticholinergics
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MoA of SSRIs
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Inhibit presynaptic serotonin pumps that take up serotonin -> increase availability of serotonin in synaptic clefts
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Examples of SSRIs (6)
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Fluoxetine (Prozac)
Sertraline (Zoloft) Paroxetine (Paxil) Fluvoxamine (Luvox) Citalopram (Celexa) Escitalopram (Lexapro) |
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Fluoxetine (Prozac)
- half-life compared to other SSRIs? - safety in pregnancy and kids? - SFX? - Drug interactions? |
- Longest half-life with active metabolites, so no need to taper. Weekly dosing available
- Safe in pregnancy, approved for use in children - More common sleep changes and anxiety - Can elevate levels of neuroleptics, leading to increased side effects |
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Sertraline (Zoloft)
- SFX? - Drug interactions? |
- Highest risk for GI disturbances, more common sleep changes
- Very few drug interactions |
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Paroxetine (Paxil)
- Drug interactions? - SFX? - Half-life compared to other SSRIs? |
- Highly protein bound --> several drug interactions
- More anticholinergic effects like sedation, constipation, weight gain - Short half-life --> withdrawal phenomena if not taken consistently |
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Fluvoxamine (Luvox)
- Current indications? - SFX? - Drug interactions? |
- Currently approved only for use in OCD
- Nausea and vomiting more common - Lots of drug interactions |
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Citalopram (Celexa)
- Drug interactions? - SFX? |
- Fewest drug-drug interactions
- Possibly fewer sexual side effects |
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Escitalopram (Lexapro)
- Structure? - Cost? |
- Levo-enantiomer of citalopram; similar efficacy, possibly fewer SFX
- More $$$ than citalopram |
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Side effects of SSRIs (7)
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- Sexual dysfunction: decreased interest, anorgasmia, delayed ejaculation; these typically do not resolve in a few weeks
- GI disturbance: nausea, diarrhea; giving with food helps - Insomnia: also vivid dreams; often resolves over time - HA - Anorexia, weight loss - Restlessness: an akathisia-like state at initiation and termination of SSRIs - Seizures: 0.2%, slightly lower than TCAs --serotonin syndrome |
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FDA black box warning on SSRIs for...
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… "increased suicidal thinking and behavior."
This is most documented in children and adolescents, but may be accurate for adults as well. |
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SSRIs should not be used for at least ___ before or after use of an ____.
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2 weeks, MAOI
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Serotonin syndrome can be caused by SSRI + ____
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triptans, dextromorphan
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Examples of SNRIs (serotonin-NE reuptake inhibitors) (2)
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Venlafaxine (Effexor)
Duloxetine (Cymbalta) |
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Venlafaxine (Effexor)
- Indications? - Drug interations? - Dosing options? - SFX? - New form? |
-Used in depression, anxiety d/o's (like GAD), and may have some use in ADHD
-Low drug interaction potential -Extended-release (XR form) allows once-daily dosing -SE profiles similar to SSRIs; can increase BP (don't use in pts with untx or labile bp) -New form, desvenlafaxine (Pristiq), is the active metabolite of venlafaxine and is $$$ |
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Duloxetine (Cymbalta)
- Indications? - SFX? - Cost? |
-Used for depression and neuropathic pain or in fibromyalgia
-SFX similar to SSRIs, but more dry mouth and constipation relating to its norepinephrine effects, may be more liver SFX's in pts with liver disease or heavy alcohol use -Expensive |
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Bupropion (Wellbutrin)
- Drug class? - SFX? - Indications? - Contraindications? |
- Norepinephrine-Dopamine Reuptake Inhibitors
- Relative lack of sexual side effects compared to SSRIs, increased risk of seizures (lowers seizure threshold) and psychosis at high doses and increased anxiety in some - Some efficacy in treatment of adult ADHD - Contraindicated in patients with seizure or active eating disorders and in those currently on an MAOI |
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Trazodone (Desyrel) and Nefazodone (Serzone)
- Drug class? - Indications? - SFX? - Black box warning? |
- Serotonin Receptor Antagonists and Agonists
- Useful in treatment of refractory major depression, major depression with anxiety, and insomnia (d/t its sedative effects) - No sexual side effects and does not affect REM sleep; nausea, dizziness, orthostatic hypotension, cardiac arrhythmias, sedation, and priapism (esp. with "trazoBONE") - Nefazodone carries black box warning for rare but serious liver failure |
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Mirtazapine (Remeron)
- Drug class? - Indications? - SFX? |
- Alpha2-Adrenergic Receptor Antagonists
- Useful in the treatment of refractory major depression, esp. in pts who need to gain weight (elderly) -SFX include sedation, weight gain, dizziness, somnolence, tremor, dry mouth, constipation, and rare agranulocytosis; no sexual SFX and few drug interactions |
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Examples of Tricyclic Antidepressants (6)
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Tertiary Amines (highly anticholinergic, more sedating, greater lethality in OD)
-Amitriptyline (Elavil) -Imipramine (Tofranil) -Clomipramine (Anafranil) -Doxepin (Sinequan) Secondary amines (metabolites of tertiary amines; less anticholinergic, less sedating) -Nortriptyline (Pamelor, Aventyl): Least likely to cause orthostatic hypotension; Useful therapeutic blood levels and in treating chronic pain -Desipramine (Norpramin): More activating; least sedating; least anticholinergic |
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ok
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Tertiary Amines (highly anticholinergic, more sedating, greater lethality in overdose)
-Amitriptyline (Elavil): Useful in chronic pain, migraines, and insomnia -Imipramine (Tofranil): Has IM form; Useful in enuresis and panic disorder -Clomipramine (Anafranil): Most serotonin specific, useful in tx of OCD -Doxepin (Sinequan): Useful in tx chronic pain; Emerging use as a sleep aid in low doses Secondary Amines (metabolites of tertiary amines; less anticholinergic, less sedating) -Nortriptyline (Pamelor, Aventyl): Least likely to cause orthostatic hypotension; Useful therapeutic blood levels and in treating chronic pain -Desipramine (Norpramin): More activating; least sedating; least anticholinergic |
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Tetracyclic Antidepressants
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Amoxapine (Ascendin)
-Metabolite of antipsychotic loxapine -May cause EPS and has similar SE profile to typical antipsychotics Maprotiline (Ludiomil) -Higher rates of seizure, arrhythmia, and fatality on overdose |
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Mainstay of treatment for TCA overdose?
Major complications of TCAs MAOIs are considered more effective in ... Selegiline (EMSAM patch) |
IV sodium bicarbonate
3 Cs -Cardiotoxicity -Convulsions -Coma Atypical depression characterized by hypersomnia, increased appetite, and increased sensitivity to interpersonal rejection an MAOI used to treat depression that does not require following the dietary restrictions when used in low dosages. However, decongestants, opiates (Demerol), and serotonergic drugs must still be avoided. |
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Side Effects of TCAs
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-TCAs are highly protein-bound and lipid soluble -> can interact with other medications that have high protein binding
-SE mostly due to their lack of specificity and interaction with other receptors -Anti-Histaminic: sedation -Anti-Adrenergic: (cardiovascular side effects): orthostatic hypotension, dizziness, reflex tachy, arrhythmias, ECG changes (widening QRS, QT, and PR intervals); avoid in pts with preexisting conduction abnl or recent MI -Anti-Muscarinic: dry mouth, constipation, urinary retention, blurred vision, tachy, exacerbation of narrow angle glaucoma -Weight gain -Lethal in overdose - must assess suicide risk! Agitation, tremors, ataxia, delirium, hypoventilation from CNS depression, myoclonus, hyperreflexia, seizures, ad coma are signs -Seizures: 0.3%, more common at higher plasma levels and with clomipramine and tetracyclines -Serotonergic effects: Erectile/ejaculatory dysfunction in males, anorgasmia in females |
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mechanism of action and use of MAOIs
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-Prevent the inactivation of biogenic amines such as NE, serotonin, dopamine, and tyramine (an intermediate in the conversion of tyrosine -> NE)
-By irreversibly inhibiting the enzymes MAO-A and MAO-B. MAOIs increase the # of neurotransmitters available in synapses -MAO-A preferentially deactivates serotonin, MAO-B preferentially deactivates NE/epi; BOTH act on dopamine and tyramine -Not used as first-line agents bc of increased safety and tolerability of newer agents, but still considered very effective for certain types of refractory depression and in refractory panic/anxiety disorder -Phenelzine (Nardil) -Tranylcypromine (Parnate) -Isocarboxazid (Marplan) |
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Side Effects of MAOIs
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-Serotonin Syndrome (wait at least 2 weeks before switching from SSRI to MAOI, and at least 5-6 weeks with fluoxetine
-Hypertensive Crisis: MAOIs with tyramine-rich foods (red wine, cheese, chicken liver, fava beans, cured meats cause a buildup of stored catecholamines) or sympathomimetics -Orthostatic hypotension (most common) -Drowsiness, weight gain, sexual dysfunction, dry mouth, sleep dysfunction -People with pyridoxine deficiency can have paresthesias, treated with B6 -Rarely liver toxicity, seizures, and edema -Start slow and go slow! |
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Antidepressant use in:
OCD Panic Disorder Eating Disorders Dysthymia Social Phobia GAD PTSD IBS Enuresis Neuropathic Pain Chronic Pain Fibromyalgia Migraine Headaches Smoking Cessation Premenstrual Dysphoric Disorder Depressive Phase of Manic Depression Insomnia |
OCD: SSRIs in high doses, TCAs (clomipramine)
Panic Disorder: SSRIs, TCAs (imipramine), MAOIs Eating Disorders: SSRIs in high doses, TCAs, MAOIs Dysthymia: SSRIs Social Phobia: SSRIs, TCAs, and MAOIs GAD: SSRIs, SNIRs (venlafaxine), TCAs PTSD: SSRIs IBS: SSRIs, TCAs Enuresis: TCAs (imipramine) Neuropathic Pain: TCAs (amitriptyline and nortriptyline), duloxetine Chronic Pain: SSRIs, TCAs Fibromyalgia: SSRIs Migraine Headaches: TCAs (amitriptyline), SSRIs Smoking Cessation: Bupropion Premenstrual Dysphoric Disorder: SSRIs Depressive Phase of Manic Depression: SSRIs Insomnia: Mirtazapine, TCAs (amitriptyline) |
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When suspecting serotonin syndrome?
A patient on clozapine should have routine... When prescribing Lithium, it is important to monitor... |
Discontinue medication. Can try calcium channel blockers (oral nifedipine). If carefully monitored, can try chlorpromazine or phentolamine.
routine WBC counts and absolute neutrophil count to monitor for agranulocytosis. These WBC counts should be performed weekly for the first 6 months of treatment and can decrease in frequency thereafter. Lithium levels, creatinine, and thyroid levels. |
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Antipsychotics
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-Typical or first generation antipsychotics aka neuroleptics are classified according to potency and treat psychosis by blocking dopamine (D2) receptors.
-Atypical or second-generation block both dopamine (D2) and serotonin (2A) receptors. -Both have similar efficacies in treating positive psychotic symptoms. Second generation better in treating negative symptoms. |
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Low-Potency Typical Antipsychotics
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-Have a lower affinity for dopamine receptors and therefore a higher dose is required.
-Higher incidence of anticholinergic and antihistaminic side effects than high-potency traditional antipsychotics. -Lower incidence of EPS and neuroleptic malignant syndrome. -More lethality in overdose due to QTc prolongation and the potential for heart block and ventricular tachycardia. -Rare risk of agranulocytosis, and slightly higher seizure risk than higher-potency medications. -Chlorpromazine (Thorazine): Commonly causes orthostatic hypotension; can cause bluish skin discoloration; can -> photosensitivity; can treat n/v and intractable hiccups -Thoridazine (Mellaril): Associated with retinitis pigmentosa |
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Midpotency Typical Antipsychotics
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Have midrange properties
-Loxapine (Loxitane): Higher risk of seizure; metabolite is an antidepressant -Thiothixene (Navane): Can cause ocular pigment changes -Trifluoperazine (Stelazine): Can reduce anxiety -Perphenazine (Trilafon) |
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High-Potency Typical Antipsychotics
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-Have greater affinity for dopamine receptors, and therefore a relatively low dose is needed to achieve effect.
-Cause less sedation, orthostatic hypotension, and anticholinergic effects -Greater risk for EPS and tardive dyskinesia -Haloperidol (Haldol): Decanoate form available (long-acting IM form) -Fluphenazine (Prolixin): Decanoate form available -Pimozide (Orap): Associated with heart block, ventricular tachycardia, and other cardiac effects |
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The positive sxs of schizphrenia are thought to be treated by...
The negative sxs of schizphrenia are thought to occur due to... EPS are thought to occur through... Increased prolactin is related to dopamine in the ____ area. |
the action of medications in the mesolimbic dopamine pathway. The mesolimbic pathway includes the nucleus accumbens, the fornix, the amygdala, and the hippocampus.
dopamine action in the mesocortical pathway. the dopamine pathways in the nigrostriatum. tuberoinfundibular |
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Side Effects of Typical Antipsychotics
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-Antidopaminergic effects:
--EPS: Parkinsonism, akathisia, dystonia --Hyperprolactinemia-> decreased libido, galactorrhea, gynecomastia, impotence, amenorrhea, osteoporosis -Anti-HAM effects -Tardive dyskinesia: choreoathetoid movements in pts who have used neuroleptics >6 mo; most often in older women; 50% remit spontaneously, many cases permanent -Neuroleptic malignant syndrome: most commonly in young males early in treatment with both atypical and typical antipsychotics -Elevated liver enzymes, jaundice -Ophthalmologic problems (irreversible retinal pigmentation with high doses of thioridazine, deposits in lens and cornea with chlorpromazine) -Dermatologic problems including rashes and photosensitivity (blue-gray skin discoloration with chlorpromazine) -Seizures: antipsychotics lower seizure thresholds; low-potency more likely |
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Treatment of EPS
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Reducing the dose of the antipsychotic and administering an anticholinergic medication such as benztropine (Cogentin), an antihistaminergic medication such as diphenhydramine, or an antiparkinsonian medication such as amantadine (Symmetrel)
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NMS is characterized by:
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FALTERED
Fever: most common presenting symptom Autonomic instability: tachy, labile HTN, diaphoresis Leukocytosis Tremor Elevated CPK Rigidity Excessive sweating: diaphoresis Delirium Not an allergic reaction; patient is not prevented from restarting the same neuroleptic at a later time |
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Onset of Neuroleptic Side Effects
30% of treatment resistant psychosis will respond to: |
-Acute dystonia: hours to days
-EPS/Akathisia: days to months -TD: months to years Abnormal Involuntary Movement Scale (AIMS) can be used to quantify and monitor for tardive dyskinesia. Clozapine (Clozaril) |
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About atypical antipsychotics
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-Less likely to cause EPS, tardive dyskinesia,or NMS
-May be more effective at tx negative sx of schizophrenia -Also used to treat acute mania, bipolar disorder, and as adjunctive medication in unipolar depression -Clozapine (Clozaril) -Risperidone (Risperdal) -Quetiapine (Seroquel) -Olanzapine (Zyprexa) -Ziprasidone (Geodon) -Aripiprazole (Abilify) -Paliperidone (Invega) -Asenapine (Saphris) -Iloperidone (Fanapt) |
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Clozapine (Clozaril)
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-Less likely to cause TD
-Only antipsychotic shown to be more efficacious -Associated with tachycardia and hypersalivation -More anticholinergic side effects than other atypical or high-potency typicals -Myocarditis can develop -1-2% incidence of agranulocytosis and 2-5% incidence of seizures -Must stop if the ANC drops < 1500/uL -Only antipsychotic shown to decrease the risk of suicide |
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-Risperidone (Risperdal)
-Quetiapine (Seroquel) -Olanzapine (Zyprexa) -Ziprasidone (Geodon) -Aripiprazole (Abilify) |
Risperidone (Risperdal):
-Can cause increased prolactin, some orthostatic hypotension, and reflex tachycardia -Has long-acting injectable form called Consta Quetiapine (Seroquel): Common SE include sedation and orthostatic hypotension Olanzapine (Zyprexa): SE weight gain Ziprasidone (Geodon): Less likely to cause weight gain Aripiprazole (Abilify): -Unique mechanism of partial D2 agonism -Can be more activating (akathisia) and less sedating; less potential for weight gain |
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-Paliperidone (Invega)
-Asenapine (Saphris) -Iloperidone (Fanapt) |
Newer. expensive medications
-Paliperidone (Invega): metabolite of risperidone; long-acting injectable form (Sustenna) -Asenapine (Saphris) -Iloperidone (Fanapt) |
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FDA approved to treat mania
Only mood stabilizer shown to decrease suicidality? Blood levels useful for which mood stabilizers? |
Quetiapine, Olanzapine, Aripiprazole, Risperidone, and Ziprasidone
Lithium Lithium, valproic acid, carbamazepine, clozapine |
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Side Effects of Atypical Antipsychotics
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-Metabolic syndrome: must be monitored with baseline weight, waist circumference (measured at iliac crest), blood pressure, fasting glucose, and fasting lipids (triglycerides)
-some anti-HAM -weight gain -hyperlipidemia -hyperglycemia - rarely, DKA -liver function - monitor yearly for elevated LFTs and ammonia -QTc prolongation |
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About Mood Stabilizers
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-Treat acute mania and help prevent relapses of manic episodes in bipolar disorder and schizoaffective disorder. Less commonly may be used for:
-Potentiation of antidepressants in patients with major depression refractory to monotherapy -Potentiation of antipsychotics in patients with schizophrenia -Enhancement of abstinence in treatment of alcoholism -Treatment of aggression and impulsivity (dementia, intoxication, mental retardation, personality disorders, general medical conditions) -Mood stabilizers include lithium and anticonvulsants. most commonly valproic acid, lamotrigine, and carbamazepine |
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Lithium
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-Drug of choice in acute mania and as prophylaxis for both manic and depressive episodes of bipolar and schizoaffective disorders.
-Also used in cyclothymia and unipolar depression -Metabolized by the kidney, therefore adjust dose and monitor levels closely if pt has renal dysfnc -Prior to initiating, patients should have an ECG, basic chemistries, thyroid function tests, a CBC, and pregnancy test -Onset of action 5-7 days -Blood levels correlate with clinical efficacy and should be checked after 5 days, then every 2-3 days until therapeutic -Major drawback: high incidence of side effects and very narrow therapeutic index: 0.6-1.2; toxic > 1.5; lethal >2.0 |
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Factors that affect Lithium levels
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-NSAIDs (decrease)
-Aspirin -Dehydration (increase) -Salt deprivation (increase) -Sweating (salt loss) (increase) -Impaired renal function (increase) -Diuretics, especially thiazides |
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Side Effects of Lithium
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-Toxic levels cause altered mental status, coarse tremors, convulsions, and death
-Need to regularly monitor blood levels of lithium, TSH, and kidney function -Fine tremor -Nephrogenic DI -GI disturbance -Weight gain -Sedation -Thyroid enlargement, hypothyroidism -ECG changes -Benign leukocytosis (can sometimes be advantageous when combined with other meds that decrease WBC (clozapine)) -Ebstein's anomaly: cardiac defect in babies |
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Carbamazepine (Tegretol)
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-Anticonvulsant
-Especially useful in treating mixed episodes and rapid-cycling bipolar disorder, and less effective for the depressed phase -Also used in management of trigeminal neuralgia -Acts by blocking sodium channels and inhibiting action potentials -Onset of action 5-7 days -CBC and LFTs must be obtained before initiating treatment and monitored regularly |
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Side effects of Carbamazepine?
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-Most common are GI and CNS (drowsiness, ataxia, sedation, confusion)
-Possible skin rash (Stevens-Johnson Syndrome) -Leukopenia, hyponatremia, aplastic anemia, thrombocytopenia, and agranulocytosis -Elevation of LFTs, causing hepatitis -Teratogenic effects (neural tube defects) -Significant drug interactions with many drugs metabolized by CYP450 pathway, including inducing its own metabolism through autoinduction, requiring increasing dosages -Toxicity: confusion, stupor, motor restlessness, ataxia, tremor, nystagmus, twitching, and vomiting |
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Valproic Acid (Depakote and Depakene)
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-Anticonvulsant
-Useful in treating mixed episodes of bipolar disorder as well as rapid cycling -Opens chloride channels -Monitoring LFTs and CBC necessary -Drug levels are usually checked after 3- days. Normal range: 50-150 ug/mL |
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Lamotrigine (Lamictal)
Oxcarbazepine (Trileptal) |
-Anticonvulsant
-Efficacy for bipolar depression, though little efficacy for acute mania or prevention of mania -Works on sodium channels that modulate glutamate and aspartate -Most common SE: dizziness, sedation, headaches, and ataxia -Most serious SE: Stevens-Johnson syndrome in 10%; most likely in the first 4-6 weeks, but minimized by starting with low doses and increasing them slowly -Valproate will increase lamotrigine levels and lamotrigine will decrease valproate levels Oxcarbazepine (Trileptal) -Anticonvulsant; As effective in mood d/o as carbamazepine, but better tolerated; less risk of rash and hepatic toxicity |
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Gabapentin (Neurontin)
Pregabalin (Lyrica) Tiagabine (Gabitril) Topiramate (Topomax) |
All Anticonvulsants
Gabapentin (Neurontin) -Often used adjunctively to help with anxiety, sleep; Little efficacy in bipolar disorder Pregabalin (Lyrica) -Used in GAD and fibromyalgia; Little efficacy in bipolar disorder Tiagabine (Gabitril): may be helpful with anxiety Topiramate (Topomax) -Helpful with impulse control disorder and anxiety; Beneficial SE of weight loss; Can cause hypochloremic, non-anion gap metabolic acidosis and kidney stones; most limiting SE is cognitive slowing |
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Side Effects of anticonvulsants
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GI side effects
weight gain sedation alopecia pancreatitis hepatotoxicity or benign aminotransferase elevations increased ammonia thrombocytopenia teratogenic effects during pregnancy (neural tube defects) |
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Anxiolytics include:
Common indications for anxiolytics/hypnotics: |
benzodiazepines, barbiturates, and buspirone
anxiety disorders muscle spasm seizures sleep disorders alcohol withdrawal anesthesia induction |
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general information about Benzodiazepines (BDZs)
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-work by potentiating the effects of GABA
-reduce anxiety -many become dependent on these mediations and require increasing amounts for the same clinical effect -potential for abuse -choice of benzo is based on time to onset of action, duration of action, and method of metabolism -relatively safer in overdose than barbiturates -can be lethal when mixed with alcohol; respiratory depression causes death |
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Long Acting Benzos
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-half-life > 20 hours
-Diazepam (Valium) --rapid onset --used during detoxification from alcohol of sedative-hypnotic-axiolytics and for seizures --less commonly prescribed to treat anxiety than previously -Clonazepam (Klonopin) --Treatment of anxiety, including panic attacks --avoid with renal dysfunction --longer half-life allows for once daily dosing |
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Intermediate Acting Benzos
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-Half-life 6-20 hours
-Alprazolam (Xanax) --treatment of anxiety, including panic attacks; short onset of action -> euphoria, high abuse potential -Lorazepam (Ativan) --Treatment of panic attacks, alcohol and sedative-hypnotic-anxiolytic detoxification, agitation; not metabolized by liver -Oxazepam (Serax) --Alcohol and sedative-hypnotic-anxiolytic detoxification; not metabolized by liver -Temazepam (Restoril) --Decreasingly used for treatment of insomnia; primarily used in medical and surgical settings -Midazolam (Versed) --Primarily used in medical and surgical settings |
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Side effects of anxiolytics/hypnotics
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drowsiness
impairment of intellectual function reduced motor coordination (careful in elderly) anterograde amnesia withdrawal can be life threatening and causes seizures toxicity: respiratory depression in overdose, especially when combined with acohol |
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Non-Benzodiazepine Hypnotics
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Zolpidem (Ambien) / Zaleplon (Sonata) / Eszopiclone (Lunesta): Work by selective receptor binding to benzo receptor I, which is responsible for sedation
-used for short-term treatment of insomnia; less tolerance/dependence occurs with prolonged use (but can still occur) -Zaleplon has shorter half-life than zolpidem which has a shorter half-life than eszopiclone -reports of anterograde amnesia, hallucinations, sleepwalking, and other behaviors may limit tolerability, as well as the more common GI SE Diphenhydramine (Benadryl): antihistamine; SE include sedation, dry mouth, constipation, urinary retention, blurry vision Chloral hydrate (Noctec, Somnote): Not commonly prescribed due to tolerance and dependence; Lethal in overdose, causing hepatic and liver failure Ramelteon (Rozerem): Selective melatonin MT1 and MT2 agonst; No tolerance or dependence |
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Buspirone (BuSpar)
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-Non-Benzodiazepine Anxiolytics: anxiolytic action is at 5HT-1A receptor (partial agonist)
-has slower onset of action than BDZ (takes 1-2 weeks for effect) -not considered as effective as other options, and so it is often used in combination with another agent (eg. SSRI) for treatment of anxiety -does not potentiate the CNS depression of alcohol (useful in alcoholics), and has a low potential for abuse/addiction |
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Hydroxyzine (Atarax)
Barbiturates Propranolol |
-Non-Benzodiazepine Anxiolytics
-an antihistamine -SE include sedation, dry mouth, constipation, urinary retention and blurry vision -useful for pts who want quick-acting, short-term medication, but who cannot take benzos for various reasons eg. butalbitol, phenobarbitol, amobarbitol, pentobarbitol; rarely used now bc of lethality of OD and SE profile BB; useful in tx autonomic effects of panic attacks or performance anxiety, such as palpitations, sweating, and tachycardia; can also be used to treat akathisia (SE of typical antipsychotic) |
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Psychostimulants
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Used in ADHD and refractory depression
-Dextroamphetamine and amphetamines (Dexedrine, Adderall): Dextroamphetamine is the D-isomer of amphetamine; Adderall is Schedule II, which means Rx is triplicate and high potential for abuse; monitor bp and watch for weight loss, insomnia -Methylphenidate (Ritalin, Concerta): CNS stimulant, similar to amphetamine; Schedule II; watch for leukopenia, anemia, increased LFTs (monitor labs); monitor bp and watch for weight loss, insomnia -Atomoxetine (Strattera): Presynaptic NE transporter inhibitor; less appetite suppression and insomnia; rare liver toxicity, possible increased suicidal ideation in children/adolescents -Modafanil (Provigil): used in narcolepsy |
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Acetylcholinesterase Inhibitors
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Donepezil (Aricept)
-once daily dosing -some GI effects -mild to moderate dememtia Galantamine (Reminyl) Rivastigmine (Excelon): has a patch, less SE Tacrine (Cognex) Memantine (Namenda): Moderate to severe dementia; Better together with acetylcholinesterase inhibitor |
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Possible psychiatric symptoms caused by:
Procainamide, quinidine Albuterol Isoniazid Tetracycline Nifedipine, verapamil Cimetidine Steroids |
Procainamide, quinidine: confusion, delirium
Albuterol: anxiety, confusion Isoniazid: psychosis Tetracycline: depression Nifedipine, verapamil: depression Cimetidine: depression, psychosis Steroids: aggressiveness/agitation, hypomania, anxiety, psychosis |
