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368 Cards in this Set
- Front
- Back
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What are the "HAM" side effects? What drugs cause these? |
- anti-Histamine (sedation, weight gain) - anti-Adrenergic (hypotension) - anti-Muscarinic (dry mouth, blurred vision, urinary retention)
- Caused by TCAs (eg, amitriptyline) and low-potency anti-psychotics (eg, chlorpromazine) |
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What side effects are associated with TCAs? |
"HAM" side effects: - anti-Histamine (sedation, weight gain) - anti-Adrenergic (hypotension) - anti-Muscarinic (dry mouth, blurred vision, urinary retention) |
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What side effects are associated with low-potency antipsychotics (eg, chlorpromazine)? |
"HAM" side effects: - anti-Histamine (sedation, weight gain) - anti-Adrenergic (hypotension) - anti-Muscarinic (dry mouth, blurred vision, urinary retention) |
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What symptoms are associated with "serotonin syndrome"? What drugs cause this? |
"HARM": - Hyperthermia - Autonomic instability (delirium) - Rigidity - Myoclonus
- Confusion - Flushing - Diaphoresis - Tremor - Myoclonic jerks - Hyperthermia - Hypertonicity - Rhabdomyolysis - Renal failure - Death
Occurs when there is too much serotonin, classically when SSRIs and MAOIs are combined
Treatment: stop drugs |
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What side effects can classically occur when SSRIs and MAOIs are combined? |
Serotonin Syndrome:
"HARM": - Hyperthermia - Autonomic instability (delirium) - Rigidity - Myoclonus
- Confusion - Flushing - Diaphoresis - Tremor - Myoclonic jerks - Hyperthermia - Hypertonicity - Rhabdomyolysis - Renal failure - Death
Treatment: stop drugs |
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What are the symptoms in a hypertensive crisis? What drugs can cause this? |
- Caused by taking MAOIs and eating foods with tyramine (red wine, cheese, chicken liver, cured meats) or MAOIs with sympathomimetics - Caused by a buildup of stored catecholamines
- Chest pain - Arrhythmias - Headache - Epistaxis - Dyspnea - Faintness or vertigo - Severe anxiety - Agitation - Altered mental status - Paresthesias - Vomiting |
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What side effects can occur if you take MAOIs and eat foods high in tyramine or take MAOIs with a sympathomimetic? |
Hypertensive Crisis: - Chest pain - Arrhythmias - Headache - Epistaxis - Dyspnea - Faintness or vertigo - Severe anxiety - Agitation - Altered mental status - Paresthesias - Vomiting |
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What are the extra-pyramidal side effects? What drugs can cause this? |
- Parkinsonism: mask-like face, cogwheel rigidity, pill-rolling tremor - Akathisia: restlessness and agitation - Dystonia: sustained contraction of muscles of neck, tongue, eyes, diaphragm
- Occurs with high-potency traditional anti-psychotics (eg, haloperidol, fluphenazine); occurs within days of starting med - Reversible; can be life-threatening |
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What medication can be used to treat extra-pyramidal side effects produced by neuroleptics? |
Benztropine --> antagonizes ACh and Histamine receptors |
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What are the symptoms of hyperprolactinemia? What drugs can cause this? |
- Galactorrhea - Amenorrhea / infertility
- Occurs with high-potency traditional anti-psychotics (haloperidol, fluphenazine) and risperidone |
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What are the symptoms of Tardive Dyskinesia? What drugs cause this?
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- Choreoathetoid muscle movements, usually of mouth and tongue
- Caused by years of anti-psychotic use (particularly high-potency typical antipsychotics) - Can be irreversible |
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What symptoms occur with Neuroleptic Malignant Syndrome? What drugs can cause this? |
- Fever - Tachycardia - Hypertension - Tremor - Elevated creatine phophokinase (CPK) - "Lead pipe" rigidity - Medical emergency with 20% mortality rate
- Can be caused by all anti-psychotics after a short or long time (inreased with high-potency, traditional antipsychotics)
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What side effects can high-potency traditional anti-psychotics cause? |
Extrapyramidal Side Effects (EPS) - Parkinsonism: mask-like face, cogwheel rigidity, pill-rolling tremor - Akathisia: restlessness and agitation - Dystonia: sustained contraction of muscles of neck, tongue, eyes, diaphragm - Can be life threatening: dystonia of the diaphragm causing asphyxiation - Occurs within days of starting the med
Hyperprolactinemia: - Galactorrhea - Amenorrhea / infertility
Tardive Dyskinesia: - Choreoathetoid muscle movements, usually of mouth and tongue - Occurs after years of use; can be irreversible
Neuroleptic Malignant Syndrome: - Fever, tachycardia, hypertension, tremor, elevated CPK, "lead pipe" rigidity - Medical emergency with 20% mortality rate |
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What psychiatric medications induce CYP450? Implications? |
- Smoking (1A2) - Carbamazepine (1A2, 2C9, 3A4) - Barbiturates (2C9) - St. John's Wort (3C19, 3A4)
Inducers --> make the system metabolize faster --> drug levels decrease |
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What psychiatric medications inhibit CYP450? Implications? |
- Fluvoxamine (1A2, 2D6, 3A4) - Fluoxetine (2C19, 2C9, 2D6) - Paroxetine (2D6) - Duloxetine (2D6) - Sertraline (2C19)
Inhibitors --> make the system metabolize slower --> drug levels increase |
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What are the common cytochrome P450 enzymes that are important in metabolizing psychiatric drugs? |
- CYP3A4 - CYP2D6 - CYP1A2 - CYP2C9 - CYP2C19 |
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What are the types of "kinesias" (impairments of body function)? |
- Tardive dyskinesia - Acute dystonia - Akathisia - Bradykinesia |
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What is the term for grimacing and tongue protrusion? |
Tardive dyskinesia |
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What is the term for twisting and abnormal postures? |
Acute dystonia |
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What is the term for inability to sit still? |
Akathisia |
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What is the term for decreased or slow body movements? |
Bradykinesia |
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What are common side effects of anti-cholinergic meds? |
Constipation |
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What class of medications can exacerbate Alzheimer disease? |
Anti-cholinergics |
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What are the major categories of anti-depressants? |
- SSRIs - TCAs - MAOIs - Miscellaneous |
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Which type of antidepressants is best? |
They are all equally effective in treating major depression, but differ in side effect and safety profiles |
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How often do patients respond to antidepressants? |
70% have a response 30% of this is placebo effect |
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How long does it take for antidepressants to work? |
Most require a trial of 3-4 weeks minimum to determine if there is an effect
Some patients require 1-2 weeks and some 6-8 weeks to notice an effect |
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What withdrawal is associated with discontinuing antidepressants? How can you limit this? |
- Dizziness - Headaches - Nausea - Insomnia - Malaise
- Depending on the dose and half-life, may need to be tapered |
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What are the most common agents used to treat major depression? |
SSRIs |
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How should you determine which antidepressant to start someone on? |
- Patient's symptoms - Prevoius treatment responses by the patient or a family member to a particular drug - Comorbid conditions - Risk of suicide - Cost |
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What is the mechanism of SSRIs? |
Inhibit pre-synaptic serotonin pumps that take up serotonin --> increased availability of serotonin in synaptic clefts
(mechanism may be more complex) |
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What causes the difference in efficacy and side effects with different SSRIs? |
Minimal structural differences |
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What are the advantages of SSRIs? |
- Low incidence of side effects, most of which resolve with time - No food restrictions - Much safer in overdose |
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What are examples of SSRIs? |
- Fluoxetine (Prozac) - Sertraline (Zoloft) - Paroxetine (Paxil) - Fluvoxamine (Luvox) - Citalopram (Celexa) - Escitalopram (Lexapro) |
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What is the trade name of Fluoxetine? Half-life? Safety? Side effects? |
Prozac (SSRI) - Longest half-life with active metabolites, therefore, no need to taper - 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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What is the trade name of Sertraline? Safety? Side effects? |
Zoloft (SSRI) - Highest risk for GI side effects - Very few drug interactions - More common sleep changes |
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What is the trade name of Paroxetine? Half-life? Safety? Side effects? |
Paxil (SSRI) - Short half-life leading to withdrawal phenomena if not taken consistently - More anti-cholinergic effects like sedation, constipation, weight gain - Highly protein bound --> several drug interactions |
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What is the trade name of Fluvoxamine? Use? Side effects? |
Luvox (SSRI) - Only approved for OCD - Nausea and vomiting more common - Lots of drug interactions |
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What is the trade name of Citalopram? Safety? Side effects? |
Celexa (SSRI) - Fewest drug-drug interactions - Possibly fewer sexual side effects |
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What is the trade name of Escitalopram? Safety? Side effects? |
Lexapro (SSRI) - Levo-enantiomer of citalopram; similar efficacy but possibly fewer side effects - More expensive |
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What drugs taken with SSRIs can increase the risk for serotonin syndrome? |
- OTC cold remedies (eg, cough medicine) - MAOIs - Triptans |
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How can you treat the sexual side effects of SSRIs? |
- Augment regimen with bupropion (wellbutrin) - Change to a non-SSRI antidepressant - Add medications like sildenafil for men |
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What is the black box warning against SSRIs? |
Increased suicidal thinking and behavior - Most common in children and adolescents, but may be accurate for adults as well |
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Why do SSRIs have fewer side effects than TCAs and MAOIs? |
They are serotonin selective (they do not act on histamine, adrenergic, or muscarinic receptors) |
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What causes most of the SSRI side effects? |
Extensive number of serotonin receptors throughout the body, including the GI tract |
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What are the side effects of SSRIs? |
- Sexual dysfunction (25-30%) - GI disturbance - Insomnia - Headache - Anorexia, weight loss - Restlessness - Seizures - Serotonin syndrome - Black-box warning: increased suicidal thinking and behavior |
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How common are sexual side effects with SSRIs? How does this affect the patient? |
- 25-30% are affected - Decreases interest in sex, anorgasmia, delayed ejaculation - Typically does not resolve in a few weeks |
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What are the GI side effects of SSRIs? How can you limit this? |
- Mostly nausea and diarrhea - Giving with food can help |
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What are the sleep symptoms related to taking SSRIs? |
- Insomnia - Vivid dreams - Often resolve over time |
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How do SSRIs affect weight? |
Often leads to anorexia and weight loss |
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What symptom has been reported at initiation and termination of SSRIs? |
Restlessness |
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How common are seizures in patients taking SSRIs? How does this compare to other antidepressants? |
0.2%, slightly lower than TCAs |
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A patient on SSRIs who has fever, diaphoresis, shivering, tachycardia, hypertension, delirium, and neuromuscular excitability (especially hyperreflexia and "electric jolt" limb movements) has what going on? |
Serotonin Syndrome |
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If you are switching a patient from MAOIs to SSRIs or vice versa, what do you need to be mindful of? |
Need at least 2 weeks of separation to prevent serotonin syndrome |
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Which SSRI has a long half-life? Implications? |
Fluoxetine (Prozac) - no need to taper when stopping |
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Which SSRI has a short half-life? Implications? |
Paroxetine (Paxil) - may cause withdrawal phenomena if not taken consistently |
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Which SSRI can increase levels of neuroleptics, leading to increased side effects? |
Fluoxetine (Prozac) |
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Which SSRI is safe in pregnancy and children? |
Fluoxetine (Prozac) |
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Which SSRI has the highest risk for GI disturbances? |
Sertraline (Zoloft) |
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Which SSRI has a high incidence of anti-cholinergic effects (sedation, constipation, weight gain)? |
Paroxetine (Paxil) |
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Which SSRI is only approved for OCD? |
Fluvoxamine (Luvox) |
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SSRIs can affect levels of what medication, requiring increased monitoring when starting and stopping SSRIs? |
Warfarin |
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What are the types of SNRIs (serotonin-norepinephrine reuptake inhibitors)? |
- Venlafaxine (Effexor) - Desvenlafaxine (Pristiq) - Duloxetine (Cymbalta) |
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What is the trade name of Venlafaxine? Uses? Side effects? |
Effexor (SNRI) - Depression, anxiety (GAD), ADHD - Low drug interaction potential - Side effects similar to SSRIs - Can increase BP; should not be used in patients with untreated HTN or labile BP |
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What is the trade name Desvenlafaxine? Type? |
Pristiq (SNRI) - New form, active metabolite of venlafaxine - Expensive |
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What is the trade name of Duloxetine? Uses? Side effects? |
Cymbalta (SNRI) - Used for depression with neuropathic pain or in fibromyalgia - Side effects similar to SSRIs, but more dry mouth and constipation (due to NE effects) - May be more liver side effects in patients with liver disease or heavy alcohol use - Expensive! |
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What antidepressant is also used for GAD and possibly ADHD? |
Venlafaxine (Effexor) - SNRI |
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What antidepressant is used for depression and neuropathic pain or fibromyalgia? |
Duloxetine (Cymbalta) - SNRI |
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What antidepressant can cause liver side effects (especially in patients with liver disease or heavy alcohol use)? |
Duloxetine (Cymbalta) - SNRI |
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What antidepressant is a norepinephrine-dopamine reuptake inhibitor? |
Bupropion (Wellbutrin) |
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What is the trade name of Bupropion? Uses? Side effects? |
Wellbutrin - NE/DA reuptake inhibitor - Used for depression and some efficacy for adult ADHD; smoking - Relative lack of sexual side effects, as compared to SSRIs - Increased risk of seizures and psychosis at high doses; may increase anxiety in some - Contraindicated in patients with seizure or active eating disorders and those on MAOIs |
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What are the contraindications to Bupropion (Wellbutrin)? |
- Seizure disorders - Active eating disorders - Pts on MAOIs |
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What are the serotonin receptor antagonists and agonists? |
- Trazodone (Desyrel) - Fefazodone (Serzone) |
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What are the uses of Trazodone and Fefazodone? |
- Refractory major depression - Major depression with anxiety - Insomnia (secondary to its sedative effects) |
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What are the benefits and side effects of Trazodone and Fefazodone? |
- Do not have sexual side effects like SSRis - Do not affect REM sleep
- Nausea, dizziness, orthostatic hypotension, cardiac arrhythmias, sedation, priapism - Nefazodone carries a black box warning for rare but serious liver failure (1 in 250,000-300,000) |
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What is priapism? What can cause this? |
Potentially painful medical condition in which the erect penis does not return to its flaccid state despite the absence of stimulation, within 4 hours
More common with trazodone
("Trazodone causes priapism: tRAZodone will RAISE the bone") |
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What antidepressant is an alpha-2 adrenergic receptor antagonist? |
Mirtazapine (Remeron) |
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What is the trade name of mirtazapine? Uses? Side effects? |
Remeron - alpha-2 adrenergic receptor antagonist: - Used for refractory major depression, especially in patients who need to gain weight - Side effects: sedation, weight gain, dizziness, somnolence, tremor, dry mouth, constipation, rare agranulocytosis - No sexual side effects and few drug interactions |
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What drug is best for depression in the elderly because it helps with sleep and appetite? |
Mirtazapine (Remeron) |
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What is the mechanism of TCAs? |
Heterocyclic antidepressants: - Inhibit reuptake of NE and serotonin - Increase availability of monoamines at synapse |
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Why shouldn't you consider TCAs as first-line meds? |
- Higher incidence of side effects - Require greater monitoring of dosing - Can be LETHAL in overdose |
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What are the types of TCAs? |
- Tricyclic antidepressants: tertiary amines and secondary amines - Tetracyclic antidepressants |
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What are the names of tricyclic antidepressants? |
Tertiary amines: - Amitriptyline (Elavil) - Imipramine (Tofranil) - Clomipramine (Anafranil) - Doxepin (Sinequan)
Secondary amines: - Nortriptyline (Pamelor, Aventyl) - Desipramine (Norpramin) |
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Which TCA is useful for chronic pain, migraines, and insomnia? |
Amitriptyline (Elavil) - Tertiary amine |
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Which TCA is useful for enuresis (inability to hold urine) and panic disorder? |
Imipramine (Tofranil) - Tertiary amine |
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Which TCA is useful for OCD? |
Clomipramine (Anafranil) - Tertiary amine |
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Which TCA is useful for chronic pain and as a sleep aid at low doses? |
Doxepin (Sinequan) - Tertiary amine |
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Which TCA is useful for chronic pain and is less likely to cause orthostatic hypotension? |
Nortriptyline (Pamelor, Aventyl) - Secondary amine |
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Which TCA is notable for being more activating, less sedating, and the least anti-cholinergic? |
Desipramine (Norpramin) - Secondary amine |
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What are the implications of being a tertiary vs secondary amine TCA? |
- Tertiary amines: highly anti-cholinergic, more sedating, greater lethality in overdose - Secondary amines: metabolites of tertiary amines (less anticholinergic, less sedating) |
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What are the characteristics of Amitriptyline? |
Elavil - Tertiary amine TCA - Highly anticholinergic, more sedating, greater lethality in overdose - Useful for chronic pain, migraines, insomnia |
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What are the characteristics of Imipramine? |
Tofranil - Tertiary amine TCA - Highly anticholinergic, more sedating, greater lethality in overdose - Useful for enuresis and panic disorder - IM form available |
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What are the characteristics of Doxepin? |
Sinequan - Tertiary amine TCA - Highly anticholinergic, more sedating, greater lethality in overdose - Useful in treating chronic pain - Emerging use as sleep aid in low doses |
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What are the characteristics of Nortriptyline? |
Pamelor, Aventyl - Secondary amine TCA - Metabolite of tertiary amine - less anticholinergic and less sedating - Least likely to cause orthostatic hypotension - Useful therapeutic blood levels - Useful in treating chronic pain |
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What are the characteristics of Desipramine? |
Norpramin - Secondary amine TCA - Metabolite of tertiary amine - less anticholinergic and less sedating - More activating - Least anticholinergic |
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What can be used to treat an overdose of TCAs? |
IV Sodium Bicarbonate |
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What are the Tetracyclic antidepressants? |
- Amoxapine (Asendin) - Maprotiline (Ludiomil) |
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Which TCA can cause extra-pyramidal side effects? |
Amoxapine (Asendin) - tetracyclic TCA - Metabolite of antipsychotic loxapine - May cause EPS and has similar side effect profile to typical antipsychotics |
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Which TCA has higher rates of seizure, arrhythmmia, and fatality on overdose? |
Maprotiline (Ludiomil) |
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How much does it take to overdose on TCAs? |
A 1-week supply (as little as 1-2g) can be lethal! |
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What are the major complications of TCAs? |
3 C's: - Cardiotoxicity - Convulsions - Coma |
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What are the side effects of all TCAs? |
- Anti-histamine --> sedation - Anti-adrenergic - Anti-muscarinic - Weight gain - Seizures - Serotonergic effects |
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What causes TCAs to have so many side effects? |
Lack of specificity and interaction with other receptors
TCAs are highly protein bound and lipid soluble, and therefore can interact with other meds that have high protein binding |
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What are the anti-histaminic side effects of TCAs? |
Sedation |
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What are the anti-adrenergic side effects of TCAs? |
Cardiovascular: - Orthostatic hypotension - Dizziness - Reflex tachycardia - Arrhythmias - ECG changes (widening of QRS, QT, and PR intervals) - Avoid in patients with pre-existing conduction abnormalities or recent MI |
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What are the anti-muscarinic / anti-cholinergic side effects of TCAs? |
- Dry mouth - Constipation - Urinary retention - Blurred vision - Tachycardia - Exacerbation of narrow angle glaucoma |
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How common are seizures in patients taking TCAs? |
0.3% rate, more common at higher plasma levels and with clomipramine and tetracyclics (amoxapine and maprotiline) |
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What are the signs of TCA overdose? |
- Agitation - Tremors - Ataxia - Delirium - Hypoventilation from CNS depression - Myoclonus - Hyperreflexia - Seizures - Coma |
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What are the serotonergic side effects of TCAs? |
- Erectile / ejaculatory dysfunction in males - Anorgasmmia in females |
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In what patients are TCAs contraindicated? |
- Patients with pre-existing conduction abnormalities - Patients with recent MI - Patients with higher suicide risk! |
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Which antidepressants are more effective in "atypical" depression (hypersomnia, increased appetite, increased sensitivity to interpersonal rejection)? |
MAOIs |
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What are the MAOIs? |
- Phenelzine (Nardil) - Tranylcypromine (Parnate) - Isocarboxazid (Marplan) |
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What is the mechanism of MAOIs? |
MAOIs prevent the inactivation of biogenic amines such as NE, serotonin, dopamine, and tyramine (intermediate in the conversion of tyrosine to NE)
By irreversibly inhibiting the enzymes MAO-A and -B, MAOIs increase the number of NTs available in synapses |
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What is the effect of MAO-A? |
Preferentially deactivates serotonin
Also acts on dopamine and tyramine |
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What is the effect of MAO-B? |
Preferentially deactivates NE and Epi
Also acts on dopamine and tyramine |
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Why aren't MAOIs used as first-line agents? |
Increased safety and tolerance of newer agents |
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What is the utility of MAOIs? |
Very effective for certain types of - Refractory depression - Refractory panic / anxiety disorder |
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What MAOI can be used as a patch? |
Selegiline (EPSAM patch) |
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What can you do and not do if using Selegiline (EPSAM patch)? |
- Does not require dietary restrictions when used in low dosages - Decongestants, opiates (Demerol), and seratonergic drugs must still be avoided! |
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What are the side effects of MAOIs? |
- Serotonin syndrome - Hypertensive crisis - Orthostatic hypotension - Drowsiness - Weight gain - Sexual dysfunction - Dry mouth - Sleep dysfunction - Paresthesias if pyridoxine deficiency (treat with B6) - Rarely, liver toxicity, seizures, edema |
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When does serotonin syndrome occur? |
SSRIs and MAOIs are taken together or if other drugs cause increased serotonin levels |
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What are the initial findings of serotonin syndrome? |
- Lethargy - Restlessness - Confusion - Flushing - Diaphoresis - Tremor - Myoclonic jerks |
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What are the later findings of serotonin syndrome? |
- Hyperthermia - Hypertonicity - Rhabdomyolysis - Renal failure - Convulsions - Coma or death |
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How can you prevent serotonin syndrome? |
Wait at least 2 weeks before switching from SSRI to MAOI (or vice versa); wait at least 5-6 weeks before switching if they used fluoxetine (longer half-life) |
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What can cause a hypertensive crisis? |
MAOIs + tyramine-rich foods or sympathomimetics |
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What are tyramine-rich foods? |
- Red wine - Cheese - Chicken liver - Fava beans - Cured meats |
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What are the symptoms of a hypertensive crisis? |
- Markedly elevated BP - Headache - Sweating - Nausea / vomiting - Photophobia - Autonomic instability - Chest pain - Arrhythmmias - Death |
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What is the most common side effect of MAOIs? |
Orthostatic hypotension |
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What should be your first step when you suspect serotonin syndrome? |
- Discontinue medication - Try calcium channel blockers (oral nifedipine) - If carefully monitored, can try chlorpromazine (typical antipsychotic) or phentolamine (anti-HTN, antagonizes alpha-adrenergic receptors) |
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What side effect can occur in patients with a pyridoxine deficiency when taking MAOIs? Treatment? |
Can cause paresthesias Treat with B6 |
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What antidepressant can lower the seizure threshold but is not usually associated with sexual side effects? |
Bupropion (Wellbutrin) |
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What antidepressant can cause dry mouth, retention, fatigue, blurry vision? |
TCAs - due to anticholinergic effects |
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What antidepressants can be used for OCD? |
- SSRIs (in higher doses) - TCAs (clomipramine) |
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What antidepressants can be used for panic disorder? |
- SSRIs - TCAs (imipramine) - MAOIs |
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What antidepressants can be used for eating disorders? |
- SSRIs (in high doses) - TCAs - MAOIs |
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What antidepressants can be used for dysthymia? |
SSRIs |
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What antidepressants can be used for social phobia? |
- SSRIs - TCAs - MAOIs |
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What antidepressants can be used for GAD? |
- SSRIs - SNRI (venlafaxine / effexor) - TCAs |
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What antidepressants can be used for PTSD? |
SSRIs |
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What antidepressants can be used for irritable bowel syndrome? |
- SSRIs - TCAs |
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What antidepressants can be used for enuresis? |
TCA (Imipramine) |
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What antidepressants can be used for neuropathic pain? |
- TCAs (Amitriptyline and Nortriptyline) - Duloxetine |
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What antidepressants can be used for chronic pain? |
- SSRIs - TCAs |
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What antidepressants can be used for fibromyalgia? |
SSRIs |
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What antidepressants can be used for migraine headaches? |
- TCAs (amitriptyline) - SSRIs |
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What antidepressants can be used for smoking cessation? |
Bupropion |
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What antidepressants can be used for premenstrual dysphoric disorder? |
SSRIs |
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What antidepressants can be used for the depressive phase of manic depression? |
SSRIs |
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What antidepressants can be used for insomnia? |
- Mirtazapine - TCAs (Amitriptyline) |
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Antipsychotics are used to treat what? |
- Psychotic disorders - Psychotic symptoms associated with psychiatric and other medical illnesses |
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What are the types of anti-psychotics? How do they differ? |
- Typical (1st gen), neuroleptics: classified by potency, treat psychosis by blocking D2 receptors - Atypical (2nd gen): block both D2 and serotonin 2a receptors |
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How do 1st gen and 2nd gen antipsychotics differ in their treatment of schizophrenia? |
- Both have similar efficacies in treating the presence of positive psychotic symptoms, such as hallucinations and delusions - 2nd gen may be more effective in treating negative symptoms, such as flattened affect and social withdrawal |
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Why are atypical antipsychotics largely replacing typical antipsychotics? |
More favorable side effect profile
However, there is some evidence for metabolic syndrome, weight gain, and other previously underappreciated effects, as well as the cost of these meds, that currently makes both classes recognized as first line |
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What are the low-potency typical antipsychotics? |
- Chlorpromazine (Thorazine) - Thioridazine (Mellaril) |
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What are the mid-potency typical antipsychotics? |
- Loxapine (Loxitane) - Thiothixene (Navane) - Trifluoperazine (Stelazine) - Perphenazine (Trilafon) |
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What are the high-potency typical antipsychotics? |
- Haloperidol (Haldol) - Fluphenazine (Prolixin) - Pimozide (Orap) |
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What does potency refer to? |
Action on dopamine, not the level of efficacy |
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What are the characteristics of low-potency typical antipsychotics? |
- Lower affinity for dopamine receptors, requiring higher doses - Higher incidence of anticholinergic and antihistamine side effects - More lethality in overdose due (d/t QTc prolongation and potential for heart block and ventricular tachycardia) - Rare risk for agranulocytosis - Slightly higher seizure risk
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What are the side effects specific to low-potency typical antipsychotics? |
- Anti-cholinergic effects - Anti-histamine effects - QTc prolongation - Potential for heart block and VT - Rare risk for agranulocytosis - Slightly higher seizure risk |
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What are the low-potency typical antipsychotics? |
- Chlorpromazine (Thorazine) - Thioridazine (Mellaril) |
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What are the characteristics of Chlorpromazine? |
Low-potency typical antipsychotic - Trade name: Thorazine - Commonly causes orthostatic hypotension - Can cause bluish skin discoloration - Can lead to photosensitivity - Can treat nausea and vomiting, as well as intractable hiccups |
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What are the characteristics of Thoioridazine? |
Low-potency typical antipsychotic - Trade name: Mellaril - Associated with retinitis pigmentosa |
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What are the mid-potency typical anti-psychotics? |
- Loxapine (Loxitane) - Thiothixene (Navane) - Trifluoperazine (Stelazine) - Perphenazine (Trilafon) |
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What are the characteristics of Loxapine? |
Mid-potency typical antipsychotic: - Trade name: Loxitane - Higher risk of seizure - Metabolite is an antidepressant |
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What are the characteristics of Thiothixene? |
Mid-potency typical antipsychotic: - Trade name: Navane - Can cause ocular pigment changes |
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What are the characteristics of Trifluoperazine? |
Mid-potency typical antipsychotic: - Trade name: Stelazine - Can reduce anxiety |
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What are the characteristics of Perphenazine? |
Mid-potency typical antipsychotic: - Trade name: Trilafon |
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What are the high-potency typical antipsychotics? |
- Haloperidol (Haldol) - Fluphenazine (Prolixin) - Pimozide (Orap) |
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What are the characteristics of high-potency typical antipsychotics? |
- Greater affinity for dopamine receptors, and therefore require relatively lowr doses to achieve effects - Cause less sedation, orthostatic hypotension, and anticholinergic effects - Greater risk for extra-pyramidal symptoms and tardive dyskinesia |
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What are the characteristics of Haloperidol? |
High-potency typical antipsychotic: - Trade name: Haldol - Decanoate form available = long-acting intramuscular form (useful for patients who don't like taking oral meds) |
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What are the characteristics of Fluphenazine? |
High-potency typical antipsychotic: - Trade name: Prolixin - Decanoate form available = long-acting intramuscular form (useful for patients who don't like taking oral meds)
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What are the characteristics of Pimozide? |
High-potency typical antipsychotic: - Trade name: Orap - Associated with heart block, ventricular tachycardia, and other cardiac effects |
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How can you give high-potency neuroleptics to treat acute agitation or psychosis? |
IM injection |
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Which typical antipsychotic can be used to treat intractable hiccups? |
Chlorpromazine (Thorazine) - low-potency |
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Which typical antipsychotic can cause ocular pigment changes? |
Thiothixene (Navane) - mid-potency |
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Which typical antipsychotic can lead to photosensitivity? |
Chlorpromazine (Thorazine) - low-potency |
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Which typical antipsychotic can lead to bluish skin discoloration? |
Chlorpromazine (Thorazine) - low-potency |
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Which typical antipsychotic is associated with retinitis pigmentosa? |
Thioridazine (Mellaril) - low-potency |
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Which typical antipsychotic is associated with heart block, ventricular tachycardia, and other cardiac effects? |
Pimozide (Orap) - high-potency |
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Which typical antipsychotic commonly causes orthostatic hypotension? |
Chlorpromazine (Thorazine) - low-potency |
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How are the positive symptoms of schizophrenia treated by antipsychotics? |
Action of meds in the mesolimbic dopamine pathway - this includes the nucleus accumbens, fornix, amygdala, and hippocampus |
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What are the components of the mesolimbic dopamine pathway? |
Positive symptoms are treated by action of antipsychotics at these locations: - Nucleus accumbens - Fornis - Amygdala - Hippocampus |
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What causes the negative symptoms of schizophrenia? |
Dopamine action in the mesocortical pathway |
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What is the significance of the mesocortical pathway in schizophrenia? |
Negative symptoms are thought to occur due to dopamine action in this location |
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What are the implications of the anti-dopaminergic effect of anti-psychotics? |
Hyperprolactinemia
Extra-pyramidal symptoms |
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Why do antipsychotics caues hyperprolactinemia? |
Decreased dopamine action in the tuberoinfundibular area leads to increased prolactin release |
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What are the symptoms of hyperprolactinemia? |
- Decreased libido - Galactorrhea - Gynecomastia - Impotence - Amenorrhea - Osteoporosis |
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What are the features of extra-pyramidal symptoms? |
- Parkinsonism - Akathisia - Dystonia |
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What are the symptoms of parkinsonism (extra-pyramidal symptoms)? |
- Bradykinesia - Masklike face - Cogwheel rigidity - Pill-rolling tremor |
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What are the symptoms of akathisia (extra-pyramidal symptoms)? |
- Subjective anxiety and restlessness - Objective fidgetiness - Patients may report a sensation of inability to sit still |
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What are the symptoms of dystonia (extra-pyramidal symptoms)? |
- Sustained painful contraction of muscles of neck (torticollis), tongue, eyes (oculogyric crisis) - Life-threatening if they involve the airway or diaphragm |
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How can you treat extra-pyramidal symptoms (parkinsonism, akathisia, and dystonia)? |
- Reduce the dose of the anti-psychotic - Administer anti-cholinergic medication such as Benztropine (Cogentin), an anti-histaminergic medication such as Diphenhydramine (Benadryl), or an anti-parkinsonian medication such as Amantadine (Symmetrel) |
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Which medications can be used to treat extra-pyramidal symptoms? Mechanism? |
- Benztropine (Cogentin) - anti-cholinergic - Diphenhydramine (Benadryl) - anti-histaminergic - Amantadine (Symmetrel) - anti-parkinsonian |
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What are the anti-HAM effects caused by typical anti-psychotics? |
- Anti-histamine: sedation, weight gain - Anti-alpha-1 adrenergic: orthostatic hypotension, cardiac abnormalities, sexual dysfunction - Anti-muscarinic (anti-cholinergic): dry mouth, tachycardia, urinary retention, blurry vision, constipation, precipitation of narrow-angle glaucoma |
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What are the anti-histamine effects of typical anti-psychotic? |
- Sedation - Weight gain |
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What are the anti-alpha-1 adrenergic effects of typical anti-psychotic? |
- Orthostatic hypotension - Cardiac abnormalities - Sexual dysfunction |
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What are the anti-muscarinic effects of typical anti-psychotic? |
Anti-cholinergic - Dry mouth - Tachycardia - Urinary retention - Blurry vision - Constipation - Precipitation of narrow-angle glaucoma |
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What is the term for choreoathetoid (writhing) movements of the mouth and tongue (or other body parts)? |
Tardive Dyskinesia |
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What are the symptoms of Tardive Dyskinesia? |
Choreoathetoid (writhing) movements of mouth and tongue (or other body parts) |
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Who is affected by Tardive Dyskinesia? |
- Patients who have used neuroleptics for >6 months - Most often in older women |
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What is the prognosis for patients who get Tardive Dyskinesia from anti-psychotics? |
50% will spontaneously remit, but many will be permanent |
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How do you treat Tardive Dyskinesia? |
Discontinuation of current anti-psychotic if clinically possible and changing to a medication with less potential to cause Tardive Dyskinesia |
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Which drug is less likely to cause Tardive Dyskinesia? |
Clozapine - the first atypical antipsychotic |
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What is the term for the following symptoms caused by antipsychotics: fever, autonomic instability (tachycardia, labile HTN, diaphoresis), etc? |
Neuroleptic Malignant Syndrome |
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Who is most likely to get Neuroleptic Malignant Syndrome? |
Young males early in treatment with both atypical and typical antipsychotics |
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What are the characteristic signs/symptoms of Neuroleptic Malignant Syndrome? |
FALTERED: - Fever (most common symptom) - Autonomic instability (tachycardia, labile HTN, diaphoresis) - Leukocytosis - Tremor - Elevated creatine phosphokinase (CPK) - Rigidity (lead pipe rigidity considered almost universal) - Excessive sweating (diaphoresis) - Delirium |
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What is the prognosis of Neuroleptic Malignant Syndrome? |
Medical emergency - 20% mortality rate if left untreated |
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How do you treat Neuroleptic Malignant Syndrome? |
Discontinue current medications and administer supportive medical care (hydration, cooling, etc) |
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Which drugs are infrequently used to treat neuroleptic malignant syndrome because of their own side effects and unclear efficacy? |
- Sodium Dantrolene - Bromocriptine - Amantadine |
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Can you ever reuse a medication that caused neuroleptic malignant syndrome? |
Not prevented from restarting the same neuroleptic at a later time; this is not an allergic reaction |
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What ophthalmologic problems may be caused by antipsychotics? Which meds? |
- Irreversible retinal pigmentation (high doses of Thioridazine) - Deposits in lens and cornea (Chlorpromazine) |
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What dermatologic problems may be caused by antipsychotics? Which meds? |
Rashes and photosensitivity (blue-gray skin discoloration with Chlorpromazine) |
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Which antipsychotics are more likely to lead to seizures? |
- All anti-psychotics lower the seizure threshold. - Low-potency anti-psychotics are more likely to cause seizures than high potency. |
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What are the chances of developing tardive dyskinesia? |
Roughly 1% chance of developing for each year on a typical antipsychotic |
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What is the typical onset for the different neuroleptic side effects? |
- Acute dystonia: hours to days - EPS / akathisia: days to months - Tardive dyskinesia: months to years |
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What can be used to quantify and monitor for tardive dyskinesia? |
Abnormal involuntary movement scale |
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Which side effect is most likely to occur within hours to days of use of antipsychotics? |
Hours to days |
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Which side effect is most likely to occur within days to months of use of antipsychotics? |
Extra-pyramidal symptoms and akathisia |
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Which side effect is most likely to occur within months to years of use of antipsychotics? |
Tardive dyskinesia |
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Case: 31 yo overweight woman presents to clinic following discharge from in-pt psych unit. Police found her in a mall talking to herself and telling passerby's that the devil had "stolen her soul." She was disheveled and scared. During hospitalization she was diagnosed with schizophrenia, and olanzapine was titrated to 30 mg at bedtime for delusional thinking and disorganized behavior. She has been living with her parents, and hygiene and self-care have improved. She reports occasional auditory hallucinations telling her that her parents do not like her, she recognizes they are not real and is not distressed by them. She has become involved in a vocational skills program and hopes to work at a local supermarket. During her last appt with her PCP she was told she had elevated fasting glucose (115), gained 12# in 3 months, waist circumference was 36", and TG were 180. BP was normal, and she reported a family history of DM and HTN.
What is the next step? |
- Given her adequate partial response, she should continue on an anti-psychotic - Labs suggest metabolic syndrome, increasing risk for CV disease - Olanzapine and other atypicals have been associated with weight gain and impaired glucose metabolism (unclear if it was normal prior to starting)
- Recommend: start lifestyle modifications and close monitoring of her weight, blood sugar, lipids, and waist circumference - May consider other atypicals (ziprasidone or aripiprazole) or typicals |
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Which atypical antipsychotics are less associated with weight gain? |
- Ziprasidone (Geodon) - Aripiprazole (Abilify) |
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What is the mechanism of atypical antipsychotics? |
Block both dopamine and serotonin receptors |
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What are the benefits of atypical antipsychotics? |
- Less likely to cause EPS, tardive dyskinesia, or neuroleptic malignant syndrome - More effective in treating negative symptoms of schizophrenia - Also used to treat acute mania, bipolar disorder, and as adjuncts in unipolar depression |
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What are the uses of atypical antipsychotics? |
- Schizophrenia - Acute mania - Bipolar disorder - Unipolar disorder - Personality disorders - Certain psychiatric disorders in childhood |
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What are the types of atypical antipsychotics? |
- Clozapine (Clozaril) - Risperidone (Risperdal) - Quetiapine (Seroquel) - Olanzapine (Zyprexa) - Ziprasidone (Geodon) - Aripiprazole (Abilify) - Paliperidone (Invega) - Asenapine (Saphris) - Iloperidone (Fanapt) |
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Which atypical antipsychotic is the most effective? |
Clozapine (Clozaril) BUT it is associated with agranulocytosis |
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What is the trade name of Clozapine? Benefits? Side effects? |
Clozaril: - 30% of treatment resistant psychosis will respond to clozapine - Only anti-psychotic shown to decrease risk of suicide - Less likely to cause tardive dyskinesia - S.E.: tachycardia, hypersalivation, anti-cholinergic effects, myocarditis, 1-2% incidence of agranulocytosis, 2-5% incidence of seizures |
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At what point must you stop clozapine? |
If absolute neutrophil count drops <1500 / µL |
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What is the incidence of agranulocytosis with clozapine? |
1-2% |
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What is the incidence of seizures with clozapine? |
2-5% |
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What is the trade name of Risperidone? Benefits? Side effects? |
Risperdal: - Long-acting injectable form called Consta - Approved to treat mania - Can cause increased prolactin - Some orthostatic hypotension and reflex tachycardia |
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What is the trade name of Quetiapine? Benefits? Side effects? |
Seroquel: - Approved to treat mania - Common side effects include sedation and orthostatic hypotension
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What is the trade name of Olanzapine? Benefits? Side effects? |
Zyprexa: - Approved to treat mania - Common side effect is weight gain |
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What is the trade name of Ziprasidone? Benefits? Side effects? |
Geodon: - Approved to treat mani - Less likely to cause weight gain |
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What is the trade name of Aripiprazole? Benefits? Side effects? |
Abilify: - Unique mechanism of partial D2 agonism - Approved to treat mani - Can be more activating (akathisia) and less sedating - Less potential for weight gain |
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What is the trade name of Paliperidone? Benefits? Side effects? |
Invega: - Metabolite of risperidone - Long-acting injectable form (Sustenna) - Newer, expensive medication |
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What is the trade name of Asenapine? |
Saphris - Newer, expensive atypical antipsychotic |
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What is the trade name of Iloperidone? |
Fanapt: - Newer, expensive atypical antipsychotic |
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Which medications work by reversible inhibition of acetylcholine esterase? Use? |
Alzheimer medications: - Tacrine - Donepazil |
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Which antipsychotics are FDA approved for treatment of mania? |
- Quetiapine (Seroquel) - Olanzapine (Zyprexa) - Aripiprazole (Abilify) - Risperidone (Risperdal) - Ziprasidone (Geodon) |
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Which atypical antipsychotic is unique because of its partial D2 agonism? |
Aripiprazole (Abilify) |
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Which atypical antipsychotic can be more activating (akathisia) and less sedating? |
Aripiprazole (Abilify) |
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What monitoring must be done for patients on clozapine? |
Weekly blood draws for the first 6 months to check absolute neutrophil count and WBC counts because this med can cause agranulocytosis
With time you can decrease the frequency of blood draws |
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What are the side effects common to atypical antipsychotics? |
- Metabolic syndrome - Some anti-HAM effects (anti-Histamine, anti-Adrenergic, anti-Muscarinic/cholinergic) - Weight gain - Hyperlipidemia - Hyperglycemia (rarely, diabetic ketoacidosis) - Liver malfunction - QTc prolongation |
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How do you monitor for metabolic syndrome in patients going on atypical antipsychotics? |
- Baseline weight - Waist circumference (measure at iliac crest) - Blood pressure - Fasting glucose - Fasting lipids (triglycerides) |
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How do you monitor liver function in patients going on atypical antipsychotics? |
Monitor yearly for elevation in LFTs and ammonia |
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How can antipsychotics be used to help patients on mood stabilizers? |
May be used as adjuncts to mood stabilizers early in the course of a manic episode |
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What are the uses of mood stabilizers? |
- Acute mania - Prevent relapses of manic episodes in bipolar disorder and schizoaffective disorder - Adjuncts for antidepressants - Aduncts for schizophrenia - Enhance abstinence in alcoholism treatment - Treat aggression and impulsivity (dementia, intoxication, mental retardation, personality disorders, general medical conditions) |
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What are the mood stabilizers? |
- Lithium - Anticonvulsants: valproic acid, lamotrigine, carbamazepine |
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What is the only mood stabilizer to decrease suicidality? |
Lithium |
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Which mood stabilizers require blood level testing? |
- Lithium - Valproic acid - Carbamazepine - Clozapine |
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What is the drug of choice for acute mania? |
Lithium |
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What is the drug of choice for prophylaxis for both manic and depressive episodes in bipolar and schizoaffective disorder? |
Lithium |
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What are the uses of lithium? |
- Acute mania - Prophylaxis for manic and depressive episodes in bipolar and schizoaffective disorder - Cyclothymia - Unipolar depression |
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How is lithium metabolized? Implications? |
Kidney - adjust the dose and monitor levels closely if patient has renal dysfunction |
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What tests should be done before starting a patient on lithium? |
- ECG - Basic chemistries - Thyroid function tests - CBC - Pregnancy test |
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How long does it take for lithium to be effective? |
5-7 days |
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How often should you check blood levels of lithium? What does this information tell you? |
Blood levels correlate with clinical efficacy and should be checked after 5 days, and then every 2-3 days until therapeutic |
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What are the drawbacks of lithium therapy? |
- High evidence of side effects - Very narrow therapeutic index |
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What is the therapeutic index for lithium? |
- Therapeutic range: 0.6 - 1.2 (can become toxic even within this range) - Toxic >1.5 - Lethal >2.0 |
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What medications affect lithium levels? |
- NSAIDs: decrease lithium levels - Aspirin - Diuretics, especially thiazides |
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What non-medication factors affect lithium levels? |
- Dehydration: increases lithium - Salt deprivation: increases lithium - Sweating (salt loss): increases lithium - Impaired renal function: increases lithium |
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What are the side effects of toxic levels of lithium (>2.0)? |
- Altered mental status - Coarse tremors - Convulsions - Death |
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What tests should be done regularly in patients on lithium? |
- Lithium levels - TSH - Kidney function |
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What are the side effects of lithium? |
- Fine tremor - Nephrogenic diabetes insipidus - GI disturbance - Weight gain - Sedation - Thyroid enlargement, hypothyroidism - ECG changes - Benign leukocytosis - Ebstein's anomaly |
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What can happen to babies born to mothers on lithium? |
Ebstein's anomaly: cardiac defect |
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What are the anticonvulsants used for psychiatric disorders? |
- Carbamazepine (Tegretol) - Valproic Acid (Depakote and Depakene) - Lamotrigene (Lamictal) - Oxcarbazepine (Trileptal) - Gabapentin (Neurontin) - Pregabalin (Lyrica) - Tiagabine (Gabitril) - Topiramate (Topamax) |
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What is the trade name of Carbamazepine? Uses? |
Tegretol: - Mixed episodes - Rapid-cycling bipolar disorder (less effective for depressed phase) - Trigeminal neuralgia |
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What is the mechanism of Carbamazepine (Tegretol)? |
Blocks sodium channels and inhibits action potentials |
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How long does it take for Carbamazepine (Tegretol) to become effective? |
5-7 days for onset of action |
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What needs to be monitored in patients taking Carbamazepine (Tegretol)? |
Check before initiating treatment, monitor regularly: - CBC - LFTs |
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What are the side effects of Carbamazepine (Tegretol)? |
- GI side effects - CNS effects: drowsiness, ataxia, sedation, confusion - Stevens-Johnson Syndrome - Blood counts: leukopenia, aplastic anemia, thrombocytopenia, agranulocytosis - Hyponatremia - Elevated liver enzymes --> hepatitis |
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What is the possible effect of Carbamazepine (Tegretol) on blood counts? |
Agranulocytosis - Leukopenia - Aplastic anemia - Thrombocytopenia |
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What are the effects of the use of Carbamazepine (Tegretol) during pregnancy? |
Neural tube defects |
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What is the significance of the cytochrome P450 pathway on Carbamazepine (Tegretol)? |
Drug interactions with many drugs metabolized by the P450 pathway, including inducing its own metabolism through auto-induction, requiring increasing doses |
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What are the findings of Carbamazepine (Tegretol) toxicity? |
- Confusion - Stupor - Motor restlessness - Ataxia - Tremor - Nystagmus - Twitching - Vomiting |
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What is the utility of Valproic Acid (Depakote and Depakene)? |
- Mixed episodes of bipolar disorder - Rapid cycling bipolar disorder |
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What do you need to monitor in patients taking Valproic Acid (Depakote and Depakene)? |
LFTs and CBC
Blood levels of Valproic Acid after 3-5 days (normal is 50-150 µg/mL) |
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What are the side effects of Valproic Acid (Depakote and Depakene)? |
- GI side effects - Weight gain - Sedation - Alopecia - Pancreatitis - Hepatotoxicity or benign aminotransferase elevations - Increased ammonia - Thrombocytopenia |
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What are the teratogenic effects of Valproic Acid (Depakote and Depakene)? |
Neural tube defects |
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What is the trade name for Lamotrigine? Uses? |
Lamictal: - Bipolar depression (little efficacy for acute mania or prevention of mania) |
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What is the mechanism of Lamotrigine (Lamictal)? |
Works on sodium channels that modulate glutamate and aspartate |
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What are the most common side effects of Lamotrigine (Lamictal)? |
- Dizziness - Sedation - Headaches - Ataxia - Stevens-Johnson Syndrome (10%) |
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Which anticonvulsant drugs can cause Stevens-Johnson syndrome? |
- Lamotrigine (Lamictal) - 10%, most likely in first 4-6 weeks, but minimized by starting with low doses and increasing slowly - Carbamazepine (Tegretol) |
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How does Lamotrigine (Lamictal) affect Valproate? |
- Valproate will increase Lamotrigine (Lamictal) - Lamotrigine (Lamictal) will decrease Valproate |
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What is the trade name of Oxcarbazepine? Uses? Risks? |
Trileptal: - As effective in mood disorders as Carbamazepine, but better tolerated - Less risk of rash and hepatic toxicity |
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What is the trade name of Gabapentin? Uses? |
Neurontin: - Often used adjectively to help with anxiety and sleep - Little efficacy in bipolar disorder |
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What is the trade name of Pregabalin? Uses? |
Lyrica: - Used in GAD and fibromyalgia - Little efficacy in bipolar disorder |
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What is the trade name of Tiagabine? Uses? |
Gabitril: - May be helpful with anxiety |
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What is the trade name of Topiramate? Uses? Side effects? |
Topamax: - Helpful with impulse control disorder and anxiety - Beneficial side effect is weight loss - Can cause hypochloremic, non-anion gap metabolic acidosis and kidney stones - Most limiting effect is cognitive slowing |
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Which anticonvulsant is used adjectively to help with anxiety and sleep? |
Gabapentin (Neurontin) |
|
|
Which anticonvulsant is used in generalized anxiety disorder and fibromyalgia? |
Pregabalin (Lyrica) |
|
|
Which anticonvulsant is helpful for impulse control disorder and anxiety? |
Topiramate (Topamax) |
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Which anticonvulsant can cause kidney stones? |
Topiramate (Topamax) |
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Which anticonvulsant is limited in its use by cognitive slowing? |
Topiramate (Topamax) |
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|
What are the types of anxiolytics? |
- Benzodiazepines - Barbiturates - Buspirone |
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|
What are the common indications for anxiolytics / hypnotics? |
- Anxiety disorders - Muscle spasm - Seizures - Sleep disorders - Alcohol withdrawal - Anesthesia induction |
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|
Which benzodiazepines can be safely used in chronic alcoholics or liver disease? |
Use benzodiazepines that are not metabolized by the liver. There are a LOT of them: - Lorazepam - Oxazepam - Temazepam |
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What is the mechanism of benzodiazepines? |
Potentiate the effects of GABA |
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What should you not mix with benzodiazepines? Why? |
Alcohol - can be lethal by causing respiratory depression |
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What are the long-acting (half-life >20 hours) benzodiazepines? |
- Diazepam (Valium) - Clonazepam (Klonopin) |
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What are the intermediate acting (half-life 6-20 hours) benzodiazepines? |
- Alprazolam (Xanax) - Lorazepam (Ativan) - Oxazepam (Serax) - Temazepam (Restoril) |
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What are the short-acting (half-life <6 hours) benzodiazepines? |
- Triazolam (Halcion) - Midazolam (Versed) |
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What is the trade name of Diazepam? Half-life? Onset? Uses? |
Valium: - Half-life: >20 hours - Rapid onset - Used during detox from alcohol or sedative-hypnotic anxiolytics, seizures - Less commonly used for anxiety |
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What is the trade name of Clonazepam? Half-life? Uses? Contraindications |
Klonopin: - Half-life: >20 hours (once daily dosing) - Uses: anxiety, panic attacks - Avoid with renal dysfunction |
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What is the trade name of Alprazolam? Half-life? Onset? Uses? |
Xanax: - Half-life: 6-20 hours - Short onset of action --> euphoria, high abuse potential - Uses: anxiety, panic attacks |
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What is the trade name of Lorazepam? Half-life? Onset? Uses? |
Ativan: - Half-life: 6-20 hours - Uses: panic attacks, alcohol and sedative-hypnotic anxiolytic detoxification, and agitation - Not metabolized by liver |
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What is the trade name of Oxazepam? Half-life? Onset? Uses? |
Serax: - Half-life: 6-20 hours - Uses: alcohol and sedative-hypnotic anxiolytic detoxification - Not metabolize by liver |
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What is the trade name of Temazepam? Half-life? Onset? Uses? |
Restoril: - Half-life: 6-20 hours - Uses: insomnia (decreasingly used due to dependence) - Not metabolized by liver |
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What is the trade name of Triazolam? Half-life? Onset? Uses? |
Halcion: - Half-life: <6 hours - Use: insomnia - Primarily used in medical and surgical settings |
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What is the trade name of Midazolam? Half-life? Onset? Uses? |
Versed: - Half-life: <6 hours - Primarily used in medical and surgical settings |
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What can be used for benzodiazepine overdose? |
Flumazenil (but don't induce withdrawal too quickly, that can be life threatening) |
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What are the side effects of benzodiazepines? |
- Drowsiness - Impairment of intellectual function - Reduced motor coordination (careful in elderly) - Anterograde amnesia - Withdrawal can be life threatening and cause seizures |
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What are the effects of toxic dosing of benzodiazepines? |
Respiratory depression in overdose, especially when combined with alcohol |
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What are the non-benzodiazepine hypnotics? |
- Zolpidem (Ambien) - Zaleplon (Sonata) - Eszopiclone (Lunesta) - Diphenhydramine (Benadryl) - Chloral Hydrate (Noctec, Somnote) - Ramelteon (Rozarem)
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What is the trade name for Zolpidem? Mechanism? Uses? |
Ambien: - Selective receptor binding to benzodiazepine receptor 1, responsible for sedation - Used short-term for insomnia |
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What is the trade name for Zaleplon? Mechanism? Uses? |
Sonata: - Selective receptor binding to benzodiazepine receptor 1, responsible for sedation - Used short-term for insomnia |
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What is the trade name for Eszopiclone? Mechanism? Uses? |
Lunesta: - Selective receptor binding to benzodiazepine receptor 1, responsible for sedation - Used short-term for insomnia |
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Can you develop tolerance to Zolpidem, Zaleplon, and Eszopiclone? |
Yes, but less tolerance and dependence with prolonged use than with benzodiazepines |
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How do the half-lives compare for Zolpidem, Zaleplon, and Eszopiclone? |
Zaleplon < Zolpidem < Eszopiclone |
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What are the side effects of Zolpidem, Zaleplon, and Eszopiclone? |
- Anterograde amnesia - Hallucinations - Sleep walking - GI side effects |
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What is the trade name of Diphenhydramine? Mechanism? Side effects? |
Benadryl: - Anti-histamine - Sedation, dry mouth, constipation, urinary retention, blurry vision |
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What is the trade name of Chloral Hydrate? Uses? Side effects? |
Noctec, Somnote: - Not commonly used as a hypnotic due to tolerance and dependence - Lethal in overdose, causing hepatic and liver failure |
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What is the trade name of Ramelteon? Mechanism? Side effects? |
Rozerem: - Selective melatonin MT1 and MT2 agonist - No tolerance or dependence |
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What are the non-benzodiazepine anxiolytics? |
- Buspirone (BuSpar) - Hydroxyzine (Atarax) - Barbiturates (eg, Butalbitol, Phenobarbital, Amobarbitol, Pentobarbitol) - Propranolol |
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What is the trade name of Buspirone? Mechanism? Side effects? |
BuSpar: - Partial agonist of 5HT-1A receptor - Slower onset of action than benzos (1-2 weeks) - Not as effective as other options, often used in combination with another agent (e.g., SSRI) for treatment of anxiety - Does not potentiate CNS depression of alcohol (useful in alcoholics), and low potential for abuse/addiction |
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What is the trade name of Hydroxyzine? Mechanism? Side effects? |
Atarax: - Anti-histamine anxiolytic - Side effects: sedation, dry mouth, constipation, urinary retention, blurry vision - Useful for patients who want quick-acting short-term med but who can't take benzos |
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What are the barbiturates? Use? |
- Butalbitol, Phenobarbitol, Amobarbitol, Pentobarbitol - Rarely used now because of the lethality of overdose and side effect profile |
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What is the mechanism of Propranolol? Uses? |
- Beta-blocker - Treats autonomic side effects of panic attacks or performance anxiety, such as palpitations, sweating, and tachycardia - Can be used to treat Akathisia (side effect of typical anti-psychotics) |
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What are the types of psychostimulants? |
- Dextroamphetamine and Amphetamine (Dexedrine, Adderall) - Methylphenidate (Ritalin, Concerta) - Atomoxetine (Strattera) - Modafanil (Provigil) |
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What is the trade name for dextroamphetamine and amphetamine? Uses? Side effects? |
Dexedrine or Adderall: - Used for ADHD and refractory depression - Adderall is schedule II, which means prescription in triplicate and high potential for abuse - Monitor BP and watch for weight loss, insomnia |
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What do you need to monitor in patients on dextroamphetamine and amphetamine (dexedrine, adderall)? |
Monitor BP and watch for weight loss and insomnia |
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What is the trade name for methylphenidate? Uses? Side effects? |
Ritalin or Concerta - Used for ADHD and refractory depression - CNS stimulant similar to amphetamine - Schedule II, which means Rx in triplicate and high potential for abuse - Watch for leukopenia, anemia, elevated LFTs - Monitor BP and watch for weight loss and insomnia |
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What do you need to monitor in patients on methylphenidate (ritalin, concerta)? |
- Watch for leukopenia, anemia, elevated LFTs - Monitor BP and watch for weight loss, insomnia |
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What is the trade name for Atomoxetine? Uses? Side effects? |
Strattera - Used for ADHD and refractory depression - Presynaptic norepinephrine transporter inhibitor - Less appetite suppression and insomnia - Rare liver toxicity, possible increased suicidal ideation in children/adolescents |
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What is the trade name for Modafanil? Uses? |
Provigil - Psychostimulant - Used in narcolepsy |
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What are the cognitive enhancers? |
Acetylcholinesterase inhibitors: - Donepezil (Aricept) - Galantamine (Reminyl) - Rivastigmine (Excelon)
Unknown: - Tacrine (Cognex)
NMDA antagonist: - Memantine (Namenda) |
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What is the trade name of Donepezil? Mechanism? Uses? Side effects? |
Aricept - Acetylcholinesterase inhibitor - Mild to moderate dementia - Once daily dosing - Some GI effects |
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What is the trade name of Galantamine? Mechanism? Uses? |
Reminyl - Acetylcholinesterase inhibitor - Used in dementia (cognitive enhancer) |
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What is the trade name of Rivastigmine? Mechanism? Uses? Side effects? |
Excelon - Acetylcholinesterase inhibitor - Used for dementia (cognitive enhancer) - Has a patch, less side effects |
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What is the trade name of Tacrine? Mechanism? Uses? |
Cognex - Used for dementia (cognitive enhancer) |
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What is the trade name of Memantine? Mechanism? Uses? Side effects? |
Namenda - NMDA receptor antagonist - Used for moderate to severe dementia - Works better with acetylcholinesterase inhibitors |
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What medications may cause psychosis? |
- Sympathomimetics - Analgesics - Antibiotics (eg, isoniazid) - Anti-cholinergics - Anti-convulsants - Anti-histamines - Corticosteroids - Anti-Parkinsonian agents |
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What medications may cause agitation / confusion / delirium? |
- Anti-psychotics - Anti-depressants - Anti-arrhythmics - Anti-neoplastics - Corticosteroids - Cardiac glycosides - NSAIDs - Anti-asthmatics - Antibiotics - Anti-HTN - Anti-Parkinsonian agents - Thyroid hormones |
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What medications may cause depression? |
- Anti-HTN - Anti-Parkinsonian agents - Corticosteroids - Calcium channel blockers - NSAIDs - Antibiotics - Peptic ulcer drugs |
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What medications may cause anxiety? |
- Sympathomimetics - Anti-asthmatics - Anti-Parkinsonian agents - Hypoglycemic - NSAIDs - Thyroid hormones |
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What medications may cause sedation / poor concentration? |
- Anti-anxiety agents / hypnotics - Anti-cholinergics - Antibiotics - Anti-histamines |
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What are the psychiatric side effects of procainamide? |
- Confusion - Delirium |
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What are the psychiatric side effects of quinidine? |
- Confusion - Delirium |
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What are the psychiatric side effects of albuterol? |
- Anxiety - Confusion |
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What are the psychiatric side effects of isoniazid? |
Psychosis |
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What are the psychiatric side effects of tetracyclines? |
Depression |
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What are the psychiatric side effects of Nifedipine and Verapamil? |
Depression |
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What are the psychiatric side effects of Cimetidine? |
- Depression - Psychosis |
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What are the psychiatric side effects of Steroids? |
- Aggressiveness / agitation - Hypomania - Anxiety - Psychosis |
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What are the non-medication, non-therapy methods of treating psychiatric disorders? |
- Electroconvulsive therapy (ECT) - Deep brain stimulation (DBS) - Repetitive transcranial magnetic stimulation (rTMS) - Light therapy |
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What is the procedure for giving electroconvulsive therapy (ECT)? |
- General anesthesia (methohexital) - Muscle relaxant (succinylcholine) - Generalized tonic-clonic seizure is induced using unilateral or bilateral electrodes - Bilateral electrode placements decrease the number of treatments needed, but increase memory impairment and confusion |
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What determines efficacy of electroconvulsive therapy (ECT)? |
Length of post-octal suppression and other factors, not on seizure duration |
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What is electroconvulsive therapy (ECT) used for? |
- Depression, especially with psychotic features - Acute mania - Catatonia - Pts who can't tolerate meds or who have failed other treatments |
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How long do you do electroconvulsive therapy (ECT) for? |
Discontinue after symptomatic improvement, typically 8-12 sessions given 3x / week and monthly maintenance ECT to prevent relapse of symptoms |
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What are the most common side effects of electroconvulsive therapy (ECT)? |
- Muscle soreness - Headaches - Amnesia - Confusion - Bilateral electrode placements decrease the number of treatments needed, but increase memory impairment and confusion |
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What is the method of deep brain stimulation (DBS)? |
Surgical treatment involving the implantation of a medical device that sends electrical impulses to specific parts of the brain |
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What are the benefits of deep brain stimulation (DBS)? |
- Chronic pain - Parkinson disease - Tremor - Dystonia - Affective disorders, including major depression |
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What is the method of repetitive transcranial magnetic stimulation (rTMS)? |
- Non-invasive method to excite neurons in the brain - Weak electrical currents are induced in the tissue by rapidly changing magnetic fields, a process called electromagnetic induction - Brain activity can be triggered with minimal discomfort |
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What are the uses of repetitive transcranial magnetic stimulation (rTMS)? |
- Major depression - Auditory hallucinations |
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What are the side effects of repetitive transcranial magnetic stimulation (rTMS)? |
- Rare seizures - Discomfort at delivery site |
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What is the method of delivering light therapy? |
- Lasers - Light-emitting diodes - Fluorescent lamps - Dichroic lamps - Very bright, full-spectrum light |
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What are the uses of light therapy? |
- Seasonal affective disorder - Non-seasonal psychiatric disorders |
