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46 Cards in this Set
- Front
- Back
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Chloropromazine is what generation antipsychotic? Binds most tightly to what receptor? Pros? Cons?
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• 1st generation
• α1 & 5HT2 > D2 >D1 • Pros: inexpensive, Cons: lots of side efx |
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Haloperidol is what generation antipsychotic? Binds most tightly to what receptor? Pros? Cons?
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• 1st generation
• D2 > D1 = D4 > α1 > 5HT Cons: **Lots of EPS** |
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Clozapine is what generation antipsychotic? Binds most tightly to what receptor? What is an associated side-effect? Pros? Cons?
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• 1st generation
• D4 = α1 • > 5HT > D2 = D1 Also potent at H1 which leads to *sedation* • Pros: may help Tx-resistant pts, ***agranulocytosis in 2% of pts** |
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What are the side effects of 1st generation antipsychotics?
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• Affects on ANS (anti-muscarinic, some anti α-adrenergic)
• Akathisia, Dystonias, Tardive Dyskinesia (may be irreversible!!) • Amenorrhea-galactorrhea • Weight gain *****Neuroleptic malignant syndrome***** |
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What 1st generation anti-psychotic is associated with cardiotoxicity & retinal pigmentation?
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Thioridazine
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What 2nd generation anti-psychotic has broad efficay, few EPS at low doses, EPS & hypotension at high doses, and has the availability of depo dosing?
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Risperidone
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What 2nd generation anti-psychotic is good for (-) and (+) symptoms, has few EPS, but causes significant weight gain?
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Olanzapine
mne: Person looks like an O after weight gain |
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What 1st generation antipsychotic can cause blue-grey skin discoloration and/or rash?
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Thiothixene
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Describe the absorption, distribution, metabolism, & excretion of antipsychotics
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• Most are highly lipid soluble & protein bound
• Large Vd • Much longer duration of action than predicted by T1/2 • Extensive first pass metabolism (except Thioridiazine) • Excreted mostly unchanged |
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What antipsychotic does not undergo extensive 1st pass metabolism (unlike the rest of the antipsychotics) & and can cause fatal v-tach?
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Thioridiazine
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Is Bipolar more common in males or females? What is the usual age of onset?
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• More common in females 1.2:1, ♀:♂
• Age of onset ≈ 18-20 |
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What antipsychotic works by augmenting the AP and also by the ↑ effects of the 5HT1 G-protein receptor (blocks 2nd messenger conversion to IP1 and Inositol, causing a build up of PIP2 and IP3 which then go on to ↑ effects in the cell)
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Lithium
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What are the adverse effects of Li+?
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Tremor, Polydipsia & polyuria, edema, leukocytosis,
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How should Li+ Tx be managed during pregnancy?
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↑ renal clearance during pregnancy (↓ postpartum) ∴ ↑ dose during pregnancy,↓ after.
• Enters breast milk, can cause hepatosplenomegaly in newborn, poor suckling |
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What anti-seizure drugs can be used for bipolar disorder in lieu of Li+? Pros? Cons?
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• Valproic acid. Cons: Teratogenic do NOT give during pregnancy, 1-2% spina bifida
• Carbamazepine: Less efficacious |
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What is the most common type of depression (>60%)? Next ( ≈ 25%)? Least most commone (≈10-15%?)
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• Reactive depression (loss & adverse life events)
• Major Depression (autonomous, not caused by ∆s in life) • Bipolar (characterized by episodes of mania) |
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What is the diagnostic criteria for major depression?
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• Five or more of the following in the same 2 wk period (must include one of the first two)
• Depressed mood, Loss of interest/pleasure, weight loss/∆ in appetite, Insomnia/hypersomnia, psychomotor agitation/slowness, fatigue, feelings of worthlessness, ↓ ability to concentrate, recurrent thoughts of death/suicide |
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What hypothesis of the pathophys of depression accounts for the fact that it often takes weeks-months for antidepressants to take effect?
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• Neurotrophic hypothesis of gene expression ( ↓ signal transduction leads to ↓ gene expression, CREB & BDNF)
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Where is the origin of the majority of the NE pathways in the brain? Serotonin pathways?
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• Locus Coeruleus
• Raphe nuclei |
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What SSRI has the longest T 1/2?
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• Fluoxetine
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What SNRIs have extensive hepatic metabolism? What receptors do they bind?
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• Venlaxafine, Duloxetine
• Bind NE and 5HT receptors |
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What 5HT antagonist (what class?) has potent CYP3A4 inhibition?
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• Heterocyclcs
•Nefazadone |
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What α2 antagonist (what class?) has an active metabolite that is a potent D2 blocker?
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• Tetracyclics/Unicyclics
•Amoxapine |
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What class of antidepressants is contraindicated with MAO-i?
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• SSRIs can lead to serotonin syndrome
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What class of antidepressants have the risk of overdose? What drugs are in this class?
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• Tricyclics
• Amitryptiline, Clomipramine, Desipramine, Doexepin, Imipramine, Nortriptyline, Protriypline, Trimipramine |
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What 5HT antagonist (what class?) is useful for sleep?
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• Trazadone (Heterocyclics)
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What 5HT antagonist (what class?) is notable for fewer sexual side efx?
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• Nefazadone (Heterocyclics)
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What tetracyclic has DA receptor antagonism? What side effx can result?
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• Amoxapine (Tetracyclics)
• Side effx: parkinsonism, amenorrhea, tardive dyskinesia |
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What tetracyclic has anithistamine effx? What side effx can result?
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• Mirtazapine (Tetracyclics)
• Side effx: sedation, weight gain |
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What class of antidepressant drugs can preciptiate hypertensive crisis with aged cheeses, red wine or liver?
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• MAO-I as the result of the accumulation of tyramine
• Also risk of interaction with SSRI: serotonin syndrome |
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What class of antidepressant drugs is helpful with pts w/ atypical depression?
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MAO-i
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What class of antidepressant drugs has better efficacy, but less compliance?
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• TCAs (also risk of overdose)
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What class of antidepressant drugs are usually 1st choice, but more expensive?
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• SSRIs
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What were the findings of the STAR-D study?
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• Remission should be the first goal of Tx
• If 1st Tx fails, switching or augmenting is reasonable • Docs should give max/tolearble dose for at least 8 wks before deciding that an intervention has failed • After 2 medication trials refer to a psychiatrist • Most pts will enter remission |
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What is a situation to use extreme caution when using antidepressants?
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Bipolar disorder: may produce a sudden switch from depression to hypomanic or manic depressant states
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What is a major concern when giving antidepressants to children?
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Greater risk of adverse events representing suicidal thinking or behavior (suicidality) during the first few months of treatment in those receiving antidepressants. The average risk of such events in patients receiving antidepressants was 4%, twice the placebo risk of 2%.
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An overdose of this class of antidepressants presents as coma, shock, respiratory depression, agitation, muscle seizures, arrhythmias
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• Tricyclics
• Amitryptiline, Clomipramine, Desipramine, Doexepin, Imipramine, Nortriptyline, Protriypline, Trimipramine |
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An overdose of this tetracyclic can cause servere neurotoxicity and seizures
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Amoxapine
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An overdose of this tetracyclic can cause servere seizures and cadiaotoxicity
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Maprotiline
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What class of antidepressants is useful for anxiety disorders?
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SSRIs:
Venlafaxine Duloxetine |
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What class of antidepressants is useful for OCD?
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Fluvoxetine
Clomipramine |
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What class of antidepressants is useful for bed wetting (enuresis)?
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TCAs
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What class of antidepressants is useful for pain?
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TCAs
SSRIs: Venlafaxine & Duloxetine |
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What antidepressant is useful for smoking cessation?
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Bupoprion
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What antidepressant is useful for bulimia and premenstrual dysphoric disorder?
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Fluoxetine
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What antidepressant is useful for attention deficit hyperkinetic disorder? attention deficit hyperactivity disorder?
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Imipramine & desipramine
Atomoxetine |
