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TCA - tertiary amine, very sedating due to blockade of H1 |
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TCA - secondary amine, active metabolite of imipramine, preferentially blocks NE |
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TCA - secondary amine, active metabolite of amitryptyline that preferentially blocks noradrenergic reuptake |
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TCA - tertiary amine, preferential NE blocker |
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block the reuptake of serotonin and norepinephrine from respective serotonin and noradrenergic terminals |
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65+ or with other CNS depressants |
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Which TCAs have the greatest SE? |
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tertiary SE > secondary SE anti-Ch, anti-a1, anti-H1, weight gain, sexual dysfunction |
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Prozac = SSRI longest half life (2-4 days and its active metabolite lasts 7-15 days) least 5-HT selective |
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Zoloft = SSRI high protein binding |
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Paxil = SSRI highest affinity for 5-HT transporters |
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Lexapro = SSRI the S isomer of citalopram, more selective than citalopram |
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Luvox = SSRI most drug-drug interactions due to inhibition of CYP1A2, 2C19, 2D6, 3A4) shorter half life |
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blocks 5HT reuptake all have nearly equivalent therapeutic effects in treating depression |
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Which SSRIs have the most interaction with CYP proteins? |
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Definition
fluoxetine and fluvoxamine |
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sexual dysfunction, discontinuation syndrome |
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Which SSRI is the most teratogenic, causing CV defects in fetus? |
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SNRI SE - sexual dysfunction, HTN |
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SNRI active metabolite of venlafaxine, only undergoes Phase II metabolism |
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SNRI approved for MDD and peripheral neuropathic pain. may be effective for fibromyalgia |
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selective and comparable inhibition of 5-HT and NE reuptake |
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Mixed Action (atypical) Antidepressant
a2-adrenergic receptor antagonist. Enhances NE & 5-HT release via blockade of these inhibitory receptors on NE & 5-HT terminals. SE - sedation (due to H1 antagonism) |
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Mixed Action (atypical) Antidepressant
High affinity selective blockade of 5-HT transporters, high affinity partial agonist at 5-HT1A receptors |
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Mixed Action (atypical) Antidepressant
High affinity selective blockade of 5-HT transporters, high affinity full agonist at 5-HT1A, partial agonist at 5-HT1B. High affinity antagonist at 5-HT3 & 5-HT7. |
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Mixed Action (atypical) Antidepressant
No clearly est target sites of action. Also marketed as Zyban for quitting smoking. No anticholinergic, antihistaminergic or orthostatic hypotensive effects. Weight loss. No effect on sexual function. May have ‘energizing’ or stimulatory effects. Potential seizures at high doses. |
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Mixed Action (atypical) Antidepressant
5-HT reuptake inhibitor and a 5-HT2A receptor antagonist. Less effective than other AD. Serzone (tradename) removed from market due to potential liver toxicity, but still available as a generic drug. |
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What class of drugs are indicated for atypical depression? (as well as MDD and anxiety) |
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MAO - irreversible
long duration of action – 10-14 day washout required |
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MAO - irreversible
long duration of action – 10-14 day washout required |
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MAO - irreversible
a preferential MAO-B inhibitor. Emsam® is the transdermal patch, which does not require a modified diet at the lowest dose |
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MAO - reversible shorter duration of action than irreversible MAOIs. Less likely to interact with tyramine. |
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binds/inhibits the enzymes (MAO-A & MAO-B) that metabolize the monoamines & tyramine. Binding may produce either irreversible (most MAOIs) or reversible enzyme inhibition. |
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Serotonin Syndrome = myoclonus, autonomic dysfunction, hyperactive reflexes, unstable BP, hyperthermia, disorientation. Due to interactions with drugs that lead to a major inc in 5-HT – eg. SSRI + MAOI.
Hypertensive Crisis – potentially lethal; due to dietary and/or drug interactions |
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How does a pt switch from SSRI (or other antidepressant) to an MAOI? |
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Definition
discontinue by tapering down. Wait for 2 weeks before safely beginning of MAOI. Need a longer washout with fluoxetine. |
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How does a pt switch from an MAOI to another antidepressant? |
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Definition
discontinue irreversible MAOI and wait at least 2 weeks before beginning new med or discontinue reversible MAOI and wait 48 hours before beginning new med |
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DOC to treat initial anxiety attack? |
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paradoxical excitement, confusion, tolerance/dependence, withdrawal, sedation, antereograde amnesia |
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Binding to Benzodiazepine Receptors (BZ1 & BZ2) located on subunits of the GABAa Receptor Complex. Binding of BZs increases the affinity of GABA for it’s binding site on the GABAa receptor which increases the frequency of opening of chloride channels. Increased intracellular chloride hyperpolarizes the cells resulting in an overall inhibitory effect. |
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partial 5-HT1A agonist Requires desensitization of 5-HT1A inhibitory autoreceptors on 5-HT neurons, thus has a delayed therapeutic response. Also acts as a D2 antagonist. |
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What bipolar drug is effective in all phases of the illness? |
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proposed MOA for lithium? |
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Definition
may inhibit enzymes of inositol recycling, which depletes the substrate (PIP2) for IP3 and DAG production. This effect on second messengers that mediate NT action causes an inc in 5-HT effects and dec in NE/DA effects. |
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what is the only proven drug to reduce suicide in bipolar pts? |
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slurred speech, ataxia, fine tremors, excessive thirst and urination, renal toxicity, inhibition of thyroid hormone secretion, Li+ toxicity in newborns |
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renal impairment, elderly, pregnant women |
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What three anticonvulsants are used in the treatment of bipolar? |
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Definition
valproic acid, carbamazepine, lamotrigine |
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bipolar drugs that inhibits metabolism of phenytoin, Phenobarbital and carbamazepine? |
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Which bipolar drug has the most antidepressant effect? |
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Which bipolar drug can cause SJS or TEN? |
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which bipolar drug inc risk of cleft lip/palate during 1st trimester? |
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which bipolar drug inc risk of spina bifida? |
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Definition
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Definition
combo olanzapine and fluoxetine used to treat bipolar |
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treatment of immediate effects of alcohol withdrawal? |
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benzos -- diazepam is assoc with less of a chance of recurrent withdrawal but lorazepam is good for pts with cirrhosis |
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psychostimulants, atomoxetine |
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Li, carbamazepine, valproic acid, atypical antipsychotics |
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treatment of anorexia nervosa? |
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paroxetine and martazipine |
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SSRIs, SNRIs, TCAs, buspirone |
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treatment of depression with insomnia? |
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treatment of depression in a smoker trying to quit? |
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treatment of depression in elderly? |
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treatment of MDD with psychotic features? |
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SSRIs or clomipramine (TCA) |
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treatment of panic disorder? |
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treatment of social phobias? |
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treatment of schizophrenia? |
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treatment of Tourette's syndrome? |
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Definition
antipsychotics (haloperidol, risperidone) |
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venlafaxine, duloxetine, paroxetine, escitalopram |
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traditional antipsychotics (EPS only for haloperidol) |
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SE: retinal deposits/retinopathy |
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SE: Ebstein's cardiac anomaly |
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Lithium side effects Movement tremor Nephrogenic diabetes insipidus hypOthyroidism Pregnancy problems |
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SSRI with TCA, SNRI, MAOI, dextromethorphan or St. Johns |
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SE: diabetic peripheral neuropathy |
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SE: 3 C's = convulsions, coma, cardiotoxicity |
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SE: HTN crisis w/ tyramine |
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common SE of clozapine, desipramine, and bupropion? |
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