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53 Cards in this Set
- Front
- Back
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TCAs - list
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Amitriptyline, Desipramine
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TCAs - mechanism
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-block neuronal reuptake pumps for 5HT and NE. Causes increased [] in synapse
-blocks many NT receptors - e.g., muscarinic, cholinergic, alpha1, H1 (source of side effects) |
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TCAs - side effects
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drowsiness, constipation, dry mouth
side effects get better w/ time HEART - causes tachycardia, palpiations --orthostatic hypotension --increases appetite / weight gain --impotence - delayed orgasm |
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TACs are particularly good for what?
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melancholic depression
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TCAs - OD?
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low TI
potential for fatal OD with arrythmias, acidosis, delerium, seizures |
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TCA OD Tx?
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lavage (not dialysis)
lidocaine for arrythmias |
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Which TCA has the most adverse effects and highest cardiac toxicity?
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Amitriptyline
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Which TCA has the best overall adverse effect profile?
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Desipramine
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SSRIs - list?
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Fluoxitine, Paroxitine, Sertraline
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SSRI - mechanism
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selectively block reputake of 5HT
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SSRI - any effect on NE reuptake?
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No!!!
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SSRI - TI higher or lower than TCAs?
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higher
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SSRI - side effects?
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initially - GI upset, CNS stimulation. Note this is due to increased 5HT levels, and typically improve with time. This has nothing to do with receptor levels.
-CNS stim causes insomnia, anxiety, headache -sexual side effects. |
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SSRIs - indications?
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anxiety disorders, eating disorders, ATYPICAL DEPRESSION, pain, ADD/ADHD
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SSRI side effects - c.f. TCAs
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NO sedation, heart effects (including arrhythmias), no vascular effects, NO cardiac tox
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Fluoxitine unique how?
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very long lasting metabolite (norfluoxitine)
very long half life (can take 1x/week) CYP inhibitor. Thus is can increase [] of other drugs in blood be caseful with St John's Wort and MAOIs! |
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SSRI OD toxicity?
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"seratonin syndrome" = hyperthermia, muscle rigidity, myoclonus, fluctuations in vital signs and mental status.
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Tx for OD of SSRI?
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supportive... not dialysis
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Paroxitine - unique side effects
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increased sexual side effect frequency.
weight gain Category D in pregnancy (not safe) inhibits CYP enzyme metabolism. |
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SNRI list
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Venlafaxine
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SNRI mechanism
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inhibits 5HT AND NE!!!
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What happens when you discontinue SNRIs?
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Discontinuation Syndrome: sweating, tachycardia, urinary retention, increased BP.
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Bioavailability of SNRI?
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bioavailability is LOW because it is not highly protein bound. Therefore half life is short.
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MAOI list
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Tranylcypromine
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MAOI mechanism
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IRREVERSIBLY inhibit MAO - this increases NE and 5HT in nerve terminals.
Note enzymes must be regenerated to work again. |
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MAOI - location of action (periphery vs brain)
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Both.
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MAOIs useful for what?
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useful for "atypical" depression
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MAOI adverse effects
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orthostatic hypotension
CNS stimulation GI distress sexual dysfunction DRUG INTERACTIONS!!! Note there are not cardiac tox, sedation, anticholinergic effects |
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Tranylcypromine is metebolized into what?
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amphetamine
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OD toxicity of Tranylcypromine?
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uncommon. includes agitation, delerium, coma, hyperthermia, shock, seizures.
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MAOI drug interactions
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dextromethorphan and meperidine results in severe tox / fatality.
Tyramine syndrome - acute hypertensive crisis. Note interactions with MAOIs makes changing drugs difficult as you must wait 2-5 weeks to switch. |
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Bupropion mechanism
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inhibits reuptake of DA, 5HT, NE
little to no effect on NT receptors. |
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Bupropion useful for what?
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smoking cessation, depression
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Bupropion - unique side effect
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high potential for seizures
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Nefazadone - mechanism
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5HT receptor antagonist
5HT reputake block NT receptor block: 5HT2, a1 Note the 5HT2 receptor block produces theraputic response. |
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Nefazadone - important side effect
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sedation is prominent
possible hepatotox |
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Nefazadone bioavailability?
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low, but produces active metabolites.
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Mirtazapine mechanism
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NT receptors: block presynaptic autoreceptors (alpha2, 5HT1a) that inhibit NE and 5HT release.
efficacy is due to increased NE and 5HT it does block other receptors, causing side effects (Ach, alpha1) |
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Mirtazapine - does it block reuptake?
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NO!
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Mirtazapine - side effects
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sedative
weight gain dizziness anticholinergic (dry mouth, constiptation) |
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Lithium - indication
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used for maintenance of bipolar.
adjunct with ADs for tx of depression NOT!!! useful for use in acute manic episode!!! |
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Lithium - theraputic index?
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Very low! Thus, there are many adverse effects
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Lithium adverse effects
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tremor
sedation / fatigue hypothyroidism edema (due to increased aldo) rephron inflammation, loss of ADH effectiveness |
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Lithium drug interactions
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Na+ depleting diuretics.
Note that Li increases Na excretion, which causes a decrease in Li extretion. Also NSAIDS, ACE, mannitol |
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Valproic acid - used for what?
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anticonvulsant
mood stabilizer for tx of mania |
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Is haldol useful for Tx of affective disorders?
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yes - for mania.
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Do SSRIs have any effect on NT receptors?
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NO!
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SSRIs - bioavailability?
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high due to being protein bound
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Name an autoreceptor antagonist
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Mirtazapine
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Name a dopamine reputake inhibitor
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Bupropion
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Name a serotonin receptor antagonist
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Trazodone
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Source of TCA orthostatic hypotension?
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alpha1 receptor block!
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What characterizes atypical depression?
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mood reactivity
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