Term
| Antidepressants come in 3 classes, what are they? |
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Definition
Monoamine (such as serotonin or NE) uptake inhibitors
MAO inhibitors
Atypical |
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Term
| Mechanism of action common to all antidepressants? |
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Definition
on the molecular level: inhibition of uptake of 5-HT and/or NE (but not DA)
on cellular level: neutrophric hypothesis
Works genomically (hence delayed effects) |
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Term
| What are the 1st generation NE/5HT uptake blockers? |
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Definition
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Term
| What other properities do TCAs have (what receptors can by antagonize) |
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Definition
| muscarinic (ACh), histaminergic, and a1-adrenergic antagonist properties and block some ion channels |
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Term
| How do the TCAs make it through the BBB? |
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Definition
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Term
| How long does it take for the TCA to take effect? |
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Definition
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Term
CNS side fx of TCAs:
therapeutic and high doses |
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Definition
sedation (a1 or H1 antagonist effects)
insomnia, restlessness, fine hand tremor (M effects)
high doses: mania in ppl w/ bipolar, seizures in ppl prone to epilepsy, toxic psychosis (anticholinergic effect) |
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Term
| Peripheral side effects of TCA |
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Definition
3 things: cardio, autonomic, constitutional
cardio: orthostatic hypotension (a1 blockade) and reflex tachycardia; direct cardiac toxicity w. quinidine-like effect
Autonomic: cholinergic blockade (dry mouth, pupil dilation, blurred vission, exacerbation of narrow angle glaucoma, urinary retention, consitpaiton, impotence
Constitutional: weight gain |
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Term
| Overdose of TCA causes... |
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Definition
| arrhythmias, hypotension, seizures, coma |
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Term
| lethal dose of TCAs is how many times the daily dose? |
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Definition
| 10-20x (only prescribe a weeks supply worth) |
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Term
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Definition
unipolar (major) depression, panic disorder
adjunctive tx in chronic pain, sleep disorders, OCD (clomipramine only) |
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Term
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Definition
| clomipramine, imipramine, desipramine, amitryptiline |
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Term
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Definition
| fluoxetine, fluvoxamine, paroxetine, sertraline |
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Term
| What are the atypical antidepressants? |
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Definition
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Term
| What are the non selectie MAOIs? |
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Definition
| phenelzine, tranylcypromine |
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Term
| What is the selective MAOI-B? |
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Definition
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Term
| Imipramine is what kind of drug? |
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Definition
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Term
| desipramine is what kind of drug? |
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Definition
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Term
| amitryptiline is what kind of drug? |
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Definition
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Term
| clomipramine is what kind of drug? |
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Definition
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Term
| fluoxetine is what kind of drug? |
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Definition
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Term
| Sertraline is what kind of drug? |
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Definition
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Term
| paroxetine is what kind of drug? |
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Definition
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Term
| fluvoxamine is what kind of drug? |
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Definition
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Term
| bupropion is what kind of drug? |
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Definition
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Term
| tranylcypromie is what kind of drug? |
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Definition
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Term
| phenelzine is what kind of drug? |
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Definition
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Term
| selegiline is what kind of drug? |
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Definition
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Term
| t or f? fluoxetine has effects on a-1 adrenergic, histamine, muscarinic activity? |
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Definition
| false. it is a selective 5-HT blocker |
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Term
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Definition
| no urinary excretion, purely hepatic metabolism |
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Term
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Definition
| 2 days (due to zero urinary excretion) |
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Term
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Definition
| nausea, insomnia, sexaul side effects |
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Term
| What would happen if you combined SSRIs with MAOIs? |
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Definition
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Term
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Definition
| major depression, anxiety disorders, panic disorder, OCD |
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Term
compare TCAs and SSRIs in terms of:
therapeutic index
side effects
effectiveness |
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Definition
therapeutic index: SSRIs have much larger
side effects: SSRIs don't have the side effects that TCAs do (b/c they have no effect on alpha1, H1, M receptors)
tca's more effective in tx severe depression |
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Term
| Mechanism of action: bupropion |
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Definition
| NE uptake inhibitor structurally related to amphetamines so it is a stimulant rather than sedative |
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Term
| Side effect profile: bupropion |
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Definition
no cardiac or anti-ACh effects, no wt gain, no sexual dysfunction
highly prone to seizures in susceptible individuals and may cause HT |
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Term
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Definition
depression assoc w. psychomotor retardation
at lower dose, attenuate discomfort of nicotine withdrawal |
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Term
| where are the MAOs located in the body? |
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Definition
| where the two nervous sys are: CNS and gut |
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Term
| mechanism of action: MAOIs |
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Definition
| MAO inhibition increases synaptic levels of 5-HT especially well (only degradative enzyme for it). effect on DA or NE is slight |
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Term
| What is the wine and cheese syndrome? |
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Definition
| a severe hypertensive crisis that results from potentiation of indirectly acting sympathomimetic amines (in food or drugs) b/c MAO is being inhibited in the periphery |
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Term
| What is the serotonin syndrome? |
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Definition
| basically excessive 5HT leads to hyperthermia, muscle rigidity, myoclonus |
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Term
| What are the 4 drug-drug interactions you have to watch out for when administering an MAOI? |
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Definition
1. sympathomimetic amines (wine and cheese syndrome)
2. serotonin uptake inhibitors (serotonin syndrome)
3. levo-DOPA - agitation (Central) and hyptertension (peripheral)
4. Meperidine (serious potentially fatal interaction - it is an opiod mu agonist. Mu receptors when activated are responsible for producing spinal/supraspinal analgesia, euphoria, respiratory depression, miosis, and constipation) |
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Term
| Used for: non selective MAOI |
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Definition
2nd/3rd line drugs in unipolar depression
Narcolepsy (b/c of REM sleep suppression)
Parkinson's disease |
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Term
| Which AD recently started coming in a transdermal formation and has a low risk of HT crisis? |
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Definition
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