Antidepressant Agents

Front 1

major classes of antidepressants?

Back 1

TCA
2nd/3rd generation AD
SSRIs
MAO-I

Front 2

cellular target of MAO-Is?

Back 2

inhibit activity of MAO-A and to some extent MAO-B; MAO-A degrades NE and 5-HT; MAO-B degrades DA; results in increased amount of neurotransmitter in the presynaptic vesicle

Front 3

what does MAO-A degrade?

Back 3

NE, 5-HT

Front 4

what does MAO-B degrade?

Back 4

DA

Front 5

seligilene (eldepryl)?

Back 5

selective MAO-B inhibitor

Front 6

phenylzine (nardil)?

Back 6

irreversible inhibition of MAO-A and B

Front 7

tranylcypromine (parnate)?

Back 7

prolonged inhibition of MAO-A, but not irreversible

Front 8

toxic effects of MAO-Is?

Back 8

postural hypotension (secondary to desensitization of peripheral α receptors); insomnia, impotence (secondary to excessive autonomic activity); weight gain (uncertain); fatal hypertensive crisis (secondary to symphatomimetic amine ingestion); hyperpyrexia, convulsions (idiosyncratic administration of meperidine); serotonin syndrome (concomitant use of more than one antidepressant)

Front 9

most important toxic effect of MAO-Is?

Back 9

fatal hypertensive crisis secondary to sympathomimetic amine ingestion (tryamine, phenylpropanolamine, ephedrine)

Front 10

what substances should be avoided with MAO-Is to avoid fatal hypertensive crisis?

Back 10

tyramine, phenylpropanolamine, ephedrine

Front 11

cellular target of TCA?

Back 11

inhibit NE and/or 5-HT reuptake pumps causing an increase in synaptic concentrations

Front 12

amitriptyline (elavil)?

Back 12

TCA

Front 13

imipramine (tofranil)?

Back 13

TCA

Front 14

toxicity and side effects of TCAs?

Back 14

sympathomimetic: arrythmia, tremor, insomnia;
antihistaminic: initial sedation (developed tolerance after 1-2 weeks);
antimuscarinic: dry mouth, blurred vision ,tachycardia, urinary retention;
overdose: cardiac conduction defects

Front 15

which compound are TCAs chemically related to and what is the consequence?

Back 15

phenothiazines --> retain some adrenergic, cholinergic, and histmine receptor blockade

Front 16

which drugs enhance TCA effects by interfering with hepatic metabolism?

Back 16

antipsychotics
methylphenidate

Front 17

which drugs reduce TCA effects by increasing hepatic metabolism?

Back 17

barbiturates

Front 18

TCA interact with which compounds to cause serotonin syndrome?

Back 18

MAO-I
SSRIs

Front 19

general characteristics of second/third generation antidepressants?

Back 19

inhibit 5-HT > NE reuptake, and have fewer promiscuous receptor blockage activity

Front 20

which antidepressant has a unique mechanism?

Back 20

mirtazipine: blocks 5-HT and α2 receptors

Front 21

trazodone?

Back 21

directly inhibit 5-HT receptors
inhibit 5-HT > NE reuptake

Front 22

side effects of trazodone?

Back 22

priapism and drowsiness due to blockage of α1 and H1 receptors respectively

Front 23

nefazodone?

Back 23

directly inhibit 5-HT receptors
inhibit 5-HT > NE reuptake

Front 24

venlafaxine?

Back 24

5-HT >> NE pump inhibition
some DA reuptake inhibition
well tolerated
effective in treatment of major depression and anxiety disorders

Front 25

bupropion (wellbutrin; zyban)?

Back 25

unknown mechanism
weak inhibition of monoamine reuptake

Front 26

side effects and contraindications for bupropion?

Back 26

dose-dependent increase in seizures;
contraindicated in patients taking zyban for smoking cessation and epileptics

Front 27

amoxapine?

Back 27

metabolite of an antipsychotic (loxapine);
associated with extrapyramidal side effects

Front 28

maprotiline?

Back 28

potent NE reuptake inhibitor;
few sedative side effects

Front 29

mirtazipine?

Back 29

blocks 5-HT and α2 receptors (unique);
blocks H1 receptor causing sedation;
significant weight gain

Front 30

SSRIs mechanism?

Back 30

inhibition of 5-HT pump;
long half-life and active metabolites

Front 31

fluoxetine (prozac)?

Back 31

SSRI

Front 32

toxicity and side effects of SSRIs?

Back 32

5-10% incidence of nausea, insomnia, anxiety, decreased libido, ED (secondary to excessive 5-HT, generally develop tolerance)

Front 33

use of lithium?

Back 33

preventing manic episodes; not used for acute treatment of manic phase

Front 34

mechanism of action of lithium?

Back 34

depress noradrenergic or serotonergic transmission by decreasing the formation of postsynaptic second messengers (inositol triphosphate and diacyllycerol)

Front 35

what is lithium intoxication associated with?

Back 35

sodium depletion: severe diarrhea, sweating, fever, low Na diet, thiazide diuretics, NSAIDs

Front 36

side effects of lithium?

Back 36

initial: GI irritation, muscular weakness, tremors, edema;
1.5-3 mEq/L: ataxia, drowsiness, muscle rigidity;
3 mEq/L: cardiac arrythmia, seizures, coma;
nontoxic goiter;
nephrogenic diabetes insipidus

Front 37

in what heart condition is lithium contraindicated?

Back 37

sick sinus syndrome (depress sinus node)

Front 38

drug interactions with lithium?

Back 38

diuretics, particularly thiazides: Na depletion leads to Li retention;
NSAIDs: increase Li reabsorption

Front 39

general relationship of renal lithium excretion to sodium intake?

Back 39

Na loading causes an increase in Li excretion whereas Na depletion causes Li retention