Antidepressants Flashcards
First Gen drugs
tricyclics and MAO inhibitors
2nd and 3rd Gen drugs
tetracyclics and unicyclics; 5-HT2 antagonists; SSRI; SNRI
drugs that inhibit 5-HT reuptake w/ greater potency but not technically SSRIs
trazodone and venlafaxine
drug that inhibits NE reuptake w/ greater potency
maprotiline
drugs that have little effect on re-uptake of either 5-HT or NE
bupropion and mirtazapine
tricyclic dibenzazepine tertiary amine
imipramine
tricyclic dibenzazepine secondary amine
desipramine
tricyclic dibenzocycloheptadiene tertiary amine
amitriptyline
tricyclic dibenzocycloheptadiene secondary amine
protriptyline
tricyclic dibenzoxepine tertiary amine
doxepine
probably primary action of alleviation of depression of TCAs
blockage of NE reuptake
sedative effects of TCAs are enhanced by …
CNS depressants
co-administration of TCAs with … can lead to sever hyperpyrexia, hypertension, tremors, convulsions, coma or death
MAOIs
inhibitors of cytochrome P450 … will increase concentration of TCAs
erythromycin, clarithromycin, fluoxetine
inducer of cyp-450
carbamazepine
MAOIs of both MAO A and B
phenelzine and trancylcypromine
located in gut and peripheral tissues; preferentially oxidizes 5-HT, but not NE or dopamine
MAO-A
located in platelets; preferentially metabolizes dopamine
MAO-B
MAOIs block metabolism of … and other amines found in aged cheese, beer and chianti, may escalate levels of monoamines
L-dopa
if MAOIs are given with other anti depressants (esp. SSRIs) may cause …
malignant serotonin syndrome
1st clinically available atypical; tetracyclic; used to treat psychoses and mood disorders; blocks NE greater than 5-HT; sedation and may cause seizures
maprotiline
N-demethylated metabolite of antipsychotic drug loxapine; action resembles secondary amine TCAs but also blocks dopamine and 5-HT2a; anticholinergic and parkinsons like side effects
amoxapine
triazole derivatives; inhibition of 5-HT2a; weak re uptake inhibition of serotonin and NE; short plasma half life; treatment of depression, insomnia of SSRIs, panic attacks; sedation, CV side effects, priapism of males
trazodone and nefodazone
aminoketone; weak inhibitor of NE, 5-HT and DA re-uptake; depression; smoking cessation; seasonal affective disorder; agitation; insomnia, anorexia and weight loss, seizures
bupropion
blocks presynaptic A2 receptors; increases amine release by removing feed back inhibition; no effect on serotonin re uptake; CV effects (serious), sedation, dry mouth, blurred vision, weight gain
mirtazapine
SSRIs
fluoxetine, sertraline, paroxetine, citalopram, escitalopram
half life and daily dose of fluoxetine
70 and 20-80
half life and daily dose of sertraline
25 and 50-200
half life and daily dose of paroxetine
20 and 10-50
half life and daily dose of citalopram/escitalopram
35 and 20-40
fluoxetine taken with lithium, TCAs, warfarin
increased action of 2nd drug
fluvoxamine taken with alprazolam, theophylline, TCAs and warfarin
increased blood levels of 2nd drug
MAOIs taken with SSRIs, food containing tyramine
hypertensive crisis, serotonin syndrome
nefazodone taken with alprazolam, triazolam
increased blood levels of 2nd drug
paroxetine, sertraline taken with warfarin, TCAs
increased blood levels of 2nd drug
TCAs taken with sedative/hypnotics, ethanol
increased CNS depression
highly sedating
amitriptyline, doxepin, trazadone, mirtazapine
anti muscarinic effects
amitriptyline and doxepin
SSRIs generally lack … and are safe in overdose
sedating activities
main line drug of bipolar disorder
lithium salts
diabetes insipidus
chronic toxicity of lithium salts
plasma levels of lithium are elevated by
thiazide diuretics (chlorothiazide) and ACE inhibitors (catopril)
NSAIDs decrease …
renal excretion
alcohol and caffeine promote …
lithium excretion
