Behav Med Pharm I
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| SSRI MOA | Selectively inhibit 5-HT reuptake by blocking 5-HT transporter | ||||
| SSRI: Most potent SSRIs re: blocking 5-HT transporter | paroxetine & citalopram | ||||
| SSRIs that produce effect on NE: | Fluoxetine and paroxetine (doses > 40mg) | ||||
| SSRIs: Advantages | Low affinity for histamine- 1, alpha-1, muscarinic (M) rec; so low sedation, no orthostasis, dry mouth or CV issues | ||||
| SSRI w/longest half life | fluoxetine | ||||
| Most common AE reason for SSRI early DC | GI problems (titrate slowly, take w/meals) | ||||
| most common SSRI AE when starting drug | Akathisia (esp w/fluoxetine) | ||||
| Tx for SSRI akathisia | Start low, early AM, benzo, trazo, propanolol | ||||
| Sexual dysfn greatest/least with: | greatest: paroxetine; least: citalopram | ||||
| SSRI AE: sedation greatest with: | paroxetine (d/t anticholinergic properties) | ||||
| Serotonin syndrome S/S | Hyperreflexia, tremor, GI complaints, CV problems, seizures, respiratory depression, coma, death; concern re: SSRI combo w/other drugs | ||||
| SSRI withdrawal S/S | Nightmares, flu-like symptoms, GI, shock-like sensations, & insomnia (seen usually in 2 to 7 days after abrupt d/c) | ||||
| SSRI withdrawal worst with: | paroxetine & sertraline (switch to fluox?) | ||||
| SSRI benefit seen in: | atypical, psychotic, and dysthymia | ||||
| Fluoxetine effective dose range | 20-40 mg/day | ||||
| Wt gain: SSRIs with greatest/least | Least: fluox; greatest: paroxetine | ||||
| Paroxetine effective dose range | 30-50 mg/day | ||||
| Citalopram/escitalopram effective dose range | 20-60 mg/day | ||||
| Lexapro effective dose range | 10-20mg/day | ||||
| Classes: equal in depression tx | SSRI, SNRI, atypicals | ||||
| SNRI MOA | Block reuptake of 5-HT and NE (& DA) | ||||
| SNRI MOA: Venlafaxine only produces effects on NE at: | a higher dose (so push dose pretty high) | ||||
| SNRI MOA: Duloxetine has a high level of effect on: | both 5-HT and NE | ||||
| SNRI good to tx: | refractory depression, melancholy; more physical pain sx of depn; comorbid pain (duloxetine: DM periph neuropathy) | ||||
| SNRI AE profile (which worse?) | Venlafaxine > duloxetine | ||||
| SNRI side fx | GI (1st 3 wks); HTN (dose-dept (DBP) venlafaxine); withdrawal sim to SSRI | ||||
| Use venlafaxine IR cautiously in pts with: | HTN & cardiac dysfunction (use dulox or venla XR) | ||||
| Mirtazapine (atypical) MOA | unique: blocks central alpha-2 recs increasing NE & 5-HT; antag 5-HT2, 5-HT3 post-synaptic recs | ||||
| Mirtazapine AE | Somnolence, wt gain/inc appetite (used in cachectic pts), ortho hypotn | ||||
| Bupropion MOA | Weak reuptake inhibitor of NE and DA | ||||
| Bupropion active metabolite: | hydroxybupropion; has amphetamine properties (potent reuptake inhibitor of both NE and DA) | ||||
| Bupropion AE | Lower seizure threshold; vivid nightmares, delusions, psychosis | ||||
| Do not give Bupropion to pts with: | eating disorders (low electrolytes): seizure risk | ||||
| Bupropion dosing | Highest dose s/b usu 300; dose at early AM and noon (d/t insomnia, etc) | ||||
| Atypical: good option for pts with sedation / fatigue / sexual dysfunction | Bupropion | ||||
| TCA MOA | Block the reuptake of 5-HT and N; 1stGen: greater effect on 5-HT reuptake (Doxepin); 2ndGen: greater effect on NE reuptake (esp desipramine; clomipramine) | ||||
| TCAs with best blockade of alpha- 1 & histamine- 1 recs: | Amitriptyline & doxepin | ||||
| TCA AE | Anticholinergic (dry mouth, urin hesitancy, GERD; Cardiovascular (ortho hypotn, tachy, conduction, HTN); CNS (tremor, sedation, myoclonic twitch); wt gain; sexual dysfn | ||||
| TCA dosing | Start at low dose, titrate slowly, switch to less offensive agent; Bethanechol for anticholinergic AE; lethal in OD | ||||
| MAOI MOA | Block destruction of monoamines by presynaptic neuronal MAO; effect both central & periph; MAO-A = on NE & 5-HT; MAO-B = on phenylethylamine & DA | ||||
| Irreversible MAO-I = | Phenelzine & tranylcypromine | ||||
| MAOI AE | Wt gain; rash (selegiline); diet restrictn (liver, cheese, wine, yeast) | ||||
| STAR-D General findings | 6 wks necessary for pts achieve response; pts unable to tolerate med preferred switch; pts able to tolerate med preferred augmentation | ||||
| STAR-D: Buproprion-SR: | better results than buspirone | ||||
| STAR-D Level 1 | start citalopram | ||||
| STAR-D Level 2 | switch to: buprop SR, CBT, sert, venla XR; or augment w/bupro SR, buspar, CBT | ||||
| STAR-D Level 2a | (if CBT in level 2): switch to: buprop SR or venla XR | ||||
| STAR-D Level 3 | switch to mirtaz or nortrip; or augment w/lithium (poss T3 if bupro, sert, venla) | ||||
| STAR-D Level 4 | switch to tranylcypromine or mirtaz combo w/venla XR |
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Created by:
Abarnard
on 2010-01-24