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