Chapter 3 CNS - serotonin-norepinephrine uptake inhibitors

Question 1

Nefazodone (serzone)

Answer 1

• inhibits uptake of serotonin and norepinephrine

indication
* depression

effects
* rash, HTN, tachycardia, SOB, many CNS effects, decreased appetite, priaprism (refer to trazodone)
* life-threatening hepatic failure occurs rarely

PO, twice daily, reduce dose with liver dysfunction, metabolized extensively by liver!

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can increase effect of triazolam (halcion) and alprazolam (xanax)

• CONTRAINDICATED WITH CISAPRIDE (GERD tx heartburn) or PIMOZIDE (ORAP) — antipsychotic

Question 2

Venlafazxine (effexor)
Desvenlafaxine (pristiq)

Answer 2

• inhibits 5-HT and NE uptake

indication
* anxiety, depression

effects
* sustained HTN
* photosensitivity

PO, 2-3 doses/day, reduce dose w/ renal and hepatic problems
* active metabolite — o-desmethylvenlafaxine

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Increase effects of triazolam (halcion) and alprazolam (xanax)

Question 3

Duloxetine (cymbalta)

Answer 3

• inhibits 5-HT and NE uptake

indication:
* depression
* diabetic neuropathic pain

effects:
* hepatotoxicity
* sexual dysfunction

PO

substrate CYP2D6 and 1A2

Question 4

Milnacipran (savella)
Levomilnacipran (fetzima)

Answer 4

• inhibits 5-HT and NE uptake

indication:
* depression
* fibromyalgia (chronic (long-lasting) disorder that causes pain and tenderness throughout the body, as well as fatigue and trouble sleeping)

effect
* suicide risk, serotonin syndrome, HTN

PO

CONTRAINDICATED with monoamine oxidase inhibitors
Isocarboxazid (Marplan)
Phenelzine (Nardil)
Selegiline (Emsam)
Tranylcypromine (Parnate)

minimal CYP450 metabolism

Levomilnacipran (same except for contraindication)