SERZONE
Pronunciation: nef-AY-zoe-doen


What it isSerotonin 5-HT2 antagonist and reuptake inhibitor; depression.
Why this oneIt causes little sexual dysfunction and does not suppress REM sleep, unlike most antidepressants.
What limits itRare but fatal hepatic failure ended its widespread use. A strong CYP3A4 inhibitor.
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Depression | Adults | 200 mg/day BID | 300–600 mg/day BID | 600 mg/day |
| Depression | Elderly/debilitated | 100 mg/day BID | titrate to response | 600 mg/day |
Titration Increase in increments of 100–200 mg/day at intervals of no less than 1 week
Renal Undefined
Hepatic Undefined (contraindicated if prior nefazodone-associated liver injury)
Available strengths
Pregnancy Category C; use only if potential benefit justifies risk to fetus
Lactation Undefined
Generic entry2003
⚠ BOXED WARNINGS
Legacy pregnancy categoryC
Defining liabilityRare but potentially fatal hepatic failure and clinically important CYP3A inhibition.
This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.
Not a clinically significant SRI; receptor antagonism is not serotonin elevation.
It binds the serotonin transporter, and its SERT peg is drawn to that textbook affinity. The pale halo around the peg marks binding that, by Gillman’s human-effect criteria, does not produce clinical serotonin reuptake inhibition.
Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.
Non-elevating action5-HT2A antagonist
Evidence confidenceHigh
Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.
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