Zuranolone

ZURZUVAE

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What it isOral neurosteroid GABA-A positive allosteric modulator; postpartum depression.

Why this oneA 14-day oral course with response in days, where brexanolone needs a 60-hour infusion.

What limits itDriving is prohibited for 12 hours after each dose. Sedation; Schedule IV, and effect beyond 45 days is unstudied.

FDA-approved for

postpartum depression (2023)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Causes driving impairment from CNS depression; do not drive or engage in hazardous activities for at least 12 h after each dose during the 14-day course.

FDA dosing	Population	Start	Target	Max
Postpartum depression	Adults	50 mg QHS ×14 days	50 mg QHS	50 mg QHS

Renal Moderate-severe (eGFR <60): 30 mg QHS ×14 days; mild: no change

Hepatic Severe (Child-Pugh C): 30 mg QHS ×14 days; mild-moderate: no change

14-day treatment course; safety/effectiveness beyond 14 days not established

Instructions

Take in the evening with fat-containing food (400-1000 cal, 25-50% fat)
Reduce to 40 mg QHS if CNS depressant effects occur
With a strong CYP3A4 inhibitor: reduce to 30 mg; avoid CYP3A4 inducers
Missed dose: take the next dose the following evening; do not double up
Use effective contraception during treatment and for 1 week after the final dose

Cautions

CNS depressant effects (somnolence, confusion) and driving impairment; additive with other CNS depressants; fall risk
Suicidal thoughts and behavior (worsening depression)
Embryo-fetal toxicity

Adverse reactions

Somnolence
Dizziness
Diarrhea
Fatigue
Nasopharyngitis
Urinary tract infection

Pregnancy May cause fetal harm based on animal studies (malformations, embryofetal/offspring mortality, neuronal death); human data insufficient.

Lactation Present in human milk at low levels (relative infant dose <1%).

⚠ BOXED WARNING

Impaired ability to drive for 12 hours after each dose

Cost, est. cash$15,000–$17,000/14-day course

Generic entry2037 est.

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability1 / 4

Sedation liability1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilitySexual/GI effects, hyponatremia, discontinuation and serotonin toxicity; overdose danger varies substantially by agent.

Mechanism of action: Zuranolone ballicule

Zuranolone ballicule: receptor binding, kinetics and half-life diagram

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Memory aids: mascots and interaction avatars

Zuranolone ZURZUVAE mascot mnemonic cartoon — **“Zu Zu Zu ran alone”**

CYP3A4 substrate

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