Drug Guide
Zuranolone
Classification
Therapeutic: Anxiolytic, Antidepressant, Antianxiety Agent
Pharmacological: GABA-A receptor positive allosteric modulator
FDA Approved Indications
- Treatment of postpartum depression in adult women
Mechanism of Action
Zuranolone is a positive allosteric modulator of GABA-A receptors, enhancing GABAergic inhibitory neurotransmission in the central nervous system, which results in anxiolytic and antidepressant effects.
Dosage and Administration
Adult: 100 mg once daily for 14 days, orally; dosing may vary based on clinical response and tolerability.
Pediatric: Not approved for pediatric use.
Geriatric: No specific dosage adjustments; start at lower doses if necessary, monitor closely.
Renal Impairment: No specific adjustments necessary; however, caution advised.
Hepatic Impairment: Data limited; use caution and monitor for adverse effects.
Pharmacokinetics
Absorption: Rapid absorption; peak plasma concentrations typically occur within 2 hours.
Distribution: Widely distributed; highly protein-bound.
Metabolism: Primarily metabolized by CYP3A4 and other liver enzymes.
Excretion: Excreted mainly via the feces and urine.
Half Life: Approximately 13-17 hours.
Contraindications
- Hypersensitivity to zuranolone or excipients.
Precautions
- Use with caution in patients with liver impairment; monitor hepatic function. Caution advised in patients with history of psychiatric disorders or suicidal ideation.
Adverse Reactions - Common
- Dizziness (Common)
- Somnolence (Common)
- Fatigue (Common)
Adverse Reactions - Serious
- Suicidal thoughts or behaviors (Rare)
- Severe allergic reactions (Rare)
- Hypersensitivity reactions including rash (Rare)
Drug-Drug Interactions
- CYP3A4 inhibitors or inducers may affect zuranolone plasma levels.
Drug-Food Interactions
- No significant food interactions identified.
Drug-Herb Interactions
- Caution with concomitant use of herbal products affecting CYP pathways.
Nursing Implications
Assessment: Assess for mood improvement and watch for adverse neurological effects including sedation and dizziness.
Diagnoses:
- Risk for injury related to dizziness or sedation.
- Imbalanced nutrition: less than body requirements if nausea or GI discomfort occurs.
Implementation: Administer as prescribed; monitor patient response and side effects.
Evaluation: Evaluate effectiveness through mood assessments; monitor for adverse reactions.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Do not operate heavy machinery until response is known.
- Report any suicidal thoughts or unusual side effects to healthcare provider.
- Avoid alcohol and CNS depressants.
Special Considerations
Black Box Warnings:
- Suicidality has been observed in patients taking drugs that modulate GABA receptors, particularly in young adults.
Genetic Factors: Genetic variations affecting CYP3A4 may influence drug levels.
Lab Test Interference: No known interference.
Overdose Management
Signs/Symptoms: Drowsiness, dizziness, confusion, respiratory depression in severe cases.
Treatment: Supportive care, airway management, monitor vital signs, activated charcoal if ingestion is recent, consider hospitalization.
Storage and Handling
Storage: Store at room temperature, away from moisture, heat, and light.
Stability: Stable under recommended storage conditions for the duration of efficacy.