Drug Guide
Fezolinetant
Classification
Therapeutic: Vasomotor symptom treatment in menopause
Pharmacological: Selective neurokinin 3 receptor (NK3) antagonist
FDA Approved Indications
- Treatment of moderate to severe vasomotor symptoms associated with menopause
Mechanism of Action
Fezolinetant works by antagonizing neurokinin 3 receptors in the hypothalamus, which modulates the neurokinin B pathway involved in the regulation of hot flashes and other vasomotor symptoms.
Dosage and Administration
Adult: Initially, 45 mg orally once daily, can be adjusted based on response and tolerability.
Pediatric: Not indicated.
Geriatric: No specific dose adjustment recommended, but caution advised due to potential increased sensitivity.
Renal Impairment: Use with caution; no specific dose adjustment established.
Hepatic Impairment: Use is not recommended in severe hepatic impairment; adjust dose in mild to moderate impairment.
Pharmacokinetics
Absorption: Rapidly absorbed after oral administration.
Distribution: Widely distributed in tissues; volume of distribution not specified.
Metabolism: Primarily metabolized in the liver via CYP3A4 and CYP2C8 enzymes.
Excretion: Excreted mainly via feces and urine.
Half Life: Approximately 11 hours.
Contraindications
- Hypersensitivity to fezolinetant or any component of the formulation.
Precautions
- Use with caution in patients with hepatic impairment, as pharmacokinetics may be altered.
Adverse Reactions - Common
- Nausea (Unknown)
- Headache (Unknown)
- Vaginal bleeding (Unknown)
Adverse Reactions - Serious
- Elevated liver enzymes (Rare)
- Serious hypersensitivity reactions (Very rare)
Drug-Drug Interactions
- CYP3A4 inhibitors may increase fezolinetant levels; CYP3A4 inducers may decrease levels.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor vasomotor symptoms and liver function tests periodically.
Diagnoses:
- Risk for injury related to vasomotor symptoms.
Implementation: Administer orally once daily; advise patients to report any abnormal symptoms, especially signs of liver dysfunction.
Evaluation: Assess efficacy in reducing vasomotor symptoms and monitor for adverse effects.
Patient/Family Teaching
- Take medication as prescribed, at the same time daily.
- Report any symptoms of liver problems, such as jaundice or dark urine.
- Discuss potential side effects and the importance of regular liver function tests.
Special Considerations
Black Box Warnings:
- None currently issued for fezolinetant.
Genetic Factors: Unknown impact; no pharmacogenomic data available.
Lab Test Interference: None known.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, drowsiness, or other unexpected symptoms.
Treatment: Supportive care; there is no specific antidote. Consider gastric decontamination if ingestion is recent.
Storage and Handling
Storage: Store at room temperature, away from moisture and heat.
Stability: Stable under recommended storage conditions.