fezolinetant

Contraindicated in:

Cirrhosis;
Severe renal impairment or end-stage renal disease;
AST, ALT, or total bilirubin ≥2 times upper limit of normal (ULN)
;
Concurrent use with CYP1A2 inhibitors.

Use Cautiously in:

None.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: hot flush

GI: ↑liver enzymes, abdominal pain, diarrhea, HEPATOTOXICITY

MS: back pain

Neuro: insomnia

Interactions ⬆ ⬇

Drug-drug:

CYP1A2 inhibitors, including fluvoxamine, mexiletine, and cimetidine, may ↑ levels and risk of toxicity; concurrent use contraindicated.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 45 mg once daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a neurokinin 3 receptor antagonist that blocks neurokinin B binding on the kisspeptin/neurokinin B/dynorphin neuron to regulate neuronal activity in the thermoregulatory center.

Therapeutic effects:

Reduction in frequency and severity of vasomotor symptoms due to menopause.

Classifications ⬆ ⬇

Therapeutic Classification: menopausal agents

Pharmacologic Classification:

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption unknown.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP1A2 isoenzyme, with some metabolism by the CYP2C9 and CYP2C19 isoenzymes. Primarily excreted in the urine (77%; 1% as unchanged drug), with 15% excreted in the feces (<1% as unchanged drug).

Half-Life: 9.6 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1–4 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient to take as directed. Take missed doses as soon as remembered, unless there is <12 hr before next dose is due. Return to regular schedule next day.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise patient to discontinue fezolinetant immediately and seek medical attention if signs or symptoms of liver abnormalities (new onset fatigue, ↓ appetite, nausea, vomiting, pruritus, jaundice, pale feces, dark urine, abdominal pain) occur.

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Indications ⬇

Contraind./Precautions ⬆ ⬇