General

Pronunciation:
fez-oh-lin-e-tant

Trade Name(s)

• Veozah

Ther. Class.

menopausal agents

Pharm. Class.

temporary class

Indications

Moderate to severe vasomotor symptoms due to menopause.

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 Effect(s):

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

Pharmacokinetics

Absorption: Extent of absorption unknown.

Distribution: Extensively distributed to tissues.

Metabolism and 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)

Contraindication/Precautions

Contraindicated in:

• Cirrhosis;
• Severe renal impairment or end-stage renal disease;
• Concurrent use with CYP1A2 inhibitors.

Use Cautiously in:

None.

Adverse Reactions/Side Effects

Derm: hot flush

GI: ↑ liver enzymes, abdominal pain, diarrhea

MS: back pain

Neuro: insomnia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

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

Route/Dosage

PO (Adults): 45 mg once daily.

Availability

Tablets: 45 mg

Assessment

• Assess vasomotor symptoms (feelings of warmth in the face, neck, and chest, or sudden intense feelings of heat and sweating (hot flashes or hot flushes) before starting and periodically during therapy.

Lab Test Considerations:

Monitor for hepatic function and injury with ALT, AST, and serum bilirubin (total and direct) before starting therapy and 3 mo, 6 mo, and 9 mo after starting therapy and when symptoms (nausea, vomiting, yellowing of the skin or eyes) occur suggesting liver injury. Do not start therapy if concentration of ALT or AST ≥ two times the upper limit of normal (ULN) or if total bilirubin is elevated (≥2× ULN) for the evaluating laboratory.

Implementation

• PO Administer once daily without regard to food, at the same time each day.  DNC: Swallow tablets whole; do not break, crush, or chew. 

Patient/Family Teaching

• Instruct patient to take fezolinetant 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. Advise patient to read  Patient Information  before starting and with each Rx refill in case of changes.
• Advise patient to notify health care professional promptly if signs and symptoms of liver problems (nausea, vomiting, yellowing of the eyes or skin, pain in the right upper abdomen) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

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