Indications
Fezolinetant is used to treat moderate to severe hot flushes and night sweats (vasomotor symptoms) caused by menopause. It is a non-hormonal option, which can be useful for women who cannot or prefer not to use hormone replacement therapy.
How It Works
Hot flushes start in the brain’s temperature control centre (the hypothalamus). After menopause, falling oestrogen lets a nerve signal called neurokinin B become overactive in this area. Fezolinetant blocks the neurokinin 3 (NK3) receptor that this signal acts on, which helps the body control temperature again and reduces how often and how strongly hot flushes occur.
Dosage and Administration
The usual dose is one 45 mg tablet once a day, at about the same time each day, with or without food. Swallow it whole with water. If you miss a dose, take it as soon as you remember on the same day, unless it is nearly time for the next dose; do not take two doses on the same day. Your doctor will review whether you still need it from time to time.
Interactions
Do not take with medicines that strongly or moderately block the liver enzyme CYP1A2, such as Fluvoxamine, Ciprofloxacin, Enoxacin and Mexiletine, as these greatly raise Fezolinetant levels. Weaker CYP1A2 blockers, including some oral contraceptives and Cimetidine, may also raise levels. Smoking may lower its level. Tell your doctor about all medicines and herbal products you use.
Contraindications
Do not use if you are allergic to Fezolinetant, have liver cirrhosis or active liver disease with raised liver enzymes, have severe kidney disease or kidney failure, are pregnant, or take a moderate or strong CYP1A2 inhibitor.
Side Effects
Common side effects include stomach pain, diarrhoea, difficulty sleeping, back pain and raised liver enzymes. Some people notice tiredness or headache. Rarely, liver injury has occurred.
Stop taking it and get urgent medical help if you have yellowing of the skin or eyes, dark urine, pale stools, itching, nausea or vomiting with loss of appetite, or pain in the upper right side of the abdomen, or signs of an allergic reaction such as swelling of the face or difficulty breathing.
Pregnancy and Lactation
Fezolinetant is meant for women who have gone through menopause and must not be used in pregnancy. It is not recommended during breastfeeding.
Precautions and Warnings
- Liver blood tests are done before starting and regularly during the first months of treatment, and whenever symptoms of liver problems appear.
- Use with care in mild to moderate liver or kidney problems.
- Not studied in women over 65 years or in those still having periods; discuss with your doctor.
- Not for use in children.
Overdose
Experience with overdose is limited. Higher doses may increase side effects such as headache, nausea and liver changes. Seek medical advice; treatment is supportive.
Therapeutic Class
Non-hormonal treatment for menopausal vasomotor symptoms, neurokinin 3 (NK3) receptor antagonist
Storage
Store below 30°C in a dry place, away from light and out of the reach of children.
Prepared by the Oshud Alo team from standard drug references. For information only; always follow your doctor's advice.