Fezolinelant
Indications
Fezolinetant (listed here under the spelling Fezolinelant) is a non-hormonal medicine used to treat moderate to severe hot flushes and night sweats (vasomotor symptoms) caused by menopause.
How It Works
Body temperature is controlled by a centre in the brain called the hypothalamus. After menopause, falling oestrogen levels allow a brain chemical called neurokinin B to over-activate this centre, triggering hot flushes. Fezolinetant blocks the neurokinin-3 (NK3) receptor that neurokinin B acts on, helping to restore normal temperature control. It does not contain hormones.
Dosage and Administration
The usual adult dose is 45 mg once daily, taken at about the same time each day, with or without food. Swallow the tablet whole with water; do not crush or chew it. If a dose is missed, take it as soon as you remember on the same day, then continue as normal; do not take two doses on the same day.
Interactions
- CYP1A2 inhibitors such as Fluvoxamine, Ciprofloxacin, Mexiletine and Enoxacin: greatly raise Fezolinetant levels; must not be combined.
- Hormone-containing medicines: not studied together; ask your doctor.
- Tell your doctor about all medicines and supplements you use.
Contraindications
- Allergy to Fezolinetant.
- Use of moderate or strong CYP1A2 inhibitors.
- Known cirrhosis of the liver.
- Severe kidney impairment or kidney failure.
Side Effects
Common side effects include stomach pain, diarrhoea, difficulty sleeping, back pain and raised liver enzymes in blood tests. Rarely, serious liver injury has been reported.
Get urgent medical help, and stop taking the medicine, if you have yellowing of the skin or eyes, dark urine, pale stools, pain in the upper right stomach, unusual tiredness, nausea or vomiting, itching, or signs of a severe allergic reaction.
Pregnancy and Lactation
Fezolinetant is intended for women after menopause and is not for use during pregnancy or breastfeeding.
Precautions and Warnings
- Liver blood tests are done before starting and regularly during the first months of treatment, then as advised.
- Tell your doctor about liver or kidney problems.
- Not studied in women with breast cancer or other hormone-sensitive cancers who are having treatment; ask your specialist.
Overdose
There is limited experience with overdose; side effects may increase. Seek medical help if too much is taken.
Therapeutic Class
Neurokinin-3 (NK3) receptor antagonist, non-hormonal treatment for menopausal vasomotor symptoms.
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.
All brands of Fezolinelant