Generic
Ospemifene
2 brands available in the market
At a glance
Ospemifene is a selective estrogen receptor modulator (SERM) used for treatment of moderate to severe dyspareunia and vaginal dryness, symptoms of vulvar and vaginal atrophy due to menopause.
Description
Ospemifene is a next-generation SERM that selectively binds to estrogen receptors and either stimulates or blocks estrogen's activity in different tissue types. It has an agonistic effect on the endometrium.
Indications
- Moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy due to menopause
- Moderate to severe vaginal dryness, a symptom of vulvar and vaginal atrophy due to menopause
Therapeutic class
Drugs used in Vaginal and Vulval Condition
Pharmacological class
SERM (Selective Estrogen Receptor Modulator)
Pharmacology
Ospemifene binds to estrogen receptors to produce estrogenic effects in vulvar and vaginal tissues, increasing vaginal epithelial thickness and relieving vaginal dryness and dyspareunia.
Mechanism of action
Relieves dyspareunia and vaginal dryness by activating estrogen receptors to restore vaginal tissue.
Dosage
Adult Dose (Oral):
- Dyspareunia: 60 mg tablet with food once daily
- Vaginal dryness: 60 mg tablet with food once daily
Administration
- Take with food
- Swallow tablet whole
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Side Effects:
- Hot flush
- Vaginal discharge
- Muscle spasms
- Hyperhidrosis
- Vascular disorders
- Cardiovascular disorders
Precautions & warnings
- Risk of stroke and MI
- Risk of DVT and PE
- Risk of endometrial cancer (agonistic effect on endometrium)
- Do not use in patients with history of breast cancer
- Discontinue 4-6 weeks before surgery
Contraindications
- Undiagnosed abnormal genital bleeding
- Known or suspected estrogen-dependent neoplasia
- Active DVT, PE or history
- Active arterial thromboembolic disease (stroke, MI) or history
- Hypersensitivity
- Pregnancy or women who may become pregnant
- Severe hepatic impairment
Drug interactions
- Metabolized by CYP3A4 and CYP2C9; fluconazole increases exposure 2.7-fold
- Rifampin decreases exposure by 58%
- Ketoconazole increases exposure 1.4-fold
- Do not use with estrogens and estrogen agonists/antagonists
Food interactions
Take with food for better absorption.
Use in pregnancy
Use in Pregnancy: Ospemifene is highly unsafe during pregnancy; definite evidence of severe fetal harm. Completely contraindicated.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Ospemifene is contraindicated during breastfeeding; do not breastfeed.
Pediatric use
Not indicated for children.
Geriatric use
No clinically meaningful differences in safety or effectiveness observed in patients ≥65 years.
Renal / hepatic impairment
Renal Impairment: Pharmacokinetics similar to normal in severe renal impairment; no dose adjustment needed.
Hepatic Impairment: Do not use in severe hepatic impairment (Child-Pugh C).
Overdose effects
Limited information on overdose; symptomatic treatment.
Storage conditions
Keep below 30°C; protect from light & moisture; keep out of reach of children.
Chemical structure
Ospemifene