Ospemifene
Generic Details
Generic Name
Ospemifene
Other Names
- Osphena
Drug Class
- Selective estrogen receptor modulator (SERM)
Chemical Formula
C24H23ClO2
Molecular Weight
378.89 g/mol
Mechanism of Action
- Ospemifene acts selectively as an estrogen agonist/antagonist on estrogen receptors in different tissues.
Indications
- Treatment of moderate to severe dyspareunia (painful intercourse) due to menopause
Common Dosage Forms
- Tablet
Typical Dosage
- 60 mg orally once daily with food
Pediatric Dosage
- Not established
Geriatric Dosage
- No dosage adjustment required
Side Effects
- Hot flashes
- Vaginal discharge
- Muscle spasms
- Sweating
- Headache
Contraindications
- History of thrombotic or thromboembolic disorders
- Undiagnosed abnormal uterine bleeding
Pregnancy Category
- Category X - Contraindicated in pregnancy
Lactation Safety
- Not recommended during breastfeeding
Drug Interactions
- Strong CYP3A4 inhibitors may increase ospemifene levels
Overdose Symptoms
- Nausea
- Vomiting
- Vaginal bleeding
Antidote for Overdose
- No specific antidote, symptomatic treatment
Storage Conditions
- Store at room temperature away from moisture and heat
Pharmacokinetics
- Absorption: Rapidly absorbed
- Distribution: Approximately 90% bound to plasma proteins
- Metabolism: Metabolized in the liver via multiple CYP enzymes
- Excretion: Primarily in feces
Precautions
- Monitor for signs of venous thromboembolism
Warnings
- Increased risk of endometrial cancer
- Cardiovascular disorders