Formulary
Ospemifene: Indications, Dosing, Side Effects and Interactions
Ospemifene is a selective oestrogen receptor modulator that has an oestrogen-like effect in the vagina, increasing the cellular maturation and mucification of...
MedNext Academy | 3 min read
Ospemifene: Indications, Dosing, Side Effects and Interactions
Ospemifene is a selective oestrogen receptor modulator that has an oestrogen-like effect in the vagina, increasing the cellular maturation and mucification of...
Drug action
Ospemifene is a selective oestrogen receptor modulator that has an oestrogen-like effect in the vagina, increasing the cellular maturation and mucification of the vaginal epithelium.
Indications and dose
**Moderate to severe symptomatic vulvar and vaginal atrophy [in post-menopausal women who are not candidates**
- **Adult** (By Mouth): for local vaginal oestrogen therapy] 60 mg once daily.
Cautions
Risk factors for stroke; risk factors for venous thromboembolism (discontinue if prolonged immobilisation)
Contraindications
Breast cancer (suspected or actively treated); endometrial hyperplasia; history of venous thromboembolism; sex-hormone dependent malignancy (suspected or active); unexplained vaginal bleeding
Side effects
Common or very common Genital discharge; hot flush; increased risk of infection; muscle spasms; skin reactions; vaginal discharge; vaginal haemorrhage Uncommon Endometrial thickening; hypersensitivity; tongue swelling
Interactions
**Severe interactions:**
- This increase is not considered to be clinically significant given the inherent pharmacokinetic variability of ospemifene .
- Ospemifene did not cause a clinically meaningful change in the exposure to the substrates, indicating that ospemifene does not affect those enzyme activities in vivo to a clinically significant...
**Other interactions (20):**
- Effects of other medicinal products on ospemifene Fluconazole, a moderate CYP3A / moderate CYP2C9 / strong CYP2C19 inhibitor, increased the AUC of ospemifene by 2.7-fold.
- These results suggest that co-administration of ospemifene with any medicinal product that inhibits both CYP3A4 and CYP2C9 activity (e.g.
- Therefore, caution is recommended when co-administering ospemifene with fluconazole.
- In case of impaired tolerance of ospemifene, the latter should be stopped as long as treatment with fluconazole lasts.
- Ketoconazole, a strong CYP3A4 inhibitor and moderate P-glycoprotein inhibitor, increased the AUC of ospemifene by 1.4-fold.
- There is therefore no reason to expect that strong CYP3A4 inhibitors would cause a clinically meaningful change in ospemifene exposure.
Pregnancy
Manufacturer advises avoid-toxicity in animal studies.
Hepatic impairment
Manufacturer advises avoid in severe impairment-no information available.
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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