- Moderate to severe dyspareunia due to menopausal vulvar/vaginal atrophy.
- Moderate to severe vaginal dryness due to menopausal vulvar/vaginal atrophy.
Has agonist (estrogen-like) effects on the endometrium of the uterus; effects are tissue-specific.
- Decreased dyspareunuia.
- Decreased vaginal dryness.
Absorption: Well absorbed following oral administration; food enhances absorption 2–3 fold.
Protein Binding: >99%.
Metabolism and Excretion: Mostly metabolized by the liver (CYP3A4 and CYP2C9 enzyme systems); 75% excreted in feces, 7% in urine as metabolites; minimal amounts excreted unchanged in urine.
Half-life: 26 hr.
TIME/ACTION PROFILE (improvement in symptoms)
|PO||within 12 wk||unknown||unknown|
- Undiagnosed abnormal genital bleeding;
- History/ suspicion of estrogen-dependent cancer;
- History of/current thromboembolic disorder, including DVT, PE, MI, or stroke;
- Concurrent use of estrogens, estrogen agonists/antagonists, fluconazole, or rifampin;
- Severe hepatic impairment;
- OB: Known/suspected pregnancy (may cause fetal harm);
- Lactation: Breast feeding should be avoided.
Use Cautiously in:
- Patients with risk factors for cardiovascular disease, arterial vascular disease, or venous thromboembolism (including hypertension, obesity, family history, tobacco use, diabetes mellitus, history of DVT/PE, or systemic lupus erythematosus);
- Women with a uterus (estrogen use without a progestin ↑ risk of endometrial cancer);
- Known or suspected breast cancer.
Adverse Reactions/Side Effects
CV: DEEP VEIN THROMBOSIS/PE, MI, STROKE
Derm: hot flush, hyperhydrosis
GU: ENDOMETRIAL CANCER, genital/vaginal discharge
MS: muscle spasms
Misc: HYPERSENSITIVITY REACTIONS (including angioedema)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Fluconazole may ↑ levels and risk of toxicity; avoid concurrent use.
- Ketoconazole or other CYP3A4 or CYP2C9 inhibitors may ↑ levels and risk of toxicity.
- Rifampin may ↓ levels and effectiveness; avoid concurrent use.
- Avoid concurrent use of other estrogens or estrogen agonist/antagonists due to ↑ estrogen effects.
- May displace or be displaced by other drugs that are highly protein bound.
PO (Adults): 60 mg once daily.
Tablets: 60 mg
- Assess amount of pain during intercourse and vaginal dryness prior to and periodically during therapy.
- Determine methods previously used to treat dyspareunia.
- Assess BP before and periodically during therapy.
Monitor for hypersensitivity reactions (angioedema, urticaria, rash, pruritus). If symptoms occur, discontinue ospemifene and treat symptomatically.
- PO Administer once daily with food.
- Instruct patient to take ospemifene as directed. Advise patient to read Patient Information sheet before starting therapy and with each Rx refill in case of changes.
Advise patient to report signs and symptoms of unusual vaginal bleeding, changes in vision or speech, sudden new severe headaches, severe pains in chest or legs with or without shortness of breath, weakness, or fatigue promptly to health care professional immediately.
- Inform patient that ospemifene may cause hot flashes, vaginal discharge, muscle spasm, and increased sweating.
- Patients who still have a uterus should discuss addition of progestin with health care professional.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Advise patient to notify health care professional of medication regimen before treatment or surgery.
Advise women to follow yearly exams (pelvic exam, breast exam, mammogram) to monitor for breast and uterine cancer.
Caution patient that cigarette smoking, high BP, high cholesterol, diabetes, and being overweight during estrogen therapy may increase risk of heart disease.
- Ospemifene should not be taken during pregnancy or breast feeding. Instruct patient to notify health care professional immediately if pregnancy is planned or suspected or if breast feeding.
- Advise patient to discuss dose and need for ospemifene every 3–6 mo.
- Decrease in pain during intercourse.
- Decreased vaginal dryness.