Dosing & Uses
Dosage Forms & Strengths
tablet
- 60mg
Dyspareunia
Estrogen agonist/antagonist indicated for treatment of moderate-to-severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause
60 mg PO qDay with food
Use for the shortest duration consistent with treatment goals and risks for the individual woman
Periodically reevaluate to determine if treatment is still necessary
Vaginal Dryness
Indicated for treatment of moderate-to-severe vaginal dryness, a symptom of vulvar and vaginal atrophy, due to menopause
60 mg PO qDay with food
Use for the shortest duration consistent with treatment goals and risks for the individual woman
Periodically reevaluate to determine if treatment is still necessary
Dosage Modifications
Renal impairment: No dosage adjustment required
Mild-to-moderate hepatic impairment: No dosage adjustment required
Severe hepatic impairment: Not studied; do not use
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
1-10%
Hot flush (7.5%)
Vaginal discharge (3.8%)
Muscle spasms (3.2%)
Hyperhidrosis (1.6%)
Genital discharge (1.3%)
Postmarketing reports
Hypersensitivity
Angioedema
Rash
Rash, erythematous
Generalized rash
Pruritus
Urticaria
Neoplasms: Benign, malignant and unspecified, endometrial hyperplasia, endometrial cancer
Vascular disorders: Deep vein thrombosis, thrombosis, pulmonary embolism
Warnings
Black Box Warnings
Endometrial cancer
- Elicits estrogenic agonistic effects in the endometrium
- Increased risk of endometrial cancer in women with a uterus who uses unopposed estrogens (ie, without a progestin to reduce endometrial hyperplasia)
- Adequate diagnostic measures, including directed and random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding
Cardiovascular effects
- Incidence rates of thromboembolic and hemorrhagic stroke were 1.13 and 3.39 per thousand women years, respectively in the ospemifene 60 mg treatment group and 3.15 and 0 with placebo
- Incidence of DVT was 2.26 per thousand women years (2 reported cases) in the ospemifene 60 mg treatment group and 3.15 per thousand women years (1 reported case) with placebo
Contraindications
Undiagnosed abnormal genital bleeding
Known or suspected estrogen-dependent neoplasia
History of, or active DVT or PE
History of, or active arterial thromboembolic disease (eg, stroke, MI)
Known or suspected pregnancy or women who may become pregnant
Documented hypersensitivity to drug or ingredients
Cautions
Manage risk factors for cardiovascular disorders, arterial vascular disease (eg, hypertension, DM, smoking, hypercholesterolemia, obesity), and/or venous thromboembolism to reduce risk for progression to serious disease
Increased risk for endometrial hyperplasia (see Black Box Warnings)
Has not been studied in women with breast cancer; do not use with known or suspected breast cancer or history of breast cancer
Do not use with severe hepatic impairment (not studied)
Ospemifene is primarily metabolized by CYP3A4 and CYP2C9; CYP2C19 also contributes to its metabolism; avoid moderate-to-strong inhibitors of these isoenzymes as they may increase risk of adverse effects
May initiate or increase occurrence of hot flashes in some women
Pregnancy & Lactation
Pregnancy
Contraindicated in women who are or may become pregnant; if a woman becomes pregnant while taking this drug, she should be apprised of the potential hazard to a fetus
Based on animal data, ospemifene is likely to increase risk for adverse outcomes during pregnancy and labor
Adverse findings at maternally toxic doses included embryofetal lethality in rats and rabbits, and neonatal mortality and difficult labor in rats
Reproductive effects observed are consistent with, and are considered to be related to ospemifene’s estrogen receptor activity
Lactation
Unknown if excreted in human breast milk
Do not breastfeed
Animal studies
- Excreted in rat milk and detected at concentrations higher than that in maternal plasma
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Estrogen agonist/antagonist with tissue selective effects; its biological actions are mediated through binding to estrogen receptors resulting in activation of estrogenic pathways in some tissues and blockade in others
Absorption
Peak plasma time: 2 hr (fasted); 2.5 hr (high fat/high calorie meal)
Peak plasma concentration: 533 ng/mL (fasted); 1198 ng/mL (high fat/high calorie meal)
AUC: 4165 ng•h/mL (fasted); 7521 ng•h/mL (high fat/high calorie meal)
Distribution
Protein bound: >99%
Vd: 448 L
Metabolism
Metabolized by CYP3A4, CYP2C9, and CYP2C19
Elimination
Half-life: 26 hr
Total body clearance: 9.16 L/hr
Excretion: 75% feces, 7% urine
Administration
Oral Administration
Take with food; food increases bioavailability by ~2-3 fold
Images
Patient Handout
Formulary
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