Ospemifene

Ospemifene is used to treat moderate-to-severe dyspareunia (painful sexual intercourse) and moderate-to-severe vaginal dryness, symptoms of vulvar and vaginal atrophy, due to menopause.

Ospemifene is available under the following different brand names: Osphena.

Dosage Forms and Strengths

Tablets

• 60 mg

Dosage Considerations – Should be Given as Follows:

Dyspareunia

• Estrogen agonist/antagonist indicated for treatment of moderate-to-severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause
• 60 mg orally once daily 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 orally once daily 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 in pediatric patients

Safety and efficacy not established in pediatric patients.

Common side effects of ospemifene include:

• Hot flush
• Vaginal discharge
• Muscle spasms
• Increased sweating
• Genital discharge

Postmarketing side effects of ospemifene reported include:

• Hypersensitivity
• Angioedema
• Rash
• Itching
• Hives
• Neoplasms: Benign, malignant and unspecified, endometrial hyperplasia, endometrial cancer
• Vascular disorders: Deep vein thrombosis, thrombosis, pulmonary embolism

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Severe interactions of ospemifene include:
  • bazedoxifene/conjugated estrogens
  • clomiphene
  • conjugated estrogens
  • dienogest/estradiol valerate
  • estradiol
  • estrogens conjugated synthetic
  • estrogens esterified
  • estropipate
  • raloxifene
  • Serious interactions of ospemifene include:
  • apalutamide
  • idelalisib
  • ivosidenib
  • voxelotor
• Ospemifene has moderate interactions with at least 99 different drugs.
• Mild interactions of ospemifene include:
  • cimetidine
  • nitazoxanide
  • omeprazole

Warnings

This medication contains ospemifene. Do not take Osphena if you are allergic to ospemifene or any ingredients contained in this drug.

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 (i.e., 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

Contraindications

• Undiagnosed abnormal genital bleeding
• Known or suspected estrogen-dependent neoplasia
• History of, or active deep vein thrombosis (DVT) or pulmonary embolism (PE)
• History of, or active arterial thromboembolic disease (e.g., stroke, heart attack)
• Known or suspected pregnancy or women who may become pregnant
• Documented hypersensitivity to drug or ingredients

Effects of Drug Abuse

• No information available.

Short-Term Effects

• See "What Are Side Effects Associated with Using Ospemifene?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Ospemifene?"

Cautions

• Manage risk factors for cardiovascular disorders, arterial vascular disease (e.g., high blood pressure diabetes mellitus, smoking, high cholesterol, obesity), and/or venous thromboembolism to reduce risk for progression to serious disease
• Increased risk for endometrial hyperplasia
• 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 and Lactation

Ospemifene is contraindicated in women who are or may become pregnant. If a woman becomes pregnant while taking ospemifene, 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.

It is unknown if ospemifene is excreted in human breast milk. Do not breastfeed while using ospemifene.