OSPHENA Dosage & Rx Info | Uses, Side Effects

Osphena Generic Name & Formulations

Legal Class

General Description

Ospemifene 60mg; tabs.

Pharmacological Class

Estrogen (agonist/antagonist).

How Supplied

Tabs—30, 90

Storage

Store at 20ºC to 25ºC (68ºF to 77ºF); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF).

Manufacturer

Duchesnay USA, Inc.

Generic Availability

Mechanism of Action

Osphena is an estrogen receptor agonist/antagonist with tissue selective effects. Its biological actions are mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).

Osphena Indications

Indications

Moderate to severe dyspareunia or vaginal dryness due to menopause.

Osphena Dosage and Administration

Adult

60mg once daily with food.

Children

Not applicable.

Osphena Contraindications

Contraindications

Undiagnosed abnormal genital bleeding. Estrogen-dependent neoplasia. Active DVT, PE, or history of. Active arterial thromboembolic disease (eg, stroke, MI) or a history of. Pregnancy.

Osphena Boxed Warnings

Boxed Warning

Endometrial cancer. Cardiovascular disorders.

Osphena Warnings/Precautions

Warnings/Precautions

Increased risk of endometrial cancer in women with intact uterus (adding progestins has been shown to reduce endometrial hyperplasia risk). Evaluate if undiagnosed persistent or recurring abnormal genital bleeding occurs. Increased risk of cardiovascular disorders (eg, MI, stroke, VTE); discontinue if suspected or occurs. Known, suspected, or history of breast cancer: do not use. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Use for shortest duration consistent with treatment goals and risks. Perform yearly breast exams (including mammography). Severe hepatic impairment: not recommended. Reevaluate periodically. Nursing mothers: not recommended.

Osphena Pharmacokinetics

Absorption

Peak median serum concentration: reached at ~2 hours (range: 1–8 hours). Steady state: reached after 9 days of administration.

Distribution

Apparent volume of distribution: 448 L. Serum protein bound: >99%.

Metabolism

Hepatic (CYP3A4, CYP2C9, CYP2C19).

Elimination

Fecal (75%), renal (7%). Half-life: ~26 hours. Apparent total body clearance: 9.16 L/hr.

Osphena Interactions

Interactions

Avoid concomitant other estrogens or estrogen agonists/antagonists. Antagonized by rifampin. Potentiated by fluconazole (avoid), ketoconazole. May affect or be affected by highly protein-bound drugs. May increase risk of adverse reactions with concomitant CYP3A4 and CYP2C9 inhibitors.

Osphena Adverse Reactions

Adverse Reactions

Hot flush, vaginal discharge/hemorrhage, muscle spasms, headache, hyperhidrosis, night sweats.

Osphena Clinical Trials

See Literature

Osphena Note

Not Applicable

Osphena Patient Counseling