Ospemifene

Ospemifene is indicated for:

• The Treatment of Moderate to Severe Dyspareunia, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause.
• The Treatment of Moderate to Severe Vaginal Dryness, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause.

Ospemifene 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).

Ospemifene is an estrogen agonist/antagonist which has agonistic effects on the endometrium. Use of Ospemifene should be for the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women should be re-evaluated periodically as clinically appropriate to determine if treatment is still necessary.

• Treatment of Moderate to Severe Dyspareunia, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause: Take one 60 mg tablet with food once daily.
• Treatment of Moderate to Severe Vaginal Dryness, a Symptom of Vulvar and Vaginal Atrophy, Due to Menopause: Take one 60 mg tablet with food once daily.

• Do not use estrogens or estrogen agonist/antagonist concomitantly with Ospemifene.
• Do not use fluconazole concomitantly with Ospemifene. Fluconazole increases serum concentrations of Ospemifene.
• Do not use rifampin concomitantly with Ospemifene. Rifampin decreases serum concentration of Ospemifene.

Ospemifene is contraindicated in women with any of the following conditions:

• Undiagnosed abnormal genital bleeding
• Known or suspected estrogen-dependent neoplasia
• Active DVT, pulmonary embolism (PE), or a history of these conditions
• Active arterial thromboembolic disease [for example, stroke and myocardial infarction (MI)], or a history of these conditions
• Hypersensitivity (for example, angioedema, urticaria, rash, pruritus) to Ospemifene or any ingredients
• Ospemifene is contraindicated in women who are or may become pregnant. Ospemifene may cause fetal harm when administered to a pregnant woman. Ospemifene was embryo-fetal lethal with labor difficulties and increased pup deaths in rats at doses below clinical exposures, and embryo-fetal lethal in rabbits at 10 times the clinical exposure based on mg/m 2 . If this drug is used during pregnancy, or if a woman becomes pregnant while taking this drug, she should be apprised of the potential hazard to a fetus.

Adverse reactions (≥1 percent) include hot flush, vaginal discharge, muscle spasms, headache, hyperhidrosis, vaginal hemorrhage, night sweats.

Pregnancy: Ospemifene is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or 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 the risk of 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. The reproductive effects observed are consistent with and are considered to be related to the estrogen receptor activity of Ospemifene.

Lactation: It is not known whether Ospemifene is excreted in human breast milk. There are no data on the effects of Ospemifene on the breastfed child or the effects on milk production. Do not breastfeed while taking Ospemifene. Ospemifene was excreted in rat milk

• Venous Thromboembolism: Risk of DVT and pulmonary embolism
• Known, suspected, or history of breast cancer
• Severe Hepatic Impairment

Drugs used in Vaginal and Vulval condition.

Pediatric Use: Ospemifene is not indicated in children. Clinical studies have not been conducted in the pediatric population.

Geriatric Use: Of the 2209 Ospemifene-treated women enrolled in the ten phase 2/3 trials of Ospemifene, >19 percent were 65 years of age or older. No clinically meaningful differences in safety or effectiveness were observed between these women and younger women less than 65 years of age.

Renal Impairment: The pharmacokinetics of ospemifene in women with severe renal impairment (CrCL <30 mL/min) was similar to those in women with normal renal function. No dose adjustment of Ospemifene is required in women with renal impairment.

Hepatic Impairment: The pharmacokinetics of ospemifene has not been studied in women with severe hepatic impairment (Child-Pugh Class C); therefore, do not use Ospemifene in women with severe hepatic impairment.

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.