Adult Dosing

Moderate to severe dyspareunia

• 60 mg PO Daily

Pediatric Dosing

• Not indicated for use in children

[Outline]

• Adult Dosing
• Pediatric Dosing

• Moderate to severe dyspareunia

• Hypersensitivity to any of the ingredients of the product
• 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 such as stroke, myocardial infarctions (MI), or a history of these conditions
• Pregnant women

• Ospemifene is an estrogen agonist/antagonist with tissue selective effects. In the endometrium it has estrogen agonistic effects. There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy reduces the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer
• Estrogen-alone therapy has an increased risk of stroke and deep vein thrombosis (DVT)
• Ospemifene 60 mg was associated with cerebral thromboembolic and hemorrhagic stroke incidence rates of 0.72 and 1.45 per thousand women, respectively vs. 1.04 and 0 per thousand women, respectively in placebo. For deep vein thrombosis, the incidence rate was 1.45 per thousand women vs. 1.04 per thousand women in placebo

Renal Dose Adjustment

• Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

• Mild-moderate hepatic impairment (Child-Pugh Class A or B): No dose adjustments
• Severe hepatic impairment (Child-Pugh Class C): Use not recommended

• Ospemifene is an estrogen agonist/antagonist with tissue selective effects. In the endometrium it has estrogen agonistic effects. There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy reduces the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer [US black box warning]
• Estrogen-alone therapy has an increased risk of stroke and deep vein thrombosis (DVT) [US black box warning]
• Ospemifene 60 mg was associated with cerebral thromboembolic and hemorrhagic stroke incidence rates of 0.72 and 1.45 per thousand women, respectively vs. 1.04 and 0 per thousand women, respectively in placebo. For deep vein thrombosis, the incidence rate was 1.45 per thousand women vs. 1.04 per thousand women in placebo [US black box warning]
• Closely monitor risk factors for cardiovascular disorders, arterial vascular disease, hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, obesity, /or venous thromboembolism (VTE), personal history or family history of VTE, obesity, and systemic lupus erythematosus
• 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
• Use lowest effective dose for the shortest possible duration
• Ospemifene has not been adequately studied in women with breast cancer; therefore it should not be used in women with known or suspected breast cancer or with a history of breast cancer
• Ospemifene should not be used in women with severe hepatic impairment

Pregnancy Category:X; use is contraindicated

Breastfeeding: It is not known whether the drug is excreted in human breast milk. According to the manufacturer data, because the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue therapy or discontinue nursing.

• CV: Thromboembolic and hemorrhagic stroke, venous thromboembolism, deep vein thrombosis
• REPRODUCTIVE: Vaginal discharge, genital discharge, endometrial cancer, endometrial thickening
• MUSC: Muscle spasms
• DERM: Hyperhidrosis

• Estrogen agonist/antagonist; binds to receptors and results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism)
• Metabolism: Hepatic; CYP3A4, CYP2C9 and CYP2C19 substrates
• Excretion: Feces (75%) and urine (7%)
• Half-life: 26 hours

US Trade Name(s)

• Osphena

US Availability

Osphena

• TABS: 60 mg

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]

Obstetrics/Gynecology

Sex Hormones

Estrogen