ospemifene (Rx)

Brand and Other Names:Osphena
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and ospemifene

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

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            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

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            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.

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            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

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            Administration

            Oral Administration

            Take with food; food increases bioavailability by ~2-3 fold

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.