ospemifene (Rx)Brand and Other Names:Osphena

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 60mg
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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

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

ospemifene and

No Results

     
     activity indicator 
    No Interactions Found
    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

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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

            • Increased risk of stroke and DVT reported in postmenopausal women who received daily oral conjugated estrogens [0.625 mg]-alone therapy over 7.1 years as part of the Women’s Health Initiative study
            • In ospemifene clinical trials, the incidence of DVT was 1.45 per thousand women with ospemifene 60 mg compared with 1.04 per thousand women taking 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 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 Category: X

            Lactation: Unknown whether distributed in human breast milk; do not breastfeed

            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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            Images

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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.
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            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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