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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            Contraindicated (9)

            • bazedoxifene/conjugated estrogens

              ospemifene, bazedoxifene/conjugated estrogens. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • clomiphene

              ospemifene, clomiphene. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • conjugated estrogens

              ospemifene, conjugated estrogens. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • dienogest/estradiol valerate

              ospemifene, dienogest/estradiol valerate. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • estradiol

              ospemifene, estradiol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • estrogens conjugated synthetic

              ospemifene, estrogens conjugated synthetic. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • estrogens esterified

              ospemifene, estrogens esterified. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • estropipate

              ospemifene, estropipate. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            • raloxifene

              ospemifene, raloxifene. Either increases effects of the other by pharmacodynamic synergism. Contraindicated.

            Serious - Use Alternative (8)

            • abametapir

              abametapir will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • apalutamide

              apalutamide will decrease the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP2C19 inducer, with drugs that are CYP2C19 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered.

              apalutamide will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • fexinidazole

              fexinidazole will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • idelalisib

              idelalisib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • ivosidenib

              ivosidenib will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

              ivosidenib will decrease the level or effect of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP2C9 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • lonafarnib

              lonafarnib will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Lonafarnib may increase the AUC and peak concentration of CYP2C19 substrates. If coadministration unavoidable, monitor for adverse reactions and reduce the CYP2C19 substrate dose in accordance with its approved product labeling.

            • tucatinib

              tucatinib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • voxelotor

              voxelotor will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (103)

            • acetazolamide

              acetazolamide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • acitretin

              acitretin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • alpelisib

              alpelisib will decrease the level or effect of ospemifene by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

            • apalutamide

              apalutamide will decrease the level or effect of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Coadministration of apalutamide, a weak CYP2C9 inducer, with drugs that are CYP2C9 substrates can result in lower exposure to these medications. Evaluate for loss of therapeutic effect if medication must be coadministered.

            • armodafinil

              armodafinil increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • aspirin

              aspirin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • atazanavir

              atazanavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • bosentan

              bosentan decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              bosentan decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • bumetanide

              bumetanide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • cannabidiol

              cannabidiol will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of sensitive CYP2C19 substrates, as clinically appropriate, when coadministered with cannabidiol.

              cannabidiol will increase the level or effect of ospemifene by decreasing metabolism. Modify Therapy/Monitor Closely. Cannabidiol may potentially inhibit CYP2C9 activity. Consider reducing the dose when concomitantly using CYP2C9 substrates.

            • capecitabine

              capecitabine increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • carbamazepine

              carbamazepine decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              carbamazepine decreases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              carbamazepine decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • chlorthalidone

              chlorthalidone, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • cisplatin

              cisplatin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • clarithromycin

              clarithromycin increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • clindamycin

              clindamycin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • cobicistat

              cobicistat will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • conivaptan

              conivaptan increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • conjugated estrogens, vaginal

              ospemifene, conjugated estrogens, vaginal. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely.

            • dabrafenib

              dabrafenib will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • darunavir

              darunavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dexamethasone

              dexamethasone decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • diphenhydramine

              diphenhydramine, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • doxycycline

              doxycycline, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • efavirenz

              efavirenz decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • elagolix

              elagolix will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak CYP2C19 inhibitor. Caution with sensitive CYP2C19 substrates.

              elagolix decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • encorafenib

              encorafenib, ospemifene. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • enzalutamide

              enzalutamide decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              eslicarbazepine acetate will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • etravirine

              etravirine decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fedratinib

              fedratinib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • fenoprofen

              fenoprofen, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • fexinidazole

              fexinidazole will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • fluconazole

              fluconazole increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely.

              fluconazole increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

            • fluorouracil

              fluorouracil increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • flurbiprofen

              flurbiprofen increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • fluvoxamine

              fluvoxamine will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosphenytoin

              fosphenytoin decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              fosphenytoin decreases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              fosphenytoin decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • furosemide

              furosemide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • gemfibrozil

              gemfibrozil increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              gemfibrozil increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • glipizide

              glipizide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • glyburide

              glyburide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • ibuprofen

              ibuprofen increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              ibuprofen, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • iloperidone

              iloperidone increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • imatinib

              imatinib increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • indinavir

              indinavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • indomethacin

              indomethacin increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              indomethacin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • isoniazid

              isoniazid increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              isoniazid increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • itraconazole

              itraconazole increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ketoconazole

              ketoconazole increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Modify Therapy/Monitor Closely.

              ketoconazole increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • lopinavir

              lopinavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              lopinavir decreases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • lorlatinib

              lorlatinib will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lumacaftor/ivacaftor

              lumacaftor/ivacaftor, ospemifene. affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C19 substrates. .

              lumacaftor/ivacaftor, ospemifene. affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C9 substrates. .

            • marijuana

              marijuana, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • meclofenamate

              meclofenamate, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • mefenamic acid

              mefenamic acid increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              mefenamic acid, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • mifepristone

              mifepristone will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mitotane

              mitotane decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • modafinil

              modafinil increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • naproxen

              naproxen, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • nefazodone

              nefazodone increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nelfinavir

              nelfinavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nevirapine

              nevirapine decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nicardipine

              nicardipine increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              nicardipine increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nitisinone

              nitisinone will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. Nitisinone inhibits CYP2C9. Caution if CYP2C9 substrate coadministered, particularly those with a narrow therapeutic index.

            • oxcarbazepine

              oxcarbazepine decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • pentobarbital

              pentobarbital decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              phenobarbital decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • phenytoin

              phenytoin decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              phenytoin decreases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              phenytoin decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              phenytoin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • piroxicam

              piroxicam increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              piroxicam, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • posaconazole

              posaconazole increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • primidone

              primidone decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              primidone decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • quinidine

              quinidine increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ribociclib

              ribociclib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifabutin

              rifabutin decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              rifampin decreases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              rifampin decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • rifapentine

              rifapentine decreases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              rifapentine decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • ritonavir

              ritonavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rucaparib

              rucaparib will increase the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • saquinavir

              saquinavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • secobarbital

              secobarbital decreases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • spironolactone

              spironolactone, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • stiripentol

              stiripentol, ospemifene. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

              stiripentol will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of CYP2C19 substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

            • sulfadiazine

              sulfadiazine increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • sulfamethoxazole

              sulfamethoxazole increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              sulfamethoxazole, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • sulindac

              sulindac, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • tacrolimus

              tacrolimus, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • tazemetostat

              tazemetostat will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • ticlopidine

              ticlopidine increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • tipranavir

              tipranavir increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tolbutamide

              tolbutamide increases levels of ospemifene by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

              tolbutamide, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • tolmetin

              tolmetin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • triclabendazole

              triclabendazole will increase the level or effect of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • valproic acid

              valproic acid, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • vincristine

              vincristine, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • vincristine liposomal

              vincristine liposomal, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            • voriconazole

              voriconazole increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • warfarin

              warfarin, ospemifene. Either increases levels of the other by plasma protein binding competition. Modify Therapy/Monitor Closely.

            Minor (4)

            • chloramphenicol

              chloramphenicol increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • cimetidine

              cimetidine increases levels of ospemifene by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • nitazoxanide

              nitazoxanide, ospemifene. Either increases levels of the other by Mechanism: plasma protein binding competition. Minor/Significance Unknown.

            • omeprazole

              omeprazole increases levels of ospemifene by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

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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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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Osphena oral
            -
            60 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            ospemifene oral

            OSPEMIFENE - ORAL

            (os-PEM-i-feen)

            COMMON BRAND NAME(S): Osphena

            WARNING: Ospemifene may increase your risk of uterine cancer. Tell your doctor right away if you develop changes in menstrual period, unusual vaginal bleeding/discharge, or pain/pressure below your "belly button" (navel).Ospemifene may rarely cause serious blood clots to form in the legs or lungs. Tell your doctor if you have a history of blood clots (such as deep vein thrombosis, pulmonary embolism). Also talk to your doctor about risk factors for developing strokes (sometimes fatal) while taking this medication. Some risk factors include tobacco use, alcohol use, having high cholesterol/diabetes, or a history of heart disease. Talk to your doctor about these risks and the benefits of using ospemifene.

            USES: This medication is used to treat painful sexual intercourse and vaginal dryness in women after menopause. Painful intercourse and vaginal dryness are symptoms of changes in and around your vagina, due to menopause.This drug is different from hormones (including estrogens and progestins). It works by acting like estrogen in some parts of the body. Ospemifene belongs to a class of drugs known as selective estrogen receptor modulators (SERM).

            HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking ospemifene and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with food as directed by your doctor, usually once daily.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.Tell your doctor if your condition does not improve or if it worsens.

            SIDE EFFECTS: See also Warning section.Hot flashes, vaginal discharge, muscle spasms, and sweating may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication may rarely cause blood clots (such as pulmonary embolism, stroke, heart attack, deep vein thrombosis). You may be at increased risk for blood clots if you are severely dehydrated, or have a history of blood clots, heart/blood vessel disease, heart failure, stroke, or if you are immobile (such as on very long plane flights or being bedridden). Before using this medication, if you have any of these conditions report them to your doctor or pharmacist. Get medical help right away if any of these side effects occur: shortness of breath/rapid breathing, chest/jaw/left arm pain, unusual sweating, confusion, sudden dizziness/fainting, pain/swelling/warmth in the groin/calf, sudden/severe headaches, trouble speaking, weakness on one side of the body, sudden vision changes.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: See also Warning and Side Effects sections.Before taking ospemifene, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: unusual vaginal bleeding, active or past history of blood clots (such as deep venous thrombosis, pulmonary embolism), active or past history of heart/blood vessel disease (such as heart attack, stroke), cancer, liver disease.Tell your doctor if you just had or will be having surgery or if you will be confined to a bed or chair for a long time (such as a long plane flight). These conditions increase your risk of getting blood clots. You may need to stop this medication for a time or take special precautions.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication must not be used during pregnancy. It may harm an unborn baby. If you become pregnant or think you may be pregnant, tell your doctor right away.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: estrogens, tibolone.Other medications can affect the removal of ospemifene from your body, which may affect how ospemifene works. Examples include fluconazole, rifampin, among others.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Keep all regular medical and laboratory appointments. You should have a complete physical examination, breast and pelvic examination, and PAP test (for vaginal cancer) as directed by your doctor, usually at least once a year. You should also have periodic mammograms as determined by your doctor. Follow your doctor's instructions for examining your own breasts. Report any unusual vaginal bleeding, breast pain, or lumps right away.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each 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.