estrogens esterified/methyltestosterone (Rx)

Brand and Other Names:Covaryx, Estratest, more...Estratest H.S.
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

estrogens esterified/methyltestosterone

tablet

  • 0.625mg/1.25mg
  • 1.25mg/2.5mg

Menopausal Vasomotor Symptoms

Treatment of moderate-to-severe vasomotor symptoms associated with menopause in patients not improved by estrogens alone

Use lowest dose that will control symptoms

Typical dosage range: 0.625 mg/1.25 mg PO qDay up to 1.25 mg/2.5 mg qDay

Administration should be cyclic (eg, 3 weeks on and 1 week off)

Attempts to discontinue or taper medication should be made at 3-6 month intervals

Not indicated

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Interactions

Interaction Checker

and estrogens esterified/methyltestosterone

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            Contraindicated (1)

            • ospemifene

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

            Serious - Use Alternative (20)

            • abametapir

              abametapir will increase the level or effect of estrogens esterified 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.

              abametapir will increase the level or effect of estrogens esterified by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP1A2 substrates. If not feasible, avoid use of abametapir.

            • anastrozole

              estrogens esterified decreases effects of anastrozole by pharmacodynamic antagonism. Contraindicated. Estrogen may diminish the pharmacologic action of anastrozole. Coadministration not recommended.

            • antithrombin alfa

              estrogens esterified decreases effects of antithrombin alfa by pharmacodynamic antagonism. Contraindicated. Risk of thromboembolic disorders.

            • apalutamide

              apalutamide will decrease the level or effect of estrogens esterified 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.

            • cyclosporine

              methyltestosterone increases effects of cyclosporine by decreasing metabolism. Avoid or Use Alternate Drug. Androgens may potentiate the hepatoxic effects of cyclosporine, when coadministered.

            • enzalutamide

              enzalutamide will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin base

              erythromycin base will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • fexinidazole

              fexinidazole will increase the level or effect of estrogens esterified 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.

            • givosiran

              givosiran will increase the level or effect of estrogens esterified by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP1A2 substrates with givosiran. If unavoidable, decrease the CYP1A2 substrate dosage in accordance with approved product labeling.

            • idelalisib

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

            • lorlatinib

              lorlatinib will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • pexidartinib

              methyltestosterone and pexidartinib both increase Other (see comment). Avoid or Use Alternate Drug. Pexidartinib can cause hepatotoxicity. Avoid coadministration of pexidartinib with other products know to cause hepatoxicity.

            • pretomanid

              methyltestosterone, pretomanid. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Pretomanid regimen associated with hepatotoxicity. Avoid alcohol and hepatotoxic agents, including herbal supplements and drugs other than bedaquiline and linezolid.

            • tucatinib

              tucatinib will increase the level or effect of estrogens esterified 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 estrogens esterified 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.

            • warfarin

              methyltestosterone increases effects of warfarin by anticoagulation. Avoid or Use Alternate Drug.

            Monitor Closely (92)

            • albiglutide

              methyltestosterone increases effects of albiglutide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

              estrogens esterified decreases effects of albiglutide by pharmacodynamic antagonism. Use Caution/Monitor. Estrogens may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

            • amobarbital

              amobarbital will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • epoetin alfa

              methyltestosterone increases effects of epoetin alfa by pharmacodynamic synergism. Use Caution/Monitor. Concurrent administration of androgens can increase the patient's response to epoetin alfa, reducing the amount required to treat anemia. Because of potential adverse effects drug combination should be avoided.

            • aprepitant

              aprepitant will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Estrogens are CYP3A4 substrates, and the efficacy of estrogens when used for hormone replacement may be reduced.

            • artemether/lumefantrine

              artemether/lumefantrine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • atazanavir

              atazanavir, estrogens esterified. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Atazanavir may increase or decrease levels of estrogens esterified. Use alternatives if available.

            • belzutifan

              belzutifan will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • bosentan

              bosentan will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butabarbital

              butabarbital will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • carbamazepine

              carbamazepine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cenobamate

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

            • chloramphenicol

              chloramphenicol increases levels of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. May increase side effects.

            • cimetidine

              cimetidine will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • clarithromycin

              clarithromycin will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • conivaptan

              conivaptan will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cyclosporine

              cyclosporine will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dabrafenib

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

            • darifenacin

              darifenacin will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • darunavir

              darunavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dasatinib

              dasatinib will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • deferasirox

              deferasirox will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dexamethasone

              dexamethasone will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • diltiazem

              diltiazem will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dronedarone

              dronedarone will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • efavirenz

              efavirenz will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • elagolix

              elagolix will decrease the level or effect of estrogens esterified 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.

            • encorafenib

              encorafenib, estrogens esterified. 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.

            • erythromycin base

              erythromycin base will decrease the level or effect of estrogens esterified by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Modify Therapy/Monitor Closely.

              erythromycin base will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will decrease the level or effect of estrogens esterified by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Modify Therapy/Monitor Closely.

              erythromycin ethylsuccinate will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin lactobionate

              erythromycin lactobionate will decrease the level or effect of estrogens esterified by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Modify Therapy/Monitor Closely.

              erythromycin lactobionate will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • erythromycin stearate

              erythromycin stearate will decrease the level or effect of estrogens esterified by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Modify Therapy/Monitor Closely.

              erythromycin stearate will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • eslicarbazepine acetate

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

            • etravirine

              etravirine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • exemestane

              estrogens esterified decreases levels of exemestane by increasing metabolism. Use Caution/Monitor. Estrogens should not be given concomitantly with exemestane; these drugs could interfere with the pharmacologic action and efficacy of exemestane.

              estrogens esterified decreases effects of exemestane by pharmacodynamic antagonism. Use Caution/Monitor. Estrogens or estrogen-containing products, including combined oral contraceptives, should not be given concomitantly with exemestane; these drugs could interfere with the pharmacologic action and efficacy of exemestane.

            • exenatide injectable solution

              estrogens esterified decreases effects of exenatide injectable solution by pharmacodynamic antagonism. Use Caution/Monitor. Estrogens may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

            • exenatide injectable suspension

              estrogens esterified decreases effects of exenatide injectable suspension by pharmacodynamic antagonism. Use Caution/Monitor. Estrogens may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

            • fedratinib

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

            • fexinidazole

              fexinidazole will increase the level or effect of estrogens esterified by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • fluconazole

              fluconazole will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • grapefruit

              grapefruit will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • griseofulvin

              griseofulvin will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • hemin

              estrogens esterified decreases effects of hemin by pharmacodynamic antagonism. Use Caution/Monitor. Drugs that increase delta-aminolevulinic acid synthetase may decrease hemin effect.

            • hyaluronidase

              estrogens esterified decreases effects of hyaluronidase by Other (see comment). Use Caution/Monitor. Comment: Estrogens, when given in large systemic doses, may render tissues partially resistant to the action of hyaluronidase. Patients may require larger amounts of hyaluronidase for equivalent dispersing effect.

            • hydrocortisone

              hydrocortisone will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • iloperidone

              iloperidone increases levels of estrogens esterified 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.

            • indinavir

              indinavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • insulin aspart

              methyltestosterone increases effects of insulin aspart by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

            • insulin glargine

              methyltestosterone increases effects of insulin glargine by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

            • insulin glulisine

              methyltestosterone increases effects of insulin glulisine by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

            • insulin regular human

              methyltestosterone increases effects of insulin regular human by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

            • istradefylline

              istradefylline will increase the level or effect of estrogens esterified 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 will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ketoconazole

              ketoconazole will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lamotrigine

              estrogens esterified decreases levels of lamotrigine by increasing hepatic clearance. Use Caution/Monitor. Concurrent use may cause lamotrigine levels to decrease by almost 50%. Dose adjustment is required.

            • lapatinib

              lapatinib will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • levoketoconazole

              levoketoconazole will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              levoketoconazole will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • liraglutide

              methyltestosterone increases effects of liraglutide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

              estrogens esterified decreases effects of liraglutide by pharmacodynamic antagonism. Use Caution/Monitor. Estrogens may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

            • lonapegsomatropin

              estrogens esterified will decrease the level or effect of lonapegsomatropin by Other (see comment). Use Caution/Monitor. Oral estrogens may reduce serum insulin-like growth factor-1 response to lonapegsomatropin. Patients receiving oral estrogen replacement may require higher lonapegsomatropin dosages.

            • siponimod

              siponimod and methyltestosterone both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

            • lopinavir

              lopinavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • maraviroc

              estrogens esterified increases levels of maraviroc by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .

            • meropenem/vaborbactam

              meropenem/vaborbactam will decrease the level or effect of estrogens esterified by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Use Caution/Monitor.

            • miconazole vaginal

              miconazole vaginal will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • mifepristone

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

            • mitotane

              mitotane decreases levels of estrogens esterified 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.

            • nafcillin

              nafcillin will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nefazodone

              nefazodone will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nelfinavir

              nelfinavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nevirapine

              nevirapine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • pentobarbital

              pentobarbital will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenytoin

              phenytoin will decrease the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. If the estrogen is being used for contraception then loss of contraception may occur.

            • posaconazole

              posaconazole will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • quinidine

              quinidine will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely.

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ribociclib

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

            • rifabutin

              rifabutin will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifapentine

              rifapentine will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ritonavir

              ritonavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • secobarbital

              secobarbital will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • siponimod

              siponimod and estrogens esterified both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.

            • somapacitan

              estrogens esterified decreases effects of somapacitan by Other (see comment). Modify Therapy/Monitor Closely. Comment: Oral estrogens may reduce the serum IGF-1 response to somapacitan. Patients may require higher somapacitan dosages. See drug monograph for starting dose recommendations.

            • St John's Wort

              St John's Wort will decrease the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • stiripentol

              stiripentol, estrogens esterified. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP1A2 inhibitor and inducer. Monitor CYP1A2 substrates coadministered with stiripentol for increased or decreased effects. CYP1A2 substrates may require dosage adjustment.

            • tacrolimus

              methyltestosterone increases effects of tacrolimus by decreasing metabolism. Use Caution/Monitor.

              tacrolimus will increase the level or effect of estrogens esterified by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tazemetostat

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

            • tolazamide

              methyltestosterone increases effects of tolazamide by pharmacodynamic synergism. Use Caution/Monitor. It is important to monitor all patients with type 2 diabetes on antidiabetic agents receiving androgens for changes in glycemic control. Potential for hypoglycemia.

            Minor (56)

            • acarbose

              methyltestosterone increases effects of acarbose by pharmacodynamic synergism. Minor/Significance Unknown.

            • amitriptyline

              estrogens esterified, amitriptyline. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • amoxapine

              estrogens esterified, amoxapine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • boron

              boron increases levels of estrogens esterified by altering metabolism. Minor/Significance Unknown.

            • chlorpropamide

              methyltestosterone increases effects of chlorpropamide by pharmacodynamic synergism. Minor/Significance Unknown.

            • clomipramine

              estrogens esterified, clomipramine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • cortisone

              methyltestosterone, cortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • cyanocobalamin

              estrogens esterified decreases levels of cyanocobalamin by altering metabolism. Minor/Significance Unknown.

            • desipramine

              estrogens esterified, desipramine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • dexamethasone

              methyltestosterone, dexamethasone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • dosulepin

              estrogens esterified, dosulepin. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens and progestins may decr tricyclic antidepressant effects, while increasing TCA plasma concentration and adverse effects.

            • doxepin

              estrogens esterified, doxepin. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • fludrocortisone

              methyltestosterone, fludrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • folic acid

              estrogens esterified decreases levels of folic acid by altering metabolism. Minor/Significance Unknown.

            • glimepiride

              methyltestosterone increases effects of glimepiride by pharmacodynamic synergism. Minor/Significance Unknown.

            • glipizide

              methyltestosterone increases effects of glipizide by pharmacodynamic synergism. Minor/Significance Unknown.

            • glyburide

              methyltestosterone increases effects of glyburide by pharmacodynamic synergism. Minor/Significance Unknown.

            • hydrocortisone

              methyltestosterone, hydrocortisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • imipramine

              estrogens esterified, imipramine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • insulin detemir

              methyltestosterone increases effects of insulin detemir by pharmacodynamic synergism. Minor/Significance Unknown.

            • insulin lispro

              methyltestosterone increases effects of insulin lispro by pharmacodynamic synergism. Minor/Significance Unknown.

            • insulin NPH

              methyltestosterone increases effects of insulin NPH by pharmacodynamic synergism. Minor/Significance Unknown.

            • isoniazid

              isoniazid will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • L-methylfolate

              estrogens esterified decreases levels of L-methylfolate by altering metabolism. Minor/Significance Unknown.

            • lofepramine

              estrogens esterified, lofepramine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens and progestins may decr tricyclic antidepressant effects, while increasing TCA plasma concentration and adverse effects.

            • magnesium chloride

              estrogens esterified decreases levels of magnesium chloride by Other (see comment). Minor/Significance Unknown. Comment: Magnesium shifted from blood to tissue storage.

            • magnesium citrate

              estrogens esterified decreases levels of magnesium citrate by Other (see comment). Minor/Significance Unknown. Comment: Magnesium shifted from blood to tissue storage.

            • magnesium hydroxide

              estrogens esterified decreases levels of magnesium hydroxide by Other (see comment). Minor/Significance Unknown. Comment: Magnesium shifted from blood to tissue storage.

            • magnesium oxide

              estrogens esterified decreases levels of magnesium oxide by Other (see comment). Minor/Significance Unknown. Comment: Magnesium shifted from blood to tissue storage.

            • magnesium sulfate

              estrogens esterified decreases levels of magnesium sulfate by Other (see comment). Minor/Significance Unknown. Comment: Magnesium shifted from blood to tissue storage.

            • maprotiline

              estrogens esterified, maprotiline. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens and progestins may decr tricyclic antidepressant effects, while increasing TCA plasma concentration and adverse effects.

            • metformin

              methyltestosterone increases effects of metformin by pharmacodynamic synergism. Minor/Significance Unknown.

            • methylprednisolone

              methyltestosterone, methylprednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • metyrapone

              estrogens esterified decreases effects of metyrapone by unspecified interaction mechanism. Minor/Significance Unknown. A subtherapeutic response to metyrapone can be seen in patients on estrogen therapy. It is generally advisable to discontinue estrogens prior to and during metyrapone administration.

            • miglitol

              methyltestosterone increases effects of miglitol by pharmacodynamic synergism. Minor/Significance Unknown.

            • mycophenolate

              mycophenolate decreases effects of estrogens esterified by unknown mechanism. Minor/Significance Unknown. Clinical significance unclear.

            • nateglinide

              methyltestosterone increases effects of nateglinide by pharmacodynamic synergism. Minor/Significance Unknown.

            • nortriptyline

              estrogens esterified, nortriptyline. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • phytoestrogens

              phytoestrogens decreases effects of estrogens esterified by pharmacodynamic antagonism. Minor/Significance Unknown.

            • pioglitazone

              methyltestosterone increases effects of pioglitazone by pharmacodynamic synergism. Minor/Significance Unknown.

            • pleurisy root

              pleurisy root decreases effects of estrogens esterified by unspecified interaction mechanism. Minor/Significance Unknown. Theoretical interaction.

            • prednisolone

              methyltestosterone, prednisolone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • prednisone

              methyltestosterone, prednisone. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • protriptyline

              estrogens esterified, protriptyline. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

            • pyridoxine

              estrogens esterified decreases levels of pyridoxine by altering metabolism. Minor/Significance Unknown.

            • pyridoxine (Antidote)

              estrogens esterified decreases levels of pyridoxine (Antidote) by altering metabolism. Minor/Significance Unknown.

            • repaglinide

              methyltestosterone increases effects of repaglinide by pharmacodynamic synergism. Minor/Significance Unknown.

            • rose hips

              estrogens esterified decreases levels of rose hips by increasing elimination. Minor/Significance Unknown.

            • rosiglitazone

              methyltestosterone increases effects of rosiglitazone by pharmacodynamic synergism. Minor/Significance Unknown.

            • saw palmetto

              saw palmetto decreases effects of methyltestosterone by pharmacodynamic antagonism. Minor/Significance Unknown.

            • saxagliptin

              methyltestosterone increases effects of saxagliptin by pharmacodynamic synergism. Minor/Significance Unknown.

            • sitagliptin

              methyltestosterone increases effects of sitagliptin by pharmacodynamic synergism. Minor/Significance Unknown.

            • tolbutamide

              methyltestosterone increases effects of tolbutamide by pharmacodynamic synergism. Minor/Significance Unknown.

            • trazodone

              estrogens esterified, trazodone. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens and progestins may decr tricyclic antidepressant effects, while increasing TCA plasma concentration and adverse effects.

            • triamcinolone acetonide injectable suspension

              methyltestosterone, triamcinolone acetonide injectable suspension. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. May enhance edema formation.

            • trimipramine

              estrogens esterified, trimipramine. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Estrogens may inhibit hepatic metabolism of tricyclic antidepressants. However, interactions are not common.

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            Adverse Effects

            Frequency Not Defined

            Edema

            Headache

            Acne, alopecia

            Breast soreness,

            Menstrual irregularities

            Bloating

            Nausea

            Hypercalcemia

            Hypercholesterolemia

            Cholestatic hepatitis

            Vomiting

            Anaphylaxis

            Suppression of clotting factors II, V, VII

            Polycythemia

            Paresthesia

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            Warnings

            Black Box Warnings

            Estrogens Increase Risk of Endometrial Cancer

            • Close clinical surveillance of all women taking estrogens is important
            • Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding
            • There is no evidence that the use of "natural" estrogens results in a different endometrial risk profile than synthetic estrogens at equivalent estrogen doses

            Cardiovascular Risks

            • Estrogens with & without progestins should not be used to prevent cardiovascular disease
            • Estrogens plus progestins: Women’s Health Initiative (WHI) Estrogen Plus Progestin substudy reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, & deep vein thrombosis (DVT) in postmenopausal women (aged 50-79 yr) during 5.6 yr of treatment w/ daily PO conjugated estrogens (CE 0.625 mg) combined w/ medroxyprogesterone acetate (MPA 2.5 mg) compared w/ placebo
            • Estrogens alone: A substudy of the WHI Study reported increased risk for stroke & DVT in postmenopausal women (aged 50-79 yr) during 6.8 yr of treatment w/ oral conjugated estrogens (0.625 mg/day) alone compared w/ placebo
            • Unopposed estrogen in women with intact uterus is assocated with increased risk of endometrial cancer

            Dementia Risks

            • Estrogens with & without progestins should not be used to prevent dementia
            • Women's Health Initiative Memory Study (WHIMS), a substudy of the WHI study, reported increased risk of developing probable dementia in postmenopausal women aged 65 yr or older during 4 yr of treatment w/ daily CE 0.625 mg combined w/ MPA 2.5 mg, compared w/ placebo
            • Estrogens alone: A substudy of the WHIMS reported an increased risk of developing probable dementia in postmenopausal women aged 65 yr or older during 5.2 yr of treatment w/ conjugated estrogens 0.625 mg alone compared w/ placebo
            • Unknown whether these findings apply to younger postmenopausal women

            Dose & Duration

            • In the absence of comparable data, these risks should be assumed to be similar for other doses of CE and MPA & other combinations & dosage forms of estrogens & progestins
            • Because of these risks, estrogens w/ or without progestins should be prescribed at lowest effective dose & for shortest duration consistent w/ treatment goals and individual risks

            Contraindications

            Pregnancy, lactation

            Estrogen-dependent neoplasia

            Breast cancer

            Estrogen dependent tumor

            Liver dysfunction or disease

            Undiagnosed abnormal vaginal bleeding

            Active/history of DVT/PE

            Active/recent thromboembolic disease

            Hypersensitivity

            Cautions

            Cardiac disease, renal disease, DM, endometriosis, hyperlipidemias, HTN, hypothyroidism

            Increased risk of VTE

            Fluid retention may exacerbate asthma, epilepsy, migraines, & cardiac or renal dysfunction

            Increased risk of ovarian and endometrial cancer

            Concomitant warfarin, oral anticoagulants: may need to incr anticoagulant dose

            Estrogen may cause retinal vascular thrombosis; discontinue if migraine, proptosis, loss of vision, diplopia, or other vision abnormalities occur

            Women with thrombophilias may experience increased risk of venous thromboembolism

            Use caution in patients with familial defects of lipoprotein metabolism; triglycerides and HDL cholesterol may increase while LDL cholesterol may decrease

            See also individual monographs:

            • Estrogens, esterifed
            • Methyltstosterone
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            Pregnancy & Lactation

            Pregnancy Category: X

            Lactation: Excreted into breast milk; contraindicated

            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

            Esterified estrogen: reduces LHRH release from hypothalamus, reduces gonadotropin release from pituitary; incr synthesis of DNA, RNA, & various proteins in target tissues

            Methyltestosterone: synthetic testosterone derivatives with predominantly anabolic & minor androgenic activity; promoting growth & development of male sex organs & maintaining secondary sex characteristics in androgen-deficient males

            Pharmacokinetics

            Half-Life: Methyltestosterone: 10-100 min (PO)

            Protein bound: 50-80% (esterified estrogens); 98% (methyltestosterone)

            Excretion

            • Esterified estrogens: Urine as conjugates, most estrogens are also excreted in bile & undergo enterohepatic recycling
            • Methyltestosterone: Urine (90%); feces (6%)

            Metabolism

            • Esterified estrogens: Liver, undergoes extensive first-pass metabolism to less active products such as estriol; kidneys, gonads, & muscle tissues may be involved in metabolism to some extent
            • Methyltestosterone: Hepatic
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            Images

            No images available for this drug.
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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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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.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            Code Definition
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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.