Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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 (95)
- 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.
- ceritinib
ceritinib will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- 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.
- fosaprepitant
fosaprepitant 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.
- 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.
- lenacapavir
lenacapavir will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.
- 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 (60)
- acarbose
methyltestosterone increases effects of acarbose by pharmacodynamic synergism. Minor/Significance Unknown.
- acetazolamide
acetazolamide will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. 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.
- anastrozole
anastrozole will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- 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.
- cyclophosphamide
cyclophosphamide will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 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.
- larotrectinib
larotrectinib will increase the level or effect of estrogens esterified by affecting hepatic/intestinal enzyme CYP3A4 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.
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
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
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.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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Formulary
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