conjugated estrogens, vaginal (Rx)

Brand and Other Names:Premarin Vaginal Cream
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

vaginal cream

  • 0.625mg/g

Atrophic Vaginitis and Kraurosis Vulvae

Administer cyclic regimen (daily for 21 days followed by 7 days off) intravaginally

Start at 0.5 g dosage strength; may adjust dosage (0.5 to 2 g) based on individual response

Moderate to Severe Dyspareunia

Treats symptom of vulvar and vaginal atrophy due to menopause

0.5 g intravaginally in a twice-weekly (eg, Monday and Thursday) continuously or in a cyclic regimen of daily administration for 21 days followed by 7 days off

Dosing Considerations

In postmenopausal women with a uterus, a progestin should also be considered to reduce risk of endometrial cancer

Women without a uterus do not need a progestin; in some cases, however, hysterectomized women with a history of endometriosis may need a progestin

Use of estrogen-alone, or in combination with a progestin, should be with lowest effective dose and for shortest duration consistent with treatment goals and risks for the individual

Postmenopausal women should be re-evaluated periodically as clinically appropriate to determine if treatment is still necessary

Administration

Plastic applicator calibrated in 0.5 g increments to a maximum of 2 g

Not indicated

Next:

Interactions

Interaction Checker

and conjugated estrogens, vaginal

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (14)

              • carbamazepine

                carbamazepine will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • cimetidine

                cimetidine will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • clarithromycin

                clarithromycin will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • erythromycin base

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

              • erythromycin ethylsuccinate

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

              • erythromycin lactobionate

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

              • erythromycin stearate

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

              • itraconazole

                itraconazole will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • ketoconazole

                ketoconazole will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • nefazodone

                nefazodone will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • quinidine

                quinidine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

              • rifabutin

                rifabutin will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • rifampin

                rifampin will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • St John's Wort

                St John's Wort will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              Monitor Closely (114)

              • albiglutide

                conjugated estrogens, vaginal 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.

              • ambrisentan

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

                ambrisentan will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • amiodarone

                amiodarone will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • amobarbital

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

              • anastrozole

                conjugated estrogens, vaginal decreases effects of anastrozole by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

              • antithrombin alfa

                conjugated estrogens, vaginal decreases effects of antithrombin alfa by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • antithrombin III

                conjugated estrogens, vaginal decreases effects of antithrombin III by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • aprepitant

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

              • argatroban

                conjugated estrogens, vaginal decreases effects of argatroban by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • armodafinil

                armodafinil will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • artemether/lumefantrine

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

              • atazanavir

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

              • atorvastatin

                atorvastatin will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • axitinib

                conjugated estrogens, vaginal decreases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • bemiparin

                conjugated estrogens, vaginal decreases effects of bemiparin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • bivalirudin

                conjugated estrogens, vaginal decreases effects of bivalirudin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • bosentan

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

              • budesonide

                budesonide will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • butabarbital

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

              • butalbital

                butalbital will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • cannabidiol

                cannabidiol, conjugated estrogens, vaginal. affecting hepatic enzyme CYP1A2 metabolism. Modify Therapy/Monitor Closely. Owing to the potential for both CYP1A2 induction and inhibition with the coadministration of CYP1A2 substrates and cannabidiol, consider reducing dosage adjustment of CYP1A2 substrates as clinically appropriate.

              • chloramphenicol

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

              • clarithromycin

                clarithromycin will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • clotrimazole

                clotrimazole will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • conivaptan

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

              • cortisone

                cortisone will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • crofelemer

                crofelemer increases levels of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 and transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

              • cyclosporine

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

                cyclosporine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • dalteparin

                conjugated estrogens, vaginal decreases effects of dalteparin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • darifenacin

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

              • darunavir

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

              • dasatinib

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

              • deferasirox

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

              • dexamethasone

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

              • DHEA, herbal

                DHEA, herbal will increase the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • diltiazem

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

              • dronedarone

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

                dronedarone will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • efavirenz

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

              • enoxaparin

                conjugated estrogens, vaginal decreases effects of enoxaparin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • erythromycin base

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

              • erythromycin ethylsuccinate

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

              • erythromycin lactobionate

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

              • erythromycin stearate

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

              • eslicarbazepine acetate

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

              • etravirine

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

              • exenatide injectable solution

                conjugated estrogens, vaginal 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

                conjugated estrogens, vaginal 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.

              • felodipine

                felodipine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • fluconazole

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

              • fludrocortisone

                fludrocortisone will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • fondaparinux

                conjugated estrogens, vaginal decreases effects of fondaparinux by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • fosamprenavir

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

              • fosphenytoin

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

                fosphenytoin will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • grapefruit

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

              • griseofulvin

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

              • hemin

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

              • heparin

                conjugated estrogens, vaginal decreases effects of heparin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • hyaluronidase

                conjugated estrogens, vaginal decreases effects of hyaluronidase by Other (see comment). Use Caution/Monitor. Comment: Enhanced tissue resistance to hyaluronidase.

              • hydrocortisone

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

              • indinavir

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

                indinavir will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • ketoconazole

                ketoconazole will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • lamotrigine

                conjugated estrogens, vaginal decreases levels of lamotrigine by increasing hepatic clearance. Use Caution/Monitor.

              • lapatinib

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

                lapatinib will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • liraglutide

                conjugated estrogens, vaginal 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.

              • loratadine

                loratadine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • lovastatin

                lovastatin will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • lumefantrine

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

              • maraviroc

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

              • marijuana

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

              • meropenem/vaborbactam

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

              • methylprednisolone

                methylprednisolone will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • metronidazole

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

              • miconazole vaginal

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

              • modafinil

                modafinil will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • nafcillin

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

              • nefazodone

                nefazodone will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • nelfinavir

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

              • nevirapine

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

              • nicardipine

                nicardipine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • nifedipine

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

                nifedipine will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • nilotinib

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

                nilotinib will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • nilutamide

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

              • ospemifene

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

              • oxcarbazepine

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

              • pentobarbital

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

              • phenindione

                conjugated estrogens, vaginal decreases effects of phenindione by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • phenobarbital

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

                phenobarbital will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • phenytoin

                phenytoin will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

                phenytoin will decrease the level or effect of conjugated estrogens, vaginal 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 conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • prednisone

                prednisone will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • primidone

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

              • protamine

                conjugated estrogens, vaginal decreases effects of protamine by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • quercetin

                quercetin will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • quinupristin/dalfopristin

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

              • ranolazine

                ranolazine will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • rifampin

                rifampin will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • rifapentine

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

              • ritonavir

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

                ritonavir will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • rufinamide

                rufinamide will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • secobarbital

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

              • simvastatin

                simvastatin will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • sirolimus

                sirolimus will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • somapacitan

                conjugated estrogens, vaginal 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 conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • tacrolimus

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

              • teniposide

                teniposide will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • tesamorelin

                tesamorelin will decrease the level or effect of conjugated estrogens, vaginal by altering metabolism. Use Caution/Monitor. May decrease efficacy; monitor

              • tolvaptan

                tolvaptan will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • topiramate

                topiramate will decrease the level or effect of conjugated estrogens, vaginal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • trazodone

                trazodone will decrease the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • verapamil

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

                verapamil will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              • voriconazole

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

              • warfarin

                conjugated estrogens, vaginal decreases effects of warfarin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Risk of thromboembolic disorders.

              • zafirlukast

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

              Minor (35)

              • amitriptyline

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

              • amoxapine

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

              • androstenedione

                androstenedione increases effects of conjugated estrogens, vaginal by pharmacodynamic synergism. Minor/Significance Unknown.

              • ascorbic acid

                conjugated estrogens, vaginal decreases levels of ascorbic acid by increasing elimination. Minor/Significance Unknown.

              • boron

                boron increases levels of conjugated estrogens, vaginal by altering metabolism. Minor/Significance Unknown.

              • clomipramine

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

              • cyanocobalamin

                conjugated estrogens, vaginal decreases levels of cyanocobalamin by altering metabolism. Minor/Significance Unknown.

              • desipramine

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

              • dosulepin

                conjugated estrogens, vaginal, 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

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

              • exemestane

                conjugated estrogens, vaginal decreases levels of exemestane by increasing metabolism. Minor/Significance Unknown.

              • folic acid

                conjugated estrogens, vaginal decreases levels of folic acid by altering metabolism. Minor/Significance Unknown.

              • imipramine

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

              • isoniazid

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

              • L-methylfolate

                conjugated estrogens, vaginal decreases levels of L-methylfolate by altering metabolism. Minor/Significance Unknown.

              • lofepramine

                conjugated estrogens, vaginal, 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

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

              • magnesium citrate

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

              • magnesium hydroxide

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

              • magnesium oxide

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

              • magnesium sulfate

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

              • maprotiline

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

              • metyrapone

                conjugated estrogens, vaginal decreases effects of metyrapone by unspecified interaction mechanism. Minor/Significance Unknown.

              • mycophenolate

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

              • nortriptyline

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

              • phytoestrogens

                phytoestrogens decreases effects of conjugated estrogens, vaginal by pharmacodynamic antagonism. Minor/Significance Unknown.

              • pleurisy root

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

              • progesterone, natural

                progesterone, natural, conjugated estrogens, vaginal. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Combination may produce breast tenderness.

              • protriptyline

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

              • pyridoxine

                conjugated estrogens, vaginal decreases levels of pyridoxine by altering metabolism. Minor/Significance Unknown.

              • pyridoxine (Antidote)

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

              • ropinirole

                conjugated estrogens, vaginal increases levels of ropinirole by unspecified interaction mechanism. Minor/Significance Unknown.

              • rose hips

                conjugated estrogens, vaginal decreases levels of rose hips by increasing elimination. Minor/Significance Unknown.

              • trazodone

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

              • trimipramine

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

              Previous
              Next:

              Adverse Effects

              1-10%

              Breast pain (4.9%)

              Headache (3.5%)

              Pelvic pain (2.8%)

              Vulvovaginal disorder (2.8%)

              Vasodilation (2.1%)

              Leukorrhea (2.1%)

              Moniliasis (1.4%)

              Pain (1.4%)

              Muscle cramps (1.4%)

              Pruritus (1.4%)

              Dysuria (1.4%)

              Vaginal hemorrhage (1.4%)

              Vaginitis (1.4%)

              <1%

              Abdominal pain

              Dizziness

              Breast enlargement

              Urinary urgency

              Postmarketing Reports

              Genitourinary system: Abnormal uterine bleeding or spotting, dysmenorrhea or pelvic pain, increase in size of uterine leiomyomata, vaginitis (including vaginal candidiasis), change in cervical secretion, cystitis-like syndrome, application site reactions of vulvovaginal discomfort, (including burning, irritation, and genital pruritus), endometrial hyperplasia, endometrial cancer, precocious puberty, leukorrhea

              Breasts: Tenderness, enlargement, pain, discharge, fibrocystic breast changes, breast cancer, gynecomastia in males

              Cardiovascular: DVT, PE, MI, stroke, increased BP

              Gastrointestinal: Nausea, vomiting, abdominal cramps, bloating, increased incidence of gallbladder disease

              Skin: Chloasma that may persist when drug is discontinued, loss of scalp hair, hirsutism, rash

              Eyes: Retinal vascular thrombosis, intolerance to contact lenses

              Central nervous system: Headache, migraine, dizziness, mental depression, nervousness, mood disturbances, irritability, dementia

              Miscellaneous: Increase or decrease in weight, glucose intolerance, edema, arthralgias, leg cramps, changes in libido, urticaria, exacerbation of asthma, increased triglycerides, hypersensitivity

              Previous
              Next:

              Warnings

              Black Box Warnings

              Endometrial cancer

              • Estrogens increase risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens
              • 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 the use of synthetic estrogens at equivalent estrogen doses

              Breast cancer

              • Using conjugated estrogens in combination with medroxyprogesterone increases risk of invasive breast cancer

              Cardiovascular risks

              • Estrogens with 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 (MI), stroke, invasive breast cancer, pulmonary embolism (PE), and deep vein thrombosis (DVT) in postmenopausal women (aged 50-79 years) during 5.6 years of treatment with daily PO conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) in comparison with placebo
              • Estrogens alone: A substudy of the WHI study reported increased risk for stroke and DVT in postmenopausal women (aged 50-79 years) during 6.8 years of treatment with daily PO conjugated estrogens (0.625 mg) alone in comparison with placebo

              Dementia risks

              • Estrogens with or 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 years during 4 years of treatment with daily PO conjugated estrogens (0.625) mg combined with medroxyprogesterone acetate (2.5 mg) in comparison with placebo
              • Estrogens alone: A substudy of the WHIMS reported increased risk of developing probable dementia in postmenopausal women aged ≥65 years during 5.2 years of treatment with daily PO conjugated estrogens (0.625 mg) alone in comparison with placebo
              • Unknown whether these findings apply to younger postmenopausal women

              Dose and duration

              • In the absence of comparable data, these risks should be assumed to be similar for other doses of conjugated estrogens and medroxyprogesterone acetate, as well as for other combinations and dosage forms of estrogens and progestins
              • Because of these risks, estrogens with or without progestins should be prescribed at the lowest effective dosage and for the shortest duration consistent with treatment goals and individual risks

              Contraindications

              Undiagnosed abnormal genital bleeding

              Known, suspected, or history of breast cancer

              Known or suspected estrogen-dependent neoplasia

              Active DVT, PE, or a history of these conditions

              Active arterial thromboembolic disease (eg, stroke, MI), or a history of these conditions

              Known anaphylactic reaction or angioedema to conjugated estrogen preparations

              Known liver dysfunction or disease

              Known protein C, protein S, or antithrombin deficiency, or other known thrombophilic disorders

              Known or suspected pregnancy

              Cautions

              Systemic absorption occurs with use of vaginal cream

              Studies of the addition of a progestin for 10 or more days of a cycle of estrogen administration, or daily with estrogen in a continuous regimen, may lower incidence of endometrial hyperplasia compared to estrogen treatment alone; endometrial hyperplasia may be a precursor to endometrial cancer

              There are possible risks that may be associated with use of progestins with estrogens compared to estrogen-alone regimens, including increased risk of breast cancer

              If feasible, estrogens should be discontinued at least 4 to 6 weeks before surgery of the type associated with an increased risk of thromboembolism, or during periods of prolonged immobilization

              Most studies show no significant increased risk of endometrial cancer associated with use of estrogens for <1 year; the greatest risk appears to be associated with prolonged use, with increased risks of 15-to 24-fold for 5 to 10 years or more; this risk has been shown to persist for at least 8-15 years after estrogen therapy discontinued

              All women should receive yearly breast examinations by a healthcare provider and perform monthly breast self-examinations; in addition, mammography examinations should be scheduled based on patient age, risk factors, and prior mammogram results

              Risk of cardiovascular, endometrial cancer, breast cancer, and dementia; see Black Box Warnings

              Estrogens increase the risk of gallbladder disease

              Discontinue estrogen if severe hypercalcemia, severe hypertriglyceridemia occurs

              Monitor thyroid function in women on thyroid replacement therapy

              Estrogens may be poorly metabolized in women with impaired liver function; for women with a history of cholestatic jaundice associated with past estrogen use or with pregnancy, caution should be exercised, and in the case of recurrence, medication should be discontinued

              Hormonal therapy for menopausal symptoms associated with increased risk for ovarian cancer; the exact duration of hormone therapy use associated with increased risk of ovarian cancer, is unknown

              Retinal vascular thrombosis has been reported in patients receiving estrogens; discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine; if examination reveals papilledema or retinal vascular lesions, estrogens should be permanently discontinued

              May cause fluid retention; women with conditions that might be influenced by this factor, such as cardiac or renal dysfunction, warrant careful observation when estrogen-alone prescribed

              A few cases of malignant transformation of residual endometrial implants reported in women treated post-hysterectomy with estrogen-alone therapy; for women known to have residual endometriosis post-hysterectomy, addition of progestin should be considered

              Estrogen therapy should be used with caution in women with hypoparathyroidism as estrogen-induced hypocalcemia may occur

              Rare cases of anaphylaxis and angioedema reported; may exacerbate symptoms of hereditary angioedema

              May cause an exacerbation of asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas

              Premarin cream may weaken latex condoms; the potential for the vaginal cream to weaken and contribute to the failure of condoms, diaphragms, or cervical caps made of latex or rubber should be considered

              Hypothyroidism

              • Estrogen administration leads to increased thyroid-binding globulin (TBG) levels; women with normal thyroid function can compensate for increased TBG by making more thyroid hormone, thus maintaining free T4 and T3 serum concentrations in the normal range
              • Women dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of their thyroid replacement therapy; these women should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range

              Venous Thromboembolism

              • Manage appropriately risk factors for arterial vascular disease (for example, hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (VTE) (for example, personal history or family history of VTE, obesity, and systemic lupus erythematosus)
              • Should VTE occur or be suspected, estrogen-alone therapy should be discontinued immediately
              Previous
              Next:

              Pregnancy & Lactation

              Pregnancy Category: X

              Lactation: Distributed in human breast milk; caution when breast feeding, estrogens may decrease the quantity and quality of milk

              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.

              Previous
              Next:

              Pharmacology

              Mechanism of Action

              Estrogens act through binding to nuclear receptors in estrogen-responsive tissues

              Absorption

              Peak plasma concentration: 42 pg/mL (estrone); 12.8 pg/mL (estradiol)

              Peak plasma time: 7.4 hr (estrone); 8.5 hr (estradiol)

              AUC: 826 pg•hr/mL (estrone); 231 pg•hr/mL (estradiol)

              Distribution

              Protein binding: Largely bound to sex hormone binding globulin (SHBG) and albumin

              Widely distributed throughout body, higher concentration in sex hormone target organs

              Metabolism

              Liver

              Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is a major urinary metabolite

              Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the intestine followed by reabsorption

              Elimination

              Excretion: Estradiol, estrone, and estriol are excreted in the urine along with glucuronide and sulfate conjugates

              Previous
              Next:

              Images

              No images available for this drug.
              Previous
              Next:

              Patient Handout

              A Patient Handout is not currently available for this monograph.
              Previous
              Next:

              Formulary

              FormularyPatient Discounts

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

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

              Adding plans allows you to:

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

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

              Tier Description
              1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
              2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
              3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
              Additional Offers
              Email to Patient

              From:

              To:

              The recipient will receive more details and instructions to access this offer.

              By clicking send, you acknowledge that you have permission to email the recipient with this information.

              Email Forms to Patient

              From:

              To:

              The recipient will receive more details and instructions to access this offer.

              By clicking send, you acknowledge that you have permission to email the recipient with this information.

              Previous
              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.