drospirenone/estradiol (Rx)

Brand and Other Names:Angeliq
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

drospirenone/estradiol

tablet

  • 0.25mg/0.5mg
  • 0.5mg/1mg

Hormone Replacement Therapy

1 tablet PO daily

Use the lowest dose that will control symptoms

Renal Impairment

Do not administer

Hepatic Impairment

Do not administer

Other Indications & Uses

Hormone replacement therapy for women with intact uterus: Treatment of menopause-associated hot flashes and vulvar/vaginal atrophy

Safety and efficacy not established

Hormone replacement therapy

1 tablet PO daily

Use the lowest dose that will control symptoms

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Interactions

Interaction Checker

and drospirenone/estradiol

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              Serious - Use Alternative (14)

              • amiloride

                amiloride and drospirenone both increase serum potassium. Avoid or Use Alternate Drug.

                amiloride, drospirenone. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Hyperkalemia.

              • belzutifan

                belzutifan will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of belzutifan with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective nonhormonal contraception. Based on animal studies, belzutifan can cause fetal harm.

              • calaspargase pegol

                calaspargase pegol, drospirenone. unknown mechanism. Avoid or Use Alternate Drug. Due to the potential for an indirect interaction between calaspargase pegol and oral contraceptives, concomitant use of these drugs is not recommended. Use another non-oral contraceptive method for females of childbearing potential.

              • eplerenone

                drospirenone, eplerenone. Mechanism: pharmacodynamic synergism. Contraindicated. Hyperkalemia.

              • fedratinib

                drospirenone will increase the level or effect of fedratinib by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of fedratinib (a CYP3A4 and CYP2C19 substrate) with dual CYP3A4 and CYP2C19 inhibitor. Effect of coadministration of a dual CYP3A4 and CYP2C19 inhibitor with fedratinib has not been studied.

              • isavuconazonium sulfate

                isavuconazonium sulfate will increase the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

              • lonafarnib

                drospirenone will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.

              • mobocertinib

                mobocertinib will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of mobocertinib with hormonal contraceptives may lead to contraceptive failure or increased breakthrough bleeding. Advise females of reproductive potential to use effective non-hormonal contraception.

              • potassium acid phosphate

                drospirenone and potassium acid phosphate both increase serum potassium. Avoid or Use Alternate Drug.

              • potassium chloride

                drospirenone and potassium chloride both increase serum potassium. Avoid or Use Alternate Drug.

              • potassium citrate

                drospirenone and potassium citrate both increase serum potassium. Avoid or Use Alternate Drug.

              • potassium phosphates, IV

                drospirenone and potassium phosphates, IV both increase serum potassium. Avoid or Use Alternate Drug.

              • spironolactone

                drospirenone and spironolactone both increase serum potassium. Avoid or Use Alternate Drug.

                drospirenone, spironolactone. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Hyperkalemia.

              • triamterene

                drospirenone and triamterene both increase serum potassium. Avoid or Use Alternate Drug.

                drospirenone, triamterene. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Hyperkalemia.

              Monitor Closely (137)

              • acebutolol

                acebutolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • aceclofenac

                drospirenone and aceclofenac both increase serum potassium. Modify Therapy/Monitor Closely.

              • acemetacin

                drospirenone and acemetacin both increase serum potassium. Modify Therapy/Monitor Closely.

              • albiglutide

                drospirenone decreases effects of albiglutide by passive renal tubular reabsorption due to increased pH. Use Caution/Monitor. Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

              • albuterol

                drospirenone increases and albuterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • aldesleukin

                aldesleukin increases effects of drospirenone by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.

              • arformoterol

                drospirenone increases and arformoterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • aspirin

                drospirenone and aspirin both increase serum potassium. Modify Therapy/Monitor Closely.

              • aspirin rectal

                drospirenone and aspirin rectal both increase serum potassium. Modify Therapy/Monitor Closely.

              • aspirin/citric acid/sodium bicarbonate

                drospirenone and aspirin/citric acid/sodium bicarbonate both increase serum potassium. Modify Therapy/Monitor Closely.

              • atazanavir

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

              • atenolol

                atenolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • atogepant

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

              • avapritinib

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

              • axitinib

                drospirenone increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • benazepril

                benazepril and drospirenone both increase serum potassium. Use Caution/Monitor.

              • bendroflumethiazide

                drospirenone increases and bendroflumethiazide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • betaxolol

                betaxolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • bisoprolol

                bisoprolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • bumetanide

                drospirenone increases and bumetanide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • canagliflozin

                drospirenone and canagliflozin both increase serum potassium. Use Caution/Monitor.

              • candesartan

                candesartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • captopril

                captopril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • carbenoxolone

                drospirenone increases and carbenoxolone decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • carvedilol

                carvedilol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • celecoxib

                drospirenone and celecoxib both increase serum potassium. Modify Therapy/Monitor Closely.

              • celiprolol

                celiprolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • chlorothiazide

                drospirenone increases and chlorothiazide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • chlorthalidone

                drospirenone increases and chlorthalidone decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • choline magnesium trisalicylate

                drospirenone and choline magnesium trisalicylate both increase serum potassium. Modify Therapy/Monitor Closely.

              • clobazam

                clobazam will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Clobazam is a weak CYP3A4 inducer; effectiveness of hormonal contraceptives may be diminished when given concurrently with clobazam. Additional non-hormonal forms of contraception are recommended.

              • cyclopenthiazide

                drospirenone increases and cyclopenthiazide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • cyclosporine

                drospirenone, cyclosporine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Monitor serum cyclosporine concentrations, and for signs and symptoms of renal and hepatic toxicity.

              • darunavir

                darunavir will increase the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Significant changes (increase or decrease) can occur in estrogen plasma levels. Efficacy of hormonal contraceptives may be reduced. Use of a nonhormonal contraceptive is recommended.

              • diclofenac

                drospirenone and diclofenac both increase serum potassium. Modify Therapy/Monitor Closely.

              • diflunisal

                drospirenone and diflunisal both increase serum potassium. Modify Therapy/Monitor Closely.

              • digoxin

                drospirenone and digoxin both increase serum potassium. Modify Therapy/Monitor Closely.

              • disopyramide

                drospirenone increases effects of disopyramide by pharmacodynamic synergism. Use Caution/Monitor. Additive cardiovascular depression.

              • dobutamine

                drospirenone increases and dobutamine decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • dopexamine

                drospirenone increases and dopexamine decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • enalapril

                enalapril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • ephedrine

                drospirenone increases and ephedrine decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • epinephrine

                drospirenone increases and epinephrine decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • epinephrine racemic

                drospirenone increases and epinephrine racemic decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • eprosartan

                eprosartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • esmolol

                esmolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • ethacrynic acid

                drospirenone increases and ethacrynic acid decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • etodolac

                drospirenone and etodolac both increase serum potassium. Modify Therapy/Monitor Closely.

              • exenatide injectable solution

                drospirenone, exenatide injectable solution. Other (see comment). Use Caution/Monitor. Comment: Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. The effect of exenatide to slow gastric emptying may reduce the extent and rate of oral medications that require rapid GI absorption. Advise patients to take oral contraceptives at least 1 hr before exenatide. .

              • exenatide injectable suspension

                drospirenone, exenatide injectable suspension. Other (see comment). Use Caution/Monitor. Comment: Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. The effect of exenatide to slow gastric emptying may reduce the extent and rate of oral medications that require rapid GI absorption. Advise patients to take oral contraceptives at least 1 hr before exenatide.

              • fenbufen

                drospirenone and fenbufen both increase serum potassium. Modify Therapy/Monitor Closely.

              • fenoprofen

                drospirenone and fenoprofen both increase serum potassium. Modify Therapy/Monitor Closely.

              • finerenone

                drospirenone will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.

                drospirenone and finerenone both increase serum potassium. Modify Therapy/Monitor Closely. Finerenone dose adjustment based on current serum potassium concentration. Monitor serum potassium and adjust finerenone dose as described in the prescribing information as necessary.

              • flibanserin

                drospirenone will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Increased flibanserin adverse effects may occur if coadministered with multiple weak CYP3A4 inhibitors.

              • flurbiprofen

                drospirenone and flurbiprofen both increase serum potassium. Modify Therapy/Monitor Closely.

              • formoterol

                drospirenone increases and formoterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • fosinopril

                fosinopril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • furosemide

                drospirenone increases and furosemide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • gentamicin

                drospirenone increases and gentamicin decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • hydrochlorothiazide

                drospirenone increases and hydrochlorothiazide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • ibuprofen

                drospirenone and ibuprofen both increase serum potassium. Modify Therapy/Monitor Closely.

              • ibuprofen IV

                drospirenone and ibuprofen IV both increase serum potassium. Modify Therapy/Monitor Closely.

              • imidapril

                imidapril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • indapamide

                drospirenone increases and indapamide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • indomethacin

                drospirenone and indomethacin both increase serum potassium. Modify Therapy/Monitor Closely.

              • irbesartan

                irbesartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • isoproterenol

                drospirenone increases and isoproterenol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • ivacaftor

                drospirenone increases levels of ivacaftor by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor when coadministered with weak CYP3A4 inhibitors .

              • juniper

                juniper, drospirenone. Other (see comment). Use Caution/Monitor. Comment: Juniper may potentiate or interfere with diuretic therapy. Juniper has diuretic effects, but may cause kidney damage at large doses.

              • ketoprofen

                drospirenone and ketoprofen both increase serum potassium. Modify Therapy/Monitor Closely.

              • ketorolac

                drospirenone and ketorolac both increase serum potassium. Modify Therapy/Monitor Closely.

              • ketorolac intranasal

                drospirenone and ketorolac intranasal both increase serum potassium. Modify Therapy/Monitor Closely.

              • labetalol

                labetalol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • lamotrigine

                drospirenone will decrease the level or effect of lamotrigine by increasing hepatic clearance. Use Caution/Monitor. Combination oral contraceptives have been shown to significantly decrease plasma concentrations of lamotrigine, likely due to induction of lamotrigine glucuronidation.

              • lemborexant

                drospirenone will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.

              • levalbuterol

                drospirenone increases and levalbuterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • liraglutide

                drospirenone decreases effects of liraglutide by passive renal tubular reabsorption due to increased pH. Use Caution/Monitor. Oral contraceptives may decrease hypoglycemic effects of antidiabetics by impairing glucose tolerance. Monitor for glycemic control in diabetic patients.

              • lisinopril

                lisinopril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • lomitapide

                drospirenone increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

              • lornoxicam

                drospirenone and lornoxicam both increase serum potassium. Modify Therapy/Monitor Closely.

              • losartan

                losartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • maraviroc

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

              • meclofenamate

                drospirenone and meclofenamate both increase serum potassium. Modify Therapy/Monitor Closely.

              • mefenamic acid

                drospirenone and mefenamic acid both increase serum potassium. Modify Therapy/Monitor Closely.

              • meloxicam

                drospirenone and meloxicam both increase serum potassium. Modify Therapy/Monitor Closely.

              • metaproterenol

                drospirenone increases and metaproterenol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • metformin

                drospirenone decreases effects of metformin by pharmacodynamic antagonism. Use Caution/Monitor.

              • methyclothiazide

                drospirenone increases and methyclothiazide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely. .

              • metolazone

                drospirenone increases and metolazone decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • metoprolol

                metoprolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • midazolam intranasal

                drospirenone will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.

              • mifepristone

                mifepristone decreases effects of drospirenone by pharmacodynamic antagonism. Use Caution/Monitor. Backup contraceptive method recommended.

              • moexipril

                moexipril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • nabumetone

                drospirenone and nabumetone both increase serum potassium. Modify Therapy/Monitor Closely.

              • nadolol

                nadolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • naproxen

                drospirenone and naproxen both increase serum potassium. Modify Therapy/Monitor Closely.

              • nebivolol

                nebivolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • noni juice

                drospirenone and noni juice both increase serum potassium. Use Caution/Monitor.

              • norepinephrine

                drospirenone increases and norepinephrine decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • olmesartan

                olmesartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • oxaprozin

                drospirenone and oxaprozin both increase serum potassium. Modify Therapy/Monitor Closely.

              • parecoxib

                drospirenone and parecoxib both increase serum potassium. Modify Therapy/Monitor Closely.

              • penbutolol

                penbutolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • perindopril

                perindopril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • pindolol

                pindolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • pirbuterol

                drospirenone increases and pirbuterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • piroxicam

                drospirenone and piroxicam both increase serum potassium. Modify Therapy/Monitor Closely.

              • pivmecillinam

                pivmecillinam increases effects of drospirenone by unspecified interaction mechanism. Use Caution/Monitor. Hyperkalemia.

              • potassium citrate/citric acid

                drospirenone and potassium citrate/citric acid both increase serum potassium. Use Caution/Monitor.

              • potassium iodide

                potassium iodide and drospirenone both increase serum potassium. Use Caution/Monitor.

              • propranolol

                propranolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • quinapril

                quinapril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • ramipril

                ramipril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • sacubitril/valsartan

                sacubitril/valsartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • salicylates (non-asa)

                drospirenone and salicylates (non-asa) both increase serum potassium. Modify Therapy/Monitor Closely.

              • salmeterol

                drospirenone increases and salmeterol decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • salsalate

                drospirenone and salsalate both increase serum potassium. Modify Therapy/Monitor Closely.

              • siltuximab

                siltuximab, drospirenone. Other (see comment). Use Caution/Monitor. Comment: CYP450 activity in the liver is down regulated by infection and inflammation stimuli including cytokines (eg, IL-6); inhibition of IL-6 by siltuximab may restore CYP450 enzymatic activity; caution if coadministered with CYP substrates that have a narrow therapeutic index.

              • sotalol

                sotalol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • succinylcholine

                drospirenone and succinylcholine both increase serum potassium. Modify Therapy/Monitor Closely.

              • sulfasalazine

                drospirenone and sulfasalazine both increase serum potassium. Modify Therapy/Monitor Closely.

              • sulindac

                drospirenone and sulindac both increase serum potassium. Modify Therapy/Monitor Closely.

              • tazemetostat

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

              • telmisartan

                telmisartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • temocillin

                temocillin increases effects of drospirenone by unspecified interaction mechanism. Use Caution/Monitor. Hyperkalemia.

              • terbutaline

                drospirenone increases and terbutaline decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • ticarcillin

                ticarcillin increases effects of drospirenone by unspecified interaction mechanism. Use Caution/Monitor. Hyperkalemia.

              • timolol

                timolol and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • tinidazole

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

              • tolfenamic acid

                drospirenone and tolfenamic acid both increase serum potassium. Modify Therapy/Monitor Closely.

              • tolmetin

                drospirenone and tolmetin both increase serum potassium. Modify Therapy/Monitor Closely.

              • tolvaptan

                drospirenone and tolvaptan both increase serum potassium. Modify Therapy/Monitor Closely.

              • torsemide

                drospirenone increases and torsemide decreases serum potassium. Effect of interaction is not clear, use caution. Modify Therapy/Monitor Closely.

              • trandolapril

                trandolapril, drospirenone. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Risk of hyperkalemia.

              • valsartan

                valsartan and drospirenone both increase serum potassium. Modify Therapy/Monitor Closely.

              • voclosporin

                voclosporin and drospirenone both increase serum potassium. Use Caution/Monitor.

              • xipamide

                xipamide increases effects of drospirenone by pharmacodynamic synergism. Use Caution/Monitor.

              Minor (33)

              • agrimony

                agrimony increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • birch

                birch increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • brimonidine

                brimonidine increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • cadexomer iodine

                cadexomer iodine, drospirenone. Mechanism: decreasing renal clearance. Minor/Significance Unknown. Hyperkalemia.

              • calcium acetate

                drospirenone decreases levels of calcium acetate by increasing renal clearance. Minor/Significance Unknown.

              • calcium carbonate

                drospirenone decreases levels of calcium carbonate by increasing renal clearance. Minor/Significance Unknown.

              • calcium chloride

                drospirenone decreases levels of calcium chloride by increasing renal clearance. Minor/Significance Unknown.

              • calcium citrate

                drospirenone decreases levels of calcium citrate by increasing renal clearance. Minor/Significance Unknown.

              • calcium gluconate

                drospirenone decreases levels of calcium gluconate by increasing renal clearance. Minor/Significance Unknown.

              • cornsilk

                cornsilk increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • enasidenib

                enasidenib, drospirenone. unknown mechanism. Minor/Significance Unknown. Coadministration of enasidenib may increase or decrease the concentrations of combined hormonal contraceptives. Clinical significance of this interaction is unknown.

              • epoprostenol

                epoprostenol increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown. Additive hypotensive effects.

              • forskolin

                forskolin increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • goldenrod

                goldenrod increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • iodinated glycerol

                iodinated glycerol, drospirenone. Mechanism: decreasing renal clearance. Minor/Significance Unknown. Hyperkalemia.

              • iodine

                iodine, drospirenone. Mechanism: decreasing renal clearance. Minor/Significance Unknown. Hyperkalemia.

              • magnesium chloride

                drospirenone increases levels of magnesium chloride by decreasing renal clearance. Minor/Significance Unknown.

              • magnesium citrate

                drospirenone increases levels of magnesium citrate by decreasing renal clearance. Minor/Significance Unknown.

              • magnesium hydroxide

                drospirenone increases levels of magnesium hydroxide by decreasing renal clearance. Minor/Significance Unknown.

              • magnesium oxide

                drospirenone increases levels of magnesium oxide by decreasing renal clearance. Minor/Significance Unknown.

              • magnesium sulfate

                drospirenone increases levels of magnesium sulfate by decreasing renal clearance. Minor/Significance Unknown.

              • maitake

                maitake increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • minoxidil

                drospirenone increases effects of minoxidil by pharmacodynamic synergism. Minor/Significance Unknown.

              • octacosanol

                octacosanol increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • reishi

                reishi increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • ruxolitinib

                drospirenone will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

              • shepherd's purse

                shepherd's purse, drospirenone. Other (see comment). Minor/Significance Unknown. Comment: Theoretically, shepherd's purse may interfere with BP control.

              • sulfadiazine

                drospirenone increases levels of sulfadiazine by unspecified interaction mechanism. Minor/Significance Unknown.

              • sulfamethoxazole

                drospirenone, sulfamethoxazole. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Hyperkalemia.

                drospirenone increases levels of sulfamethoxazole by unspecified interaction mechanism. Minor/Significance Unknown.

              • sulfisoxazole

                drospirenone increases levels of sulfisoxazole by unspecified interaction mechanism. Minor/Significance Unknown.

              • tizanidine

                tizanidine increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypotension.

              • treprostinil

                treprostinil increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.

              • trimethoprim

                drospirenone, trimethoprim. Mechanism: unspecified interaction mechanism. Minor/Significance Unknown. Hyperkalemia.

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              Adverse Effects

              >10%

              Breast pain (19%)

              Upper respiratory infection (19%)

              Abdominal pain (11%)

              1-10%

              Edema

              Peripheral edema

              Headache

              Accidental injury, back pain, pain in extremity

              Endometrial disorder

              Leukorrhea

              Vaginal hemorrhage

              Abdominal enlargement

              Flu syndrome

              Sinusitis

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              Warnings

              Contraindications

              Hypersensitivity

              Undiagnosed abnormal genital bleeding

              Known, suspected, or history of cancer of the breast

              Known or suspected estrogen-dependent neoplasia

              Active DVT, PE, or a history of these conditions

              Active arterial thromboembolic disease (for example, stroke and MI), or history of these conditions

              Renal impairment

              Known liver impairment or disease

              Adrenal insufficiency

              Known or suspected pregnancy

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

              Known anaphylactic reaction, angioedema, or hypersensitivity

              Cautions

              Use caution in bone mineral density changes, current/history of depression, DM, HTN, hyperlipidemia, obesity, endometriosis, family history of breast cancer, DVT/PE, smoking

              Discontinue if the following develop: jaundice, visual problems, 4-6 wk before major surgery, any symptoms of VTE, massive BP increase, unusually severe migraines or first-time migraines, depression

              Increased risk of post-op thromboembolic complications, arterial/venous thromboembolic disorder, hyperkalemia, exacerbation of endometriosis

              Do not use with conditions that predispose to hyperkalemia

              Conditions exacerbated by fluid retention (eg, asthma, migraine, cardiac/renal dysfunction, epilepsy)

              Patients on warfarin/oral anticoagulants: oestrogens increase thromboembolic risk; increase in anticoagulant dose may be warranted

              History of migraine with aura

              Cholelithiasis

              Exogenous estrogens may exacerbate symptoms of angioedema in women with hereditary angioedema

              Consider topical vaginal products when used solely for vulvovaginal atrophy

              Increased risk of ovarian cancer reported in women who used hormonal therapy for menopausal symptoms

              Manage appropriately risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus)

              A 2 to 4-fold increase in risk of gallbladder disease requiring surgery in postmenopausal women receiving estrogens reported

              Retinal vascular thrombosis 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 discontinued

              There are, possible risks that may be associated with use of progestins with estrogens compared to estrogen-alone regimens, including a possible increased risk of breast cancer, adverse effects on lipoprotein metabolism (e.g., lowering HDL, raising LDL), and impairment of glucose tolerance

              In patients with pre-existing hypertriglyceridemia, estrogen therapy may be associated with elevations of plasma triglycerides leading to pancreatitis and other complications

              Estrogens may be poorly metabolized in patients with impaired liver function; exercise caution in patients with a history of cholestatic jaundice associated with past estrogen use or with pregnancy; in the case of recurrence, discontinue medication

              Patients dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of thyroid replacement therapy; these patients should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range

              Use caution in individuals with severe hypocalcemia

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              Pregnancy & Lactation

              Pregnancy Category: contraindicated in pregnancy

              Lactation: enters breast milk/not recommended

              Pregnancy Categories

              A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

              B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

              C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

              D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

              X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

              NA: Information not available.

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              Pharmacology

              Mechanism of Action

              Estradiol: Endogenous estrogen; reduces the release of gonadotropin-releasing hormone from hypothalamus, reduces release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from pituitary gland; increases synthesis of DNA, RNA, and various proteins in target tissues. Estrogen replacement reduces elevated levels of estrogen and progesterone LH and FSH in postmenopausal women

              Drospirenone: Progestin; spironolactone analog with antimineralocorticoid and antiandrogenic activity

              Pharmacokinetics

              Half-Life elimination: 36-42 hr (drospirenone)

              Vd: 4.2 L/kg (drospirenone)

              Metabolism: Hepatic

              Bioavailability: 76-85% (drosperidone)

              Metabolites: Inactive

              Excretion: Urine, feces

              Peak plasma time

              • Drospirenone: 1 hr
              • Estradiol: 6-8 hr

              Peak plasma concentration

              • Drospirenone: 13-24 ng/mL
              • Estradiol: 34-54 pg/mL

              Protein bound

              • Drospirenone: 97% bound to serum proteins (not SHBG or corticosteroid binding globulin)
              • Estradiol: 98% (37% to globulin and 61% to albumin)
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              Images

              No images available for this drug.
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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Formulary

              FormularyPatient Discounts

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              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.
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              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.