Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- fezolinetant
drospirenone will increase the level or effect of fezolinetant by affecting hepatic enzyme CYP1A2 metabolism. Contraindicated. Fezolinetant AUC and peak plasma concentration are increased if coadministered with drugs that are weak, moderate, or strong CYP1A2 inhibitors
Serious - Use Alternative (16)
- 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.
- mavacamten
mavacamten will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Progestin and ethinyl estradiol are CYP3A4 substrates. Mavacamten may decrease systemic exposures of ethinyl estradiol and progestin, which may lead to contraceptive failure or an increase in breakthrough bleeding. Advise patients to use a contraceptive method that is not affected by CYP450 enzyme induction (eg, intrauterine system) or add nonhormonal contraception (eg, condoms) during coadministration and for 4 months after last mavacamten dose.
- 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.
- omaveloxolone
omaveloxolone will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Omaveloxolone may reduce efficacy of hormonal contraceptives (eg, pill, patch, ring), implants, and progestin-only pills owing to weak CYP3A4 induction.
- 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 (142)
- 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.
- carbamazepine
carbamazepine will decrease the level or effect of drospirenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Advise patients to use alternative contraceptive method during coadministration; continue alternative contraception for 28 days after discontinuing therapy to ensure contraception reliability
- 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.
- lonapegsomatropin
drospirenone will decrease the level or effect of lonapegsomatropin by Other (see comment). Use Caution/Monitor. Oral estrogens may reduce serum insulin-like growth factor-1 response to lonapegsomatropin. Patients receiving oral estrogen replacement may require higher lonapegsomatropin dosages.
- 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.
- mavacamten
drospirenone will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Inititiation of weak CYP2C19 inhibitors may require decreased mavacamten dose.
- 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.
- sparsentan
sparsentan and drospirenone both increase serum potassium. Use Caution/Monitor. Monitor serum potassium frequently.
- 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.
- warfarin
drospirenone increases effects of warfarin by unspecified interaction mechanism. Use Caution/Monitor.
- xipamide
xipamide increases effects of drospirenone by pharmacodynamic synergism. Use Caution/Monitor.
Minor (34)
- 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.
- ruxolitinib topical
drospirenone will increase the level or effect of ruxolitinib topical 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.
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
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
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.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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Formulary
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