Drospirenone Estradiol

Drospirenone Estradiol Brand Name– Angeliq

What is Drospirenone Estradiol

Estradiol and drospirenone products are a combination of an estrogen and progestin used together to treat vasomotor and genitourinary symptoms associated with menopause in women with an intact uterus.

Unopposed estrogen has been associated with increased risk of endometrial hyperplasia in women with an intact uterus.

The addition of a progestin, such as drospirenone, substantially reduces this risk. However, the addition of a progestin to an estrogen regimen may present additional risks for individual women.

Patients should be prescribed HRT products with the indication of use and individual risk:benefit in mind, and for the shortest duration consistent with the treatment goals of the individual. Boxed warnings for HRT relate to cardiovascular, dementia and cancer risks in the menopausal/post-menopausal population.

Drospirenone is a fourth generation progestin and an analog of spironolactone with antimineralocorticoid and antiandrogenic properties. These properties of drospirenone may minimize salt and water retention and may have beneficial effects on blood pressure in postmenopausal women.

However, due to the antimineralocorticoid activity, drospirenone has a potassium-sparing effect and has the potential to increase serum potassium concentrations; therefore, drospirenone should not be used in patients with adrenal, renal, or hepatic insufficiency and should be used with caution in patients taking potassium-elevating medications. 

Estradiol drospirenone products for the treatment of symptoms related to menopause were first FDA-approved in 2005.

Indications

  1. atrophic vaginitis
  2. hot flashes
  3. menopause

For treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae) in women with an intact uterus

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. alopecia
  4. amenorrhea
  5. anaphylactoid reactions
  6. angioedema
  7. anxiety
  8. arthralgia
  9. biliary obstruction
  10. bowel ischemia
  11. breakthrough bleeding
  12. breast cancer
  13. breast discharge
  14. breast enlargement
  15. candidiasis
  16. cervical dysplasia
  17. cervicitis
  18. cholecystitis
  19. cholelithiasis
  20. cholestasis
  21. colitis
  22. dementia
  23. depression
  24. diarrhea
  25. diplopia
  26. dysmenorrhea
  27. edema
  28. elevated hepatic enzymes
  29. emotional lability
  30. endometrial cancer
  31. endometrial hyperplasia
  32. erythema multiforme
  33. erythema nodosum
  34. fatigue
  35. fluid retention
  36. galactorrhea
  37. headache
  38. hepatitis
  39. hirsutism
  40. hypercalcemia
  41. hyperglycemia
  42. hyperkalemia
  43. hypertension
  44. hypocalcemia
  45. impaired cognition
  46. jaundice
  47. leukorrhea
  48. libido decrease
  49. libido increase
  50. mastalgia
  51. melasma
  52. migraine
  53. muscle cramps
  54. myocardial infarction
  55. nausea
  56. new primary malignancy
  57. ovarian cancer
  58. pancreatitis
  59. papilledema
  60. peliosis hepatis
  61. pelvic pain
  62. peripheral edema
  63. pruritus
  64. pulmonary embolism
  65. rash
  66. retinal thrombosis
  67. stroke
  68. teratogenesis
  69. thromboembolism
  70. thrombosis
  71. urinary incontinence
  72. urticaria
  73. vaginal bleeding
  74. vaginal discharge
  75. vaginal irritation
  76. vaginitis
  77. visual impairment
  78. vomiting
  79. weight gain

Monitoring Parameters

  • LFTs
  • pap smear
  • pelvic exam
  • serum creatinine/BUN
  • serum lipid profile
  • serum potassium

Contraindications

  • adrenal insufficiency
  • asthma
  • breast cancer
  • breast-feeding
  • cardiac disease
  • cerebrovascular disease
  • cervical cancer
  • children
  • contact lenses
  • coronary artery disease
  • dementia
  • depression
  • diabetes mellitus
  • endometrial cancer
  • endometrial hyperplasia
  • endometriosis
  • gallbladder disease
  • geriatric
  • hepatic disease
  • hepatocellular cancer
  • hereditary angioedema
  • history of angioedema
  • hypercalcemia
  • hypercholesterolemia
  • hyperkalemia
  • hypertension
  • hypertriglyceridemia
  • hypocalcemia
  • hyponatremia
  • hypoparathyroidism
  • hypothyroidism
  • infants
  • jaundice
  • migraine
  • myocardial infarction
  • new primary malignancy
  • obesity
  • ovarian cancer
  • pancreatitis
  • porphyria
  • pregnancy
  • protein C deficiency
  • protein S deficiency
  • renal disease
  • renal failure
  • renal impairment
  • seizure disorder
  • stroke
  • surgery
  • systemic lupus erythematosus (SLE)
  • thromboembolic disease
  • thromboembolism
  • thrombophlebitis
  • thyroid disease
  • tobacco smoking
  • uterine cancer
  • uterine leiomyomata
  • vaginal bleeding
  • vaginal cancer
  • visual disturbance

Interactions

  • Acarbose
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Propoxyphene
  • Acetohexamide
  • Albiglutide
  • Aliskiren
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Aliskiren; Hydrochlorothiazide, HCTZ
  • Aliskiren; Valsartan
  • Alogliptin
  • Alogliptin; Metformin
  • Alogliptin; Pioglitazone
  • Alpha-glucosidase Inhibitors
  • Amikacin
  • Amiloride
  • Amiloride; Hydrochlorothiazide, HCTZ
  • Aminoglycosides
  • Amiodarone
  • Amobarbital
  • Amoxicillin
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amoxicillin; Clavulanic Acid
  • Ampicillin
  • Ampicillin; Sulbactam
  • Amprenavir
  • Anastrozole
  • Angiotensin II receptor antagonists
  • Angiotensin-converting enzyme inhibitors
  • Apalutamide
  • Aprepitant, Fosaprepitant
  • Armodafinil
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Atazanavir
  • Atazanavir; Cobicistat
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • Azelastine; Fluticasone
  • Azithromycin
  • Aztreonam
  • Bacitracin
  • Barbiturates
  • Beclomethasone
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Betamethasone
  • Bexarotene
  • Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Boceprevir
  • Bosentan
  • Bromocriptine
  • Budesonide
  • Budesonide; Formoterol
  • Butabarbital
  • Calaspargase pegol
  • Calcium
  • Canagliflozin
  • Canagliflozin; Metformin
  • Carbamazepine
  • Carbapenems
  • Carbenicillin
  • Cefaclor
  • Cefadroxil
  • Cefazolin
  • Cefdinir
  • Cefditoren
  • Cefepime
  • Cefiderocol
  • Cefixime
  • Cefotaxime
  • Cefotetan
  • Cefoxitin
  • Cefpodoxime
  • Cefprozil
  • Ceftaroline
  • Ceftazidime
  • Ceftazidime; Avibactam
  • Ceftibuten
  • Ceftizoxime
  • Ceftolozane; Tazobactam
  • Ceftriaxone
  • Cefuroxime
  • Cenobamate
  • Cephalexin
  • Charcoal
  • Chenodiol
  • Chloramphenicol
  • Chlorpropamide
  • Ciclesonide
  • Cimetidine
  • Ciprofloxacin
  • Clarithromycin
  • Clindamycin
  • Clobazam
  • Cobicistat
  • Colistimethate, Colistin, Polymyxin E
  • Conivaptan
  • Corticosteroids
  • Cortisone
  • Cosyntropin
  • Cyclosporine
  • Dabrafenib
  • Dalbavancin
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  • Dantrolene
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  • Dapagliflozin; Metformin
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  • Daptomycin
  • Daratumumab; Hyaluronidase
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deferasirox
  • Deflazacort
  • Delafloxacin
  • Delavirdine
  • Demeclocycline
  • Dexamethasone
  • Dicloxacillin
  • Diltiazem
  • Dipeptidyl Peptidase-4 Inhibitors
  • Doripenem
  • Doxycycline
  • Dulaglutide
  • Duloxetine
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elvitegravir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Empagliflozin
  • Empagliflozin; Linagliptin
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enasidenib
  • Encorafenib
  • Enzalutamide
  • Eplerenone
  • Eravacycline
  • Ertapenem
  • Ertugliflozin
  • Ertugliflozin; Metformin
  • Ertugliflozin; Sitagliptin
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Ethotoin
  • Exemestane
  • Exenatide
  • Felbamate
  • Fidaxomicin
  • Flibanserin
  • Fluconazole
  • Fludrocortisone
  • Flunisolide
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluticasone
  • Fluticasone; Salmeterol
  • Fluticasone; Umeclidinium; Vilanterol
  • Fluticasone; Vilanterol
  • Fluvoxamine
  • Formoterol; Mometasone
  • Fosamprenavir
  • Fosphenytoin
  • Gemifloxacin
  • Gentamicin
  • Glimepiride
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • Glipizide
  • Glipizide; Metformin
  • Glyburide
  • Glyburide; Metformin
  • Glycylcyclines
  • grapefruit juice
  • Griseofulvin
  • Hemin
  • Heparin
  • Hyaluronidase
  • Hyaluronidase, Recombinant; Immune Globulin
  • Hydantoins
  • Hydralazine
  • Hydralazine; Hydrochlorothiazide, HCTZ
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Hydrochlorothiazide, HCTZ; Spironolactone
  • Hydrochlorothiazide, HCTZ; Triamterene
  • Hydrocortisone
  • Icosapent ethyl
  • Idelalisib
  • Imatinib
  • Imipenem; Cilastatin
  • Imipenem; Cilastatin; Relebactam
  • Incretin Mimetics
  • Indinavir
  • Insulin Degludec; Liraglutide
  • Insulin Glargine; Lixisenatide
  • Insulins
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isotretinoin
  • Itraconazole
  • Ivosidenib
  • Kanamycin
  • Ketoconazole
  • Lamotrigine
  • Lefamulin
  • Leflunomide
  • Lenalidomide
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letrozole
  • Levofloxacin
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Linagliptin
  • Linagliptin; Metformin
  • Lincomycin
  • Lincosamides
  • Linezolid
  • Liothyronine
  • Liraglutide
  • Lixisenatide
  • Lomitapide
  • Lopinavir; Ritonavir
  • Lorlatinib
  • Lumacaftor; Ivacaftor
  • Meglitinides
  • Melatonin
  • Mephobarbital
  • Meropenem
  • Meropenem; Vaborbactam
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methohexital
  • Methylprednisolone
  • Metreleptin
  • Metronidazole
  • Metyrapone
  • Midazolam
  • Mifepristone
  • Miglitol
  • Miltefosine
  • Mineral Oil
  • Minocycline
  • Minoxidil
  • Mitotane
  • Mivacurium
  • Modafinil
  • Mometasone
  • Morphine
  • Morphine; Naltrexone
  • Moxifloxacin
  • Nafcillin
  • Nefazodone
  • Nelfinavir
  • Neomycin
  • Nevirapine
  • Nilotinib
  • Nitrofurantoin
  • Nitroprusside
  • Nonsteroidal antiinflammatory drugs
  • Norfloxacin
  • Ofloxacin
  • Omadacycline
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Ospemifene
  • Oxacillin
  • Oxcarbazepine
  • Paromomycin
  • Pegaspargase
  • Penicillin G
  • Penicillin G Benzathine
  • Penicillin G Benzathine; Penicillin G Procaine
  • Penicillin G Procaine
  • Penicillin V
  • Pentobarbital
  • Pexidartinib
  • Phenobarbital
  • Phentermine; Topiramate
  • Phenytoin
  • Piperacillin
  • Piperacillin; Tazobactam
  • Pitolisant
  • Plazomicin
  • Polymyxin B
  • Polymyxins
  • Posaconazole
  • Potassium
  • Potassium-sparing diuretics
  • Pramlintide
  • Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
  • Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
  • Prednisolone
  • Prednisone
  • Primidone
  • Propoxyphene
  • Pyrimethamine; Sulfadoxine
  • Raloxifene
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifamycins
  • Rifapentine
  • Riluzole
  • Ritonavir
  • Rituximab; Hyaluronidase
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  • Ropinirole
  • Rufinamide
  • Saquinavir
  • Sarilumab
  • Saxagliptin
  • Secobarbital
  • Semaglutide
  • SGLT2 Inhibitors
  • Siltuximab
  • Simvastatin; Sitagliptin
  • Sitagliptin
  • Somatropin, rh-GH
  • Spironolactone
  • St. John’s Wort, Hypericum perforatum
  • Streptogramins
  • Streptomycin
  • Succinylcholine
  • Sugammadex
  • Sulfadiazine
  • Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
  • Sulfasalazine
  • Sulfisoxazole
  • Sulfonamides
  • Sulfonylureas
  • Tacrine
  • Tazemetostat
  • Tedizolid
  • Telavancin
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  • Telotristat Ethyl
  • Teriflunomide
  • Testolactone
  • Tetracycline
  • Thalidomide
  • Thiazolidinediones
  • Thiopental
  • Thyroid hormones
  • Ticarcillin
  • Ticarcillin; Clavulanic Acid
  • Tigecycline
  • Tinidazole
  • Tipranavir
  • Tizanidine
  • Tobramycin
  • Tocilizumab
  • Tolazamide
  • Tolbutamide
  • Topiramate
  • Toremifene
  • Trandolapril; Verapamil
  • Tranexamic Acid
  • Trastuzumab; Hyaluronidase
  • Triamcinolone
  • Triamterene
  • Tricyclic antidepressants
  • Trimethoprim
  • Tucatinib
  • Ulipristal
  • Ursodeoxycholic Acid, Ursodiol
  • Vancomycin
  • Verapamil
  • Voriconazole
  • Warfarin
  • Zafirlukast
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