Estradiol

Estradiol Brand Names

Alora | Climara | Delestrogen | Depgynogen | Depo-Estradiol | Depogen | Divigel | DOTTI | Elestrin | Esclim | Estrace | Estraderm | Estrasorb | Estring | EstroGel | Evamist | FemPatch | Femring | Femtrace | Gynodiol | Gynogen LA | Imvexxy | Menostar | Minivelle | Vagifem | Valergen | Vivelle | Vivelle-Dot | Yuvafem

What is Estradiol

Estradiol is the principal intracellular human estrogen and is substantially more active than its metabolites, estrone and estriol, at the cellular level. Estradiol can be obtained from natural sources or prepared synthetically.

There is no evidence that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens.

Due to almost complete first-pass metabolism, estradiol must be given in a micronized oral dosage form to ensure therapeutic effect.

Esterification of estradiol to estradiol cypionate or valerate increases the parenteral duration of action of estradiol to allow for parenteral intramuscular administration.

Estradiol is primarily used to prevent osteoporosis and relieve vasomotor and genitourinary symptoms associated with menopause (natural or surgical), for postmenopausal osteoporosis prevention, and is also used to treat female hypogonadism and other abnormalities of female gonadotropin dysfunction.

Various estrogen products have been marketed in the U.S. since 1938.

Estradiol is available in many dosage forms, including oral tablets, transdermal systems, topical emulsions, topical gels, topical sprays, vaginal creams, vaginal rings, and parenteral depot injections. Vaginal therapies are preferred in postmenopausal women with exclusive genitourinary symptoms, due to lower systemic absorption/exposure with most of these dosage forms.

Many estradiol products have been FDA-approved since the 1990’s, in accordance with the FDA’s guidance to provide efficacious low-dose estrogen therapies in alternate drug delivery systems.

Indications

1. atrophic vaginitis
2. dyspareunia
3. hot flashes
4. hypogonadism
5. menopause
6. oophorectomy
7. osteoporosis prophylaxis
8. ovarian failure
9. palliative treatment of breast cancer
10. prostate cancer

For treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae), whether menopause is natural or surgical (e.g., due to oophorectomy)

for systemic treatment of the vasomotor symptoms (hot flashes) and genitourinary symptoms of menopause

Side Effects

1. abdominal pain
2. acne vulgaris
3. alopecia
4. amenorrhea
5. anaphylactoid reactions
6. angioedema
7. anxiety
8. arthralgia
9. back pain
10. biliary obstruction
11. bladder discomfort
12. breakthrough bleeding
13. breast cancer
14. breast discharge
15. breast enlargement
16. candidiasis
17. cervical dysplasia
18. cervicitis
19. cholecystitis
20. cholelithiasis
21. cholestasis
22. colitis
23. dementia
24. depression
25. diarrhea
26. diplopia
27. dysmenorrhea
28. edema
29. elevated hepatic enzymes
30. emotional lability
31. endometrial cancer
32. endometrial hyperplasia
33. erythema
34. erythema multiforme
35. erythema nodosum
36. fatigue
37. fluid retention
38. galactorrhea
39. GI obstruction
40. gingivitis
41. gynecomastia
42. headache
43. hematoma
44. hepatitis
45. hirsutism
46. hypercalcemia
47. hyperglycemia
48. hypertension
49. hypocalcemia
50. impaired cognition
51. infection
52. injection site reaction
53. insomnia
54. irritability
55. jaundice
56. libido decrease
57. libido increase
58. maculopapular rash
59. mastalgia
60. melasma
61. menorrhagia
62. migraine
63. muscle cramps
64. myocardial infarction
65. nausea
66. new primary malignancy
67. ovarian cancer
68. pancreatitis
69. papilledema
70. paresthesias
71. peliosis hepatis
72. pruritus
73. pulmonary embolism
74. pulmonary oil microembolism
75. rash
76. retinal thrombosis
77. skin discoloration
78. skin irritation
79. stroke
80. teratogenesis
81. thromboembolism
82. thrombosis
83. toxic-shock syndrome
84. urinary incontinence
85. urticaria
86. vaginal bleeding
87. vaginal discharge
88. vaginal irritation
89. vaginal pain
90. vaginitis
91. vesicular rash
92. visual impairment
93. vomiting
94. weight gain
95. xerosis

Monitoring Parameters

• pap smear
• pelvic exam

Contraindications

• accidental exposure
• 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
• hypertension
• hypertriglyceridemia
• hypocalcemia
• hypoparathyroidism
• hypothyroidism
• infants
• intravenous administration
• jaundice
• migraine
• myocardial infarction
• neonates
• new primary malignancy
• obesity
• ovarian cancer
• pancreatitis
• porphyria
• pregnancy
• protein C deficiency
• protein S deficiency
• renal disease
• 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
• Acebutolol
• Acetaminophen; Propoxyphene
• Albiglutide
• Aliskiren; Amlodipine
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Aliskiren; Hydrochlorothiazide, HCTZ
• Aliskiren; Valsartan
• Alogliptin; Metformin
• Alpha-blockers
• Alpha-glucosidase Inhibitors
• Amiloride
• Amiloride; Hydrochlorothiazide, HCTZ
• Amiodarone
• Amlodipine
• Amlodipine; Atorvastatin
• Amlodipine; Benazepril
• Amlodipine; Celecoxib
• Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
• Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
• Amlodipine; Olmesartan
• Amlodipine; Telmisartan
• Amlodipine; Valsartan
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Amprenavir
• Anastrozole
• Angiotensin II receptor antagonists
• Angiotensin-converting enzyme inhibitors
• Aprepitant, Fosaprepitant
• Armodafinil
• Atazanavir
• Atazanavir; Cobicistat
• Atenolol
• Atenolol; Chlorthalidone
• Azelastine; Fluticasone
• Azilsartan
• Azilsartan; Chlorthalidone
• Barbiturates
• Beclomethasone
• Benazepril
• Benazepril; Hydrochlorothiazide, HCTZ
• Bendroflumethiazide; Nadolol
• Beta-blockers
• Betamethasone
• Betaxolol
• Bexarotene
• Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
• Bismuth Subsalicylate; Metronidazole; Tetracycline
• Bisoprolol
• Bisoprolol; Hydrochlorothiazide, HCTZ
• Bosentan
• Brigatinib
• Brimonidine; Timolol
• Bromocriptine
• Budesonide
• Budesonide; Formoterol
• Bumetanide
• Calcium
• Canagliflozin
• Canagliflozin; Metformin
• Candesartan
• Candesartan; Hydrochlorothiazide, HCTZ
• Captopril
• Captopril; Hydrochlorothiazide, HCTZ
• Carbamazepine
• Carteolol
• Carvedilol
• Cenobamate
• Central-acting adrenergic agents
• Chenodiol
• Chloramphenicol
• Chlorothiazide
• Chlorthalidone
• Chlorthalidone; Clonidine
• Ciclesonide
• Cimetidine
• Clarithromycin
• Clindamycin
• Clobazam
• Clonidine
• Conivaptan
• Corticosteroids
• Cortisone
• Cosyntropin
• Cyclosporine
• Danazol
• Dantrolene
• Dapagliflozin
• Dapagliflozin; Metformin
• Dapagliflozin; Saxagliptin
• Daratumumab; Hyaluronidase
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Deflazacort
• Delavirdine
• Demeclocycline
• Dexamethasone
• Diltiazem
• Dipeptidyl Peptidase-4 Inhibitors
• Dirithromycin
• Dorzolamide; Timolol
• Doxazosin
• Doxycycline
• Dulaglutide
• Duloxetine
• Efavirenz
• Efavirenz; Emtricitabine; Tenofovir
• Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
• Elagolix
• Elagolix; Estradiol; Norethindrone acetate
• Empagliflozin
• Empagliflozin; Linagliptin
• Empagliflozin; Linagliptin; Metformin
• Empagliflozin; Metformin
• Enalapril, Enalaprilat
• Enalapril; Felodipine
• Enalapril; Hydrochlorothiazide, HCTZ
• Eprosartan
• Eprosartan; Hydrochlorothiazide, HCTZ
• Ertugliflozin
• Ertugliflozin; Metformin
• Ertugliflozin; Sitagliptin
• Erythromycin
• Erythromycin; Sulfisoxazole
• Esmolol
• Ethacrynic Acid
• Ethotoin
• Exemestane
• Exenatide
• Felbamate
• Felodipine
• Fluconazole
• Fludrocortisone
• Flunisolide
• Fluoxetine
• Fluoxetine; Olanzapine
• Fluticasone
• Fluticasone; Salmeterol
• Fluticasone; Umeclidinium; Vilanterol
• Fluticasone; Vilanterol
• Formoterol; Mometasone
• Fosamprenavir
• Fosinopril
• Fosinopril; Hydrochlorothiazide, HCTZ
• Fosphenytoin
• Furosemide
• Glipizide; Metformin
• Glyburide; Metformin
• Glycylcyclines
• grapefruit juice
• Griseofulvin
• Guanabenz
• Guanfacine
• Hemin
• Hyaluronidase
• Hyaluronidase, Recombinant; Immune Globulin
• Hydantoins
• Hydralazine
• Hydralazine; Hydrochlorothiazide, HCTZ
• Hydralazine; Isosorbide Dinitrate, ISDN
• Hydrochlorothiazide, HCTZ
• Hydrochlorothiazide, HCTZ; Irbesartan
• Hydrochlorothiazide, HCTZ; Lisinopril
• Hydrochlorothiazide, HCTZ; Losartan
• Hydrochlorothiazide, HCTZ; Methyldopa
• Hydrochlorothiazide, HCTZ; Metoprolol
• Hydrochlorothiazide, HCTZ; Moexipril
• Hydrochlorothiazide, HCTZ; Olmesartan
• Hydrochlorothiazide, HCTZ; Propranolol
• Hydrochlorothiazide, HCTZ; Quinapril
• Hydrochlorothiazide, HCTZ; Spironolactone
• Hydrochlorothiazide, HCTZ; Telmisartan
• Hydrochlorothiazide, HCTZ; Triamterene
• Hydrochlorothiazide, HCTZ; Valsartan
• Hydrocortisone
• Icosapent ethyl
• Imatinib
• Incretin Mimetics
• Indinavir
• Insulin Degludec; Liraglutide
• Insulin Glargine; Lixisenatide
• Insulins
• Irbesartan
• Isradipine
• Itraconazole
• Ivosidenib
• Ketoconazole
• Labetalol
• Lenalidomide
• Letrozole
• Levobetaxolol
• Levobunolol
• Levothyroxine
• Levothyroxine; Liothyronine (Porcine)
• Levothyroxine; Liothyronine (Synthetic)
• Linagliptin; Metformin
• Lincomycin
• Lincosamides
• Liothyronine
• Liraglutide
• Lisinopril
• Lixisenatide
• Loop diuretics
• Lopinavir; Ritonavir
• Lorlatinib
• Losartan
• Mecamylamine
• Meglitinides
• Melatonin
• Metformin
• Metformin; Pioglitazone
• Metformin; Repaglinide
• Metformin; Rosiglitazone
• Metformin; Saxagliptin
• Metformin; Sitagliptin
• Methyclothiazide
• Methyldopa
• Methylprednisolone
• Metolazone
• Metoprolol
• Metreleptin
• Metyrapone
• Midazolam
• Mifepristone
• Miglitol
• Mineral Oil
• Minocycline
• Minoxidil
• Modafinil
• Moexipril
• Mometasone
• Nadolol
• Nebivolol
• Nebivolol; Valsartan
• Nefazodone
• Nelfinavir
• Neomycin
• Nevirapine
• Nicardipine
• Nifedipine
• Nilotinib
• Nimodipine
• Nisoldipine
• Nitrofurantoin
• Nitroprusside
• Olmesartan
• Omadacycline
• Ombitasvir; Paritaprevir; Ritonavir
• Ospemifene
• Oxcarbazepine
• Penbutolol
• Perindopril
• Perindopril; Amlodipine
• Phenoxybenzamine
• Phentermine; Topiramate
• Phentolamine
• Phenytoin
• Pindolol
• Posaconazole
• Potassium-sparing diuretics
• Pramlintide
• Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
• Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
• Prazosin
• Prednisolone
• Prednisone
• Propoxyphene
• Propranolol
• Pyrimethamine; Sulfadoxine
• Quinapril
• Raloxifene
• Ramipril
• Reserpine
• Ribociclib; Letrozole
• Rifamycins
• Ritonavir
• Rituximab; Hyaluronidase
• Romidepsin
• Ropinirole
• Sacubitril; Valsartan
• Saquinavir
• Sarecycline
• Selegiline
• Semaglutide
• SGLT2 Inhibitors
• Somatropin, rh-GH
• Sotalol
• Spironolactone
• St. John’s Wort, Hypericum perforatum
• Sulfadiazine
• Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole
• Sulfasalazine
• Sulfisoxazole
• Sulfonamides
• Sulfonylureas
• Sunscreens
• Tacrine
• Tazemetostat
• Telaprevir
• Telmisartan
• Terazosin
• Testolactone
• Tetracycline
• Tetracyclines
• Thiazide diuretics
• Thiazolidinediones
• Thyroid hormones
• Timolol
• Tipranavir
• tobacco
• Topiramate
• Toremifene
• Torsemide
• Trandolapril
• Trandolapril; Verapamil
• Tranexamic Acid
• Trastuzumab; Hyaluronidase
• Triamcinolone
• Triamterene
• Tricyclic antidepressants
• Ursodeoxycholic Acid, Ursodiol
• Valproic Acid, Divalproex Sodium
• Valsartan
• Verapamil
• Voriconazole
• Warfarin
• Zafirlukast