17-beta estradiol (E2, Estrace, Estinyl, Delestrogen, Elestrin, Evamist, Imvexxy)
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Introduction
Tradenames: Estrace, Delestrogen Delestrogen. Estradiol cypionate & estradiol valerate.
Indications
- symptoms of menopause
- moderate to severe vasomotor symptoms, hot flashes
- treatment of atrophic vaginitis
- atrophic dystrophy of the vulva
- atrophic urethritis
- estradiol vaginal inserts (Imvexxy) for dyspareunia resulting from menopause[7]
- female hypogonadism
- ovariectomy
- primary ovarian failure
- endometriosis[6]
- dysmenorrhea
- menorrhagia
- acne[6]
- inoperable breast cancer
- inoperable prostate cancer
- prevention of postmenopausal osteoporosis
- may be useful for depression in perimenopausal women
Dosage
- moderate to severe vasomotor symptoms
- osteoporosis prevention
- hypogonadism:
- prostate cancer:
Tabs: 0.5, 1, 2 mg. Injection (cypionate): 5 mg/mL (5 mL) (valerate): 20 mg/mL, 40 mg/mL syringe 2.5-3 mL, needle 22 g, 1.5 inch
Topical:vaginal cream (Estrace) 42 gram tube atrophic vaginitis:
- 2-4 g/day for 2 weeks
- reduce to 1-2 g for 2 weeks
- maintenance 1 g 3x/week
Gel: Elestrin (bioidentica) postmenopausal vasomotor symptoms
Evamist: transdermal spray, 1.53 mg/spray
Vaginal rings: see Estring, Femring
Pharmacokinetics
elimination via liver
elimination via kidney
Adverse effects
- common (> 10%)
- nausea, peripheral edema, enlargement of the breasts, breast tenderness, anorexia, bloating
- less common (1-10%)
- uncommon (< 1%)
- intolerance to contact lenses, breast tumors, amenorrhea, alterations in frequency & flow of menses, hypertension, thrombophlebitis & venous thrombosis, stroke, myocardial infarction, edema, depression, dizziness, anxiety, chloasma, melasma, rash, hyperglycemia, GI distress, increased serum triglycerides, increased LDL, cholestatic jaundice, increased susceptibility to Candida infection
- other
Drug interactions
- estradiol increases effects of:
- agents that decrease effectiveness of estrogens
Laboratory
Mechanism of action
- most potent & major secretory product of the ovary
- development & maintenance of female reproductive system
More general terms
More specific terms
Additional terms
Component of
- estradiol/progesterone
- estradiol/oxytetracycline
- estradiol/norethindrone/relugolix
- benzoate/estradiol/testosterone
- benzoate/estradiol
- estradiol/testosterone
- estradiol/norgestimate
- estradiol/ethinyl estradiol/norgestrel
- estradiol/ethinyl estradiol/norgestimate
- estradiol/ethinyl estradiol/norethindrone
- estradiol/ethinyl estradiol/levonorgestrel
- estradiol/ethinyl estradiol/ferrous fumarate/iron/norethindrone
- estradiol/ethinyl estradiol
- drospirenone/estradiol/ethinyl estradiol
- desogestrel/estradiol/ethinyl estradiol
- contraceptive/estradiol/ethinyl estradiol/levonorgestrel
- estradiol/ethinyl estradiol/ferrous fumarate/norethindrone
- estradiol/norethindrone
- estradiol/etonogestrel
- estradiol/trenbolone (Revalor)
- Angeliq (drospirenone, estradiol)
- Estrasorb
- estradiol/methoxyprogesterone
- drospirenone/estradiol
- estradiol/levonorgestrel
- estramustine (Emcyt)
- Activella
- Ortho-Prefest
- Climara Pro
- Lunelle
- Estring
- Femring
- transdermal estradiol
- dienogest/estradiol (Natazia)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 Department of Veterans Affairs, VA National Formulary
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 8(7):41 2001
- ↑ Prescriber's Letter 15(4): 2008 Estrogen-Containing Hormone Replacement Products for Postmenopausal Women Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=240407&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 6.2 Deprecated Reference
- ↑ 7.0 7.1 Brown T FDA Approves Imvexxy for Moderate to Severe Dyspareunia. Medscape - May 31, 2018. https://www.medscape.com/viewarticle/897436