Therapeutic Classification: hormones
Pharmacologic Classification: estrogens
Absorption: Well absorbed after oral administration. Readily absorbed through skin and mucous membranes.
Distribution: Widely distributed to tissues.
Metabolism/Excretion: Mostly metabolized by the liver and other tissues. Enterohepatic recirculation occurs, and more absorption may occur from the GI tract.
Half-life: Gel: 36 hr.
CV: edema, hypertension, MI, THROMBOEMBOLISM.
Derm: oily skin, acne, pigmentation, urticaria.
EENT: intolerance to contact lenses, worsening of myopia or astigmatism.
Endo: gynecomastia (men), hyperglycemia.
F and E: hypercalcemia, sodium and water retention.
GI: nausea, weight changes, anorexia, jaundice, vomiting.
GU: women: amenorrhea, dysmenorrhea, breakthrough bleeding, cervical erosions, loss of libido, vaginal candidiasis;.
men: erectile dysfunction, testicular atrophy.
Metab: ↑ appetite.
MS: leg cramps.
Neuro: headache, dementia, dizziness, lethargy, STROKE.
Misc: breast tenderness, MALIGNANCY (BREAST, ENDOMETRIAL, OVARIAN).
Estrogens should be used in the lowest doses for the shortest period of time consistent with desired therapeutic outcome. Concurrent use of progestin is recommended during cyclical therapy to decrease the risk of endometrial carcinoma in patients with an intact uterus.
Symptoms of Menopause, Atrophic Vaginitis, Moderate to Severe Dyspareunia, Female Hypogonadism, Ovarian Failure/Osteoporosis
- PO (Adults): 0.45–2 mg once daily or in a cycle.
- IM (Adults): 1–5 mg monthly (estradiol cypionate) or 10–20 mg (estradiol valerate) monthly.
- Topical, Gel (Adults): Apply contents of one packet (Divigel) or one actuation from pump (EstroGel, Elestrin) once daily.
- Topical, Spray EvaMist (Adults): 1 spray once daily, may be ↑ to 2–3 sprays once daily.
- Transdermal (Adults): Climara: 25 mcg/24-hr transdermal patch applied weekly. Vivelle-Dot: 25–50 mcg/24-hr transdermal patch applied twice weekly. Menostar: 14 mcg/24-hr transdermal patch applied every 7 days. Progestin may be administered for 10–14 days of each mo. Dotti, Lyllana, or Minivelle: 37.5 mcg/24-hr transdermal patch applied twice weekly (for treatment of vasomotor symptoms); 25 mcg/24-hr transdermal patch applied twice weekly (for prevention of postmenopausal osteoporosis).
- Vag (Adults): Cream: 2–4 g (0.2–0.4 mg estradiol) once daily for 1–2 wk, then ↓ to 1–2 g/day for 1–2 wk; then maintenance dose of 1 g 1–3 times weekly for 3 wk, then off for 1 wk; then repeat cycle once vaginal mucosa has been restored; Vaginal ring (Estring): 2-mg (releases 7.5 mcg estradiol/24 hr) every 3 mo; Vaginal ring (Femring): 12.4 mg (releases 50 mcg estradiol/24 hr) every 3 mo or 24.8 mg (releases 100 mcg estradiol/24 hr) every 3 mo (Femring requires concurrent progesterone); Vaginal insert (Vagifem, Yuvafem, or Imvexxy): 1 insert once daily for 2 wk, then 1 insert twice weekly.
Postmenopausal Breast Cancer
- PO (Adults): 10 mg 3 times daily.
Prostate Cancer
- PO (Adults): 1–2 mg 3 times daily.
- IM (Adults): 30 mg every 1–2 wk (estradiol valerate).
(Generic available)
Estradiol
- Tablets: 0.5 mg; 1 mg; 2 mg;
- In combination with: dienogest (Natazia); drospirenone (Angeliq); elagolix/norethindrone (Oriahnn); norethindrone (Activella, Amabelz, Mimvey); norgestimate (Prefest); progesterone (Bijuva); relugolix/norethindrone (Myfembree). See Appendix [not included in this PDA edition].
Estradiol Cypionate
- Injection (in oil): 5 mg/mL;
Estradiol Transdermal Preparations
- Gel packet (Divigel): 0.25 mg/pkt; 0.5 mg/pkt; 0.75 mg/pkt; 1 mg/pkt; 1.25 mg/pkt;
- Gel pump (Elestrin): 0.52 mg/actuation;
- Gel pump (Estrogel): 0.75 mg/actuation;
- Transdermal patch: 14 mcg/24-hr release rate; 25 mcg/24-hr release rate; 37.5 mcg/24-hr release rate; 50 mcg/24-hr release rate; 60 mcg/24-hr release rate; 75 mcg/24-hr release rate; 100 mcg/24-hr release rate;
- Spray: 1.53 mg/spray;
- In combination with: levonorgestrel (Climara Pro); norethindrone (Combipatch). See Appendix [not included in this PDA edition].
Estradiol Vaginal Preparations
- Vaginal cream: 0.01%;
- Vaginal tablet (Vagifem or Yuvafem): 10 mcg;
- Vaginal insert (Imvexxy): 4 mcg; 10 mcg;
- Vaginal ring (Estring): 2 mg (releases 7.5 mcg/day over 90 days);
- Vaginal ring (Femring): 12.4 mg (releases 50 mcg/day over 90 days); 24.8 mg (releases 100 mcg/day over 90 days);
Estradiol Valerate
- Injection (in oil): 10 mg/mL; 20 mg/mL; 40 mg/mL;
estradiol cypionate: Depo-Estradiol
Estradiol Tablets: Estrace
Estradiol Transdermal Gel: Divigel, Elestrin, EstroGel
estradiol transdermal spray: EvaMist
estradiol transdermal system: Alora
, Climara, Dotti, Estraderm, Lyllana, Menostar, Minivelle, Vivelle-Dot
Estradiol Vaginal Cream: Estrace
Estradiol Vaginal Insert: Imvexxy
estradiol vaginal ring: Estring, Femring
estradiol vaginal tablet: Vagifem, Yuvafem
estradiol valerate: Delestrogen
estradiol transdermal system: Estradot, Oesclim