(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
- 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 ↓ 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.
- Gel (Adults ): Apply contents of one packet (Divigel) or one actuation from pump (EstroGel, Elestrin) once daily.
- 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).
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
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.
estradiol transdermal system : Estradot, Oesclim