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Drug overview for DEPO-ESTRADIOL (estradiol cypionate):
Generic name: ESTRADIOL CYPIONATE (ES-tra-DYE-ol sip-EYE-oh-nate)
Drug class: Estrogens
Therapeutic class: Endocrine
Estradiol (a principal endogenous estrogen) is a steroidal estrogen.
No enhanced Uses information available for this drug.
Generic name: ESTRADIOL CYPIONATE (ES-tra-DYE-ol sip-EYE-oh-nate)
Drug class: Estrogens
Therapeutic class: Endocrine
Estradiol (a principal endogenous estrogen) is a steroidal estrogen.
No enhanced Uses information available for this drug.
DRUG IMAGES
DEPO-ESTRADIOL 5 MG/ML VIAL
The following indications for DEPO-ESTRADIOL (estradiol cypionate) have been approved by the FDA:
Indications:
Advanced prostatic carcinoma
Female hypogonadism
Hypoestrogenism due to bilateral oophorectomy
Metastatic prostate carcinoma
Primary ovarian failure
Vasomotor symptoms associated with menopause
Professional Synonyms:
Advanced cancer of prostate gland
Advanced malignant neoplasm of prostate
Advanced prostate cancer
Advanced prostate malignancy
Advanced prostatic cancer
Female hypogonadism syndrome
Metastatic malignancy of prostate
Metastatic malignant neoplasm of prostate
Metastatic malignant tumor of prostate
Metastatic prostate cancer
Indications:
Advanced prostatic carcinoma
Female hypogonadism
Hypoestrogenism due to bilateral oophorectomy
Metastatic prostate carcinoma
Primary ovarian failure
Vasomotor symptoms associated with menopause
Professional Synonyms:
Advanced cancer of prostate gland
Advanced malignant neoplasm of prostate
Advanced prostate cancer
Advanced prostate malignancy
Advanced prostatic cancer
Female hypogonadism syndrome
Metastatic malignancy of prostate
Metastatic malignant neoplasm of prostate
Metastatic malignant tumor of prostate
Metastatic prostate cancer
The following dosing information is available for DEPO-ESTRADIOL (estradiol cypionate):
Dosage of estradiol, estradiol acetate, estradiol cypionate, estradiol valerate, and ethinyl estradiol must be individualized according to the condition being treated and the tolerance and therapeutic response of the patient. To minimize the risk of adverse effects, the lowest possible effective dosage should be used. When short-term estrogen therapy is indicated (e.g., for the management of vasomotor symptoms associated with menopause; vulvar and vaginal atrophy), therapy should be discontinued as soon as possible; attempts to reduce dosage or discontinue the drug should be made at 3- to 6-month intervals.
Because of the potential increased risk of cardiovascular events, breast cancer, and venous thromboembolic events, estrogen and estrogen/progestin therapy should be limited to the lowest effective doses and shortest duration of therapy consistent with treatment goals and risks for the individual woman. Estrogen and estrogen/progestin therapy should be periodically reevaluated.
Estrogen therapy is administered continuously or cyclically. While estrogen therapy alone may be appropriate in women who have undergone a hysterectomy, many clinicians currently recommend that a progestin be added to estrogen therapy in women with an intact uterus. Addition of progestin therapy for 10 or more days of a cycle of estrogen administration or daily with estrogen in a continuous regimen reduces the incidence of endometrial hyperplasia and the attendant risk of endometrial carcinoma in women with an intact uterus.
Morphologic and biochemical studies of the endometrium suggest that 10-13 days of progestin are needed to provide maximum maturation of the endometrium and to eliminate any hyperplastic changes. The manufacturer of Menostar(R) recommends that women with an intact uterus receive a progestin for 14 days every 6-12 months. When a progestin is used in conjunction with an estrogen, the usual precautions associated with progestin therapy should be observed.
Clinicians prescribing progestins should be aware of the risks associated with these drugs and the manufacturers' labeling should be consulted. The choice and dosage of a progestin may be important factors in minimizing adverse effects.
When long-acting parenteral preparations are used in the management of conditions associated with estrogen deficiency, the drugs are usually administered once every 3-4 weeks.
For the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial oral dosage of estradiol is 1 or 2 mg daily in a cyclic regimen. For replacement therapy in female hypogonadism, female castration, or primary ovarian failure, the usual initial oral dosage of estradiol is 1 or 2 mg daily. Subsequent dosage should be adjusted according to the patient's therapeutic response, using the lowest possible effective maintenance dosage.
For the prevention of osteoporosis, an oral dosage of estradiol 0.5 mg daily in a cyclic regimen has been used. The lowest effective dosage of estradiol for this indication has not been determined.
When estradiol is used in fixed combination with norethindrone acetate (Activella(R)) for the management of moderate to severe vasomotor symptoms associated with menopause, the management of vulvar and vaginal atrophy associated with menopause, or prevention of postmenopausal osteoporosis, the usual dosage is 1 mg of estradiol combined with 0.5 mg of norethindrone acetate daily.
When estradiol is used in fixed combination with drospirenone (Angeliq(R)) for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy associated with menopause, the usual dosage is 1 mg of estradiol combined with 0.5 mg of drospirenone daily.
When estradiol is used with norgestimate (Prefest(R)) for the management of moderate to severe vasomotor symptoms associated with menopause, the management of vulvar and vaginal atrophy associated with menopause, or prevention of postmenopausal osteoporosis, the usual dosage is 1 mg of estradiol daily for 3 days followed by 1 mg of estradiol with 0.09 mg of norgestimate daily for 3 days; the regimen is continued without interruption.
For the palliative treatment of advanced, metastatic carcinoma of the breast in appropriately selected men and postmenopausal women, the usual oral dosage of estradiol is 10 mg 3 times daily. Estrogen therapy is usually continued in these patients for at least 3 months.
For the palliative treatment of advanced carcinoma of the prostate, the usual oral dosage of estradiol is 1-2 mg 3 times daily.
Transdermal estradiol is commercially available as systems that are applied once or twice weekly. Estradiol transdermal systems that are applied twice weekly include Alora(R) (available as a system delivering 0.025 mg/24 hours, 0.05 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours), Estraderm(R) (available as a system delivering 0.05 mg/24 hours or 0.1 mg/24 hours), and Vivelle(R) and Vivelle-Dot(R) (available as a system delivering 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours). Estradiol transdermal systems that are applied once weekly include Climara(R) (available as a system delivering 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours, 0.06 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours) and Menostar(R) (available as a system delivering 0.014 mg/24 hours).
In addition, transdermal estradiol/norethindrone (CombiPatch(R)) is commercially available as a system delivering 0.05 mg/24 hours of estradiol and 0.14 mg/24 hours of norethindrone acetate and as a system delivering 0.05
mg/24 hours of estradiol and 0.25 mg/24 hours of norethindrone acetate. Transdermal estradiol/levonorgestrel (Climara Pro(R)) is commercially available as a system delivering 0.045
mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel.
When Alora(R) or Estraderm(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial dosage of transdermal estradiol is one system delivering 0.05 mg/24 hours applied twice weekly in a continuous regimen in women who have undergone a hysterectomy or a cyclic regimen (3 weeks on drug followed by 1 week without the drug, and then the regimen is repeated as necessary) in women with an intact uterus.
When Climara(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the usual initial dosage of transdermal estradiol is one system delivering 0.025 mg/24 hours applied once weekly in a continuous regimen. Subsequent dosage should be adjusted according to the severity of the symptoms and the patient's therapeutic response, using the lowest possible effective maintenance dosage.
When Vivelle(R) or Vivelle-Dot(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial dosage of transdermal estradiol is one system delivering 0.0375 mg/24 hours applied twice weekly in a cyclic or continuous regimen. Subsequent dosage should be adjusted according to the patient's therapeutic response, using the lowest possible effective maintenance dosage.
In women who have undergone hysterectomy, transdermal estradiol Vivelle-Dot(R) may be applied twice a week in a continuous regimen.
When estradiol/levonorgestrel (Climara Pro(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause in women with an intact uterus, one system delivering 0.045 mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel is applied once weekly in a continuous regimen.
When estradiol/norethindrone acetate (CombiPatch(R)) is used for the management of moderate to severe vasomotor systems associated with menopause, for the management of vulvar and vaginal atrophy, or for the treatment of hypoestrogenism secondary to hypogonadism, castration, or primary ovarian failure, CombiPatch(R) may be administered as a continuous combined regimen or as a continuous sequential regimen. In the continuous combined regimen, one CombiPatch(R) system delivering 0.05 mg/24 hours of estradiol and 0.14
mg/24 hours of norethindrone acetate is applied twice weekly in a continuous regimen. If necessary, the dosage of norethindrone acetate may be increased by using the dosage system that delivers 0.25 mg/24 hours of norethindrone acetate.
In the continuous sequential regimen, one system of transdermal estradiol delivering 0.05 mg/24 hours (i.e., Vivelle(R)) is applied twice weekly for the first 14 days of a 28-day cycle then one estradiol/norethindrone acetate (CombiPatch(R)) system delivering 0.05 mg/24 hours of estradiol and 0.14
mg/24 hours of norethindrone acetate is applied twice weekly for the remaining 14 days of the cycle. If necessary, the dosage of norethindrone acetate may be increased by using the dosage system that delivers 0.25 mg/24 hours of norethindrone acetate.
When Alora(R) is used for the prevention of postmenopausal osteoporosis, the minimum dose that has been shown to be effective is one system delivering 0.025 mg/24 hours applied twice weekly in a continuous regimen.
When Climara(R) is used for the prevention of postmenopausal osteoporosis, the minimum dose that has been shown to be effective is one system delivering 0.025 mg/24 hours applied once weekly in a continuous regimen.
For the prevention of osteoporosis, the usual initial dosage of transdermal estradiol (Estraderm(R)) is one system delivering 0.05 mg/24 hours applied twice weekly in a cyclic regimen in women with an intact uterus. In women who have undergone hysterectomy, one Estraderm(R) system is applied twice weekly in a continuous regimen.
Subsequent dosage can be adjusted according to the patient's response.
For the prevention of osteoporosis, the usual dosage of transdermal estradiol (Menostar(R)) is one system delivering 0.014 mg/24 hours applied once weekly in a continuous regimen.
When Vivelle(R) or Vivelle-Dot(R) is used for the prevention of postmenopausal osteoporosis, the usual dosage is one system delivering 0.025 mg/24 hours applied twice weekly.
When estradiol/levonorgestrel (Climara Pro(R)) is used for the prevention of postmenopausal osteoporosis in women with an intact uterus, one system delivering 0.045 mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel is applied once weekly in a continuous regimen.
In women who are currently not receiving an oral estrogen, transdermal estradiol therapy can be initiated immediately. In women who are currently receiving an oral estrogen, transdermal estradiol therapy can be initiated 1 week after discontinuance of oral therapy or sooner if symptoms reappear before the week has passed.
Commercially available estradiol 0.06% topical gel (Elestrin(R)) is supplied in a non-aerosol metered-dose pump. Each depression of the pump delivers 0.87
g of gel containing 0.52 mg of estradiol. When estradiol gel (Elestrin(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the usual initial dosage is 0.87
g of gel (0.52 mg of estradiol) applied topically once daily. Prior to using the pump for the first time, the pump must be primed by fully depressing the pump 10 times; this gel should be discarded in a manner that avoids accidental exposure or ingestion by household members or pets.
Commercially available estradiol 0.06% topical gel (EstroGel(R)) is supplied in a non-aerosol metered-dose pump. Each depression of the pump delivers 1.25
g of gel containing 0.75 mg of estradiol. When estradiol gel (EstroGel(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause or the treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause, 1.25
g of gel (0.75 mg of estradiol) is applied topically once daily. Prior to using the pump for the first time, the pump must be primed by fully depressing the 93-g pump twice or depressing the 25-g pump 3 times; this gel should be discarded in a manner that avoids accidental exposure or ingestion by household members or pets.
Commercially available estradiol hemihydrate 0.25% topical emulsion (Estrasorb(R)) is supplied in foil-laminated pouches. Each pouch contains 1.74
g of emulsion. When estradiol topical emulsion (Estrasorb(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the contents of 2 pouches (delivering a total of 0.05 mg of estradiol/24 hours) are applied topically once daily.
Commercially available estradiol transdermal spray (Evamist(R)) is supplied in a metered-dose pump. The metered pump delivers a metered 90-mcL spray that contains 1.53 mg of estradiol per actuation.
When estradiol transdermal spray is used for the management of moderate to severe vasomotor symptoms associated with menopause, the recommended initial dose is one spray to the inner forearm once daily. Subsequent dosage is based on clinical response. One, two, or three sprays may be administered each morning to adjacent, non-overlapping areas of the inner forearm.
For the management of symptoms of vulvar and vaginal atrophy associated with menopause, 2-4 g of estradiol vaginal cream may be administered intravaginally once daily for 1-2 weeks, then gradually reduced to one-half the initial dosage for a similar period. Maintenance dosages of 1 g of estradiol vaginal cream administered intravaginally 1-3 times weekly may be used after restoration of the vaginal mucosa has occurred.
When estradiol vaginal ring (Estring(R)) is used for the management of postmenopausal urogenital symptoms, one ring (delivering estradiol 0.0075 mg/24 hours) is inserted into the upper third of the vaginal vault; the ring is to remain in place for 3 months. After 3 months, the ring should be removed and, if appropriate, replaced with a new ring. If the ring is expelled, the ring should be rinsed in lukewarm water and reinserted.
For the management of atrophic vaginitis, one vaginal tablet containing 25 mcg of estradiol (Vagifem(R)) is inserted intravaginally once daily (preferably at the same time each day) for 2 weeks (initial dosage). For maintenance therapy for this condition, one vaginal tablet containing 25 mcg of the drug is inserted intravaginally twice weekly.
Because of the potential increased risk of cardiovascular events, breast cancer, and venous thromboembolic events, estrogen and estrogen/progestin therapy should be limited to the lowest effective doses and shortest duration of therapy consistent with treatment goals and risks for the individual woman. Estrogen and estrogen/progestin therapy should be periodically reevaluated.
Estrogen therapy is administered continuously or cyclically. While estrogen therapy alone may be appropriate in women who have undergone a hysterectomy, many clinicians currently recommend that a progestin be added to estrogen therapy in women with an intact uterus. Addition of progestin therapy for 10 or more days of a cycle of estrogen administration or daily with estrogen in a continuous regimen reduces the incidence of endometrial hyperplasia and the attendant risk of endometrial carcinoma in women with an intact uterus.
Morphologic and biochemical studies of the endometrium suggest that 10-13 days of progestin are needed to provide maximum maturation of the endometrium and to eliminate any hyperplastic changes. The manufacturer of Menostar(R) recommends that women with an intact uterus receive a progestin for 14 days every 6-12 months. When a progestin is used in conjunction with an estrogen, the usual precautions associated with progestin therapy should be observed.
Clinicians prescribing progestins should be aware of the risks associated with these drugs and the manufacturers' labeling should be consulted. The choice and dosage of a progestin may be important factors in minimizing adverse effects.
When long-acting parenteral preparations are used in the management of conditions associated with estrogen deficiency, the drugs are usually administered once every 3-4 weeks.
For the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial oral dosage of estradiol is 1 or 2 mg daily in a cyclic regimen. For replacement therapy in female hypogonadism, female castration, or primary ovarian failure, the usual initial oral dosage of estradiol is 1 or 2 mg daily. Subsequent dosage should be adjusted according to the patient's therapeutic response, using the lowest possible effective maintenance dosage.
For the prevention of osteoporosis, an oral dosage of estradiol 0.5 mg daily in a cyclic regimen has been used. The lowest effective dosage of estradiol for this indication has not been determined.
When estradiol is used in fixed combination with norethindrone acetate (Activella(R)) for the management of moderate to severe vasomotor symptoms associated with menopause, the management of vulvar and vaginal atrophy associated with menopause, or prevention of postmenopausal osteoporosis, the usual dosage is 1 mg of estradiol combined with 0.5 mg of norethindrone acetate daily.
When estradiol is used in fixed combination with drospirenone (Angeliq(R)) for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy associated with menopause, the usual dosage is 1 mg of estradiol combined with 0.5 mg of drospirenone daily.
When estradiol is used with norgestimate (Prefest(R)) for the management of moderate to severe vasomotor symptoms associated with menopause, the management of vulvar and vaginal atrophy associated with menopause, or prevention of postmenopausal osteoporosis, the usual dosage is 1 mg of estradiol daily for 3 days followed by 1 mg of estradiol with 0.09 mg of norgestimate daily for 3 days; the regimen is continued without interruption.
For the palliative treatment of advanced, metastatic carcinoma of the breast in appropriately selected men and postmenopausal women, the usual oral dosage of estradiol is 10 mg 3 times daily. Estrogen therapy is usually continued in these patients for at least 3 months.
For the palliative treatment of advanced carcinoma of the prostate, the usual oral dosage of estradiol is 1-2 mg 3 times daily.
Transdermal estradiol is commercially available as systems that are applied once or twice weekly. Estradiol transdermal systems that are applied twice weekly include Alora(R) (available as a system delivering 0.025 mg/24 hours, 0.05 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours), Estraderm(R) (available as a system delivering 0.05 mg/24 hours or 0.1 mg/24 hours), and Vivelle(R) and Vivelle-Dot(R) (available as a system delivering 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours). Estradiol transdermal systems that are applied once weekly include Climara(R) (available as a system delivering 0.025 mg/24 hours, 0.0375 mg/24 hours, 0.05 mg/24 hours, 0.06 mg/24 hours, 0.075 mg/24 hours, or 0.1 mg/24 hours) and Menostar(R) (available as a system delivering 0.014 mg/24 hours).
In addition, transdermal estradiol/norethindrone (CombiPatch(R)) is commercially available as a system delivering 0.05 mg/24 hours of estradiol and 0.14 mg/24 hours of norethindrone acetate and as a system delivering 0.05
mg/24 hours of estradiol and 0.25 mg/24 hours of norethindrone acetate. Transdermal estradiol/levonorgestrel (Climara Pro(R)) is commercially available as a system delivering 0.045
mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel.
When Alora(R) or Estraderm(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial dosage of transdermal estradiol is one system delivering 0.05 mg/24 hours applied twice weekly in a continuous regimen in women who have undergone a hysterectomy or a cyclic regimen (3 weeks on drug followed by 1 week without the drug, and then the regimen is repeated as necessary) in women with an intact uterus.
When Climara(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the usual initial dosage of transdermal estradiol is one system delivering 0.025 mg/24 hours applied once weekly in a continuous regimen. Subsequent dosage should be adjusted according to the severity of the symptoms and the patient's therapeutic response, using the lowest possible effective maintenance dosage.
When Vivelle(R) or Vivelle-Dot(R) is used for the management of moderate to severe vasomotor symptoms associated with menopause or for the management of vulvar and vaginal atrophy, the usual initial dosage of transdermal estradiol is one system delivering 0.0375 mg/24 hours applied twice weekly in a cyclic or continuous regimen. Subsequent dosage should be adjusted according to the patient's therapeutic response, using the lowest possible effective maintenance dosage.
In women who have undergone hysterectomy, transdermal estradiol Vivelle-Dot(R) may be applied twice a week in a continuous regimen.
When estradiol/levonorgestrel (Climara Pro(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause in women with an intact uterus, one system delivering 0.045 mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel is applied once weekly in a continuous regimen.
When estradiol/norethindrone acetate (CombiPatch(R)) is used for the management of moderate to severe vasomotor systems associated with menopause, for the management of vulvar and vaginal atrophy, or for the treatment of hypoestrogenism secondary to hypogonadism, castration, or primary ovarian failure, CombiPatch(R) may be administered as a continuous combined regimen or as a continuous sequential regimen. In the continuous combined regimen, one CombiPatch(R) system delivering 0.05 mg/24 hours of estradiol and 0.14
mg/24 hours of norethindrone acetate is applied twice weekly in a continuous regimen. If necessary, the dosage of norethindrone acetate may be increased by using the dosage system that delivers 0.25 mg/24 hours of norethindrone acetate.
In the continuous sequential regimen, one system of transdermal estradiol delivering 0.05 mg/24 hours (i.e., Vivelle(R)) is applied twice weekly for the first 14 days of a 28-day cycle then one estradiol/norethindrone acetate (CombiPatch(R)) system delivering 0.05 mg/24 hours of estradiol and 0.14
mg/24 hours of norethindrone acetate is applied twice weekly for the remaining 14 days of the cycle. If necessary, the dosage of norethindrone acetate may be increased by using the dosage system that delivers 0.25 mg/24 hours of norethindrone acetate.
When Alora(R) is used for the prevention of postmenopausal osteoporosis, the minimum dose that has been shown to be effective is one system delivering 0.025 mg/24 hours applied twice weekly in a continuous regimen.
When Climara(R) is used for the prevention of postmenopausal osteoporosis, the minimum dose that has been shown to be effective is one system delivering 0.025 mg/24 hours applied once weekly in a continuous regimen.
For the prevention of osteoporosis, the usual initial dosage of transdermal estradiol (Estraderm(R)) is one system delivering 0.05 mg/24 hours applied twice weekly in a cyclic regimen in women with an intact uterus. In women who have undergone hysterectomy, one Estraderm(R) system is applied twice weekly in a continuous regimen.
Subsequent dosage can be adjusted according to the patient's response.
For the prevention of osteoporosis, the usual dosage of transdermal estradiol (Menostar(R)) is one system delivering 0.014 mg/24 hours applied once weekly in a continuous regimen.
When Vivelle(R) or Vivelle-Dot(R) is used for the prevention of postmenopausal osteoporosis, the usual dosage is one system delivering 0.025 mg/24 hours applied twice weekly.
When estradiol/levonorgestrel (Climara Pro(R)) is used for the prevention of postmenopausal osteoporosis in women with an intact uterus, one system delivering 0.045 mg/24 hours of estradiol and 0.015 mg/24 hours of levonorgestrel is applied once weekly in a continuous regimen.
In women who are currently not receiving an oral estrogen, transdermal estradiol therapy can be initiated immediately. In women who are currently receiving an oral estrogen, transdermal estradiol therapy can be initiated 1 week after discontinuance of oral therapy or sooner if symptoms reappear before the week has passed.
Commercially available estradiol 0.06% topical gel (Elestrin(R)) is supplied in a non-aerosol metered-dose pump. Each depression of the pump delivers 0.87
g of gel containing 0.52 mg of estradiol. When estradiol gel (Elestrin(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the usual initial dosage is 0.87
g of gel (0.52 mg of estradiol) applied topically once daily. Prior to using the pump for the first time, the pump must be primed by fully depressing the pump 10 times; this gel should be discarded in a manner that avoids accidental exposure or ingestion by household members or pets.
Commercially available estradiol 0.06% topical gel (EstroGel(R)) is supplied in a non-aerosol metered-dose pump. Each depression of the pump delivers 1.25
g of gel containing 0.75 mg of estradiol. When estradiol gel (EstroGel(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause or the treatment of moderate to severe symptoms of vulvar and vaginal atrophy associated with menopause, 1.25
g of gel (0.75 mg of estradiol) is applied topically once daily. Prior to using the pump for the first time, the pump must be primed by fully depressing the 93-g pump twice or depressing the 25-g pump 3 times; this gel should be discarded in a manner that avoids accidental exposure or ingestion by household members or pets.
Commercially available estradiol hemihydrate 0.25% topical emulsion (Estrasorb(R)) is supplied in foil-laminated pouches. Each pouch contains 1.74
g of emulsion. When estradiol topical emulsion (Estrasorb(R)) is used for the management of moderate to severe vasomotor symptoms associated with menopause, the contents of 2 pouches (delivering a total of 0.05 mg of estradiol/24 hours) are applied topically once daily.
Commercially available estradiol transdermal spray (Evamist(R)) is supplied in a metered-dose pump. The metered pump delivers a metered 90-mcL spray that contains 1.53 mg of estradiol per actuation.
When estradiol transdermal spray is used for the management of moderate to severe vasomotor symptoms associated with menopause, the recommended initial dose is one spray to the inner forearm once daily. Subsequent dosage is based on clinical response. One, two, or three sprays may be administered each morning to adjacent, non-overlapping areas of the inner forearm.
For the management of symptoms of vulvar and vaginal atrophy associated with menopause, 2-4 g of estradiol vaginal cream may be administered intravaginally once daily for 1-2 weeks, then gradually reduced to one-half the initial dosage for a similar period. Maintenance dosages of 1 g of estradiol vaginal cream administered intravaginally 1-3 times weekly may be used after restoration of the vaginal mucosa has occurred.
When estradiol vaginal ring (Estring(R)) is used for the management of postmenopausal urogenital symptoms, one ring (delivering estradiol 0.0075 mg/24 hours) is inserted into the upper third of the vaginal vault; the ring is to remain in place for 3 months. After 3 months, the ring should be removed and, if appropriate, replaced with a new ring. If the ring is expelled, the ring should be rinsed in lukewarm water and reinserted.
For the management of atrophic vaginitis, one vaginal tablet containing 25 mcg of estradiol (Vagifem(R)) is inserted intravaginally once daily (preferably at the same time each day) for 2 weeks (initial dosage). For maintenance therapy for this condition, one vaginal tablet containing 25 mcg of the drug is inserted intravaginally twice weekly.
No enhanced Administration information available for this drug.
| DRUG LABEL | DOSING TYPE | DOSING INSTRUCTIONS |
|---|---|---|
| DEPO-ESTRADIOL 5 MG/ML VIAL | Maintenance | Adults inject 0.2 milliliter (1 mg) by intramuscular route every 4 weeks |
No generic dosing information available.
The following drug interaction information is available for DEPO-ESTRADIOL (estradiol cypionate):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for DEPO-ESTRADIOL (estradiol cypionate):
Drug contraindication overview.
No enhanced Contraindications information available for this drug.
No enhanced Contraindications information available for this drug.
There are 15 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Acute myocardial infarction |
| Antithrombin III deficiency |
| Carcinoma of breast |
| Cerebrovascular accident |
| Deep venous thrombosis |
| Endometrial carcinoma |
| Estrogen-dependent neoplasm |
| History of deep vein thrombosis |
| History of pulmonary embolism |
| Predisposition to thrombosis |
| Protein C deficiency disease |
| Pulmonary thromboembolism |
| Severe hepatic disease |
| Thromboembolic disorder |
| Thrombophilia |
There are 11 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Bed-ridden |
| Coronary artery disease |
| Dementia |
| Family history of malignant tumor of breast |
| Hereditary angioedema |
| Hypercalcemia |
| Invasive surgical procedure |
| Malignant neoplasm of the ovary |
| Papilledema |
| Retinal thrombosis |
| Tobacco smoker |
There are 12 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Asthma |
| Edema |
| Gallbladder disease |
| Hepatic porphyria |
| Hypertriglyceridemia |
| Hypoparathyroidism |
| Hypothyroidism |
| Migraine |
| Seizure disorder |
| Systemic lupus erythematosus |
| Unspecified lump in breast |
| Uterine leiomyoma |
The following adverse reaction information is available for DEPO-ESTRADIOL (estradiol cypionate):
Adverse reaction overview.
No enhanced Common Adverse Effects information available for this drug.
No enhanced Common Adverse Effects information available for this drug.
There are 21 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
| None. |
Endometrial hyperplasia Gastroenteritis |
| Rare/Very Rare |
|---|
|
Acute myocardial infarction Cerebrovascular accident Change in corneal curvature Deep venous thrombosis Endometrial carcinoma Gallbladder obstruction Hepatitis Hypertension Hypocalcemia Influenza Involuntary muscle movement Malignant neoplasm of the ovary Neoplasm of breast Pulmonary thromboembolism Retinal thrombosis Thromboembolic disorder Thrombotic disorder Unspecified lump in breast Urticaria |
There are 29 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Abdominal distension Abdominal pain with cramps Anorexia Breast milk flow decreased Dysmenorrhea Gynecomastia Mastalgia Nausea Peripheral edema Sinusitis Vulvovaginal candidiasis Weight gain |
Bronchitis Diarrhea Dizziness Headache disorder Libido changes Migraine Mood changes Vaginal discharge Vomiting |
| Rare/Very Rare |
|---|
|
Abnormal vaginal bleeding Amenorrhea Back pain Body fluid retention Chest pain Menorrhagia Nipple discharge Upper respiratory infection |
The following precautions are available for DEPO-ESTRADIOL (estradiol cypionate):
No enhanced Pediatric Use information available for this drug.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
No enhanced Pregnancy information available for this drug.
No enhanced Lactation information available for this drug.
No enhanced Geriatric Use information available for this drug.
The following prioritized warning is available for DEPO-ESTRADIOL (estradiol cypionate):
WARNING: Estrogens, either used alone or with another hormone (progestin), have rarely caused very serious side effects. Discuss the risks and benefits of hormone treatment with your doctor. Estrogens should not be used to prevent heart disease or dementia.
Estrogens can increase the risk of cancer of the uterus (endometrial cancer). Taking a progestin as directed by your doctor can help decrease this risk. Tell your doctor right away if you have any unusual vaginal bleeding.
In postmenopausal women, estrogens, taken with or without a progestin, increase the risk of cancer of the breast/ovaries, stroke, dementia, and serious blood clots. When used along with a progestin, estrogens also increase the risk of heart disease (such as heart attacks). The risk for serious side effects may depend on the dose of estrogen and the length of time it is used.
This medication should be used at the lowest effective dose and for the shortest amount of time. Discuss the use of this medication with your doctor regularly (for example, every 3 to 6 months) to see if you still need to use it. If you will be using this medication long-term, you should have regular complete physical exams (for example, once a year) as directed by your doctor. See also Notes section.
WARNING: Estrogens, either used alone or with another hormone (progestin), have rarely caused very serious side effects. Discuss the risks and benefits of hormone treatment with your doctor. Estrogens should not be used to prevent heart disease or dementia.
Estrogens can increase the risk of cancer of the uterus (endometrial cancer). Taking a progestin as directed by your doctor can help decrease this risk. Tell your doctor right away if you have any unusual vaginal bleeding.
In postmenopausal women, estrogens, taken with or without a progestin, increase the risk of cancer of the breast/ovaries, stroke, dementia, and serious blood clots. When used along with a progestin, estrogens also increase the risk of heart disease (such as heart attacks). The risk for serious side effects may depend on the dose of estrogen and the length of time it is used.
This medication should be used at the lowest effective dose and for the shortest amount of time. Discuss the use of this medication with your doctor regularly (for example, every 3 to 6 months) to see if you still need to use it. If you will be using this medication long-term, you should have regular complete physical exams (for example, once a year) as directed by your doctor. See also Notes section.
The following icd codes are available for DEPO-ESTRADIOL (estradiol cypionate)'s list of indications:
| Advanced prostatic carcinoma | |
| C61 | Malignant neoplasm of prostate |
| Female hypogonadism | |
| E28.39 | Other primary ovarian failure |
| Hypoestrogenism due to bilateral oophorectomy | |
| E89.4 | Postprocedural ovarian failure |
| E89.40 | Asymptomatic postprocedural ovarian failure |
| E89.41 | Symptomatic postprocedural ovarian failure |
| Metastatic prostate carcinoma | |
| C61 | Malignant neoplasm of prostate |
| Primary ovarian failure | |
| E28.3 | Primary ovarian failure |
| E28.31 | Premature menopause |
| E28.310 | Symptomatic premature menopause |
| E28.319 | Asymptomatic premature menopause |
| E28.39 | Other primary ovarian failure |
| Vasomotor symptoms associated with menopause | |
| N95.1 | Menopausal and female climacteric states |
| N95.9 | Unspecified menopausal and perimenopausal disorder |
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