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Drug overview for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
Generic name: NORETHINDRONE ACETATE/ETHINYL ESTRADIOL (ES-troe-jen/proe-JES-tin)
Drug class: Contraceptives
Therapeutic class:
Estradiol (a principal endogenous estrogen) is a steroidal estrogen. Norethindrone acetate is a synthetic progestin.
Norethindrone acetate is used for the treatment of secondary amenorrhea and for the treatment of abnormal uterine bleeding caused by hormonal imbalance in patients without underlying organic pathology such as fibroids or uterine cancer. The drug also is used for the treatment of endometriosis. For the use of low-dose norethindrone as a progestin-only oral contraceptive, see Progestins 68:12. For the use of norethindrone or norethindrone acetate in combination with estrogens as an oral contraceptive, see Estrogen-Progestin Combinations 68:12.
Generic name: NORETHINDRONE ACETATE/ETHINYL ESTRADIOL (ES-troe-jen/proe-JES-tin)
Drug class: Contraceptives
Therapeutic class:
Estradiol (a principal endogenous estrogen) is a steroidal estrogen. Norethindrone acetate is a synthetic progestin.
Norethindrone acetate is used for the treatment of secondary amenorrhea and for the treatment of abnormal uterine bleeding caused by hormonal imbalance in patients without underlying organic pathology such as fibroids or uterine cancer. The drug also is used for the treatment of endometriosis. For the use of low-dose norethindrone as a progestin-only oral contraceptive, see Progestins 68:12. For the use of norethindrone or norethindrone acetate in combination with estrogens as an oral contraceptive, see Estrogen-Progestin Combinations 68:12.
DRUG IMAGES
NORETHIND-ETH ESTRAD 0.5-2.5
The following indications for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol) have been approved by the FDA:
Indications:
None.
Professional Synonyms:
None.
Indications:
None.
Professional Synonyms:
None.
The following dosing information is available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
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.
Norethindrone acetate is administered orally.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
Drug contraindication overview.
No enhanced Contraindications information available for this drug.
No enhanced Contraindications information available for this drug.
There are 0 contraindications.
There are 0 severe contraindications.
There are 0 moderate contraindications.
The following adverse reaction information is available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
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 0 severe adverse reactions.
There are 0 less severe adverse reactions.
The following precautions are available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
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 |
Although progestins have been used beginning in the first trimester of pregnancy to prevent habitual abortion or to treat threatened abortion, there is no adequate evidence from well-controlled studies to substantiate the efficacy of progestins for these uses; however, there is evidence of potential adverse effects on the fetus when these drugs are administered during the first 4 months of pregnancy. In addition, in most women, the cause of abortion is a defective ovum, which progestins could not be expected to influence. Because of their uterine-relaxant effects, progestins may delay spontaneous abortion of fertilized defective ova.
Masculinization of the female fetus has reportedly occurred when progestins were used during pregnancy. Clitoral hypertrophy and fusion of the labia have been reported in a few female neonates born to women who had received medroxyprogesterone during pregnancy; hypospadias in male neonates born to women receiving progestational agents occurs at approximately twice the rate of occurrence in male neonates born to women not receiving the drugs. An association between intrauterine exposure to female sex hormones and congenital anomalies, including cardiovascular and limb defects, has been suggested.
(See Cautions: Pregnancy, Fertility, and Lactation, in Estrogen-Progestin Combinations 68:12.) Use of progestins, including norethindrone, is not recommended during the first 4 months of pregnancy. If a woman becomes pregnant while receiving norethindrone or is inadvertently exposed to the drug during the first 4 months of pregnancy, she should be advised of the potential risks to the fetus. Norethindrone should not be used to induce withdrawal bleeding as a test for pregnancy.
Masculinization of the female fetus has reportedly occurred when progestins were used during pregnancy. Clitoral hypertrophy and fusion of the labia have been reported in a few female neonates born to women who had received medroxyprogesterone during pregnancy; hypospadias in male neonates born to women receiving progestational agents occurs at approximately twice the rate of occurrence in male neonates born to women not receiving the drugs. An association between intrauterine exposure to female sex hormones and congenital anomalies, including cardiovascular and limb defects, has been suggested.
(See Cautions: Pregnancy, Fertility, and Lactation, in Estrogen-Progestin Combinations 68:12.) Use of progestins, including norethindrone, is not recommended during the first 4 months of pregnancy. If a woman becomes pregnant while receiving norethindrone or is inadvertently exposed to the drug during the first 4 months of pregnancy, she should be advised of the potential risks to the fetus. Norethindrone should not be used to induce withdrawal bleeding as a test for pregnancy.
Progestins are reportedly distributed into milk. The manufacturers warn that the possible effects of progestins in milk on nursing infants have not been determined.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
No Known Risk
No known risk. This drug has no known risks to nursing infants and does not adversely affect lactation.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
| Drug Name | Excretion Potential | Effect on Infant | Notes |
|---|---|---|---|
| Ethinyl Estradiol | Excreted.This drug is known to be excreted in human breast milk. | This drug has been shown to have an adverse effect on the nursing infant. | May decrease milk production, use lowest dose |
No Known Risk
No known risk. This drug has no known risks to nursing infants and does not adversely affect lactation.
| Drug Name | Excretion Potential | Effect on Infant | Notes |
|---|---|---|---|
| Norethindrone | Excreted.This drug is known to be excreted in human breast milk. | It is not known whether this drug has an adverse effect on the nursing infant. (No data or inconclusive human data) | May inhibit lactation at high doses |
No enhanced Geriatric Use information available for this drug.
Precaution Exists
Geriatric management or monitoring precaution exists.
Precaution Exists
Geriatric management or monitoring precaution exists.
| Drug Name | Narrative | REN | HEP | CARDIO | NEURO | PULM | ENDO |
|---|---|---|---|---|---|---|---|
| Estrogenic Agents (systemic) | General-Use lowest possible dose for shortest duration and in combination with a progestin as indicated to reduce the risk of endometrial hyperplasia and breast cancer. Cardiovascular-May increase risk for thromboembolic events. Avoid use in patients with known, suspected, or history of arterial or venous thromboembolic disease. Neuro/Psych-May increase the risk for dementia. Genitourinary-May aggravate urinary incontinence. | N | N | Y | Y | N | N |
The following prioritized warning is available for NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol):
WARNING: Estrogens, either used alone or with a progestin, have rarely caused very serious side effects. Discuss the risks and benefits of hormone treatment with your doctor. Estrogens and progestins should not be used to prevent heart disease or dementia.
In postmenopausal women, estrogen when used with a progestin can increase the risk of heart disease (such as heart attacks), stroke, serious blood clots in the lungs/legs, dementia, and cancer of the breast/ovaries. 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 a progestin, have rarely caused very serious side effects. Discuss the risks and benefits of hormone treatment with your doctor. Estrogens and progestins should not be used to prevent heart disease or dementia.
In postmenopausal women, estrogen when used with a progestin can increase the risk of heart disease (such as heart attacks), stroke, serious blood clots in the lungs/legs, dementia, and cancer of the breast/ovaries. 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 NORETHINDRON-ETHINYL ESTRADIOL (norethindrone acetate/ethinyl estradiol)'s list of indications:
No ICD codes found for this drug.
No ICD codes found for this drug.
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