Please wait while the formulary information is being retrieved.
Drug overview for ALYACEN (norethindrone-ethinyl estradiol):
Generic name: NORETHINDRONE-ETHINYL ESTRADIOL (proe-JES-tin/ES-troe-jen)
Drug class: Contraceptives
Therapeutic class:
Estrogen-progestin combinations are contraceptive combinations containing Norethindrone acetate is a synthetic progestin. estrogenic and progestinic steroids.
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-ETHINYL ESTRADIOL (proe-JES-tin/ES-troe-jen)
Drug class: Contraceptives
Therapeutic class:
Estrogen-progestin combinations are contraceptive combinations containing Norethindrone acetate is a synthetic progestin. estrogenic and progestinic steroids.
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
No Image Available
The following indications for ALYACEN (norethindrone-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 ALYACEN (norethindrone-ethinyl estradiol):
Estrogen-progestin oral contraceptives are usually classified according to their formulation:
*those monophasic preparations containing 50 mcg of estrogen,
*those monophasic preparations containing less than 50 mcg of estrogen (usually 20-35 mcg),
*those containing less than 50 mcg of estrogen with 2 sequences of progestin doses (biphasic),
*those containing less than 50 mcg of estrogen with 3 sequences of progestin doses (triphasic), and
*those containing 3 sequences of estrogen (e.g., 20, 30, 35 mcg) with a fixed dose of progestin (estrophasic).
Although the progestin content of the formulations also varies, oral contraceptives usually are described in terms of their estrogen content. The estrogenic and progestinic dominance of oral contraceptives depends mainly on the amount of estrogen and the amount and specific progestin contained in the formulation. The estrogenic or progestinic dominance of an oral contraceptive may contribute to hormone-related adverse effects and may be useful in selecting an alternate formulation when unacceptable adverse effects occur with a given formulation.
Whenever possible, the smallest dosage of estrogen and progestin should be used. The amount of both hormones should be considered in the choice of an oral contraceptive preparation. It is prudent and in keeping with good principles of therapeutics to minimize exposure to estrogen and progestin.
The combination used should be one which contains the least amount of estrogen and progestin that is compatible with a low failure rate and with the individual needs of the woman. Common adverse effects are usually most pronounced during the first oral contraceptive cycle and generally disappear or diminish after 3 or 4 cycles; there does not appear to be any advantage in changing preparations during this period. If minor adverse effects persist after the fourth cycle, a different combination of drugs or a different dosage may be tried.
Most fixed combinations are available as 21- or 28-day dosage preparations (conventional-cycle oral contraceptives). Some 28-day preparations contain 21 hormonally active tablets and 7 inert or ferrous fumarate-containing tablets; other 28-day preparations contain 24 hormonally active tablets and 4 inert or ferrous fumarate-containing tablets. In establishing an oral contraceptive dosage cycle, the menstrual cycle is usually considered to be 28 days.
The first day of bleeding is counted as the first day of the cycle.
One fixed-combination extended-cycle oral contraceptive (e.g., Seasonale(R)) is available as a 91-day dosage preparation containing 84 hormonally active tablets and 7 inert tablets. Other extended-cycle oral contraceptive preparations (e.g., LoSeasonique(R), Seasonique(R),) are available as 91-day preparations with 84 hormonally active tablets containing estrogen/progestin and 7 tablets containing low-dose estrogen.
One fixed-combination continuous-regimen (noncyclic) oral contraceptive (i.e., Lybrel(R)) is available as a 28-day dosage preparation containing 28 hormonally active tablets.
Each vaginal contraceptive ring containing ethinyl estradiol and etonogestrel (NuvaRing(R)) is intended to be used for one cycle which consists of a 3-week period of continuous use of the ring followed by a 1-week ring-free period. When the vaginal ring is used for contraception, one ring (delivering ethinyl estradiol 0.015 mg/24 hours and etonogestrel 0.12 mg/24 hours) is inserted into the vagina at the beginning of the cycle. After 3 weeks, the vaginal ring is removed on the same day of the week as it was inserted and at about the same time of day.
After a 1-week ring-free period, a new ring is inserted on the same day of the week as in the previous cycle. Withdrawal bleeding usually occurs within 2-3 days after removal of the ring. For contraceptive effectiveness, a new ring must be inserted 1 week after the previous ring was removed even if menstrual bleeding is not finished.
To initiate therapy, the vaginal ring (containing ethinyl estradiol and etonogestrel) usually is inserted on or before day 5 of the cycle (the first day of bleeding is counted as the first day of the menstrual cycle) in women who did not use hormonal contraception in the preceding month. During the first cycle, a back-up method of contraception (e.g., condom, spermicide) is recommended until the contraceptive ring has been used continuously for 7 days. The manufacturer states that women switching from estrogen-progestin oral contraceptives to the vaginal ring should insert the ring within 7 days of the last hormonally active tablet and no later than the day that a new oral contraceptive cycle would have been started; a back-up method of contraception is not needed.
Women switching from progestin-only contraceptives to the vaginal ring should insert the ring on any day of the month if they are switching from a progestin-only oral contraceptive (without skipping any day between receiving the last progestin oral contraceptive and the initial administration of the vaginal ring). In addition, women switching from a progestin-only contraceptive injection should insert the vaginal ring on the same day as the next contraceptive injection would have been due. Women who are switching from a progestin-only implant or a progestin-containing intrauterine device should insert the vaginal ring on the same day as the implant or the intrauterine device is removed.
A back-up method of contraception is recommended in all women switching from progestin-only contraceptives until the vaginal ring has been used continuously for 7 days.
When the woman forgets to insert a new vaginal ring at the start of any cycle, the ring should be inserted as soon as she remembers and back-up contraception must be employed until the ring has been used continuously for 7 days. If the vaginal ring is left in place for up to 1 extra week (up to 4 weeks total), the ring should be removed and a new ring can be inserted after a 1-week drug-free interval. If the ring is left in place for longer than 4 weeks, pregnancy should be ruled out and a back-up method of contraception must be used until a new ring has been used continuously for 7 days.
Women may start using the vaginal contraceptive ring in the first 5 days following a complete first-trimester abortion; a back-up method of contraception is not needed in these women. If the contraceptive preparation is not used within the mentioned 5 days, the woman should follow the general instructions for women who did not use hormonal contraception in the preceding month.
If a nonlactating woman chooses to initiate contraception postpartum with the contraceptive vaginal ring (NuvaRing(R)) before menstruation has started, the possibility that ovulation and conception may have occurred prior to initiation of contraceptive therapy should be considered, and back-up contraception must be employed for the first 7 days.
When the transdermal system containing ethinyl estradiol and norelgestromin (Ortho Evra(R)) is used for contraception, it is applied topically in a cyclic regimen using a 28-day cycle. One transdermal system (containing ethinyl estradiol 0.75 mg and norelgestromin 6 mg) is applied once weekly (same day each week) for 3 weeks, followed by a 1-week drug-free interval (drug-free interval should not exceed 7 days); then the regimen is repeated. Systemic exposure to estrogen is greater with the transdermal system (Ortho Evra(R)) than with oral contraceptive preparations because of differences in the pharmacokinetic profiles of the preparations.
Administration of the transdermal contraceptive system usually begins on the first day of the menstrual cycle or on the first Sunday after menstrual bleeding has started. A back-up method of contraception (condom, spermicide, diaphragm) should be employed for the first 7 days after application of the first system if therapy is started after day 1 of the menstrual cycle. A back-up method of contraception is not needed if the first system is applied on the first day of the menstrual cycle.
The manufacturer states that women switching from estrogen-progestin oral contraceptives to the estrogen-progestin transdermal system should apply the transdermal system on the first day of withdrawal bleeding. If there is no withdrawal bleeding within 5 days of the last hormonally active tablet, pregnancy must be ruled out. If therapy with the transdermal system is initiated after the first day of bleeding, a back-up method of contraception should be used for 7 days.
If more than 7 days elapse after receiving the last hormonally active tablet, the possibility of ovulation and conception should be considered.
When a woman has not adhered to the prescribed transdermal contraceptive regimen by not applying the estrogen and progestin-containing system at the initiation of any cycle (i.e., day 1/first week), the system should be applied as soon as it is remembered and a new dosage cycle started the same day; back-up contraception must be employed for the first 7 days of the new cycle. In addition, if the transdermal system has not been changed in the middle of the cycle (i.e., on day 8/week 2 or day 15/week 3) for 1-2 days (up to 48 hours), a new system should be applied as soon as it is remembered and the application schedule employed should be continued; back-up contraception is not needed. However, if the transdermal system has not been changed for more than 2 days (48 hours or more) in the middle of the cycle, a new dosage cycle should be started; back-up contraception must be employed for the first 7 days of the new cycle.
When the transdermal system is not removed at the end of the application schedule (i.e., on day 22/week 4), the system should be removed as soon as it is remembered and the application schedule employed should be continued (i.e., system applied on day 28); back-up contraception is not needed.
Women may start using the transdermal contraceptive system immediately after a first-trimester abortion; a back-up method of contraception is not needed. If the contraceptive preparation is not used within 5 days of a first-trimester abortion, the woman should follow instructions as if initiating transdermal contraception for the first time.
Several regimens employing short-course, high-dose oral combinations of ethinyl estradiol and norgestrel or levonorgestrel have been used safely and effectively for postcoital contraception+. One widely studied and used regimen (the ''Yuzpe'' regimen) consists of an oral dose of 100 mcg of ethinyl estradiol and 1 mg of norgestrel (administered as 2 tablets each containing 50 mcg and 0.5 mg of the drugs, respectively) within 72 hours after unprotected intercourse, initiating the first dose at a time when it would make convenient administering the subsequent repeat dose 12 hours later. Alternative combination regimens that have been used consist of a dose of 120 mcg of ethinyl estradiol and 1.2
mg of norgestrel or 0.5-0.6 mg of levonorgestrel (e.g., administered as 4 tablets each containing 30 mcg of ethinyl estradiol and 0.3 mg of norgestrel or 0.125-0.15 mg of levonorgestrel) within 72 hours after intercourse, repeating the dose 12 hours later.
Another combination regimen that has been used consists of a dose of 100 mcg of ethinyl estradiol and 0.5 mg of levonorgestrel (e.g., administered as 5 tablets each containing 20 mcg of ethinyl estradiol and 0.1 mg of levonorgestrel) within 72 hours after intercourse, repeating the dose 12 hours later. Because postcoital efficacy diminishes as the time between intercourse and initiation of estrogen-progestin combination therapy increases, such therapy should be initiated as soon as possible but preferably within 72 hours following unprotected intercourse.
If necessary, the first dose can be given up to 120 hours after unprotected intercourse. Women should be advised that taking more than the prescribed dose probably will not further decrease the risk of pregnancy, but will increase the risk of severe adverse GI effects.
If women are given a conventional mnemonic package of an oral estrogen-progestin combination for use in taking a postcoital contraceptive regimen, they should be instructed carefully regarding the number and color of the tablets to be taken with each dose and that only a portion of the contents of the package actually will be used.
Table 1. Dosage of estrogen-progestin combinations for postcoital contraception
Estrogen-progestin combination Number and color of tablets per dose formulation (brand name) Ethinyl estradiol (50 mcg) with 2 white tablets (any of 21 tablets) norgestrel (0.5 mg) (Ovral(R)) Ethinyl estradiol (50 mcg) with 2 white tablets (any of first 21 norgestrel (0.5 mg) (Ovral(R)-28) tablets) Ethinyl estradiol (30 mcg) with 4 white tablets (any of 21 tablets) norgestrel (0.3 mg) (Lo-Ovral(R)) Ethinyl estradiol (30 mcg) with 4 white tablets (any of first 21 norgestrel (0.3 mg) (Lo-Ovral(R)-28) tablets) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of 21 levonorgestrel (0.15 mg) tablets) (Nordette(R)) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of first levonorgestrel (0.15 mg) 21 tablets) (Nordette(R)-28) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of 21 levonorgestrel (0.15 mg) (Levlen(R) tablets) 21) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of first levonorgestrel (0.15 mg) (Levlen(R) 21 tablets) 28) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of last 10 levonorgestrel (0.125 mg) tablets) (Tri-Levlen(R) 21) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of tablets levonorgestrel (0.125 mg) 12-21) (Tri-Levlen(R) 28) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of last 10 levonorgestrel (0.125 mg) tablets) (Tri-Phasil(R) 21) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of tablets levonorgestrel (0.125 mg) 12-21) (Tri-Levlen(R) 28) Ethinyl estradiol (20 mcg) with 5 pink tablets (any of first 21 levonorgestrel (0.1 mg) (Lessina(R) tablets) 28)
Dose is administered initially and then repeated 12 hours later
For increasing folate concentrations in women using oral contraceptives, the combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) or ethinyl estradiol 30 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Safyral(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of acne vulgaris, the triphasic oral estrogen-progestin combination of ethinyl estradiol 35 mcg in fixed combination with norgestimate 0.18, 0.215, or 0.25
mg (Ortho-Tri-Cyclen(R)) or norethindrone 1 mg in fixed combination with ethinyl estradiol 20, 30, or 35 mcg (Estrostep(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of acne vulgaris, the estrogen-progestin combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg (Yaz(R)) or ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of premenstrual dysphoric disorder, the combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg (Yaz(R)) or ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
*those monophasic preparations containing 50 mcg of estrogen,
*those monophasic preparations containing less than 50 mcg of estrogen (usually 20-35 mcg),
*those containing less than 50 mcg of estrogen with 2 sequences of progestin doses (biphasic),
*those containing less than 50 mcg of estrogen with 3 sequences of progestin doses (triphasic), and
*those containing 3 sequences of estrogen (e.g., 20, 30, 35 mcg) with a fixed dose of progestin (estrophasic).
Although the progestin content of the formulations also varies, oral contraceptives usually are described in terms of their estrogen content. The estrogenic and progestinic dominance of oral contraceptives depends mainly on the amount of estrogen and the amount and specific progestin contained in the formulation. The estrogenic or progestinic dominance of an oral contraceptive may contribute to hormone-related adverse effects and may be useful in selecting an alternate formulation when unacceptable adverse effects occur with a given formulation.
Whenever possible, the smallest dosage of estrogen and progestin should be used. The amount of both hormones should be considered in the choice of an oral contraceptive preparation. It is prudent and in keeping with good principles of therapeutics to minimize exposure to estrogen and progestin.
The combination used should be one which contains the least amount of estrogen and progestin that is compatible with a low failure rate and with the individual needs of the woman. Common adverse effects are usually most pronounced during the first oral contraceptive cycle and generally disappear or diminish after 3 or 4 cycles; there does not appear to be any advantage in changing preparations during this period. If minor adverse effects persist after the fourth cycle, a different combination of drugs or a different dosage may be tried.
Most fixed combinations are available as 21- or 28-day dosage preparations (conventional-cycle oral contraceptives). Some 28-day preparations contain 21 hormonally active tablets and 7 inert or ferrous fumarate-containing tablets; other 28-day preparations contain 24 hormonally active tablets and 4 inert or ferrous fumarate-containing tablets. In establishing an oral contraceptive dosage cycle, the menstrual cycle is usually considered to be 28 days.
The first day of bleeding is counted as the first day of the cycle.
One fixed-combination extended-cycle oral contraceptive (e.g., Seasonale(R)) is available as a 91-day dosage preparation containing 84 hormonally active tablets and 7 inert tablets. Other extended-cycle oral contraceptive preparations (e.g., LoSeasonique(R), Seasonique(R),) are available as 91-day preparations with 84 hormonally active tablets containing estrogen/progestin and 7 tablets containing low-dose estrogen.
One fixed-combination continuous-regimen (noncyclic) oral contraceptive (i.e., Lybrel(R)) is available as a 28-day dosage preparation containing 28 hormonally active tablets.
Each vaginal contraceptive ring containing ethinyl estradiol and etonogestrel (NuvaRing(R)) is intended to be used for one cycle which consists of a 3-week period of continuous use of the ring followed by a 1-week ring-free period. When the vaginal ring is used for contraception, one ring (delivering ethinyl estradiol 0.015 mg/24 hours and etonogestrel 0.12 mg/24 hours) is inserted into the vagina at the beginning of the cycle. After 3 weeks, the vaginal ring is removed on the same day of the week as it was inserted and at about the same time of day.
After a 1-week ring-free period, a new ring is inserted on the same day of the week as in the previous cycle. Withdrawal bleeding usually occurs within 2-3 days after removal of the ring. For contraceptive effectiveness, a new ring must be inserted 1 week after the previous ring was removed even if menstrual bleeding is not finished.
To initiate therapy, the vaginal ring (containing ethinyl estradiol and etonogestrel) usually is inserted on or before day 5 of the cycle (the first day of bleeding is counted as the first day of the menstrual cycle) in women who did not use hormonal contraception in the preceding month. During the first cycle, a back-up method of contraception (e.g., condom, spermicide) is recommended until the contraceptive ring has been used continuously for 7 days. The manufacturer states that women switching from estrogen-progestin oral contraceptives to the vaginal ring should insert the ring within 7 days of the last hormonally active tablet and no later than the day that a new oral contraceptive cycle would have been started; a back-up method of contraception is not needed.
Women switching from progestin-only contraceptives to the vaginal ring should insert the ring on any day of the month if they are switching from a progestin-only oral contraceptive (without skipping any day between receiving the last progestin oral contraceptive and the initial administration of the vaginal ring). In addition, women switching from a progestin-only contraceptive injection should insert the vaginal ring on the same day as the next contraceptive injection would have been due. Women who are switching from a progestin-only implant or a progestin-containing intrauterine device should insert the vaginal ring on the same day as the implant or the intrauterine device is removed.
A back-up method of contraception is recommended in all women switching from progestin-only contraceptives until the vaginal ring has been used continuously for 7 days.
When the woman forgets to insert a new vaginal ring at the start of any cycle, the ring should be inserted as soon as she remembers and back-up contraception must be employed until the ring has been used continuously for 7 days. If the vaginal ring is left in place for up to 1 extra week (up to 4 weeks total), the ring should be removed and a new ring can be inserted after a 1-week drug-free interval. If the ring is left in place for longer than 4 weeks, pregnancy should be ruled out and a back-up method of contraception must be used until a new ring has been used continuously for 7 days.
Women may start using the vaginal contraceptive ring in the first 5 days following a complete first-trimester abortion; a back-up method of contraception is not needed in these women. If the contraceptive preparation is not used within the mentioned 5 days, the woman should follow the general instructions for women who did not use hormonal contraception in the preceding month.
If a nonlactating woman chooses to initiate contraception postpartum with the contraceptive vaginal ring (NuvaRing(R)) before menstruation has started, the possibility that ovulation and conception may have occurred prior to initiation of contraceptive therapy should be considered, and back-up contraception must be employed for the first 7 days.
When the transdermal system containing ethinyl estradiol and norelgestromin (Ortho Evra(R)) is used for contraception, it is applied topically in a cyclic regimen using a 28-day cycle. One transdermal system (containing ethinyl estradiol 0.75 mg and norelgestromin 6 mg) is applied once weekly (same day each week) for 3 weeks, followed by a 1-week drug-free interval (drug-free interval should not exceed 7 days); then the regimen is repeated. Systemic exposure to estrogen is greater with the transdermal system (Ortho Evra(R)) than with oral contraceptive preparations because of differences in the pharmacokinetic profiles of the preparations.
Administration of the transdermal contraceptive system usually begins on the first day of the menstrual cycle or on the first Sunday after menstrual bleeding has started. A back-up method of contraception (condom, spermicide, diaphragm) should be employed for the first 7 days after application of the first system if therapy is started after day 1 of the menstrual cycle. A back-up method of contraception is not needed if the first system is applied on the first day of the menstrual cycle.
The manufacturer states that women switching from estrogen-progestin oral contraceptives to the estrogen-progestin transdermal system should apply the transdermal system on the first day of withdrawal bleeding. If there is no withdrawal bleeding within 5 days of the last hormonally active tablet, pregnancy must be ruled out. If therapy with the transdermal system is initiated after the first day of bleeding, a back-up method of contraception should be used for 7 days.
If more than 7 days elapse after receiving the last hormonally active tablet, the possibility of ovulation and conception should be considered.
When a woman has not adhered to the prescribed transdermal contraceptive regimen by not applying the estrogen and progestin-containing system at the initiation of any cycle (i.e., day 1/first week), the system should be applied as soon as it is remembered and a new dosage cycle started the same day; back-up contraception must be employed for the first 7 days of the new cycle. In addition, if the transdermal system has not been changed in the middle of the cycle (i.e., on day 8/week 2 or day 15/week 3) for 1-2 days (up to 48 hours), a new system should be applied as soon as it is remembered and the application schedule employed should be continued; back-up contraception is not needed. However, if the transdermal system has not been changed for more than 2 days (48 hours or more) in the middle of the cycle, a new dosage cycle should be started; back-up contraception must be employed for the first 7 days of the new cycle.
When the transdermal system is not removed at the end of the application schedule (i.e., on day 22/week 4), the system should be removed as soon as it is remembered and the application schedule employed should be continued (i.e., system applied on day 28); back-up contraception is not needed.
Women may start using the transdermal contraceptive system immediately after a first-trimester abortion; a back-up method of contraception is not needed. If the contraceptive preparation is not used within 5 days of a first-trimester abortion, the woman should follow instructions as if initiating transdermal contraception for the first time.
Several regimens employing short-course, high-dose oral combinations of ethinyl estradiol and norgestrel or levonorgestrel have been used safely and effectively for postcoital contraception+. One widely studied and used regimen (the ''Yuzpe'' regimen) consists of an oral dose of 100 mcg of ethinyl estradiol and 1 mg of norgestrel (administered as 2 tablets each containing 50 mcg and 0.5 mg of the drugs, respectively) within 72 hours after unprotected intercourse, initiating the first dose at a time when it would make convenient administering the subsequent repeat dose 12 hours later. Alternative combination regimens that have been used consist of a dose of 120 mcg of ethinyl estradiol and 1.2
mg of norgestrel or 0.5-0.6 mg of levonorgestrel (e.g., administered as 4 tablets each containing 30 mcg of ethinyl estradiol and 0.3 mg of norgestrel or 0.125-0.15 mg of levonorgestrel) within 72 hours after intercourse, repeating the dose 12 hours later.
Another combination regimen that has been used consists of a dose of 100 mcg of ethinyl estradiol and 0.5 mg of levonorgestrel (e.g., administered as 5 tablets each containing 20 mcg of ethinyl estradiol and 0.1 mg of levonorgestrel) within 72 hours after intercourse, repeating the dose 12 hours later. Because postcoital efficacy diminishes as the time between intercourse and initiation of estrogen-progestin combination therapy increases, such therapy should be initiated as soon as possible but preferably within 72 hours following unprotected intercourse.
If necessary, the first dose can be given up to 120 hours after unprotected intercourse. Women should be advised that taking more than the prescribed dose probably will not further decrease the risk of pregnancy, but will increase the risk of severe adverse GI effects.
If women are given a conventional mnemonic package of an oral estrogen-progestin combination for use in taking a postcoital contraceptive regimen, they should be instructed carefully regarding the number and color of the tablets to be taken with each dose and that only a portion of the contents of the package actually will be used.
Table 1. Dosage of estrogen-progestin combinations for postcoital contraception
Estrogen-progestin combination Number and color of tablets per dose formulation (brand name) Ethinyl estradiol (50 mcg) with 2 white tablets (any of 21 tablets) norgestrel (0.5 mg) (Ovral(R)) Ethinyl estradiol (50 mcg) with 2 white tablets (any of first 21 norgestrel (0.5 mg) (Ovral(R)-28) tablets) Ethinyl estradiol (30 mcg) with 4 white tablets (any of 21 tablets) norgestrel (0.3 mg) (Lo-Ovral(R)) Ethinyl estradiol (30 mcg) with 4 white tablets (any of first 21 norgestrel (0.3 mg) (Lo-Ovral(R)-28) tablets) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of 21 levonorgestrel (0.15 mg) tablets) (Nordette(R)) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of first levonorgestrel (0.15 mg) 21 tablets) (Nordette(R)-28) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of 21 levonorgestrel (0.15 mg) (Levlen(R) tablets) 21) Ethinyl estradiol (30 mcg) with 4 light-orange tablets (any of first levonorgestrel (0.15 mg) (Levlen(R) 21 tablets) 28) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of last 10 levonorgestrel (0.125 mg) tablets) (Tri-Levlen(R) 21) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of tablets levonorgestrel (0.125 mg) 12-21) (Tri-Levlen(R) 28) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of last 10 levonorgestrel (0.125 mg) tablets) (Tri-Phasil(R) 21) Ethinyl estradiol (30 mcg) with 4 yellow tablets (any of tablets levonorgestrel (0.125 mg) 12-21) (Tri-Levlen(R) 28) Ethinyl estradiol (20 mcg) with 5 pink tablets (any of first 21 levonorgestrel (0.1 mg) (Lessina(R) tablets) 28)
Dose is administered initially and then repeated 12 hours later
For increasing folate concentrations in women using oral contraceptives, the combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) or ethinyl estradiol 30 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Safyral(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of acne vulgaris, the triphasic oral estrogen-progestin combination of ethinyl estradiol 35 mcg in fixed combination with norgestimate 0.18, 0.215, or 0.25
mg (Ortho-Tri-Cyclen(R)) or norethindrone 1 mg in fixed combination with ethinyl estradiol 20, 30, or 35 mcg (Estrostep(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of acne vulgaris, the estrogen-progestin combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg (Yaz(R)) or ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
For the treatment of premenstrual dysphoric disorder, the combination of ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg (Yaz(R)) or ethinyl estradiol 20 mcg in fixed combination with drospirenone 3 mg and levomefolate calcium 0.451 mg (Beyaz(R)) is used in the same dosage and administration (i.e., timing of initiation of therapy) as used in contraception.
Norethindrone acetate is administered orally. Estrogen-progestin combination contraceptives are administered orally, intravaginally, and percutaneously by topical application of a transdermal system to the skin.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for ALYACEN (norethindrone-ethinyl estradiol):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for ALYACEN (norethindrone-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 ALYACEN (norethindrone-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 ALYACEN (norethindrone-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.
Although preliminary evidence suggested that oral contraceptives could cause serious fetal toxicity when administered to pregnant women, current evidence does not suggest an association between inadvertent use of oral contraceptives in early pregnancy and teratogenic effects (including cardiovascular and limb defects, which have been reported following use of sex hormones). In addition, extensive epidemiologic studies have revealed no increased risk of birth defects in neonates born to women who used estrogen-progestin contraceptives prior to pregnancy. However, since the risks of estrogen-progestin contraceptive use clearly outweigh any possible benefit in women who are pregnant, these agents are contraindicated in such women.
Although estrogens and/or progestins were previously used to treat threatened or habitual abortion, there is considerable evidence that estrogens are ineffective and no evidence from well-controlled studies that progestins are effective for these uses. Progestin-only or estrogen-progestin contraceptives should not be used to induce withdrawal bleeding as a test of pregnancy. Data concerning pregnancy outcomes following unsuccessful emergency postcoital contraception with estrogen-progestin combinations are limited, in part because such women may choose abortion following failure of postcoital contraception.
Pooled data from several controlled trials that followed pregnancies that occurred despite postcoital estrogen-progestin combinations indicate delivery of 45 healthy neonates, 1 neonate with absent left kidney, and 2 neonates with minor anomalies. In addition, numerous studies evaluating teratologic risk of conception during cyclic (routine) oral contraceptive regimens (for both currently available low-dose oral contraceptive regimens and older, high-dose preparations (e.g., 150 mcg of ethinyl estradiol daily) that are no longer available) indicate no increased fetal risks. Exposure to the amount of estrogen-progestin in postcoital contraceptive regimens is not large when compared with the total amount of the estrogen-progestin cyclic (routine) oral contraceptive regimens, and there currently is no evidence of substantial risk to the fetus with such short-term exposure.
Estrogen-progestin postcoital contraceptive regimens are contraindicated in pregnancy because of lack of efficacy, not because of adverse effects on the fetus. In women who have missed 2 consecutive menstrual periods during estrogen-progestin conventional-cycle contraceptive use, the drug should be withheld until pregnancy has been ruled out. In women using a fixed-combination extended-cycle oral contraceptive (e.g., LoSeasonique(R), Seasonale(R), Seasonique(R)), the possibility of pregnancy should be considered after one missed menstrual period.
When the woman has not adhered to the prescribed oral contraceptive regimen, the possibility of pregnancy should be considered after one missed menstrual period and the drug should be withheld until pregnancy has been ruled out. A back-up method of contraception should be instituted until the possibility of pregnancy has been eliminated. If pregnancy is confirmed, the woman should be informed of the potential hazard to the fetus and the advisability of continuing the pregnancy should be weighed against the risks of exposure of the fetus to the drugs.
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.
Although preliminary evidence suggested that oral contraceptives could cause serious fetal toxicity when administered to pregnant women, current evidence does not suggest an association between inadvertent use of oral contraceptives in early pregnancy and teratogenic effects (including cardiovascular and limb defects, which have been reported following use of sex hormones). In addition, extensive epidemiologic studies have revealed no increased risk of birth defects in neonates born to women who used estrogen-progestin contraceptives prior to pregnancy. However, since the risks of estrogen-progestin contraceptive use clearly outweigh any possible benefit in women who are pregnant, these agents are contraindicated in such women.
Although estrogens and/or progestins were previously used to treat threatened or habitual abortion, there is considerable evidence that estrogens are ineffective and no evidence from well-controlled studies that progestins are effective for these uses. Progestin-only or estrogen-progestin contraceptives should not be used to induce withdrawal bleeding as a test of pregnancy. Data concerning pregnancy outcomes following unsuccessful emergency postcoital contraception with estrogen-progestin combinations are limited, in part because such women may choose abortion following failure of postcoital contraception.
Pooled data from several controlled trials that followed pregnancies that occurred despite postcoital estrogen-progestin combinations indicate delivery of 45 healthy neonates, 1 neonate with absent left kidney, and 2 neonates with minor anomalies. In addition, numerous studies evaluating teratologic risk of conception during cyclic (routine) oral contraceptive regimens (for both currently available low-dose oral contraceptive regimens and older, high-dose preparations (e.g., 150 mcg of ethinyl estradiol daily) that are no longer available) indicate no increased fetal risks. Exposure to the amount of estrogen-progestin in postcoital contraceptive regimens is not large when compared with the total amount of the estrogen-progestin cyclic (routine) oral contraceptive regimens, and there currently is no evidence of substantial risk to the fetus with such short-term exposure.
Estrogen-progestin postcoital contraceptive regimens are contraindicated in pregnancy because of lack of efficacy, not because of adverse effects on the fetus. In women who have missed 2 consecutive menstrual periods during estrogen-progestin conventional-cycle contraceptive use, the drug should be withheld until pregnancy has been ruled out. In women using a fixed-combination extended-cycle oral contraceptive (e.g., LoSeasonique(R), Seasonale(R), Seasonique(R)), the possibility of pregnancy should be considered after one missed menstrual period.
When the woman has not adhered to the prescribed oral contraceptive regimen, the possibility of pregnancy should be considered after one missed menstrual period and the drug should be withheld until pregnancy has been ruled out. A back-up method of contraception should be instituted until the possibility of pregnancy has been eliminated. If pregnancy is confirmed, the woman should be informed of the potential hazard to the fetus and the advisability of continuing the pregnancy should be weighed against the risks of exposure of the fetus to the drugs.
Progestins are reportedly distributed into milk. The manufacturers warn that the possible effects of progestins in milk on nursing infants have not been determined. Estrogen-progestin contraceptives may decrease the quantity and quality of milk if given in the immediate postpartum period.
Small amounts of the hormonal agents in estrogen-progestin contraceptives are distributed into milk and adverse effects such as jaundice and breast enlargement have been reported in nursing infants of women receiving cyclic regimens; therefore, because of the theoretical risk, some clinicians recommend that lactating women receiving high-dose postcoital contraceptive regimens use alternative milk sources for their infants for at least 24 hours after completion of the regimen. When possible, the use of cyclic estrogen-progestin contraceptives should be deferred until the infant has been weaned. Long-term follow-up after oral contraceptive use showed no apparent clinical effect on breast-feeding mothers or children whose mothers were breast-feeding and using oral contraceptives.
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.
Small amounts of the hormonal agents in estrogen-progestin contraceptives are distributed into milk and adverse effects such as jaundice and breast enlargement have been reported in nursing infants of women receiving cyclic regimens; therefore, because of the theoretical risk, some clinicians recommend that lactating women receiving high-dose postcoital contraceptive regimens use alternative milk sources for their infants for at least 24 hours after completion of the regimen. When possible, the use of cyclic estrogen-progestin contraceptives should be deferred until the infant has been weaned. Long-term follow-up after oral contraceptive use showed no apparent clinical effect on breast-feeding mothers or children whose mothers were breast-feeding and using oral contraceptives.
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 ALYACEN (norethindrone-ethinyl estradiol):
WARNING: Do not use this medication if you smoke cigarettes/use tobacco and are over 35 years old. Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from hormonal birth control (such as the pill, patch, ring). The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.
WARNING: Do not use this medication if you smoke cigarettes/use tobacco and are over 35 years old. Smoking raises your risk of stroke, heart attack, blood clots, and high blood pressure from hormonal birth control (such as the pill, patch, ring). The risk of these serious problems increases with age and with the number of cigarettes you smoke. Do not smoke or use tobacco.
The following icd codes are available for ALYACEN (norethindrone-ethinyl estradiol)'s list of indications:
No ICD codes found for this drug.
No ICD codes found for this drug.
Formulary Reference Tool