Quadraphasis continuous graduated estrogen contraceptive
View Patent ↗A quadraphasic estrogenic/progestogenic contraceptive regimen that provides for a low level of estrogen in the initial phase and in the fourth phase is disclosed. Also described is a contraceptive kit that may be used to practice the method of the invention.
1. A method of contraception comprising the steps of sequentially administering to a female of child bearing age:
(a) a composition I containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and about 2 to about 9 mcg of ethinyl estradiol for about 5 to about 9 days, wherein composition I is the first composition used by the female of child bearing age in the method of contraception;
(b) a composition II containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and about 10 to about 50 mcg of ethinyl estradiol for about 5 to about 9 days;
(c) a composition III containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and about 10 to about 50 mcg of ethinyl estradiol for about 8 to about 12 days; and
(d) a composition IV substantially free of a progestogen and containing about 2 to about 9 mcg of ethinyl estradiol for about 2 to about 6 days, wherein the amount of ethinyl estradiol in composition III is greater than the amount of ethinyl estradiol in composition II by at least 5 mcg of ethinyl estradiol, the progestogen in composition I, II, and III is norethindrone acetate or norethinedrone and the sequential administration of compositions I, II, III and IV is repeated after the completion of the administration of composition IV.
2. The method according to claim 1 , wherein composition I contains an estrogen in an amount equivalent to about 2 to about 5 mcg of ethinyl estradiol.
3. The method according to claim 1 , wherein the progestogen in each of compositions I, II and III is norethindrone acetate in an amount from about 0.5 to about 1.5 mg.
4. The method according to claim 1 , wherein the progestogen in each of compositions I, II, and III is norethindrone acetate at a constant concentration.
5. The method according to claim 4 , wherein composition I contains an amount of ethinyl estradiol from about 2 to about 5 mcg.
6. The method according to claim 5 , wherein composition I contains about 5 mcg of ethinyl estradiol.
7. The method according to claim 1 , wherein the daily administration of compositions I, II, III and IV is for a 20 to 34 day period.
8. The method according to claim 7 , wherein the daily administration of compositions I, II, III and IV is for a 28 day period.
9. The method according to claim 6 , wherein composition I contains about 1.0 mg of norethindrone acetate and is administered for about 7 days, composition II contains about 1.0 mg of norethindrone acetate and is administered for about 7 days, composition III contains about 1.0 mg of norethindrone acetate and is administered for about 10 days, and composition IV contains about 5 mcg of ethinyl estradiol and is administered for about 4 days.
10. The method according to claim 9 , wherein composition II contains about 25 mcg of ethinyl estradiol and composition III contains about 30 mcg of ethinyl estradiol.