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Hormonal contraceptives

Hormones used for contraception are two female sex hormones: estrogen and progestin. Progestin are synthetic analogues with properties similar to natural progesterone. These hormones have the following modes of action: preventing the release of eggs from the ovaries (process known as ovulation); changing the lining of the uterus (womb) to prevent pregnancy; and changing the mucus at the cervix to prevent sperms from entering the uterus.

Based on these two hormones, there are two main types of hormonal contraceptive formulations: (i) progestin-only; and (ii) combination product which contain both estrogen and a progestin. Synthetic progestins differ from natural progesterone in terms of pharmacological effects. Progestins are classified either based on structure or on time of market introduction (generation)[1]:

Generation

Progestin

First

Ethynodiol diacetate

Norethidrone

Norethidrone acetate

Norgestrel

Medroxyprogesterone acetate

Second

Levonorgestrel

Third

Desogestrel

 

The estrogen component in a combination product is very little, between 30 to 35 mcg per day and so the antiovulatory effect is predominantly due to the progestin component. The side-effect profile vary with different progestin types. In the evolution of hormonal contraceptive formulations, modifications are made to the progestin type to improve side-effect profile or lowering dose of estrogen.

The first hormonal contraceptive, Enovid™ was approved by USFDA in 1960[2]. Over the years, new mode of administrations have been developed, in addition to oral formulations, to improve tolerability, compliance and delivery such as: injectable, vaginal, implantable and transdermal.




[1] Apgar BS; Greenberg G. Using progestins in clinical practice, Am Fam Physician 65, 8 (2000): 1839-1846

[2] American Society of Reproductive Medicine. Hormonal contraception: recent advances and controversies. Fertility and Sterility 90, 3 (2008): 103-113

 

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