Progestins are classified according to their structure in C19 and C21 progestagens. The C19 ones are derived from testosterone, the C21 ones from progesterone. C21 progestagens include cyproterone acetate, dydrogesterone, medroxyprogesterone acetate, chlormadinone acetate, megestrol and promegestone. Of these, dydrogesterone is structurally most similar to progesterone. C19 progestagens include norethisterone, (levo)norgestrel, lynestrenol, desogestrel, norgestimate, gestodene and tibolone.

Different progestins have different combinations of androgen (testosterone-like) and progesterone activity. If the activity of 1 mg of norethindrone is taken as the baseline, 1 mg of the other progestins have activities as follows:

Norethindrone was synthetized for the first time in 1951 by the Mexican chemist Luis E. Miramontes. This substance became the basis for the contraceptive pill.

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Drospirenone-ethinyl called good option for PCOS - Expert Opinion
From OB/GYN News, 6/15/02 by Bruce Jancin

VAIL. COLO. -- The oral contraceptive drospirenone-ethinyl estradiol is a particularly attractive option for treatment of polycystic ovary syndrome in patients who don't desire pregnancy, Dr. Alan H. DeCherney said at a conference on obstetrics and gynecology sponsored by the University of Colorado.

"There's no evidence that Yasmin [drospirenone-ethinyl estradiol] is better than other OCs in polycystic ovary syndrome (PCOS), but theoretically--and I'm sure there are a number of studies going on to prove whether it's true--the fact that you replace the progestin with a spironolactone analogue makes me think that this would work much better in PCOS. I've switched most of my patients on OCs who have PCOS to Yasmin. It makes sense theoretically and it's certainly no worse than any other birth control pill," said Dr. DeCherney, professor and chair of ob.gyn. at the University of California, Los Angeles.

Each tablet of the contraceptive contains 0.03 mg of ethinyl estradiol and 3 mg of drospirenone, a novel progestin and spironolactone analogue with both antiandrogenic and antimineralocorticoid properties. Younger physicians may not be aware that for a long time, spironolactone at 25 mg b.i.d. to 100 mg b.i.d. was a popular second-line drug for the treatment of PCOS. Spironolactone effectively reduced patients' hirsutism and reversed endometrial hyperplasia while decreasing testosterone production. The problem was that it caused heavy vaginal bleeding and orthostatic hypotension at higher doses.

OCs are effective for the treatment of PCOS in two ways. Through their contraceptive effect, they lower serum LH and FSH. The estrogen in the OC stimulates the ovary to make more sex hormone--binding globulin, which in turn reduces testosterone levels.

There has been a recent flurry of interest in routinely putting all PCOS patients, or at least the half who are insulin resistant, on an insulin-sensitizing agent such as metformin. Dr. DeCherney favors using metformin indefinitely in these patients except during pregnancy because the drug corrects a key underlying metabolic defect in PCOS.

"I think it's a good idea in the real world to put patients on it right away as soon as the diagnosis is made because patients with PCOS are prone to get type 2 diabetes and endometrial hyperplasia. It takes about 3 months to get the maximum effect."

It's important that patients understand that metformin increases fertility. OCs or another form of birth control are vital in a woman with PCOS who goes on metformin.

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