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| home : pages : what's new in medicine vol. 5 : yasmin - birth control pill... : | |||||
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YASMIN - BIRTH CONTROL PILL CONTAINING PROGESTIN THAT RESEMBLES NATURAL PROGESTERONE.Until recently , all progestogens available in the US were derivatives of 19-nortestosterone which are strongly progestogenic.AT the World Congress of Gynecology and Obstetrics ÜSept.2000, held in Washington DC , a new type progestin-drospirenone was widely discussed.Drospirenone , a derivative of 17 alpha-spironolactone, is also strongly progestogenic; however, drospirenone has a unique pharmacological profile, notably antimineralocorticoid properties, which make it more similar to endogenous progesterone.In the second half of a normal menstrual cycle, progesterone levels rise.. Progesterone binds to its specific receptor, but also to the mineralocorticoid receptor; thus progesterone acts as a mineralocorticoid antagonist. For this reason, natriuresis is slightly enhanced in the luteal phase,and, as a reflection of the negative balance, plasma renin and aldosterone rise by 20-50%.This rise is of a compensatory nature, and prevents further sodium losses. All conventional synthetic progestogens, whether they are derivatives of 17 alpha-hydroxyprogesterone or 19-nortestosterone, lack the mineralocorticoid effect of natural progesterone. Ethinylestradiol, as the estrogenic component of combined oral contraceptives, is a sodium Ü retaining hormone.This effect is mainly due to a significant increase of the hepatic synthesis of renin substate (angiotensinogen). Even with low-dose oral contraceptives, systolic and diastolic blood pressuresmay be raised in susceptible individuals.DROSPIRENONE is a new progestogen, derived from 17alpha-spirolactone, and the relationship between its progestogenic and its antimineralocorticoid potency is almost identical to that of natural progesterone. It was found that the oral administration of 2 mg drospirenonefor 6 days led to a cumulative sodium loss of 84 mmol and a significant rise in in plasma renin and aldosterone, compared with placebo.2 mg drospirenone given from cycle days 5 to 25 to regularly menstruating women suppressed ovulation and led to a slight natriuresis without a change in BP, while renin and aldosterone slightly increased.Consequently , an oral contraceptive was designed containing 30mcq of EE and 3 mg of drospirenone YASMIN in the hope of developing of contraceptive that might prevent the Na retention brought about by the effect of EE.It was shown, that the addition of drospirenone to EE did prevent the small rise in body weight and BP observed in some women taking a conventional oral contraceptive.In comparison to bcp containing desogestrel ( Desogen, Ortho-Cept) , Yasmin kept body weight permanently lower then the other pills. Yasmin may become an especially well tolerated combined oral contraceptive, due to the striking similarity between its progestogenic component drospirenone and progesterone. Yasmin provides effective OC, excellent cycle control, good tolerability and a weight loss that confers a significant beneficial effect on compliance in women with a tendency to gain weight due to water retention. The pharmacological profile of drospirenone is very similar to natural progesterone, in particular, it has antimineralocorticoid activity. This counteracts E- mediated fluid retention, resulting in stable or slightly lowered body weight.In addition , D has antiandrogenic activity and therefore a positive effect on skin conditions. It also significantly reduces the symptoms of premenstrual dysphoric disorder, a severe form of premenstrual syndrome. --> return to menu / back ... (click) --> return to top of the page (click) |
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