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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The latest advance in the 30-year evolution of oral contraceptives (OCs) is the development of three new progestogens: desogestrel, norgestimate, and gestodene. These three new agents are derivatives of levonorgestrel, a gonane hormone, and have been used to develop pills that provide effective pregnancy prevention at lower doses than oral contraceptives using the older steroids. Desogestrel is a prohormone that must first be metabolized into its biologically active form. Norgestimate is already active, but it will be metabolized in part to levonorgestrel. Gestodene is biologically active in its native form. Among the improvements in metabolic parameters seen with this new generation of progestogens are a lack of impact on blood pressure, a balanced effect on coagulation, and a reduced impact on carbohydrate metabolism compared with earlier, higher-dose formulations. The new pills also seem to produce no negative effects on lipid and lipoprotein biosynthesis, and perhaps even improve the ratio of low-density lipoprotein to high-density lipoprotein. Cycle control with all three progestogens is improved, with much lower incidence of intermenstrual bleeding (IMB). Efficacy is as good as with other OCs. Another benefit of the new low-dose progestogens, however, is the low incidence of minor side effects observed in women using these contraceptives. Low incidences of weight gain, headache, and nausea were reported, and the dropout rate because of side effects was low in both international and US trials. Serious side effects are rarely seen with pills containing the new progestogens.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:The new era in oral contraception: pills containing gestodene, norgestimate, and desogestrel. 143 6

New progestin molecules have been synthesized for the purpose of maintaining the antiovulatory and antiestrogenic effects of existing progestins while suppressing their undesirable androgenic effects. Desogestrel, gestodene, and norgestimate are 3 third generation progestins now available in Europe in combined oral contraceptives (OCs) containing ethinyl estradiol. The 3 gonane molecules all result from modifications in the structure of levonorgestrel which neutralize its androgenic activity. The 3 molecules maintain their affinity for the androgen receptors. A review of the literature suggests that the third generation OCs have no major disadvantages compared to other low dose preparations now being marketed. Among the fundamental differences between levonorgestrel and the 3 new gonanes, the absence of the androgenic effect reveals the predominant estrogenic effect on HDL cholesterol and sex hormone binding globulin (SHBG). It appears however that the absence of androgenic effect does not affect the antiestrogenic power of the molecule at the level of the target cells such as the endometrium, or at the level of the pituitary cells. As with all low-dose formulations, a nonnegligible percentage of patients conserves ovarian activity with follicular maturation and estrogen secretion. It remains to be demonstrated whether the 2-10% of users reporting undesirable effects such as breast tenderness, swelling, headaches, and irritability are those in whom ovarian activity is not completely suppressed. The percentage of women using the third generation gonanes who conserve ovarian activity seems to be lower than that of users of the older low-dose formulations. Carbohydrate tolerance differs little from that observed with levonorgestrel. Modifications of coagulation factors reflect the estrogen content and do not differ in the third generation gonanes and older low-dose formulations. It is difficult to identify major clinical advantages of any 1 of the new preparations because of the minor differences between them. Prospective, longterm epidemiologic studies will be needed to confirm possible cardiovascular benefits and the absence of increased mammary pathology.
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PMID:[Disadvantages of third generation progestins]. 1231 28

A postmarketing observational study was carried out in a prospective, open and multi-centric manner monitoring a treatment period of 4 cycles (4 x 28 days) among Indian women of child bearing age to determine the acceptability and reliability of desogestrel (75 microg/day), an oestrogen-free pill. It involved 299 subjects recruited at each of 20 centres spread all over India. The study duration for each subject was 16 weeks with follow-up visits at 4, 8 and 16 weeks intervals. At each follow-up visit, subjects were evaluated for any failure of contraception, change in bleeding pattern and other adverse events. Of the study subjects, 238 (79.6%) continued the study for 4 cycles and were thus considered eligible for analysis of bleeding patterns with no failure of contraception. In addition, the physician's as well as patient's global assessment, demonstrated a "very good" response in majority of subjects (> 84%). A sizeable number of cases (47.9%) had infrequent episodes (1 to 5) of bleeding--spotting during the shifted reference period, while 41.2% experienced amenorrhoea. There was no clinically significant change in blood pressure or body weight. Of the 299 such subjects enrolled, 53 subjects were lost to follow-up and did not come for the 1st follow-up visit. Hence, out of the 246 subjects, 21.1% presented with 78 separate adverse events during 960 treatment cycles. None of the reported adverse events were severe and there was not even a single serious adverse effect during the course of the study. Nausea, breast tenderness and headache (7.7%, 10.1% and 9.7% respectively) were the most frequent adverse events observed during the study. Desogestrel 75 mg/day was well accepted in majority of Indian women. It provides good contraceptive efficacy, with a lower incidence of irregular bleeding and spotting episodes.
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PMID:A postmarketing observational study assessing acceptability and reliability of desogestrel only contrapceptive pill (Cerazette) in Indian women. 1744 70