Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 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

The objective was to review and compare the chemistry, pharmacokinetics, efficacy, and tolerability of the newer progestins desogestrel, norgestimate, and gestodene. Data sources were primary literature on desogestrel, norgestimate, and gestodene identified from a comprehensive MEDLINE English-literature search from 1984 through 1994, with additional studies selected by review of the references. Only human clinical and pharmacokinetic trials performed in Europe, Canada, and the US were included. All available data from human studies were reviewed; both comparative and noncomparative studies were included. The newer progestins were designed to minimize the adverse effects (e.g., acne, hirsutism, nausea, blood pressure elevation, carbohydrate and lipid metabolism changes, hemostatic changes) observed with older oral contraceptives (OCs) while maintaining efficacy and good menstrual cycle control. Desogestrel, norgestimate, and gestodene have minimal amounts of androgenicity and antiestrogenic potential. All of these agents are highly bioavailable when administered orally, hepatically metabolized, and obtain steady-state concentrations after 8-10 days of continuous administration. These agents have similar Pearl Indexes and slightly better cycle control than older agents. They appear to cause fewer adverse effects such as acne and hirsutism, and similar rates of weight gain, blood pressure changes, and lipid and carbohydrate metabolism changes. Desogestrel, norgestimate, and gestodene appear to offer clinical advantages because of their decreased androgenicity; however, available data are based on relatively small studies of short duration. Women whose cycles are currently well controlled with other OCs should not be switched to a newer progestin. However, any of the combination OC products that contain these progestins may be prescribed for women intolerant of older agents or to first-time users of OCs because of their apparent efficacy, improved cycle control, superior safety, tolerability, and comparable prices. Patients who have significant acne or hirsutism with older products and diabetic women may experience clinically significant benefit with the newer agents.
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PMID:Desogestrel, norgestimate, and gestodene: the newer progestins. 852 92

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