Disease relevance of norgestrel

• However, only norgestrel had an ameliorative effect on epithelial hyperplasia and metaplasia [1].
• Norgestrel and gestodene stimulate breast cancer cell growth through an oestrogen receptor mediated mechanism [2].
• The genotoxicity study of two widely used contraceptive synthetic progestins, i.e. norgestrel and norethindrone was carried out on human lymphocyte chromosomes using chromosomal aberrations (CA), sister chromatid exchanges (SCE) and cell growth kinetics as parameters [3].
• The urticaria was not adequately controlled by antihistamines or Prempak-C (conjugated oestrogens and norgestrel) [4].
• These data suggest a systemic metabolic effect of norgestrel which may play a role in accelerating atherogenesis [5].

High impact information on norgestrel

• Among patients with hemorrhagic stroke, the odds ratio for aneurysmal bleeding associated with current use of low-dose oral contraceptives containing norgestrel or levonorgestrel was 4.46 (CI, 1.58 to 12.53) [6].
• In human Jurkat T cells we demonstrate differential regulation of select kallikreins by CD3 receptor, Concanavilin A (Con A), interleukin 2 (IL2), and lipopolysaccharide (LPS)-mediated activation and by exposure to steroid hormones, dexamethasone, norgestrel, androstan and estradiol [7].
• Bone density changes during two years treatment with tibolone or conjugated estrogens and norgestrel, compared with untreated controls in postmenopausal women [8].
• We studied the influence of the 19-norprogestins norgestrel and gestodene compared to a 'non' 19-norprogestin medroxyprogesterone acetate (MPA) on MCF-7 cell proliferation [2].
• The effects of an oral contraceptive containing ethinyloestradiol and norgestrel on CYP3A activity [9].

Chemical compound and disease context of norgestrel

• Monophasic ethinyl estradiol/norgestimate was associated with an incidence of breakthrough bleeding and spotting similar to that of monophasic ethinyl estradiol/norgestrel and an incidence of amenorrhea less than that of ethinyl estradiol/norgestrel [10].
• Cyproterone acetate, a progestin used in the treatment of hirsutism, acne and prostate cancer as well as norgestrel and norethindrone that are widely used as oral contraceptives also inhibit 3 beta-HSD activity at Ki values of 1.5, 1.7 and 2.5 microM, respectively [11].
• The MWS, an observational study, showed an increased breast cancer risk in users of estrogens combined with either medroxyprogesterone acetate (MPA), norethisterone, or norgestrel [12].
• New epidemiological studies have demonstrated a higher risk of venous thromboembolism among users of oral contraceptives (OCs) with third-generation progestogens desogestrel or gestodene compared with users of OCs with second-generation progestogens levonorgestrel or norgestrel [13].

Biological context of norgestrel

• The effects of norgestrel on carbohydrate and lipid metabolism over one year [14].
• Studies of carbohydrate metabolism were conducted before and after 18 months of daily use of a 0.075-mg norgestrel preparation by 50 "normal" women [5].
• But another drug norgestrel was found to affect the genetic material [3].
• Norgestrel was gradually released into the systemic circulation, blood levels being highest during menstruation [15].
• Preliminary results of the endometrial and ovarian response to luteal phase norgestrel [16].

Anatomical context of norgestrel

• It was concluded that norgestrel itself and possibly its metabolites are potent mutagens beyond a particular dose in human lymphocytes [3].
• In all the cell lines deacetylation of the progestogen Ngmate to norgestrel oxime was complete within 24 h [17].
• 17beta-Estradiol was most effective in stimulating the motility of human spermatozoa, while norgestrel caused the strongest inhibition of forward movement [18].
• Characterization of progesterone receptor in human uterine cytosol with a synthetic progestin, norgestrel [proceedings] [19].
• 4. Clinical studies with these devices indicate that the women usually ovulate (with the exception of the high-dose norethindrone-releasing devices) while sperm penetration of the cervix was inhibited by all four fromulations, most consistently by the norgestrel-releasing devices [20].

Associations of norgestrel with other chemical compounds

• OBJECTIVE: To compare a traditional 28-day cycle to an extended 49-day cycle of the 30 microg ethinyl estradiol (E2)/300 microg norgestrel monophasic birth control pill regimen [21].
• SHBG-BC was significantly increased in the norethindrone oral contraceptive group, unchanged in the norgestrel oral contraceptive group, and significantly reduced in both contraceptive vaginal ring groups [22].
• A selective, reliable and rapid method for the simultaneous determination of progesterone and norgestrel concentrations in human serum after taking oral contraceptive tablet has been developed using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS-MS) with atmospheric pressure chemical ionization (APCI) interface [23].
• Norgestrel, ethynodiol diacetate, and norethindrone alter carbohydrate metabolism, but norgestrel produces the most marked changes [24].
• Mean Cmax and AUC values for norgestrel decreased by 12% and 10%, respectively, when administered with ABT-761 [25].

Gene context of norgestrel

• Progesterone, the parent of norgestrel, shared the latter's suppressive activity for gamma-glutamyltransferase and alkaline phosphatase biosynthesis, and behaved like its derivative towards the other enzymes [26].
• Some biological and biochemical effects (i.e. KPI, cervical mucus, SHBG and ceruloplasmin) as well as serum ethynylestradiol and serum norgestrel, following the use of two oral contraceptives containing the same amount of norgestrel (dl-norgestrel 0.5 mg) and either 30 microgram or 50 microgram of ethynylestradiol were compared [27].
• Norgestrel-stimulated T47D mice showed significantly more PSA in the tumors compared to tumors of the control mice [28].
• Norgestrel reduced TeBG binding capacity but not CBG binding capacity [29].
• In contrast to the findings of the previous study, norgestrel lowered LDL and produced less substantial decreases in HDL and HDL2 [30].

Analytical, diagnostic and therapeutic context of norgestrel

• Effect of temperature on separation of norgestrel enantiomers by high-performance liquid chromatography [31].
• We studied three groups of adult female cynomolgus macaques fed a moderately atherogenic diet: a control group, a group given ethinyl estradiol and norgestrel, and another group given ethinyl estradiol and ethynodiol diacetate [32].
• Intrauterine devices (IUD's) containing 0, 5, or 10 per cent by weight of progesterone, melengestrol acetate (MGA), norethindrone, norgestrel, medroxyprogesterone acetate, isoxsuprine, or R2323 or wound with fine copper wire were placed in one or both horns of cycling female rats [33].
• Quantitative approach for the screening of cyclodextrins by nuclear magnetic resonance spectroscopy in support of chiral separations in liquid chromatography and capillary electrophoresis enantioseparation of norgestrel with alpha-, beta- and gamma-cyclodextrins [34].
• Carbohydrate and lipid metabolism were studied with the use of a three-hour oral glucose tolerance test in 71 women before and after one year of daily oral norgestrel, 0.075 mg., treatment [14].

References