Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: DrugBank:APRD00569 (Ortho Tri-Cyclen)
 42 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Norgestimate (NGM), a derivative of 19-nortestosterone with very specific affinity for the progesterone receptor, has been used in combination with ethinyl estradiol (EE) in low doses in both monophasic and triphasic oral contraceptives (OCs). An open-label comparative clinical trial was conducted with 4234 healthy women using triphasic levonorgestrel (LNG)/EE and NGM/EE through a total of 22,312 menstrual cycles. Contraceptive efficacy was excellent with both preparations with no statistically significant between-regimen differences in pregnancy rates. The theoretical Pearl index was 0.12 for the NGM/EE triphasic, and 0.34 for the LNG/EE triphasic. Adverse experiences in both groups were typical of those which could occur among women taking low-dose OCs. The % of subjects who discontinued treatment due to use-related adverse experiences was similar among the 2 preparations; 8.6% for the NGM/EE triphasic and 6.8% for the LNG/EE triphasic. In a separate mechanism of action study, specific endocrine parameters were investigated in 20 subjects who used the NGM/EE triphasic for 4 cycles. Ovulation suppression was demonstrated in statistically significant decreases from pretreatment values in serum levels of luteinizing hormone, follicle stimulating hormone, progesterone, and estradiol. Significant on-treatment increases in serum levels of sex hormone binding globulin evidenced minimal androgenicity. All hormonal values returned to or toward normal in the posttreatment cycle. The study results support those obtained in large noncomparative studies of the NGM/EE triphasic. This phased-dose combination suppresses ovulation and is a very effective, minimally androgenic contraceptive with good safety profile.
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PMID:Comparative contraceptive efficacy and mechanism of action of the norgestimate-containing triphasic oral contraceptive. 132 57

Imperfect use of contraceptive methods notably increases the likelihood of pregnancy. One means of improving user adherence with hormonal contraception is to minimize the dosing schedule. Two forms of hormonal contraceptive have currently achieved this goal: the transdermal patch and the vaginal ring. The first and only transdermal contraceptive patch to receive worldwide regulatory approval (ethinylestradiol/norelgestromin) is a convenient approach to contraception that has a similar efficacy to oral contraceptives (OCs), but with the benefit of once-weekly administration. In addition, transdermal delivery of contraceptive hormones eliminates variability in gastrointestinal absorption, avoids hepatic first-pass metabolism, and prevents the peaks and troughs in serum concentrations that are seen with OCs. Norelgestromin, the progestin contained in the patch, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor; however, norelgestromin has negligible direct or indirect androgenic activity, suggesting that it may be suitable for women with disorders related to androgen excess (such as hirsutism, acne, and lipid disorders).Contraceptive effectiveness is usually a function of the efficacy of a contraceptive in combination with compliance with its dosing regimen. The efficacy of the contraceptive patch has been clearly demonstrated in three phase III trials, two of which were randomized comparisons with an OC. The likelihood of pregnancy was similar between these contraceptive methods; however, compliance with the patch was notably better, particularly in younger women. The safety and tolerability profile of the patch was similar to that of the OC. A cost-effectiveness analysis has suggested that the contraceptive patch is more cost effective than the OC, due to decreased costs related to unwanted pregnancy.
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PMID:A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch. 1710 21