Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Norgestimate”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 109 records · Page 6Linked to original sources
PubMed1996

Comparative pharmacology of newer progestogens.

The newer progestogens desogestrel, norgestimate, gestodene, dienogest and nomegestrol share the common property of having weak or no androgenic effects, but there is great variation between agents in their pharmacokinetic properties and hormonal activities. Both desogestrel (acting as 3-keto-desogestrel) and norgestimate (acting mainly through levonorgestrel) are prodrugs. While nomegestrol is derived from 19-norprogesterone, the other compounds are 19-nortestosterone derivatives: desogestrel, norgestimate and gestodene belong to the subgroup of 13-ethyl-gonanes with an ethinyl group at C17 alpha, and dienogest represents an estrane (13-methyl-gonane) with a cyanomethyl group at C17 alpha. Both dienogest and nomegestrol have antiandrogenic properties. In proportion to the dose, the highest serum concentrations are observed after intake of gestodene. When combined with ethinylestradiol, gestodene and 3-keto-desogestrel accumulate in serum during daily treatment because of slowed-down elimination. This is probably caused both by binding to sex hormone-binding globulin (SHBG) and by inhibition of inactivating enzymes. Dienogest does not accumulate in serum, although at a dose of 2 mg very high serum concentrations of dienogest are reached. The most potent progestogens are gestodene and desogestrel, while the effect of dienogest and nomegestrol on endometrium and cervix is less, even though in a similar range. As the ovulation-inhibiting effect is brought about not only by receptor-mediated interactions but also by a direct inhibition of steroid biosynthesis, dienogest and nomegestrol are much less effective than gestodene, desogestrel and norgestimate. Ethinylated progestogens, particularly gestodene, have been demonstrated to inhibit cytochrome P450 enzymes. Both gestodene and desogestrel may moderately reduce SHBG levels and counteract the stimulating effect of ethinylestradiol on hepatic serum proteins, while dienogest and nomegestrol have no influence. Compared with progestogens with androgenic properties which may restrict the stimulatory action of ethinylestradiol on haemostatic parameters, the newer progestogens do not seem to be superior with respect to haemostasis. There are no data on the direct effect of the compounds on the arterial and venous vessel wall. Due to the less pronounced antagonism on ethinylestradiol-induced changes in lipid metabolism, the newer progestogens appear to be beneficial rather than deleterious, although atherosclerosis was probably not promoted by the older formulations because of the direct effect of ethinylestradiol on the arterial wall. There is no evidence for a lesser impact of the newer progestogens on carbohydrate metabolism, which is mostly impaired by the estrogen component in oral contraceptives. Formulations containing the newer progestogens are, however, preferable in patients with hyperandrogenaemia, the symptoms of which may be improved by the suppression of total and free testosterone and an increase in SHBG; an additional beneficial effect of the antiandrogenic properties of dienogest or nomegestrol remains to be proven.

Animals↗
PubMed1987

A comparison of the potencies and activities of progestogens used in contraceptives.

The potencies and activities of six progestational agents, norethindrone, levonorgestrel, desogestrel, medroxyprogesterone acetate (MPA), progesterone (P) and norgestimate have been evaluated using standard laboratory bioassays. The endocrine activities measured are those most closely related to the clinically important actions of contraceptives. Relative potencies varied with parameter measured, route of administration and species showing clearly that each progestogen is a distinct pharmacological entity. The order of potency using oral administration for either ovulation inhibition or endometrial stimulation in rabbits was desogestrel greater than levonorgestrel greater than MPA greater than norgestimate greater than norethindrone. Levonorgestrel was more androgenic than desogestrel, and P, norethindrone, norgestimate and MPA were essentially devoid of androgen activity. This profile demonstrates clear differences in the potencies and activities of these progestogens and in their selectivity for target organs.

Androgens↗
PubMed2004

Ovarian follicular development is initiated during the hormone-free interval of oral contraceptive use.

We evaluated ovarian follicular development in women during compliant use of oral contraceptives (OC). Thirty-six healthy women received: [35 microg ethinyl estradiol (21)/180 microg norgestimate (7), 215 microg norgestimate (7), 250 microg norgestimate (7)]; [30 microg ethinyl estradiol (21)/150 microg desogestrel (21)]; or [20 microg ethinyl estradiol (21)/100 microg levonorgestrel (21)] for 3 consecutive 28-day cycles. Transvaginal ultrasonography was performed every third day to monitor follicular development. If a follicle reached > or = 14 mm, ultrasonography was performed daily and blood drawn every other day to determine estradiol-17beta concentrations. Seventeen of 36 women (47%) grew follicles > or = 10 mm. Nine of the 17 women (53%) grew follicles > or = 14 mm, in association with increased serum concentrations of estradiol-17beta. Thirty-seven of 43 follicles > or = 10 mm (86%) emerged during the hormone-free interval (HFI). No ovulations were observed. Our results supported the hypothesis that follicular development to an ostensibly ovulatory diameter occurs during compliant OC use, in association with loss of endocrine suppression during the HFI.

Adolescent↗
PubMed1998

The tolerability of a triphasic norgestimate/EE-containing OC: results from a double-blind, placebo-controlled trial.

Objective: To compare adverse event data collected during administration of a triphasic norgestimate ethinyl estradiol (EE) containing oral contraceptive (OC) [ORTHO TRI-CYCLEN(R)] or placebo.Methods: Four-hundred fifty-two females between the ages of 15 and 49 years were enrolled in two multicenter, double-blind, randomized, placebo-controlled studies. These studies were conducted to evaluate the effectiveness of triphasic norgestimate/EE in the treatment of acne vulgaris (Redmond G, Olson W, Lippman J, et al. Norgestimate and ethinyl estradiol in the treatment of acne vulgaris: a randomized placebo-controlled trial. Obstet Gynecol 1997;89:X-X; Lucky A, Henderson T, Olson W, et al. The effectiveness of norgestimate and ethinyl estradiol in treating acne vulgaris. J Am Acad Dermatol, in press). Participants returned to the study centers monthly for evaluation. At each visit, interviews were conducted to elicit and record the occurrence of adverse events. Reports were derived by nondirected questioning.Results: The table below describes the number and percentage of subjects reporting the event during the 6-month period. Note that, over the range of percentages observed, the differences detectable with a power of 0.80 range from approximately 4% to 12%.Conclusion: Excellent tolerability for the triphasic norgestimate/EE OC is demonstrated by a low rate of side effects that did not differ in a statistically significant manner from placebo.

Journal Article↗
PubMed1997

Steroid hormone regulation of prostate-specific antigen gene expression in breast cancer.

We have recently reported that about 30-40% of female breast tumours produce prostate-specific antigen (PSA) and that PSA production is associated with the presence of oestrogen (ER) and progesterone (PR) receptors. We have now developed a tissue culture system to study the regulation of the PSA gene in breast cancer. The breast carcinoma cell line T-47D produces PSA when stimulated by androgens, progestins and glucocorticoids/mineralocorticoids but not oestrogens. PSA mRNA appears approximately 2 h after stimulation; PSA protein appears after 4-8 h. Among 38 compounds tested, only androgens and progestins were able to stimulate PSA production at concentrations below 10(-9) M. Evidence that the progesterone and androgen receptors can regulate the PSA gene independently was provided as follows: (a) the progestin norgestimate, which does not bind to the androgen receptor, up-regulates the PSA gene at concentrations as low as 10(-10) M; (b) triamicinolone acetonide, which does not bind to the androgen receptor (AR) but binds to the PR, acts similarly to norgestimate; (c) the antiandrogen cyproterone acetate, which blocks the androgen receptor but has progestational activity, up-regulates the PSA gene at concentrations as low as 10(-10) M; (d) the antiprogestine mifepristone completely blocks the stimulation of the specific progestin norgestimate. Our tissue culture system identified androgen-progestin agonist activities of 17 alpha-ethinyloestradiol, the antioestrogen RU56, 187 and the antiprogestin mifepristone. Our data suggest that the expression of the PSA gene in the female breast is under the control of androgens and progestins. Our tissue culture system is a highly sensitive in vitro method for evaluating the biological activity of candidate compounds having agonist and antagonist steroid hormone activity.

Androgens↗
PubMed2000

Inhibition of skin 5 alpha-reductase by oral contraceptive progestins in vitro.

Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5 alpha-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5 alpha-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5 alpha-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5 alpha-reductase activity with an IC50 value of 10 microM, followed by levonorgestrel (IC50 52 microM), dienogest (IC50 55 microM), cyproterone acetate (IC50 87 microM) and gestodene (IC50 98 microM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5 alpha-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women.

3-Oxo-5-alpha-Steroid 4-Dehydrogenase↗
PubMedDate not supplied

The use of a large-scale surveillance system in Planned Parenthood Federation of America clinics to monitor cardiovascular events in users of combination oral contraceptives.

BACKGROUND: The publication of a series of papers based on three large, case-controlled studies raised questions about the safety of oral contraceptives (OCs) containing either desogestrel or gestodene as the progestational agent. In light of these studies, the Planned Parenthood Federation of America (PPFA) assessed the risk of thromboembolic events in patients who attended its clinics in the United States (U.S.). These PPFA patients were prescribed contraceptives containing one of the following progestins: desogestrel, levonorgestrel, norethindrone, or norgestimate. All of the contraceptives used contained either 30 or 35 microg of estrogen. METHODS: In this retrospective analysis, the association between the occurrence of a thromboembolic event, OC use, and progestin type was assessed in a group of PPFA patients. These patients were prescribed 2,265,087 woman-years (WY) of OCs from January 1, 1993 to December 31, 1995. RESULTS: Seventy events (deep vein thromboses [DVTs], pulmonary emboli [PEs], myocardial infarctions [MIs], and cerebral-vascular accidents [CVAs] were reported; a rate of 3 events per 100,000 WY of use. Five deaths occurred, at a rate of 0.22 per 100,000 WY of use. This low rate of incidents appears to be related to the younger age of PPFA patients and to the use of uniform guidelines for the selection and follow-up patients. Only the lower relative risk of PE reached statistical significance, when either norethindrone or norgestimate was compared to desogestrel-containing pills, but the absolute risk of these events was lower than in other published studies. Though the overall risk varied from a low of 1.895 events per 100,000 WY for norgestimate OC users to a high of 3.969 events per 100,000 WY for desogestrel OC users, these differences were not statistically significant. CONCLUSIONS: This study supports the conclusion that OCs containing 30 or 35 microg of estrogen, combined with one of the four previously identified progestins, carry an extremely low risk of a thromboembolic event, particularly when prescribing is based on a defined medical protocol. Overall, these four groups of low-dose estrogen-containing OCs appear safer than any previously published study has indicated.

Adult↗
PubMed1988

[New progestational hormones].

The pharmacology and the application in oral hormonal contraceptives of four new progestogens--gestodene, desogestrel, norgestimate, and dienogest--are described in a survey. Although derived from 19-norethisterone these progestogens exhibit in clinical dosages no androgenic effects. Both in animal and in human tests gestodene possesses the highest progestogenic potency followed by levonorgestrel, desogestrel, norgestimate, and dienogest. The monophasic preparations with the new progestogens (femovan--gestodene, marvelon--desogestrel, cilest--norgestimate, certostat--dienogest) are safe contraceptives and the incidence of bleeding disturbancies amount to about 5%. After administration of these monophasic contraceptives the concentration of SHBG in serum increases and as a result of this the level of free testosterone decreases. Further a favourable effect on lipid metabolism is observed. In spite of a different progestogen content these combination pills are almost without influence on biochemical parameters and carbohydrate metabolism.

Contraceptives, Oral, Hormonal↗
PubMed1995

Comparative evaluation of the androgenicity of four low-dose, fixed-combination oral contraceptives.

Changes in endogenous androgen metabolism were compared in healthy women taking one of four low-dose modern oral contraceptives (OCs). One hundred women were randomized to (1) 35 micrograms ethinyl estradiol (EE) + 250 micrograms norgestimate (Cilest); (2) 20 micrograms EE + 150 micrograms desogestrel (Mercilon); (3) 30 micrograms EE + 150 micrograms desogestrel (Marvelon); or (4) 30 micrograms EE + 75 micrograms gestodene (Femodene). During the luteal phase of the pretreatment cycle, body weight and blood pressure were recorded, and plasma levels of the following variables were recorded: sex-hormone-binding globulin (SHBG), cortisol-binding globulin (CBG), testosterone, free testosterone, dihydrotestosterone, androstenedione, dihydroepiandrosterone sulfate (DHEAS), and hydroxyprogesterone. The free androgen index was also calculated. These variables were remeasured during the third week of OC intake and during the fourth and sixth cycles. There were no statistically significant differences in androgenic variables among the four OCs. The DHEAS concentration decreased less with the 20 micrograms EE + desogestrel formulation compared with either 30 micrograms EE + desogesterel or norgestimate-containing formulations (20% vs. 45%). Concentrations of SHBG and CBG increased significantly in all four groups (average 263 +/- 119% and 94 +/- 26%, respectively); CBG increased less in women taking 20 micrograms EE + desogestrel (about 75%) than in the other formulations (about 100%). The four modern, low-dose OCs tested had similar impacts on endogenous androgen metabolism, yielding significant decreases in testosterone, dihydrotestosterone, androstenedione, and DHEAS. All of these formulations may be beneficial in women with androgen-related syndromes such as acne and hirsutism. Large studies are under way to establish which of the third-generation OCs is the least androgenic. In vitro studies suggest that norgestimate has the least androgenic profile.

Adult↗
PubMed1992

Long-term profile of a new progestin.

Major complications attributable to oral contraceptives (OCs) may occur in the circulatory system. The inherent risk factors, such as race and family history, are unchangeable. Others may be altered by patient counseling and subsequent adjustment of certain behaviors. Hypercoagulability is estrogen dose related. Older, high-dose-estrogen OC users were at 40% increased risk of mortality from thromboembolic phenomena. Reduction in estrogen content has unmasked the androgenic effects of some synthetic progestogens. These effects may include progression of atherogenesis, effected through changes in cholesterol and lipoproteins; reduction in sex hormone binding globulin (SHBG), which enhances the androgenic effect; and changes in carbohydrate metabolism. This review of clinical findings is based on four studies; three had prospective cohort designs, and one was a prospective randomized comparison of a norgestimate-containing OC with a norgestrel-containing one. Numbers of subjects ranged from 20 to 59,701; the largest evaluated 343,348 cycles of treatment. Study intervals were from 4 to 24 months. The findings reported here are from the individual studies. 1. The normal value for cholesterol is less than 200 mg/dL. Of 2,197 women who met this cut-off point, 95% remained below it after 6 months of treatment. Of 756 who initially exceeded this value, 25% were below after 6 months and 75% remained above it. All studies to date have demonstrated that norgestimate produces consistent and significant elevations in high-density lipoprotein levels and variable change in low-density lipoproteins. A similar effect was noted on serum triglyceride values.(ABSTRACT TRUNCATED AT 250 WORDS)

Blood Coagulation↗
PubMed1992

Noncontraceptive benefits of modern low-dose oral contraceptives.

Most oral contraceptive formulations in current use contain 50 micrograms or less of ethinyl estradiol and 1 mg or less of the various progestins: norethindrone (0.5-1 mg), norgestrel (0.3-0.5 mg), or levonorgestrel (0.05-0.25 mg) [1]. The new generation of progestins--norgestimate, desogestrel and gestodene--are derived from levonorgestrel, the biologically active enantiomer of norgestrel. These steroids have specific metabolic and pharmacologic activity that allow oral contraception at lower doses than previous progestins. Desogestrel and norgestimate are both prodrugs and must undergo hepatic and gastrointestinal metabolism to become biologically active compounds. Gestodene is immediately and completely bioavailable [2]. For the new formulations containing less than 50 micrograms of ethinyl estradiol, the incidence of complications has decreased. With most of the early medical problems identified, current research can now focus on other aspects of oral contraception such as compliance and OC use failure. Prominent noncontraceptive health benefits have been observed in OC users and represent new directions for future research. When the risk-benefit ratio of OC use is evaluated in healthy women today, it clearly favors the benefits. However, these will not be fully realized without an increase in method compliance.

Blood Coagulation↗
PubMed1989

[New progestins in oral hormonal contraceptives].

Three new progestins with a high gestagenic potency have been developed as derivatives of the levonorgestrel (in brackets: biological active substance in the human): desogestrel (3-keto-desogestrel), norgestimate (norgestimate), gestodene (gestodene). In combination with low dosages of ethinylestradiol (30-35 micrograms) an excessive steroid overload can be avoided, which is not necessary for contraceptive efficacy and control of the menstrual cycle. As an effect of dose reducing during long-time studies only a mild impact on the lipids and carbohydrates, and blood coagulation could be observed. The clinical side effects are moderate and for most patients acceptable.

Contraceptives, Oral, Hormonal↗
PubMed1987

New progestogens in oral contraceptives.

The aim of using new synthetic progestogens (gestodene and norgestimate) in oral hormonal contraceptives is to find a combination that has a more beneficial effect on metabolism and endometrium than presently available formulations. Our studies with low-dose pills containing 30 micrograms ethinyl estradiol/150 micrograms levonorgestrel or 30 micrograms ethinyl estradiol/150 micrograms desogestrel compared with the new pills with 35 micrograms ethinyl estradiol/250 micrograms norgestimate or 30 micrograms ethinyl estradiol/75 micrograms gestodene revealed no significant alterations of serum glucose after glucose loading. With all four combination pills, insulin levels were slightly elevated when compared with controls. Studies of the lipid metabolism showed that depending on the type and estrogen combination, progestogens have different effects on lipid metabolism. The new progestogens seem to have a more pronounced effect on triglycerides, whereas total cholesterol and high-density lipoprotein cholesterol remain almost unchanged. In general, it could be shown that low-dose oral contraceptives have little impact on lipid metabolism. Studies with low-dose monophasic preparations, including the new formulations, reveal only a low effect on blood coagulation. According to our and other data on the new progestogens in oral contraceptives available so far, it can be expected that such low-dose monophasic and triphasic combination pills will be beneficial during longtime use with respect to side effects on the cardiovascular system and control of the menstrual cycle.

Contraceptives, Oral, Combined↗
PubMed1998

Cerebral thrombosis and oral contraceptives. A case-control study.

To assess the influence of oral contraceptives (OC) on the risk of cerebral thrombosis and transient cerebral ischemic attacks, a 5-year case-control study including all Danish hospitals was conducted. All women 15-44 years old who suffered a cerebral thromboembolic attack (CTA) during the period 1994-95 and 1200 age matched control subjects were included. Of 309 patients and 1200 control subjects questionnaires sent out, 271 patients (87.7%) and 1074 control subjects (89.5%) responded and agreed to participate. After exclusion of women with nonvalid diagnoses, previous thromboembolic diseases, or current pregnancy, 219 patients and 1041 control subjects were available for analysis. After confounder control and with nonusers as reference, current users of first generation OC (50 micrograms of ethinyl estradiol [EE] or estrans) had an odds ratio (OR) of CTA of 1.86 (95% confidence interval [CI] 0.88-3.92); users of second generation OC (levonorgestrel or norgestimate) had an OR of 2.37 (1.35-4.16); and users of third generation OC (desogestrel or gestodene) had an OR of 1.32 (0.78-2.22). Users of OC with 50, 30-40, or 20 micrograms EE had OR of 2.65 (1.11-6.34), 1.60 (1.05-2.43), and 1.59 (0.57-4.58), respectively. Odds ratios for specific progestin types were as follows: estrans 1.37 (0.60-3.13), levonorgestrel 2.43 (1.40-4.21), norgestimate 7.09 (1.87-26.8), desogestrel 1.62 (0.72-3.63), and gestodene 1.24 (0.67-2.30). Duration of use was without significant influence on the risk and the OR were constant across the age bands. Compared with women who had never used OC, former users had an OR of CTA of 0.95 (0.66-1.51). In conclusion, use of OC with 50 micrograms of EE and OC with second generation progestins increased the risk of CTA significantly. OC with third generation progestins did not have any significant influence on the risk of CTA. The risk of CTA among former users of OC was not increased.

Adolescent↗
PubMed2002

Pharmacokinetic overview of Ortho Evra/Evra.

OBJECTIVE: The pharmacokinetics of norelgestromin, the primary active metabolite of norgestimate, plus ethinyl estradiol (EE), delivered by the once-weekly contraceptive patch (Ortho Evra/Evra), have been studied in eight trials. This overview summarizes the relevant pharmacokinetic data for the contraceptive patch. DESIGN: Review article. RESULT(S): The amount of norelgestromin and EE absorbed from the patch is proportional to patch size: the 20-cm(2) patch (Ortho Evra) delivers norelgestromin, 150 microg/d, and EE, 20 microg/d, to the systemic circulation. After single and multiple applications of the contraceptive patch, daily serum concentrations (area under the serum concentration-versus-time curve) of norelgestromin and EE were within the ranges generally seen with oral norgestimate, 250 microg/EE 35 microg (Ortho-Cyclen/Cilest), but without the peaks and troughs characteristic of oral dosing. Moreover, the contraceptive patch maintains serum concentrations of norelgestromin and EE within these ranges for up to 10 days, suggesting that clinical efficacy would be maintained even if a scheduled change is missed for as long as two full days. Regardless of the location of patch application (abdomen, buttock, upper outer arm, or torso [excluding breasts]) and even under conditions of heat, humidity, exercise, and cool-water immersion, efficacious concentrations of norelgestromin and EE are achieved. Coadministration of the patch with tetracycline did not affect the pharmacokinetics of norelgestromin and EE. CONCLUSION(S): The contraceptive patch exhibits an excellent pharmacokinetic profile, maintaining efficacious serum hormone concentrations under varying conditions.

Administration, Cutaneous↗
PubMed2004

Clinical profile of contraceptive progestins.

The term progestogen has been widely utilized to indicate the general class of agents that includes both progesterone and its synthetic analogs, whereas the term progestin refers only to synthetic progestational steroids. The development of progestins has been influenced in a major way by the search for orally active hormonal contraceptives, since it is likely that hormonal contraceptives will continue to utilize a progestin, the only possible alternative being represented by the utilization of antiprogestins. Synthetic progestogens in clinical use today belong to three main chemical families: progesterone derivatives (progesterone, retro-progesterone, 19-norprogesterone and 17alpha-hydroxyprogesterone); gonane and 19-nortestosterone derivatives (norethisterone, levonorgestrel, desogestrel, gestodene, norgestimate); a spironolactone derivative. Biological potency of progestogens varies depending on the end-point measured, usually ovulation inhibition and endometrial transformation; with both these tests, the most active compounds are all gonane derivatives, with a potency over a 100 times that of the natural hormone. When administered in adequate doses, a progestin inhibits fertility by inhibiting ovulation. This action is mainly exerted at the hypothalamic level where, physiologically, progesterone decreases the number of LH pulses. When progestogens are delivered directly to the uterine cavity, their action seems to be purely local. It has been amply proven that--even when administered in doses that do not constantly inhibit ovulation--a progestin can still remain effective as a contraceptive by acting at the level of the cervical mucus and, at least in part, of the endometrium. Progestogens utilized today differ largely in their pharmacokinetics. In general, after intake, these compounds are rapidly absorbed and distributed so that peak serum concentrations are reached between 1 and 4 h. Third-generation progestins (desogestrel, gestodene, norgestimate) have common characteristics: a higher affinity for progesterone receptors than their predecessors, a lower affinity for androgen receptors, a higher selectivity of action, a higher central inhibitory activity, a higher potency at the level of the endometrium, and an overall metabolic neutrality, in terms of effects on lipid and carbohydrate metabolism. In general, progestins can induce two types of adverse effects: changes in lipid metabolism and bleeding irregularities. Whereas the newer compounds seem to have overcome the first of these adverse effects, the second remains untouched: to this day, proper cycle control can only be achieved with combined hormonal contraceptives.

Contraceptive Agents↗
PubMed2002

Insulin sensitivity in non-obese women with polycystic ovary syndrome during treatment with oral contraceptives containing low-androgenic progestin.

BACKGROUND: Combined oral contraceptives (COC) effectively suppress hyperandrogenism in women with polycystic ovary syndrome (PCOS), though deterioration of insulin sensitivity during treatment is assumed. The study aim was to investigate insulin action and androgen production during treatment with COC containing low-androgenic progestin. METHODS: A total of 13 PCOS women and nine controls was enrolled into the study. Only non-obese women with a body mass index (BMI) <or=30 kg/m(2) were included. Hyperinsulinaemic euglycaemic clamp techniques were performed before and after 6 months of treatment with a monophasic COC containing norgestimate. RESULTS: Anthropometric parameters [BMI, waist:hip ratio (WHR)] remained unaltered during the study in both groups. No deterioration in glucose disposal rate (M), insulin sensitivity index (ISI) or metabolic clearance rate of glucose (MCRG) was observed during treatment in PCOS subjects. Fasting glucose decreased significantly (P < 0.01), but fasting insulin remained unchanged. Significant decreases in concentrations of testosterone (P < 0.001), androstenedione (P < 0.01) and dihydroepiandrosterone (DHEA) (P < 0.001), a decrease in the free androgen index, and an increase in concentrations of sex hormone-binding globulin were found in PCOS subjects. CONCLUSIONS: The norgestimate-containing COC significantly decreased androgen production and concentrations of free androgens, without reducing insulin sensitivity in non-obese PCOS subjects.

Adult↗
PubMed1995

Classification and comparison of oral contraceptives containing new generation progestogens.

New generation-oral contraceptives containing desogestrel or gestodene, and possibly also norgestimate, are more or less similar with respect to contraceptive efficacy, cycle control and acceptability. They also show a more favourable metabolic profile in comparison with older preparations. The desogestrel-containing preparations Gracial and Marvelon, and possibly also the gestodene-containing preparation Gynera, have demonstrated a good efficacy in well-controlled studies in the treatment of mild to moderate acne and/or hirsutism. There may be differences between new generation oral contraceptives with respect to their effects on metabolic variables like high-density lipoprotein cholesterol and sex hormone-binding globulin. These differences are most probably modulated by variations in both the pharmacokinetics and selectivity of the progestogenic components. Of particular relevance here may be the recent finding that approximately 20% of administered norgestimate is metabolized into levonorgestrel. For use in clinical practice, it is of considerable help to have different preparations containing a range of oestrogen doses with the same progestogen. They allow the clinician to 'tailor make' the choice of oral contraceptives for those starting pill use or those switching to another combination due to symptomatology or changed circumstances, e.g. advancing age, smoking, etc. In this respect, desogestrel-containing oral contraceptives allow the most flexible approach.

Androgens↗