SHBG, testosterone, androstenedione, 17-OH-Progesterone plasma levels in PCO affected women treated with a triphasic oral contraceptive. [Clinico-laboratory research on the pharmacodynamic characteristics of Rigevidon] The effects of an oral contraceptive containing ethinyloestradiol and norgestrel on CYP3A activity. Rx drugs

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Acta Eur Fertil. 1987 Nov-Dec;18(6):375-80.
SHBG, testosterone, androstenedione, 17-OH-Progesterone plasma levels in PCO affected women treated with a triphasic oral contraceptive.

Negri P, Agnello G, Borghesani F, Tomain L, Minisci N, D'Errico G, Cavallini AR.

Istituto di Clinica Ostetrica e Ginecologica dell'Universita degli Studi di Ferrara.

A triphasic oral contraceptive Trigynon (Schering) or Triphasil (Wyeth) was administered to 13 anovulatory women with hyperandrogenism, enlarged polycystic ovaries and reversal of LH/FSH ratio. After three months of treatment total Testosterone, Androstenedione and 17-OH-Progesterone levels significantly decreased while SHBG significantly increased. Reduction of hair growth and improvement of acne were noted. Side effects were minimal.

PIP: A trial of a triphasic oral contraceptive in 13 women with polycystic- ovary syndrome is presented, backed up with data on levels of sex hormone binding globulin (SHBG), testosterone, androstenedione, 17-OH-progesterone and other hormones. This illness is really a hyperandrogenic response of the ovary secondary to high gonadotropin levels and unopposed estrogens with low SHBG. Only mediocre results have been reported with low-dose oral contraceptive treatment, compared to earlier high-dose pills. The pills used here contained 50 mcg levonorgestrel (LNG) with 30 mcg ethinyl estradiol (EE) for 6 days, 75 mcg LNG and 40 mcg EE for 5 days, and 125 mcg LNG with 30 mcg EE for 10 days. After 3 months of treatment LH levels fell from 29.7 to 3.6 mIU/m1; FSH fell from 12.3 to 2.6 mIU/m1, and the LH/FSH ratio decreased from 2.34 to 1.38. All androgens declined significantly (p0.01), into the normal range. Serum cortisol rose significantly from 16.9-36.7 mcg/100 ml. SHBG rose from 1.67-3.0 mcg/100 ml, the high limit of normal. Hirsutism and acne improved in all but 1 patient. 1 woman dropped out because of weight gain, and another because of nausea and headache. These results suggest that triphasic oral contraceptives may be safe and effective for chronic anovulatory syndrome.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3454501&dopt=Abstract

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Farmakol Toksikol. 1987 Jan-Feb;50(1):97-100.
[Clinico-laboratory research on the pharmacodynamic characteristics of Rigevidon]

[Article in Russian]

Korkhov VV, Nikanorova SA.

A contraceptive effect of Rigevidon depends on the drug influence on cyclic secretion of gonadotropic hormones. Rigevidon fails to exert a significant effect on prolactin secretion. The drug withdrawal results in a comparatively rapid restoration (within the first three months) of the generative function.

PIP: The effect of the new combined oral contraceptive agent Rigevidon on the hypothalamo-hypophyseal-ovarian system was studied in 50 women (age not specified). Rigevidon was given for 21 days with subsequent 7-day interval. Duration of administration was 10-12 cycles. Functional state of the ovaries and gonadotropic function of the pituitary gland was evaluated by measuring the blood levels of estradiol, progesterone, follicle-stimulating hormone (FSH) and luteinizing hormone (LH). During Rigevidon administration in doses producing the contraceptive effect, all women showed the monophasic type of basal temperature. FSH levels on days 7-9 and 20-23 of cycle 3, 6 and 10-12 did not differ significantly from those in controls; there was a 2.8 times decrease FSH levels on days 14-16 of cycle 3 and a 3.8 times decrease on days 14-16 of cycle 10-12. Marked decrease in LH levels was observed on days 14-16 of cycle (5 times) and during the 6th cycle (9.2 times). Significant decrease in estradiol levels was recorded on days 7-9 and 14-16 of cycle 3,6 and 10-12. Progesterone levels were decreased significantly on days 7-9 and 20-23 of cycle 3, 6 and 10-12; significant decrease in progesterone levels on days 14-16 was observed only during cycle 3. Prolonged administration of Rigevidon (10-12 cycles) produced no changes in prolactin secretion. After cessation of Rigevidon administration, the LH and estradiol levels were decreased only on days 14-16 of cycle 1. The test with LH releasing hormone (100 mc) on days 12-14 after Rigevidon cessation showed normal sensitivity of the pituitary gland to hypothalamic stimulation. The results of this study indicate that the contraceptive effect of Rigevidon is associated with inhibition of ovulation and cyclic secretion of FSH and LH.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3556564&dopt=Abstract

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Br J Clin Pharmacol. 2002 Jan;53(1):67-74.
The effects of an oral contraceptive containing ethinyloestradiol and norgestrel on CYP3A activity.

Belle DJ, Callaghan JT, Gorski JC, Maya JF, Mousa O, Wrighton SA, Hall SD.

Department of Drug Disposition, Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.

AIMS: To examine the effects of an oral contraceptive containing ethinyloestradiol and norgestrel on intestinal and hepatic CYP3A activity using midazolam as a probe substrate. METHODS: In a nonblinded sequential study, nine healthy women received simultaneous doses of intravenous midazolam (0.05 mg kg(-1)) and oral 15N3-midazolam (3 mg) on days 0, 4, 6, 8, and 14. On study day 5, Ovral(50 microg ethinyloestradiol/500 microg norgestrel) was administered for 10 days. Serum and urine samples were assayed for midazolam, 15N3-midazolam and metabolites by liquid chromatography-mass spectrometry. A Digit Symbol Substitution Test (DSST) was used to assess changes in the pharmacodynamic activity of midazolam. RESULTS: Moderate (% CV 26-46) interindividual variability in the pharmacokinetics of midazolam were observed. Compared with baseline, AUC(0,infinity)iv ratios (95% CIs) after 2, 4, and 10 days treatment with OC were 89% (79, 101), 96% (85, 109), and 88% (77, 99), respectively. The AUC(0,infinity)oral ratios (95% CIs) were 101% (82, 125), 105% (85, 130), and 114% (92, 141), respectively, after 2, 4, and 10 days OC treatment compared with baseline. Concomitant administration of the oral contraceptive, Ovral for 2, 4 or 10 days did not significantly alter the area under the curve, clearance, or half-life of midazolam after either oral or intravenous administration. No alterations in pharmacodynamic effects of midazolam were observed between treatment days. Mean DSST scores strongly correlated with mean total midazolam blood concentrations (r = -0.936). CONCLUSIONS: Administration of Ovral for 10 days had no impact on intestinal or hepatic CYP3A activity as determined by midazolam metabolism.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11849197&dopt=Abstract

word match triphasil online literature

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