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At least 721 records · Page 40Linked to original sources
PubMed1983

Lorazepam and oxazepam kinetics in women on low-dose oral contraceptives.

Women on low-dose estrogen oral contraceptives (OC) and drug-free control women matched for age, weight, and cigarette smoking habits, received single 2-mg IV doses of lorazepam or single 30-mg oral doses of oxazepam, two benzodiazepines metabolized by glucuronide conjugation. Kinetics were determined from multiple plasma concentrations measured during 48 hr after dosing. Mean kinetic variables for lorazepam in control and OC groups (n = 15 in each group) were: volume of distribution (Vd), 1.33 and 1.45 l/kg; elimination t1/2, 13.1 and 12.2 hr; total clearance, 1.25 and 1.50 ml/min/kg; free fraction in plasma, 10.3% and 10.3% unbound. For oxazepam, kinetic variables in the two groups (n = 14 and 17) were: Vd, 1.05 and 1.19 l/kg; t1/2, 7.6 and 7.2 hr; total clearance, 1.60 and 2.03 ml/min/kg; free fraction, 4.6% and 4.9% unbound. None of these differences were significant. Thus, metabolic clearance by glucuronidation of lorazepam and oxazepam is not significantly affected by OC, in contrast with the highly significant reduction in clearance of the oxidized benzodiazepine diazepam.

Adult↗
PubMed1983

[Combined pericervical and intramuscular administration of prostaglandin for the termination of pregnancy in the 2d and 3d trimester].

In 64 patients with pathological pregnancies (missed abortion, molar pregnancy, intrauterine fetal death, fetal malformation, maternal disease) termination of pregnancy was induced by local application of PGE2 by means of a portio cap and subsequent intramuscular application of Sulproston. In 21 women 1,5 mg and in 43 2,25 mg PGE2 or more were used for cervical priming. In 21 cases expulsion of the fetus could be obtained during or shortly after the priming procedure. In the remaining 43 women Sulproston was administered on the following day with a starting dose of 200 mcg and 100 mcg subsequently at two hours intervals up to a total dose of 500 mcg. With the exception of 3 cases this led to the expulsion of the products of conception. In the remaining 3 patients abortion was obtained on the third day by additional Sulproston-application. The mean expulsion time was 6,3 +/- 2,1 hours, being significantly lower when the fetus was not alive compared to viable pregnancies. Side effects during the priming procedure were only observed in 3 cases; the total rate of side effects was 57,8% and the incidence of use of analgetics 51,5%. The softening effect of locally applied prostaglandins apparently adds in an advantageous manner to the strong contractile effects of Sulproston resulting in shorter expulsion intervals, lower total dosage of prostaglandins and a reduction of the incidence of side effects and the use of analgetics.

Abortion, Induced↗
PubMed1983

Poly(DL-lactide-co-glycolide)/norethisterone microcapsules: an injectable biodegradable contraceptive.

Microcapsules made from a biocompatible, biodegradable polymeric excipient, poly(DL-lactide-co-glycolide) (DL-PLGA) that contained 22 weight percent (wt %) norethisterone (NET), were prepared by a solvent-evaporation microencapsulation process. The effects of changing both the lactide-to-glycolide ratio of the DL-PLGA and the size of the microcapsules on the rate of NET release and the rate of excipient biodegradation were determined in vivo. NET release rates were determined in baboons after injecting the microcapsule formulations intramuscularly. Serum samples obtained at various times following treatment were analyzed for NET, progesterone, and estrogen by radioimmunoassay (RIA). Biodegradation kinetics were determined by injecting NET microcapsules made from radiolabeled DL-PLGA intramuscularly into the hind legs of rats. Residual radioactivity at the injection site was determined at various times after treatment by combustion analysis of the muscle tissue. Changing the ratio of the comonomers to include more glycolide (DL-lactide:glycolide-96:4, 92:8, 87:13, 74:26) increased the rate of NET release and accelerated the biodegradation of the copolymer excipient. Decreasing the size of the microcapsules increased the rate of NET release. On the basis of these studies a NET microcapsule formulation has been identified for clinical testing which releases NET for 3 months and biodegrades completely within 6 months.

Animals↗
PubMed1985

Effects of oral contraceptives on blood coagulation. A review.

A review of the data from studies of oral contraceptives on coagulation and the fibrinolytic enzyme systems reveal an increase of a variety of coagulation factors. This is dose dependent and related to estrogens and appreciable above a dose of 0.5 micrograms of ethynylestradiol. Smaller amounts are less effective or not at all active. The mechanism of this increase is unknown. The pathophysiological significance is not yet clear. There is no available data that associate the increase of coagulation factors with disseminated intravascular coagulation. Conclusive evidence that low dose progesterone has any effect on the coagulation system is lacking.

Blood Coagulation↗
PubMed1988

Endometrial response to the use of a sequential oral contraceptive.

Belgium is 1 of the few countries where sequential oral contraceptives are still commercially available. The authors investigated the endometrial effect of Ortho-Novum SQ (14 tablets of 100 mcg mestranol and 7 tablets of 100 mcg mestranol + 2 mg norethisterone) in 222 biopsy specimens obtained from 184 asymptomatic Caucasian women (mean +or- s.d, age and parity, 34.6 +or- 6.7 and 2.0 +or- 1.0, respectively) who had used this sequential OC during an average of 52.5 months. Notwithstanding predominantly longterm use of Ortho-Novum SQ, 43% of the tissue samples had normal proliferative or luteal endometrium. The data suggest a positive correlation between the endometrial response and the duration of pill use. No premalignant or malignant changes were found. In 15 of 24 subjects for whom multiple biopsy specimens were available, the histological picture was static; 7 showed regression and only in 2 were the changes progressive, although never more severe than minor 'class 2' lesions. These results, which are at variance with those reported for users of other sequential brands (mainly Oracon), suggest that prolonged use of Ortho-Novum SQ does not enhance the risk of endometrial cancer in premenopausal women having no additional risk factors for the development of this type of neoplasia.

Anatomy↗
PubMed1983

Two years' experience with two levonorgestrel-releasing intrauterine devices and one copper-releasing intrauterine device: a randomized comparative performance study.

A randomized comparative performance study of two levonorgestrel intrauterine devices (IUDs) and a copper (Nova-T) IUD (Leiras, Turku, Finland) was performed at two clinics in Finland and one in Brazil. The 24-month cumulative event rates per 100 women are reported. Six thousand woman-months of use were recorded with the levonorgestrel IUD and 3000 with the Nova-T device. Pregnancy rates at 2 years of use were 0.6 and 0 with the two levonorgestrel IUDs and 3.3 with the Nova-T IUD. Removal rates because of bleeding and/or pain were low with all three IUDs: 7.5, 7.6, and 7.1, respectively, at 24 months. Recordings of the number of days of bleeding showed significantly fewer days of bleeding during use of the levonorgestrel IUDs than the Nova-T IUD from the second month of use onward, until the end of the second year. No infections were recorded in association with use of the levonorgestrel IUDs, and only one termination because of infection was recorded for the Nova-T IUD. The continuation rates of use at 24 months were 66.6, 60.7, and 71.9 for the two levonorgestrel IUDs and the Nova-T IUD, respectively; the differences were not statistically significant.

Adolescent↗
PubMed1983

A new ultra-low-dose combination oral contraceptive.

Data were compiled from 17 U.S. sites during a study of levonorgestrel, 0.15 mg, and ethinyl estradiol, 0.03 mg. A total of 1,130 women participated in 11,604 cycles of treatment. Efficacy, cycle characteristics, bleeding irregularities and side effects were studied. Weight and blood pressure means were analyzed with the paired t-test. Subject acceptance of this new combination oral contraceptive was high.

Adolescent↗
PubMed1984

The use of biodegradable norethisterone implants as a 6-month contraceptive system.

The effects of a 6-month contraceptive system of biodegradable norethisterone (NET) implants on the menstrual cycle, estradiol and progesterone levels, the presence of side effects, its contraceptive effectiveness, and the NET levels achieved were studied in a group of nine women. There was practically no disruption of the menstrual cycle and no important side effects. Ovulation was inhibited in four subjects, and another four subjects remained ovulatory. In all the subjects a cyclic secretion of estradiol was maintained. No pregnancies occurred. The circulatory levels of NET were very stable throughout the 6-month period of implant use.

Adult↗
PubMed1985

Lipid metabolic studies in women with a polycystic ovary syndrome during treatment with a low-dose desogestrel-ethinylestradiol combination.

Twenty women with the polycystic ovary syndrome (PCO) were treated with a combination of desogestrel and ethinylestradiol (EE) and the effects on lipids and lipoproteins were compared with those induced in a group of 13 regularly menstruating, healthy women. All women were examined before and after 3 months of treatment. Compared with the regularly menstruating women, the PCO women had significantly higher body weights and blood pressure as well as elevated levels of triglycerides in serum and VLDL. During treatment, 14 out of 20 women affected by PCO lost weight. No significant change in blood pressure was observed. In the PCO group, moderate increments were encountered in serum cholesterol, phospholipids and triglycerides. No significant changes were seen in LDL-cholesterol or HDL-cholesterol. The ratio LDL-cholesterol/HDL-cholesterol did not alter. The level of total cholesterol in VLDL rose during treatment. These changes in serum and lipoprotein lipids in PCO patients were of the same type and magnitude as those found in the control group, apart from an increase in HDL-cholesterol in the latter. The only remaining difference after treatment was a slightly higher level of VLDL triglycerides in the PCO women. Thus only moderate changes were induced in lipid and lipoprotein patterns by the combination of desogestrel and EE. A "positive" influence on lipids and lipoproteins cannot be considered as a further advantage, added to the list of indications when hormonal treatment is used in PCO-affected women. The clinical implications of elevated triglycerides remain to be clarified.

Adult↗
PubMed1980

The use of medroxyprogesterone acetate for relief of climacteric symptoms.

Climacteric symptoms in the menopausal woman are perplexing to the physician. Recent literature concerning the relationship of estrogen to carcinogenesis has caused many women to discontinue this medication; thus, there is a need for an alternative therapy for the relief of these symptoms. The drug medroxyprogesterone acetate (Depo-Provera) was assessed in a double-blind, randomized, placebo-controlled study involving 48 subjects. Only one of the placebo-treated patients claimed any relief from climacteric symptoms while only two of the patients who received the study drug noted little or no relief (P < 0.0001). Relief from climacteric symptoms began at 4 to 7 days after entry into the study and extended for 8 to 20 weeks. The only side effects were withdrawal bleeding and a slight, transient weight gain. Depo-Provera appears to be a reliable substitute for estrogen in the treatment of climacteric symptoms. Further investigations with this medication seem indicated.

Adult↗
PubMed1984

Return of ovulation following a single injection of depo-medroxyprogesterone acetate: a pharmacokinetic and pharmacodynamic study.

The effect of a single dose of 150 mg of depo-medroxyprogesterone acetate (DMPA) on pituitary, ovarian and endometrial function was assessed in relation to the peripheral levels of the compound in 8 women. The levels of medroxyprogesterone acetate (MPA), follitropin (FSH), lutropin (LH), prolactin, estradiol (E2) and progesterone ( Prog .) were measured 3 times a week during a pretreatment (control) cycle and then daily during postinjection weeks 14-17, 22-25 and 30-33. An endometrial biopsy specimen was obtained during postinjection weeks 17, 25 and 33. In three out of 8 subjects the daily hormone assays carried out during postinjection weeks 30-33 indicated anovulatory periods; in these subjects peripheral blood was drawn daily during postinjection weeks 46-49 and a fourth endometrial biopsy was taken during week 49.

Adult↗
PubMed1986

The effect of the contraceptive pill on blood pressure: a randomized controlled trial of three progestogen-oestrogen combinations in Szeged, Hungary.

As part of an international multicentered investigation a double-blind comparative clinical trial was conducted at the Department of Obstetrics and Gynecology, University Medical School, Szeged, Hungary, in order to study the effect of different combined oral contraceptives on blood pressure. Healthy, normotensive women were randomly allocated to either of the following oral contraceptives: 250 micrograms levonorgestrel + 50 micrograms ethinyloestradiol (LN 250 + EE 50), 250 micrograms levonorgestrel + 30 micrograms ethinyloestradiol (LN 250 + EE 30), 1 mg norethisterone acetate + 50 micrograms ethinyloestradiol (NA 1 + EE 50). Standardized blood pressure measurements were carried out at admission and 3, 6, 9, and 12 months after admission. Blood pressure change from admission to subsequent visits was analysed in subjects who were seen by the same observer both at admission and the follow-up under consideration. The systolic blood pressure slightly but not significantly increased in groups LN 250 + EE 50 and NA 1 + EE 50, whereas the diastolic pressure showed a minimal decrease. In group LN 250 + EE 30 both systolic and diastolic blood pressure increased significantly (+5.58 and +3.20 mm Hg, respectively) at the 12-month follow-up. The study supports previous findings that combined oral contraceptive use is associated with a moderate rise in blood pressure. The progestogen-to-oestrogen ratio in the pill may be as important in this context as the dose of either component itself.

Adolescent↗