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Biomedical subjects

G Klinger

Publications and source records attributed to G Klinger.

At least 73 records · Page 4Linked to original sources
PubMed1990

[Pharmacokinetics of ethinyl estradiol following the administration of combination contraceptive preparations].

A radioimmunoassay for ethinylestradiol (EE2) which was developed in the pharmacological department of VEB Jenapharm has been modified and fully validated. It was the purpose of the present study to extend the still limited data concerning EE2-serum levels after a single and repeated ingestion of combination pills with different doses of EE2. 10 volunteers aged 17-25 years with normal body weight and length received a single tablet of either Gravistat (0.05 mg ethinylestradiol + 0.125 mg levonorgestrel) or Minisiston (0.03 mg ethinylestradiol + 0.125 mg levonorgestrel). 11 other women were involved into the study after ingestion of the 21st tablet of a contraceptive cycle. Peak serum levels which were significantly higher in the Gravistat- than in the Minisiston-group were observed 90 to 120 minutes after the oral administration. Detectable EE2 levels were determined in all volunteers after 24 hours. Pharmacokinetic data showed pronounced interindividual variations. Whereas the mean 24 hours levels of EE2 increased progressively during the treatment cycles, kinetic values obtained at the end of the cycle exhibited a significantly higher level than those after ingestion of a single dose. Area under curve (AUC) was calculated by the trapezoidal rule with the aid of a compartment free model.

Adolescent↗
PubMed1990

[Determination of lithium in serum and saliva of patients with manic-depressive disorder].

The slight therapeutic breadth involved means that manic depressive lithium prophylaxis may call for life-long routine management. The lithium/serum-level checks required hitherto are here compared with a non-invasive method, that of determining the lithium level from a mixture of the patient's saliva, a method involving no danger that will eventually assume considerable importance.

Adult↗
PubMed1989

[Experiences with the antigestagen mifepristone (RU 486) in the interruption of early pregnancy].

50 healthy women (mean age 29.9 +/- 6.4 years) with early unwanted pregnancy (mean duration 39.3 +/- 2.9 days post menstruationem) received a single oral dose of 600 mg of Mifepristone. Uterine bleedings occurred in all patients within 8 to 110 hours (43 +/- 23.3 hours) after the application, but its duration was very different and correlated with the results of treatment. 39 patients reported on an amount of bleeding exceeding by far the menstrual strength. But in most cases this heavy bleeding lasted only 1-3 days. Frequency of complete abortion was 80% (40 women). 4 patients had an incomplete abortion, and in 6 women the pregnancy was unaffected by the treatment. "Medical abortion" provides a novel alternative to the surgical procedure and is fairly accepted by the patients. Its efficacy, however, should be improved by focusing on early pregnancies not exceeding 10 days after the expected menstrual period and, perhaps, the additional usage of low doses of prostaglandin E derivatives.

Abortion, Induced↗
PubMed1988

[Prolactin stimulation using the metoclopramide test in females taking oral contraceptives].

In 31 patients taking oral contraceptives (o.c.) for a period between 1 year to more than 3 years, basal serum prolactin levels and metoclopramide induced prolactin values were determined 30 and 60 minutes following an i.v. injection of 10 mg of metoclopramide. The basal prolactin levels were elevated in 7 women to more than 1,000 mU l. The 3 groups of patients taking o.c. with different estrogen doses showed higher drug induced increase of their prolactin levels than the controls. These differences were statistically significant between groups I and III and the control group. No differences could be found between the challenged values of the users groups. The prolactin increase challenged with 200 micrograms TRH in 5 women under o.c. was considerably smaller than that observed in the metoclopramide groups, but exceeded the TRH induced levels found in the controls. The significance of these findings is discussed with special reference to the promotion of prolactinomas.

Adult↗
PubMed1988

[Metamizol-caffeine elimination in females with increased serum aminotransferase activities treated with steroidal oral contraceptives].

The elimination of caffeine from the plasma and the excretion of the major metabolites of metamizol (AnalginR) in the urine was studied in 25 women on long-term oral steroid contraceptives. Both tests allowed to draw conclusions about metabolic liver function. A steroid-induced delay of the elimination of caffeine in clinically healthy women with/without serologic elevation of aminotransferase activities was demonstrated. --We regard this as the consequence of an inhibition of the cytochrome P-450-dependent poly-functional oxidases of the P-450MC type, which was produced by oral contraceptives. The differences in the elimination of metamizol were not significant.

Adult↗
PubMed1987

[Elimination of caffeine and metamizole in the menstrual cycle of the fertile female].

The elimination of caffeine from serum and that of the main metabolites of metamizol in serum were investigated in 9 healthy women on days 1, 8, 14 and 21 of the menstrual cycle. In the luteal phase, when the progesterone level is highest and the estradiol concentration is high as well, the elimination of caffeine is about 25% longer than in the follicular phase. In contrast to caffeine, the metabolism of metamizol is slightly accelerated if the endogenous hormone level is high. The present results suggest that endogenous hormones have different effects on biotransformation activities. These results are without practical consequences yet.

Adult↗
PubMed1986

[Radioimmunologic determination of the progestagen dienogest in plasma and saliva].

Following oral administration of 2 mg of dienogest (17 alpha-cyanomethyl-17 beta-hydroxy-4,9-estradien-3-one) to female volunteers, the dienogest concentration courses in plasma and saliva were determined by means of a specific radioimmunoassay (RIA). Three different procedures of the plasma sample preparation prior to the RIA were compared. The dienogest RIA was directly applied to saliva. There is a high correlation between the dienogest concentrations in plasma and saliva. The dienogest plasma elimination half life of about 9 hrs is not significantly different from that derived from saliva. The salivary dienogest concentrations indicate a relatively high non-protein bound portion of this steroid drug in plasma. Following repeated oral administration of dienogest (tau = 24 hrs), there is no significant cumulation of plasma dienogest.

Administration, Oral↗
PubMed1984

[Testing of the steroid-related suppressive effect on the hypothalamo-hypophyseal system using twofold stimulation].

Intravenous administration of gonadotropin-releasing hormone (GnRH) induces not only a rapid release of pituitary LH and FSH stored, but also stimulates biosynthesis of these hormones by a long acting process. Repeated injection of GnRH after an interval of 90 to 120 minutes evokes an increased response compared with the first period of stimulation. This pattern of reaction is principally maintained on therapy with steroidal contraceptives. The twofold stimulation provides additional information on hypothalamic-pituitary reactivity exceeding the results yielded by the simple GnRH stimulation test. On the contrary examination of prolactin response to twofold TRH-administration gives no increased diagnostic aid.

Contraceptives, Oral, Combined↗
PubMed1983

Studies on pharmacokinetics of STS 557 in animal species and man.

Following oral and i.v. administration of [14 alpha, 15 alpha-3H]-STS 557 to beagle dogs, baboons, rats and female volunteers, plasma level courses of total radioactivity and STS 557, and radioactivity excretion in urine and feces have been investigated. Bioavailability of orally administered STS 557 was found to be 80--90% in man and beagle dog, 70--80% in baboon and rat. Concerning the systemic availability following oral administration of equivalent doses, the following order was established: beagle dog greater than man greater than baboon greater than rat. Equilibrium dialysis indicates species differences in plasma protein binding and a considerable part of STS 557 to be present in plasma unbound. STS 557 is rather rapidly eliminated from the plasma compartment of all species investigated with half lives less than or equal to 10 h. As an additional time parameter of pharmacokinetics the "mean residence time" was used. Urinary excretion of STS 557 metabolites is dominant in all species, including the rat. In contrast to the great part of STS 557 in plasma total radioactivity, only small amounts of unchanged STS 557 are excreted in urine. First results of current studies in rabbits are presented, too.

Animals↗
PubMed1983

Long term toxicological studies on the progestin STS 557.

The toxicity of 17 alpha-cyanomethyl-17 beta-hydroxy-estra-4, 9-dien-3-one (STS 557) was studied by its oral administration of 0.1, 1.0 or 10.0 mg/kg/day to Wistar rats for six months, and of 0.01, 0.1 or 1.0 mg/kg/day to beagle dogs for six months, respectively. Levonorgestrel at a dose of 1.0 mg/kg/day was used as the standard in the dog study. With respect to the progestational activity of the compound the main target organs were the hypophysis, the reproductive organs and the adrenals. Mammary hyperplasia was observed in dogs treated with STS 557 or levonorgestrel at the dose of 1.0 mg/kg/day, but in no case mammary nodules could be detected. At the dose of 1.0 mg/kg/day STS 557 and levonorgestrel were found to increase the plasma insulin response to i.v. glucose in bitches, but neither the mean blood glucose levels nor the glucose utilization were affected. Moreover, during administration of both steroids to dogs temporary changes in serum concentrations of triglycerides and total cholesterol were noted. The results obtained in rats and dogs from functional and morphological investigations did not reveal any toxic side effects of STS 557 on the liver, the kidneys, the bone marrow or on blood coagulation. The effects on the reproductive organs observed following STS 557 especially in dogs are related to both the hormonal effects of the compound and the specific response of the dog to potent progestagens.

Animals↗