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Biomedical subjects

G Klinger

Publications and source records attributed to G Klinger.

At least 19 recordsLinked to original sources

Pharmacokinetics of ethinylestradiol and levonorgestrel after administration of two oral contraceptive preparations.

Serum concentration profiles and pharmacokinetic parameters (cmax, tmax, AUC24, AUC0-00, MRT) of ethinylestradiol (EE2) and levonorgestrel (LNG) were obtained following administration of two combined oral contraceptives. The constituents of the preparations were as follows: Gravistat (0.05 mg EE2, 0.125 mg LNG); Minisiston (0.03 mg EE2, 0.125 mg LNG). In 20 of the volunteers blood samples were taken before and up to 36 hours following the intake of a single table. In 11 women the investigation was carried out at day 21 of a treatment cycle (steady-state condition). In spite of pronounced interindividual variations of the pharmacokinetic data, a clear dependency of EE2 concentration curves on the estrogen dose of the respective preparation could be demonstrated. Under the condition of steady-state (21st day of administration) there was a slight but significant rise of the EE2 peak serum concentrations and a pronounced increase of the LNG levels, closely reflected by elevation of the AUC values. SHBG serum concentration was significantly increased by the 10th day of treatment in all subjects receiving Gravistat, whereas the mean value in the Minisiston-group did not remarkably change. Although LNG is known to be bound to SHBG with high affinity, the missing parallelism between LNG- and SHBG-concentrations suggests other (additional?) mechanisms for the elevated LNG-binding capacity in women taking combined EE2-LNG preparations.

Administration, Oral

In vitro phagocytosis by crevicular phagocytes in various forms of periodontitis.

Phagocytes from the gingival crevice fluid (CF-cells) of 11 patients with localized juvenile and post-juvenile periodontitis (LJP/PJP), 14 with rapidly progressive periodontitis (RPP), 11 with adult periodontitis (AP), and 14 controls without periodontal disease were examined. Phagocytic activity in vitro was assessed. Crevicular washings were obtained from healthy sites of controls and diseased sites of patients after completion of the oral hygiene phase (professional and home care). The cells were carefully processed to avoid mechanical damage. The in vitro phagocytosis by uptake of opsonized C. albicans was performed in a moist chamber (30 minutes, 37 degrees C) and examined by light microscopy. CF-cells were differentiated on the basis of their morphological appearance. The majority of cells in crevicular washings were PMNs, some macrophages, and few lymphocytes. Phagocytic activity in patients with LJP/PJP and RPP was significantly decreased in comparison with that from AP and the control group. The decreased percentage of cells phagocytosing opsonized C. albicans was associated with the enhanced adherence of opsonized C. albicans. Moreover cell viability of CF-cells from LJP/PJP sites was significantly reduced. The data from the present study suggest that the in vitro phagocytosis of crevicular phagocytes in juvenile and rapidly progressive periodontitis lesions is diminished.

Adolescent

[Periodontology in Jena--25 years of teaching, research and therapy].

Periodontology is a young department and has developed in Jena in the last 25 years; since 1982 it is a part in state examination. Maintenance of teeth is possible until old age and requires periodontology as a part of therapy. Biochemically, microbiologically and immunologically methods make it possible to differentiate unlike forms of periodontitis and their special therapy.

Germany, East

Hormone analytical and carrier protein alternations following administration of mifepristone (RU 486) for termination of early pregnancy.

Outpatient terminations were performed on 50 biochemically confirmed pregnancies of 33 to 43 days amenorrhea with a single oral dose of 600 mg of mifepristone (RU 486). 37 women were randomly assigned to an additional endocrine investigation, comprising serum levels of beta hCG, progesterone (P), estradiol (E2), cortisol (C), sexual hormone binding globulin (SHBG), and cortisol binding globulin (CBG) on days 0 and 7 prior to and following the drug administration. Of these 37 patients, 30 experienced a complete expulsion of the uterine contents, 28 until day 7, 2 subjects on day 9 and 10, respectively. The remaining 7 women either showed an unaffected pregnancy or the symptoms of incomplete abortion, which made a surgical intervention necessary. In the successfully treated cases the levels of beta hCG, P and E2 decreased significantly, the nonresponders showed unchanged or even increasing hormone values. No significant changes of cortisol concentrations were found in the group of nonresponders, while the successful cases exhibited a slight elevation probably due to the abortion-associated processes. No considerable therapy-dependent differences were observed in the levels of SHBG. A small but significant decrease in the mean CBG value could be calculated in the group of responders.

Abortion, Spontaneous

[The effect of physical training on the pharmacokinetics of steroidal contraceptives].

In 8 female sports students (runners) aged 20 and 21 years and 10 women between 20 and 40 years of age, who regularly underwent body building training, serum levels of ethinylestradiol (EE2) and levonorgestrel (LNG) have been determined under conditions of exercise as well as in rest, prior to and following the intake of 1 tablet of Gravistat (0.05 mg EE2, 0.125 mg LNG). Blood samples were obtained at points 0, 2, 6 and 24 hours. Exercise (5000 meter running and intensive body building training of one hour duration, respectively) was started immediately after intake of the steroid combination. There were no significant differences in the serum concentration levels obtained during exercise and rest. But exercise consistently resulted in a slight decrease of EE2 and LNG serum concentrations and the area under curve values.

Adult

[Pharmacokinetics of contraceptive steroids with reference to long-term administration].

Pharmacokinetic investigations (c0h, c2h, c6h, c24h, AUC24) were carried out both in the first and last four days of a treatment cycle in patients of different ages, who used oral contraceptives at least for 12 months. 57 women took the preparation Trisiston (three-step-formulation with the components 0.03 mg ethinylestradiol (EE2) + 0.05 mg levonorgestrel (LNG), 0.04 mg EE2 + 0.075 mg LNG, 0.03 mg EE2 + 0.125 mg LNG), 23 subjects used Gravistat (0.05 mg EE2 + 0.125 mg LNG) and 17 patients were under Certostat, a preparation still in clinical evaluation (0.05 mg EE2 + 2.0 mg Dienogest (DNG)). The levels of EE2, LNG and DNG were measured by means of radioimmunoassays. Between the concentrations obtained after administration of a first and single tablet (earlier investigations) and those determined in long-time users during the first 4 days following the tablet-free interval no qualitative and quantitative differences were observed. Between the levels of EE2 and LNG determined in the first and last days of the treatment cycle, marked differences were found in patients under the formulations Trisiston and Gravistat, but not in those taking Certostat. It is concluded that a cyclic and reversible cumulating effect emerges under the influence of LNG-containing contraceptives, the mechanism of which cannot be explained solely by the increase of carrier protein capacity. It seems possibly due to an alteration of steroid metabolism resulting from the interaction between both components.

Adolescent

[Effect of levonorgestrel and ethinyl estradiol and their combination on biotransformation reactions].

Caffeine is mainly metabolized by 3-methylcholanthreneinducible cytochrome P-450, whereas metamizol (Analgin) is probably mainly metabolized by the phenobarbital inducible cytochrome P-450 family. Therefore the elimination of caffeine from serum and the elimination of the main metabolites of metamizol in urine reflect the activity of these two cytochrome P-450 families. Sex hormones can influence the activity of cytochrome P-450. Intake of levonorgestrel (0.125 mg) daily for 14 days reduced the metabolism of caffeine slightly, but the elimination of metamizol-metabolites is not influenced. Longterm administration of levonorgestrel (0.250 mg daily) for three months did not change the metabolisms of both model substances tested. In contrast, ethynylestradiol (0.050 mg) alone and also the combination with levonorgestrel markedly retarded the elimination rate of caffeine and metamizol-metabolites. This fact should be taken into consideration in drug therapy.

Adult

[Management of patients with rapidly progressive periodontitis].

At present diagnosis and therapy of rapidly progressive periodontitis is still difficult in the daily practice. It is possible to define this form of periodontitis by suitable clinical and paraclinical characteristics. In searching a practical therapeutic concept, including effective motivation, first results of a sufficient therapy confirm the possibility of a successful strategy in the treatment of patients with rapidly progressive peridontitis.

Adult

[Inter- and intra-individual variability of pharmacokinetic parameters for contraceptive steroids].

Serum levels of ethinylestradiol (E2) and levonorgestrel (LNG) have been determined in 10 volunteers of similar age after administration of 1 tablet of the oral contraceptives Gravistat and Ediwal, respectively, each containing 0.05 mg E2 and 0.125 mg LNG, using a cross over design. The studies were carried out at intervals of 4 weeks, within the follicular phase of the menstrual cycle and under standardized conditions. Wide variations were observed between the women in the calculated pharmacokinetic parameters, while there was a relatively close correspondence between the intra-individually obtained values, except for one case.

Adult

[The action of Sequostat in comparison to Sequence Ovosiston on selected metabolic parameters].

The effects of two sequential oral contraceptive preparations, Sequostat (6 days ethinylestradiol 0.05 mg, 15 days ethinylestradiol 0.05 mg + norethisterone acetate 1.0 mg) and Sequence-Ovosiston (9 days mestranol 0.1 mg, 12 days mestranol 0.08 mg + chlormadinone acetate 2.0 mg) on triglycerides, total cholesterol, HDL- and LDL-Cholesterol, glucose tolerance, total plasma proteins, plasma protein fractions, plasma transaminases, gamma-glutamyl-transferase, alkaline phosphatase and antithrombin III were studied in two groups of 46 and 29 young women respectively. Investigations were performed prior to the hormonal intake and after treatment for 3, 6 and 12 months. In nearly all parameters studied significant but minimal changes could be demonstrated which in most cases showed a minor degree in the Sequostat-group, while Sequence-Ovosiston exerted a less effect on glucose tolerance. A significant increase of HDL-cholesterol and a reduction of LDL/HDL-cholesterol relation could be demonstrated at least in the first six months, resulting from the estrogen dominance of the contraceptives.

Adolescent

[Efficiency of long-term dental treatment].

250 patients in long-term treatment (about 12, 4 years) were examined concerning their oral symptoms (DMF/T, CPITN, GPM, Plaque-index, Sulcus-bleeding-index of Mühlemann and Son), number of teeth, number of extracted teeth and teeth with endodontic treatment during the treatment period. These patients were compared with 250 patients, who were not under regularly treatment. There are clear differences between both groups. It can be concluded that long-term treatment with exact fillung therapy, endodontic and periodontic treatment is able to maintain teeth until a high age of life.

Adult

[Effect of removal of calculus on periodontium by hand- and roto-pro-instruments].

It was the aim of this clinically longitudinal study to find out the consequence of the removal of calculus with hand- and roto-pro-instruments of the periodontium in 50 patients suffering from periodontal diseases. There are no clinically provable differences between the two methods of the removal of calculus. Both methods cause a statistically significant effect on the inflammatory factors of the periodontium.

Dental Calculus

[Effect of a new gestagen--dienogest--and its combination with ethinyl estradiol on the activity of biotransformation reactions].

Caffeine is mainly metabolized by 3-methyl-cholanthrene-inducible cytochrome P-450, whereas metamizol (Analgin) is probably mainly metabolized by phenobarbital inducible cytochromes P-450. Therefore the elimination of caffeine from serum and the amount of the main metabolites of metamizol excreted into urine reflect the activity of these two cytochrome P-450 families. Sex hormones can influence the activity of cytochrome P-450. Dienogest is a new gestagen, used for temporary contraception. We investigated the effect of this new sexual hormone alone and in combination with ethynylestradiol on the elimination of both testdrugs. In 10 healthy volunteers dienogest 2 mg daily for 14 days have no effect on the metabolism of model drugs whereas the combination with 0.05 mg ethynylestradiol has an influence on the elimination of caffeine and metamizol.

Adult

[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

[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