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Biomedical subjects

H Hüller

Publications and source records attributed to H Hüller.

At least 37 records · Page 2Linked to original sources

[Blood level oriented ambulatory cyclosporin A therapy following kidney transplantation].

It is reported on the blood level-oriented oral long-term therapy with cyclosporin-A (Sandimmun) in 20 patients after kidney transplantation. The Cy-A-concentrations were measured in the whole blood by means of a radioimmunoassay (Sandoz) under steady state conditions. The mathematical analysis of the steady state daily minimum concentrations in the whole blood depending upon the dosage rate allows individual calculations of the dosage for the stabilisation of the therapeutic concentration desirable for the individual patient in each case. In the majority of the patients a non-linear relation between the steady state blood concentration and the dosage rate was present. The observation of a defined therapeutic area under the conditions of the ambulatory treatment could be achieved without any problems. The control intervals were 4-6 weeks. The long-term stability of the individual pharmacokinetic parameters can at present not be judged reliably, since the average observation time is still too short. In 6 patients who are controlled on the way demonstrated already for several months no systemic changes in the behaviour of the blood level were to be seen.

Cyclosporins↗

[Quantitative determination and kinetics of dihydralazine in hypertension patients].

For the quantitative determination of dihydralazine (1) a derivative with acetylacetone in biological material was formed at pH = 4.9, extracted with n-hexane, and measured gaschromatographically with N-P-FID. Acid labile 1 was hydrolyzed with HCl (1 mol/l) for 24 h. The detection limit was 25 nmol/l plasma. Kinetic studies were performed in 16 patients with essential hypertension under steady-state conditions after the oral application of 50 mg 1. The acetylator phenotype was determined with sulfamethazine. Complete dihydralazine plasma level-time courses were found in only 5 cases. The concentrations were below the detection limit in 4 patients for the whole period. Only single values could be registered in the remaining patients. Maximal plasma levels of the free (58-314 nmol/l) and acid labile 1 (147-367 nmol/l) were reached 20-40 min after the application. The elimination half life was 23-47 min for the free 1, 55-92 min for the acid labile 1. Less than 0.5% of the applied drug were excreted into the 24 h urine in its free form, about 0.4% as acid labile derivatives. No correlation could be found between the acetylator phenotype of the patients and the kinetic behaviour of the drug. Preliminary studies concerning the biliary excretion of 1 after i. m. application in two patients with T-drain showed an accumulation of the free compound with bile/plasma ratios up to 7.4.

Acetylation↗

[The pharmacokinetics of bendamustine (Cytostasane) in humans].

The pharmacokinetics of bendamustine (Cytostasane) was determined in plasma on seven patients after its intravenously and oral application, respectively. Cytostasane was given in a dosis of 4.2-5.5 mg . kg-1 as an intravenous infusion over 3 min and as gelatine capsules in a 7-d intervall. Its elimination from the plasma is fast, monoexponentially and two-phasic after intravenous application (t1/2 alpha = 9.6 min, t1/2 beta = 36.1 min). The AUC was 11.17 micrograms . ml-1 . h, the central distribution volume 11.15 l and the distribution volume in steady state 20.51 l. The mean total clearance was 528.9 ml . min-1. After oral application maximal plasma levels of Cytostasane were detectable before 1 h. The mean oral bioavailability was 0.57, ranged from 0.25 to 0.94. Cytostasane undergoes metabolism. Its hydrolysis in plasma is slow (t1/2 = 1.67 h). After Cytostasane the depression of leucocytes was mild.

Bendamustine Hydrochloride↗

Comparative bioavailability of two carbamazepine tablets.

The comparative bioavailability of two commercial carbamazepine tablets (Finlepsin and Tegretol) was investigated. In a single-dose study in eight healthy volunteers and in a multiple-dose study in five epileptic patients carbamazepine absorption from both drug products was shown to have the same extent and reliability. Despite a somewhat increased rate of absorption in Finlepsin, as regards the fit of the drug level in the therapeutic range under chronic treatment conditions, there was no difference between the two preparations. On the basis of these results we conclude that Finlepsin and Tegretol are bioequivalent drug products.

Adult↗

Drugs in pregnancy - a prospective study.

A prospective study starting with 1182 women in the early stage of pregnancy investigated prescribed drug therapy; self-medication; consumption of coffee, cigarettes, and alcohol; and a series of social and sociologic factors. The main results are as follows: compared with international reports, drug consumption during gravidity was low. During the first weeks of gravidity, 11% of the women took drugs. Drug consumption increased during gravidity, reaching a maximum of 26% of the pregnant women taking drugs. Drugs most frequently prescribed were antiemetics, analgesics, sedatives, iron preparations, and vitamins. Self-medication (1 or 2%) was extremely low; in most cases analgesics were used. Coffee consumption declined, particularly during the last trimester; consumption of cigarettes showed a distinct decrease from 27% to 12%.

Alcohol Drinking↗

Effect of theophylline on the riboflavin-sensitized photodegradation of bilirubin in vitro.

Under in vitro conditions, theophylline accelerates the rate of bilirubin photodestuction sensitized by riboflavin, but does not do so in absence of this dye. The effect depends on the concentrations of theophylline and/or riboflavin, on the bilirubin/albumin ratio, and seems to implicate bilirubin unbound to serum albumin. Possible causes of the theophylline action and clinical implication regarding thephototherapy of neonatal jaundice are discussed.

Bilirubin↗

Investigation of drugs in ambulant patients.

In contrast to the drug testing under clinical conditions, many other problems appear in regard to outpatients. These investigations were carried out on 49 outpatients with various degrees of angina pectoris under the conditions of an intraindividual comparison with d,l-oxyfedrine (Myofedrin), l-oxyfedrine (ildamen) or placebo for a period of 16 weeks and a daily dose of 48 mg applied orally altogether. The severity degrees of the angina pectoris were diminished after the chronic application of l- and d,l-oxyfedrine. There are no differences in the activity and side-effects.

Ambulatory Care↗

Pharmacokinetics and therapeutic efficacy of metronidazole at different dosages.

Metronidazole, a drug effective against certain protozoal and anaerobic infections, was given female patients with Trichomoniasis urogenitalis. Group I received twice daily 250 mg of metronidazole (supplied as 250 mg tablets Vagimid). Group II received in a single dose 1.0 g (4 tablets); and group III, 2.0 g (8 tablets). Serum and urine metronidazole levels were measured polarographically. Kinetic parameters were determined from the measured values of the concentration time curve by a computing program. An exact control of the therapeutic result was carried out. In all patients peak serum levels occurred within 1-3 hr and averaged 5.1 +/- 1.7 microgram/ml after 250 mg doses, 19.6 +/- 3.8 microgram/ml after 1.0 g doses and 40.6 +/- 9.3 microgram/ml after 2.0 g doses. About 35% of the administered dose was recovered in the urine in 12 hr and about 50% in 24 hr. Metronidazole shows protein binding of 10-20% equally in vivo and in vitro. Minimum trichomonacidic concentrations of nearly 1 microgram/ml were still present 12 hr after oral application of 250 mg metronidazole, and 24 hr to 36 hr, respectively after 1.0 g and 2.0 g daily doses. The cure rate was 100%. No serious side effects ocurred in any of the patients.

Adolescent↗

The estimation of drug plasma levels in epileptics.

The estimation of antiepileptic drugs in plasma is an indispensble resource in the handling of seizure patients in many countries. Using our results, simple methods for the estimation of antiepileptic drugs are discussed.

Anticonvulsants↗

Problems in the kinetic evaluation of capacity-limited processes by means of the analog computer MEDA 82 T.

A method for the calculation of dose-dependent pharmaco-kinetics by means of a combined zero and first-order model at the analog computer is presented. The results of the combined model can be converted into Michaelis-Menten parameters using simple equations. The method is usable for i.v. injection and for e.v. modes of application in the case of cmax greater than c = co/e.

Computers, Analog↗

[Drug combinations].

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Anti-Bacterial Agents↗