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Biomedical subjects

M Arr

Publications and source records attributed to M Arr.

At least 37 records · Page 2Linked to original sources

Pharmacokinetic and clinical studies with carfecillin.

The pharmacokinetics of carfecillin (Carbenicillin-phenyl-ester) were studied in 10 healthy subjects, in 5 patients with hepatic cirrhosis and in 5 cases of renal insufficiency. In healthy subjects maximal carbenicillin serum levels attained by therapeutic doses were about 20 microgram/ml; concentrations in the urine surpassed 1000 mu/ml. The phenol moiety was detectable as free phenol in sera (less than 1 microgram/ml) and urine (less than 3 microgram/ml), but its major part was transformed to glucuronide and sulphate conjugates. Pharmacokinetics were not altered significantly by hepatic lesion. In renal insufficiency, serum levels of both carbenicillin and conjugated phenol were higher and their decrease delayed, while urine concentration was low. Carfecillin treatment was successful in 20 out of 30 patients with UTI.

Bacterial Infections↗

On human biotransformation of some penicillins.

Urinary excretion of ampicillin, amoxicillin and oxacillin was studied in five healthy volunteers. Determinations were carried out by chemical methods (PC, TLC, spectrophotometry). Beside the parent compounds and their penicilloic acids, an alphaamino-substituted derivative was demonstrated. The total recovery of amoxicillin was nearly complete, recovery of ampicillin and oxacillin was about 50%. The combination of aminopenicillins with oxacillin did not alter significantly the excretion of the individual compounds.

Amoxicillin↗

The human biotransformation of nalidixic acid.

Authors have developed new chemical methods for studying the human metabolism of nalidixic acid. The methods are suited for the quantitative determination of nalidixic acid, hydroxynalidixic acid, nalidixic acid glucuronide, hydroxynalidixic acid-glucuronide, and of free and total glucuronic acid excretion. The total urinary excretion of NA and its metabolites was found to be 50 to 100% of the ingested dose. The percentual distribution of the individual metabolites was as follows: NA 0,5-5, HNA2,5-6, NAG24-80, and HNAG11-26%. It was unanimously proved by enzymatic decomposition and specific chemical reactions that the excreted conjugates were monoglucuronides. The significance of individual differences, bilirubin metabolism, urinary pH and the pharmacokinetical behaviour of the individual metabolites is discussed from the therapeutic view.

Biotransformation↗