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Biomedical subjects

R Gugler

Publications and source records attributed to R Gugler.

At least 145 records · Page 8Linked to original sources

Pharmacokinetics of ketamine in man.

A method for the analysis of ketamine and of its metabolites is described using gas-liquid chromatography for separation and flame ionization detection. The lower limit of detection for ketamine in serum was 0.025 mug/ml. The pharmacokinetic behaviour of ketamine after intravenous injection may be described in terms of an open two-compartment model. The serum half-life of ketamine was in alpha-phase about 11 min, the predominant half-life for the beta-phase 2.5 h. The half-life of ketamine and its metabolities in urine was comparable to that in serum. It could be shown that the duration of anaesthesia is not only correlated ti ist rapid metabolic breakdown and elimination, but also to the distribution of the drug peripheral tissue.

Chromatography, Gas↗

Effect of portacaval shunt on the disposition of drugs with and without first-pass effect.

The pharmacokinetic parameters of lidocaine, antipyrine and salicylamide were studied in dogs before and after construction of a portacaval shunt. The systemic availability of antipyrine was not altered significantly by the surgical procedure whereas the availability of lidocaine and salicylamide, drugs with a marked first-pass effect, was increased from 14.8 +/- 2.8 to 81.3 +/- 5.2% and from 21.8 +/- 7.8 to 57.5 +/- 2.5%, respectively. Of the 78% first-pass extraction of salicylamide, 36% is due to hepatic extraction whereas the remaining 42% is accounted for by intestinal wall extraction. The presence of a portacaval shunt also reduced the plasma clearance of lidocaine and antipyrine, but not salicylamide. The apparent volume of distribution was decreased only with salicylamide. Surgical construction of a portacaval shunt in dogs in a good model to evaluate first-pass effect. Physicians should adjust downward the dose of drugs with a first-pass effect. Physicians should adjust downward the dose of drugs with a first-pass effect in patients with a surgical portacaval shunt or endogenous portal systemic shunts such as seen in cirrhosis of the liver.

Animals↗

Pharmacokinetics of a new beta-adrenoceptor blocking agent, LF 17-895, in man.

The pharmacokinetics of a new potent beta-adrenoceptor blocking drug, bis-4-(2-hydroxy-3-isopropylamino-propoxy)-2-methyl indole sulphate (LF 17-895), have been studied in 5 volunteers after single oral (10 mg) and intravenous (4 mg) doses in a cross-over design. Following oral administration adsorption was rapid with peak plasma concentrations recorded after 3 h. Following the intravenous dose a biphasic decline of the plasma level curve was observed. The half-life of plasma elimination during beta-phase was 4.6 +/- 0.7 (p.o.) and 4.7 +/- 0.3 (i.v.) h, respectively. Absorption of the drug was 88.3 +/- 9.6% comparing the areas under the curve. 28.4 +/- 2.2% of the dose given i.v. was excreted in urine unchanged. When the pharmacokinetic data obtained with LF 17-895 were compared with those of pindolol, which differs only in lacking one methyl group in position 2 at the indole ring, only minor differences were seen: absorption of pindolol as well as plasma elimination were slightly faster.

Administration, Oral↗