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Biomedical subjects

I Setnikar

Publications and source records attributed to I Setnikar.

At least 55 records · Page 3Linked to original sources
PubMed1977

Antimicrobial activity of tibezonium (TBZ).

The activity in vitro of tibezonium (Rec 15-0691), a new 1,5-benzodiazepine derivative, has been investigated. The drug was found active especially against Streptococcus, Diplococcus and Corynebacterium strains which are agents of oropharyngeal diseases. The activity of tibezonium was pH dependent against Staphylococcus aureus SG 511 and Streptococcus pyogenes 821 (at pH 8.0-8.5 It was more active) and the presence of horse serum provoked a small decrease of the antimicrobial properties. No interference on the activity of the tibezonium has been found in presence of smokers and non-smokers saliva.

Anti-Bacterial Agents↗
PubMed1975

Flavoxate and 3-methylflavone-8-carboxylic acid. Assay methods in blood and urine, plasma-red cells repartition and stability.

The following assay methods for pharmacokinetic studies on flavoxate (F) and on its main metabolite, i.e. 3-methylflavone-8-carboxylic acid (A), are described. 1. Spectrophotometry for the assay of F and of A in plasma, 2. TLC-Spectrodensitometry and GLC for the assay of A in urine after acid hydrolysis, 3. TLC-Spectrodensitometry for determining the F : A ratio in plasma or in urine. It was found that F hydrolyzes into A. This process depends on the pH and on the medium. In water, at pH 5.0, F is stable, while in phosphate buffer at pH 7.4 the semi-hydrolysis time is 60 min. In a solution with bovine serum albumin, in rat, rabbit, dog or human plasma the semi-hydrolysis times are between 5 and 60 min. Finally the plasma-red cells repartitions of F and of A were studied in vitro in rat, rabbit, dog and human blood and found between 0.8 and 2.0 for F and between 2.1 and 4.6 for A.

Animals↗
PubMed1975

Effects of different drugs on the urinary excretion of nifurpipone (NP) and of nitrofurantoin (NTF) in the rat.

A study was made on possible interferences of several drugs on the urinary excretion of nifurpipone and of nitrofurantoin orally administered to rats. Phenobarbital, a microsomial enzyme inducer, SKF 525 A, a microsomial enzyme inhibitor, probenecid, an inhibitor of the tubular acid secretory system, quanine, an inhibitor of the tubular alkaline secretory system, and hydrochlorothiazide, a diuretic, were studied. None of these treatments altered in an important way the urinary excretion of nifurpipone or of nitrofurantoin.

Administration, Oral↗
PubMed1975

Protein binding of flavoxate and of 3-methylflavone-8-carboxylic acid.

The protein binding properties of piperidino-3-methylflavone-8-carboxylate (flavoxate, F) and of its main metabolite, i.e. 3-methylflavone-8-carboxylic acid (M), were investigated by dialysis-equilibrium technique. During the dialysis, F hydrolyzes to a notable extent into M. Therefore a true equilibrium of F could not be obtained. With this limitation, the results show that F has a small protein affinity. The protein binding properties of M were separately investigated with bovine albumin, human albumin and with human, rat, rabbit and dog plasma. The Freundlich's isotherms, which describe the affinities of albumin to M, were calculated. They show that unconjugated M, possibly present in plasma, is by 99.5% in a protein-bound form.

Animals↗
PubMed1975

Pharmacokinetics of flavoxate in rats.

The plasma levels, the urinary excretion and the biliary excretion of piperidinoethyl-3-methylflavone-8-carboxylate (flavoxate, F) were studied in rats after i.v. and after oral administration. Parallel experiments were made with 3-methyl-flavone-8-carboxylic acid (M), the main metabolite of F. The substances are found in blood and are excreted in the urine and in the bile. The quantities excreted in the urine after oral administration are similar to those excreted after i.v. administration, showing that the enteric availability of the drugs is almost complete. The end product in urine and in bile is represented by a substance which yields M after a strong acid hydrolysis. There are marked pharmacokinetic differences between F and M, probably related to their physical properties.

Administration, Oral↗
PubMed1975

Flavoxate, a potent phosphodiesterase inhibitor.

The c-AMP phosphodiesterase inhibiting properties of flavoxate and of its main metabolite i.e. 3-methylflavone-8-carboxylic acid (MFCA), were assayed in vitro and compared to those of theophylline. Flavoxate and MFCA are competitive phosphodiesterase inhibitors, and are 21 and respectively 5 times more potent than theophylline. The smooth muscle relaxing activity of flavoxate possibly relies on this enzymatic mechanism.

Animals↗