Clinical pharmacokinetics of co-trimazine.

The clinical pharmacokinetics of co-trimazine (trimethoprim plus sulphadiazine) are reviewed and compared with those of co-trimoxazole (trimethoprim plus sulphamethoxazole). Both combination drugs have similar serum half-life values in persons with normal renal function (half-life of 8 to 12 hours), but the sulphamethoxazole metabolites are retained more than trimethoprim in reduced renal function. Sulphadiazine is less metabolised and the total sulphonamide load of therapeutic doses of co-trimazine is therefore less than for co-trimoxazole.

Knee arthroscopy with local anesthesia in ambulatory patients. Methods, results and patient compliance.

Knee arthroscopy in locally anesthetized ambulatory patients has been performed by filling the knee joint with 50 ml to 60 ml of 0.5% prilocaine, with adrenaline and with additional local infiltration at the sites of puncture. During the arthroscopic procedure the joint cavity is further distended with a mixture of the same local anesthetic diluted 1:10 with physiological saline or Ringer's acetate.

Development of sulphonamide-trimethoprim combinations for urinary tract infections. Part 3: Pharmacokinetic characterization of sulphadiazine and sulphamethoxazole given with trimethoprim.

Plasma levels and renal excretion of sulphonamide and trimethoprim following oral administration of co-trimazine (140 mg sulphadiazine + 90 mg trimethoprim) and co-trimoxazole (800 mg sulphamethoxazole + 180 mg trimethoprim) were monitored in healthy volunteers after a single dose and in the steady state after 12-hourly dosage. The plasma levels of free, non-protein bound components after co-trimazine were approximately half those after co-trimoxazole and thus correlated with the doses given. Urine recovery of trimethoprim was better after co-trimazine (70%) than after co-trimoxazole (58%).

Development of sulphonamide-trimethoprim combinations for urinary tract infections. Part 2: Comparative pharmacokinetics of five sulphonamides.

The pharmacokinetics and renal excretion of the sulphonamides sulphachloropyridazine, sulphadiazine, sulphaisodimidine, sulphamerazine, and sulphamethoxazole were investigated in a cross-over study with doses of 800 mg each. The serum half-life, urine levels, distribution volume, protein binding and potential antibacterial activity in the urine renders sulphadiazine the preferred component in a combination tablet together with trimethoprim for the treatment of urinary tract infections.

Development of sulphonamide-trimethoprim combinations for urinary tract infections. Part I: Comparison of the antibacterial effect of sulphonamides alone and in combination with trimethoprim.

Plasma half life and in vitro activity were major criteria for selection of sulphonamides which are likely to give a strong synergistic action with trimethoprim in vivo. On the basis of literature data six sulphonamides, sulphadiazine, sulphachloropyridazine, sulphamethoxazole, sulphaisodimidine, sulphamerazine and sulphamethomidine appeared particularly suitable for combination with trimethoprim. An investigation of the activity in vitro of these compounds and their combinations with the latter against clinically isolated, sulphonamide-sensitive Klebsiella-Enterobacter and Escherichia coli strains showed optimal synergy at trimethoprim-sulphonamide ratios between 1:10 and 1:40, but that appreciable mutual potentiation occurred within a rather broad range of concentration ratios.

Synergistic activity of co-trimazine and co-trimoxazole in the urine.

Co-trimazine (sulphadiazine, 410 mg + trimethoprim, 90 mg) is a new drug combination developed especially for use in the treatment of urinary tract infections. In cross-over experiments in volunteers receiving daily doses of co-trimazine (2 X 500 mg and 1 X 1000 mg), co-trimoxazole (2X960 mg), or nitrofurantoin (3X50 mg), the degree of antibacterial activity of co-trimazine in the urine was at least as high as that of co-trimoxazole and much higher and more consistent than that of nitrofurantoin. In further cross-over experiments in volunteers receiving co-trimazine 2X1000 mg or co-trimoxazole 2X960 mg for four days no or only slight activity was found in the urine against a sulphonamide-resistant Group D streptococcus, but distinct synergistic activity between the components was found against four Escherichia coli strains sensitive to trimethoprim and sensitive or resistant to sulphonamides.

Antibacterial activity of co-trimazine in vitro and in vivo.

Co-trimazine is a new drug combination especially designed for the treatment of urinary tract infections. It consists of trimethoprim (90 mg) and sulphadiazine (410 mg). When combined in vitro, the components show high activity and a high frequency of synergy against urinary tract pathogens.

Effect of in vitro treatment with reducing drugs on structure and function of human secretory immunoglobulin A.

Samples of unstimulated whole saliva from 15 healthy children with 0.5--6 mg/100 ml of secretory IgA and from 10 healthy adults with 4--18 mg/100 ml of secretory IgA were pooled and treated in vitro with dithiothreitol and alpha-mercaptopropionylglycine. The effect of these reducing drugs on the immunochemical properties of secretory IgA was evaluated.

Studies on an iron-poly(sorbitol-gluconic acid) complex for parenteral treatment of iron deficiency anaemia.

A preparation containing an iron-poly(sorbitol-gluconic acid) complex for parenteral treatment of iron deficiency anaemia is described. The physical and chemical properties of the iron complex have been studied by using electrophoresis and gel permeation chromatography. A rapid absorption from the injection site after intramuscular administration to rabbits takes place, 70% of the iron being absorbed after 24-48 hours.

Ampicillin polymers as elicitors of passive cutaneous anaphylaxis.

The ability of ampicillin polymers to elicit passive cutaneous anaphylaxis (PCA) reactions in guinea pigs was analyzed. Mediating antibodies were raised in rabbits against a crude preparation of 6-aminopenicillanic acid (6-APA). It was found that large ampicillin polymers were potent elicitors, 1,000-fold better than benzylpenicillin polymers.

Blood levels of lidocaine after various infusion rates in patients with acute myocardial infarction.

Blood levels of lidocaine were estimated following two different infusion rates in patients with acute myocardial infarction. Forty-one patients received lidocaine as a bolus injection of 75 mg. directly followed by an infusion.