Imidazole binding to human serum albumin.

Imidazole is a substance released by the organism when a new salicylate derivative, imidazole salicylate is administered. A study was made of the binding of imidazole to human serum albumin by an in vitro assay employing an ultrafiltration technique. For the concentration range that imidazole was found in plasma following administration of the drug to healthy volunteers, the mean binding percentages were: 12.

Pharmacokinetic evaluation of fosmidomycin, a new phosphonic acid antibiotic.

The pharmacokinetics of fosmidomycin in phase I with a total of 127 healthy male volunteers is described through single--and repeated--dose studies using oral and parenteral routes of administration. The study results indicate that fosmidomycin is well tolerated even when given in repeated doses of 8 g/day i.v.

Pharmacokinetic profile of imidazole 2-hydroxybenzoate, a novel nonsteroidal antiinflammatory agent.

Imidazole 2-hydroxybenzoate is a novel nonsteroidal antiinflammatory agent which clinico-pharmacologically and pharmacokinetically has to be understood as imidazole and salicylic acid. The pharmacokinetic profile of both components after single and multiple oral (tablets, drops), and topical administration (gel 5%)--the latter in a pilot study--was evaluated as well as protein-binding, relative bioavailability and the metabolic pattern. Absorption and elimination of the two compounds were fast.

Fosmidomycin, a new phosphonic acid antibiotic. Part II: 1. Human pharmacokinetics. 2. Preliminary early phase IIa clinical studies.

The pharmacokinetics of fosmidomycin in phase I with a total of 127 healthy male volunteers is described through single and repeated dose studies using oral and parenteral routes of administration. The study results indicate that fosmidomycin is well tolerated when even given in repeated doses of 8 g/day i.v.

Fosmidomycin: a new phosphonic acid antibiotic. Part I: Phase I tolerance studies.

The pharmacokinetics of fosmidomycin in phase I with a total of 127 healthy male volunteers is described through single and repeated dose studies using oral and parenteral routes of administration. The study results indicate that fosmidomycin is well tolerated even when given in repeated doses of 8 g/day i.v.

Pharmacokinetic pilot study with imidazole 2-hydroxybenzoate using new analytical methods.

Imidazole 2-hydroxybenzoate is a new antiphlogistic compound with analgesic and antipyretic properties undergoing clinical investigations. The purpose of this pilot study was to evaluate new methods for the quantitation of imidazole, salicylic acid and salicyluric acid in plasma and urine. Imidazole metabolites caused considerable methodologic difficulties in plasma and urine.

Lipid-lowering agents and their meaning in the treatment of the fat metabolism-atherosclerosis functional circle.

The clinical pharmacology of lipid-lowering agents and their meaning in the treatment of the fat metabolism-atherosclerosis functional circle are described. All the aspects associated with these important problems are carefully analyzed and the possible consequences for their rational use are interpreted. The current view of the actual situation in this field is presented and the trends in the development of prophylactic and therapeutic treatment with lipid-lowering agents in the fat metabolism-atherosclerosis functional circle are shown.

A double-blind, placebo-controlled evaluation of (dl)-3,7-dihydro-1,8-dimethyl-3-(2-methylbutyl)-1H-purine-2,6-dione in exercise-induced bronchospasm.

The investigational drug, (dl)-3, 7-dihydro-1, 8-dimethyl-3-(2-methylbutyl)-1 H-purine-2, 6-dione, has been proven to be an active bronchodilator and antiallergic compound in animal and clinical studies. Adult asthmatic patients who demonstrated greater than or equal to 20% improvement in FEV1 after inhalation of aerosolized isoproterenol or its equivalent and greater than or equal to 20% reduction in FEV1 after a graded treadmill exercise received theophylline (3, 6 mg/Kg, every 6 h) for 4 days. Further selection of patients was made by demonstrating that theophylline effectively blocked exercise-induced reduction in FEV1 and was effective in increasing FEV1 by 20% when measured 2 h after oral administration.

Comparative bronchodilatory activity of cetiedil citrate monohydrate, theophylline, orciprenaline and placebo in adult asthmatics.

In 40 patients, a seven day observation period in which oral bronchodilators and corticosteroids were eliminated, cetiedil (100 mg, t.i.d.