PubMed Health⌕ Search
Home/Archive/PubMed

PubMed · 6334657

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

H P Kuemmerle·G Hitzenberger·G Nieder·J Rasper·H Jaeger
View original source ↗Export metadata ↓

Abstract

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. They were below the detectable limit. Salicylic acid metabolites were present in plasma also under the limit of detection (0.5 microgram/ml). In urine the metabolite salicyluric acid was measured in considerable quantities, whereas gentisinic acid was under the limit of detection. Three healthy volunteers were given a single p.o. dose of 750 mg imidazole 2-hydroxybenzoate in order to examine the practicability of these new methods a well as to evaluate the pharmacokinetics. The data are presented and interpreted. Further studies in this respect are advised.

Explore related subjects

Anti-Inflammatory Agents, Non-SteroidalBiotransformationChromatography, High Pressure LiquidHippuratesHumansImidazolesKineticsModels, BiologicalPilot ProjectsSalicylatesSalicylic AcidJournal Article

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

H P Kuemmerle, G Hitzenberger, G Nieder, J Rasper, H Jaeger. 1984. Pharmacokinetic pilot study with imidazole 2-hydroxybenzoate using new analytical methods.. https://pubmed.ncbi.nlm.nih.gov/6334657/

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related citations

PubMed2007

Stereodifferentiating drug-biomolecule interactions in the triplet excited state: studies on supramolecular carprofen/protein systems and on carprofen-tryptophan model dyads.

Stereoselective interaction between a chiral nonsteroidal antiinflammatory drug, namely carprofen (CP), and human serum albumin (HSA) was studied, and the results were compared with those obtained with model dyads. In the presence of albumin the same triplet-triplet transition was detected for both CP stereoisomers; however, time-resolved measurements revealed a remarkable stereodifferentiation in the CP/HSA interaction. For each stereoisomer, the decay dynamics evidenced the presence of two components with different lifetimes that can be correlated with complexation of CP to the two possible albumin binding sites (site I and site II). This assignment was confirmed by using ibuprofen, a site II displacer. Thus, the shorter lived components, for which stereodifferentiation was more important (tauR/tauS ca. 4), were ascribed to the CP triplet state in site I; the lifetime shortening can be attributed to electron-transfer quenching by the only tryptophan (Trp) of the protein. Laser flash photolysis of model dyads containing covalently linked CP and Trp revealed formation of the expected Trp radical cation, providing support for such a mechanism. Moreover, significant stereodifferentiation was observed between the (R)- and (S)-CP-Trp dyads. In the case of CP/HSA complexes, as well as in the model compounds, the stereodifferentiation detected in the decays is in good agreement with that observed in the formation of the only CP photoproduct, resulting from a photodehalogenation process. Moreover, stereodifferentiation was also found to occur for the photobinding of CP to the protein.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2007

Statins may be beneficial for patients with slow coronary flow syndrome due to its anti-inflammatory property.

The phenomenon of slow progression of angiographic contrast in the coronary arteries in the absence of stenosis in the epicardial vessels in some patients presenting with chest pain has been recently called as slow coronary flow syndrome because the underlying pathophysiological mechanisms as well as therapeutics of this unique phenomenon is less well understood. Although this phenomenon was first reported on in 1972 by Tambe, few studies have focused on the etiology of this unique angiographic finding since that time. Several hypotheses have been poised to elucidate this phenomenon, including a form of early phase of atherosclerosis, small vessel dysfunction, Hagen-Poiseuille's equation model, imbalance between vasoconstrictor and vasodilatory factors, and platelet function disorder. During the last several years there has been arisen the most interesting concept of "atherosclerosis as a inflammation disease", which is involving the different entities of coronary artery disease covering slow coronary flow syndrome. The angiographic finding appeared as slow flow is an important clinical entity because it may be the cause of angina at rest or during exercise, acute myocardial infarction, and hypertension. Despite the good prognosis, patients complained commonly of persistent uncomfortable chest, which can significantly impair quality of life. There is no effective therapy for patients with slow coronary flow syndrome up to now. Statins have been showed the important benefits for the large populations of individuals at high risk of coronary artery disease. In addition to lowering lipid profile, statins have pleiotropic effects on improving vascular function. Increasing evidence, suggests that reduction of cardiovascular events conferred by statins relates not only to cholesterol lowering but also to direct effects on endothelium function as well as anti-thrombotic and anti-inflammatory actions. Accordingly, we hypotheses that these pleiotropic effects of statin may be beneficial for patients with slow coronary flow syndrome due to its pharmacological basis.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2007

Conservative treatment for patent ductus arteriosus in the preterm.

BACKGROUND: A patent ductus arteriosus (PDA) is common among preterms, and prophylactic medical treatment has been advocated as the first-line approach. Conservative treatment may result in similar outcome, but without exposure to the harmful side effects of medication. A retrospective analysis revealed a ductal closure rate of 94% after conservative treatment with adjustment of ventilation (lowering the inspiratory time and increasing positive end expiratory pressure) and fluid restriction. OBJECTIVE: To study prospectively over one year the rate of PDA closure, and morbidity and mortality following conservative treatment. METHOD: Prospective study (1 January 2005 - 31 December 2005) including 30 newborns <or=30 weeks' gestation, all of whom were being ventilated and required surfactant. Echocardiography was performed 48-72 h after birth. Clinically important PDA was conservatively treated as described above. The percentage of children with PDA, ductal ligation and major complications was determined. RESULTS: Ten neonates (33%) developed a clinical important PDA. Following conservative treatment the duct closed in all neonates (100%), and none required ductal ligation or medical treatment. The rates of major complications were no higher than those reported by the Vermont Oxford Network and in the literature. CONCLUSION: The managed care plan resulted in an overall ductal closure rate of 100%. These results suggest that conservative treatment of PDA is a worthy alternative to prophylactic medical treatment.

Anti-Inflammatory Agents, Non-Steroidal↗