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Biomedical subjects

A Jurgens

Publications and source records attributed to A Jurgens.

6 recordsLinked to original sources

Biochemical activity, pharmacokinetics and tolerability of tepoxalin, a cyclooxygenase/5-lipoxygenase inhibitor, in man.

Tepoxalin, a novel inhibitor of cyclooxygenase (CO) and 5-lipoxygenase (5-LO), was investigated for biochemical activity and pharmacokinetics in two studies. Study I was a 4-period, double-blind, randomized, single rising dose using 2 alternating panels (A, B) with interspersed placebo design (A: 25, 100, 400 mg, B: 50, 200, 800 mg p.o.). Study II was a 3-panel, randomized, placebo-controlled, double-blind, multiple dose study (A: 100 mg, B: 200 mg, C: 400 mg). In both studies, CO inhibition was assessed by generation of serum thromboxane (TxB2), 5-LO activity by LTB4 production ex vivo in Caionophore-stimulated blood. Plasma drug concentrations were assayed by HPLC for tepoxalin and its identified acid metabolite. It was found in both studies that at all dose levels the TxB2 generation was markedly suppressed (> 95% 2 h postdose). In study I, at 2 h postdose, % inhibition of LTB4 biosynthesis was marginal for the 3 lower doses but significant at 200 (14%), 400 (25%) and 800 mg (43%). In study II, the only significant inhibition occurred at the 400 mg dose at 6 h postdose on day 1 (17%) and on day 8 at 4, 6 and 8 h postdose (32, 42 and 32% respectively). In both studies and at all doses, plasma concentrations of tepoxalin varied widely between subjects. Linearity between plasma concentrations and dose could not be ascertained, and correlation between drug plasma levels and effect on LTB4 synthesis was poor. Single doses up to 800 mg and multiple doses up to 400 mg of tepoxalin were generally well tolerated.

Adult↗

Urinary and biliary excretion of aluminoxamine and ferrioxamine in dogs with various renal function.

We assessed the pharmacokinetics of aluminoxamine and ferrioxamine in dogs with sustained intermittent bile duct ligation and either normal renal function or stable chronic renal failure. A first group of male beagle dogs were given aluminoxamine and ferrioxamine, while a second group received desferrioxamine after loading them with iron and aluminum. Only minute amounts of ferrioxamine and aluminoxamine were found in the bile after administration of these compounds. The distribution volume of aluminoxamine and ferrioxamine appeared to be confined to the extracellular space and their renal excretion correlated with renal function. Administration of desferrioxamine to iron and aluminum-loaded dogs resulted in an increased biliary ferrioxamine but negligible aluminoxamine excretion. Renal clearance of the in vivo formed ferrioxamine and aluminoxamine in this group strongly correlated with renal function. Our observations indicate that biliary excretion of intravenously administered ferrioxamine and aluminoxamine is negligible even in renal failure. The data presented in this study provide indirect evidence that desferrioxamine administration to iron- and aluminum-loaded dogs results in the intra-hepatic formation of ferrioxamine which is partly excreted in the bile. Biliary excretion of aluminoxamine after desferrioxamine administration remained negligible.

Aluminum↗

[Carcinoma of superior aerodigestive pathways in the Otolaryngological Services of the Santa Creu and Sant Pau Hospital in Barcelona].

We have studied 1,353 patients with squamous cell carcinoma of the head and neck diagnosed between June 1984 and December 1991, at the Service of Otolaryngology of the Hospital de la Santa Creu i Sant Pau of Barcelona. We have analysed tumor location, age, sex, tobacco and alcohol consumption, tumor staging, and the incidence of nodal involvement as they relate to the extension of the primary tumor. We have found the features accepted for the south of Europe such as a high male predominance, and a very high incidence of advanced stages at the moment of diagnosis for all the regions except for the glottis. The glottis has been the only region--in the present study--where we have achieved an early diagnosis in a high proportion of cases.

Adolescent↗