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Biomedical subjects

V Rejholec

Publications and source records attributed to V Rejholec.

66 records · Page 4Linked to original sources
PubMedDate not supplied

Interspecies pharmacokinetic scaling of metazosin, a novel alpha-adrenergic antagonist.

Based on pharmacokinetic data from mice, rats, and rabbits, the prediction of pharmacokinetics of intravenous metazosin in man has been performed. The correlations were based upon allometric scaling of plasma clearance and the volume of distribution at steady-state. A one-compartment body model approximating clinical pharmacokinetics fits well the elimination phase of subsequently measured metazosin concentrations in volunteers. Fitting human pharmacokinetic data to allometric equations enabled us to superimpose pharmacokinetic curves from different species.

Adrenergic alpha-Antagonists↗
PubMedDate not supplied

[Long-term therapy of rheumatoid arthritis with perclusone].

124 patients afflicted with rheumatoid arthritis were being treated with gold salts or antimalarial preparations with the addition of corticoids as well as other antirheumatic preparations. If the Lansbury-Index fell under 30% of the initial value, the therapy was interrupted, and that in 84 patients. One half of these patients were then given Perclusone (Clofezone) in the dose of 600 mg daily for 4 years. The other half of patients -- as control group-- were given various non-steroid antirheumatics, mostly acetylsalicylic acid, phenylbutazon or indomethacin in normal doses. The course of the disease of both groups was followed up clinically and the Lansbury-Index as well as the number and duration of reactivations were determined. In the group treated with Perclusone, the previously obtained remissions remained substantially more stable, only rarely reactivations ensued and their duration was then also remarkably shorter. Tolerance of Perclusone was very good, no side-effects whatsoever have been ascertained. In the group treated with other antirheumatics distinctly more frequent and longer-lasting reactivations were ascertained. Tolerance of these drugs was generally worse and they had to be changed more frequently. Perclusone has thus proved efficient as a very good stabilizing drug in patients suffering from rheumatoid arthritis.

Administration, Oral↗
PubMedDate not supplied

Pharmacokinetics of flobufen and its main active metabolite in the rat.

Pharmacokinetic study of the anti-inflammatory [3H] flobufen (I) and its active metabolite (II) has been carried out in rats given po and iv doses of 2, 10, and 50 mg/kg I and equimolar doses of II. Various pharmacokinetic parameters of I and II [dose normalized AUC; mean residence time (MRT); systemic blood clearance; steady state volume of distribution, (Vss)] are dose-independent. I is completely absorbed from the gastrointestinal tract and is rapidly (MRT = 7.2 hr) converted to II, which is slowly (MRT = 2.6 days) eliminated from the blood. The fraction of total blood clearance that forms II is 0.83 following iv dose of I. The Vss of the less lipophilic metabolite II is somewhat lower (0.36-0.46 liters/kg) than that of the parent drug (0.51-0.56 liters/kg).

Animals↗
PubMedDate not supplied

Interleukin-2 activated cells from peripheral blood of patients with systemic lupus erythematosus.

The effect of recombinant interleukin-2 (IL-2) on proliferative and cytotoxic response of peripheral blood mononuclear cells (PBMC) was investigated in a group of 21 patients with systemic lupus erythematosus (SLE). There was a significant decrease in thymidine uptake of peripheral blood mononuclear cells when compared with controls. However, IL-2 induced cytotoxicity was not diminished and minimal frequencies of lymphokine-activated killer (LAK) cells precursors remained in the range of control group. These data provide an evidence about the dissection between proliferative and cytotoxic response of PBMCs to exogenous interleukin-2 in patients with SLE in vitro. The factors contributing to this effect and the clinical significance of these findings remains to be answered.

Adolescent↗