[Functional state of the vessel endothelium in patients with systemic lupus erythematosis].

SLE patients show the formation of endothelial dysfunction manifested by the decreuse of endothelial dependent vasodilatation in response to reactive hyperemia test and incapuse of carotid artery intima-media thickness (IMT). Disorder of Endothelial dependent vasodilation damage in SLE patients is associated with age, damage index and inflammatory process activity. An association with the duration of the disease was not been found. (IMT) thickness increase is associated with the age, damage index and has no correlation with the duration of the disease. The rate of atherosclerotic plaques in the carotid artery in SLE patients exceeds by 1.8 times that of the control group. Atherosclerotic identification rate was found to have tight association with age, disease activity and damage index. Atherosclerotic damage degree is associated with damage index and disease activity and has no correlation with age and the duration of the disease.

[Efficacy and safety of treatment with methotrexate, leflunomide, detralex, and their combination of patients with rheumatoid arthritis]. / Efektyvnist' ta bezpeka likuvannia khvorykh na revmatoïdnyi artryt metotreksatom, leflunomidom, detraleksom ta ïkh poiednanniam.

A comparative evaluation was done of efficacy and safety of methotrexate, leflunomide singly and of combination of methotrexate with leflunomide or detralex. A total of 189 patients with rheumatoid arthritis (RA) were examined. A 6-month course of controllable treatment was instituted in them. The time-related course of clinical-and-laboratory indices allowed judgement about efficiency of the treatments administered. The functional condition of the patients was assessed according to HAQ. As to efficacy and toxicity, leflunomide (in a dose of 20 mg/daily) was comparable to methotrexate (7.5 to 10 mg/per week) whereas the combination leflunomide-methotrexate has been shown to considerably accelerate regression of clinical symptoms of RA while the use of detralex in the therapeutic complex proved to enhance efficiency of pharmacotherapy with methotrexate and to reduce the incidence rate of its side effects.

[The effect of combined therapy on the ortofen concentration of the blood plasma and synovial fluid in patients with rheumatoid arthritis]. / Vplyv kombinovanoï terapiï na kontsentratsiiu ortofenu v plazmi krovi ta synovial'nii ridyni u khvorykh na revmatoïdnyi artryt.

A pharmacologic investigation confirmed the possibility of deliberate correction of pharmacological properties of the nonsteroidal anti-inflammatory preparation orthophen in a clinical setting by combining it with those drugs (cimetidin and cocarboxylase) capable of inhibiting elimination of orthophen from the body. In consequence, the level of the drug gets elevated not only in blood plasma but also in the synovial fluid of those joints affected by inflammation, which fact secures high efficiency of the antiinflammatory therapy.

[Kinetics of tramal, benzofurocain and amidopyridine demethylation under inhibitory conditions produced by cimetidin, orthophen and thiamine diphosphate]. / Aktyvnist'demetylasy v umovakh ingibirovaniia tsimetydynom, ortofenom i tiamindifosfatom.

Demethylation kinetics of analgetics tramal, benzofurocain and amidopyrine has been studied through the experiments on microsomal fraction of white rats' liver. It was found that tramal demethylation is apparently catalysed with the help of two enzymes, possessing various affinities towards the substrate. Kinetics of benzofurocain and amidopyrine demethylation is satisfactory described with the help of Michaelis-Menten equation. Cimetidine, thiamine diphosphate and orthophen (at concentrations close to therapeutic ones) exhibit mixed-type inhibition in respect of all three demethylaze substrates under study.

[The pharmacokinetic determinants of the analgesic effect of benzofurocaine in patients with burns and wounds of the joints]. / Farmakokinetychni determinanty analhetychnoho efektu benzofurokaïnu u khvorykh z opikamy ta urazhenniam suhlobiv.

The non-narcotic analgetic benzofurocaine in intravenous administration at the dose level of 300 mg exerts an apparent analgesic effect in those patients with various pathogenetic mechanisms of the pain syndrome. The pharmacologic effect of the drug depends upon its blood plasma content. The character of the interrelationship is described by hysteresis curve suggesting the pharmacologic effect to be behind the time of building up of maximum blood drug concentration. The pharmacokinetic determinants of the analgesic action of benzofurocaine are the area under the pharmacokinetic curve, half-life period, and average time of drug retention in blood. There is a close direct correlation between the above determinants.