[Alflutop - in modern symptom - modifying osteoarthritis therapy].

One of the serious problems during the treatment of osteoarthritis (OA) is the developing of adverse drug events during therapy. Nonsteroidal anti - inflammatory drugs (NSAIDs) are the first drugs with the high incidence and severity of adverse events. This article describes OA treatment strategies approaches for OA are presented using the complex drug Alflutop, which has a composition similar to the human hyaline cartilage. The drug has anti - inflammatory and analgesic effects, normalizes the function of the affected joints, improves the quality of patients' life, also has a structure - modifying effect. Such therapy is safe, well tolerable for patients, and can be used used as a starting complex OA treatment.

[Study on phenotypical activity of isoenzyme CYP3A4 in children].

The urine levels of cortisol and 6-beta-hydroxycortisol in 30 healthy children were determined with high performance liquid chromatography. The activity of cytochrome P450 isoenzyme CYP3A4 was estimated by the ratio of 6-beta-hydroxycortisol and cortisol. Differences in the CYP3A4 activity depended on the age sex. At the age of 4 to 9 years the value of the ratio was 9.21 +/- 0.67 which in fact was statistically higher than that in the children at the age of 0 to 3 years (p<0.001). In the female children at the age of 0 to 3 years the value of the isoenzyme CYP3A4 activity was actually lower (p<0,05) vs. the female children of the higher ages and the male children at the age of 0 to 3 years. The results are useful for further researches on improvement of drugs dosing and prevention of adverse reactions.

[Antihypertensive and nephroprotective effectiveness of AT1-angiotensin II receptor blocker valsartan in average therapeutic and maximal daily dose in patients with arterial hypertension and chronic kidney disease].

The results of the study which show efficiency of an antihypertensive and nephroprotective angiotensin II receptor blocker valsartan in patients with arterial hypertension of and chronic kidney disease are presented. Dose dependence of nephroprotective and antihypertensive effects of valsartan is demonstrated as well as high safety profile of the drug in average and maximal therapeutic doses.

[Correction of aldosterone level as marker of RAAS dysfunction in patients with arterial hypertension degree II-III and chronic kidney diseases].

The hyperactivation of renin-angiotensin-aldosterone system (RAAS) underlies the development and the progression of arterial hypertension and chronic kidney diseases. Aldosterone is the main unit of RAAS and self-sufficient predictor of the development of cardiovascular events. In this study, the angiotensin receptor blocker valsartan, ACE inhibitor enalapril, and direct renin inhibitor aliskiren were used for the correction of blood pressure and aldosterone levels in patients with hypertension and chronic kidney diseases. The data obtained suggest that the proposed complex therapy provides the most complete blood pressure reduction and aldosterone level correction (as evidence of RAAS activity recovery), greatly improves the prognoses, and ensures maximum nephroprotection in the patients with arterial hypertension and chronic kidney diseases.

[Omeprazol and ezomeprazol pharmacokinetics, duration of antisecretory effect, and reasons for their probable changes in duodenal ulcer].

There were authentic distinctions between the groups of healthy volunteers and patients with a peptic ulcer disease in Cmax, Tmax, AUC(0-t), AUC(0-infinity), CIt, Vd of omeprazole and Cmax of esomeprazole (Nexium, AstraZeneca). When the pharmacokinetics of omeprazole and ezomeprazole were compared in both groups, there were authentic distinctions in Cmax, AU(0-t), AUC(0-infinity), CIt, T1/2. The patients who had taken omeprazole the time of hypoacide condition was much shorter than in other groups. Disintegration test modeling pHmax for pH oscillation with large amplitude, that is typical for ulcer disease, demonstrated a possibility of early partial release of omeprazole, its acid-depended degradation and reduction of its bioavailability.

Experimental and clinical pharmacokinetics of amitryptiline: comparative analysis.

Pharmacokinetics of two amitriptyline tablets, Amitryptiline Nycomed and Amitryptiline, was investigated clinically and experimentally after a single oral dose of 50 mg. A statistically significant correlation between amitryptiline serum concentrations in dogs and healthy humans (r=0.683, p<0.006) was established. In humans, standartized values of peak concentration and area under the concentration curve were significantly higher, specific volume of distribution and total clearance were lower, and half-life and mean retention time were significantly higher than in dogs. Characteristics of apparent bioavailability in dogs and healthy people did not statistically differ.

[The pharmacodynamic and pharmacokinetic characteristics of furosemide and furesis]. / Osobennosti farmakodinamiki i farmakokinetiki furosemida i furezisa.

The object of the work was comparative study of the special features of the pharmacodynamic and pharmacokinetic properties of the diuretics furosemide and furesis in an ambulant regimen with the subject lying in an antiorthostatic position. Six practically healthy males were examined. They were given per os either 40 mg furosemide or one tablet of furesis (49 mg furosemide and 50 mg triamterine). Blood from the vein and urine were repeatedly tested.

[The pharmacodynamics and pharmacokinetics of furosemide during ordinary life activities and during head-down tilt hypokinesia in a healthy subject]. / Farmakodinamika i farmakokinetika furosemida v usloviiakh obychnoi zhiznedeiatel'nosti i pri antiortostaticheskoi gipokinezii u zdorovogo cheloveka.

The object of the work was comparative study of the characteristics of pharmacodynamics and pharmacokinetics of the diuretic furosemide during ordinary vital activity of man and under conditions of antiorthostatic hypokinesia. Six practically healthy males were examined. They took part successively in two experimental series: series 1--during an ordinary motor regimen under ambulatory conditions; series 2--under conditions of antiorthostatic hypotension (ANOH, 12 degrees). In both series with absolute correspondence of the procedures and order of manipulations the subjects were given 40 mg furosemide per os, venous blood and urine were repeatedly tested, and the physiological data were recorded. In combined action of an antiorthostatic position of the body and the diuretic an additive effect was encountered, i.e., increased therapeutic effect of, furosemide. The blood serum electrolyte composition practically did not change in this case. After oral administration of 40 mg furosemide maximal concentration of the drug in the blood (977 +/- 151 ng/ml) was found on the average in a group in 1.3 +/- 0.2 h. The drug half-life period in this case was 1.1 +/- 0.4 h; total clearance was 24.7 +/- 2.8 liter/h, and the distribution volume was 33.7 +/- 12.7 liters. In maintenance of antiorthostasis furosemide pharmacodynamics and pharmacokinetics changed but the individual character of the dynamics of drug concentration in the blood persisted. No statistically significant differences in the mean group pharmacokinetic parameters of the drug during an ordinary motor regimen and in antiorthostatic hypokinesia were encountered. Furosemide given in antiorthostatic hypokinesia led to diminished filling of the upper and middle parts of the lungs with blood despite the attendant decrease in the tonus of the resistant vessels.

[The pharmacokinetics of different drug forms of nifedipine when used singly and in a course as monotherapy and in combination with Cordanum and triampur preparations in patients with arterial hypertension]. / Izuchenie farmakokinetiki razlichnykh lekarstvennykh form nifedipina pri odnokratnom i kursovom primenenii v monoterapii i v sochetanii s preparatami kordanum i triampur u bol'nykh s arterial'noi gipertoniei.

Pharmacokinetics of three drugs derived from nifedipine: corinfar, corinfar retard, and SL adalate in the cases of a single and course administration in patients with arterial hypertension and the effect of cordanum and triampur on pharmacokinetics of corinfar retard in combined repeated administration have been studied. The studies were carried out in 6 groups of patients with arterial Hypertension, each group included 10 patients. Nifedipine concentration in blood plasma was determined using a special HPLC procedure within 24 h after administration of the drugs at a dose 20 mg. A pharmacokinetic characteristics of new drug adalate SL with two-step liberation of nifedipine. A possibility of autoinhibition was noted for corinfar and adalate SL in course therapy. A conclusion was made that cordanum and triampur did not affect the pharmacokinetics of corinfar retard.

[The pharmacokinetics of the new Russian prolonged-action form of diclofenac sodium--Ortopek--in a single oral dose]. / Farmakokinektika novoi otechestvennoi prolongirovannoi formy diklofenaka natriia--ortopéka--pri odnorazovom prieme vnutr'.

Ortopak tablets, 100 mg, were investigated. The pharmacokinetics of Ortopak was studied in 10 rheumatoid arthritis patients after a single oral dose of 100 mg. Ortophenum and voltaren-retard (Ciba-Geigy) were used for comparison. Diclophenac-sodium was measured in the patient's plasma by using high performance liquid chromatography. Ortopak was shown to be eliminated from the patient's body much slower than Ortophenum. The bioequivalence of Ortopak versus Ortophenum was 62.7%. The pharmacokinetic properties of Ortopak were similar to those of Voltaren-retard, which were close to those of diclophenac-sodium in the blood plasma within the therapeutic range.

[The pharmacodynamic and hypotensive efficacy of proxodolol in an acute drug test on hypertension patients]. / Farmakodinamika i gipotenzivnaia éffektivnost' proksodolola v usloviiakh ostrogo lekarstvennogo testa u bol'nykh gipertonicheskoi bolezn'iu.

The antihypertensive efficacy and hemodynamic effects of the new hybrid (beta-, alpha-) adrenoceptor blocking agent proxodolol were studied in 74 patients with mild, moderate, and severe arterial hypertension who received a single dose of 10, 20, or 40 mg. Oral and intravenous proxodolol showed a significant dose-dependent antihypertensive action which was independent of the type of hemodynamics and manifested itself by decreasing cardiac output.

[Pharmacokinetic characteristics of ethacizine in patients with disorders of heart rhythm]. / Osobennosti farmakokinetiki étatsizina u bol'nykh s narusheniiami ritma serdechnoi deiatel'nosti.

Significant differences in values of the volume of ethacizine distribution and clearance at oral administration in patients with myocardial infarction from those in patients with other pathology were established. A considerable decrease of ethacizine bioavailability in myocardial infarction patients was shown.

[A new Soviet drug, ethacizine, in the treatment of ventricular rhythm disorders]. / Novyi otechestvennyi preparat étatsizin v lechenii zheludochkovykh narushenii ritma.

The intravenous form of the Soviet anti-arrhythmic pharmaceutical ethacizine has been studied clinically. The pharmaceutical was administered to 30 patients with ventricular rhythm disorders during 3 to 15 minutes, at an average dose of 0.63 mg per 1 kg body weight, under the Holter monitor control. On the average the effect became apparent 6.5 min, after the injection and lasted on the average 149 +/- 15 min. Etacizine was effective in 77% of cases. It was established that there was no pronounced negative effect on the heart rate and the arterial pressure. Uzineg the tetrapolar rheography method it was shown that there was no pronounced negative effect on the central hemodynamics. The observation was made that etacizine induced a moderate decrease of the conductivity in atria AV-system and ventricles. Etacisin could be successfully used for rapid suppression of the ventricle rhythm disorders in various forms of coronary disease of the heart.