A pilot study of golexanolone, a new GABA-A receptor-modulating steroid antagonist, in patients with covert hepatic encephalopathy.

Background & Aims: Golexanolone is a novel small molecule GABA-A receptor-modulating steroid antagonist under development for the treatment of cognitive and vigilance disorders caused by allosteric over-activation of GABA-A receptors by neurosteroids. It restored spatial learning and motor coordination in animal models of hepatic encephalopathy (HE) and mitigated the effects of intravenous allopregnanolone in healthy adults in a dose-dependent fashion. Herein, we report data on the safety, pharmacokinetics (PK) and efficacy of golexanolone in adult patients with cirrhosis.

Safety and Immunogenicity of the GamTBvac, the Recombinant Subunit Tuberculosis Vaccine Candidate: A Phase II, Multi-Center, Double-Blind, Randomized, Placebo-Controlled Study.

GamTBvac is a candidate tuberculosis vaccine with two fusion proteins, containing Ag85a, ESAT6, CFP10, and a dextran-binding domain (DBD). Phase II of a double-blind, randomized, multicenter, placebo-controlled study in parallel groups in healthy adults to evaluate the safety and immunogenicity of GamTBvac in 180 previously-vaccinated with Bacillus Calmette-Guérin vaccine (BCG) healthy volunteers without (MTB) infection was conducted. The dose (0.

[Methods for the protection against counterfeit medications. Part 2. The assessment of interlot dispersion of the metoprolol succinate tablets fabricated by different manufacturers].

This paper reports the results of analysis of the metoprolol succinate tablets fabricated by two different manufacturers, Akrikhin (Russia) and AstraZeneka (Sweden) by near-IR spectroscopy in the combination with the chemometric processing of the data obtained (discriminative analysis). It is concluded that this method is applicable for the assessment of interlot dispersion of the metoprolol succinate tablets.

[The methods for the protection against counterfeit medications. Part 1. The estimation of the quality of metoprolol succinate substance and tablets from different manufacturers in terms of "identity" and "active ingredient content"].

This paper was designed to report the results of analysis of metoprolol succinate substance and tablets obtained from two manufacturers, Akrikhin (Russia) and AstraZeneca (Sweden). The analysis was performed by spectroscopy in the near IR region and followed by the chemometric treatment of the data obtained. The method was used to confirm the "identity" of metoprolol succinate tablets.

Trimetazidine in Angina Combination Therapy--the TACT study: trimetazidine versus conventional treatment in patients with stable angina pectoris in a randomized, placebo-controlled, multicenter study.

The aim of this study was to assess the efficacy and acceptability of trimetazidine (TMZ) in combination with hemodynamic agents (beta-blockers or long-acting nitrates) in 177 stable angina patients. In this randomized, placebo-controlled study (TACT: Trimetazidine in Angina Combination Therapy), stable angina patients resistant to nitrates or beta-blockers were selected. After a 1-week selection period (W0), patients who had a difference of <10% in duration between 2 positive exercise tests, defined as 1-mm ST-segment depression (STD) 80 milliseconds after J point with angina pain or 1.

[Trimetazidine in pectoris patients older than 65 years with stable angina].

Aim: To study efficacy of trimetazidine including action on quality of life in patients over 65 years of age with stable angina pectoris.

Material: Seventy two patients (75% men, age 65-80 years) with stable class II-III angina not completely controlled by baseline conventional combined antianginal therapy (nitrates, beta-blockers, and calcium antagonists).

Methods: Trimetazidine (60 mg/day) was added to baseline therapy for 12 weeks.

[Antihypertensive efficacy, tolerance and safety of lisinopril (sinopril) and captopril (capoten) in patients with mild and moderate arterial hypertension].

Aim: To compare effectiveness, tolerance and safety of two inhibitors of angiotensin-converting enzyme--sinopril (lisinopril) and capoten (captopril)--in outpatient treatment of patients with mild and moderate hypertension.

Materials And Methods: The patients were randomly assigned to sinopril or capoten groups. Sinopril was given in daily dose 10-40 mg, capoten--in daily dose 25-100 mg for 8 weeks.

[Experimental validation of the use of betamecil in ophthalmology].

Wound-healing activity of 2% betamicil ointment in comparison with the traditional stimulants of corneal repair regeneration (methyluracyl and solcoseril) was studied in experiments. The rate of epithelialization of a standard trephination wound in rabbit cornea (28 animals), mitotic activity of the anterior corneal epithelium, and strength of the regenerated tissue were assessed after use of different stimulants and in control. A maximal positive effect of local betamicil (2% ointment) was observed: the wounds epithelialized 57% sooner than in control, but there was no reliable difference from solcoseril; the regenerate of linear corneal wound was 1.

[Role of Helicobacter pylori in the etiology of duodenal ulcer recurrence after selective proximal vagotomy].

126 patients with duodenal peptic ulcer were examined before and in different periods after operation for selective proximal vagotomy (SPV). Endoscopy was performed and Helicobacter pylori (HP) was detected by the urease, bacteriological, and histological methods. The urease test proved to be the most informative, simple, and available method for revealing infection of the gastric mucosa by HP.

[Leocaine--a new generation of local anesthetics].

Leocaine is a new crystal beta-modification of beta-dimethylaminoethyl ether of n-butylaminobenzoic acid hydrochloride. Its chemical formula is the same as for dicaine, but it has a number of advantages over this drug. The anesthetic activity of leocaine is 2.

[The preoperative assessment of concomitant ischemic heart disease in patients with an abdominal aortic aneurysm].

To reveal and evaluate the severity of concurrent coronary heart disease (CHD) in patients with atherosclerotic aneurysm of the abdominal aorta and to optimize preoperative preparation and intraoperative management, 38 patients underwent comprehensive physical examination, echocardiography, a set of ECG exercise tests. Concurrent CHD was encountered in 87% of cases with abdominal aortic aneurysm. The specific feature of CHD in this aortic abnormality is the predominance of its severe forms as evidenced by findings of coronary circulatory reserve.

[Functional state of the myocardium during transesophageal cardiac pacing in patients with ischemic heart disease selected for surgical treatment based on nuclear stethoscope findings].

A nuclear stethoscope was used to examine central hemodynamic parameters and myocardial contractility in 70 patients with coronary heart disease (CHD). The findings were analyzed according to the degree of cicatricial changes in the myocardium and coronary atherosclerotic lesion. The patients, unlike apparently healthy individuals, were found to show an increase in systolic cardiac output and a decrease in left ventricular ejection fraction in response to transesophageal cardiac pacing.

[Detection of cardiac insufficiency by computer-assisted monitoring of the response of intra-cardiac hemodynamics to exercise test in patients with ischemic heart disease with similar lesions of the coronary arteries (patient selection for the aortocoronary bypass)].

Preoperative identification of cardiac insufficiency in patients with ischemic heart disease (IHD) has proved essential for the success of surgery on the coronary arteries. To provide for an objective assessment of the contractile function of the myocardium in selecting candidates for surgery among IHD patients with over 70-percent narrowing of one, two, and three coronary arteries, use was made of the central hemodynamics indices in response to the loading test during right heart catheterization with computer-assisted monitoring and mathematical analysis. Two patient groups were distinguished during the hemodynamic loading test: group I showing a high and effective chronotropic reserve (+X) and group II presenting a negative chronotropic reserve (-X).

[Indications for aortocoronary shunting in relation to ejection fraction and segmental activity of the left ventricle (data of the coronarography, ventriculography and intra-cardiac hemodynamics)].

The left-ventricular ejection fraction, reflecting the contractile capacity of the myocardium according to the clinical data, is the most objective criterion in indication for the operation for aortocoronary shunting. The indices of central hemodynamics appearing in response to the exercise test during intracardiac catheterization of the right heart and monitor-computer control with mathematical analysis were used in objective appraisal of the left-ventricular ejection fraction in selecting for surgical treatment patients suffering from ischemic heart disease with normal and reduced ejection fraction of the left ventricle. Two gradations of patients with ischemic heart disease were set apart during the hemodynamic exercise test: the first--patients with a high and effective chronotropic reserve--subgroup I("+X") and the second--patients with a poor and ineffective chronotropic reserve--subgroup II("--X").

[Radionuclide ventriculography in the evaluation of left-ventricular function in patients with arterial hypertension].

Systemic and intracardiac hemodynamic parameters were examined in 29 patients with arterial hypertension by radionuclide ventriculography. No impairments were found in resting left ventricular pump function in the patients. Left ventricular diastolic function exhibited 24 and 34.

[Thyroid hormone content of the blood plasma and tolerance for physical loading in ischemic heart disease patients].

Blood thyroid hormones were measured before and after the rationed exercise test in 79 patients with angiographically verified diagnosis of coronary heart disease. A relationship was demonstrated between postexercise blood T3 variation and functional coronary circulation reserve. Hormonal baselines, and exercise-induced blood T4 changes were basically similar in patients with coronary disease of different severity.

[The scissors phenomenon in the reaction of hormonal systems to the physical load test in ischemic heart disease patients].

A difference between baseline and final plasma hormonal (insulin, cortisol, somatotrophic hormone, triiodothyronine (T3) and thyronine (T4) levels, related to the pattern of response to physical stress, was demonstrated in 67 coronary patients with angiographically verified diagnosis. Post-exercise increase in these hormones was associated with their lowered baseline and elevated final blood levels, as compared to those patients who showed a decrease in hormonal levels in response to exercise, with the baselines exceeding final values.

[Atherosclerotic lesion of the coronary arteries in ischemic heart disease patients with differing levels of insulin, cortisol and somatotropic hormone and the type of reactions of these hormones to physical loading].

Plasma insulin, cortisol and somatotropic hormone (STH) levels of coronary patients are related to the extent of atherosclerotic lesion of coronary arteries. The relationship between coronary atherosclerosis and hormonal activity becomes particularly evident through the pattern of hormonal response (a rise or a fall) to rationed exercise. An elevated insulin baseline and reduced postexercise levels are typical for coronary patients with only slightly narrowed (25% or less) coronary arteries.