Тематичний Архів | Category Archives: Clinical Pharmacology

E.G. Nesukai.Zofenopril: ACE inhibitor with the special properties.

Zofenopril It is a sulfhydryl-containing, lipophilic ACE inhibitor with a very high affinity for cardiac ACE. It shows some physical and chemical properties, features of pharmacodynamics and pharmakokinetics which are absent in other drugs of this class. Most clinical value have high lipophilicity, which is associated with the prolonged effect of tissue ACE inhibition, antioxidant activity and cardioprotective properties. Sufficient experience of zofenopril application is presently accumulated in different cardiovascular diseases. Zofenopril is an effective antihypertensive ACE inhibitor that has been shown to improve blood pressure control in international placebo controlled randomised clinical trials and was effective as antihypertensives of other basic classes. In preclinical studies the sulfhydryl-group–containing ACE inhibitor zofenopril significantly reduced the frequency and severity of exertional and spontaneous cardiac ischemia. The anti-ischemic and cardioprotective effects of zofenopril have been confermed by the results of randomized controlled studies carried out under the SMILE program in patients with myocardial infarction. In the SMILE study, the early administration of zofenopril in nonthrombolyzed patients with myocardial infarction has been shown to reduce the incidence of death or severe congestive heart failure. The results of the SMILE-ISCHEMIA study extend the use of zofenopril in terms of cardioprotection and prevention of coronary events from the early to the late phase of myocardial infarction. In light of these results, zofenopril may be recommended as a secondary prevention drug treatment in post–myocardial infarction patients with coronary artery disease.

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M.I. Lutay, I.P. Golikova, A.F. Lysenko, V.V. Tovstukha.Efficiency of the fixed S-amlodipin and atorvastatin combination for patients with high and very high cardiovascular risk.

Efficiency and good tolerability of the fixed combination of S-amlodipin 2.5 mg with atorvastatin 10 mg during 12-weeks treatment of patients with high and very high cardiovascular risk was demonstrated in the paper. Among very high risk patients, 94 and 33 % patients, accordingly, achieved their blood pressure and low-density lipoproteins cholesterol (50 % reduction) targets, among high risk patients – 92 and 60 %. Patients with coronary artery disease taking 5/20 mg fixed combination showed improvement of exercise tolerance (increase of the average power workload by 20 W and workload duration by 118 sec). Fixed combination of S-amlodipin and atorvastatin was well tolerated: no serious clinical and laboratory side effects were registered.

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V.P. Ivanov.Influence of different modes of diuretic therapy on exercise tolerance, structural and functional heart status and quality of life in patients with systolic chronic heart failure.

In this study the influence of different modes of diuretic therapy on exercise tolerance, structural and functional heart status and quality of life in hypertensive patients with chronic systolic heart failure II–III functional class NYHA are reviewed.

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L.M. Yena, V.Ye. Kondratiuk.The efficiency and safety of S-amlodipine in elderly patients with essential hypertension.

Clinical efficiency and safety of 12-weeks treatment with S-amlodipine, as well its influence on central, intracardial hemodynamics, daily dynamics of blood pressure (BP) and ECG, structural and functional state of the heart were studied in elderly hypertensives. Target level of BP was achieved in 67 % patients under daily S-amlodipine dosage 5.0–7.5 mg. The positive influence of S-amlodipine on BP circadian rhythm, left ventricular hypertrophy regression, improvement of diastolic function and decrease of cardiac arrhythmias were shown. Treatment with S-amlodipine appeared to be safe in elderly hypertensives: no cases of severe of adverse events and adverse drug reactions were reported. Facial flushing and headache (7 %) were transitory and didn’t demand medicine withdrawal, while the case of the peripheral edema was registered under dosage of S-amlodipine 7.5 mg.

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J. Scholze, P. Bramlage, P. Trenkwalder, R. Kreutz Efficiency and safety of fixed combination of lercanidipine and enalapril in routine practice. Comparison of office, ambulatory and self-measured blood pressure.

The aim of the research was to study safety and efficiency of fixed combination of lercanidipine and enalapril in routine practice. This was a prospective, open, non-controlled study with 3-months follow-up. The patients received enalapril 20 mg and lercanidipine 10 mg in fixed combination. Office, ambulatory and self-measured blood pressure (BP) levels were measured. In total, 622 patients in the age 61.3±13.3 years were included, among them 54.2% males. Office BP decreased in average by 29.2/14.2 mm Hg, pulse BP – by 15.0±16.4 mm Hg. The number of patients with microalbuminuria decreased from 14.6 to 6.5% (Р<0.001). Side effects were registered in 3.4%. In conclusion, fixed combination of lercanidipine and enalapril was effective and well tolerated, improved parameters of BP and microalbuminuria.

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M.I. Lutai, I.P. Golikova, M.V. Bychko New possibilities of the combined hypolipidemic therapy: experience of clinical application of the fixed atorvastatin and ezetimibe combination.

Efficiency and good tolerability of the fixed combination of atorvastatin 10 mg and ezetimibe 10 mg is demonstrated in the article. This combination was used for treatment of dyslipidemia in patients with high and very high total cardiovascular risk, in which the target total cholesterol (TC) and low-density lipoproteins (LDL) cholesterol levels were not reached at background monotherapy with average and high doses of statins. The combination drug reduced TC by 32%, LDL cholesterol – by 47% after 4-week treatment. Percentage of patients achieving their LDL-cholesterol targets was 40% for very high risk patients and 66% for high risk patients. Ezetimibe and atorvastatin fixed combination was well tolerated, with a safety profile similar to statins alone.

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Т.А. Аbdullayev, О.Kh. Аllaberganov, B.U. Mardanov, R.Sh. Bekbulatova Clinical and hemodynamic effects of trimetazidine in patients with hypertrophic cardiomyopathy.

The aim of investigation was to study efficiency of trimetazidine in patients with hypertrophic cardiomyopathy (HCMP). The study included 38 patients with HCMP (38.4±2.9 years), 74% – males. The investigations included 12-lead ECG, echocardiography, Holter ECG monitoring, exercise test, subjective evaluation of the anginal pain. The patients from the first group (n=20) received trimetazidine 70 mg daily in addition to carvedilol, second group (n=18) – only traditional treatment. The follow-up duration was 3 months. More that half of patients had angina symptoms. Combined treatment with carvedilol and trimetazidine decreased angina and improved exercise tolerance.

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Ye.G. Nesukai Diagnostics and treatment of autonomic nervous system dysfunction in women with climacteric syndrome.

In 30 women with a climacteric syndrome (average age (54.9±0.7) years) we estimated autonomic disorders by questionnaires; autonomic balance was determined by cardiointervalography; ambulatory blood pressure monitoring was performed baseline and two months after prescribing phenibut 250 mgs TID. In 2 months of phenibut treatment in patients with a climacteric syndrome frequency of autonomic disorders diminished considerably, memory and concentration of attention got better, normalization of autonomic balance and sleep was noticed, as well as diminished blood pressure variability.

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R.L. DashdamirovThe influence of eprosartan on quality of life and hemodynamic parameters in patients with arterial hypertension and metabolic syndrome

The arm of the study was to assess influence of long-term therapy with angiotensin II receptor blocker eprosartan on blood pressure, left ventricular hypertrophy, lipid, carbohydrate metabolism, anxiety and depression in 64 hypertensive patients with metabolic syndrome. The results of our study demonstrated that apart from good antihypertensive effect, eprosartan caused regression of left ventricular hypertrophy, increased quality of life and decreased degree of depression. No negative effect on lipid and carbohydrate metabolism was revealed.

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I.V. MartynivDose-dependent hypotensive and renoprotective effect of atorvastatin in patients with arterial hypertension

The effect of atorvastatin on blood pressure, lipid profile and level of microalbuminuria (MAU) was studied in 138 patients in stage II hypertension (70 patients with essential hypertension and 68 patients with symptomatic renoparenchimal arterial hypertension). In addition to pronounced lipid-lowering effect, atorvastatin has hypotensive and renoprotective effect manifested by further reducing MAU in patients against background of hypotensive therapy. These properties of the drug are pleiotropic, because are not related to reduction of serum lipids and occur with prolonged (more than 6 months) use of atorvastatin in a dose of 20 mg daily

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