[Assessment of equivalence of the original tamsulosin and its generics].

Generics constitute a significant part of the modern pharmaceutical market. The use of generics in the case of their equivalence to the original drug allows to reduce the burden of health care costs. Often, however, the quality of generics does not match that of the original drug. The results of study suggest that the investigated generics of tamsulosin may not be fully recognized as pharmaceutically equivalent to the original drug.

[Evolution of oral drug forms of metoprolol: advantages of long acting modified release forms with modified release].

Review oral modified release drug forms of beta-adrenoblocker metoprolol which is used in arterial hypertension and ischemic heart disease is presented. Metoprolol has salts such as tartrate which is used for production of immediate release (IR) and sustained release (SR) forms and succinate used for production of controlled release form (CR/XL). Metoprolol SR has monolith matrix type, metoprolol CR/XL-system of multiple pellets. Effect of metoprolol tartrate (IR) on mortality was demonstrated in a number of studies in patients with arterial hypertension (AH) (MAPHY), myocardial infarction (SMT, GMT, MIAMI), dilated cardiomyopathy and heart failure (MDC). Studies of efficacy of metoprolol SR are scarce. Antihypertensive efficacy of metoprolol SR in patients with AH did not exceed that of a metoprolol IR or CR/XL. First retrospective analysis of efficacy of metoprolol tartrate and succinate (CR/XL) in patients after myocardial infarction allowed to obtain comparable results of 34% mortality lowering. In a prospective study in patients with chronic heart failure (COMET) metoprolol tartrate IR was not superior to carvedilol when mortality lowering was concerned. At the same time administration of controlled release metoprolol (CR/XL) in 2 large clinical trials (RESOLVD, MERITAHF) was advantageous in patients with chronic heart failure relative to lowering of mortality and rate of hospitalizations. A novel controlled release form of metoprolol has been created as a tartrate salt on the basis of pellet technology (CD/ERT) and its bioequivalence to metoprolol CR/XL has been proved.

[Interaction of omnic (tamsulozine) and its generic analogues with alpha-adrenoreceptors].

In current practice of pharmacotherapy of prostatic adenoma alpha1-adrenoblockers are first-line drugs the efficacy and safety of which have been proved in many randomized studies. Because of the appearance of a large amount of generic analogues of tamsulozine on the market we studied the ability of tamsulozine analogues to bind with alpha-adrenoreceptors on rat and human prostate affected by adenoma. Significant differences on the receptor level of interaction were found. Omnik, compared to other generic analogues of tamsulozine, has the highest affinity to alpha1-adrenoreceptors.

[Economics of nephroprotection in arterial hypertension and type 2 diabetes mellitus].

Based on results of large-scale controlled trials of irbesartan (I), valsartan (V) and amlodipine (A) (PRIME and MARVAL) we carried out the Markov s modeling of their pharmacoeconomic parameters in arterial hypertension (AH) combined with diabetes mellitus type 2 (DM 2) and microalbuminuria (MAU) projected for 8-years perspective. Cost and efficacy was evaluated taking into account years of life gained and outcomes of concomitant diseases and complications. Indexes of cost/efficacy (C/E) were calculated for each drug. Among investigated drugs I appeared to be the most economic at the account of retardation of development of terminal nephropathy and cardiovascular diseases. The use of I compared with V could save 565300 rub/100 patients/year. C/E of I was 26.5 and 37.4% lower that those of V and A, respectively. Costs of year of life saved was 12716, 16432, and 18325 for I, V, and A, respectively. Comparative pharmacoeconomic modeling of 8-year economic perspectives of I, V and A demonstrated financial benefits of I.

[Original drugs or generics: how to choose?].

The paper elwcidates the issue of interchangeability of original and generic preparations. Based on the analysis of the current literature, the authors claim that the trials which are conducted at the state registration of medical preparations to confirm the pharmacokinetic parameters do not always testify to the similarity of therapeutic effects of original preparations and generics. The choice of antiepileptic drugs remains an important issue due to the wide prevalence of the disease, the need for the long-term therapy and the narrow therapeutic index of basic preparations. The results presented in the paper suggest an extremely cautious approach to the use of generic drugs in the treatment of epilepsy because of the possible destabilization of disease course. The authors conclude that there is a need for creation of a database on interchangeability of original and generic preparations that will be available to the broad medical community.

[Medicamentous test for the screening of pharmacogenic risk of aminoglycoside ototoxicity].

The primary objective of this work was to assess the informative value (sensitivity and specificity) of the diagnostic screening of subjects at high risk of aminoglycoside ototoxicity. The method is based on the vegetative resonance test. It is argued that this test meets the requirements to diagnostic screening procedures and allows for the evaluation of susceptibility to aminoglycosides from such phenotypic trait as responsiveness to resonance between oscillations of aminoglycosides and elongated cells in neuroepithelium of the acoustic analyzer. Sensitivity and specificity of the test was estimated to be 87 and 94% respectively using the "nerve and cochlear duct" organopreparation and the parameter of "acquired toxic information".

[Clinical and pharmacoeconomic peculiarities of the treatment with cerebrolysin in the period of rehabilitation of is ischemic stroke.].

The results of the clinical and pharmacoeconomic study of cerebrolysin in the rehabilitative therapy of ischemic stroke presented in the paper revealed the statistically significant regress of neurological disturbances in patients receiving cerebrolysin in daily dosages of 10 and 20 ml as compared to the control group. The rehabilitation of motor functions was more rapid than sensitive ones in patients receiving cerebrolysin comparing to those switched to the basic antihypertensive and antiaggregate therapy. The positive dynamics of speech rehabilitation was observed, the regress of aphatic disturbances being more significant for daily dosage of 20 ml. Rehabilitation rate in the period of treatment with cerebrolysin was higher for daily dosage of 20 ml than that of 10 ml. A prolonged effect of the drug during the long period after its withdrawal was found that resulted in higher rates of rehabilitation to the 11th week in patients receiving cerebrolysin as compared to the control group. Average total cost of direct medical expenses per a patient estimated in the pharmacoeconomic analysis for the groups receiving cerebrolysin and the control group was higher in the former groups, in particular in that with 20 ml dosage of cerebrolysin. A cost-efficacy analysis revealed that the cost of cerebrolysin treatment per effective unit (a cost of one score on the Lindmark scale and the Barthel scale) was less or comparable in patients receiving cerebrolysin comparing to the control group. The study suggests clinical and pharmacoeconomic expediency of cerebrolysin treatment in rehabilitative period of ischemic stroke.

[Ivabradine--the first selective and specific I(f) inhibitor, novel preparation for treatment of stable angina].

Results of large epidemiological studies allowed to establish that heart rate (HR) is an independent risk factor, elevating rates of total, cardiovascular and sudden mortality. Ivabradine bounds specifically with f channels of sinus node cells providing HR lowering. In experiments with the use of the method of registration of transmembrane currents in cells of sinoatrial node it was revealed that Ivabradine blocks f-channels in a dose-dependent manner. Due to specific action on sinus node and selective suppression of I(f)-currents ivabradine causes dose dependent decrease of HR both at rest and maximal physical exercise without changes of mean blood pressure. It was shown in 3 large clinical studies that Ivabradine together with favorable tolerability profile possesses pronounced antianginal and anti-ischemic efficacy which is at least the same as efficacy of currently available drugs for the treatment of angina beta-adrenoblockers and calcium antagonists. Firstly this confirms clinical significance of concept of specific and selective inhibition of I(f) ionic current in the treatment of patients with ischemic heart disease and stable angina. Secondly this allows to consider the preparation as alternative to available antianginal drugs in case of the presence of contraindications to them or development of side effects at the background of standard therapy.

[Hypotensive, organoprotective, and metabolic effects of Angiotensin converting enzyme inhibitor moexipril in women with postmenopausal syndrome].

Hypotensive, organoprotective, and metabolic effects of angiotensin converting enzyme inhibitor moexipril (7.5-15 mg/day for 16 weeks) with or without combination with hydrochlorothiazide was studied in 34 women (mean age 59.6+/-1.6 years) with postmenopausal metabolic syndrome and hypertension. Thirty four women had dyslipidemia, 22 -- disturbances of carbohydrate metabolism, 18 -- obesity (mean body mass index 31.1+/-0.8 kg/m(2)). Treatment was associated with lowering of office systolic(-20.1%) and diastolic (-17.4%) blood pressure (BP). Target BP (140/90 mm Hg) was achieved in 27 patients. There also occurred significant lowering of mean 24 hour, diurnal, and nocturnal systolic and diastolic BP (p<0.05), significant changes of values of systolic and diastolic BP time indexes, normalization of which was observed both during day and night hours. Significant lowering of total cholesterol (-11.6%, p<0.05), low density lipoprotein cholesterol (-16.3%, p<0.02), and in patients with obesity of triglycerides (-27%, p<0.02) was revealed at the background of treatment with moexipril. In a group as a whole we observed significant lowering of excretion of albumins and b2-microglobulin; most pronounced antiproteinuretic effect was noted in patients with high microproteinuria and obesity. Vasodilating function of vessels improved in all patients with postmenopausal metabolic syndrome, mainly at the account of increment of endothelium dependent vasodilation and normalization of index of vasodilatation.

[Comparative efficacy and safety of contemporary Angiotensin converting enzyme inhibitors moexipril and spirapril in women with postmenopausal metabolic syndrome].

Moexipril (7.4-15 mg/day) was given to 34, spirapril (3-6 mg/day) -- to 18 postmenopausal women with hypertension and metabolic syndrome for 16 weeks. Hydrochlorthiazide was added when therapy was not sufficiently effective. Both angiotensin converting enzyme inhibitors had similar hypotensive activity: blood pressure normalized in 71 and 61% of moexipril and spirapril treated women, respectively. Both drugs promoted normalization of metabolism of lipid (lowering of levels of cholesterol, atherogenic lipoproteins and triglycerides) and carbohydrates (lowering of hyperinsulinemia). Patients with postmenopausal metabolic syndrome had elevation of leptin level up to 27.5+/-5.5 pg/ml. Moexipril and spirapril caused lowering of elevated levels of leptin. These drugs did not affect levels of sex hormones. They exerted vasoprotective (normalization of endothelium dependent and independent vasodilatation) and nephroprotective (attenuation and normalization of microalbuminuria) effects. Thus spirapril and moexipril are effective in treatment of hypertension in patients with postmenopausal metabolic syndrome.

[An X-rays study of the cervical part of spinal cord for detection of atherosclerosis of carotid and vertebral arteries].

The paper is intended for neurologists and radiologists and addresses a problem of accurate and scrupulous assessment of soft cervical tissues. The most distinct changes of infiltrations, which vary by the form and intensity, were detected in the projection of the extracranial segments of the carotid and/or vertebral arteries on the X-ray- and spondylograms of the cervical part. The presence of calcium deposits found in 13% out of 300 patients over 55 years of age was confirmed by the duplex study of the great brain arteries. A simple and logic algorithm of diagnosis of carotid arteries atherosclerosis, working in accordance to from-the-simple-to-the-complex principle, was suggested. It includes scrupulous clinical examination - palpation, auscultation followed by assessment of the soft cervical tissues on cervical X-ray-and spondylogram and finally, if necessary, duplex and/or CT-MRI in "vascular regime".

[Moexipril influence on quality of life in postmenopausal women with arterial hypertension].

AIM: To evaluate a hypotensive effect and metabolic neutrality and safety of ACE inhibitor moexipril in postmenopausal women with arterial hypertension (AH), influence on quality of life. MATERIAL AND METHODS: Thirty two hypertensive postmenopausal women (age 63.1 +/- 0.8 years) received moexipril for 4 months. The history of AH was 10.4 +/- 2.3 years, on the average. After a free of drugs week moexipril was given in a dose 7.5 mg/day with titration to 15 mg in 2 weeks and addition (if the target pressure was not achieved) of hydrochlorothiaside in a dose 12.5 mg. The examination included 24-h monitoring of blood pressure, estimation of microalbuminuria (MAU), endothelial function and blood biochemistry. Initially and after 4 weeks of the treatment quality of life was assessed (scales SF-36 and EuroQol). RESULTS: The initial level of office BP was 164.33/94.50 mm Hg, in 3 months a target level was achieved (136/84 mm Hg). It persisted for the next month. Moexipril corrected endothelial function and vascular elasticity in all the patients. MAU fell from 28.28 to 8.10 mg/l. Quality of life improved. Lipid and carbohydrate changes were not registered. CONCLUSION: Moexipril has a hypotensive and nephroprotective effects, improves endothelial function and quality of life in hypertensive postmenopausal women.