Aim. To evaluate the clinical efficacy and safety of the selective imidazoline I1-receptor agonist moxonidine versus the angiotensin-converting enzyme inhibitor captopril in patients with uncomplicated hypertensive crisis (UHC). Subjects and methods. Two hundred and twenty-five patients (125 women, 100 men) aged 56,2±14,4 years with UHC were examined. The patients were randomized to a group of once-daily 0.4 mg moxonidine orally (n=113) and a group of once-daily 25 mg captopril (n=112). Dynamic measurements of blood pressure (BP) and heart rate, electrocardiogram recording, and determinations of blood creatinine, potassium, and glucose levels were made along with general clinical examination. The efficacy indices in patients were time to the onset of antihypertensive action, degree of BP lowering, and duration of antihypertensive effect. duration. 24-hour BP monitoring was used to evaluate the efficacy of the drugs compared. The time course of changes in the parameters was analyzed for 12 hours. Results. Both groups achieved an antihypertensive effect as a significant reduction in systolic and diastolic BP 30 and 60 min after therapy initiation, respectively; at the same time BP decreases did not exceed 25% of the baseline levels. Moxonidine was found to be more effective mainly in the duration of its antihypertensive effect with a steady BP decline throughout the follow-up. There was evidence that moxonidine exerted a positive metabolic effect, particularly in significantly reducing blood creatinine levels. In the moxonidine group, the patients with above satisfactory efficacy were 26,9% significantly more and those with above satisfactory tolerance were 18,8% more. Conclusion. The findings suggest that moxonidine versus captopril is highly effective and well tolerated in patients with UHC. The drug may be successfully used to treat UHC, starting in the prehospital period, especially in patients with concomitant diseases (diabetes mellitus, metabolic syndrome, chronic renal failure).

Aim. Investigation of comparative dissolution kinetics of generic medicinal products containing moxonidine versus reference drug. Material and methods. Objects of the research were film-coated tablets containing moxonidine (INN) in a dose 0.4 mg: a reference drug Physiotens® and 4 generic drugs. In vitro dissolution test of moxonidine from the study drugs was performed using comparative dissolution kinetics test (CDKT). The CDKT was performed in the media with the following pH: 1.2 (1:9 mixture of 0.1 M hydrochloric acid and water), 4.5 (acetate buffer solution, prepared as per State Pharmacopoeia, XIII), and 6.8 (phosphate buffer solution, prepared as per State Pharmacopoeia, XIII). The sampling for dissolved moxonidine was performed 5, 10, 15, 20, and 30 min after the test was started. An high performance liquid chromatography method with ultraviolet detection at 220 nm was used to assay. Results. Within 15 min more that 85% of moxonidine dissolved from the reference drug and all study drugs at pH 1.2; dissolution profiles were similar without calculation of similarity factor f2. Similarly, at pH 4.5 dissolution profiles of study drugs #2 and #3 were similar to that of the reference drug, and the similarity factor f2 was not calculated. However, in case of study drugs #1 and #4 significant differences were observed at a single time point (15 min), which suggests that their dissolution profiles are non-similar to that of the reference drug. Similarity factors f2 were calculated 17.52 and 35.30, respectively (less than 50). At pH 6.8 similarity factors f2 for all study generic drugs were also less than 50 (23.8, 49.8, 38.6, and 35.9), so their dissolution curves were non-similar to that of reference drug. Conclusion. In our study we observed difference in release in vitro of medicinal products containing moxonidines: none of the study drugs was fully similar to the reference drug in all media. The differences observed at pH 6.8 were noteworthy, where the samples had or faster kinetics (study drugs #2 and #3), or slower dissolution kinetics (test drugs #1 and #4). Observed differences in moxonidine release rate may impact absorption of active pharmaceutical ingredient into the blood following drug administration.

This article presents the results of the clinical and statistical evaluation of the calls of patients with atrial fibrillation (AF) by the data of the emergency medical service in Moscow. Ambulance teams was performed a voluntary questionnaire survey of 5003 patients with AF. There were 17% of emergency calls for heart rhythm disturbances from the total number of cardiovascular diseases and 88% of these arrhythmias was AF. A clear trend was observed in the prevalence of AF in men of working age and in women in the older age group. Among the respondents prevails paroxysmal form of AF in 70.1% of cases. The average score on the risk scale of thromboembolic complications in patients with atrial fibrillation/flutter CHA2DS2-VASc was 3.56±1.71. The average score on the scale of risk assessment of ischemic stroke in patients with nonrheumatic atrial fibrillation/flutter CHADS2 was 1.85±1.13. The number of patients with a score of two or more on both scales was 87.7% and 59.3% respectively. 28% of patients with AF asked for medical help at least 48 hours after the onset of the paroxysm. Regular observation by a cardiologist is carried out in 50.5% of cases, by a therapist in 62.8%, jointly by a therapist and a cardiologist in 45% respectively. Continuous oral anticoagulant therapy is performed in 29.8% of patients with AF. The percentage of medical evacuations of patients with AF increased from 23.8% in 2015 to 27.1% in 2016. The study showed that regular clinical and statistical analysis of the effectiveness of medical care for patients with AF at all stages of medical surveillance is necessary.

The paper reviews the clinical practice potential of a combined action antihypertensive medication urapidil for the treatment of patients with acute elevation of blood pressure (BP) and confirms urapidil effectiveness and good tolerability. Urapidil action mechanisms, pharmacodynamics, and pharmacokinetics are discussed, together with the results of the key clinical trials which have demonstrated antihypertensive effectiveness and safety of this agent. Additional beneficial effects of urapidil, such as reduction of the increased pulmonary artery BP and improvement of bronchial conductivity, are also described.

Обсуждают результаты экспериментальных и клинических исследований, посвященных препарату урапидил, совмещающему центральный антигипертензивный эффект с периферической вазодилатацией. Отражены области применения, подчеркнута хорошая переносимость и безопасность препарата. Подробно изложены способы применения урапидила при различных клинических ситуациях, сопровождающихся острым повышением артериального давления.