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THE DRUG PHYSIOTENS, THE FEATURES OF THE DRUG AND ITS USE IN THE
FIELD OF CARDIOLOGY, IN PATIENTS WITH HEAVY BODY WEIGHT
Axmedov Shamshod Jamshidovich
Faculty of Medicine, International University of Asia, Uzbekistan.
https://doi.org/10.5281/zenodo.15002529
Abstract.
Moxonidine (Fisiotens®) is an antihypertensive drug that selectively interacts
with imidazoline I1-receptors located in the brainstem, resulting in a decrease in sympathetic
activity and blood pressure (BP). Moxonidine (Fisiotens®) has high affinity to imidazoline I1 -
receptors and only slightly binds to central α2 -adrenoreceptors, due to interaction with which
dry mouth and sedative effect are mediated; reduces tissue resistance to insulin. Decrease in
systolic and diastolic BP at a single and prolonged administration of the drug is associated with
a decrease in the pressor action of the sympathetic nervous system on peripheral vessels,
reduction of total peripheral resistance (TPR).
Keywords:
Moxonidine (Fisiotens®), α2 –adrenoreceptors, atherogenic dyslipidemia,
arterial hypertension, metabolic syndrome, imidazoline I1 –receptors, catecholamine.
ПРЕПАРАТ ФИЗИОТЕНЗ, ОСОБЕННОСТИ ПРЕПАРАТА И ЕГО ПРИМЕНЕНИЕ
В ОБЛАСТИ КАРДИОЛОГИИ, У ПАЦИЕНТОВ С БОЛЬШОЙ МАССОЙ ТЕЛА
Аннотация.
Моксонидин (Физиотенз®) — антигипертензивный препарат,
селективно взаимодействующий с имидазолиновыми I1-рецепторами, расположенными в
стволе головного мозга, что приводит к снижению симпатической активности и
артериального давления (АД). Моксонидин (Физиотенз®) обладает высоким сродством к
имидазолиновым I1-рецепторам и лишь в незначительной степени связывается с
центральными α2-адренорецепторами, за счет взаимодействия с которыми
опосредуются сухость во рту и седативный эффект; снижает резистентность тканей
к инсулину. Снижение систолического и диастолического АД при однократном и
длительном введении препарата связано с уменьшением прессорного действия
симпатической нервной системы на периферические сосуды, уменьшением общего
периферического сопротивления (ОПС).
Ключевые слова:
Моксонидин (Физиотенз®), α2 –адренорецепторы, атерогенная
дислипидемия, артериальная гипертензия, метаболический синдром, имидазолиновые I1 –
рецепторы, катехоламины.
Metabolic syndrome (MS) as a set of metabolic disorders and associated pathological
manifestations (atherogenic dyslipidemia, insulin resistance, hypersympathicotonia, arterial
hypertension, abdominal obesity, endothelial dysfunction, increased blood coagulation
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properties) are recognised as risk factors for the development of atherosclerotic diseases and
cardiovascular mortality [1, 2]. The prevalence of MS in the adult population reaches 23-24%,
and at the age of up to 49 years it is more often detected in men, and at the age of over 70 years -
in women [3, 4]. These observations gave grounds to consider, along with other factors, the role
of menopause in the development of MS. menopause in the development of MS. In 1997
menopausal metabolic syndrome (MMS) was singled out. metabolic syndrome (MMS) as a type
of MS, the development of which is based on estrogen deficiency [5, 6].
The aim of the study:
-to study the effect of long-term use of moxonidine (Physiotez) on arterial hypertension,
lipid and carbohydrate metabolism, autonomic dysfunction, psychoemotional status - on risk
factors of atherosclerotic diseases in women with MS. The results of observation of 32 women
aged from 45 to 68 years (58.3.3 years) were analysed. 45 to 68 years (58.3±2.3 years), suffering
from mild and moderate arterial hypertension (AH) stage II in combination with MMC. The
mean duration of AH was 8.2±1.4 years. All women had manifestations of menopausal
syndrome. Prior to the study, the patients did not receive hypotensive drugs for a week,
anthropometric measurements, clinical examination, office BP determination (according to
Korotkov) were performed. BP determination (according to Korotkov), electrocardiography,
bicycle ergometry, biochemical tests: total cholesterol (TC), high-density lipid cholesterol
(HDL) and low-density lipid cholesterol (HDL), triglycerides, fasting and post-exercise blood
glucose. fasting blood glucose and after a 75 g glucose load [8]. The Weyl index was used to
assess the state of the autonomic nervous system. The severity of menopausal syndrome (MS)
was determined by the Kupperman index based on the vasomotor and general reactions (the
number of ‘hot flashes’, their severity, sweating, etc.).
Our observations have shown a good hypotensive effect of M, that is consistent with the
data of other studies conducted both in women with estrogen deficiency [9,10] and in mixed
groups where the hormonal factor was not taken into account [11-15] . The mechanism of
hypotension is associated with a decrease in sympathoadrenal hyperactivity, secretion of
catecholamines, renin, aldosterone, and a decrease in peripheral arterial tone [6, 16]. The
efficacy of M in the treatment of AH is comparable to that of modern first-line antihypertensive
drugs (IAPP, beta-adrenoreceptor blockers and calcium channel blockers) [18, 19], regardless of
the level of estrogenic activity.
At the same time, positive dynamics of the general condition of women was observed
during M treatment. Along with normalisation of BP and disappearance of clinical
manifestations of hypertension, the severity of menopausal syndrome decreased significantly: the
frequency of ‘hot flashes’, intensity of sweating, headache, cardialgia stopped, psychoemotional
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status improved. The number of women with mild course of CS increased from 10 to 21 (at the
expense of more severe forms), Kupperman index decreased from 33.8±1.2 to 22.4±1.1
(P<0.05). The manifestations of autonomic dysfunction decreased - Weyl index decreased from
43.3±2.2 to 26.1±0.9 (P<0.05).
The quality of life’ improved by 1.28 points (P<0.05). The favourable effect of M on the
course of menopause, general condition, emotional sphere and standard of living of patients
deserves special attention, which allows to give preference to imidazoline receptor agonists when
building a treatment programme for menopausal women to achieve a better result.
Conclusions
Moxonidine has provided a vector for speculation about the possible link between
hypertension, overweight and stress. My personal experience of using the drug shows that I have
no objections to the hypotensive effect of moxonidine, the dose of 0.2 mg is rarely used, I
prescribe immediately 0.4-0.6mg/day. Studies indicate the benefits of moxonidine in the
treatment of AH in overweight. In our national guidelines from the WNOC, 2004, the
moxonidine class is indicated for the treatment of AH in MS and diabetes mellitus (DM). In the
recommendations of the European Society of Hypertension ESH, 2003, as recommendations for
the therapy of patients with RAS hyperactivity, MS and DM (called the most rational
combinations of two or more hypotensive drugs).
- The imidazoline receptor agonist moxonidine (Fisiotenz) in the 6-month treatment of
menopausal women with metabolic syndrome reduces total metabolic syndrome. syndrome
reduces the total risk of cardiovascular diseases due to normalisation of BP (in 81,2% of
patients), positive effect on lipid and carbohydrate metabolism (increase of HDL cholesterol by
15%, decrease of glycaemia in 2 hours after glucose load by 17,48%), reduction of autonomic
dysfunction.
- Moxonidine (Physiotensis) favourably affects the course of menopausal syndrome,
improves the quality of life of patients.
- In the course of long-term treatment moxonidine (Physiotenz) is well well tolerated by
84.4% and satisfactory - 15.6% of patients.
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