Description
Moxarel Pharmacodynamics
Moxonidine is a hypotensive agent, the action of which is associated with the influence on the central mechanisms of regulation of the activity of the sympathetic nervous system and blood pressure. In brain stem structures (rostral layer of lateral ventricles) moxonidine selectively stimulates imidazoline-sensitive receptors involved in tonic and reflex regulation of sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP).
Moxonidine differs from other sympatholytic hypotensive agents by its lower affinity for ?2-adrenoreceptors, which explains the lower probability of development of sedative effect and dry mouth when using it.
Administration of moxonidine is accompanied by a decrease in systemic vascular resistance and BP. The hypotensive effect of moxonidine has been confirmed in double-blind placebo-controlled randomized trials.
The results of a clinical study involving 42 patients with arterial hypertension and left ventricular hypertrophy (LVH) demonstrated that with a similar reduction in blood pressure, the combination of angiotensin II receptor antagonists with moxonidine reduces LVH to a greater extent than the combination of a thiazide diuretic and a calcium channel blocker (15% versus 11%; p < 0.5).
Moxonidine improves insulin sensitivity index by 21% (compared with placebo) in patients with obesity, insulin resistance, and moderate arterial hypertension.
Indications
Arterial hypertension.
Contraindications
-Hypersensitivity to moxonidine, other components of the drug;
-angioneurotic edema in anamnesis;
-Sinus node weakness syndrome or sinoatrial block;
-Severe hepatic insufficiency;
-Trioventricular block of II and III degree;
-Severe bradycardia (resting heart rate (HR) less than 50 bpm);
-acute and chronic heart failure (functional class III-IV according to NYHA classification);
-Severe renal insufficiency;
-Under 18 years of age (the efficacy and safety of moxonidine have not been established);
-Period of breastfeeding;
-Hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Dosage and administration
- Orally, regardless of meals.
- In most cases, the initial dose of Moxarel® is 0.2 mg per day. Maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 intakes, is 0.6 mg.
- Individual correction of daily dose is necessary depending on patient’s tolerance to the therapy.
- No dose adjustment is required for patients with hepatic insufficiency.
- The initial dose for patients on hemodialysis is 0.2 mg/day. In case of necessity and good tolerability the daily dose may be increased up to maximum 0.4 mg per day.
- In patients with renal insufficiency, a cautious selection of the dose is recommended, especially at the beginning of treatment. The initial dose should be 0.2 mg per day. If necessary and in case of good tolerability, daily dose of this medicine can be increased up to maximum 0.4 mg for patients with moderate renal insufficiency (CKD more than 30 ml/min, but less than 60 ml/min) and 0.3 mg for patients with severe renal insufficiency (CKD less than 30 ml/min).
