Moxonidine - instructions for use, dose, side effects, contraindications

The drug is a selective agonist I₁-imidazoline receptors, which are located in the ventrolateral region of the medulla oblongata. They are responsible for the reflex and tonic control of the sympathetic nervous system. By stimulating these receptors of the neurons of the solitary tract, moxonidine directly activates the parasympathetic nervous system, as a result of reducing the heart rate, and through a system of inhibitory interneurons promotes inhibition activity vasomotor center and thus - decrease downlink sympatheticeffects on the cardiovascular system. Arterial pressure (systolic and diastolic) decreases gradually. Moxonidine differs from other sympatholytic antihypertensive agents with a lower affinity for α₂adrenoreceptors, which explains the lower probability of sedation and dry mouth.

Pharmacokinetics:

Absorption of the drug is 90%. Absolute bioavailability is approximately 88%. Time to reach C_max - about 1 hour. The intake of food does not affect the pharmacokinetics of moxonidine. The connection with plasma proteins is 7%, metabolized in the liver, excreted by the kidneys, the half-life period is 2-3 hours.

Indications:

Arterial hypertension.

ICD-10

IX.I10-I15.I10 Essential [primary] hypertension

IX.I10-I15.I15 Secondary Hypertension

Contraindications:

Syndrome of weakness of sinus node, hypersensitivity, violation of sinoatrial and atrioventricular conductivity II-III severe cardiac rhythm disturbances, angioedema, history of heart failure, severe liver and kidney disorders, unstable angina, Parkinson's disease, epilepsy,depressive conditions, pregnancy, age 18 years, age over 75, breast-feeding, peripheral circulation disorders, hemodialysis, simultaneous administration with tricyclic antidepressants.

Carefully:

Ischemic heart disease or unstable angina, severe arrhythmias, intermittent claudication, history of angioedema, epilepsy, glaucoma, Raynaud's disease, atrioventricular blockade of I degree, severe cerebrovascular disorders, myocardial infarction, severe coronary artery disease, chronic cardiac insufficiency of I and II functional class.

Pregnancy and lactation:

Category FDA not determined. Adequate and strictly controlled studies of moxonidine safety in pregnancy have not been conducted, so it should be used in this category of patients only if the expected benefit for the mother exceeds the possible risk to the fetus.

Do not use during lactation, because moxonidine excreted in breast milk. If moxonidine is needed during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Orally during or after a meal, with plenty of liquid. The initial dose is 0.2 mg once a day, the maximum daily dose is 0.6 mg (divided into two doses), the maximum single dose is 0.4 mg.

For patients who suffer from kidney failure, a single dose should not exceed 0.2 mg, and a daily dose of 0.4 mg.

Side effects:

From the side of the central nervous system: headache, dizziness (vertigo), drowsiness, increased fatigue; fainting.

From the cardiovascular system: marked reduction in blood pressure, orthostatic hypotension, bradycardia, peripheral edema.

From the digestive system: dry mouth, diarrhea, nausea, vomiting, indigestion.

From the skin and subcutaneous tissues: skin rash, itching; angioedema.

From the side of the psyche: insomnia; nervousness.

From the side of the hearing organ and labyrinthine disorders: infrequent - ringing in the ears.

From the musculoskeletal system: backache; pain in the neck.

On the part of the body as a whole: asthenia; peripheral edema.

Overdose:

Dry mouth, excessive decrease in blood pressure, drowsiness, weakness. Treatment is symptomatic.

Interaction:

Joint use of the drug with antihypertensive drugs (eg, thiazide diuretics, blockers of "slow" calcium channels) leads to an additive effect and an increase in the hypotensive effect.

Tricyclic antidepressants reduce the effectiveness of the drug.

β-Adrenoblockers - increased bradycardia, severity of negative foreign and dromotropic effects. If it is necessary to cancel simultaneously taken β-adrenoblockers and moxonidine, β-blockers are first canceled, and in a few days moxonidine.

Anxiolytics, barbiturates, ethanol - Increased oppressive effect on the central nervous system.

Lorazepam - in patients receiving lorazepam and moxonidine, a slight improvement in weakened cognitive functions is possible.

Benzodiazepine derivatives - increased sedative effect with simultaneous administration with moxonidine.

Special instructions:

At the time of taking the drug, it is necessary to control blood pressure, electrocardiograms and heart rate.

The withdrawal of the drug should be gradual.

Impact on the ability to drive vehicles and manage mechanisms

Taking into account the possible occurrence of drowsiness and dizziness, during the treatment patients should be careful when it is necessary to engage in potentially dangerous activities that require concentration of attention and high speed of psychomotor reactions.

Instructions

Moxonidine (Moxonidinum)