Moxarel, pills 0.2mg, 30pcs

Composition

Active ingredient:

moxonidine;

Auxiliary substances:

lactose monohydrate;

MCC;

colloidal silicon dioxide;

povidone K 30;

croscarmellose sodium;

magnesium stearate.

Pharmacological action

Pharmacodynamics

Moxonidine is an antihypertensive agent with a central mechanism of action. In the brain stem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors involved in tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure.

Moxonidine differs from other adrenergic antihypertensive agents by a lower affinity for α1-adrenergic receptors, which explains the lower probability of developing sedation and dryness of the oral mucosa.

Taking moxonidine leads to a decrease in systemic vascular resistance and blood pressure.

Moxonidine improves the insulin sensitivity index in patients with obesity, insulin resistance and moderate arterial hypertension.

Pharmacokinetics

Suction. After oral use, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. Tmax — about 1 h. Food intake does not affect the pharmacokinetics of the drug.

Distribution. The binding to plasma proteins is 7.2%.

Metabolism. The main metabolite is dehydrogenated moxonidine. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared to moxonidine.

Output. T1 / 2 of moxonidine and the metabolite is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% in unchanged form and 13% in the form of dehydromoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestine.

Special patient groups

Elderly patients. Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients were noted, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability.

Children. Moxonidine is not recommended for use in patients younger than 18 years of age, and therefore no pharmacokinetic studies have been conducted in this group.

Impaired renal function. Moxonidine clearance is strongly correlated with creatinine clearance. In patients with moderate renal insufficiency (creatinine clearance 30-60 ml / min) Plasma Css and final T1 / 2 are approximately 2 and 1.5 times higher than in patients with normal renal function (creatinine clearance greater than 90 ml / min). In patients with severe renal insufficiency (creatinine clearance less than 30 ml / min) Css in blood plasma and final T1 / 2 is 3 times higher than in patients with normal renal function. use of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate to severe renal insufficiency. In patients with end-stage renal insufficiency (creatinine clearance less than 10 ml/min) on hemodialysis, Css in blood plasma and final T1 / 2, respectively, is 6 and 4 times higher than in patients with normal renal function.

In all groups, the maximum concentration of moxonidine in blood plasma is 1.5–2 times higher. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly eliminated during hemodialysis.

Indications

Arterial hypertension.

Contraindications

• severe heart rhythm disturbances;
• the syndrome of weakness of the sinus node and
• AV blockade II and III degree;
• bradycardia (heart rate less than 50 beats/min);
• acute and chronic heart failure (III-IV functional class NYHA classification);
• the simultaneous use of tricyclic antidepressants;
• severe renal insufficiency (CC less than 30 ml/min), including patients on hemodialysis;
• age older than 75 years;
• age to 18 years (efficacy and safety not established moxonidine);
• the period of breastfeeding;
• lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
• hypersensitivity to the Active ingredient, other components of the drug.

With caution

• , impaired renal function (creatinine clearance more than 30 ml / min);
• severe hepatic insufficiency (more than 9 points according to the Child-Pugh classification);
• AV block of the first degree;
• severe coronary vascular diseases;
• severe CHD or unstable angina (insufficient experience);
• chronic heart failure.

Side effects

From the central nervous system:  often — headache, dizziness (vertigo), drowsiness; infrequently-fainting.

From the CCC side:  infrequently — a marked decrease in Blood pressure, orthostatic hypotension, bradycardia.

From the gastrointestinal tract:  very often — dryness of the oral mucosa; often-nausea, diarrhea, vomiting, dyspepsia.

Skin and subcutaneous tissue disorders:  often — skin rash, pruritus; infrequently-angioedema.

Mental disorders:  often — insomnia; infrequently-nervousness.

Hearing disorders and labyrinth disorders:  infrequently-ringing in the ears.

Musculoskeletal and connective tissue disorders:  often-back pain; infrequently-neck pain.

General disorders and disorders at the injection site:  often-asthenia; infrequently-peripheral edema.

Interaction

The combined use of moxonidine with other antihypertensive agents leads to an additive effect.

Tricyclic antidepressants may reduce the effectiveness of central antihypertensive agents, and therefore they are not recommended to be taken together with moxonidine.

Moxonidine may enhance the effects of tricyclic antidepressants, tranquilizers, ethanol, sedatives, and sleeping pills.

Moxonidine is able to moderately improve impaired cognitive function in patients receiving lorazepam.

use of moxonidine together with benzodiazepine derivatives may be accompanied by an increase in the sedative effect of the latter.

Simultaneous use of moxonidine with beta-blockers leads to increased bradycardia, the severity of ino-and dromotropic effects.

When moxonidine is co-administered with moclobemide, there is no pharmacodynamic interaction. Moxonidine is released by tubular secretion, so its interaction with other drugs released by tubular secretion is not excluded.

How to take, course of use and dosage

Inside, regardless of food intake.

In most cases, the initial dose of Moxarel®is indicated. it is 0.2 mg / day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg. The initial dose for patients with moderate or severe renal insufficiency, as well as for patients on hemodialysis, is 0.2 mg / day. If necessary and with good tolerability, the daily dose can be increased to 0.4 mg.

Overdose

Symptoms:

headache, sedation, drowsiness, marked decrease in blood pressure. Blood pressure, dizziness, fatigue, asthenia, bradycardia, dryness of the oral mucosa, vomiting and pain in the epigastric region, respiratory depression, impaired consciousness. Short-term increases are also potentially possible Blood pressure, tachycardia, hyperglycemia.

Treatment:

There is no specific antidote to the drug. In the case of a marked decline use of BCC and dopamine recovery fluids is recommended. Bradycardia can be treated with atropine. Alpha-adrenergic antagonists may reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose. In severe cases of overdose, it is recommended to carefully monitor the disturbance of consciousness and avoid respiratory depression. Moxonidine is slightly eliminated during hemodialysis.

Special instructions

Currently, there is no evidence that discontinuation of Moxarel® leads to an increase in blood pressure. However, it is not recommended to stop taking Moxarel® Instead, you should gradually reduce the dose of the drug over 2 weeks.

If it is necessary to cancel the simultaneous use of beta-blockers and Moxarel®, first cancel beta-blockers and only after a few days moxonidine.

Regular monitoring is necessary during treatment Blood pressure, heart rate, and ECG recording. Stop taking Moxarel ® gradually.

Alcohol consumption should be excluded during treatment with Moxarel®.

Influence on the ability to drive vehicles and work with mechanisms. Effect of Moxarel® the ability to drive vehicles or operate machinery was not studied. However, taking into account the possible occurrence of dizziness and drowsiness, patients should exercise caution when engaging in potentially dangerous activities that require increased attention, such as driving vehicles or operating machinery.

Form of production

Tablets

Storage conditions

In a dark place, at a temperature not exceeding 25 °C.

Shelf life

3 years

Active ingredient

Moxonidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension