Instruction for use: Moxarel

Dosage form: film-coated tablets

Active substance: Moxonidinum

ATX

C02AC05 Moxonidine

Pharmacological group

Hypotensive central agent [I1-imidazoline receptor agonists]

Nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

Composition

Tablets covered with a film coating.

active substance: Moxonidine 0.2 mg; 0.3 mg; 0.4 mg

Auxiliary substances: lactose monohydrate - 64/64/64 mg; MCC - 29.8 / 29.7 / 29.6 mg; Silicon dioxide colloid - 1/1/1 mg; Povidone K30 - 2/2/2 mg; Croscarmellose sodium - 2/2/2 mg; Magnesium stearate - 1/1/1 mg

Membrane film: hypromellose - 1,8 / 1,8 / 1,8 mg; Talc - 0.6 / 0.6 / 0.6 mg; Titanium dioxide - 0.33 / 0.31 / 0.31 mg; Macrogol 4000 (polyethylene glycol 4000) - 0.27 / 0.27 / 0.27 mg; Iron oxide red (iron oxide) - 0 / 0.02 / 0 mg; Iron oxide yellow (iron oxide) - 0/0 / 0.02 mg or dry mixture for film coating (hypromellose 60/60/60%, talc 20/20/20%, titanium dioxide 11 / 10.33 / 10.33%, macrogol 4000 (polyethylene glycol 4000) 9/9/9%, iron oxide red (iron oxide) 0 / 0.67 / 0%, iron oxide yellow 0/0 / 0.67% 3/3/3 mg

Description of dosage form

Tablets, 0.2 mg: round, biconcave, film-coated white or almost white.

Tablets, 0.3 mg: round, biconvex, covered with a film coat of pink color.

Tablets, 0,4 mg: round, biconcave, film-coated yellow.

On the cross-section - the core is white or almost white.

Pharmachologic effect

Mode of action - hypotensive.

Pharmacodynamics

Moxonidine is an antihypertensive drug with a central mechanism of action. In stem brain structures (the rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors that participate 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 sympatholytic antihypertensive agents with a lower affinity for α2-adrenergic receptors, which explains the lower probability of developing a sedative effect and dryness of the oral mucosa.

The use of moxonidine leads to a decrease in systemic vascular resistance and blood pressure.

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

Pharmacokinetics

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

Distribution. The connection with plasma proteins is 7.2%.

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

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

Special patient groups

Patients of advanced age. Clinically insignificant changes in pharmacokinetic parameters of moxonidine in elderly patients, probably caused by a decrease in the intensity of its metabolism and / or slightly higher bioavailability, were noted.

Children. Moxonidine is not recommended for use in patients younger than 18 years of age, and therefore pharmacokinetic studies have not been conducted in this group.

Impaired renal function. The excretion of moxonidine is largely correlated with the clearance of creatinine. In patients with moderate renal insufficiency (Cl creatinine 30-60 ml / min) Css in plasma and final T1 / 2 are approximately 2 and 1.5 times higher than in patients with normal renal function (Cl creatinine more than 90 ml / min ). In patients with severe renal failure (Cl creatinine less than 30 ml / min), Css in the blood plasma and the final T1 / 2 is 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine leads to predictable cumulation in patients with moderate and severe renal insufficiency. In patients with terminal renal failure (Cl creatinine less than 10 ml / min) on hemodialysis, Css in plasma and final T1 / 2, respectively, are 6 and 4 times higher than in patients with normal renal function.

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

Indications of Moxarel

Arterial hypertension.

Contraindications

Hypersensitivity to the active substance, other components of the drug;

Severe heart rhythm disturbances;

Syndrome of weakness of the sinus node;

AV blockade II and III degree;

Pronounced bradycardia (heart rate less than 50 beats per minute);

Acute and chronic heart failure (NYHA class III-IV functional class);

Simultaneous use with tricyclic antidepressants (see "Interaction");

Severe renal failure (Cl creatinine less than 30 mL / min), including patients on hemodialysis;

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

The period of breastfeeding;

Patients older than 75 years;

Age to 18 years (efficacy and safety of moxonidine not established).

With caution: impaired renal function (Cl creatinine more than 30 mL / min); Severe hepatic insufficiency (more than 9 points according to the Child-Pugh classification); AV-blockade of the 1st degree; Severe coronary artery disease; Severe ischemic heart disease or unstable angina (experience with use is inadequate); Chronic heart failure.

Application in pregnancy and lactation

Clinical data on the treatment of pregnant women with Moxarel® are not available.

Prescribe Moxarel® to pregnant women with caution only after a thorough assessment of the risk-benefit ratio, when the benefit to the mother exceeds the potential risk to the fetus.

Moxonidine penetrates into breast milk. Breastfeeding women during the period of treatment are recommended to stop breastfeeding or to cancel the drug.

Side effects

The incidence of side effects described below was determined according to the following: very often - not less than 10%; Often - not less than 1%, but less than 10%; Infrequently - not less than 0,1%, but less than 1%; Rarely - not less than 0.01%, but less than 0.1%; Very rarely - less than 0.01% (including isolated cases).

From the side of the central nervous system: often - headache, dizziness (vertigo), drowsiness; Infrequently - a syncope.

From the CVS: infrequent - a marked decrease in blood pressure, orthostatic hypotension, bradycardia.

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

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

Mental disorders: often - insomnia; Infrequently - nervousness.

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

From the musculoskeletal and connective tissue: often - pain in the back; Infrequently - pain in the neck.

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

Interaction

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

Tricyclic antidepressants can reduce the effectiveness of antihypertensive agents of central action, and therefore it is not recommended that they be taken together with moxonidine.

Moxonidine can enhance the effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.

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

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

Simultaneous use of moxonidine with β-adrenoblockers leads to increased bradycardia, severity of foreign and dromotropic effects.

When moxonidine is administered together with moclobemide, pharmacodynamic interaction is absent. Moxonidine is excreted by tubular secretion, so its interaction with other drugs released by tubular secretion is not excluded.

Dosing and Administration

Inside, regardless of food intake.

In most cases, the initial dose of Moxarel® is 0.2 mg / day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 divided doses, is 0.6 mg. The initial dose for patients with moderate or severe renal failure, 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, dizziness, fatigue, asthenia, bradycardia, dryness of the oral mucosa, vomiting and pain in the epigastric region, respiratory depression, impaired consciousness. Potential short-term increases in blood pressure, tachycardia, and hyperglycemia are also possible.

Treatment: a specific antidote of the drug does not exist. In the case of a marked decrease in blood pressure, it is recommended that a fluid be added to restore bcc and dopamine. Bradycardia can be stopped with atropine. Α-adrenoreceptor antagonists can reduce or eliminate paradoxical hypertensive effects in overdose of moxonidine. In severe cases of overdose, it is recommended to carefully monitor the disturbance of consciousness and not to allow respiratory depression. Moxonidine is slightly excreted in hemodialysis.

Special instructions

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

If it is necessary to cancel simultaneously taken β-blockers and the drug Moxarel®, first abolish β-blockers and only after a few days moxonidine.

During treatment, regular monitoring of blood pressure, heart rate and ECG registration is necessary. Stop taking Moxarel® gradually.

During treatment with Moxarel®, alcohol should be avoided.

Influence on the ability to drive vehicles and work with machinery. The effect of the preparation Moxarel® on the ability to drive vehicles or control technology was not studied. However, taking into account the possible occurrence of dizziness and drowsiness, patients should be careful when dealing with potentially hazardous activities requiring increased attention, such as driving vehicles or controlling equipment.

Release Form

Tablets, film-coated, 0.2 mg, 0.3 mg or 0.4 mg. In contour acrylic packing from a film of PVC and aluminum foil, 10, 14, 15 or 30 pcs. 1, 2 or 3 contour cell packs according to 10 tablets, 1, 2 or 4 contour cell packs of 14 tables, 1, 2 or 4 contour cell packs of 15 tablets, 1 or 2 contourcell packs of 30 tablets. In a pack of cardboard.

Manufacturer by

ZAO VERTEX, Russia.

Conditions of supply of pharmacies

On prescription.

Storage conditions of the drug Moxarel

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

The shelf life of the drug Moxarel

3 years.

Do not use beyond the expiration date printed on the package.