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

Excipients: lactose monohydrate - 64.00 mg, cellulose microcrystalline - 29.80 mg, silicon dioxide colloidal - 1.00 mg, povidone K-30 - 2.00 mg, croscarmellose sodium - 2.00 mg, magnesium stearate - 1.00 mg.

Film Sheath: [hypromellose 1.80 mg, talc 0.60 mg, titanium dioxide 0.33 mg, macrogol 4000 (polyethylene glycol 4000) 0.27 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 3.00 mg.

Dosage of 0.3 mg

Active substance: moxonidine 0.30 mg.

Excipients: lactose monohydrate - 64.00 mg, cellulose microcrystalline - 29.70 mg, silicon dioxide colloidal - 1.00 mg, povidone K-30 - 2.00 mg, croscarmellose sodium - 2.00 mg, magnesium stearate - 1.00 mg.

Film Sheath: [hypromellose 1.80 mg, talc 0.60 mg, titanium dioxide 0.31 mg, macrogol 4000 (polyethylene glycol 4000) 0.27 mg, iron oxide red (iron oxide) 0.02 mg] or [ dry film-coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (10.33%), macrogol 4000 (polyethylene glycol 4000) (9%), iron oxide red (iron oxide) (0.67 %)] - 3.00 mg.

Dosage 0.4 mg

Active substance: moxonidine - 0.40 mg.

Excipients: lactose monohydrate - 64.00 mg, cellulose microcrystalline - 29,60 mg, silicon dioxide colloidal - 1.00 mg, povidone K-30 - 2.00 mg, croscarmellose sodium - 2.00 mg, magnesium stearate - 1.00 mg.

Film Sheath: [hypromellose 1.80 mg, talc 0.60 mg, titanium dioxide 0.31 mg, macrogol 4000 (polyethylene glycol 4000) 0.27 mg, iron oxide yellow (iron oxide) 0.02 mg] or [ dry film-coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (10.33%), macrogol 4000 (polyethylene glycol 4000) (9%), iron oxide yellow (iron oxide) (0.67 %)] - 3.00 mg.

Description:

Round, biconvex tablets, covered with a film shell of white or almost white color (dosage of 0.2 mg), Pink colour (dosage of 0.3 mg) or yellow (dosage of 0.4 mg).

On the cross section, the nucleus is white or almost white in color.

Pharmacotherapeutic group:Hypotensive central agent

ATX: & nbsp

C.02.A.C.05 Moxonidine

Pharmacodynamics:

Moxonidine is an antihypertensive drug with a central mechanism of action. In the stem structures of the brain (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 arterial pressure (BP).

Moxonidine differs from other sympatholytic gypsumotensile means with a lower affinity for α₂-adrenoceptors, which explains the lower probability of developing a sedative effect and dryness of the oral mucosa.

The administration of 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 degree of hypertension.

Pharmacokinetics:

Suction

After oral administration moxonidine quickly and almost completely absorbed in the upper parts of the gastrointestinal tract. Absolute bioavailability is approximately 88%. The time to reach the maximum concentration is about 1 hour. Eating does not affect the pharmacokinetics of the drug.

Distribution

The connection with plasma proteins is 7.2%.

Metabolism

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

Excretion

The half-life (T_1/2) of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% in the form of dehydroximexidine, while other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestine.

Pharmacokinetics in elderly patients

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

Pharmacokinetics in 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.

Pharmacokinetics in renal failure

The excretion of moxonidine is largely correlated with the clearance of creatinine (CC). In patients with moderate renal insufficiency (CK in the range of 30-60 ml / min), equilibrium concentrations in the blood plasma and the final T_1/2approximately 2 and 1.5 times higher than in patients with normal renal function (CC greater than 90 ml / min).

In patients with severe renal failure (CC less than 30 ml / min), equilibrium concentrations in the blood plasma and final T_1/2 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 (CC less than 10 ml / min) on hemodialysis, equilibrium plasma concentrations and final T_1/2 respectively, 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:

Arterial hypertension.

Contraindications:

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

- severe cardiac rhythm disturbances;

- syndrome of weakness of the sinus node;

- atrioventricular blockade of II and III degree;

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

- acute and chronic heart failure (III-IV functional class by classification NYHA);

- simultaneous use with tricyclic antidepressants (see section "Interaction with other drugs");

- severe renal failure (QC less than 30 ml / min), including patients on hemodialysis;

- age over 75 years;

- age to 18 years (efficacy and safety of moxonidine not established);

- the period of breastfeeding;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

- Impaired renal function (QC more than 30 ml / min);

- severe hepatic insufficiency (more than 9 points according to the Child-Pugh classification);

- atrioventricular blockade of the 1st degree;

- severe coronary artery disease;

- severe ischemic heart disease or unstable angina (experience with use is insufficient);

- chronic heart failure.

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.

Dosing and Administration:

Inside, regardless of food intake.

In most cases, the initial dose of Moxarel® is 0.2 mg per 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.

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 central nervous system:

often - headache, dizziness (vertigo), drowsiness;

infrequently - fainting.

From the side of the cardiovascular system:

infrequently - marked decrease in blood pressure, orthostatic hypotension, bradycardia.

From the gastrointestinal tract:

Often - dryness of the oral mucosa;

often - nausea, diarrhea, vomiting, indigestion.

From the skin and subcutaneous tissues:

often - skin rash, itching;

infrequently - angioedema.

Disorders of the psyche:

often - insomnia;

infrequently - nervousness.

From the side of the hearing organ and labyrinthine disorders:

infrequently - tinnitus.

From the musculoskeletal and connective tissue:

often - backache;

infrequently pain in the neck.

General disorders and disorders at the site of administration:

often - asthenia;

infrequently - peripheral edema.

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

There is no specific antidote. In the case of a marked decrease in blood pressure, it is recommended to administer a fluid to restore the volume of circulating blood and dopamine. Bradycardia can be stopped with atropine. Alpha-adrenoreceptor antagonists can reduce or eliminate paradoxical hypertensive effects in overdose with moxonidine.

In severe cases of overdose, it is recommended to carefully monitor impairment of consciousness and not to allow respiratory depression.

Moxonidine is slightly excreted in hemodialysis.

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 beta-blockers 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.

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® dramatically, instead you should gradually reduce the dose of the drug within two weeks.

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

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

During treatment with Moxarel®, alcohol should be avoided.

Effect on the ability to drive transp. cf. and fur:

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 in dealing with potentially hazardous activities that require increased attention, such as driving vehicles or controlling equipment that requires increased concentration.

Form release / dosage:

Tablets, film-coated, 0.2 mg, 0.3 mg or 0.4 mg.

Packaging:

10, 14, 15 or 30 tablets in a contoured cell pack of a polyvinylchloride film and aluminum foil.

1, 2 or 3 contour packs of 10 tablets, 1, 2 or 4 contour packs of 14 tablets, 1, 2 or 4 contour packs of 15 tablets, 1 or 2 contour packs of 30 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 of the year.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002550

Date of registration:31.07.2014 / 14.07.2015

Expiration Date:31.07.2019

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Representation: & nbspVERTEKS CJSC VERTEKS CJSC Russia

Information update date: & nbsp11.06.2018

Illustrated instructions

Instructions

Moxarel® (MOXAREL®)