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

auxiliary substances (core): croscarmellose sodium (impellose) - 3.0 mg; lactose monohydrate (lactopress) (sugar milk) - 95.3 mg; silicon dioxide colloid (aerosil) - 0.5 mg; sodium stearyl fumarate 1.0 mg;

auxiliary substances (shell): Opadrai II (polyvinyl alcohol, partially hydrolyzed - 1.32 mg, titanium dioxide E171 - 0.6027 mg, talc 0.6 mg, macrogol (polyethylene glycol 3350) - 0.3705 mg, soy lecithin E322 - 0.105 mg, iron dye oxide (II) yellow - 0.0003 mg, iron oxide dye (II) red - 0.0015 mg).

dosage of 0.3 mg:

active substance: moxonidine 0.3 mg

auxiliary substances (core): croscarmellose sodium (impellose) - 3.0 mg; lactose monohydrate (lactopress) (sugar milk) - 95.2 mg; silicon dioxide colloid (aerosil) - 0.5 mg; sodium stearyl fumarate 1.0 mg;

auxiliary substances (shell): Opadrai II (polyvinyl alcohol, partially hydrolyzed - 1.32 mg, titanium dioxide E 171-0.6003 mg, talc 0.6 mg, macrogol (polyethylene glycol 3350) 0.3705 mg, soy lecithin E322-0.105 mg, aluminum varnish based on the dye of the crimson [Ponso 4R] - 0.0039 mg; aluminum lacquer based on the dye sunset sunset yellow - 0.0003 mg).

dosage of 0.4 mg:

active substance: moxonidine 0.4 mg

auxiliary substances (core): Croscarmellose sodium (optional) - 3,0 mg; lactose monohydrate (lactopress) (sugar milk) - 95.1 mg; silicon dioxide colloid (aerosil) - 0.5 mg; sodium stearyl fumarate - 1,0 mg;

auxiliary substances (shell): Opadry II (polyvinyl alcohol, partially hydrolysed, 1.32 mg, titanium dioxide E171-0.5751 mg, talc 0.6 mg, macrogol (polyethylene glycol 3350) 0.3705 mg, soy lecithin E 322-0.105 mg, aluminum varnish for based indigocarmine - 0.0018 mg, aluminum varnish based on azorubin dye - 0.0153 mg, aluminum varnish based on the dye of the crimson [Ponso 4R] - 0.0123 mg).

Description:

The tablets covered with a film cover of light pink color, round, biconcave. Tablets on a break of white or almost white color (dosage of 0.2 mg).

The tablets covered with a film cover of pink color, round, biconcave. Tablets on a break of white or almost white color (dosage of 0.3 mg).

The tablets covered with a film membrane of dark pink color, round, biconcave. Tablets on a break of white or almost white color (dosage of 0.4 mg).

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 antihypertensive agents with a lower affinity for α₂adrenoreceptors, which explains the lower probability of sedation and dry mouth.

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

Moxonidine improves the insulin sensitivity index by 21% (in comparison with placebo) 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. Food intake 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 over 90% moxonidine is excreted by the kidneys (about 78% unchanged and 13% in the form of dehydrimeroxycinidine, 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 the patients with arterial hypertension

In comparison with healthy volunteers, patients with hypertension do not have any changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in old 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.

Pharmacokinetics the 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 failure (CK in the range of 30-60 ml / min), the 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_1/2respectively, 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 and other components of the drug;

- syndrome of weakness of the sinus node;

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

- atrioventricular blockade of II and III degree;

- severe cardiac rhythm disturbances;

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

- simultaneous use with tricyclic antidepressants (see.section "Interaction with other medicinal products");

- severe renal failure (CC less than 30 ml / min);

- hemodialysis;

- lactation period;

- hereditary lactose intolerance, lactase deficiency or malabsorption of glucose-galactose;

- age over 75 years;

- age under 18 years (due to lack of data on safety and effectiveness).

Carefully:

Special care must be taken with moxonidine in patients with stage I atrioventricular block (risk of developing bradycardia); severe coronary artery disease, severe coronary heart disease or unstable angina (insufficient experience), chronic heart failure, severe hepatic impairment, renal dysfunction (QC greater than 30 mL / min).

Pregnancy and lactation:

Pregnancy

Clinical data on the use of Moxonidine-SZ in pregnant women are absent. In the course of animal studies, the embryotoxic effect of the drug was established.

Moxonidine-SZ should be given to pregnant women only after a thorough assessment of the risk-benefit relationship, when the benefit to the mother exceeds the potential risk to the fetus.

Lactation period

Moxonidine-SZ penetrates into breast milk and therefore should not be given during breastfeeding.

Moxonidine-SPI is necessary to use Moxonidine-SZ during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake.

In most cases, the initial dose of Moxonidine-SZ 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. Individual correction of the daily dose is necessary depending on the patient's tolerability of the therapy.

Dose adjustment for patients with hepatic insufficiency is not required. The initial dose for patients with moderate or severe renal failure is 0.2 mg / day.

If necessary and with good tolerability, the daily dose can be increased to a maximum of 0.4 mg.

Side effects:

The frequency of side effects, given below, was determined according to the following: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); including individual messages.

From the central nervous system:

Often: headache *, dizziness (vertigo), drowsiness.

Infrequently: fainting *.

From the side of the cardiovascular system:

Infrequent: marked decrease in blood pressure, orthostatic hypotension *, bradycardia.

From the gastrointestinal tract:

Very often: dryness of the oral mucosa.

Often: diarrhea, nausea, 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:

Infrequent: ringing in the ears.

From the musculoskeletal and connective tissue:

Often: back pain.

Infrequent: pain in the neck.

General disorders and disorders at the site of administration:

Often: asthenia.

Infrequent: peripheral edema.

(* - frequency comparable to placebo).

Overdose:

There are reports of several cases of overdose without a lethal outcome, when doses up to 19.6 mg were applied at the same time.

Symptoms: headache, sedative effect, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dryness of the oral mucosa, vomiting, fatigue, epigastric pain, respiratory depression and impaired consciousness.In addition, short-term increases in blood pressure, tachycardia and hyperglycemia are also possible, as shown in several studies on the study of high doses in animals.

Treatment

There is no specific antidote. In the case of a marked decrease in blood pressure, it may be necessary to restore the volume of circulating blood by introducing fluid and dopamine (injection).

Bradycardia can be stopped with atropine (injection injection).

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

Alpha-adrenoreceptor antagonists can reduce or eliminate paradoxical hypertensive effects in overdose with moxonidine.

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.

Moxonidine may enhance the sedative effect of benzodiazepine derivatives when administered concomitantly.

Moxonidine is excreted by tubular secretion. Therefore, its interaction with other drugs released by tubular secretion is not excluded.

Beta-adrenoblockers increase bradycardia, the severity of negative foreign and dromotropic effects.

Special instructions:

If it is necessary to cancel simultaneously taken beta-blockers and the drug Moxonidine-SZ, first abolish beta-blockers and only after a few days of Moxonidine-SZ.

At present, there is no evidence that discontinuation of Moxonidine-SZ treatment leads to an increase in blood pressure. However, it is not recommended to stop taking the drug Moxonidine-SZ sharply, instead you should gradually reduce the dose of the drug within two weeks.

During treatment, exclude alcohol.

During treatment, regular monitoring of heart rate and electrocardiography is necessary.

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

The effect of Moxonidine-SZ on the ability to drive vehicles or control technology was not studied. However, taking into account the possibility of dizziness and drowsiness, patients should be careful in dealing with potentially hazardous activities requiring increased attention, such as driving vehicles or controlling equipment that requires increased concentration.

Form release / dosage:

Film-coated tablets, 0.2 mg, 0.3 mg and 0.4 mg

Packaging:

For 10, 14 or 30 tablets per contour cell package.

For 60 tablets in cans of polymer or in polymeric bottles.

Each bank, vial, 3 contour packs of 10 tablets, 1, 2 contour packs of 14 tablets or 1, 2, 3, 4 contourcell packs of 30 tablets together with instructions for use are placed in a cardboard box.

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 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-002321

Date of registration:05.12.2013 / 19.03.2018

Expiration Date:05.12.2018

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Representation: & nbspNORTH STAR CJSC NORTH STAR CJSC Russia

Information update date: & nbsp12.06.2018

Illustrated instructions

Instructions

Moxonidine-SZ (Moxonidine-SZ)