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

Excipients: giprolose (hydroxypropylcellulose) 3 mg, mannitol 68 mg, croscarmellose sodium 3.3 mg, magnesium stearate 0.5 mg, microcrystalline cellulose 25 mg;

composition of film shell: Opadrai II pink 3 mg, including: polyvinyl alcohol 1.2 mg, macrogol (0.506 mg), talc 0.444 mg, titanium dioxide 0.7206 mg, dye sunset yellow 0.0003 mg, indigo carmine dye 0.0045 mg , dye crimson [Ponso 4R] 0.0246 mg.

Dosage of 0.3 mg

1 tablet, film-coated, 0.3 mg contains:

active substance: moxonidine 0.3 mg;

Excipients: giprolose (hydroxypropyl cellulose) 3.6 mg, mannitol 81.5 mg, croscarmellose sodium 4 mg, magnesium stearate 0.6 mg, microcrystalline cellulose 30 mg;

composition of film shell: Opadry II pink 3.5 mg including 1.4 mg of polyvinyl alcohol, macrogol (polyethylene glycol) 0.707 mg Talc 0.518 mg, 0.6626 mg of titanium dioxide, dye sunset yellow 0.0889 mg, indigo dye 0 0507 mg, Crimson dye [Ponce 4R] 0.0728 mg.

Dosage 0.4 mg

1 tablet, film-coated, 0.4 mg contains:

active substance: moxonidine 0.4 mg;

Excipients: giproloza (hydroxypropyl cellulose) 4.2 mg mannitol 95 mg Croscarmellose sodium 4.7 mg Magnesium stearate 0.7 mg Microcrystalline cellulose 35 mg;

film coating: Opadry II pink 4 mg including 1.6 mg of polyvinyl alcohol, macrogol (polyethylene glycol) 0.808 mg Talc 0.592 mg, 0.9608 mg of titanium dioxide, dye sunset yellow 0.0004 mg, 0.0060 mg of dye indigo carmine , dye crimson [Ponso 4R] 0.0328 mg.

Description:Tablets are round, biconvex, covered with a filmy coat of pink color (dosage 0.2 mg and 0.4 mg) or dark pink color (dosage 0.3 mg). The cross section is almost white.Insignificant roughness is allowed.

Pharmacotherapeutic group:central antihypertensive drug

ATX: & nbsp

C.02.A.C.05 Moxonidine

Pharmacodynamics:

Selective agonist imidazoline receptors responsible for tonic and reflex control of the sympathetic nervous system (localized in the ventro-lateral region of the medulla oblongata). Reduces the pressor effect of the sympathetic system on peripheral vessels, reduces peripheral vascular resistance, reduces systolic and diastolic pressure, both with a single and long-term admission, while cardiac output and heart rate (heart rate) do not change significantly. With long-term use reduces myocardial hypertrophy of the left ventricle, neutralizes the signs of myocardial fibrosis, microarthiopathy, normalizes the capillary blood supply of the myocardium. Against the background of treatment, the activity of norepinephrine and epinephrine, renin, angiotensin II at rest and under load, atrial natriuretic peptide (under load) and aldosterone of blood plasma decrease.

Has a lower affinity for alpha₂-adrenoceptors, which explains the lower probability of developing a sedative effect and dry mouth.

Reduces the resistance of tissues to insulin. Does not affect the exchange of glucose and lipids.

Pharmacokinetics:

Absorption after oral administration - 90%. Eating does not affect the amount of absorption. Bioavailability - 88%. Relationship with blood plasma proteins - 7.2%. The maximum concentration (C_mOh ) in plasma is determined 30-180 minutes after oral administration and is 1-3 ng / ml. The volume of distribution is 1.4-3 l / kg. The main metabolite is dihydrated moxonidine. The pharmacodynamic activity of deoxidized moxonidine is about 10% compared to moxonidine. Penetrates through the blood-brain barrier. Do not cumulate with prolonged use. The half-life of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours more than 90% of moxonidine is excreted by the kidneys (78% in unchanged form, 13% in the form of dihydrated moxonidine, 8% in the form of other metabolites). Less than 1% of the dose is excreted through the intestine. Moxonidine is slightly excreted during hemodialysis.

Pharmacokinetics in patients with arterial hypertension

Patients with hypertension do not have any changes in the pharmacokinetics of moxonidine.

Pharmacokinetics in elderly patients

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 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), the equilibrium concentrations in the blood plasma and the final half-life period are approximately 2 and 1.5 times higher than in patients with normal renal function (CC greater than 90 ml / min ). In patients with severe renal insufficiency (CC less than 30 ml / min), the equilibrium concentrations in the blood plasma and the final half-life is 3 times higher than in patients with normal renal function. In patients with terminal renal failure (CC less than 10 ml / min) on hemodialysis, the equilibrium plasma concentrations and the terminal half-life, respectively, are 6 and 4 times higher than in patients with normal renal function.In patients with impaired renal function, the dosage should be selected individually.

Indications:

Arterial hypertension.

Contraindications:

- Hypersensitivity to the components of the drug;

- marked violations of the rhythm of the heart;

- syndrome of weakness of the sinus node;

- Sinoatrial and atrioventricular blockade II and III degree;

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

- acute and chronic heart failure of III and IV functional class according to classification NYHA;

- angioedema in history;

- severe hepatic insufficiency (more than 9 points on the Child-Pugh scale);

- chronic renal failure (CC less than 30 ml / min, creatinine more than 60 μmol / l);

- hemodialysis;

- simultaneous use of tricyclic antidepressants;

- age under 18 years (effectiveness and safety not established);

- age over 75 years;

- the period of lactation,

Carefully:

- Parkinson's disease (severe form);

- epilepsy;

- glaucoma;

- Depression;

- "intermittent" lameness;

- Raynaud's disease;

- atrioventricular blockade of the 1st degree;

- chronic renal failure (QC more than 30 ml / min, but less than 60 ml / min);

- severe cerebrovascular disorders;

- after a recent myocardial infarction;

- severe coronary artery disease;

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

- chronic heart failure of I and II functional class according to classification NYHA;

- violations of the liver function;

- Pregnancy.

Pregnancy and lactation:

There are no clinical data on the negative effect on the course of pregnancy. However, the drug Moxonidine Kanon should be given to pregnant women only if the potential benefit to the mother exceeds the possible risk to the fetus.

Moxonidine penetrates into breast milk, so if taking Moxonidine Kanon is necessary during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, regardless of food intake, with enough liquid.

In most cases, the initial dose of the drug Moxonidine Kanon is 0.2 mg per day, at one time, preferably in the morning hours. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day, which should be divided into 2 divided doses (morning and evening) or once.

The maximum daily dose, which should be divided into 2 doses (morning and evening), is 0.6 mg.

The maximum single dose is 0.4 mg.

Have elderly patients with normal renal function recommendations for dosage are the same as for adult patients.

Have patients with renal insufficiency (clearance of creatinine 30-60 ml / min) and patients on hemodialysis single dose should not exceed 0.2 mg, the maximum daily dose - 0.4 mg.

Side effects:

Classification of WHO frequency of development of side effects:

very often - ≥1/10 appointments (> 10%)

often from ≥1 / 100 to <1/10 of appointments (> 1% and <10%)

infrequently - from ≥1 / 1000 to <1/100 of prescriptions (> 0.1% and <1%)

rarely from ≥ 1/10000 to <1/1000 appointments (> 0.01% and <0.1%)

very rarely - <1/10000 prescriptions (<0.01%)

Disorders of the psyche

Often: decreased concentration of attention.

Infrequently: depression, anxiety, nervousness.

Disorders from the central nervous system

Often: increased fatigue, drowsiness, headache, dizziness.

Infrequently: paresthesia, insomnia, fainting.

Disorders from the gastrointestinal tract

Often: dryness of the oral mucosa, constipation, dyspeptic disorders.

Infrequently: nausea, anorexia.

Very rarely: hepatitis, cholestasis.

Disturbances from the skin and subcutaneous tissues

Infrequent: skin rash, itching, swelling of various locations.

Very rarely: angioedema.

Disorders from the genitourinary system

Infrequent: urinary retention or incontinence, impotence, decreased libido.

Disturbances from the liver and bile ducts

Rarely: hepatitis, bile stasis.

Disturbances on the part of the organ of sight

Infrequent: dry eyes, causing itching or burning sensation in the eyes.

Hearing disorders and labyrinthine disorders

Infrequent: ringing in the ears.

Vascular disorders

Often: symptoms of vasodilation.

Infrequent: lowering blood pressure (BP), orthostatic hypotension, Raynaud's syndrome, peripheral circulation disorders.

Disorders from the endocrine system

Infrequently: gynecomastia.

Disturbances from musculoskeletal and connective tissue

Often: back pain.

Infrequent: pain in the neck.

General disorders and disorders at the site of administration

Often: asthenia.

Infrequent: weakness in the legs, fainting, pain in the parotid glands.

Overdose:

Symptoms: headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, general weakness, bradycardia, fatigue, dryness of the oral mucosa, vomiting and stomach pain.Paradoxically, blood pressure, tachycardia, and hyperglycemia are also potentially possible.

Treatment: there is no specific antidote. Gastric lavage (immediately after administration), reception of activated carbon and laxatives, symptomatic therapy.

In the case of a marked decrease in blood pressure, it is recommended that the volume of circulating blood be restored by introducing a liquid and dopamine administration. Bradycardia can be stopped with atropine.

Alpha-adrenoreceptor antagonists can reduce or eliminate transient hypertension in an overdose of Moxonidine Kanon.

Interaction:

Moxonidine Kanon can be administered with thiazide diuretics and blockers of "slow" calcium channels. The combined use of the drug Moxonidine Kanon with these and other antihypertensive agents leads to an additive effect and an increase in the hypotensive effect.

In the appointment of the drug Moxonidine Kanon with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, pharmacokinetic interaction is absent.

Tricyclic antidepressants may reduce the effectiveness of antihypertensive agents of central action,so their simultaneous use is not recommended.

The drug Moxonidine Kanon moderately increases the reduced cognitive ability in patients taking lorazepam.

Administration of the drug Moxonidine Kanon together with benzodiazepine derivatives may be accompanied by an increase in the sedative effect of the latter.

The drug Moxonidine Kanon intensifies the inhibitory effect on the central nervous system of anxiolytics, barbiturates and ethanol.

Beta-adrenoblockers when combined with moxonidine increase bradycardia, the severity of negative foreign and dromotropic effects.

In the appointment of the drug Moxonidine Kanon together with moclobemide pharmacodynamic interaction is absent.

Special instructions:

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

It is not recommended to administer tricyclic antidepressants concomitantly with Moxonidine Kanon.

During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.

The drug Moxonidine Kanon can be administered with thiazide diuretics, angiotensin-converting enzyme (ACE) inhibitors and blockers of "slow" calcium channels.

Stop taking the drug Moxonidine Kanon should be gradual.

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

Taking into account the possible occurrence of drowsiness and dizziness during treatment with Moxonidine Kanon, patients should be careful with engage in potentially hazardous activities that require increased attention, such as driving a vehicle or managing equipment that requires increased concentration.

Form release / dosage:

Tablets, film-coated, 2.0 mg, 0.3 mg and 0.4 mg.

Packaging:

By 7, 10, 28 or 30 tablets in a contour mesh package and in polyvinyl chloride film and aluminum foil printed lacquered.

By 2, 4, 6, 8 contour cell packs of 7 tablets or 1,2, 3, 4, 6 contiguous cell packs of 10 tablets, or 1.2 contour cell packs of 28 tablets, or 1, 2, 3, 4 contour cell packs of 30 tablets together with instructions for use are placed in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002607

Date of registration:02.09.2014

Expiration Date:02.09.2019

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp02.09.2016

Illustrated instructions

Instructions

Moxonidine Kanon (Moxonidine Canon)