Monizol - instructions for use, doses, side effects, contraindications

active substance: 20 mg of isosorbide mononitrate; Excipients: lactose monohydrate - 80.00 mg, microcrystalline cellulose - 41.25 mg, corn starch - 5.00 mg, talc - 2.50 mg, magnesium stearate - 1.25 mg.

1 tablet of 40 mg contains:

active substance: 40 mg isosorbide mononitrate; Excipients: lactose monohydrate - 160.00 mg, microcrystalline cellulose - 82.50 mg, corn starch - 10.00 mg, talc - 5.00 mg, magnesium stearate - 2.50 mg.

Description:

Tablets of 20 mg:

Round tablets of flat-cylindrical shape with a facet on both sides, with a risk on one side, white or almost white.

Tablets 40 mg:

Round tablets of flat-cylindrical shape with a facet on both sides, with a risk on one side, white or almost white.

Pharmacotherapeutic group:Vasodilating agent - nitrate

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

Pharmacodynamics:

Peripheral vasodilator with predominant effect on venous vessels. The active substance of the drug Monizol - isosorbide - 5 - mononitrate has a vasodilating and antianginal effect. At the molecular level, it acts through the formation of nitric oxide (N0) and cyclic guanosine monophosphate (cGMP), which is considered to be a mediator of relaxation, as well as by reducing the calcium concentration in smooth muscle cells. Reduces preload (by expanding peripheral veins) and postnagruzku (due to a decrease in the total peripheral vascular resistance), reduces the need for myocardium in oxygen,expands coronary arteries and improves coronary blood flow, promotes its redistribution into ischemic areas, reduces the terminal diastolic volume of the left ventricle and reduces the systolic tension of its walls. Increases tolerance to physical activity of patients with coronary heart disease (CHD), reduces pressure in a small circle of blood circulation.

Isosorbide mononitrate causes relaxation of the musculature of the bronchi, urinary tract, gall bladder muscles, biliary tract and esophagus, as well as the small and large intestine, including sphincters.

When ingestion of isosorbide mononitrate antianginal effect is manifested after 30-45 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics:

The drug is quickly and completely absorbed into the intestine after ingestion. The maximum concentration is achieved in the blood plasma approximately 1 hour after ingestion.

Bioavailability with oral administration is from 90 to 100%. The connection with blood plasma proteins is less than 4%. It is subjected to denitrification with the formation of isosorbide or is combined with glucuronide. Isosorbide mononitrate almost completely metabolized in the liver, is not exposed to the effect of "first passage" through the liver (in contrast to isosorbide dinitrate). Metabolites are pharmacologically inactive. Isosorbide-5-mononitrate is excreted through the kidneys exclusively in the form of metabolites. Approximately 2% is displayed unchanged. The half-life is 4-5 hours, which is approximately 8 times higher than that of isosorbide dinitrate.

Tolerance: a decrease in efficacy was observed, despite the absence of a change in dosage and a constant level of nitrate in the blood. The observed tolerance decreases within 24 hours of continuing therapy.

There was no development of tolerance when taking the drug with interruptions.

Indications:

- Prevention of angina attacks and subsequent treatment of angina after a previous myocardial infarction.

- Treatment of chronic heart failure (as part of combination therapy).

Contraindications:

- Hypersensitivity to organic nitrates and other components of the drug;

- Acute circulatory disorders (shock, vascular collapse);

- cardiogenic shock,if it is impossible to correct the final diastolic pressure of the left ventricle with intra-aortic counterpulsation or through the introduction of agents that have a positive inotropic effect;

- Acute myocardial infarction with severe arterial hypotension;

- simultaneous administration of inhibitors of phosphodiesterase-5 (FED-5) (tadalafil, sildenafil, vardenafil), since the inhibitors of FED-5 potentiate the hypotensive effect of nitrates;

- severe arterial hypotension (systolic blood pressure (BP) less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg, central venous pressure below 4-5 mm Hg), hypovolemia;

- craniocerebral trauma, cerebral hemorrhage;

- deficiency of glucose-6-phosphate dehydrogenase;

- primary pulmonary hypertension;

- hereditary intolerance to galactose, a deficiency of lactase or a syndrome of malabsorption of glucose and galactose;

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

- pregnancy and lactation.

Carefully:

- Hypertrophic obstructive cardiomyopathy, constrictive pericarditis, pericardial tamponade;

- low filling pressure of the left ventricle, for example,with acute myocardial infarction (risk of lowering blood pressure and tachycardia, which may increase ischemia), decreased left ventricular function (left ventricular failure). Do not lower the systolic blood pressure below 90 mm Hg;

aortic and / or mitral stenosis;

- with a tendency to arterial hypotension (orthostatic disorders of blood circulation regulation);

- Closed-angle glaucoma (risk of increased intraocular pressure);

- diseases accompanied by increased intracranial pressure (until now a further increase in intracranial pressure was observed only with intravenous administration of high doses of nitroglycerin);

- severe anemia;

- severe renal failure;

- hepatic insufficiency (risk of development of methemoglobinemia).

Pregnancy and lactation:In pregnancy, the drug should be used in cases where the expected benefit for a woman exceeds the possible risk to the fetus. If it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Dosing and Administration:

The dose of the drug and the frequency of application are selected individually,based on the clinical efficacy and tolerability of the drug.

The drug is taken orally, after eating, with water, without chewing.

Monizol tablets 20 mg

It is advisable to start therapy with small doses of the drug: 1/2 tablet (10 mg) 2 times a day. Then gradually increase the dose to therapeutic: 1-2 tablets (20-40 mg) in 1-2 divided doses per day. If necessary, increase the dose to 3 tablets (60 mg) per day.

Monizol tablets 40 mg

Take 1/2 tablet (20 mg) 2 times a day or 1 tablet (40 mg) once a day. In some cases, the dose can be increased to 2 tablets (80 mg) in two divided doses per day. To fully achieve the therapeutic effect, the second tablet of 40 mg (with a daily dose of 80 mg) should be taken no later than 8 hours later. The duration of therapy is determined by the doctor.

The maximum daily dose is 120 mg.

If there is a headache at the beginning of the course of treatment, a single dose of the drug within the first 2-3 days can be reduced.

Side effects:

From the cardiovascular system: at the beginning of the treatment, there may be a headache ("nitrate" headache), which, as a rule, decreases after several days of therapy; dizziness, hyperemia of the facial skin, a feeling of heat, tachycardia.Sometimes, when the drug is first taken or after an increase in the dose, a decrease in blood pressure and / or orthostatic hypotension occurs, which can be accompanied by a reflex increase in the heart rate (HR), inhibition, and dizziness and a sense of weakness. In rare cases - increased attacks of angina (a paradoxical reaction to nitrates), orthostatic collapse.

Cases of collapoid states were noted, sometimes with bradycardia and syncope.

From the gastrointestinal tract: nausea, vomiting, there may be a sensation of slight burning of the tongue, dry mouth.

From the central nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment). In rare cases - ischemia of the brain.

Allergic reactions: skin rash, in some cases - exfoliative dermatitis (severe cases of exudative erythema multiforme, dissemination of impetigo and toxicodermia).

The development of tolerance, as well as cross-tolerance with other nitrocompounds in long-term continuous treatment with high doses of isosorbide mononitrate, is described.To prevent a decrease or loss of efficacy, continuous intake of high doses of the drug should be avoided.

Overdose:

Symptoms: headache, marked decrease in blood pressure with orthostatic dysregulation, reflex tachycardia. There may be weakness, dizziness, fainting, hot flashes, sweating, nausea, vomiting and diarrhea, inhibition, convulsions.

At high doses (20 mg / kg body weight) should expect methemoglobinemia, cyanosis, dyspnea and tachypnea from the formation of nitrite ions as a result of metabolism of isosorbide mononitrate.

Very high doses can lead to an increase in intracranial pressure with the onset of cerebral symptoms.

Treatment should be directed to the normalization of blood pressure, in mild cases it is necessary to put the patient in a horizontal position (legs are raised high). Induce vomiting, rinse the stomach. In addition, the basic indicators of vital functions should be monitored and, if necessary, adjusted. Patients with severe arterial hypertension and / or shock should be injected with fluid; in exceptional cases, to improve blood circulation, one can perform norepinephrine infusion(norepinephrine) and / or dopamine.

The introduction of epinephrine (adrenaline) and related compounds is contraindicated!

Depending on the degree of severity, in the cases of methemoglobinemia the following antidotes are used:

- ascorbic acid (vitamin C): 1 g orally or in the form of the sodium salt intravenously.

- oxygen therapy, hemodialysis, exchange blood transfusion.

Interaction:

When used with other vasodilators, antihypertensive agents, angiotensin converting enzyme (ACE) inhibitors, beta-blockers, slow calcium channel blockers (BCCI), diuretics, neuroleptics or tricyclic antidepressants, with phosphodiesterase-5 inhibitorstadalafil, sildenafil, vardenafil), as well as with ethanol, potentiation of the antihypertensive action of isosorbide mononitrate is possible.

With the simultaneous use of isosorbide mononitrate and dihydroergotamine, an increase in the level of dihydroergotamine in the blood plasma can occur.

The therapeutic effect of norepinephrine (norepinephrine) decreases with simultaneous intake with nitrocompounds.

When combined with amiodarone, propranolol, BCCK (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect.

Under the influence of beta-adrenostimulants, alpha-addressblockers (dihydroergotamine and others), it is possible to reduce the antianginal effect (tachycardia and excessive blood pressure decrease).

Reduces the effect of vasopressors.

Barbiturates accelerate metabolism and reduce the concentration of isosorbide mononitrate in the blood.

When combined with m-holinoblokatorami (atropine and others), the likelihood of a decrease in intraocular pressure increases.

Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.

Special instructions:

Monizol should not be used to stop angina attacks!

During the period of drug therapy, control of blood pressure and heart rate is necessary.

Care should be taken with aortic and mitral stenosis, constructive pericarditis, cardiac tamponade, orthostatic hypotension and intracranial hypertension.

Frequent administration and high doses of Monizol may cause tolerance; in this case, it is recommended to cancel for 24-48 h or after 3-6 weeks of regular admission to take a break for 3-5 days, replacing in this case isosorbide mononitrate other antianginal agents.

If necessary, use the drug against the background of arterial hypotension should simultaneously prescribe funds that have a positive inotropic effect. The drug is used alone or in combination with beta-blockers, BCCI, ACE inhibitors, cardiac glycosides or diuretics.

Do not abruptly stop using Monizol. This must be done gradually to avoid the undesirable consequences of abrupt cessation of therapy (withdrawal syndrome.)

During the treatment with the drug should be excluded from drinking alcohol!

Effect on the ability to drive transp. cf. and fur:When taking the drug (especially at the beginning of treatment), it is possible to reduce the ability to respond quickly, and therefore it is not recommended to drive vehicles and engage in other potentially hazardous activities.

Form release / dosage:Tablets 20 and 40 mg.

Packaging:

Tablets 20 mg: For 15 tablets in blisters from PVC / AL. 2 blisters with instructions for use in a pack of cardboard.

Tablets 40 mg: For 10 tablets in PVC / AL blisters. For 3 blisters with instructions for use in a pack of cardboard.

Storage conditions:

Store in the original packaging at a temperature of 15 to 25 ° C.

Keep out of the reach of children!

Shelf life:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N014347 / 01

Date of registration:29.06.2009 / 18.05.2010

Expiration Date:Unlimited

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

HEMOFARM D.O.O. SABAC Serbia

Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia

Information update date: & nbsp13.06.2018

Illustrated instructions

Instructions

Monizol (Monizol)