Isosorbide mononitrate retard - instructions for use, dose, side effects, contraindications

Composition of gelatin capsule shell: gelatin pharmaceutical, glycerol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium lauryl sulfate, purified water, azorubin E-122 dye.

Description:

Capsules hard gelatinous № 1 with a transparent colorless case and a transparent lid of red color.

The contents of the capsules are pellets of white or almost white color.

Pharmacotherapeutic group:Vasodilating agent - nitrate

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

Pharmacodynamics:

Isosorbide mononitrate - a peripheral vasodilator with a predominant effect on venous vessels, has an antianginal effect. Reduces preload (by expanding the peripheral veins) and afterload (due to a decrease in the overall peripheral vascular resistance), reduces the need for myocardium in oxygen, dilates the coronary arteries and improves coronary blood flow, promotes its redistribution into the ischemic areas, reduces the terminal diastolic volume of the left ventricle and reduces systolic the tension of its walls.Increases tolerance to physical exertion 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, gallbladder muscles, biliary tract and esophagus, as well as the small and large intestine, including sphincters.

At the molecular level, nitrates act through the formation of nitric oxide and cyclic guanosyl monophosphate, which is considered to be a mediator of relaxation. Thus, the drug acts quickly and for a long time to prevent attacks of angina pectoris. Bioavailability of isosorbide mononitrate does not depend on the characteristics of the diet (calorie, high or low fat content) and meal time.

Pharmacokinetics:Quickly and completely absorbed after ingestion. Bioavailability ranges from 90 to 100%. Isosorbide mononitrate almost completely metabolized in the liver. Metabolites are pharmacologically inactive. Isosorbide mononitrate is excreted by the kidneys almost exclusively in the form of metabolites. Approximately 2% is displayed unchanged. The half-life is 8 hours.

Indications:

Prophylaxis and long-term treatment of angina pectoris.

Chronic heart failure (as part of combination therapy). Increased pressure in a small circle of blood circulation (pulmonary hypertension) (as part of combination therapy).

Contraindications:

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

- acute circulatory disorders (shock, vascular collapse);

- cardiogenic shock if a sufficiently high end-diastolic pressure in the left ventricle is not achieved by using intra-aortic counterpulsation or by administering agents that have a positive inotropic effect;

- severe arterial hypotension (systolic blood pressure (BP) less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg);

- simultaneous administration of phosphodiesterase inhibitors, including sildenafil, vardenafil, tadalafil, as they potentiate the antihypertensive effect of nitrates;

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

- age to 18 years (efficacy and safety not established).

Carefully:

- DIpertrophic obstructive cardiomyopathy, constrictive pericarditis, pericardial tamponade;

- low filling pressure in acute myocardial infarction, impaired left chamber function (left ventricular failure). Do not lower the systolic blood pressure below 90 mm Hg;

- aortic and / or mitral stenosis;

- tendency to orthostatic disorders of vascular regulation;

- 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);

- glaucoma;

- severe anemia;

- thyrotoxicosis;

- severe renal insufficiency;

- liver failure;

- increased peristalsis of the gastrointestinal tract;

- chronic heart failure.

Pregnancy and lactation:For reasons of Isosorbide safety, retard mononitrate can be used during pregnancy and lactation only strictly according to the doctor's prescription, after careful evaluation of the benefits to the mother and possible risks to the fetus and / or child.

Dosing and Administration:

Isosorbide mononitrate retard is taken orally, 1 capsule (50 mg) in the morning after breakfast, washed down with a small amount of water.

Duration of treatment is determined individually, depending on the indications and effectiveness of the therapy and is determined by the doctor.

Side effects:

Often (≥10): A "nitrate" headache may occur at the beginning of the treatment. When continuing therapy, it usually decreases after a few days.

Often (≥1% - <10%): After the first dose or after increasing the dose, blood pressure may decrease and / or develop orthostatic hypotension, which may be accompanied by tachycardia, dizziness, and weakness. There may be stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment), dry mouth.

Rarely (≥0,1% - <1%): There may be nausea, vomiting, flushing of the facial skin, a feeling of heat and allergic reactions (skin rash).

A marked decrease in blood pressure, accompanied by a weighting of the symptoms of angina (a paradoxical reaction to nitrates).

There were cases of collapoid states, sometimes with bradyarrhythmia and syncope.

Individual cases (<0.01%):

In individual cases, the emergence of exfoliative dermatitis, as well as the appearance of a slight burning sensation of the tongue.

It describes the development of tolerance and cross-tolerance with other nitro compounds by prolonged continuous treatment with high doses of isosorbide mononitrate. To prevent a decrease or loss of efficacy, continuous intake of high doses of the drug should be avoided.

Overdose:

Symptoms:

Reduction of blood pressure with orthostatic dysregulation, reflex tachycardia and headache. May appear weakness, dizziness, "tides" heat, hyperthermia, sweating, palpitations, visual disturbances, bradycardia, nausea, vomiting, diarrhea.

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.

In chronic overdose, an increase in the level of methemoglobin is possible, although the clinical significance of this has not yet been established.

Therapy:

In addition to general recommendations, such as gastric lavage and placing the patient in a horizontal position (legs are high), one should monitor the basic indicators of vital functions and, if necessary, adjust. Patients with severe arterial hypotension and / or shock should be injected with a solution of 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:

1. ascorbic acid: 1 g inside or in the form of sodium salt intravenously;

2. Oxygen therapy, hemodialysis, exchange blood transfusion.

Interaction:

When used with other vasodilators, antihypertensive agents, angiotensin converting enzyme inhibitors, beta-blockers, slow calcium channel blockers, diuretics, neuroleptics or tricyclic antidepressants, with phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil, and also with ethanol, potentiation of the antihypertensive effect of isosorbide mononitrate is possible.

When combined with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect. Under the influence of beta-adrenostimulants, alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to decrease the antianginal effect (tachycardia and excessive blood pressure decrease).

When combined with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure.

Adsorbents, astringent and enveloping medicines reduce the absorption of isosorbide mononitrate in the digestive tract.

Special instructions:

Isosorbide mononitrate retard should not be used to stop acute attacks of angina pectoris, acute myocardial infarction. During the therapy, it is necessary to monitor blood pressure and heart rate.

With long-term use, it is possible to develop tolerance, in connection with which it is recommended after 3-6 weeks of regular intake of the drug to take a break for 3-5 days, replacing for this time isosorbide mononitrate retard with other antianginal drugs. When taking the drug, temporary hypoxemia may occur due to a relative redistribution of blood flow to the hypoventilation alveolar zone.In patients with ischemic heart disease, this can lead to temporary myocardial hypoxia. It should be avoided abrupt withdrawal of the drug (dose gradually reduce). During the treatment with the drug should be excluded from drinking alcohol.

Effect on the ability to drive transp. cf. and fur:During treatment it is not recommended to drive vehicles and engage in other potentially dangerous activities requiring a fast psychomotor reaction.

Form release / dosage:

Capsules of prolonged action of 50 mg.

Packaging:For 10 capsules in a planar cell package (PVC / aluminum), 3 contour packs with instructions for use in a pack of cardboard.

Storage conditions:List B. In dry the dark place at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006470/09

Date of registration:13.08.2009

Expiration Date:Unlimited

The owner of the registration certificate:MINSKINTERKAPS, UP MINSKINTERKAPS, UP Republic of Belarus

Manufacturer: & nbsp

MINSKINTERKAPS, UP Republic of Belarus

Information update date: & nbsp10.11.2017

Illustrated instructions

Instructions

Isosorbide mononitrate retard (Isosorbide mononitrate retard)