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

Composition of gelatin capsule shell: gelatin - 61,404 mg, glycerin - 0,095 mg, water purified - 10,585 mg, sodium lauryl sulfate - 0,044 mg, titanium dioxide 0.873 mg.

Description:

Capsules hard gelatin №1 white.

The contents of the capsules are white or almost white in color, odorless.

Pharmacotherapeutic group:Vasodilating agent - nitrate

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

Pharmacodynamics:

Has vasodilator and antianginal action.

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 (N0) and cyclic guanosyl monophosphate (cGMP), which is considered to be a mediator of relaxation. When ingestion of isosorbide mononitrate antianginal effect manifests itself after 30 minutes and lasts 2-6 hours.

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 4-5 hours.

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:

Prophylaxis and long-term therapy of angina pectoris.

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

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 less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg);

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

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

- children and adolescence up to 18 years.

Carefully:

- Hypertrophic 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.

Pregnancy and lactation:For security reasons Isosorbide mononitrate can be used during pregnancy and lactation only strictly according to the doctor's prescription, after a thorough evaluation of the benefits and possible risks, since there is currently insufficient data on the consequences of its use in pregnant and lactating mothers. If the nursing mother still takes Isosorbide mononitrate, it is necessary to establish observation of the child for the development of possible effects from the drug.

Dosing and Administration:

Frequency of admission and duration of treatment are set individually. Inside, after eating with water.

Capsules "Isosorbide mononitrate" take 20 - 40 mg per reception 2-3 times a day with an interval of 7-8 hours.

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, redness of the face and skin allergic reactions.

A marked decrease in blood pressure, accompanied by a weighting of symptoms. 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. 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:

Reduction of blood pressure with orthostatic dysregulation, reflex tachycardia and headache. May appear weakness, dizziness, "tides" of heat, nausea, vomiting and 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 fluid; In exceptional cases, norepinephrine and / or dopamine infusions can be used to improve blood circulation.

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. Vitamin C: 1 g inside or in the form of the sodium salt intravenously.

2. methylene blue: up to 50 ml of 1% solution of methylene blue intravenously.

3. toluidine blue: first 2-4 mg / kg body weight strictly intravenously; then, if necessary, repeated administration of 2 mg / kg body weight with an interval between administrations in one hour is possible.

4. oxygen therapy, hemodialysis, exchange blood transfusion.

Interaction:

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

With the simultaneous use of the drug Isosorbide mononitrate and dihydroergotamine, an increase in the level of dihydroergotamine in the blood plasma and the potentiation of hypertensive action can occur.

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

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 Do not use to stop acute attacks of angina and acute myocardial infarction. During the treatment with the drug should be excluded from the use of ethanol.

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

Form release / dosage:

Capsules of 20 and 40 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-008312/08

Date of registration:21.10.2008

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 (Isosorbide mononitrate)