isosorbide mononitrate | Monochinkwe tablets 40 mg, 30 pcs.

Release form

Tablets.

Packing

30 pcs

Pharmacological action

Pharmacodynamics

Peripheral vasodilator with a primary effect on venous vessels. It has a vasodilating and antianginal effect.

Reduces preload (due to the expansion of peripheral veins) and afterload (due to a decrease in total peripheral vascular resistance), reduces myocardial oxygen demand, expands coronary arteries and improves coronary blood flow, promotes its redistribution to ischemic areas, reduces the final diastolic volume of the left ventricle and reduces systolic tension of its walls. Increases exercise tolerance in patients with coronary heart disease, reduces pressure in the pulmonary circulation.

Isosorbide mononitrate relaxes the muscles of the bronchi, urinary tract, gall bladder muscles, bile duct and esophagus, as well as the small and large intestines, including sphincters.

At the molecular level, nitrates act through the formation of nitric oxide (NO) and cyclic guanosyl monophosphate (cGMP), which is considered a mediator of relaxation. When ingestion of isosorbide-5-mononitrate, the antianginal effect manifests itself after 30 minutes and lasts 2-6 hours.

Pharmacokinetics

Quickly and completely absorbed after oral administration. Bioavailability is from 90 to 100%. The maximum concentration in blood plasma is reached after approximately 1-1.5 hours. The therapeutic concentration of isosorbide-5-mononitrate in the blood is reached after 30 minutes and is 250 ng / ml, within 4 hours - 414 ng / ml, within 12 hours -199 ng / ml (i.e., a drop in concentration slow). Isosorbide-5-mononitrate is almost completely metabolized in the liver, and it undergoes a “first pass” effect through the liver (in contrast to isosorbua dinitrate).

Metabolites are pharmacologically inactive. Isosorbide-5-mononitrate is excreted by the kidneys almost exclusively in the form of metabolites. Approximately 2% is excreted unchanged. The half-life is 4-5 hours, which is 8 times higher than that of isosorbide dinitrate.

The development of tolerance, as well as cross tolerance with other nitro compounds during long-term continuous treatment with high doses of isosorbide - 5-mononitrate is described. To prevent a decrease or loss of effectiveness, continuous administration of high doses of the drug should be avoided.

Indications

Prevention of angina pectoris in patients with coronary artery disease, including after myocardial infarction.

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

Contraindications

Hypersensitivity to nitrates or other components of the

preparation acute circulatory disorders (shock, vascular collapse)

acute myocardial infarction with severe arterial hypotension

cardiogenic shock, if a sufficiently high final diastolic pressure in the left ventricle is not achieved by applying intra-aortic counterpulsation or by administering drugs that have a positive inotropic effect

toxic pulmonary edema

anemia (severe form)

severe hypotension (systolic blood pressure less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg)

concomitant use of phosphodiesterase inhibitors, including sildenafil, vardenafil, tadalafil, since they potentiate the antihypertensive effect of

nitrates, hereditary galactose intolerance, lactase deficiency or glucose and galactose malabsorption syndrome

children and adolescents under 18 years of age (efficacy and safety have not been established).

Precautions: hypertrophic obstructive cardiomyopathy, constrictive pericarditis, pericardial tamponade, low filling pressure in acute myocardial infarction, left ventricular failure.

Avoid lowering systolic blood pressure below 90 mmHg. aortic and / or mitral stenosis tendency to orthostatic disorders of the vascular regulation of glaucoma (risk of increased intraocular pressure) severe renal failure liver failure (risk of methemoglobinemia) hemorrhagic stroke thyrotoxicosis of the disease, accompanied by increased intracranial pressure recently suffered traumatic brain injury.

Use during pregnancy and lactation

For safety reasons, MonochincweВ® can be used during pregnancy and lactation only as prescribed by the doctor, after a careful assessment of the benefits and possible risks, since at present there is insufficient data on the consequences of its use in pregnant and lactating women mothers.

If a nursing mother nevertheless takes MonochincweВ®, it is necessary to establish monitoring of the child for the development of possible effects from the drug.

Composition

1 tablet contains:

Active substances:

isosorbide-5-mononitrate 40 mg.

Excipients:

lactose monohydrate - 160 mg,

microcrystalline cellulose - 82.5 mg,

corn starch - 10 mg,

talcum powder - 5 mg,

magnesium stearate - 2.5 mg.

Dosage and administration

Inside, after a meal with water, without chewing.

Frequency of administration and duration of treatment are set individually.

Start therapy with a dose of 20 mg (1/2 tab.) 2 times / day.

Then gradually increase the dose to a therapeutic dose of 40 mg (1 tab.) for administration 2-3 times / day with an interval of 7-8 hours.

The maximum daily dose is 120 mg.

Side effects

When taking the drug in therapeutic doses, any significant side effects, as a rule, do not develop.

Very common ( 10%): nitrate headache may occur at the start of treatment, and usually continues within a few days with continued therapy.

Often ( 1% - <10%): after the first dose or after increasing the dose of the drug, a decrease in blood pressure and / or development of orthostatic hypotension may occur, which may be accompanied by tachycardia, dizziness, and also weakness.

From the nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment).

Rarely ( 0.1% - <1%): nausea, vomiting, a slight burning sensation of the tongue, dry mouth, redness of the face, and skin allergies may occur. A marked decrease in blood pressure, accompanied by a worsening of the symptoms of angina pectoris (a paradoxical reaction to nitrates). There have been cases of collaptoid states, sometimes with bradyarrhythmia and fainting.

Selected cases (<0.01%): exfoliative dermatitis.

Drug Interaction

When used with other vasodilators, antihypertensive agents, ACE inhibitors, beta-blockers, slow calcium channel blockers (BMCC), diuretics, antipsychotics (neuroleptics) or tricyclic antidepressants, with phosphodiesterase inhibitors, including sildenafil, vardenafil, tadalafil, as well as with ethanol may increase the antihypertensive effect of the drug Monochinkwe®.

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

Reduces the effect of vasopressors.

When combined with amiodarone, propranolol, BMCC (verapamil, nifedipine, etc.), an anti-anginal effect may be enhanced.

Under the influence of beta-blockers, alpha-blockers (dihydroergotamine) it is possible to reduce the anti-anginal effect (tachycardia and excessive decrease in blood pressure).

When combined with m-cholin blockers (atropine), the likelihood of increased intraocular pressure increases.

Adsorbents, astringent and enveloping drugs reduce the absorption of isosorbide mononitrate from the gastrointestinal tract.

The therapeutic effect of norepinephrine (norepinephrine) is reduced when co-administered with nitro compounds.

Overdose

Symptoms: decreased blood pressure with orthostatic dysregulation, reflex tachycardia and headache. Weakness, dizziness, hot flashes, nausea, vomiting and diarrhea may occur. At high doses (greater than 20 mg / kg body weight), methemoglobinemia, cyanosis, dyspnoea and tachypnea should be expected due to nitrite ions due to the metabolism of isosorbide mononitrate. Very high doses can lead to increased intracranial pressure with the onset of cerebral symptoms. In chronic overdose may increase the level of methemoglobin. although the clinical significance of this has not yet been conclusively established.

Treatment: gastric lavage, the patient should be placed in a horizontal position with legs raised. Main indicators of vital functions should be monitored and, if necessary, adjusted. Patients with pronounced arterial hypotension and / or in a state of shock should be injected fluid in exceptional cases to improve blood circulation can be infused norepinephrine (norepinephrine) and / or dopamine. The introduction of epinephrine (adrenaline) and related compounds is contraindicated.

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

vitamin C: 1 g in or in the form of sodium salt in / in.

methylene blue: up to 50 ml of 1% methylene blue solution in / in.

toluidine blue: 2-4 mg / kg body weight first / then later, if necessary, repeated injections of 2 mg / kg body weight with intervals of 1 hour

Oxygen therapy, hemodialysis, blood transfusion are also performed.

Storage conditions

Store in a dark place. inaccessible to children at a temperature not exceeding 25 РC.

Expiration

5 years.

The active substance

Isosorbide mononitrate

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