Monochinqué, tablets 40 mg 30 pcs

Pharmacodynamics

Peripheral vasodilator with predominant effect on the venous vessels. It has a vasodilator and antianginal action.

Limits preload (due to the expansion of peripheral veins) and postload (due to the reduction of total peripheral vascular resistance), reduces myocardial oxygen demand, dilates coronary arteries and improves coronary blood flow, promotes its redistribution in ischemic areas, reduces left ventricular end diastolic volume and reduces systolic tension of its walls. Increases exercise tolerance in patients with coronary artery disease, reduces the pressure in the small circle of the circulation.

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

At a molecular level, nitrates act by producing nitric oxide (NO) and cyclic guanosylmonophosphate (cGMP), which is considered a mediator of relaxation. When administered orally, isosorbide-5-monononitrate has an antianginal effect as early as 30 minutes and lasts for 2-6 hours.

Pharmacokinetics

It is quickly and completely absorbed after oral administration. Bioavailability is 90 to 100%. The maximum concentration in plasma is reached after approximately 1-1.5 hours.

Therapeutic concentration of isosorbide-5-monononitrate in blood is reached after 30 minutes and is 250 ng/ml, during the 4th hour – 414 ng/ml, during the 12th hour -199 ng/ml (i.e. the concentration drop is slow). Isosorbide-5-mononitrate is almost completely metabolized in the liver, and undergoes a “first pass” effect through the liver (in contrast to isosorbium dinitrate). Metabolites are pharmacologically inactive.

Isosorbide-5-monononitrate is excreted by the kidneys almost exclusively as metabolites. Approximately 2% is excreted unchanged. The elimination 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 has been described. To prevent reduction or loss of efficacy, continuous administration of high doses of the drug should be avoided.

Indications

Prevention of angina attacks in patients with CHD, including after myocardial infarction.

The treatment of chronic heart failure (as part of combination therapy).

Active ingredient

Composition

Active ingredients:

Isosorbide-5-monononitrate 40 mg.

Auxiliary substances:

Lactose monohydrate – 160 mg,

Microcrystalline cellulose – 82.5 mg,

How to take, the dosage

Overly with water after a meal, without chewing.

Frequency of administration and duration of treatment are determined individually.

It is reasonable to start therapy with a dose of 20 mg (1/2 tablet) 2 times a day.

Then gradually increase the dose to a therapeutic dose of 40 mg (1 tablet) per administration 2-3 times/day at 7-8 hour intervals.

The maximum daily dose is 120 mg.

Interaction

The hypotensive effect is enhanced by other vasodilators, antihypertensive drugs, beta-adrenoblockers, calcium channel blockers, antipsychotics, phosphodiesterase inhibitors (sildenafil), alcohol.

Special Instructions

Monocinqué® should not be used to control acute attacks of angina pectoris and acute myocardial infarction.

The BP and HR should be monitored during therapy.

Abrupt withdrawal of the drug should be avoided (the dose should be reduced gradually).

Tolerance to Monocinqua® or cross-tolerance to other nitro compounds (decreased efficacy of the drug due to prior use of other nitro compounds) may develop. To prevent the development of tolerance to the effect of Monochinqua® , its continuous administration in high doses should be avoided.

Patients with circulatory palpitations may develop symptoms of acute circulatory failure already on the first administration of the drug.

“Nitrate” headaches can be largely prevented by taking 1/2 tablet at the beginning of therapy. Monocinqué® in the morning and evening.

Ethanol use should be avoided during treatment with the drug.

Impact on the ability to drive vehicles and other mechanisms requiring high concentration

At the time of treatment, it is not recommended to drive vehicles and engage in other potentially dangerous activities requiring rapid psychomotor reaction.

Contraindications

Hypersensitivity (including to other organic nitrates), acute myocardial infarction, acute circulatory disorders (shock, collapse), hemorrhagic stroke, severe arterial hypotension (less than 90/60 mm Hg). st), concomitant use of sildenafil phosphodiesterase inhibitor (Viagra), condition after craniocerebral trauma, closed-angle glaucoma, children under 18 years of age.

Side effects

Headache (at the beginning of treatment; with continuation of therapy – decreases); after the first administration – decrease of BP and/or development of orthostatic hypotension (accompanied by tachycardia, dizziness, weakness).

very rarely – nausea, vomiting, facial redness, skin allergic reactions.

Overdose

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

Treatment: Gastric lavage, patient should be placed in a horizontal position with elevated legs. Basic vital signs should be monitored and corrected if necessary. Patients with severe arterial hypotension and/or in a state of shock should be given fluids; in exceptional cases, infusions of noradrenaline (norepinephrine) and/or dopamine may be given to improve blood circulation. Administration of epinephrine (adrenaline) and related compounds is contraindicated.

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

Oxygen therapy, hemodialysis, exchange blood transfusions are also carried out.

Similarities