Monochinqué retard, 50 mg capsules 30 pcs

Pharmacodynamics

Peripheral vasodilator with predominant effect on the venous vessels. Antianginal drug.

Limits preload (by enlarging the peripheral veins) and postload (by reducing PPS), reduces myocardial oxygen demand. Dilates coronary arteries and improves coronary blood flow, promotes its redistribution to ischemic areas, reduces left ventricular end-diastolic volume and reduces systolic stress on its walls. Increases exercise tolerance in patients with coronary artery disease, reduces the pressure in the small circle of the circulation.

At the molecular level it acts through the formation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP), reducing the concentration of calcium in smooth muscle cells.

The special dosage form of Monocinqué® retarded release of the active ingredient provides therapeutic concentrations of the drug in the blood within 24 hours after taking a single daily dose.

The drug is recommended for long-term therapy.

Pharmacokinetics

Isosorbide-5-monononitrate is quickly and completely absorbed from the GI tract after oral administration. Bioavailability of the drug when administered orally is from 90 to 100%. Cmax in blood plasma is reached 1-1.5 hours after intake.

It is not subjected to the effect of “first passage” through the liver.

Elimation

Isosorbide-5-monononitrate is excreted by the kidneys exclusively as metabolites. Approximately 2% is excreted unchanged.

The T1/2 is approximately 5 h, which is approximately 8 times higher than that of isosorbide dinitrate.

Indications

Prevention and long-term therapy of angina pectoris of III-IV functional classes;
rehabilitation treatment after myocardial infarction;
treatment of chronic heart failure (as part of combination therapy).

Pharmacological effect

Pharmacodynamics

Peripheral vasodilator with a predominant effect on venous vessels. Antianginal drug.

Reduces preload (due to dilation of peripheral veins) and afterload (due to decreased peripheral vascular resistance), reduces myocardial oxygen demand. Dilates the coronary arteries and improves coronary blood flow, promotes its redistribution to ischemic areas, reduces the end-diastolic volume of the left ventricle and reduces the systolic tension of its walls. Increases tolerance to physical activity in patients with coronary artery disease, reduces pressure in the pulmonary circulation.

At the molecular level, it acts through the formation of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP), reducing the concentration of calcium in smooth muscle cells.

The special dosage form of Monocinque® retard with sustained release of the active substance provides a therapeutic concentration of the drug in the blood within 24 hours after taking a single daily dose.

The drug is recommended for long-term therapy.

Pharmacokinetics

Absorption and Metabolism

After oral administration, isosorbide-5-mononitrate is quickly and completely absorbed from the gastrointestinal tract. The bioavailability of the drug when taken orally ranges from 90 to 100%. Cmax in blood plasma is achieved 1-1.5 hours after administration.

It is not subject to the “first pass” effect through the liver.

Removal

Isosorbide-5-mononitrate is excreted by the kidneys exclusively in the form of metabolites. Approximately 2% is excreted unchanged.

T1/2 is approximately 5 hours, which is approximately 8 times higher than that of isosorbide dinitrate.

Special instructions

The drug is not used to relieve angina attacks.

For arterial hypertension, the drug should be used only under the supervision of a physician.

The drug is prescribed both as monotherapy and in combination with beta-blockers, calcium channel blockers, ACE inhibitors, cardiac glycosides or diuretics.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

When taking the drug, the ability to concentrate and the speed of psychomotor reactions may decrease, and therefore driving and engaging in other potentially hazardous activities is not recommended.

Active ingredient

Isosorbide mononitrate

Composition

Active ingredients:

isosorbide-5-mononitrate 50 mg.

Excipients:

sucrose,

corn starch,

ethylcellulose,

stearic acid,

talc,

red dye 4R (E124),

quinoline yellow (E104),

titanium dioxide,

gelatin.

Contraindications

Hypersensitivity to organic nitrates;
acute circulatory disorders (shock, vascular collapse);
hemorrhagic stroke;
acute stage of myocardial infarction;
simultaneous use of phosphodiesterase inhibitors (sildenafil);
severe arterial hypotension (systolic blood pressure <90 mmHg, diastolic blood pressure <60 mmHg); conditions after traumatic brain injury; angle-closure glaucoma; deficiency of glucose-6-phosphate dehydrogenase; age up to 18 years.

Side Effects

When taking Monocinque® retard at the recommended dose, no side effects are described.

However, as with the use of other nitrates, it is possible:

From the cardiovascular system: at the beginning of treatment – a “nitrate” headache, which usually decreases after a few days with continued therapy; after the first dose or after increasing the dose – arterial (including orthostatic) hypotension, accompanied by tachycardia, dizziness, weakness.

From the digestive system: very rarely – nausea, vomiting.

Dermatological reactions: very rarely – facial redness and allergic skin reactions.

Interaction

When taking Monocinque® retard simultaneously with other vasodilators, antihypertensive drugs, beta-blockers, calcium channel blockers, antipsychotic drugs, tricyclic antidepressants, sildenafil, ethanol, the hypotensive effect of Monocinque® retard may be potentiated.

Overdose

No cases of overdose have been reported.

However, if symptoms of overdose occur, generally accepted measures are recommended: induce vomiting, rinse the stomach.

It is necessary to monitor whether the patient is taking any other medications at the same time and monitor hemodynamic parameters.

Storage conditions

Store in a place protected from light, out of reach of children, at a temperature not exceeding 25°C.

Shelf life

3 years.

Manufacturer

A. Menarini Manufacturing Logistics and Services S, Italy