Monosan 20mg No. 30 tablets

Monosan ® /Monosan®

International nonproprietary name (INN):

isosorbide mononitrate

Dosage form

Pills.

Compound

1 tablet contains:

Active substance

: isosorbide-5-mononitrate 20 or 40 mg (trituration of isosorbide-5-mononitrate and monohydralactose in a ratio of 80%:20% 25 mg or 50 mg).

Excipients

: microcrystalline cellulose, corn starch, magnesium stearate, granulated lactose, talc.

Description

Round, flat tablets of white or almost white color with a score line on one side.

Pharmacotherapeutic group: Vasodilating agent, nitrate.

ATX code: C01DA14.

pharmachologic effect

The active component is a peripheral vasodilator (“vaso” - vessels + “dilator” - dilator), which acts primarily on venous vessels. The drug can stimulate the production of a special relaxing endothelial factor - nitric oxide in the vascular endothelium.

Under the influence of this factor, the intracellular enzyme guanylate cyclase is activated, which leads to an increase in the vasodilating mediator - cGMP.

As a result, the need of myocardial cells for O2 decreases, which is explained by a decrease in afterload and preload . pronounced coronary-dilating effect .

The active substance can reduce blood flow to the right atrium, reducing pressure in the pulmonary circulation and reducing the severity of negative symptoms during pulmonary edema . In areas with reduced blood circulation, a redistribution of coronary blood flow is noted under the influence of Monosan.

In patients who suffer from angina pectoris , heart disease tolerance (resistance) to physical activity increases markedly. Headaches often occur with the use of nitrates, which is explained by the ability of medications to expand the lumens of blood vessels in the dura mater and brain.

Monosan is able to reduce the rate of intraplatelet synthesis of Thx, as well as inhibit platelet aggregation. Cross tolerance is characteristic. Sensitivity to the active substance is restored quite quickly after a break in treatment.

Pharmacological properties of the drug Monosan

Monosan (isosorbide-5-mononitrate) is an organic nitrate, one of the metabolites of isosorbide dinitrate. Monosan increases the content of nitric oxide in the endothelium, stimulates guanylate cyclase and the formation of cGMP. The antianginal effect is associated with a decrease in the myocardial oxygen demand due to a decrease in preload (the drug causes expansion of the peripheral veins, due to which blood is retained in the volumetric bed; the return of blood to the heart is reduced, as a result of which the pressure in the pulmonary artery decreases, the pulmonary circulation is partially unloaded and decreases end-diastolic pressure in the left ventricle) and afterload (dilation of the arteries leads to a decrease in peripheral vascular resistance), as well as with direct vasodilation of the coronary arteries. In addition, a decrease in preload reduces left ventricular wall tension, which leads to an increase in subendocardial and intramural circulation as a result of a decrease in end-diastolic and end-systolic pressure in the left ventricle. Under the influence of the drug, cardiac output increases in patients with heart failure in response to a decrease in resistance in the arterial system (however, in the absence of heart failure, cardiac output does not change and may even decrease slightly). Monosan inhibits platelet aggregation, reduces intraplatelet synthesis of thromboxane, and increases exercise tolerance in patients with coronary artery disease. The maximum concentration of Monosan in the blood plasma after oral administration is achieved after 1 hour. Bioavailability is almost 100%. When isosorbide-5-mononitrate first passes through the liver, no biological transformation occurs; does not bind to blood plasma proteins. The half-life is 4–6 hours. The pharmacokinetics of isosorbide-5-mononitrate does not depend on the presence of cardiac, renal and liver failure. Monosan is metabolized in the liver to isosorbide and mononitrate-2-glucuronide. Both metabolites are pharmacologically inactive and are excreted by the kidneys. 2% of the drug is excreted unchanged in the urine.

Pharmacodynamics and pharmacokinetics

After oral administration, the antianginal effect is registered within 30-45 minutes and can last for almost 10 hours. The active substance is quickly and completely absorbed from the lumen of the digestive tract. Isosorbide mononitrate has a high bioavailability rate of 100%, which is explained by the absence of a first-pass effect through the hepatic system.

The Tmax indicator after administration is 1 hour. Plasma concentration varies only slightly due to individual differences. The individual level of the active substance in the blood plasma is 100 mg/ml. There is no binding to plasma proteins. Pharmacokinetics in dosages from 10 to 80 mg are characterized by linearity.

metabolized in the renal system, in contrast to Isosorbide dinitrate , which is metabolized in the hepatic system. As a result of metabolic reactions, 3 components are formed: 2 isosorbide-5-mononitrate glucuronides and isosorbide. The half-life is 4-5 hours. 2% is excreted unchanged through the renal system, 98% in the form of glucuronic metabolites. The renal clearance rate is 115 ml/min. The pharmacokinetics of the drug does not change significantly with renal and hepatocellular failure .

Overdose of the drug Monosan, symptoms and treatment

It is observed extremely rarely. Due to the fact that the nitrate ion interacts with hemoglobin, even after the use of organic nitrates in high doses, the concentration of nitrate ions in the blood plasma remains low enough that severe methemoglobinemia can develop. Symptoms : reflex tachycardia, weakness, dizziness, nausea, vomiting, diarrhea, flushing, headache, feeling of fear, orthostatic hypotension, in severe cases - cyanosis. Treatment: symptomatic - oxygen inhalation, raising the lower extremities upward, in case of taking a large number of tablets - gastric lavage. In the presence of methemoglobinemia, which is manifested by cyanosis, slow intravenous administration of methylene blue at a dose of 1 mg/kg body weight.

Contraindications

• vascular collapse;
• shock;
• arterial hypovolemia and arterial hypotension (decrease in systolic blood pressure to 100 mm Hg; drop in diastolic blood pressure below 60 mm Hg; decrease in venous central pressure to 4-5 mm Hg);
• cardiac tamponade;
• acute stage of myocardial infarction (with severe arterial hypotension);
• left ventricular failure and low diastolic blood pressure;
• toxic pulmonary edema;
• breast-feeding;
• angle-closure form of glaucoma ;
• diseases that provoke an increase in intracranial pressure (traumatic brain injury, hemorrhagic stroke and others);
• individual hypersensitivity;
• Age limit: up to adulthood.

Relative contraindications:

• constrictive pericarditis;
• tendency to orthostatic disorders of vascular regulation;
• mitral stenosis;
• elderly age;
• severe renal failure;
• liver failure (the risk of developing methemoglobinemia increases);
• hypertrophic cardiomyopathy (increased angina attacks);
• thyrotoxicosis;
• severe anemia;
• aortic stenosis.

Contraindications to the use of the drug Monosan

Hypersensitivity to nitrates, shock states, myocardial infarction in the acute period with low end-diastolic pressure, arterial hypotension (systolic pressure ≤100 mm Hg, diastolic pressure ≤60 mm Hg, central venous pressure ≤4–5 mmHg), cardiac tamponade, inadequate cerebral perfusion. During pregnancy and breastfeeding. Age up to 15 years. Conditions accompanied by increased intracranial pressure (including hemorrhagic stroke, after a head injury), with angle-closure glaucoma with high intraocular pressure.

Side effects

Digestive tract:

• burning sensation in the tongue area;
• vomit;
• feeling of dry mouth;
• nausea.

The cardiovascular system:

• tachycardia;
• feeling of heat in the body;
• facial skin hyperemia;
• nitrate headaches;
• pronounced drop in blood pressure ;
• dizziness;
• orthostatic collapse;
• increased frequency and intensification of angina attacks (a kind of paradoxical reaction).

Nervous system:

• slowing down the speed of motor and mental reactions;
• increased drowsiness ;
• stiffness;
• blurred visual perception.

Other reactions:

• establishment of tolerance (cross form - in relation to other nitrates);
• exfoliative dermatitis;
• specific skin rashes.

Side effects of the drug Monosan

headache, dizziness, arterial hypotension, orthostatic collapse, tachycardia, methemoglobinemia, exacerbation of glaucoma, increased intracranial pressure, changes in the speed of mental reactions, dry mouth, nausea, vomiting, flushing of the facial skin, general weakness, fatigue are the most typical side effects. Sometimes, with a sharp decrease in blood pressure, paradoxical “nitrate” reactions are possible - increased attacks of angina. In patients predisposed to allergic reactions, rash, itching, skin hyperemia, and exfoliative dermatitis are possible. Tolerance often develops.

Monosan, instructions for use (Method and dosage)

Tablets are used only per os. The manufacturer recommends taking the tablets with water and swallowing them whole. Assessing the severity of the underlying disease and concomitant pathology, the treating doctor selects a treatment regimen.

Treatment begins with taking 10-20 mg of Monosan 1-3 times a day. From the 3-4th day of treatment, the dosage regimen is adjusted depending on the clinical effect, possibly increasing to 20-40 mg twice a day. In some cases, the amount of medication is increased to 80 mg/day - the maximum daily dosage.

Use of the drug Monosan

Adults and teenagers over 15 years old. The doctor determines the dose and frequency of administration individually. Treatment is started with low doses (10–20 mg 1–2 times a day), which are increased during treatment if necessary. In most cases, 20 or 40 mg are prescribed 2 times a day. If necessary, the single dose can be increased to 40–60 mg (in special cases up to 80 mg) at the same frequency of administration. The maximum single dose is 80 mg, the maximum daily dose is 160 mg. The tablets can be divided in half without crushing, washed down with a sufficient amount of liquid.

Overdose

Fainting, collapse, dizziness, redness of the skin, dyspnea, hyperpnea, methemoglobinemia , diarrhea syndrome , headaches, lethargy, weakness, reflex tachycardia, hyperthermia, visual disturbances, paralysis, increased intracranial pressure , convulsions, coma, vomiting, nausea, increased sweating.

General recommendations: place the patient in a horizontal position, perform gastric lavage procedures, prescribe enterosorbent medications , monitor vital signs, and correct them if necessary.

Specific therapy: in case of shock and severe arterial hypotension, blood volume is replenished. Dopamine and/or Norepinephrine infusion is performed in exceptional cases to improve blood circulation.

Adrenaline , Epinephrine and other related compounds is unacceptable When diagnosing methemoglobinemia hemodialysis , oxygen therapy , exchange blood transfusion are performed, and ascorbic acid in the form of sodium salt.

Interaction

The active substance can increase the concentration of dihydroergotamine in the blood. A decrease in the effectiveness of vasopressor drugs has been recorded. Barbiturates are able to reduce the concentration of isosorbide and accelerate its biological transformation.

Potentiation of the hypotensive effect of isosorbide mononitrate is recorded with simultaneous treatment with Tadalafil , tricyclic antidepressants, antipsychotics, Vardenafil , Sildenafil , diuretics, beta-blockers, vasodilators, PDE-5 inhibitors.

The antianginal effect is enhanced by treatment with Propranolol , Amiodarone and drugs from the CCB group ( Nifedipine , Verapamil ). When interacting with nitro compounds, the therapeutic effect of Norepinephrine (Norepinephrine) is significantly reduced.

Enveloping medications, astringents and adsorbents reduce the absorption rate of isosorbide. M-anticholinergic agents ( Atropine ) can increase intraocular pressure during simultaneous therapy with nitrates. A decrease in the severity of the antianginal effect (fall in blood pressure, increase in pulse) is observed during treatment with alpha-blockers and beta-blockers.

Interactions of the drug Monosan

When used simultaneously with antihypertensive drugs, antidepressants (MAO inhibitors), drugs containing ethyl alcohol, and dihydroergotamine, the hypotensive effect of Monosan may be enhanced. Concomitant use with sildenafil and other PDE inhibitors is contraindicated due to the risk of uncontrolled hypotension. Opioid analgesics significantly enhance the analgesic effect of Monosan in patients during the acute period of myocardial infarction. When taking heparin and Monosan simultaneously, the antiplatelet effect is enhanced. Atropine and other M-anticholinergic drugs, as well as sympathomimetics, reduce the effectiveness of Monosan.

special instructions

The medication is not used to relieve angina attacks. Monitoring blood pressure and heart rate is mandatory. If the drug must be used against the background of arterial hypotension, then at the same time it is necessary to prescribe drugs that have a positive inotropic effect.

With frequent use of the drug in high doses, tolerance develops. In such cases, after 3-6 weeks of therapy, a temporary break of 24-48 hours is required, or for 3-5 days with the prescription of other antianginal drugs.

The dosage reduction should be done gradually. The same applies to drug withdrawal; the dose is reduced in stages. Drinking alcohol-containing drinks is prohibited. The drug can slow down the speed of motor and mental reactions, which can affect the control of vehicles and complex mechanisms.

Special instructions for the use of the drug Monosan

Psychomotor reactions may be slowed down, which should be taken into account when driving vehicles and engaging in potentially hazardous activities. Caution should be used in patients with low body weight (dystrophy), cerebrovascular accident, increased intracranial pressure, severe cerebral atherosclerosis, closed-angle glaucoma, severe anemia, severe liver dysfunction (due to the threat of methemoglobinemia), severe renal dysfunction. , patients with hyperthyroidism, with aortic or mitral stenosis, with hypertrophic cardiomyopathy, patients prone to orthostatic disorders of circulatory regulation. Not prescribed during the acute period of myocardial infarction and to eliminate acute attacks of angina. Monosan does not affect blood glucose levels, so it can be prescribed for diabetes. With prolonged use of Monosan, tolerance may develop. There is no experience with the use of the drug during pregnancy, breastfeeding, or in children (clinical trials have not been conducted).

Analogues of Monosan

Level 4 ATC code matches:
Nitrospray

Nitroglycerine

Efox

Nitromint

Pectrol

Isoket

Erinite

Cardiket

Sustak Forte

Nitrosorbide

• Monocinque;
• Cardiket;
• Isoket;
• Pectrol;
• Efox.

Reviews about Monosan

Regular use of the drug can significantly reduce the frequency of angina attacks. Patients note that the severity of attacks of chest pain during treatment is significantly reduced, and tolerance/resistance to physical activity also increases.

of breath decreases , the feeling of lack of oxygen disappears, and improves the quality of life. The drug is well tolerated and rarely causes negative side effects described in the corresponding section.

Monosana price, where to buy

In Russia, the drug costs about 100 rubles.

The cost of the medication varies depending on the dosage and pharmacy chain.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Monosan tablets 40 mg 30 pcs. Pro.Med.Cs
  150 rub. order
• Monosan tablets 20 mg 30 pcs. Pro.Med.Cs

  84 rub. order

Pharmacy Dialogue

• Monosan (tab. 40 mg No. 30) Pro.Med.Cs.

  146 RUR order

• Monosan (tab. 20 mg No. 30) Pro.Med.Cs.

  78 RUR order

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PaniPharmacy

• Monosan tablets Monosan tablets.
  40 mg No. 30, PRO.MED.CS Praha 116 UAH. order
• Monosan tablets Monosan tablets. 20 mg No. 30, PRO.MED.CS Praha

  76 UAH order

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