Instructions for Monosan tablets 20 mg No. 30
Composition
active ingredient: isosorbide mononitrate;
1 tablet contains isosorbide mononitrate diluted, equivalent to isosorbide mononitrate 20 mg or 40 mg;
excipients: lactose monohydrate, microcrystalline cellulose, corn starch, talc, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: white tablets, flat-cylindrical in shape, with a bevel and a score, with a diameter of about 7 mm (20 mg tablets) and about 9 mm (40 mg tablets).
Pharmacotherapeutic group
Drugs affecting the cardiovascular system. Vasodilators used in cardiology. Organic nitrates. Isosorbide mononitrate.
ATX code C01D A14.
Pharmacological properties
Pharmacodynamics.
Isosorbide mononitrate (isosorbide-5-mononitrate) is a metabolite of isosorbide dinitrate, causing relaxation of vascular smooth muscle and vasodilation due to the formation of nitric oxide. The effect of isosorbide dinitrate occurs more quickly than that of isosorbide mononitrate.
Isosorbide mononitrate simultaneously dilates peripheral veins and arteries, which leads to an increase in venous capacity and a decrease in venous return to the heart, and, as a result, to a reduction in ventricular end-diastolic pressure and preload. The effect on arterial vessels leads to a decrease in their systemic resistance (afterload), facilitating the work of the heart. The simultaneous effect on pre- and afterload leads to a decrease in myocardial oxygen consumption. In addition, isosorbide mononitrate causes a redistribution of blood flow to the subendocardial layers, when coronary blood flow is partially reduced due to the presence of atherosclerotic plaques. The dilation caused by nitrates improves perfusion of the post-stenotic area of the myocardium. Nitrates eliminate eccentric coronary stenosis, reducing venous spasms. Nitrates improve hemodynamics at rest and during exercise in patients with congestive heart failure. As a result of reduced oxygen demand and increased oxygen delivery, the area of damaged myocardium is limited. Isosorbide mononitrate affects other organs and systems: it relaxes bronchial muscles, muscles of the gastrointestinal, biliary and urinary tracts. The effect of the drug appears after 20 minutes and lasts for 8 hours.
Isosorbide mononitrate slightly inhibits platelet aggregation and reduces intraplatelet thromboxane synthesis.
The drug increases exercise tolerance in patients with ischemic heart disease.
Pharmacokinetics.
The maximum concentration of Monosan in blood plasma after oral administration is reached after 1 hour. Bioavailability is almost 100%. During the "first pass" through the liver, isosorbide mononitrate is not subject to biological transformation, does not bind to plasma proteins. The half-life is 4-5 hours. The pharmacokinetics of isosorbide mononitrate does not depend on the presence of cardiac, renal and hepatic insufficiency.
Isosorbide mononitrate is metabolized in the liver to isosorbide and isosorbide-5-mononitrate-2-glucuronide. Both metabolites are pharmacologically inactive and are excreted by the kidneys. Only 2% of the drug is excreted in the urine unchanged.
Indication
o Prevention of angina pectoris.
o Congestive heart failure.
Contraindication
o Hypersensitivity to the active substance or to any component of the drug.
o Acute circulatory failure, severe arterial hypotension (systolic blood pressure below
90 mm Hg) or hypovolemia, collapse; cardiogenic shock if not adequately
high end-diastolic pressure in the left ventricle by using intra-aortic
counterpulsation or drugs with a positive inotropic effect.
o Acute myocardial infarction with low left ventricular filling pressure.
o Severe anemia.
o Toxic pulmonary edema.
o Recent traumatic brain injury or cerebral hemorrhage, increased
intracranial pressure.
o Glaucoma.
o Increased sensitivity to nitrates.
o Concomitant use with sildenafil and other phosphodiesterase inhibitors.
Interaction with other medicinal products and other types of interactions
Phosphodiesterase inhibitors (e.g. sildenafil), neuroleptics, tricyclic antidepressants and vasodilators: potentiate the hypotensive effect of nitrates, therefore they should not be used simultaneously with Monosan.
Noradrenaline, acetylcholine, histamine: their effects are reduced when used simultaneously with nitrates.
Alcohol, opioid analgesics, vasodilators and drugs that lower blood pressure (such as beta-blockers, calcium antagonists, vasodilators): their hypotensive effect may be enhanced.
Sympathomimetics: may reduce the antianginal effect of nitrates.
Dihydroergotamine: Nitrates may increase plasma levels and enhance its hypertensive effect.
Heparin: increased antiplatelet effect when taken simultaneously with Monosan.
Application features
The use of isosorbide mononitrate may lead to transient hypoxia and ischemia in patients with coronary heart disease due to relative redistribution of blood flow to areas of alveolar hypoventilation.
Use with caution:
in hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, low cardiac filling pressure (e.g., acute myocardial infarction or left ventricular failure), aortic or mitral stenosis; in severe renal and/or hepatic dysfunction; in patients with hypothyroidism, hypothermia, malnutrition; in elderly patients (as they may be more sensitive to the hypotensive effect of nitrates); in patients prone to arterial hypotension, orthostatic dysfunction (a decrease in systolic blood pressure of 10-25 mm Hg below 90 mm Hg that occurs when changing body position), surgical interventions. A decrease in systolic blood pressure below 90 mm Hg should be avoided.
If the recommended interval between doses is not observed, with prolonged use of high doses, nitrate tolerance may develop as a result of depletion of tissue reserves of sulfhydryl groups. This can be avoided by adhering to a regimen with a nitrate-free period. Also, to prevent the development of tolerance, use the introduction of sulfhydryl groups into the body using, for example, acetylcysteine, methionine or captopril.
Cross-tolerance to other nitrates may occur. To prevent weakening of the effect of the drug or complete ineffectiveness of the drug, it is recommended to avoid continuous use of high doses for a long time.
After prolonged therapy with high doses, the drug should be discontinued gradually to prevent the recurrence of angina symptoms.
When taking high doses, the development of methemoglobinemia is possible.
Taking isosorbide mononitrate may affect the results of colorimetric cholesterol determination.
Nitrates may increase urinary catecholamine concentrations (epinephrine/adrenaline/norepinephrine) and urinary vanillyl-mandelic acid.
During treatment with the drug, alcohol should not be consumed.
The drug contains lactose, so it should not be prescribed to patients with lactase deficiency, galactosemia or glucose-galactose malabsorption syndrome.
Use during pregnancy or breastfeeding
The drug affects the hemodynamics of the fetus/child, therefore it is contraindicated during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, a decrease in the speed of psychomotor reactions and dizziness may occur, which must be taken into account when driving vehicles or other mechanisms.
Method of administration and doses
The drug should be taken orally before meals, without chewing and with sufficient liquid.
The dose and frequency of administration are set individually by the doctor. In order to achieve the maximum therapeutic effect, individual dosage of the drug is recommended depending on the patient's condition, his reaction to the drug and tolerability.
Start treatment with low doses, which can be increased if necessary during treatment. The recommended dose is 40 mg twice a day. In most cases, prescribe 20 mg twice a day or 40 mg twice a day in the morning and afternoon.
In order to prevent the development of tolerance to nitrates (with any dosage regimen), it is recommended to take the second tablet no earlier than 8 hours after taking the first.
When treating angina with frequent nocturnal attacks, the drug should be used in the morning and immediately before bedtime.
Hemodynamic monitoring is important for determining individual dosage.
The daily dose, depending on the severity of the disease, can reach 120 mg (maximum daily dose), divided into 3 doses.
Children
The drug should not be used in children.
Overdose
Symptoms: decrease in blood pressure below 90 mm Hg, pallor, increased sweating, weak pulse, tachycardia, dizziness upon standing, headache, feeling of heat or chills, flushing, feeling of fear, weakness, loss of consciousness, vertigo, orthostatic hypotension, cerebral symptoms, nausea, vomiting, diarrhea, methemoglobinemia, seizures, visual impairment, increased intracranial pressure, cyanosis, dyspnea, tachypnea, shortness of breath, coma.
In severe cases, administer dopamine and sympathomimetics. In the event of methemoglobinemia, administer ascorbic acid 1 g orally, 1% methylene blue intravenously, toluidine blue 2-4 mg/kg body weight intravenously, artificial ventilation of the lungs, and, if necessary, perform blood exchange transfusion. Hemodialysis is indicated.
Adverse reactions
Nervous system: headache, which gradually decreases over several days, but may be severe and persistent; inattention, dizziness, drowsiness and weakness, motor restlessness, syncope.
Cardiovascular system: arterial (including orthostatic) hypotension, collapse with cardiac arrhythmia and bradycardia, worsening of angina symptoms, bradyarrhythmia, reflex tachycardia, transient hypoxemia from myocardial hypoxia in patients with ischemic heart disease.
On the part of the digestive tract: nausea, vomiting, diarrhea, dyspepsia.
Skin and subcutaneous tissue disorders: allergic skin reactions (including rash, itching, exfoliative dermatitis), dilation of skin vessels with redness, pallor and increased sweating.
On the part of the immune system: hypersensitivity reactions are possible in patients with individual intolerance to any component of the drug.
Others: facial flushing, tinnitus, asthenia.
Cases of tolerance to the drug, including cross-tolerance to other organic nitrates, have been observed. To prevent weakening of the effect of the drug or complete ineffectiveness of the drug, it is recommended to avoid continuous use of high doses for a long time.
Expiration date
5 years.
Do not use after the expiration date.
Storage conditions
Store in the original packaging out of the reach of children at a temperature not exceeding 25 ºС.
Packaging
20 mg tablets: 10 tablets in a blister, 3 blisters in a cardboard box.
40 mg tablets: 10 tablets in a blister, 3 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
PRO.MED.CS Prague a.t. (PRO.MED.CS Prahа as).
Location of the manufacturer and its business address
Telčska 1, 140 00 Prague 4, Czech Republic
(Telsska 1, 140 00 Praha 4, Czech Republic).
