Composition
>
of 1 tab. contains:
Active ingredients:
isosorbide-5-mononitrate 40 mg.
Auxiliary substances:
microcrystalline cellulose,
corn starch,
magnesium stearate,
granulated lactose,
talc.
Pharmacological action
Monosan is an antianginal drug. Peripheral vasodilator with a predominant effect on venous vessels. It stimulates the formation of nitric oxide (an endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in the level of cGMP (a vasodilation mediator).
Reduces myocardial oxygen demand by reducing preload and afterload. It has a corona-expanding effect. Reduces blood flow to the right atrium, helps to reduce pressure in the small circle of blood circulation and regression of symptoms in pulmonary edema. Promotes redistribution of coronary blood flow in areas with reduced blood supply. Increases exercise tolerance in patients with coronary artery disease, angina pectoris.
Dilates the blood vessels of the brain, dura mater, which can be accompanied by a headache. As with other nitrates, the drug develops
cross-tolerance. After withdrawal (a break in treatment), sensitivity to the drug is quickly restored. The antianginal effect develops 30-45 minutes after taking the drug and lasts up to 8-10 hours.
Pharmacokinetics: Â
Absorption – high, bioavailability-100%. The time to reach the therapeutic concentration (100 ng / ml) is 30 minutes. TCmax – 1-1.5 h, for retard forms-8 h. Plasma protein binding-less than 4%. It undergoes denitrization to form isosorbide or combines with glucuronide. T1 / 2-5 hours is excreted by the kidneys in the form of glucuronides.
Indications
-prevention of angina attacks in patients with IHD; – chronic heart failure (as part of combination therapy);- pulmonary hypertension, pulmonary heart (as part of combination therapy).
Use during pregnancy and lactation
The use of Monosan during pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus.
Contraindications
: arterial hypotension and arterial hypovolemia (systolic blood pressure below 100 mm Hg, diastolic pressure below 60 mm Hg, central venous pressure below 4-5 mm Hg). ;- shock, vascular collapse— – left ventricular failure with low diastolic pressure;- acute myocardial infarction (with severe hypotension);— cardiac tamponade— – shock; – toxic pulmonary edema;- diseases associated with increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury);- angle-closure glaucoma— – lactation (breastfeeding);— children and adolescents under 18 years of age;- hypersensitivity to the components of the drug Monosan and to other nitrates.
With caution: with aortic and / or mitral stenosis, with a tendency to orthostatic disorders of vascular regulation, with constrictive pericarditis, in elderly patients, with severe anemia, thyrotoxicosis, with hypertrophic cardiomyopathy (possible increase in angina attacks), with liver failure (risk of developing methemoglobinemia), severe renal failure.
Side effects
From the cardiovascular system: “nitrate” headache, dizziness, transient hyperemia of the facial skin, a feeling of heat, tachycardia, a pronounced decrease in blood pressure; rarely-paradoxical increase in angina attacks, orthostatic collapse.
From the digestive system: nausea, vomiting, dry mouth, perhaps a slight burning sensation of the tongue.
From the central nervous system: stiffness, drowsiness, blurred vision, decreased ability for rapid mental and motor reactions (especially at the beginning of treatment); rarely-brain ischemia.
Allergic reactions: skin rash; rarely-exfoliative dermatitis.
Other: development of tolerance (including cross-tolerance to other nitrates).
Interaction
When used together, Monosan increases the concentration of dihydroergotamine in blood plasma.
When used in combination, barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in blood plasma.
When isosorbide mononitrate is co-administered with antihypertensive agents, peripheral vasodilators, antipsychotics (neuroleptics), tricyclic antidepressants, novocainamide, ethanol, quinidine, beta-blockers, slow calcium channel blockers, dihydroergotamine, sildenafil, it is possible to increase the hypotensive effect.
The combination of amiodarone, propranolol, slow calcium channel blockers (verapamil, nifedipine, etc. ), acetylsalicylic acid, and isosorbide mononitrate may enhance the antianginal effect.
When combined with beta-adrenostimulants, alpha-blockers, it is possible to reduce the severity of the antianginal effect (development of tachycardia, excessive decrease in blood pressure).
When combined with m-holinoblokatorami (atropine) increases the likelihood of increased intraocular pressure.
When taken simultaneously, adsorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate from the gastrointestinal tract.
How to take, course of use and dosage
Set individually depending on the severity of the disease.
The initial single dose of Monosan is 10-20 mg, the frequency of use is 1-3 times / day.
Depending on the severity of the clinical effect, from 3-5 days of therapy, a single dose of the drug can be increased to 40-60 mg with the same frequency of use.
The maximum daily dose is 80 mg.
Tablets should be taken orally after a meal, swallowed whole, with a small amount of liquid.
Overdose
Symptoms: headache, dizziness, palpitations, hyperthermia, skin hyperemia, sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnea, dyspnea, bradycardia, convulsions, visual disturbances, increased intracranial pressure, collapse, fainting, paralysis, coma.
Treatment: gastric lavage; with methemoglobinemia – inside or in / in ascorbic acid 1 g, in/in-1% solution of methylthioninium chloride (methylene blue) at a dose of 1-2 mg/kg of body weight. Symptomatic therapy for severe hypotension is intravenous phenylephrine (epinephrine and related compounds are ineffective).
Special instructions
Monosan is not used to relieve angina attacks.
During therapy, it is necessary to monitor blood pressure, heart rate.
If it is necessary to use the drug against the background of arterial hypotension, you should simultaneously take drugs that have a positive inotropic effect.
Frequent use and use in high doses may cause the development of tolerance; in this case, after 3-6 weeks of regular use, it is recommended to cancel Monosan for 24-48 hours or break therapy for 3-5 days with the replacement of the drug for this time with other antianginal drugs.
It is necessary to avoid abrupt discontinuation of the drug and reduce the dose gradually.
Influence on the ability to drive motor vehicles and manage mechanisms
During the period of use of the drug, the patient’s psychomotor reactions may decrease, so you should drive vehicles with caution and engage in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Form of production
Monosan tablets are white or almost white in color, round, flat, with a risk on one side.
Active ingredient
Isosorbide Mononitrate
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor
Indications
Heart Failure, Angina
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