It stimulates the formation of nitric oxide (endothelium-derived relaxing factor) in the vascular endothelium, causing intracellular activation of guanylate cyclase, resulting in an increase in the cGMP (vasodilation mediator). It reduces myocardial oxygen demand by reducing preload and afterload. It has koronarorasshiryayuschee action. Reduces blood flow to the right atrium, it helps reduce the pressure in the pulmonary circulation and the regression of symptoms of pulmonary edema. Promotes redistribution of coronary blood testosterone propionate 100mg flow in the area of reduced circulation. It increases exercise tolerance in patients with ischemic heart disease (IHD), angina pectoris. It extends the vessels of the brain, the dura mater, which may be accompanied by headache. It inhibits platelet aggregation, reduces the synthesis of thromboxane Thrombocyte. As to other nitrates cross-tolerance develops.After the abolition of (treatment interruption) sensitivity to it recovers quickly. Antianginal effect occurs within 30-45 minutes after ingestion and lasts up to 8-10 hours.
After oral administration of isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract (GIT). It has high bioavailability – about 100%, since there is no effect of “first pass” through the liver. The maximum concentration in plasma after oral administration is achieved within hour. Individual differences in plasma concentration after oral administration is small. The effective level of isosorbide mononitrate in the blood of about 100 mg / mL. The drug does not bind to plasma proteins.Pharmacokinetics after doses of 10-80 mg is linear, and, unlike the isosorbide dinitrate is not metabolized in the liver and kidney, where isosorbide and formed two-glucuronide isosorbide 5 -mononitrata. The half-life is about 4-5 hours. It reports the news, mainly in the form of glucuronic metabolite, 2% – unchanged. The renal clearance of the drug 115 ml / min. When hepatocellular and renal failure pharmacokinetics of isosorbide mononitrate are not significantly altered.
- Ischemic heart disease: prevention of angina attacks;
- Chronic heart failure (in combination therapy);Contraindications
- Hypersensitivity to organic nitrates or other ingredients;
- Acute circulatory disorders (shock, circulatory collapse);
- Cardiogenic shock, if you do not provide a sufficiently high end-diastolic pressure in the left ventricle through the use of intra-aortic counterpulsation or by introducing tools that have a positive inotropic effect;
- Toxic pulmonary edema;
- Severe hypotension (systolic blood pressure less than 100 mmHg, diastolic blood pressure less than 60 mmHg)
- Simultaneous administration of phosphodiesterase-5 inhibitors including sildenafil, vardenafil, tadalafil, since they potentiate the effect of nitrates antihypertensive;
- Hereditary galactose intolerance, testosterone propionate 100mg lactase deficiency or malabsorption syndrome of glucose and galactose;
- Age 18 years (effectiveness and safety have been established).Carefully
- Hypertrophic cardiomyopathy, constrictive pericarditis, pericardial tamponade;
- Low filling pressure in acute myocardial infarction, left ventricular failure. There should be no reduction in systolic blood pressure less than 90 mm Hg. v.).
- The aortic and / or mitral stenosis;
- The tendency to orthostatic vascular disorders of regulation;
- Angle-closure glaucoma;
- Severe anemia;
- Diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury);
- Severe renal failure;
- Liver failure;Pregnancy and lactation
For security reasons Monosan can be used during pregnancy and lactation only strictly prescribed by a doctor, after a thorough evaluation of the benefits and possible risks, because to date, little is known about the consequences of its use in pregnant women and nursing mothers. If a nursing mother still takes, set parental supervision for the development of the possible effects of the drug.
Dosing and Administration
The tablets should be taken orally, after meals, swallowed whole with a little liquid.
The dose and dosing frequency is determined individually depending on the severity of the disease. Begin with 10-20 mg 1-3 times a day (10 mg dose corresponds to 2.1 mg of 20 tablets). Depending on the severity of the clinical effect from 3-4 day dose can be increased up to 20-40 mg two times a day, if necessary, increasing the dose to 60 mg / day (20 mg tablet) and 80 mg / day. (40 mg tablet). The maximum daily dose of 80 mg.
Side effect On the part of the cardiovascular system: “nitrate” headache, dizziness, transient facial flushing, heat sensation, tachycardia, marked reduction of blood pressure (BP). In rare cases – increase in angina attacks (paradoxical reaction), orthostatic collapse. From the digestive system: nausea, vomiting, may occur feeling light burning tongue, dry mouth. On the part of the central nervous system:stiffness, drowsiness, blurred vision, decreased ability to to rapid mental and motor reactions (especially at the beginning of treatment). Allergic reactions: skin rash, in some cases – exfoliative dermatitis.other: the development of tolerance (including cross to the other nitrates).
Overdose Symptoms: Collapse, syncope, reflex tachycardia, weakness, dizziness, confusion, headache, visual disturbances, pyrexia, redness of the skin, increased sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia -Usually in chronic overdose), hyperpnoea , dyspnea, increased intracranial pressure, convulsions, paralysis, coma. Treatment: in testosterone propionate 100mg addition to general recommendations, such as gastric lavage and laying the patient in a horizontal position with raised legs, should monitor the main indicators of vital signs and adjust if necessary. Patients with severe hypotension and / or shock should make up the blood volume; in exceptional cases, to improve blood circulation can be performed infusion of norepinephrine and / or dopamine. Introduction of epinephrine (adrenaline) and related compounds is contraindicated. When methemoglobinemia depending on the severity administered intravenously in the form of ascorbic acid sodium salt (previously methylthioninium chloride (methylene blue) 0.1-0.15 ml / kg of a 1% solution to 50 ml); Oxygen therapy, hemodialysis, exchange transfusion.
Interaction with other drugs
increases the concentration of dihydroergotamine in the blood plasma.
Reduces the effect of vasopressors.
Barbiturates accelerate biotransformation and reduce the concentration of isosorbide mononitrate in the blood.
When combined with other vasodilators, ACE inhibitors, beta-blockers, blockers “slow” calcium channel blockers, diuretics, , antipsychotics or tricyclic antidepressants, inhibitors of phosphodiesterase-5 including sildenafil, vardenafil, tadalafil, and ethanol may potentiation of the antihypertensive action of isosorbide mononitrate.
in combination with amiodarone, propranolol blockers “slow” calcium channel blockers (verapamil, nifedipine and et al.) may increase the anti-anginal effect. Under the influence of beta-agonists, alpha-blockers (dihydroergotamine, etc.) May reduce the severity of antianginal effects (tachycardia, excessive reduction of blood pressure).
The combined use with m-holinoblokatorami (atropine, and others.) Increases the likelihood of increased intraocular pressure.
Adsorbents, binders and enveloping means reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.
The therapeutic effect of norepinephrine (noradrenaline) decreases while admission to nitro compounds.
The drug is not used for the relief of angina attacks.
During treatment requires monitoring of blood pressure and heart rate. If necessary, use the drug on a background of arterial hypotension, it should at the same time to take testosterone propionate 100mg drugs with positive inotropic effect.Frequent purpose and high doses can cause the development of tolerance; In this case, after 3-6 weeks of regular intake, recommended removal of the drug for 24-48 hours, or a break in the treatment 3-5 days with his replacement at this time other antianginal drugs.
It is necessary to avoid abrupt withdrawal of the drug and reduce dose gradually.
in the period of drug treatment should be deleted alcohol.
It is possible decrease in the ability to rapid mental and motor reactions, so care should be taken to drive and engage in potentially hazardous activities during the period of drug therapy.