Monosan - instructions for use, dose, side effects, contraindications

Composition:1 tablet contains:
Active substance:
isosorbide-5-mononitrate 20 or 40 mg (trituration of isosorbide-5-mononitrate and lactose monohydrate 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 are white or almost white with a risk on one side.

Pharmacotherapeutic group:Vasodilator, nitrate.

ATX: & nbsp

C.01.D.A.14 Isosorbide mononitrate

Pharmacodynamics:Peripheral vasodilator with predominant effect on venous vessels. Stimulates the formation of nitric oxide (endothelial relaxing factor) in the vascular endothelium, which causes activation of intracellular guanylate cyclase, resulting in an increase in cGMP (mediator vasodilation). Reduces the need for myocardium in oxygen by reducing preload and afterload. Possesses coronary dilatation. Reduces the flow of blood to the right atrium, helps reduce pressure in a small circle of circulation and regression of symptoms with pulmonary edema. Promotes redistribution of coronary blood flow in the area with reduced blood circulation. Increases tolerance to physical activity in patients with ischemic heart disease (IHD), angina pectoris.It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache. Inhibits platelet aggregation, reduces intra-platelet synthesis of thromboxane. Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored. Antianginal effect occurs 30-45 minutes after ingestion and lasts up to 8-10 hours.

Pharmacokinetics:After oral administration isosorbide mononitrate quickly and completely absorbed from the gastrointestinal tract (GIT). Has a high bioavailability - about 100%, since there is no effect of "first passage" through the liver. The maximum concentration in the blood plasma after taking the drug inside is reached within an hour. Individual differences in plasma concentration after taking the drug inside are small. The effective level of isosorbide mononitrate in the blood is about 100 mg / ml. The drug does not bind to blood plasma proteins. Pharmacokinetics at doses of 10-80 mg has a linear character, and, unlike isosorbide dinitrate, is metabolized not in the liver, but in the kidneys where isosorbide and two glucuronide isosorbide-5-mononitrate are formed. The half-life is about 4-5 hours.It is excreted by the kidneys, mainly in the form of glucuron metabolites, 2% - in unchanged form. Kidney clearance of the drug 115 ml / min. In hepatocellular and renal failure, the pharmacokinetics of isosorbide mononitrate does not change significantly.

Indications:- Ischemic heart disease: prevention of angina attacks;
Chronic heart failure (as part of combination therapy).

Contraindications:- Hypersensitivity to organic nitrates or other components of the drug;
- Acute circulatory disorders (shock, vascular collapse);
- Cardiogenic shock if a sufficiently high final diastolic pressure in the left ventricle is not achieved by using intra-aortic counterpulsation or by introducing agents that have a positive inotropic effect;
- Toxic pulmonary edema;
- Severe arterial hypotension (systolic blood pressure less than 100 mm Hg, diastolic blood pressure less than 60 mm Hg)
- Simultaneous administration of phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil, as they potentiate the antihypertensive effect of nitrates;
- Hereditary intolerance to galactose, deficiency of lactase or malabsorption syndrome of glucose and galactose;
- Age under 18 years (efficiency and safety not established).

Carefully:- Hypertrophic cardiomyopathy, constrictive pericarditis, pericardial tamponade;
- Low filling pressure for acute myocardial infarction, left ventricular failure. Do not lower the systolic blood pressure below 90 mm Hg. st.).
- Aortic and / or mitral stenosis;
- The tendency to orthostatic disorders of vascular regulation;
- Closed-angle glaucoma;
- Thyrotoxicosis;
- Severe anemia;
- Diseases accompanied by increased intracranial pressure (including hemorrhagic stroke, craniocerebral injury);
- Severe renal insufficiency;
- Liver failure.

Pregnancy and lactation:For safety reasons, Monosan can be used during pregnancy and lactation only strictly according to the doctor's prescription, after a thorough evaluation of the benefits and possible risks, since there is currently insufficient data on the effects of its use in pregnant and lactating mothers.If a nursing mother still accepts Monosan, it is necessary to establish observation of the child for the development of possible effects from the drug.

Dosing and Administration:Tablets should be taken orally, after eating, swallowed whole, with a small amount of liquid.
The dose of the drug and the frequency of reception are set individually, depending on the severity of the disease. Begin with 10-20 mg 1-3 times a day (a dose of 10 mg corresponds to 1/2 tablet 20 mg). Depending on the severity of the clinical effect from 3-4 days the dose can be increased to 20-40 mg twice a day, increasing the dose if necessary to 60 mg / day (for tablets 20 mg) and up to 80 mg / day. (for tablets of 40 mg). The maximum daily dose is 80 mg.

Side effects:From the cardiovascular system: "nitrate" headache, dizziness, transient hyperemia of the skin of the face, a feeling of heat, tachycardia, marked decrease in blood pressure (BP). In rare cases - increased attacks of angina pectoris (paradoxical reaction), orthostatic collapse.
From the digestive system: nausea, vomiting, there may be a sensation of slight burning of the tongue, dry mouth.
From the central nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment).
Allergic reactions: Skin rash, in some cases - exfoliative dermatitis.
Other: development of tolerance (including cross-over to other nitrates).

Overdose:Symptoms:
Collapse, syncope, reflex tachycardia, weakness, dizziness, confusion, headache, visual disturbances, pyrexia, redness, increased sweating, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia -Usually chronic overdose), hyperpnea, dyspnea, increased intracranial pressure, convulsions, paralysis, coma.
Treatment:
In addition to general recommendations, such as gastric lavage, and the patient lying down in a horizontal position with raised legs, should monitor the main indicators of vital signs and adjust if necessary. Patients with severe arterial hypotension and / or shock should be supplemented with a volume of circulating blood; in exceptional cases to improve blood circulation, you canto carry out infusions of norepinephrine and / or dopamine.
The introduction of epinephrine (adrenaline) and related compounds is contraindicated.
At a methemoglobinemia depending on a degree of gravity are appointed or nominated intravenously ascorbic acid in the form of sodium salt (previously used methylthioninium chloride (methylene blue) 0.1-0.15 ml / kg of 1% solution up to 50 ml); oxygen therapy, hemodialysis, exchange blood transfusion.

Interaction: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, angiotensin-converting enzyme inhibitors, beta-blockers, slow calcium channel blockers, diuretics, neuroleptics or tricyclic antidepressants, with phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil, and also with ethanol, potentiation is possible antihypertensive action of isosorbide mononitrate.
When combined with amiodarone, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine and others), there may be an increase in the antianginal effect.
Under the influence of beta-adrenostimulants, alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to reduce the antianginal effect (tachycardia, excessive blood pressure decrease).
When combined with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure.
Adsorbents, astringents and enveloping agents reduce the absorption of isosorbide mononitrate in the gastrointestinal tract.
The therapeutic effect of norepinephrine (norepinephrine) decreases with simultaneous intake with nitrocompounds.

Special instructions:The drug is not used to stop angina attacks.
During the therapy, it is necessary to monitor blood pressure and heart rate. If necessary, use the drug against the background of arterial hypotension, should simultaneously take drugs that have a positive inotropic effect. Frequent prescription and high doses can cause tolerance development; in this case, after 3-6 weeks of regular admission, it is recommended to cancel the drug for 24-48 h, or a break in treatment with the drug Monosan for 3-5 days with its replacement at this time by other antianginalmedicinal products.
It is necessary to avoid the abrupt withdrawal of the drug and reduce the dose gradually.
During the treatment with the drug should be excluded from drinking alcohol.

Effect on the ability to drive transp. cf. and fur:Perhaps a decrease in the ability to rapid mental and motor reactions, so you should carefully manage vehicles and engage in potentially hazardous activities during drug therapy.

Form release / dosage:Tablets of 20 mg and 40 mg.

Packaging:10 tablets in a blister; 3 blisters together with instructions for use in a cardboard bundle.

Storage conditions:List B. In a dry, protected from light and out of reach of children, at a temperature of 15 - 25 ° C.

Shelf life:4 years. Do not use after the expiry date printed on the package!

Terms of leave from pharmacies:On prescription

Registration number:П N015292 / 01

Date of registration:01.11.2008

Expiration Date:Unlimited

The owner of the registration certificate:PRO.MED.CS Prague as.PRO.MED.CS Prague as. Czech Republic

Manufacturer: & nbsp

PRO.MED.CS Praha, a.s. Czech Republic

Representation: & nbspPRO.MED.CS Prague as. PRO.MED.CS Prague as. Czech Republic

Information update date: & nbsp2016-12-12

Illustrated instructions

Instructions

Monosan (Monosan)