Nitrogranulong tab. of 2.9 mg No. 50

Nitrogranulong tab. 0.0029; 0.0052 No. 10, 50

Group: Means influencing a cardiovascular system

Acting with the Eastern Military District: Nitroglitserin of 2% on lactose

General characteristic

Ingredients:

active ingredient: nitroglycerine;

1 tablet contains nitroglycerine 2.9 mg or 5.2 mg;

excipients: lactoses monohydrate, potato starch, talc, magnesium stearate, povidone, white sugar, starch corn, silicon dioxide colloidal anhydrous, titan dioxide (E 171), gelatin, polyethyleneglycol 6000 (macrogoal 6000).

Dosage form. Tablets of the prolonged action.

Pharmacotherapeutic group. Vazodilatatora, applied in cardiology. Glyceryl trinitrate. Code of automatic telephone exchange C01 D A02 .

Clinical characteristics.

Indication.

Prevention of attacks of stenocardia at patients with the coronary heart disease (CHD), including in the postinfarction period.

Contraindication.

Hypersensitivity, arterial hypotension (the ABP is lower than 90/60 mm Hg.), an acute myocardial infarction with the low pressure of filling of a right ventricle, a toxic fluid lungs, a hemorrhagic stroke, intracranial hypertensia, closed-angle glaucoma, acute anemia, shock, collapse, a hypertrophic subaortic stenosis, simultaneous use with sildenafily and other inhibitors of phosphodiesterase, bradycardia (less than 50 ud. / mines), cerebral ischemia, cardiac tamponade.

Route of administration and doses.

Dosing depends on a condition of the certain patient and weight of course of a disease. To prevent development of tolerance, the mode of dosing has to include a 10-12-hour beznitratny interval.

In mild cases of Nitrogranulong is accepted on 1-2 tablets on 2.9 mg twice a day, in the morning and after a lunch. At heavier course – 1-2 tablets on 5.2 mg twice a day, in the morning and after a lunch. The lack of an evening dose provides a 12-hour interval. If necessary administration of medicament 3 times a day, but with observance of a 10-12-hour beznitratny interval can be appointed.

If attacks at the patient occur mainly at night, Nitrogranulong should be accepted after a lunch and in the evening.

Pill should be taken on an empty stomach, to swallow whole, not to get to the core and not to chew, washing down with a small amount of liquid.

Maximum daily dose should not exceed 30 mg.

Side reactions.

At initial stages of use of medicament (1-2 days), depending on a dose and most often owing to vazodilatatorny effect, the following side reactions can be observed.

from central nervous system : headache, dizziness, faint, uneasiness, psychotic reactions, block, disorientation.

from a cardiovascular system: orthostatic reactions, a lowering of arterial pressure, tachycardia, paradoxical bradycardia (in acute hypotension or a syncope), hyperaemia of the person, cyanosis, pallor, a methemoglobinemia.

from digestive system : nausea, vomiting, dryness in a mouth, an abdominal pain, diarrhea.

from the immune system: allergic reactions, including skin rash, itching, erubescence; acute anaphylaxis.

Others: general weakness, feeling of heat, disorder of vision, exacerbation of glaucoma, hypothermia.

At sudden falling of arterial blood pressure strengthening of symptoms of stenocardia (paradoxical "nitrate" reactions) can be observed.

Overdose.

Symptoms: a headache, arterial hypotension, the accelerated heartbeat, a disorder of vision, an erythema, the strengthened sweating, nausea, vomiting, cyanosis, bradycardia, spasms and a coma, in sharp cases – a methemoglobinemia, severe dizziness, a syncope, short wind, the significant weakness, drowsiness, the increased body temperature, feeling of heat, a fever. At use of high doses (more than 20 mkg/kg) – collapse, dispnoe and a tachypnea.

Treatment: gastric lavage, intake of activated carbon, depletive, restoration of normal respiratory function and arterial blood pressure (a prone position with a low headboard, liquid infusions). For elimination of a methemoglobinemia medicament of the choice is methylene blue.

Use during pregnancy or feeding by a breast.

Use of nitroglycerine during pregnancy or feeding by a breast contraindicated.

Children.

in pediatrics.

Feature of use.

Nitrogranulong do not appoint for treatment of bad attacks of stenocardia.

Should consider that uncontrolled administration of medicament can lead to development of the tolerance to nitrates which is expressed in reduction of duration and expressiveness of effect of medicament at regular use or increase in its dose for achievement of the same effect. Faltering administration of medicament within a day is necessary for prevention of emergence of a refrakternost.

Nitrogranulong should not be applied along with sildenafily.

Is necessary with care, considering risk and advantage, to take the medicament at: an uncontrolled hypovolemia, heart failure with a normal or low pulmonary pressure, a hyperthyroidism, disturbance of cerebral circulation, a heavy renal and/or liver failure (risk of developing a methemoglobinemia). With care to apply in an aortal stenosis. It is necessary to apply with care to patients with the profound cerebral atherosclerosis, to patients of advanced age. During treatment not to take alcohol. During treatment the visit of a bath, sauna, reception of a hot shower is contraindicated. The tablet cannot be chewed as through a mucous membrane of an oral cavity the excess amount of active ingredient can come to a system blood stream.

Drug contains lactose therefore to patients with rare hereditary forms of intolerance of a galactose, insufficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption it is not necessary to use drug.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

during administration of medicament should not run vehicles, to serve mechanical devices and to perform the work requiring special attention and fast psychomotor reaction.

Interaction with other medicines and other types of interactions.

At simultaneous use with other antihypertensives, phosphodiesterase inhibitors, procaineamides, APF inhibitors, blockers of calcium channels, beta blockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol and etanolsoderzhashchy medicaments the hypotensive effect of nitroglycerine amplifies; with beta blockers, blockers of calcium channels — anti-anginal action amplifies; with dihydroergotamine – increase in its concentration in plasma is possible. Use of nitroglycerine against the background of quinidine or a novokainamid can cause orthostatic collapse.

Concomitant use of alkaloids of an ergot can cause stenocardia. At simultaneous alcohol intake the side effects of medicament can be sharper and frequent.

Atropine and other medicaments having M-cholinolytic effect can reduce effect of nitroglycerine owing to decrease in secretion and biodigestion of drug. At simultaneous use with heparin the decrease in anticoagulating action of the last is possible (after medicament withdrawal perhaps considerable decrease in blood clotting that can demand a heparin dose decline). Phenobarbital activates metabolism of nitrates in a liver. Alpha adrenomimetiki, the histamine, Pituitrinum, corticosteroids, central nervous system stimulators, poison of bees, snakes, sunshine reduce anti-anginal effect of nitroglycerine. Salicylates increase nitroglycerine level in blood, barbiturates accelerate his metabolism. Donators of sulfhydryl groups (captopril, Acetylcysteinum, Unithiolum) restore reduced sensitivity to nitroglycerine.

Pharmacological properties.

Pharmacodynamics.

Anti-anginal medicament of the prolonged action. The nitroglycerine belonging to group of organic nitrates is the active vazodilatator operating both on arterial and on venous vessels. The mechanism of anti-anginal effect of medicaments of nitroglycerine of the prolonged action is connected with its peripheral vasodilating influence. Along with decrease in resistance of coronary vessels, nitroglycerine expands, mainly, post-capillary venous vessels, leading to reduction of venous return to heart; in higher doses expands also precapillary arterioles regulating peripheric vascular resistance owing to what cardiac performance and its oxygen requirement decreases. Drug promotes redistribution of a coronary blood-groove in the area with reduced blood circulation. Increases tolerance to physical activity at patients with stenocardia.

Pharmacokinetics.

After administration of medicament in a small intestine; action comes in 30-60 min. and 4-6 hours proceed. Drug substantially collapses in a liver with the participation of nitrate reductase (effect of "the first passing"), and then biotransformirutsya in nitrogen oxide (NO) in smooth muscle cells. The bioavailability is no more than 10% in comparison with the nitroglycerine applied to language. Metabolites are di - and mononitrates (only isosorbide-5-mononitrate is active), final – glycerin. Elimination half-life of metabolites makes the 4th hour. In plasma contacts proteins (60%). Metabolites are extracted generally by kidneys.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of round shape, coated, white or almost white color, upper and lower surfaces of which convex. On a break when examining under a magnifying glass the kernel surrounded with one continuous layer is visible.

Expiration date. 3 years.

Storage conditions.

in original packing at to temperature it is not higher than 25 ⁰ S. Hranit out of children's reach.

Packing.

On 10 tablets in blisters;

on 10 tablets in the blister, on 5 blisters in a pack from cardboard;

on 50 tablets in a container, on 1 container in a pack from cardboard.

Category of release. According to the prescription.