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

Active substanceIsosorbide dinitrateIsosorbide dinitrate

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Nitrosorbide

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Nitrosorbide

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UPDATE OF PFC, CJSC Russia

Dosage form: & nbspPills

Composition:

Pills white, flat-faced with a bevel, marked "R" on one side or without it.

Description:

Tablets are white, flat-faced with a bevel, marked "R" on one side or without it.

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.05.A.E.02 Isosorbide dinitrate

C.01.D.A.08 Isosorbide dinitrate

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, which results in an increase in cGMP (a mediator of vasodilation). Reduces the need for myocardium in oxygen by reducing preload and postload (reduces the final diastolic volume of the left ventricle and reduces the systolic tension of its walls). 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 coronary heart disease, angina pectoris.

It dilates the vessels of the brain, the dura mater, which can be accompanied by a headache.

Like other nitrates, cross tolerance is developing. After cancellation (interruption in treatment) sensitivity to it is quickly restored.

The onset of action after sublingual administration or chewing - 2-5 minutes, after oral administration - 15-40 minutes. The duration of action is 1-2 hours and 4-6 hours, respectively.

Pharmacokinetics:

Absorption is high. Bioavailability at ingestion - 22% (effect of "first passage" through the liver), with sublingual application - 60%. Time to reach the maximum concentration with oral intake - 1 hour. Communication with blood plasma proteins - 30%. The half-life at oral intake is 4 hours. Metabolised in the liver to 2 active metabolites: isosorbide-5-mononitrate (75-85%), half-life of which is 5 hours, and isosorbide-2-mononitrate (15-25%) with half-life - 2.5 h).It is excreted by the kidneys (almost completely in the form of metabolites).

Indications:

- Prevention and treatment of angina attacks;

- Restorative treatment after myocardial infarction (as part of combination therapy);

- chronic heart failure (as part of combination therapy).

Contraindications:

Increased sensitivity to organic nitrates; hemorrhagic stroke; severe arterial hypotension (systolic blood pressure less than 100 mm Hg, diastolic blood pressure less than 60 mm Hg. item); collapse, shock; acute myocardial infarction with severe arterial hypotension; increased intracranial pressure; toxic pulmonary edema; closed angle form of glaucoma with high intraocular pressure; craniocerebral trauma; simultaneous use of inhibitors phosphodiesterase-5

(sildenafil, vardenafil, tadalafil); severe hypovolemia; severe aortic and subaortic stenosis; severe mitral stenosis; hypertrophic cardiomyopathy (GOKMP); constrictive pericarditis; cardiac tamponade; cerebral hemorrhage; severe anemia; age to 18 years (efficacy and safety not established).

Carefully:

Severe hepatic insufficiency (risk of development of methemoglobinemia); severe renal insufficiency; acute myocardial infarction (risk of lowering blood pressure and tachycardia, which may increase myocardial ischemia); hyperthyroidism; propensity to orthostatic hypotension; elderly age; increased peristalsis of the gastrointestinal tract; malabsorption syndrome; inadequate and malnutrition.

Pregnancy and lactation:

Application at pregnancy Nitrosorbide is only possible in cases where the expected benefit for the mother exceeds the potential risk to the fetus or child, and should be controlled by a doctor. If it is necessary to use Nitrosorbide during lactation, breastfeeding should be discontinued. information is available the penetration of nitrates into breast milk.

If it is necessary to urgently use Nitrosorbide in a dose of 10 mg to stop an attack of angina pectoris To establish supervision over the child for the purpose of development of possible by-effects.

Dosing and Administration:

The drug is administered orally or sublingually.

For the prevention of angina attacks, the initial dose of the drug inside is 10 mg 4-5 times a day. With insufficient effectiveness from the 3-5th day of treatment, the dose of the drug can be increased to 60-120 mg per day.

To stop an attack of angina pectoris take 1 tablet (10 mg) Nitrosorbide sublingually (to accelerate the action, it is advisable to chew the tablet). In the combination therapy of chronic heart failure, 10-20 mg 3-4 times a day are prescribed.

Duration of treatment is determined in each case individually. If necessary, the drug is canceled gradually.

Side effects:

Frequency of occurrence: very often - more than 1/10, often - more than 1/100 and less than 1/0, infrequently - more than 1/1000 and less than 1/100, rarely

- more than 1/10000 and less than 1/1000, very rarely, less than 1/10000.

From the central nervous system:

very often - "nitrate" headache; often - drowsiness, mild dizziness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment).

From the cardiovascular system:

often - tachycardia, orthostatic hypotension; infrequently - the "paradoxical" intensification of angina attacks, collapse (sometimes accompanied by bradyarrhythmia and syncope),frequency unknown - hypotension; with prolonged use - transient hypoxemia due to the relative redistribution of blood flow to hypoventilated alveolar areas (in patients with ischemic heart disease can lead to hypoxia of the myocardium).

From the gastrointestinal tract: infrequently - nausea, vomiting, dryness of the oral mucosa; very rarely - heartburn.

From the skin: infrequently skin allergic reactions (including rash), "tides" of blood to the skin of the face; very rarely - angioedema, Stevens-Johnson syndrome; frequency unknown - exfoliative dermatitis. Other: often - asthenia; development of tolerance (including cross-over to other nitrates).

Overdose:Symptoms: collapse, syncope, headache, dizziness, palpitations, visual disturbances, skin hyperemia, perspiration, nausea, vomiting, diarrhea, methemoglobinemia (cyanosis, anoxia), hyperpnoea, dyspnoea, bradycardia, craniocerebral hypertension, paralysis, coma.

Treatment: gastric lavage; at a methemoglobinemia - in / in 1% a solution of methylene blue, 1-2 mg / kg. Symptomatic therapy (epinephrine and the related compounds are ineffective).

Interaction:

Pharmacodynamic: under the influence of alpha-adrenoblockers (dihydroergotamine, etc.), the expression of the antianginal effect of nitrosorbide (excessive decrease in blood pressure and coronary perfusion, as a consequence) can be reduced.

The combination of amiodarone and other medications, such as, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine and others) and nitrosorbide is rational for the treatment of coronary heart disease. The combined use of acetylsalicylic acid and nitrosorbide improves coronary circulation.

When combined use of nitrosorbide with antihypertensive drugs, vasodilators, antipsychotic drugs (antipsychotics), tricyclic antidepressants, novocaineamide, ethanol, quinidine, beta-adrenoblockers, blockers of "slow" calcium channels and dihydroergotamine may increase the severity of lowering blood pressure.

When combined use of nitrosorbide with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure.Simultaneous administration with phosphodiesterase-5 inhibitors (sildenafil, vardenafil, tadapafil) is contraindicated, in view of the possibility of enhancing the hypotensive effect of the drug.

Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of nitrosorbide in the gastrointestinal tract.

Special instructions:During the treatment with the drug, especially in the case of a gradual increase in the dose, it is necessary to control blood pressure and heart rate. Frequent prescription and high doses can cause tolerance development, incl. "cross", in this case it is recommended to cancel for 24-48 h, or after 3-6 weeks of regular admission to take a break for 3-5 days, replacing the preparation with other antianginal drugs for this time. Avoid abrupt discontinuation of the drug, 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:

During the period of treatment with Nitrosorbide, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 10 mg and 20 mg.

Packaging:For 10, 14, 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil.

5, 10 contiguous cell packs of 10 tablets or 4 contour packs of 14 tablets with instructions for use are placed in a pack of cardboard.

Storage conditions:List B. In a dry, cool, dark place, out of the reach of children, away from the fire.

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003302/07

Date of registration:22.10.2007

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp24.07.2013

Illustrated instructions

Instructions

Nitrosorbide (Nitrosorbide)