Nitrosorbide (Nitrosorbide)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceIsosorbide dinitrateIsosorbide dinitrate
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    UPDATE OF PFC, CJSC     Russia
    • Dosage form: & nbsppills
    Composition:1 tablet contains active substance isosorbide dinitrate 10 mg and excipients: sugar, potato starch, calcium stearate.
    Description:Tablets are white in a flat-cylindrical form.
    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%. The time to reach the maximum concentration for oral intake is 1 hour. The connection with blood plasma proteins is 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:Hypersensitivity to organic nitrates, hemorrhagic stroke, severe arterial hypotension (systolic blood pressure less than 100 mm Hg, diastolic blood pressure less than 60 mm Hg), collapse, shock, acute myocardial infarction with severe arterial hypotension, increased intracranial pressure, toxic pulmonary edema, angle-closure form of glaucoma with high intraocular pressure, craniocerebral trauma, age under 18 years (efficacy and safety not established).
    Carefully:hypertrophic cardiomyopathy (possibly an increase in angina attacks), constrictive pericarditis, cardiac tamponade; aortic and / or mitral stenosis, marked hepatic insufficiency (risk of methaemoglobinemia), severe renal failure, cerebral hemorrhage, acute myocardial infarction (risk of lowering blood pressure and tachycardia,which can enhance ischemia), severe anemia, hyperthyroidism, patients with a tendency to orthostatic hypotension, elderly patients, increased peristalsis of the gastrointestinal tract, malabsorption syndrome.
    Pregnancy and lactation:It should be used only after a careful weighing of the benefit-risk relationship associated with the use of the drug, since the experience of use in pregnant and lactating women is not enough. Action category for fetus C.
    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 angina pectoris, take one tablet (10 mg) of Nitrosorbide sublingually (to accelerate the action of the tablet, it is advisable to chew). 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:
    From the side of the cardiovascular system: "nitrate" headache, dizziness, hyperemia of the skin of the face, a feeling of heat, tachycardia, a decrease in blood pressure. In rare cases - a "paradoxical" increase in angina attacks and collapse.
    From the gastrointestinal tract: nausea, vomiting, there may be a feeling of slight burning of the tongue, dry mouth.
    From the nervous system: stiffness, drowsiness, blurred vision, decreased ability to rapid mental and motor reactions (especially at the beginning of treatment). In rare cases - cerebral ischemia. Allergic reactions: skin rash.
    Other: development of tolerance (including cross-over to other nitrates), exfoliative dermatitis.

    Overdose:
    Symptoms: collapse, fainting, 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 related compounds are ineffective).
    Interaction:
    Pharmacodynamic: under the influence of alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to reduce the antianginal effect of nitrosorbide (excessive decrease in blood pressure and coronary perfusion as a consequence).
    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, novocainamide, ethanol, quinidine, beta-adrenoblockers, blockers of "slow" calcium channels and dihydroergotamine may increase the severity of blood pressure lowering.
    When combined use of nitrosorbide with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure. With simultaneous admission with sildenafil (Viagra), a marked decrease in blood pressure is possible. Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of nitrosorbide in the gastrointestinal tract.

    Special instructions:
    During the treatment with Nitrosorbide, 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; in this case, it is recommended to cancel for 24-48 h, or after 3-6 weeks of regular intake to take a break for 3-5 days, replacing Nitrosorbide for this time with other antianginal drugs. During the treatment with Nitrosorbide, it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. Avoid abrupt discontinuation of the drug, reduce the dose gradually. During the treatment with the drug should be excluded from drinking alcohol.
    Treatment: gastric lavage; at a methemoglobinemia - in / in 1% a solution of methylene blue, 1-2 mg / kg. Symptomatic therapy ( epinephrine and related compounds are ineffective).

    Form release / dosage:
    Tablets 10 mg.

    Packaging:
    10 tablets per contour cell pack.1, 2, 3, 4, 5 or 6 contour mesh packages together with instructions for use
    put in a pack of cardboard. 3000 contour mesh packages with the appropriate number of instructions for use are placed in a cardboard box (for hospitals).
    In the case of manufacturing the drug on the production site of LLC "Ozon", Russia for 10, 50 tablets in a contour melt
    packing. By 10, 20, 30, 40, 50 or 100 tablets in cans of polyethylene terephthalate or cans of polymeric for medicinal purposes
    means.
    One bank or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package
    (pack).
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C, away from fire. Keep out of the reach of children.

    Shelf life:3 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-000272
    Date of registration:29.12.2009
    Manufacturer: & nbsp
    Information update date: & nbsp15.05.2015
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