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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    • Dosage form: & nbsppills
    Composition:
    Composition per one tablet

    Nitrosorbide -100 mg [Isosorbide dinitrate -10 mg Excipients-, sucrose -80 mg, potato starch - 9.5 mg, calcium stearate-0.5 mg].
    Description:tablets of white color, flat-cylindrical, with a bevel.
    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 to isosorbide dinitrate, cross tolerance develops. 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 administration is 1 hour. Connection 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 strokes, rehabilitation treatment after myocardial infarction (in combination therapy), chronic heart failure (in combination therapy).
    Contraindications:Increased sensitivity to organic nitrates, hemorrhagic stroke, severe hypotension (systolic blood pressure less than 100 mm Hg, diastolic blood pressure below 60 mm Hg) to collapse, shock, acute myocardial infarction with severe arterial hypotension, increased intracranial pressure, toxic pulmonary edema, form-closure glaucoma with high intraocular pressure, craniocerebral trauma, concomitant use of inhibitors of phosphodiesterase-5, age 18 years (effectiveness and safety are installed).
    Carefully:hypertrophic cardiomyopathy (possibly an increase in angina attacks), constrictive pericarditis, cardiac tamponade; aortic and / or mitral stenosis, severe hepatic insufficiency (risk of methemoglobinemia), severe renal failure, bleeding in the brain,acute myocardial infarction (risk of lowering blood pressure and tachycardia that may increase 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 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:
    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, 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 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.
    With the 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 hours, or after 3-6 weeks. regular reception to take a break for 3 5 days, replacing, at this time Nitrosorbide other antianginal agents. 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.
    Form release / dosage:
    Tablets 10 mg.
    Packaging:
    For 10 or 25 tablets in a contour mesh package.
    1 or 2 contour packs of 10 tablets, 1 or 2 contour packs of 25 tablets together with instructions for medical use are placed in a pack.
    Storage conditions: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:LSR-003429/07
    Date of registration:26.10.2007
    Manufacturer: & nbsp
    Information update date: & nbsp03.12.2012
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