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:
    tablet weight
    Nitrosorbide - 0.1 g of which:
    isosorbide dinitrate - 0.01 g
    auxiliary substances: potato starch, sugar (sucrose), calcium stearate up to 0.1 g

    Description:Tablets of white color, round, 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:
    Relaxes the smooth muscles of the vessels, providing a vasodilating effect. Like all organic nitrates, is a donor of nitric oxide II (NO). NO activates guanylate cyclase, increasing the content of cyclic guanosine monophosphate (cGMP). The latter stimulates cGMP-dependent protein kinase, which disrupts the phosphorylation of some smooth muscle cell proteins, including the light chain of myosin, which ultimately reduces contractility and subsequently leads to relaxation of smooth muscle vessels.
    It acts on the peripheral arteries and veins. Relaxation of veins leads to a decrease in venous return to the heart (preload), which reduces the filling pressure of the left ventricle. There is also (although to a lesser extent) an expansion of arterial vessels, which is accompanied by a decrease in blood pressure, a decrease in the total peripheral vascular resistance (postload). Decrease in pre- and postnagruzki leads to a decrease in oxygen consumption by the myocardium. Promotes redistribution of coronary blood flow in favor of subendocardial zones, especially in coronary artery atherosclerosis (mostly large). Vasodilation of the collateral arteries can improve the blood supply of the myocardium. Copes coronary spasm; improves hemodynamics in patients with chronic heart failure, both at rest and during physical exertion.
    Reducing myocardial oxygen consumption and improving oxygen delivery to ischemic areas, reduces the area of ​​myocardial damage. Relaxes also smooth muscles of the bronchi, gastrointestinal tract, bile and urinary tract.

    Pharmacokinetics:Absorption is high.Bioavailability at ingestion - 22% (effect of "first passage" through the liver), with sublingual application (under the tongue) - 60%. Time to reach the maximum concentration for ingestion - 1 hour. Communication with blood plasma proteins - 30%. Half-life at intake of 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 hours). It is excreted by the kidneys (almost completely in the form of metabolites).
    Indications:Prevention 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, cardiac tamponade , constrictive pericarditis, toxic pulmonary edema,angle-closure glaucoma with high intraocular pressure, toxic pulmonary edema and craniocerebral trauma, simultaneous use of phosphodiesterase-5 inhibitorstadalafil, vardenafil, sildenafil), age under 18 years (efficacy and safety not established). Hypertrophic obstructive cardiomyopathy (possibly an increase in angina attacks), severe anemia, cerebral hemorrhage.
    Intolerance to fructose, glucose-galactose malabsorption, sucrose-isomaltose deficiency.

    Carefully:Aortic and / or mitral stenosis, marked hepatic insufficiency (risk of methaemoglobinaemia), severe renal failure, acute myocardial infarction (risk of lowering blood pressure and tachycardia that may increase ischemia), hypothyroidism, patients with a tendency to orthostatic hypotension, elderly patients. Diseases accompanied by increased intracranial pressure; inadequate and malnutrition
    Pregnancy and lactation:It should be used only after a careful weighing of the benefit-risk ratio for the mother and fetus associated with the use of the drug,Since the experience of use in pregnant and lactating women is not enough.
    Dosing and Administration:
    The drug is administered orally or sublingually (under the tongue).
    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, flushing of the facial skin, fever, tachycardia, lowering of blood pressure. From the gastrointestinal tract: nausea, vomiting, there may be a feeling of slight burning of the tongue, dryness of the oral mucosa.
    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.
    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

    Overdose:Symptoms: lowering blood pressure (less than 90 mm Hg), pallor, increased sweating, threadlike pulse, tachycardia, postural dizziness, throbbing headache, asthenia, nausea, vomiting, diarrhea; increased intracranial pressure (with high doses), methemoglobinemia. Treatment: transfer of the patient to a horizontal position with raised legs, oxygen therapy, replenishment of circulating blood, the administration of norepinephrine or other vasoconstrictors (epinephrine is not recommended); with methemoglobinemia - ascorbic acid, oxygen therapy, artificial ventilation, hemodialysis.
    Interaction:
    Pharmacodynamic: under the influence of alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to reduce the anti- anginal effectisosorbide dinitrate (excessive reduction in blood pressure and, as a consequence, coronary perfusion).
    The combination of amiodarone and other medications, such as, propranolol, blockers of "slow" calcium channels (verapamil, nifedipine and others) and isosorbide dinitrate is rational for the treatment of coronary heart disease. The combined use of acetylsalicylic acid and isosorbide dinitrate improves coronary circulation.
    When joint application of isosorbide dinitrate with antihypertensive drugs, vasodilators, antipsychotic drugs (antipsychotics), tricyclic antidepressants, novocainamide, ethanol, quinidine, beta-blockers, blockers
    "slow" calcium channels and dihydroergotamine may increase the severity of lowering blood pressure.
    When combined application of isosorbide dinitrate with m-holinoblokatorami (atropine and others) increases the likelihood of increased intraocular pressure. With simultaneous administration with phosphodiesterase-5 inhibitors, a marked decrease in blood pressure is possible.
    It is advisable to use caution while using isosorbide dinitrate with the drug sapropetrin. Saprotherin is a coenzyme of nitric oxide synthetase, it potentiates the synthesis of additional amounts of nitric oxide, which is important to take into account in connection with the occurrence of an increased risk of hypotension with simultaneous application of sapropterin with all vasodilating agents, whose action is associated with nitric oxide
    Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of isosorbide dinitrate 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, at this time, Nitrosorbide with other antianginal drugs. During the treatment with Nitrosorbide, it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities,requiring 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:
    10 tablets per contour cell pack.
    For 25, 50 or 100 tablets in cans of polymeric.
    Each can of polymer or 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 contour cell packs, together with the instruction for use, is placed in a cardboard pack.
    Storage conditions:In dry, dark place at a temperature of no higher than 15 ° C away from the fire. Keep out of the reach of children.
    Shelf life:
    3 years.
    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N001474 / 01
    Date of registration:15.12.2008
    Manufacturer: & nbsp
    Information update date: & nbsp10.11.2014
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