Isosorbide dinitrate (Isosorbidi dinitras)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Nitrates and nitrate-like agents

Included in the formulation
  • Dinisorb
    concentrate d / infusion 
       
  • Isacardin®
    spray n / az. 
       
  • Isacardin®
    concentrate d / infusion 
       
  • Isoket®
    concentrate d / infusion 
    YUSB Farma SpA     Italy
  • Isoket®
    spray locally 
       
  • Cardicet®
    pills inwards 
    YUSB Pharma GmbH     Germany
  • Nitrosorbide
    pills inwards 
       
  • Nitrosorbide
    pills inwards 
       
  • Nitrosorbide
    pills inwards 
       
  • Nitrosorbide
    pills inwards 
    UPDATE OF PFC, CJSC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    VED

    Minimal chemist's assortment

    АТХ:

    C.05.A.E.02   Isosorbide dinitrate

    C.01.D.A.08   Isosorbide dinitrate

    Pharmacodynamics:

    Has antianginal, vasodilating, spasmolytic effect, has antiaggregant activity.

    Antianginal effect of the drug is associated with the expansion of peripheral vessels, mainly venous. Vein dilatation leads to a decrease in venous return to the heart (reducing myocardial overload) and end-diastolic blood pressure. Expansion of the arterial vessels leads to a decrease in the total peripheral resistance and blood pressure, hence, to a decrease in postload on the heart. In turn, the reduction of pre- and post-loading on the heart leads to a decrease in the work of the heart and its need for oxygen.Direct expansion of the coronary vessels stimulates collateral circulation with redistribution of blood flow to the ischemic site of the myocardium.

    The vasodilator effect of the drug is due to the action on smooth muscle cells of vessels with nitric oxide NO, which is released from isosorbide nitrate in the process of metabolism. Identity of nitric oxide to the endothelial relaxing factor derived from the amino acid L-arginine, activates the cytosolic enzyme of intact vascular endothelium - guaNilatcyclase, which contributes to the accumulation of cGMP. As a result, the calcium content in the cytosol of smooth muscle cells decreases, as a result of which the smooth muscles of the vessels are relaxed.

    Antiaggregant activity is due to a decrease in platelet aggregation.

    Spasmolytic effect extends to the smooth muscles of the internal organs, which leads to a decrease in the tone of the bronchi, intestines, bile ducts and ureters.

    Pharmacokinetics:

    After sublingual administration, up to 60% is rapidly absorbed; after oral administration - up to 20%. The maximum concentration in the blood plasma is reached in 2-5 minutes after sublingual administration and after oral administration - through15-40 minutes. The connection with plasma proteins is about 30%.

    Therapeutic effect develops 2-5 minutes after the beginning of sublingual administration and within 15-40 minutes after ingestion. Metabolism in the liver with the formation of an active metabolite of isosorbide-5-mononitrate. The duration of action of isosorbide dinitrate when taking conventional tablets inside is 4-6 hours, prolonged tablets - 8-12 hours, with sublingual admission - 1-2 hours and when taking tablets for chewing - from 15 minutes to 2 hours. After spraying on the oral mucosa, the effect manifests itself after 30 seconds and lasts 15-120 minutes.

    The half-life is 2-4 hours. Elimination by the kidneys in the form of metabolites.

    Indications:

    It is used to stop and prevent attacks of angina pectoris, including postinfarction; for the treatment of chronic congestive heart failure in combination with diuretics and cardiac glycosides; in acute left ventricular failure - in a solution for infusions.

    For the prevention of angina attacks, cutaneous use is used.

    Inhalation use is used as an emergency aid in acute left ventricular failureand acute myocardial infarction at the prehospital stage.

    ICD-10

    IX.I20-I25.I20.0   Unstable angina

    IX.I20-I25.I20   Angina pectoris [angina pectoris]

    IX.I20-I25.I21   Acute myocardial infarction

    IX.I26-I28.I27.0   Primary pulmonary hypertension

    IX.I30-I52.I50.0   Congestive heart failure

    IX.I30-I52.I50.1   Left ventricular failure

    Contraindications:

    Increased intracranial pressure, stroke, collapse, toxic pulmonary edema, angle-closure glaucoma, constrictive pericarditis, cardiac tamponade, marked violations of liver and kidney function, severe anemia, individual intolerance, children under 18 years of age.

    Carefully:

    Propensity to orthostatic hypotension.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside 30 minutes before meals 5-10 mg 3-4 times a day. In severe cases, the dose rises to 20-40 mg. With heart failure: 20 mg every 4-5 hours.

    Sublingually for arresting an attack of angina: 2.5-5 mg every 2-3 hours.

    Intravenous drip introduction begins at a rate of 1-2 mg / h, if necessary, the rate increases to 8-10 mg / h.

    For dermal application, the initial dose is 1 g at bedtime, before bed, and if necessary in the morning.

    The highest daily dose: 160 mg.

    The highest single dose: 40 mg.

    Side effects:

    Central and peripheral nervous system: motor anxiety, dizziness, headache, attention disturbance.

    Respiratory system: rarely - shortness of breath.

    The system of hematopoiesis: hypocoagulation.

    The cardiovascular system: sensation of fever, arterial hypotension, tachycardia, collapse.

    Digestive system: nausea, vomiting, dry mouth, burning sensation of the tongue.

    Sense organs: a disorder of vision.

    Musculoskeletal system: stiffness of movements.

    Dermatological reactions: skin rash.

    Allergic reactions.

    Overdose:

    Orthostatic hypotension, hyperthermia, convulsions. With infusion in high doses, methhemoglobinaemia develops: cyanosis of the lips, nails and palms, tachypnea, sensation of pressure in the head.

    Treatment: discontinuation of infusion, intravenous 1% methylene blue, dopamine and sympathomimetics. The patient is given a horizontal position with the legs raised, if the arterial pressure is not normalized, volume of circulating blood, connect artificial ventilation, produce an exchange blood transfusion.

    Interaction:

    Potentiates the effect of antihypertensive drugs, weakens the action of norepinephrine and epinephrine.

    With the combined intake of alcohol, a collapse develops.

    Special instructions:

    To prevent hypotension and "nitrate" headache, treatment should begin with the minimum recommended dose. With prolonged use, there is an addiction that can be cross-over. In order to prevent the development of addiction, it is recommended after 3-6 weeks of regular intake to take a break for 3-5 days.

    Patients taking isosorbide nitrate are advised to exercise caution when driving vehicles and working with moving machinery.

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