IZOSORBIDA DINITRAT (Isosorbide dinitrate)

     Chemical name : 1,4:3,6 - Diangidrido-D- glyutsita dinitrate

     Description : The white powder melkokristallichesky odourless. Almost nerastvorim water well soluble in acetone, alcohol, ether.

     Pharmacology : The drugs act-antianginalnoe, salts.

Increases of nitric oxide (endotelialnogo relaxing factor) in endotelii receptacles. Has properties primarily venous and arterial dilatatora. Decreases in the pre - and postnagruzku heart attack reduces the need for oxygen and decreases wall Poly has koronarorasshiryayuschee act to redistribute coronary blood flow in the ischemic area, lowers pressure in a small circle of blood. It was lower end diastolic pressure in the heart Poly, a temporary reduction in the average AD Systems, reduced cardiac index. Do not choose or change leads to a slight expansion. Expands vascular brain. System peripheral vascular resistance changed little, pulmonary vascular resistance reduces rack. Has improved systolic function of the heart by reducing postnagruzki and reflexive sympathetic nervous system stimulation.

When administered quickly and completely absorbed, but the bioavailability is not more than 22% (due to the effects of "first pass" through the liver); With sublingual application about 60%. Linking with low plasma proteins (30%). T1 / 2-20 min, 60 min, 4 h with / w, sublingual and oral respectively. Forms two active metabolite - isosorbide? 5-mononitrate (75-85%) and isosorbide? 2-mononitrate (15-25%), with longer periods half. Excreted kidneys (almost entirely in the form of metabolites).

Early action when administered in the form of chewing tablets and sublingvalnyh been through 2-5 minutes, capsules and tablets - min 15-40, prolonged forms-30 minutes. Duration 1-2 h, 4-6 h and 12 h, respectively. After spreading to the mucous membrane of the mouth effect is manifested through 30 and lasts 15-120 minutes. In a lengthy admission may develop tolerance.

     Application : Unstable angina (mild and preventing attacks), including unstable, acute myocardial infarction, since migrated myocardial infarction (ARE), the acute levozheludochkovaya failure, arterial hypertension, long-term heart failure, pulmonary hypertension, chronic pulmonary heart, prevention and treatment koronarospazma in koronaroangiografii.

     Contraindications : Giperchuvstvitelnost, anemia, brain haemorrhage or recently transferred trauma, hemorrhagic stroke, raising vnutricherepnogo pressure zakrytougolnaya glaucoma, Ray, shock, collapse, hypotension (sAD below 100 mm Hg. Art.) , Myocardial infarction or heart failure with low the pressure of filling the left ventricle, stenoses Aortic or mitral valves, gipertroficheskaya obstructive cardiomyopathy with output tract left ventricle, toxic swelling of the lungs, glucose deficit? 6-fosfatdegidrogenazy, pregnancy (I term), breastfeeding, childhood.

     Restrictions : To propensity to Orthostatic Hypotension, pregnancy (II and III trimester).

     Application of pregnancy and breastfeeding : Protivopokazano application I trimester of pregnancy. Appointment of II-III trimester of pregnancy is possible only on the strict condition and under constant medical supervision. At the time of treatment should stop breastfeeding.

     Side Effects : Tide blood to the face and neck, headache, dizziness, nausea, vomiting, burning feeling on the tip of the language Orthostatic Hypotension, collapse, burn concern, rigidity, violation attention, tachycardia, lifting syndrome.

     Networking : adsorbents, binders and coating means reduced intake of the digestive tract. Antigipertenzivnye means (beta adrenoblokatory, calcium antagonists, etc. vazodilatatory) digidroergotamin, procainamide, quinidine, Tricyclic antidepressants, neuroleptic, sildenafila citrate and alcohol increase hypotension, simpatomimetiki reduce antianginalny effect combination with atropine increases the likelihood of improving inner pressure.

     Overdosing : Symptoms : nitrate (cyanosis lips and nails, anoxia), a strong fear or dizziness, collapse, feeling pressure in the head, weakness, dizziness, weakness and palpitations, aetiology, elevated body temperature, brain hypertension, convulsions, nausea, vomiting, diarrhoea, dispnoe, visual impairment.

Treatment : washing stomach, symptomatic treatment, in-natal appointment metiltioniniya chloride (Methylene blue) in the dose of 1-2 mg / kg / w.

     Dosing and Administration : inside, sublingvalno in / in, inhalation, nakozhno. When strokes : capsules and tablets for 5-20 mg every 6 h (if necessary up to 20-40 mg four times daily); Dosage forms acting on 40-80 mg every 8-12 h (ingest a whole); Chewing tablets, 5 mg every 2-3 hours

Sublingvalno on 2,5-5 mg, if necessary, every 2-3 hours

In severe heart attacks and acute lack levozheludochkovoy / w : initial dose of 1-2 mg / h, the maximum dose of 8-10 mg / h.

Inhalation for cupping the strokes : 1-3 doses dispersed in the mucous membrane of the mouth every 30 seconds, in the face of delays breathing.

Nakozhno 1 g cream / 2 doses cause of skin.

     Precautions : There is a need to be cautious about the appointment of patients tend to Orthostatic Hypotension. For patients with AD initially reduced to be combined with the introduction of products with a positive inotropnym action. Recommended control and AD CHSS, especially at the beginning of treatment. In early treatment must be especially careful to persons whose work requires quick mental and motor responses. The patient should be given that the side effects against the backdrop of growing acceptance of alcohol. For prevention of adjusting after 3-6 weeks of regular admission to make a break for 3-5 days.

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