Izosorʙida mononitrat

When ATH:
C01DA14

Characteristic.

The main active metabolite of isosorbide dinitrate. White crystalline solid, without smell, stable in air and in solution, with a melting point of about 90 °C. Easily soluble in water, ethanol, methanol, xloroforme, ethyl acetate and dichloromethane.

Pharmacological action.
Antianginalnoe, vasodilator.

Application.

CHD (long-term treatment), angina and vasospastic (prevention of attacks), post-MI angina, congestive heart failure (combination therapy), pulmonary hypertension.

Contraindications.

Hypersensitivity, acute myocardial infarction with reduced left ventricular filling pressure, acute left ventricular failure, cardiogenic shock, vascular collapse, severe hypotension (Sad less than 90 mmHg.), gipertroficheskaya obstruktivnaya cardiomyopathy, constrictive pericarditis, cardiac tamponade, intracranial hemorrhage, cranial hypertension, severe anemia, glaucoma, pregnancy (I trimester) and breastfeeding.

Restrictions apply.

Acute myocardial infarction, unstable angina, acute coronary syndrome, childhood (safety and effectiveness in children have not been studied).

Pregnancy and breast-feeding.

Use of the drug during pregnancy is possible only in those cases, when the expected benefits outweigh the potential negative effects on the fetus.

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: "Nitrate" headache, weakness, excitation.

Cardio-vascular system and blood (hematopoiesis, hemostasis): transient facial redness; gipotenziya, incl. orthostatic (accompanied by reflex tachycardia, retardation, dizziness, pallor, and others.); in severe hypotension may increase the symptoms of angina (paradoxical effect of nitrates) and / or severe paradoxical bradycardia, collapse, syncope; metgemoglobinemiâ (long-term treatment).

From the digestive tract: dry mouth, nausea, vomiting.

Allergic reactions: burning and itching, exfoliative dermatitis.

Other: Sweating, transient hypoxemia, increase the level of catecholamines and vanilla-succinic acid in the urine.

Cooperation.

It enhances the antihypertensive effect of vasodilators, beta-blockers, calcium antagonists, narcotic analgesics, neuroleptics, tricyclic antidepressants, Sildenafil Citrate, alcohol. When concomitantly with alcohol intensifies reduced ability to rapid mental and motor responses. Barbiturates accelerate the biotransformation and reduce the concentration of isosorbide mononitrate in the blood. It weakens the therapeutic effect of norepinephrine. When concomitantly with NSAIDs may weaken their action.

Overdose.

Symptoms: orthostatic hypotension, the feeling of compression heads, throbbing headache, severe sweating, skin cold, covered with sticky sweat, or erythematous, heartbeat, bradycardia, asequence (blockade), labored breathing, Kussmaul breathing, bloody flux, vomiting, dizziness, confusion, syncope, coma, fever, paralysis, visual impairment.

Treatment: gastric lavage, giving a horizontal position with raised legs, / in the drip infusion solutions, monitoring the level of methemoglobin in the blood, When it is increasing — appointment of Ascorbic acid at a dose 1 g inside, methylthioninium chloride (Methylene blue) in/in to 50 ml 1% solution, toluidina blue-2-4 mg/kg body weight/fast, If necessary, reapply the dose 2 mg/kg with an interval of 1 no, or oxygen therapy, hemodialysis, exsanguinotransfusion.

Dosing and Administration.

Inside, without chewing or breaking a, drinking a small amount of liquid. The dose is determined individually. Initial dose is 10-20 mg 2 times a day, or 40-50 mg once daily in the morning after breakfast (for prolonged forms). If necessary, with 3-5 days of treatment dose can be increased to 20-40 mg 2 times a day or up to 80-100 mg once (for prolonged forms). At reception 2 twice a day is recommended to "asymmetric" scheme: first reception immediately after waking up, the second is later 7 no.

Precautions.

In cases of hypotension used only under medical supervision. In appointing the drug must be particularly careful monitoring of patients with aortic and / or mitral stenosis. Should not be used for the relief of angina attack. It is not recommended to drive and engage in other potentially hazardous activities during treatment (may reduce the concentration and the ability to rapid mental and motor responses). In continuous and prolonged use of high doses may develop tolerance. Abolition of the drug should be gradual to avoid the development of withdrawal.

Cooperation