Isoket, solution for infusions of 0,1% 10 ml N10
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Description
Isoket is a peripheral vasodilator with a predominant effect on the venous vessels. The mechanism of action is associated with the release of the active substance nitric oxide in the smooth muscles of the blood vessels. Nitric oxide causes the activation of guanylate cyclase and increases the level of cGMP, which leads to relaxation of smooth muscles. Under the influence of isosorbide dinitrate, arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. This is partly due to reflex reactions, as well as the less intense formation of nitric oxide from the molecules of the active substance in the walls of arterioles. The action of isosorbide dinitrate is mainly due to a decrease in myocardial oxygen demand due to a decrease in preload (expansion of peripheral veins and a decrease in blood flow to the right atrium) and afterload (reduction of OPSS), as well as direct coronary dilating action. Isosorbide dinitrate contributes to the redistribution of coronary blood flow in an area with reduced blood supply, reduces pressure in the pulmonary circulation. In heart failure, it helps to relieve the myocardium by reducing preload.
Active ingredients
Isosorbide dinitrate
Release form
Solution
Composition
Isosorbide dinitrate, sodium chloride, water.
Indications
Acute myocardial infarction with left ventricular failure, acute left ventricular failure, heart failure of various etiologies, unstable angina.
Precautionary measures
Contraindications: - acute vascular insufficiency (shock, vascular collapse), - severe arterial hypotension (systolic blood pressure less than 90 mm Hg, diastolic blood pressure less than 60 mm Hg), - hypertrophic obstructive cardiomyopathy, - constrictive pericarditis, - tampamus, constrictive pericarditis, - tampos obstructive cardiomyopathy, - constrictive pericarditis, - tampamus, constrictive pericarditis, - tampos obstructive cardiomyopathy, - constrictive pericarditis, - tampos, constrictive pericarditis, - tampos obstructive cardiomyopathy, - constrictive pericarditis, - tampos, cardiac pericardiomyopathy, - tampos obstructive cardiomyopathy, - constrictive pericarditis, - tampos, nodal pericarditis, - tampos obstructive cardiomyopathy, - constrictive pericarditis, - tampos, constrictive pericarditis, - tampos obstructive cardiomyopathy; heart, - cardiogenic shock (if correction of the end diastolic pressure of the left ventricle is impossible using intra-aortic counterpulsation or drugs with a positive inotropic effect), - primary pulmonary diseases (because due to relative aspredeleniya flow in zone gipoventiliruemye hypoxemia may occur), - CHD (b.p.redistribution of blood flow can lead to transient myocardial ischemia), - toxic pulmonary edema, - conditions accompanied by increased intracranial pressure (including hemorrhagic stroke, traumatic brain injury), - increased sensitivity to nitrate compounds. acute myocardial infarction with a reduced filling pressure of the left ventricle (this requires the supervision of a physician). The drug should be used with caution and it is necessary to avoid reducing systolic blood pressure below 90 mm Hg. with aortic and / or mitral stenosis, a tendency to orthostatic reactions, diseases that are accompanied by increased intracranial pressure.
Use during pregnancy and lactation
In pregnancy and lactation, the drug should be used very carefully, only in situations where the expected benefit to the mother greatly exceeds the possible risk to the fetus or child. In experimental studies revealed no damaging effects on the fetus.
Dosage and administration
The solution is administered as an intravenous infusion using automatic infusion systems in a hospital setting under constant monitoring of cardiovascular parameters. Depending on the type and severity of the disease, in addition to the usual examination (symptoms, control of blood pressure, heart rate, diuresis), invasive procedures are used to determine hemodynamic parameters. Systems for the intravenous route are polyethylene, polypropylene and polytetrafluoroethylene. Infusion materials made from polyvinyl chloride or polyurethane cause loss of the active substance as a result of adsorption, which must be compensated for by increasing the dose. The dose should be selected individually for each patient. Treatment should begin with low doses, gradually increasing to the required. The initial dose is 2-7 mg / h. In some cases, the dose can be increased to 10 mg / h. For patients with heart failure, as a rule, higher doses are required - in some cases up to 50 mg / h. The average dose is approximately 7.5 mg / h.
Side effects
Since the first use or with an increase in the dose of the drug may decrease blood pressure and / or orthostatic hypotension, which may be accompanied by a reflex pulse rate increase, inhibition, as well as dizziness and a feeling of weakness.At the beginning of treatment, a headache ("nitrate" headache) may appear, which usually disappears after a few days with the further use of the drug. In rare cases, with a marked decrease in blood pressure, there may be an increase in the symptoms of angina pectoris. In rare cases, collaptoid states are observed, sometimes with bradycardia and syncope (seizures with impaired consciousness, dizziness, associated with cerebral circulation disorders as a result of disturbances of the heart rhythm, primarily due to its significant reduction). From the digestive system: rarely - nausea, vomiting . Other: reddening of the skin, allergic skin reactions, in some cases - exfoliative dermatitis.
Interaction with other drugs
With simultaneous use of Isoketa with other vasodilators (vasodilators), antihypertensive drugs, beta-blockers, calcium channel blockers, phosphodiesterase inhibitors of type 5, used to treat erectile dysfunction (eg, sildenafil), neuroleptics, tricyclic antides, anti-erectile dysfunction (eg, Sildenafil), neuroleptics, tricyclic antidefunctional drugs (e.g. actions. With simultaneous use of Isoketa with dihydroergotamine, there may be an increase in the concentration of dihydroergotamine in the blood that leads to increased its hypotensive action.
special instructions
When using the drug Isoket, the cardiovascular system should be monitored: control of blood pressure (systolic blood pressure not lower than 100 mm Hg), ECG monitoring, heart rate, urinary output (bladder catheterization). Since 0.1% Isoket solution is a supersaturated solution, crystallization of the substance may occur. Despite the fact that under normal conditions it does not affect the activity of the drug, in the case of crystallization, the solution is not recommended. It should be noted that the ampoule is already sawn under the blue dot, therefore, no additional dosing is required.