Description of pharmacological action.
Increases the free radical content of nitric oxide (NO), which activates the guanylate cyclase and increases the content of GMP (controls the dephosphorylation of light chains of myosin) in the smooth muscle cells of the vessels. It extends predominantly venous vessels, causes the deposition of blood in the venous system and reduces the venous return of blood to the heart (preload) and the terminal diastolic filling of the left ventricle. Systemic arterial vasodilatation (widens mainly large arteries) is accompanied by a decrease in OPSS and AD, i.e. post load. Decrease in pre- and post-loading on the heart leads to a decrease in myocardial oxygen demand; reduces increased central venous pressure and wedging pressure in the pulmonary capillaries; slightly increases the heart rate (reflex tachycardia in response to a decrease in systemic BP and stroke volume, more pronounced in the vertical position of the body), weakens the resistance of the coronary arteries and improves the cardiac blood flow (except for cases of excessive reduction in systemic blood pressure or a significant increase in heart rate when coronary blood flow may worsen ).
Indications for use Nitroglycerin.
Peripheral vasodilator with predominant effect on venous vessels.
The effect of nitroglycerin is mainly associated with a decrease in the demand for myocardium in oxygen due to a decrease in preload (the expansion of peripheral veins and a decrease in the flow of blood to the right atrium) and postload (a decrease in OPSS).
It exhibits a central inhibitory effect on sympathetic vascular tone, inhibiting the vascular component of the pain syndrome. Causes the expansion of meningeal vessels, which explains the headache when it is used.
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When using sublingual forms, an attack of angina pectoris usually stops after 1.5 minutes, the hemodynamic and antianginal effect persists for 30 to 60 minutes.
Quickly and completely absorbed on the surface of the mucous membranes.
At sublingual application at once gets to a system blood flow.
At sublingual admission in a dose of 0.5 mg bioavailability is 100%, Cmax in the blood plasma is determined after 5 minutes. Has a very large volume of distribution. Binding to blood plasma proteins – 60%.
Use during pregnancy
During pregnancy and breastfeeding, taking the drug is possible only for life indications.
Hypersensitivity, severe hypotension, collapse, myocardial infarction with low end-diastolic pressure in the left ventricle and / or severe hypotension (SBP below 90 mmHg) or collapse, right ventricular infarction, bradycardia less than 50 beats. Mine, primary pulmonary hypertension, cerebral hemorrhage, head trauma, increased intracranial pressure, cerebral ischemia, cardiac tamponade, toxic pulmonary edema, severe aortic stenosis, conditions accompanied by a decrease in the end diastolic pressure in the left ventricle (isolated mitral stenosis, constructive pericarditis) , glaucoma, pregnancy, breast-feeding.
From the cardiovascular system: dizziness, nitric headache, tachycardia, skin hyperemia, fever, low blood pressure rarely (especially when overdosed) – orthostatic collapse, cyanosis.
From the gastrointestinal tract: dry mouth, nausea, vomiting, abdominal pain.
From the side of the central nervous system: rarely (especially with an overdose) – anxiety, psychotic reactions, inhibition, disorientation, blurred vision, headache (especially at the beginning of the course of treatment, with prolonged therapy decreases), dizziness and a sense of weakness.
Allergic reactions are possible.
Dosing and Administration
Nitroglycerin is recommended for taking by the doctor’s prescription.
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The tablet is kept under the tongue until complete resorption, without swallowing, immediately after the onset of pain – 0.5-1 mg per reception. In many patients with stable angina, the effect comes from a smaller dose (1 / 2-1 / 3 tablets), so if the pain quickly passes, the rest of the tablet does not have time to resolve, it is advisable to spit out. Usually, the antianginal effect is manifested after 0.5-2 min; 75% of patients noted improvement during the first 3 min, and another 15% – within 4-5 min.
In the absence of an antianginal action, during the first 5 minutes one should take another 1 tab. Of Nitroglycerin.
If there is no therapeutic effect after taking 2-3 tablets you need to call a doctor immediately. The duration of action after sublingual administration is about 45 minutes.
At frequent attacks of a stenocardia it is accepted to appoint the prolonged preparations of a nitroglycerin series. Tolerance to sublingual forms of nitroglycerin develops infrequently, but when it occurs in some patients the dose of the drug has to be gradually increased, bringing it to 2-3 tablets.