NITRO

Active material: Nitroglycerin
When ATH: C01DA02
CCF: Peripheral vasodilators. Antianginal drug
When CSF: 01.06.01.01.05
Manufacturer: ORION CORPORATION (Finland)

DOSAGE FORM, COMPOSITION AND PACKAGING

The solution for infusion concentrate clear, colorless.

Excipients: ethanol 96%, propylene glycol n / parenteral approx., water d / and.

2 ml – glass ampoule (5) – packs cardboard.

The solution for infusion concentrate clear, colorless.

Excipients: ethanol 96%, propylene glycol n / parenteral approx., water d / and.

5 ml – glass ampoule (5) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES.

Pharmacological action

Peripheral vasodilator with a primary effect on the venous vessels. Antianginal drugs. The mechanism of action involves the release of active substance nitric oxide in vascular smooth muscle. Nitric oxide causes the activation of guanylate cyclase and increases the level of cGMP, which ultimately leads to smooth muscle relaxation. Under the influence of nitroglycerin arterioles and precapillary sphincters relax to a lesser extent, than the large arteries and veins. This is partly due to the reflex reactions, and less intense form of nitric oxide molecules of the active substance in the walls of arterioles.

The action of nitroglycerin is mainly due to a decrease in myocardial oxygen demand by reducing preload (expansion of peripheral veins and reducing blood flow to the right atrium) and afterload (reduction in systemic vascular resistance). It promotes redistribution of coronary blood flow in the ischemic area of ​​subendocardial infarction. It increases exercise tolerance in patients with coronary artery disease, stenokardiey. In heart failure contributes to the unloading of the myocardium is mainly due to the decrease of preload. It reduces the pressure in the pulmonary circulation.

Pharmacokinetics

Once inside absorbed from the gastrointestinal tract, exposed effect “first pass” through the liver. With sublingual application of this effect is absent, a therapeutic plasma concentration reached within a few minutes. It is metabolized in the liver with the participation of nitrate. From dinitro metabolites of nitroglycerin can cause pronounced vasodilation; perhaps, they determine the therapeutic effects of nitroglycerin when administered.

Plasma protein binding is 60%. T_1/2 after ingestion – 4 no, if sublingual application – 20 m, After i / v administration – 1-4 m. Report mostly kidneys.

Testimony

Sublingual and buccal administration: relief and prevention of angina attacks; as a means of first aid for acute myocardial infarction and acute left ventricular failure prehospital.

Orally: relief and prevention of angina attacks, rehabilitation treatment after myocardial infarction.

For i / v administration: acute myocardial infarction, incl. Complications of acute left ventricular failure; unstable angina; pulmonary edema.

For cutaneous use: prevention of angina attacks.

Dosage regimen

Apply sublingual, buccal, inside, fur gloves, / drip. The dose and treatment regimen set individually, depending on the evidence, specific clinical situation, the dosage form.

Side effect

Cardio-vascular system: dizziness, headache, tachycardia, flushing of the skin, feeling the heat, hypotension; rarely (especially in overdose) – collapse, cyanosis.

From the digestive system: nausea, vomiting.

CNS: rarely (especially in overdose) – anxiety, psychotic reactions.

Allergic reactions: rarely – skin rash, itch.

Local reactions: tingling, burning, erythema.

Other: metgemoglobinemiâ.

Contraindications

Shock, collapse, hypotension (systolic blood pressure<100 mmHg., diastolic blood pressure<60 mmHg.), acute myocardial infarction with severe hypotension, gipertroficheskaya obstruktivnaya cardiomyopathy, constrictive pericarditis, cardiac tamponade, toxic pulmonary edema, intracranial hypertension (incl. in hemorrhagic stroke, after a recent head trauma), angle-closure glaucoma with high intraocular pressure. Hypersensitivity to nitrates.

Pregnancy and lactation

The use of nitroglycerin during pregnancy and lactation (breast-feeding) only in cases, when the intended benefits to the mother outweighs the potential risk to the fetus or infant.

Cautions

To use caution in patients with severe cerebral arteriosclerosis, disorders of cerebral circulation, a tendency to orthostatic hypotension, with severe anemia, elderly patients, as well as hypovolemia and expressed violations of the liver and kidneys (for parenteral application).

With prolonged use may develop tolerance to the effects of nitrates. To avoid tolerance recommend that a 10-12-hour break in their application for each 24-hour cycle.

If cutaneous application of nitroglycerin occurs angina, it should be to stop taking nitroglycerine under the tongue.

During treatment, avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

Nitroglycerin can reduce the speed of psychomotor reactions, that should be taken into consideration when driving vehicles or busy with other potentially hazardous activities.

Drug Interactions

While the use of vasodilators, ACE inhibitors, calcium channel blockers, beta-blockers, Diuretics, tricyclic antidepressants, MAO inhibitors, ethanol, ethanol-containing drugs may increase the hypotensive effect of nitroglycerin.

While the use of beta-blockers, calcium channel blockers enhanced antianginal.

In an application with sympathomimetics may reduce the antianginal effect of nitroglycerin, which, in turn, may reduce the pressor effect sympathomimetic (as a result of possible hypotension).

With simultaneous use of funds, having anticholinergic activity (incl. tricyclic antidepressants, dizopiramida) developing sialoschesis, dry mouth.

There are limited data on, that acetylsalicylic acid, used as an analgesic agent, increases the concentration of nitroglycerin in the blood plasma, which may be accompanied by increased hypotensive effect and headaches.

Several studies observed a decrease vasodilating effect of nitroglycerin on the background of long-term therapy with acetylsalicylic acid.

It is believed, that may increase the antiplatelet action of aspirin.

While the use of nitroglycerin decreases the action of acetylcholine, gistamina, noradrenaline.

Against the background of / in the nitroglycerin may reduce the anticoagulant effect of heparin.

With simultaneous use may increase the bioavailability of dihydroergotamine and reduced antianginal effect of nitroglycerin.

In an application with novokainamidom may increase the hypotensive effect and development of collapse.

In an application with rizatriptanom, sumatriptan increases the risk of coronary artery spasm; with sildenafilom – risk of severe hypotension and myocardial infarction; with quinidine – possible orthostatic collapse; ethanol – severe weakness or dizziness.