Nitroglycerin ampoules 0.1% 10ml №10

Description

Release form
Concentrate for solution for infusion

1 ml. contains nitroglycerin 1 mg.
Packaging
10 amp. on 10 ml.

Mechanism of action

Nitroglycerin is a peripheral vasodilator with a predominant effect on the venous vessels. Antianginal agent. 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 ultimately leads to relaxation of smooth muscle. Under the influence of nitroglycerin, 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 nitroglycerin is mainly associated with a decrease in myocardial oxygen demand due to a decrease in preload (dilation of peripheral veins and a decrease in blood flow to the right atrium) and an afterload (decrease in OPS). Promotes the redistribution of coronary blood flow in the ischemic subendocardial areas of the myocardium. Increases tolerance to physical exertion in patients with coronary artery disease, angina.In heart failure, it promotes myocardial discharge, mainly due to a decrease in preload. Reduces pressure in the pulmonary circulation.

Indications and usage

IHD: angina pectoris (treatment, prophylaxis), vasospastic stenocardia (Printsmetal), unstable stenocardia, spasm of the coronary arteries during coronary angiography, acute coronary syndrome, acute myocardial infarction, acute left ventricular failure (cardiac asthma, asthma, myocardial infarction, acute left ventricular failure (cardiac asthma, asthma, myocardial infarction, acute left ventricular failure (cardiac asthma, asthma, myocardial infarction), acute left ventricular failure (cardiac asthma, asthma, myocardial infarction, acute left ventricular insufficiency (cardiac asthma, acute myocardial infarction, acute left ventricular failure (cardiac asthma, asthma, myocardial infarction), acute left ventricular insufficiency (cardiac asthma, acute myocardial infarction, acute left ventricular failure (cardiac asthma, asthma) heart failure, controlled hypotension during surgical procedures, prevention of hypertensive reactions during endotracheal intubation, resolution skin, sternotomy, occlusion of the central retinal artery, esophageal dyskinesia, functional choleysystopathy, acute pancreatitis, biliary colic, spastic bowel dyskinesia.

Contraindications

Hypersensitivity, pronounced hypotension, collapse, myocardial infarction with low end diastolic pressure in the left ventricle and / or severe hypotension (systolic blood pressure below 90 mm Hg) or collapse, right ventricular infarction, bradycardia less than 50 beats / min, primary pulmonary hypertension, cerebral hemorrhage, head injury, increased intracranial pressure, cerebral ischemia, cardiac tamponade, toxic pulmonary edema, marked aortic stenosis, conditions,accompanied by a decrease in end-diastolic pressure in the left ventricle (isolated mitral stenosis, constrictive pericarditis), angle-closure glaucoma, pregnancy, breast-feeding.

Dosage and administration

Treatment should be carried out with an individual selection of the rate of intravenous drug administration. The solution is administered through an automatic dispenser or via an infusion pump, which allows the solution to be injected with precise dosing of the administration rate and the total dose. Automatic dispenser allows you to enter even undiluted 0.1% solution with accurate dosing of the rhythm of the injection and the total dose.
Introduction through the usual system for transfusion of liquids provides the choice of the exact dose by counting the number of drops of the liquid to be poured; for this, the solution of nitroglycerin is preliminarily diluted with 0.9% sodium chloride solution or 5% dextrose solution (glucose) —do not use other solvents to a concentration of 0, 01% nitroglycerin. Selection of the dose and rate of administration is carried out individually, taking into account blood pressure (BP), heart rate (HR), central venous pressure, ECG and other indicators.
When using a system of polyvinyl chloride tubes, the active substance is absorbed and the losses on the walls of the tubes range from 40 to 80% (it is advisable to use polyethylene and glass tubes). The solution quickly collapses in the light, so the bottles and the transfusion system must be shielded with an opaque material.

Adverse reactions

On the part of the nervous system and sensory organs: headache, dizziness, headache, weakness, motor restlessness, psychotic reactions, blurred vision, exacerbation of glaucoma.
From the side of the cardiovascular system and blood (blood formation, hemostasis): flushing of the face, palpitations, hypotension, incl. orthostatic, collapse, methemoglobinemia.
On the part of the digestive tract: dry mouth, nausea, vomiting, diarrhea,
On the part of the skin: cyanosis, skin flushing.
Allergic reactions: itching and burning, allergic contact dermatitis (when using transdermal forms).
Others: hypothermia, sensation of heat, paradoxical effects - an attack of angina, ischemia until the development of myocardial infarction and sudden death; development of tolerance.

In the acute period of myocardial infarction and with the development of acute heart failure, it is prescribed under strict hemodynamic control. With caution used in aortic and mitral stenosis, in patients with hypovolemia and low syst. HELL (less than 90 mm Hg). In hypertrophic cardiomyopathy, it can cause an increase in and / or weighting of strokes. With long-term uncontrolled intake of nitroglycerin, the appointment of high doses to patients with liver failure and children increases the risk of methemoglobinemia, manifested by cyanosis and the appearance of blood brown tint.In cases of methemoglobinemia, the drug should be urgently canceled and the antidote methylthioninium chloride (methylene blue) should be introduced. If necessary, the further use of nitrates is required to control the content of methemoglobin in the blood or the replacement of nitrates for sydnonimine.
To reduce the risk of side effects, care must be taken while taking it with drugs that have pronounced hypotensive and vasodilating properties; It is not recommended to take the drug on the background of alcohol consumption, in rooms with high ambient temperatures (bath, sauna, hot shower), as well as taking several pills simultaneously or sequentially in a short period of time at the first dose.
You can not chew pills and capsules in order to stop an attack of angina, because An excess amount of the drug from the destroyed microcapsules can enter the systemic circulation through the oral mucosa. When a headache and other unpleasant sensations occur in the head area, the improvement is achieved by prescribing Validol or menthol drops sublingually. Often, only the first doses are poorly tolerated, then the side effects subside.
With simultaneous use with Heparin, it is necessary to increase the dose of heparin and strictly control the partially activated thromboplastin time. It is used with caution in elderly patients. It is not recommended to assign buccal forms to patients with aphthous stomatitis, gingivitis, periodontal diseases and the root system of the teeth, removable upper dentures.
Uncontrolled reception can lead to the development of tolerance, expressed in reducing the duration and severity of the effect with regular use or the need to increase the dose to achieve the same effect. With regular use of prolonged forms of nitroglycerin, especially patches and ointments, the drug is almost always present in the blood, so the risk of tolerance increases significantly. To prevent the onset of resistance, intermittent administration is necessary during the day, or co-administration of Calcium antagonists, ACE inhibitors, or diuretics. Transdermal forms of nitroglycerin are recommended to be removed from the body at night, thus leaving a period free from the action of the drug. It should beware of the development of withdrawal syndrome associated with a sharp cessation of the supply of nitroglycerin into the body and manifested by the sudden development of strokes.
With the on / in the introduction of possible development of tachyphylaxis, which requires a change in dosage upwards. The degree of tolerance can be judged by the dynamics of pressure in the right atrium. The approximation of the tolerance index to 25% requires that the solution be stopped. To simulate the development of tolerance when administered intravenously may decrease the content of nitroglycerin in the solution due to a violation of the technique of administration, destruction of nitroglycerin by direct exposure to light rays or its absorption on the walls of a plastic infusion system (20–80% when using systems from polyvinyl chloride, polystyrene-butadiene, cellulose propionate, latex or polyurethane). It is recommended to use systems from chemically pure glass, polyethylene, nylon, Teflon, silicone. It is not recommended to use too long hydraulic lines. With the on / in the introduction of nitroglycerin, it must be borne in mind that after stopping the infusions and transferring the patient to pills (even long-acting) nitrates, withdrawal syndrome or an insufficient dose may occur, with an increase in the frequency of complications in the acute period of myocardial infarction — increasing angina attacks phenomena of circulatory failure, recurrence of myocardial infarction, the formation of acute cardiac aneurysm, an increase in the frequency of myocardial ruptures.

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Salicylates increase plasma nitroglycerin levels, barbiturates speed up metabolism. Nitroglycerin reduces the pressure of adrenergic agonists, the anticoagulant effect of heparin (with a / in the introduction). Antihypertensives, antiadrenergic drugs, vasodilators, Sildenafil citrate, calcium antagonists, tricyclic antidepressants, MAO inhibitors, ethanol, quinidine and Novocainamide enhance the hypotensive and systemic vasodilating effects.Methionine, N-acetylcysteine, ACE inhibitors and salicylates increase antianginal activity. Unithiol restores reduced sensitivity to nitroglycerin. Dihydroergotamine, m-cholinolytics, alpha adrenergic mimetics, histamine, pituitrin, corticosteroids, CNS stimulants and vegetative ganglia, bee venom and snakes, excessive insolation reduces vasodilator and antianginal effects.

Storage conditions
In a dark place and out of reach of children, away from fire, at a temperature of 5 ° C to 25 ° C.