Nitroglycerin

When ATH:
C01DA02

Characteristic.

Colorless oily liquid. Poorly water soluble, well - alcohol, ether, xloroforme.

Pharmacological action.
Antianginalnoe, vasodilator, venodilatiruyuschee, vasodilatig.

Application.

CHD: angina (treatment, prevention), vasospastic angina (Princmetala), unstable angina, spasm of the coronary arteries during coronary angiography, acute coronary syndrome, acute myocardial infarction, acute left ventricular failure (cardiac asthma, interstitial and alveolar pulmonary edema), congestive heart failure, controlled hypotension during surgical procedures, Warning hypertensive reactions during endotracheal intubation, skin incision, sternotomy, occlusion of the central retinal artery, dyskinesia pishtevoda, Functional holetsistopatii, acute pancreatitis, zhelchnыe colic, spasticheskaya dyskinesia kishechnika.

Contraindications.

Hypersensitivity, pronounced hypotension, collapse, myocardial infarction with low end-diastolic pressure in the left ventricle and / or severe hypotension (Sad below 90 mmHg.) or collapse, right ventricular infarction, bradycardia me 50 u. / min, Primary pulmonary hypertension, cerebral hemorrhage, head injury, increased intracranial pressure, cerebral ischemia, cardiac tamponade, toxic pulmonary edema, vыrazhennыy aortalnыy stenosis, states, accompanied by a decrease in end-diastolic pressure in the left ventricle (yzolyrovannыy mytralnыy stenosis, constrictive pericarditis), zakrыtougolynaya glaucoma, pregnancy, lactation.

Restrictions apply.

Anemia, gipertroficheskaya cardiomyopathy (idiopathic hypertrophic stenosis subaortalnыy), advanced age, severe liver and kidney, hyperthyroidism.

Pregnancy and breast-feeding.

Pregnancy is possible only in cases, the expected benefit outweighs the potential risk to 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: headache, dizziness, Tearing head, weakness, restlessness, psychotic reactions, blurred vision, aggravation of glaucoma.

Cardio-vascular system and blood (hematopoiesis, hemostasis): flushing, heartbeat, gipotenziya, incl. orthostatic, collapse, metgemoglobinemiâ.

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

For the skin: cyanosis, dermahemia.

Allergic reactions: itching and burning, contact type allergy (when using transdermal).

Other: gipotermiя, feeling the heat, paradoxical effects — stroke, ischemia until the development of myocardial infarction and sudden death; the development of tolerance.

Cooperation.

Salicylates increase the level of nitroglycerin in plasma, barbiturates accelerate metabolism. Nitroglycerin reduces the pressor effect of agonists, anticoagulant effect of heparin (at / in the introduction). Antihypertensive, antiadrenergic drugs, vasodilators, sildenafil citrate, calcium antagonists, tricyclic antidepressants, MAO inhibitors, ethanol, quinidine and procainamide increase the hypotensive effects and systemic vasodilator. Methionine, N-ацетилцистеин, ACE inhibitors and salicylates increase antianginal activity. Unitiol restores reduced sensitivity to nitroglycerin. Digidroergotamin, Mr. anticholinergics, alpha-adrenergic agonists, histamine, pituitrine, corticosteroids, CNS stimulants, and autonomic ganglia, poisons bees and snakes, excessive sun exposure reduces the vasodilator and antianginal effects.

Overdose.

Symptoms: headache, dizziness, strong feeling of pressure in the head, unusual tiredness or weakness, fainting, hot flashes or chills, increased perspiration, heartbeat, nausea and vomiting, cyanosis of the lips, nails, or palms, breathlessness, gipotenziya, weak rapid pulse, fever, increased intracranial pressure (brain symptoms until the development of convulsions and coma), metgemoglobinemiâ.

Treatment: Transfer the patient to a horizontal position (legs raised above the head to increase venous return to the heart), gastric lavage (if after ingestion it was not long), plazmozameniteli, / in the introduction of the alpha-adrenergic agonists (Phenylephrine). Avoid introduction as a means of cardiac epinephrine because of the potential gain shock-like reaction. To eliminate methemoglobinemia use oxygen under pressure or 1% methylthioninium chloride solution (Methylene blue) at a dose of 1-2 mg/kg, I /. It is recommended that monitoring of the concentration of methemoglobin in the blood.

Dosing and Administration.

B / (should be diluted 5% glucose solution and isotonic saline to a final concentration 50 or 100 ug / ml): 0,005 mg / min, the dose of 0,005 mg/min every 3-5 minutes to obtain the effect or achieve speed 0,02 mg / min (with inefficiency — further enhancing the 0,01 mg / min).

Sublingual: pills-0.15-0.5 mg per reception, if necessary, repeated at 5 m; aerosol — to attack heavily strokes — 1-2 doses under the tongue, pressing the metering valve (can be repeated, but not more 3 doses within 15 m). In the case of acute left ventricular failure can be applied 4 or more doses within a short period.

Transdermal: paste each time to a new patch of skin and leave for 12-14 h, and then removed, to provide a break for 10-12 hours in order to prevent the development of tolerance.

Inside: tablets and capsules taken without chewing and breaking a, 2-4 Times a day before meals, it is desirable for 30 min before exercise, single dose of 5-13 mg; due to poor bioavailability of single dose can increase up to 19,5 mg.

Subbukkalno: tablet is placed on the oral mucosa (for shtekoy) and kept until resorption: by 2 mg 3 once a day.

Precautions.

In the acute phase of myocardial infarction and in the development of congestive heart failure prescribed under the strict control of hemodynamics. To use caution in aortic and mitral stenosis, in patients with hypovolemia and reduced Sad (less 90 mmHg.). In hypertrophic cardiomyopathy can cause more frequent and / or worsening of angina attacks. Prolonged uncontrolled taking nitroglycerin, high doses in patients with hepatic insufficiency and children increases the risk of methemoglobinemia, manifested cyanosis and appearance of blood in a brown tint. In cases where the development of methemoglobinemia drug there is an urgent need to cancel and enter the antidote-metiltioninija chloride (Methylene blue). If necessary, further use of nitrates required control over the content of methemoglobin in the blood, or the replacement of nitrates sydnonimine.

To reduce the risk of side effects must be careful while taking medicine, has a pronounced hypotensive and vasodilating properties; it is not recommended taking the drug on a background of alcohol, in areas with high ambient temperatures (bathroom, sauna, hot showers), and taking multiple pills simultaneously or sequentially in a short period of time when the first reception.

You can not chew the tablets and capsules for, to stop an attack of angina pectoris, tk. into the systemic circulation can do an excessive amount of drug from the destroyed microcapsules through the oral mucosa. When the headache and other unpleasant sensations in the head improvement is achieved validol appointment or sublingual drops of menthol. Often poorly tolerated, only the first dose, then the side effects subside.

While the use of heparin is necessary to increase the dose of heparin and strictly control the activated partial thromboplastin time. To use caution in elderly patients. Not recommended the appointment of buccal forms of patients with aphthous stomatitis, gingivitom, periodontal disease and tooth root, removable upper denture.

Uncontrolled intake 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 doses to achieve the same effect. With regular use of prolonged forms nitroglycerin, especially plasters and ointments, drug almost always present in the blood, therefore, the risk of developing tolerance is greatly increased. In order to prevent the emergence of stability is required intermittent reception during the day, or co-administration of calcium antagonists, ACE inhibitors, or diuretics. Transdermal nitroglycerin is recommended to remove from the body at night, thus leaving the period, free of drug action. We should beware of withdrawal, associated with abrupt discontinuation of receipt of nitroglycerin in the body and is manifested by a sudden development of angina attacks.

The on / in a possible development of tachyphylaxis, that require changing the dosage upwards. The degree of tolerance can be measured by dynamic pressure in the right atrium. Approaching index tolerance 25% It requires cessation of a solution. Simulate the development of tolerance when administered intravenously can decrease of nitroglycerine in the solution due to violations of technology introduction, destruction of nitroglycerin with direct exposure to light rays or absorption on the walls of a plastic infusion system (20-80% Using systems of polyvinyl chloride, polystyrene-butadiene, cellюlozo-propionate, latex or polyurethane). It is recommended to use a system of chemically pure glass, Polyethylene, nylon, Teflon, Silicone. Do not use too long hydraulic lines. The on / in the introduction of nitroglycerin should be considered, that after stopping the infusion and transfer the patient to tablets (Even long-acting) Nitrates may be withdrawal or insufficient dose, in doing so, it increases the frequency of complications in the acute period of myocardial infarction — showing strokes, the growth phenomena of circulatory failure, recurrence of myocardial infarction, the formation of acute heart aneurysm, increased frequency of myocardial rupture.

Cooperation