Nitroglycerin is a vasodilator drug used to relieve angina attacks.
Release form and composition
Nitroglycerin is available in three dosage forms:
- Sublingual spray dosed: transparent, colorless (10 ml (200 doses) in cylinders or bottles, 1 bottle each, or a bottle in a cardboard bundle complete with a mechanical dosing pump);
- Sublingual tablets (for sublingual administration): white or almost white, flat-cylindrical, have a rough surface (40 pieces each in polymeric, tightly sealed with a polymer plug, test tubes, 1 tube in a cardboard bundle);
- Concentrate for preparation of solution for infusions: transparent, colorless (2, 5 or 10 ml in ampoules, 5 ampoules in a blister pack, 1-2 or 10 packs in a carton box).
The composition of 1 dose spray sublingual includes:
- Active ingredient: nitroglycerin - 0.4 mg;
- Additional component: 95% ethanol (in the form of a 1% solution).
The composition of 1 sublingual tablet includes:
- Active ingredient: nitroglycerin - 0.5 mg (in terms of 100% substance);
- Additional components: glucose (dextrose) - 9.3 mg; sugar (sucrose) - 7.9 mg; potato starch - 9.3 mg.
The composition of 1 ml of concentrate for the preparation of an infusion solution includes:
- Active ingredient: nitroglycerin - 1 mg;
- Additional components: potassium dihydrophosphate, sodium chloride, dextrose, water for injections.
Indications for use
- Angina pectoris (with the aim of stopping and short-term prophylaxis of strokes before impending exercise or emotional stress);
- Acute myocardial infarction, including complicated by acute left ventricular failure (for infusion);
- Unstable angina (for infusion);
- Pulmonary edema (for infusion).
- Age up to 18 years (for this age group of patients the safety and efficacy of Nitroglycerin has not been established)
- Hypersensitivity to the drug.
Additionally, depending on the form of release of Nitroglycerin, the following conditions / diseases are contraindications to the therapy:
- Any conditions that are associated with increased intracranial pressure (for a sublingual spray);
- Severe arterial hypotension with systolic blood pressure below 90 mm Hg. st. (for the spray sublingual);
- Cardiogenic shock, except in cases where measures are taken to maintain the final diastolic pressure (for a sublingual spray);
- Angina associated with hypertrophic obstructive cardiomyopathy (for sublingual spray);
- Constrictive pericarditis (for sublingual spray);
- Pericardial tamponade (for hyoid spray);
- Acute myocardial infarction and chronic heart failure with a low filling pressure of the left ventricle (for a hyoid spray);
- Primary pulmonary hypertension, severe mitral and / or aortic stenosis (for a sublingual spray);
- Shock (for tablets and spray for sublingual administration);
- Glucose-galactose malabsorption (for tablets for sublingual administration);
- Simultaneous therapy with phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, tadalafil (for tablets and spray for sublingual administration).
Nitroglycerin is prescribed with caution (after the doctor assesses the ratio of benefits with the existing risk) in the presence of such conditions / diseases as:
- Intracranial hypertension;
- Angle-closure glaucoma;
- Hemorrhagic stroke;
- Severe anemia;
- Renal failure (with severe);
- Recent head injuries;
- Hepatic impairment (for tablets for sublingual administration and infusion solution), severe hepatic impairment (for a sublingual spray);
- Heart tamponade (for sublingual tablets and infusion);
- Alcohol Abuse (for sublingual spray);
- Hypotension with low systolic pressure - less than 90 mm Hg. st. (for tablets for sublingual administration and infusion solution);
- Orthostatic hypotension and propensity to develop orthostatic hypotension (for sublingual spray);
- Migraine (for sublingual spray);
- Epilepsy (for sublingual spray);
- Constrictive pericarditis (for tablets for sublingual administration and infusion solution);
- Hypertrophic cardiomyopathy (for tablets for sublingual administration and infusion);
- Isolated mitral stenosis (for tablets for sublingual administration and infusion);
- Toxic pulmonary edema (for infusion);
- Aortic stenosis (for infusion); idiopathic hypertrophic subaortic stenosis (for sublingual tablets);
- Uncontrolled hypovolemia (decrease in circulating blood volume) with low or normal pressure in the pulmonary artery in patients with heart failure (for an infusion solution);
- Acute myocardial infarction, heart failure (chronic) with a low filling pressure of the left ventricle (for tablets for sublingual administration and infusion solution);
- Shock, including cardiogenic, except for cases with a sufficiently high filling pressure of the left ventricle, incl. provided with drugs with positive inotropic action or intra-aortic counterpulsation (for infusion solution);
- Severe cerebral atherosclerosis (for infusion);
- Brain hemorrhage (for infusion solution);
- Pregnancy and breastfeeding period;
- Elderly age (for infusion).
Dosing and Administration
To avoid complications, sublingual use of the drug is possible only after medical prescription.
Spray injected into the tongue or under it, the procedure is preferable to carry out in a sitting position, holding the breath. After a dose of nitroglycerin is injected for a few seconds, it is necessary to close the mouth without swallowing the drug right away. Shake the packaging with a spray before use should not be. When spraying, the bottle must be kept upright.
When the first symptoms of an angina attack appear, 1-2 doses of Nitroglycerin should be injected (determined by the severity of the condition). You can use an additional dose, but within 15 minutes you can use no more than 1.2 mg of the drug (3 doses). If the condition has not improved, it is recommended to consult a doctor.
The maximum single dose of Nitroglycerin - 3 doses.
When using the drug for prophylaxis, usually 5-10 minutes before the expected load or stress, 1 dose is prescribed.
Tablets for sublingual administration
The drug is taken under the tongue without swallowing the pill until complete resorption.
Nitroglycerin must be taken immediately after the first signs of an angina attack appear (or for prophylactic purposes) before the expected emotional stress or physical exertion. A single dose is 1 tablet. With stable angina, the effect of therapy may come from the use of a lower dose. If the condition has improved, the rest of the pill, which by this time did not have time to resolve, is recommended to spit out. Usually (in 75% of patients) the effect of taking Nitroglycerin is noted within 3 minutes. If after 5 minutes after taking the first dose, the condition has not improved, it is recommended to take another 1 tablet. If the seizure is not stopped, you should seek medical attention as soon as possible.
The rate of introduction of the solution of Nitroglycerin is selected by the doctor individually, taking into account blood pressure, heart rate, central venous pressure, electrocardiogram and other indicators. The drug must be administered through an infusion pump or an automatic dispenser, which will allow to precisely dose the solution, as well as control the rhythm of the injection.
The introduction of nitroglycerin using a conventional system for transfusion of liquids ensures the accuracy of its dosage. Prior to administration, the solution of Nitroglycerin should be diluted to a concentration of 0.01% in 0.9% sodium chloride solution or 5% dextrose (glucose) solution. The use of other solvents is not recommended.
The initial rate of introduction of a solution of Nitroglycerin is from 0.5 to 1 mg per hour, the maximum rate is 8-10 mg per hour.
Recommended concentrations and rate of Nitroglycerin administration are (1 ml corresponds to 20 drops): 0.0166 mg / min (1 mg / h) - 24 mg per day through an automatic dispenser (solution volume is 1 mg / ml) or 240 mg per day through system for intravenous administration (solution volume is 0.1 mg / ml); injection rate - 3-4 drops in one minute.
The duration of treatment depends on the clinical indications (from several hours to 2-3 days).
Due to the fact that the active substance is absorbed on the walls of polyvinyl chloride tubes (losses can range from 40 to 80%), the use of tubes made of polyethylene and glass is recommended. In the light, Nitroglycerin infusion solution is rapidly destroyed, therefore, the vials and transfusion systems must be screened with an opaque material. Storage of the drug in the opened ampoule is not allowed.
- Cardiovascular system: fever, lowering blood pressure, dizziness, headache, tachycardia; rarely (in most cases - with an overdose) - cyanosis, orthostatic collapse, increased symptoms of angina pectoris; sometimes - collapse with bradyarrhythmia and loss of consciousness;
- Digestive system: dryness of the oral mucosa; rarely - abdominal pain, nausea, vomiting;
- Central nervous system: weakness; rarely - lethargy, psychotic reactions, disorientation, anxiety;
- Allergic reactions: rarely - exfoliative dermatitis, skin rash, itching;
- Local reactions: flushing of the skin, burning under the tongue;
- Other: rarely - methemoglobinemia, hypothermia, blurred vision.
Do not exceed the recommended dose in the instructions.
Treatment should be interrupted with blurred vision (significant severity or preservation) or dryness of the oral mucosa.
To nitroglycerin, as well as to other organic nitrates, with frequent use may be addictive, which requires an increase in dosage.
Headache during treatment can be reduced by lowering the dose of Nitroglycerin and / or by co-administration of validol.
With frequent strokes, the use of prolonged nitroglycerin drugs is recommended.
The use of alcohol during the use of nitroglycerin is strictly prohibited.
The composition of the sublingual spray includes alcohol, which is important for women during pregnancy and breastfeeding, patients with epilepsy, functional disorders of the liver, after craniocerebral injuries and other diseases of the central nervous system, as well as in cases of alcohol abuse.
1 sublingual tablet contains 2.65 of CH10 -3 grain units (HE).
The composition of the solution for infusion includes glucose (dextrose), which must be considered in case of diabetes.
In acute myocardial infarction or acute heart failure, Nitroglycerin should be used only under close observation of patients.
In order to avoid an increase in angina attacks, abrupt withdrawal of the drug is recommended to be avoided.
Individual selection of the rate of introduction of the Nitroglycerin infusion solution avoids undesirable decrease in blood pressure. Also, blood pressure can decrease even later, against the background of the initially stabilized blood pressure, and therefore, monitoring should be carried out throughout the entire infusion period (at least 3-4 times per hour).
To obtain the necessary hemodynamic effect in patients who have previously used organic nitrates (isosorbide dinitrate, isosorbide-5-mononitrate), higher doses may be required.
During the period of therapy, caution is recommended during driving and when performing potentially hazardous types of work that require quick psychomotor reactions and increased concentration of attention.
With the joint appointment of Nitroglycerin with some drugs may develop the following effects:
- Acetylsalicylic acid: an increase in the level of nitroglycerin in the blood and enhance its action;
- Antihypertensive drugs, vasodilators, procainamide, phosphodiesterase-5 inhibitors, angiotensin-converting enzyme inhibitors, diuretics, slow calcium channel blockers, ethanol, tricyclic antidepressants, monoamine oxidase inhibitors, beta adrenoblockers: increased hypotensive effects,
- Heparin: a decrease in its effectiveness;
- Dihydroergotamine: an increase in its content in the blood and blood pressure.
Terms and conditions of storage
Keep out of the reach of children, protected from light.
- Sublingual spray: 2 years at temperatures up to 15 ° C;
- Tablets for sublingual administration: 2 years at temperatures up to 25 ° C;
- Concentrate for solution for infusion: 3 years at a temperature of 5-25 ° C.