Nitroglycerin is a means of the group of organic nitrates, mainly a venous dilator. Nitrates are able to release nitric oxide from their molecule, which is a natural endothelial relaxing factor - a mediator of direct activation of guanylate cyclase. Increasing the concentration of cGMP leads to relaxation of smooth muscle fibers, mainly venules and veins. It has an antianginal and antispasmodic effect, relaxes the smooth muscle cells of the walls of blood vessels, bronchi, digestive tract, biliary tract and ureters. When administered intravenously, it causes a decrease in preload on the heart due to the expansion of peripheral veins. Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regression of symptoms in pulmonary edema, reduces afterload, myocardial oxygen demand (by reducing preload, afterload and ventricular wall tension due to a decrease in heart volume). Promotes the redistribution of coronary blood flow in areas with reduced blood circulation. It has a central inhibitory effect on sympathetic vascular tone, inhibiting the vascular component of the formation of pain syndrome. Causes expansion of meningeal vessels, which explains the appearance of a specific "nitrate" headache. With prolonged or frequent use of long-acting nitrates, tolerance may develop. After a break in treatment, sensitivity to nitrates is restored. In order to prevent the development of tolerance, it is recommended to observe an interval in taking nitrates daily (8-12 hours), preferably at night. In most patients, this therapy is more effective than continuous treatment. When using sublingual forms, an angina attack stops after 1.5 minutes, the hemodynamic and antianginal effect persists for up to 30 minutes. Retard tablets can prevent the development of angina attacks.
Nitroglycerin is rapidly and completely absorbed from the surface of the mucous membranes and through the skin. When taken orally, the bioavailability is no more than 10% compared with sublingual nitroglycerin (the effect of the primary passage through the liver). With sublingual, buccal and / in the introduction, first-pass metabolism is excluded, and the active substance enters directly into the systemic circulation. When taken sublingually at a dose of 0.5 mg, bioavailability is almost 100%, the maximum plasma concentration is observed after 5 minutes. Up to 60% of nitroglycerin binds to plasma proteins. It is rapidly metabolized with the participation of nitrate reductase, with the formation of di- and mononitrates (only isosorbide-5-mononitrate is active), the final metabolite is glycerol. It is excreted in the urine as metabolites. The total clearance is 25-30 l / min, the half-life is 4-5 minutes. With the on / in the introduction, the half-life is 1-3 minutes, the total clearance is 30-78 l / min. The active substance is rapidly metabolized in the liver by glutathione reductase, which acts on organic nitrates. In addition, nitroglycerin is metabolized in erythrocytes using enzymatic reactions that occur with the participation of sulfhydryl radicals, as well as when interacting with reduced hemoglobin.
Indications for the use of the drug Nitroglycerin
IHD - angina pectoris, including in the postinfarction period; for intravenous administration - an acute period of myocardial infarction (including complicated by acute left ventricular failure), unstable and post-infarction angina pectoris, pulmonary edema, controlled arterial hypotension during surgical interventions to reduce bleeding in the surgical field, occlusion of the central retinal artery.
The use of the drug Nitroglycerin
Inside, sublingually, in / in. Elimination of angina pectoris. Sublingually (a tablet or capsule with a solution is kept under the tongue until completely resorbed, without swallowing), immediately after the onset of pain - 0.5-1 mg per dose. If necessary, to achieve a faster effect, the capsule should be cracked immediately, the capsule can be repeated after 30-40 minutes. Usually, the antianginal effect appears after 0.5-2 minutes, in some cases - within 4-5 minutes. In the absence of antianginal action during the first 5 minutes, another 0.5 mg of nitroglycerin should be prescribed. In the absence of a therapeutic effect after a 2-3-fold dose, the likelihood of developing a myocardial infarction should be taken into account.
When using 1% nitroglycerin solution to stop an attack, 2-3 drops of the solution are applied to a small piece of sugar and kept in the mouth without swallowing until completely absorbed. The duration of action after sublingual administration is about 45 minutes.
With frequent attacks of angina pectoris, it is advisable to prescribe prolonged forms of nitrates. If an angina attack develops during treatment with prolonged forms of nitrates, sublingual nitroglycerin should be taken to stop an acute attack. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, with its development in some patients, the dose has to be gradually increased, bringing it up to 2-3 tablets.
Long-acting nitroglycerin, intended for the prevention of angina pectoris, is taken orally with water before meals. In mild cases - 0.0029-0.0058 g 2-3 times a day. In more severe cases - 0.0052-0.01 g 2-3 times a day. The maximum daily dose is 0.0348 g. Due to the fact that the bioavailability of nitroglycerin from retard tablets is low, it is recommended, with good tolerance, to take 1-3 tablets at the same time regularly 3-4 times a day or periodically - 30-40 minutes before expected physical activity. With insufficient therapeutic effect, the dose can be gradually increased (but not more than 2 tablets per 1 dose), and after the onset of the therapeutic effect, reduced.
Aerosol for sublingual use: to stop an attack of angina pectoris - 0.4-0.8 mg by pressing the metering valve, preferably in a sitting position, while holding the breath at intervals of 30 seconds; then close your mouth for a few seconds. If necessary, re-introduction, but not more than 1.2 mg for 15 minutes. To prevent an attack - 0.4 mg 5-10 minutes before exercise. In acute left ventricular failure, developing pulmonary edema - 1.6 mg or more in a short period of time.
Treatment with nitroglycerin for intravenous administration should be carried out by individually setting the rate of administration of the solution. Enter through an automatic dispenser or through a conventional system for intravenous infusion. When using a tube system made of PVC, the active substance is absorbed and the losses on the tube walls are up to 60% (it is advisable to use polyethylene and glass tubes). The solution is rapidly destroyed in the light, so the vials and transfusion system must be shielded with opaque material. Usually, an infusion solution is used with a concentration of 100 μg / ml: a concentrated solution is diluted with 0.9% sodium chloride solution or 5% dextrose solution and injected intravenously at an initial rate of 5 μg / min. The rate of administration can be increased every 3-5 minutes by 5 mcg / min (depending on the effect, heart rate, central venous pressure and systolic blood pressure, which can be reduced by 10-25% of the original, but should not be lower than 90 mm Hg. Art.). If a therapeutic effect is not achieved at an injection rate of 20 μg / min, the injection rate can be increased by 10-20 μg / min. When a response occurs (in particular, a decrease in blood pressure), a further increase in the infusion rate is not carried out or carried out at longer intervals. To achieve a good effect, the rate of administration of 0.01% nitroglycerin solution usually does not exceed 100 mcg / min (1 ml / min). In the absence of an effect due to the use of nitroglycerin at lower doses and at an acceptable level of blood pressure, the rate of administration of 0.01% solution can reach 300-400 mcg / min (3-4 ml / min). Further increase in the rate of infusion is impractical. The duration of use is determined by clinical indications and can be 2-3 days.
Contraindications to the use of the drug Nitroglycerin
Hypersensitivity to nitroglycerin; for intravenous administration (relative contraindications) - traumatic brain injury, increased intracranial pressure, cardiac tamponade, constrictive pericarditis, hypovolemia (must be corrected before using nitroglycerin).
Side effects of Nitroglycerin
dizziness, "nitrate" headache, tachycardia, skin flushing, feeling hot, lowering blood pressure; rarely (mainly with an overdose) - orthostatic collapse, cyanosis; feeling of dry mouth, nausea, vomiting, abdominal pain; rarely (mainly with an overdose) - anxiety, psychotic reactions, lethargy, disorientation; rarely - allergic reactions (skin itching, rash); local reactions with transdermal application: hyperemia and itching of the skin, burning, allergic contact dermatitis; blurred vision, general weakness, hypothermia, methemoglobinemia.
Special instructions for the use of the drug Nitroglycerin
Use with caution, given the possible risk, with recent traumatic brain injury, acute myocardial infarction (risk of lowering blood pressure and tachycardia, which can increase ischemia), glaucoma (risk of increased intraocular pressure), severe anemia, hyperthyroidism, arterial hypotension with low systolic AD (may aggravate the condition by causing paradoxical bradycardia and angina attacks), hypertrophic cardiomyopathy (possible increase in angina attacks), severe renal failure, liver failure (risk of methemoglobinemia), during pregnancy and lactation, in children.
In acute myocardial infarction or acute heart failure, it should be used only under the condition of careful clinical observation and monitoring of hemodynamic parameters. To prevent an increase in angina attacks, abrupt withdrawal should be avoided.
During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Against the background of taking nitroglycerin, a significant decrease in blood pressure and the appearance of dizziness are possible with a sharp transition to a vertical position from a lying or sitting position; when drinking ethanol, exercising and in hot weather. It is also possible to increase angina pectoris with a sharp decrease in blood pressure, ischemia up to myocardial infarction and sudden death. With frequent use without intervals, tolerance to nitrates may develop, requiring an increase in dose. The severity of headache while taking nitroglycerin can be reduced by reducing the dose of nitroglycerin and / or simultaneously taking validol.
Drug interactions Nitroglycerin
Simultaneous use with vasodilators, antihypertensives, ACE inhibitors, β-adrenergic blockers, calcium antagonists, procainamide, tricyclic antidepressants, MAO inhibitors, phosphodiesterase inhibitors, and ethanol enhances the hypotensive effect of nitroglycerin. Appointment with dihydroergotamine can lead to an increase in its content in the blood and to an increase in blood pressure (increased bioavailability of dihydroergotamine). Care should be taken when combining nitroglycerin with heparin.
Overdose of the drug Nitroglycerin, symptoms and treatment
Manifested by a decrease in blood pressure (below 90 mm Hg), orthostatic reactions, reflex tachycardia, headache, dizziness, drowsiness, feeling hot, nausea, vomiting, with a significant overdose (more than 20 mg / kg) - collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea. With the development of overdose symptoms, further administration is stopped, the patch is removed. Lower the head end of the bed and raise the patient's legs. As a rule, blood pressure normalizes within 15-20 minutes after stopping the administration of nitroglycerin, then you can continue the introduction after re-establishing the infusion rate. To correct blood pressure, it is possible to use phenylephrine, epinephrine and other vasoconstrictors. With methemoglobinemia, depending on the severity, ascorbic acid is prescribed 1 g orally or in the form of a sodium salt IV; IV methylene blue 0.1-0.15 ml/kg 1% solution (up to 50 ml), oxygen therapy, hemodialysis, exchange transfusion.
List of pharmacies where you can buy Nitroglycerin:
- Saint Petersburg
Nitroglycerin: instructions for use and reviews
Latin name: Nitroglycerine
ATX code: C01DA02
Active substance: nitroglycerin (nitroglycerin)
Producer: NPF "Mikrokhim", LLC "Experimental plant GNTsLS" (Ukraine), LLC "Ozon", LLC "Lumi", LLC "Pharmamed", Medical and technological holding "MTX", "Samaramedprom", CJSC "Binnopharm", JSC "Biomed" them. I. I. Mechnikova, Medisorb (Russia)
Description and photo update: 16.08.2019
Nitroglycerin is a vasodilator used to treat angina attacks.
Release form and composition
Nitroglycerin is produced in the following dosage forms:
- Sublingual tablets: almost white or white, flat-cylindrical, with a rough surface (40 tablets in a polymer tube, tightly sealed with a polymer stopper, 1 tube in a cardboard box);
- Sublingual dosed spray: colorless, transparent (in bottles or cylinders of 200 doses (10 ml), 1 bottle or cylinder in a cardboard box, complete with a dosing mechanical pump);
- Concentrate for solution for infusion: colorless, transparent (in ampoules of 2, 5 or 10 ml, 5 ampoules in blister packs, 1, 2 or 10 packs in a carton box).
The composition of 1 sublingual tablet includes:
- Active substance: nitroglycerin - 0.5 mg (in terms of 100% substance);
- Auxiliary components: sugar (sucrose) - 7.9 mg, glucose (dextrose) - 9.3 mg, potato starch - 9.3 mg.
The composition of 1 dose of sublingual spray includes:
- Active substance: nitroglycerin - 0.4 mg;
- Auxiliary components: 95% ethanol (in the form of a 1% solution).
The composition of 1 ml of concentrate for the preparation of an infusion solution includes:
- Active substance: nitroglycerin - 1 mg;
- Auxiliary components: dextrose, sodium chloride, potassium dihydrogen phosphate, water for injection.
Pharmacological properties
Pharmacodynamics
Nitroglycerin is a peripheral vasodilator with a predominantly venous effect. Its action is mainly due to a decrease in myocardial oxygen demand due to a decrease in preload (decrease in blood flow to the right atrium and expansion of peripheral venous vessels) and afterload (decrease in total peripheral vascular resistance).
Nitroglycerin is able to release nitric oxide from its molecule, which is a natural endothelial relaxing factor. The compound increases the concentration of cyclic guanosine monophosphatase inside the cell, which prevents the penetration of calcium ions into smooth muscle cells and provokes their relaxation. Relaxation of the smooth muscles of the vascular wall leads to vasodilation, which reduces the load on the heart and myocardial oxygen demand. The expansion of the coronary vessels improves coronary blood flow and its redistribution in areas characterized by reduced blood circulation, which stimulates the transport of oxygen to the myocardium.
A decrease in venous return causes a decrease in pressure in the pulmonary circulation and filling pressure, an improvement in blood supply to the subendocardial layers, and a regression of symptoms characteristic of pulmonary edema. Nitroglycerin is characterized by a central inhibitory effect on sympathetic vascular tone and suppression of the vascular component responsible for the formation of pain. It also provokes the expansion of meningeal vessels, which causes a headache after taking it, and relaxes the cells of the smooth muscles of the bronchi, small and large intestines, esophagus, their sphincters, bile ducts, gallbladder, urinary tract.
The use of sublingual forms usually allows stopping an angina attack 1.5 minutes after oral administration, and the antianginal effect persists for 30-60 minutes.
Pharmacokinetics
Nitroglycerin is quickly and almost completely absorbed from the surface of the mucous membranes of the oral cavity. When taken sublingually, it immediately penetrates into the systemic circulation. The bioavailability of the drug is 100%, since the primary hepatic degradation of the substance is excluded. The maximum concentration of nitroglycerin in the blood plasma is determined after 4-5 minutes. The metabolism of the substance is carried out quite quickly with the participation of nitrate reductase. In this case, mono- and dinitrates are formed. Only isosorbide-5-mononitrate demonstrates pharmacological activity. The final metabolite is glycerol.
The drug has a very large volume of distribution (1.2–3.3 l/kg). The degree of binding to plasma proteins is 60%. Nitroglycerin is excreted in the urine as metabolites (less than 1% of the dose is excreted unchanged), the total clearance is 25-30 l / min (with infusion - up to 78 l / min). After oral sublingual administration of the drug, the half-life from blood plasma varies from 2.5 to 4.4 minutes (with infusion administration - from 1 to 3 minutes). Circulating nitroglycerin binds strongly to erythrocytes and accumulates in the walls of blood vessels.
Indications for use
Indications for the use of Nitroglycerin are:
- Angina pectoris (stopping and short-term prevention of angina attacks before emotional stress or physical exertion);
- Acute myocardial infarction, including complicated by acute left ventricular failure (infusion solution);
- Pulmonary edema (infusion solution);
- Unstable angina (infusion solution).
Contraindications
Absolute:
- Collapse;
- Age up to 18 years (the efficacy and safety of using Nitroglycerin for this age group of patients have not been established);
- Hypersensitivity to the components of the drug.
Depending on the dosage form, additional absolute contraindications to the use of Nitroglycerin are the following diseases / conditions:
- Glucose-galactose malabsorption (sublingual tablets);
- Shock (sublingual spray and tablets);
- Cardiogenic shock, except for cases of measures to maintain end-diastolic pressure (sublingual spray);
- Severe arterial hypotension with systolic blood pressure below 90 mm Hg. Art. (spray sublingual);
- Constrictive pericarditis (sublingual spray);
- Angina associated with hypertrophic obstructive cardiomyopathy (sublingual spray);
- Acute myocardial infarction and chronic heart failure with low filling pressure of the left ventricle (sublingual spray);
- Pericardial tamponade (sublingual spray);
- Any conditions associated with increased intracranial pressure (sublingual spray);
- Severe mitral and/or aortic valve stenosis, primary pulmonary hypertension (sublingual spray);
- Simultaneous use with phosphodiesterase-5 inhibitors, including vardenafil, sildenafil, tadalafil (sublingual tablets and spray).
According to the instructions, Nitroglycerin should be used with caution after assessing the benefit / risk ratio:
- hemorrhagic stroke;
- severe anemia;
- thyrotoxicosis;
- severe renal failure;
- Angle-closure glaucoma;
- Recent head trauma;
- intracranial hypertension;
- Cardiac tamponade (sublingual tablets and infusion solution);
- Liver failure (sublingual tablets and infusion solution), severe liver failure (sublingual spray);
- Arterial hypotension with low systolic pressure - less than 90 mm Hg. Art. (sublingual tablets and infusion solution);
- Orthostatic hypotension and a tendency to develop orthostatic hypotension (sublingual spray);
- Alcohol abuse (sublingual spray);
- Epilepsy (sublingual spray);
- Migraine (sublingual spray);
- Constrictive pericarditis (sublingual tablets and infusion solution);
- Isolated mitral stenosis (sublingual tablets and infusion solution);
- Hypertrophic cardiomyopathy (sublingual tablets and infusion solution);
- Toxic pulmonary edema (infusion solution);
- Idiopathic hypertrophic subaortic stenosis (sublingual tablets), aortic stenosis (infusion solution);
- Acute myocardial infarction, chronic heart failure with low filling pressure of the left ventricle (sublingual tablets and infusion solution);
- Uncontrolled hypovolemia with normal or low pressure in the pulmonary artery in patients with heart failure (infusion solution);
- Shock, including cardiogenic, except for cases with a sufficiently high filling pressure of the left ventricle, incl. provided with drugs with a positive inotropic effect or intra-aortic counterpulsation (infusion solution);
- Hemorrhage in the brain (infusion solution);
- Severe cerebral atherosclerosis (infusion solution);
- Pregnancy and lactation (for all forms of the drug);
- Elderly age (infusion solution).
Instructions for use Nitroglycerin: method and dosage
Sublingual tablets
To prevent complications, Nitroglycerin is recommended to be taken as prescribed by a doctor.
Nitroglycerin tablets are taken (sublingually) under the tongue, holding in the mouth until completely resorbed, without swallowing.
Nitroglycerin should be taken immediately when the first signs of an angina attack appear, or before the expected physical exertion or emotional stress. Single dose - 1 tablet. With stable angina, the effect may also occur from a lower dose, in which case the remainder of the tablet, which has not had time to dissolve, is recommended to spit out. In most cases (in 75% of patients), improvement is noted during the first 3 minutes of using Nitroglycerin.
If within 5 minutes an attack of angina pectoris is not stopped, you should take 1 more tablet.
In cases where there is no therapeutic effect after taking 2 tablets of Nitroglycerin, you should immediately consult a doctor.
Spray sublingual
Enter on or under the tongue, preferably in a sitting position, while holding your breath. After spraying, the spray is not swallowed immediately, but is held with the mouth closed for a few seconds.
To avoid complications, nitroglycerin should be used as prescribed by a doctor.
When the first signs of an angina attack appear, 1-2 doses of a spray are administered (depending on severity). If necessary, it is possible to introduce another 1 dose, but not more than 3 doses (1.2 mg) within 15 minutes.
If after using 3 doses for 15 minutes the condition does not improve, you should consult your doctor.
The maximum single dose is 3 spray doses.
If the indication for the use of Nitroglycerin is the prevention of angina attacks, the drug is used in 1 dose 5-10 minutes before the expected load or stress.
Do not shake the spray bottle before use. When spraying, the bottle must be held vertically.
Infusion solution
The rate of intravenous administration of Nitroglycerin is selected individually, taking into account blood pressure, heart rate, central venous pressure, ECG and other indicators. The solution should be administered through an infusomat or an automatic dispenser, allowing it to be accurately dosed and the rhythm of administration to be controlled.
The administration of Nitroglycerin using a conventional transfusion system ensures dosing accuracy by counting the number of drops of the transfused liquid. Before administration, a solution of Nitroglycerin is preliminarily diluted in 0.9% sodium chloride solution or 5% glucose (dextrose) solution to a concentration of 0.01%. Other solvents should not be used.
It is advisable to use glass and polyethylene tubes, since the active substance is absorbed on the walls of PVC tubes (losses can be 40-80%). Nitroglycerin solution is rapidly destroyed by light, so the transfusion system and vials must be shielded with opaque material. Storage of the solution in the opened ampoule is not allowed.
The initial rate of administration of the solution is 0.5-1 mg per hour, the maximum rate is 8-10 mg per hour.
The recommended concentrations and rate of administration of Nitroglycerin are: 1 mg / h (0.0166 mg / min) - 24 mg per day through an automatic dispenser (solution volume 1 mg / ml) or 240 mg per day through an intravenous system (solution volume 0 .1 mg/ml); the rate of administration is 3-4 drops per minute (1 ml corresponds to 20 drops).
The duration of therapy is determined by clinical indications and can vary from several hours to 2-3 days.
Side effects
- Central nervous system: weakness; rarely - psychotic reactions, anxiety, disorientation, lethargy;
- Digestive system: dryness of the oral mucosa; rarely - vomiting, nausea, abdominal pain;
- Cardiovascular system: headache, dizziness, fever, tachycardia, lowering blood pressure; rarely (especially with overdose) - cyanosis, orthostatic collapse, increased symptoms of angina pectoris (paradoxical reaction to nitrates); sometimes - collapse with loss of consciousness and bradyarrhythmia;
- Local reactions: burning sensation under the tongue, skin flushing;
- Allergic reactions: rarely - itching, skin rash, exfoliative dermatitis;
- Others: rarely - hypothermia, blurred vision, methemoglobinemia.
Overdose
Symptoms of an overdose of Nitroglycerin are: nausea, vomiting, increased drowsiness, severe weakness, asthenia, severe dizziness, headache, convulsive seizures, feeling hot, shortness of breath, reflex tachycardia, lowering blood pressure (below 90 mm Hg. Art.), Accompanied by orthostatic dysregulation . Taking the drug in high doses (more than 20 mg / kg) can lead to the development of tachypnea, dyspnea, cyanosis, collapse, methemoglobinemia.
If there are signs of an overdose, you should immediately give the patient a horizontal position, raising his legs, and also seek medical help.
special instructions
The therapeutic doses indicated in the instructions should not be exceeded.
1 tablet of sublingual Nitroglycerin contains 2.65×10 -3 XE (bread units).
During therapy, a significant decrease in blood pressure and the development of dizziness are possible with a sharp transition to a vertical position from a lying or sitting position, as well as in hot weather, while exercising or drinking alcohol.
If blurred vision or dryness of the oral mucosa persists or is significantly pronounced, treatment should be interrupted.
According to the instructions, Nitroglycerin, like other organic nitrates, can be addictive (in this case, an increase in dosage will be required).
The severity of headache during therapy can be reduced by reducing the dose of the drug and / or concomitantly taking Validol.
During the use of Nitroglycerin, the use of alcoholic beverages is strictly prohibited.
The composition of the sublingual spray includes alcohol, which is important for lactating and pregnant women, patients with functional disorders of the liver, epilepsy, traumatic brain injury and other diseases of the central nervous system, as well as for alcohol abuse.
The composition of the infusion solution includes glucose (dextrose), which must be taken into account in patients with diabetes mellitus.
In acute heart failure or acute myocardial infarction, nitroglycerin should be used only under the condition of careful clinical monitoring of the condition of patients.
In order to prevent an increase in angina attacks, it is recommended to avoid abrupt discontinuation of the drug.
To prevent an undesirable decrease in blood pressure, the rate of administration of the infusion solution of Nitroglycerin must be selected individually. A decrease in blood pressure can be observed not only when selecting the rate of administration of the solution, but also later, against the background of initially stabilized blood pressure (control should be carried out at least 3-4 times per hour throughout the entire infusion time).
Patients previously treated with organic nitrates (isosorbide-5-mononitrate, isosorbide dinitrate) may require a higher dose to obtain the desired hemodynamic effect.
During the use of Nitroglycerin, care must be taken when driving vehicles and performing potentially hazardous types of work that require increased concentration and quick psychomotor reactions.
drug interaction
With the simultaneous use of Nitroglycerin with certain drugs, the following effects may occur:
- Vasodilators, antihypertensives, angiotensin-converting enzyme inhibitors, phosphodiesterase-5 inhibitors, slow calcium channel blockers, tricyclic antidepressants, ethanol, diuretics, beta-blockers, monoamine oxidase inhibitors, procainamide: increased hypotensive effect of nitroglycerin;
- Sublingual tablets: 2 years at temperatures up to 25 ° C;
- Spray sublingual: 2 years at temperatures up to 15 ° C;
- Concentrate for solution for infusion: 3 years at 5-25 °C.
Nitroglycerin is a drug of synthetic origin, which is used in cardiology. Available in the form of an alcohol solution, sublingual tablets and capsules.
Pharmacological action of Nitroglycerin
According to the instructions, the active ingredient of the drug is nitroglycerin.
The drug is a peripheral vasodilator that affects the venous vessels. Nitroglycerin forms nitric oxide, which leads to the activation of guanylate cyclase and an increase in the content of cyclic guanosine monophosphate (cGMP) in smooth muscle cells. In accordance with the instructions, Nitroglycerin promotes non-specific relaxation of vascular smooth muscles, mostly venous, which is accompanied by the deposition of blood in the venous system.
When using Nitroglycerin, there is a decrease in the preload of the heart and the end diastolic filling of the left ventricle. General systemic arterial dilatation, mainly of large vessels, provides a decrease in afterload.
This medication reduces myocardial oxygen demand, normalizes systemic blood flow.
When using Nitroglycerin, relaxation of the smooth muscles of the biliary tract, bronchi, intestines, stomach, esophagus, and genitourinary system is noted.
Nitroglycerin is rapidly and completely absorbed into the systemic circulation. The period of complete elimination of the drug is 8 hours. It is excreted from the body in the form of metabolites through the kidneys.
Indications for the use of Nitroglycerin
Indications for Nitroglycerin are angina attacks, left ventricular failure, myocardial infarction.
In individual cases, the drug is used to treat biliary dyskinesia. In some cases, it is prescribed for the treatment of the central retinal artery of the eyes.
Method of application and dosage
Nitroglycerin in the form of an alcohol solution is applied directly to the tongue in 1-2 drops or moistened with a small piece of sugar and kept under the tongue until it is completely absorbed. The maximum single dose of Nitroglycerin under the tongue is 4 drops, the daily dose is 16 drops.
According to the indications, Nitroglycerin tablets are taken sublingually, immediately after the onset of pain, without swallowing. A single dose of Nitroglycerin tablets for adults is 1-2 pcs. The maximum daily dose is 6 tablets.
The rules for taking capsules correspond to the rules for taking tablets. To accelerate the therapeutic effect, the capsule can be crushed with your teeth.
The duration and frequency of use of Nitroglycerin depend on the intensity and frequency of angina pectoris.
If there is no effect within 5 minutes after taking the medicine, you must take another 1 tablet. If there is no effect after taking 2-3 tablets, you should immediately call an ambulance.
Side effects
When using Nitroglycerin, headaches, tachycardia, tinnitus, fever, lowering blood pressure, dry mouth, abdominal pain, nausea, vomiting may occur.
Contraindications
According to the instructions, Nitroglycerin is not prescribed to people who have:
- arterial hypotension;
- Circulatory disorders of the brain;
- Hyperthyroidism;
- Angle-closure glaucoma, accompanied by increased intraocular pressure;
- Idiopathic hypertrophic subaortic stenosis;
- head trauma;
- hemorrhagic stroke;
- severe anemia;
- Subarachnoid hemorrhage;
- Collapse;
- Heart failure;
- uncontrolled hypovolemia;
- Constrictive pericarditis;
- Isolated mitral stenosis;
- cardiac tamponade;
- Cranial hypertension.
Contraindications to Nitroglycerin are also under 18 years of age, pregnancy, lactation.
Take the medicine with caution in liver failure and severe renal failure.
Overdose
With an overdose of Nitroglycerin, a decrease in blood pressure, reflex tachycardia, and asthenia are possible.
Symptoms of an overdose of Nitroglycerin are also dizziness, cyanosis, dyspnea, methemoglobinemia, tachypnea.
Additional Information
Uncontrolled intake of Nitroglycerin can cause the development of tolerance to the drug.
The drug affects the speed of psychomotor reactions, so during therapy it is recommended to refrain from driving heavy machinery and vehicles.
According to the instructions Nitroglycerin should be stored in a cool place out of the reach of children.
Shelf life - 2 years.
From pharmacies, Nitroglycerin is released over the counter.
Each tablet contains: nitroglycerin (in the form of nitroglycerin with glucose) - 0.5 mg;
Excipients: potato starch, microcrystalline cellulose, anhydrous colloidal silicon dioxide, calcium stearate, lactose monohydrate.
Pharmacotherapeutic group
Peripheral vasodilators used in the treatment of heart disease. organic nitrates.
Indications for use
Relief and short-term prevention of angina attacks.
Dosage and administration
The dose and treatment regimen is set by the attending physician individually, depending on the patient's sensitivity to nitroglycerin preparations, indications, and the specific clinical situation. With caution, the drug should be used for severe violations of the liver and / or kidneys.
The usual dose of the drug for angina pectoris is 1 tablet under the tongue, in many patients with stable angina, the effect occurs from a smaller dose (1/2-1/3 tablets), therefore, if the pain passes quickly, it is recommended to spit out the rest of the tablet that has not had time to resolve . Usually, the antianginal effect appears after 0.5-2 minutes; 75% of patients report improvement within the first 3 minutes; and another 15% - within 4-5 minutes. In the absence of a therapeutic effect during the first 5 minutes, it is necessary to take another tablet of the drug. In the absence of a therapeutic effect after 2-3 times of administration, it is necessary to call a doctor (the likelihood of developing a myocardial infarction). The duration of action of nitroglycerin is about 45 minutes.
Tolerance to sublingual forms of nitroglycerin rarely develops, however, when it occurs in some patients, the dose of the drug has to be gradually increased, bringing it up to 2-3 tablets.
Side effect
From the side of the central nervous system: blurred vision, headache (especially at the beginning of the course of treatment, decreases with prolonged therapy), dizziness and a feeling of weakness, restlessness, fainting, drowsiness, cerebral ischemia.
From the sidecardiovascularsystems: arterial hypotension, reddening of the skin of the face, tachycardia, bradycardia, vascular collapse. Sometimes, with a sudden decrease in blood pressure, there may be an increase in angina symptoms (paradoxical "nitrate reactions").
From the digestive tract: a slight burning sensation in the oral cavity, rarely - nausea, vomiting, heartburn.
WITHon the part of the hematopoietic system: rarely - methemoglobinemia, cyanosis.
Other: allergic reactions are possible; rarely - exfoliative dermatitis, increased intraocular pressure; with prolonged use of the drug in high doses - drug withdrawal syndrome; development of tolerance.
Contraindications
Hypersensitivity to the active substance, other nitrates, or any of the excipients; arterial hypotension (systolic pressure less than 90 mm Hg); vascular collapse; angle-closure glaucoma; shock; acute myocardial infarction with low filling pressure of the left ventricle; toxic pulmonary edema; hemorrhagic stroke; conditions accompanied by a decrease in the filling pressure of the left ventricle (isolated mitral stenosis, constrictive pericarditis); hypertrophic cardiomyopathy; simultaneous reception with phosphodiesterase inhibitors (for example, sildenafil, vardenafil, tadalafil); anemia, increased intracranial pressure (including after traumatic brain injury), bradycardia, cardiac tamponade, aortic stenosis.
Pregnancy, breastfeeding, childhood.
Overdose
Symptoms: severe arterial hypotension, tachycardia, collapse, cyanosis, methemoglobinemia.
Treatment: in case of collapse, the patient should take a horizontal position with legs raised up. With methemoglobinemia, intravenous administration of methylene blue is indicated (an average of 0.1-0.15 ml of a 1% solution per 1 kg of body weight). In severe cases, plasma substitutes, sympathomimetics, oxygen are prescribed.
Precautions and application features
Before using the drug for the first time, you should consult your doctor!
While taking the drug, a significant decrease in blood pressure is possible, the appearance of dizziness with a sharp transition to a vertical position from a "lying" or "sitting" position, while drinking alcohol, doing physical exercises and hot weather.
With frequent use of nitroglycerin, addiction may develop, requiring an increase in dosage.
The severity of headache while taking the drug can be reduced by reducing its dose and / or concomitantly taking Validol.
During the treatment period, alcohol is not allowed.
Use with caution in cerebrovascular pathology, severe liver or kidney disease, hypothyroidism, hypoxemia, recent myocardial infarction, primary pulmonary hypertension, migraine, a tendency to develop orthostatic hypotension, malnutrition, deficiency of methemoglobin reductase, glucose-6-phosphate dehydrogenase.
To prevent hypotension, it is recommended to take nitroglycerin in the supine or sitting position. Taking nitroglycerin in a standing position can not only contribute to fainting, but also to a weakening of the antianginal effect, the development of the “steal” syndrome (increased myocardial ischemia), especially in patients with widespread atherosclerosis of the coronary vessels.
If the symptoms of angina do not go away after taking three doses of the drug, the patient should immediately consult a doctor.
In order to prevent the development of tolerance, it is recommended to maintain an interval between taking nitrates daily (8-12 hours). In the event of the development of tolerance, you should temporarily stop taking the drug (for several days) and replace it with antianginal agents of other pharmacotherapeutic groups.
The storage conditions of the drug should be strictly observed. If the integrity of the package or storage conditions are violated, the effectiveness of the drug may decrease.
Features of use in elderly patients
The use of nitrates in the elderly increases the risk of adverse reactions such as hypotension and syncope. In this category of patients, the drug is recommended to be taken with caution, if possible, in a sitting or lying position.
Use in children
The drug is contraindicated in children due to the lack of data on efficacy and safety.
Use during pregnancy and breastfeeding
The safety of use during pregnancy and lactation has not been proven. During pregnancy and breastfeeding, taking the drug is possible only if the expected benefit to the mother outweighs the possible risk to the fetus or child.
The effect of the drug on the abilitydrive a car andmami
When driving a vehicle or when operating mechanisms that require increased attention, it should be remembered that taking the drug can lead to a decrease in the reaction rate.
Interaction with other drugs
The hypotensive effect of the drug may be excessive in the case of uncontrolled simultaneous administration of antihypertensive drugs, tricyclic antidepressants, alcohol, diuretics, beta-blockers, monoamine oxidase inhibitors (MAOIs). With caution, nitroglycerin with procainamide should be taken, since it is possible to increase the hypotensive effect and the development of collapse.
The combined use of nitroglycerin with phosphodiesterase type 5 inhibitors, which are used to treat erectile dysfunction or pulmonary hypertension, is strictly contraindicated due to the risk of severe hypotension. The use of nitroglycerin is possible not earlier than 24 hours after taking drugs containing sildenafil and vardenafil, not earlier than 48 hours after taking drugs containing tadalafil.
The drug for the second century quickly and effectively makes life easier for patients with heart disease. But the study and creation of various pharmacological forms continues. For a long time, scientists and physicians have discovered many beneficial properties and found out what nitroglycerin helps from, affecting the vascular system.
How Nitroglycerin Works
The mechanism of action of nitroglycerin is no longer a mystery since the end of the twentieth century. The scientists who discovered it were awarded the Nobel Prize. The drug has a relaxing effect on the smooth muscle layer of the vascular wall, due to which the lumen of the vessel becomes wider.
The reason for this is the nitrogen released from nitroglycerin. It reacts with free oxygen and forms nitric oxide, which activates a special substance - guanylate cyclase, which is responsible in the body for relaxing smooth muscles.
Nitroglycerin - what helps the drug
Smooth muscle fibers are located not only in the vessels. They are also contained in the walls of the intestines, bronchi, ureters, bile and pancreatic ducts. Using nitroglycerin, you can relieve the spasm of these anatomical formations.
- The cardiovascular system. The main and most commonly used "target" of nitroglycerin.
- By dilating the coronary arteries, the drug increases the flow of oxygen-rich blood to the heart muscle. As a result, angina pectoris pains are stopped.
- The expansion of the venous vessels, especially with intravenous administration of the drug, reduces the venous return to the heart, "unloading" its right sections. The result is a decrease in congestion, prevention of pulmonary edema. In addition, with a decrease in the load of blood volume on the heart, its oxygen demand decreases accordingly, which also has an analgesic effect in angina pectoris.
- The drug is used in surgical interventions for controlled hypotension.
- The rehabilitation period after a heart attack is also not complete without this drug.
- Hypertension, accompanied by crises with pain in the heart and shortness of breath, is also an indication for the use of nitroglycerin.
- Bile and pancreatic ducts. Nitroglycerin relieves spasm of the walls of the ducts in biliary colic, gallbladder dyskinesia or acute pancreatitis.
- Gastrointestinal tract. The drug relieves pain with colic and dyskinesia.
- Urinary ducts. Relaxing the walls of the ureter, nitroglycerin relieves pain in renal colic.
Side effect
The wonderful property of the drug to relax smooth muscles can cause unpleasant consequences. The reason is the rapid expansion of blood vessels, a drop in blood pressure
- Headache, possible fainting.
- Cardiopalmus.
- Nausea, dyspepsia, feeling of dry mouth.
Overdose can cause nervous excitement, disorientation or lethargy. In severe intoxication, collapse, respiratory failure is observed, which requires immediate medical attention.
In case of fainting caused by taking nitroglycerin, the intake of the drug into the body should be stopped, the patient should be placed with raised legs and a slightly lowered head. Normalization of blood pressure usually occurs within 20 minutes.
Admission rules
For more than a hundred years, the pharmaceutical industry has produced a wide variety of forms of the drug. The most popular and effective are sublingual and buccal. Intravenous and dermal, as well as prolognated forms are also produced.
How to take nitroglycerin tablets under the tongue
Sublingual tablets of 0.5 mg. They should be taken to relieve angina pain. Rapid drug.
Acceptance rules. With an attack of pain like angina pectoris, you should stop the load during which it arose, sit down and put 1 tablet of nitroglycerin under the tongue. The patient will feel the effect in 1-3 minutes. Duration - up to 10 minutes. If it doesn’t help, you can take the second pill 5 minutes after the first one, and the third one 5 minutes later. The lack of pain relief within 15 minutes when using 3 tablets is a reason to seek medical help, as myocardial infarction may develop.
The conditions for storing tablets should be observed:
- in an open package (glass tube) nitroglycerin remains active for no more than two months;
- plastic packaging for nitroglycerin is not suitable; after three days of storage, it loses 80% of its effectiveness;
- the glass tube must be closed with a rubber stopper, without cotton wool, which absorbs nitroglycerin;
- An unopened package loses 32% of activity within a week.
Of the side effects most often occur headaches, a feeling of fullness, tinnitus, redness of the face. Perhaps dizziness, hypotension. This is due to the expansion of the venous vessels in the head and the difficulty of venous outflow.
To reduce side effects, you can take half a tablet of nitroglycerin, adding validol or menthol, which help improve venous outflow from the cranial cavity.
Other forms of nitroglycerin that have a quick effect
Not only tablets can be taken under the tongue. They also produce an alcohol solution of nitroglycerin, an oil solution in gelatin capsules, a spray and an aerosol, plates glued to the gums.
- Alcohol solution. 4 drops of the solution are dripped onto a sugar cube (2-3 are enough for some patients), put under the tongue. As with sublingual tablets, three doses within 15 minutes are allowed in the absence of the desired effect.
- Gelatin capsules with oil solution. The application involves placing a capsule previously crushed with teeth under the tongue.
- inhalation forms. Spray and aerosol with 1 spray emit 0.4 and 0.2 mg of nitroglycerin. One sublingual tablet corresponds to 2-4 valve presses. The effect of spraying comes faster and lasts up to 20 minutes. The drug has proven itself in pulmonary edema and cardiac asthma. The drug is sprayed into the oral cavity, holding the breath. When inhaled aerosol may develop bronchospasm.
- Plates on the gum. Contain 4, 2 or 1 mg of nitroglycerin. Polymer plates are glued to the gums of the upper jaw in the area of the canines and small molars. The effect occurs within 1 or 2 minutes, and lasts the entire period of resorption of the plate. It is individual and depending on this, the dose of the drug is selected. If resorption occurs within an hour and a half, a plate containing the drug is prescribed 1 mg, 2-3 hours - twice as much, 4-6 hours - 4 mg. If the load that causes pain has stopped earlier, it makes sense to remove the plate. If you want to increase the flow of nitroglycerin, you need to lick the plate two or three times.
Contraindications to taking nitroglycerin
Taking nitroglycerin may worsen the condition of patients with
- increased intracranial pressure;
- hemorrhage in the brain;
- allergies to nitrates;
- hypotension below 100/60 mm Hg. Art.;
- hypovolemia CVP less than 4-5 mm Hg. Art.;
- angle-closure glaucoma with high intraocular pressure;
- pregnancy, lactation;
- hypertrophic cardiomyopathy;
- severe renal and hepatic insufficiency;
- thyrotoxicosis.
The use of nitroglycerin, as well as other drugs, should be agreed with the attending physician after a thorough examination and an accurate diagnosis.
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