Nitroglycerine
Nitroglycerin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Drug interactions
- 10. Analogs
- 11. Terms and conditions of storage
- 12. Terms of dispensing from pharmacies
- 13. Reviews
- 14. Price in pharmacies
Latin name: Nitroglycerin
ATX code: C01DA02
Active ingredient: nitroglycerin (nitroglycerin)
Producer: NPF Mikrokhim, LLC Experimental Plant GNTsLS (Ukraine), LLC Ozon, LLC Lumi, LLC Farmamed, Medico-technological holding MTH, Samaramedprom, CJSC Binnopharm, JSC "Biomed" them. I. I. Mechnikova "," Medisorb "(Russia)
Description and photo update: 2019-16-08
Prices in pharmacies: from 14 rubles.
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Nitroglycerin is a vasodilator drug used to relieve angina attacks.
Release form and composition
Nitroglycerin is available 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 each in a cardboard box);
- Dosed sublingual spray: colorless, transparent (in bottles or cans of 200 doses (10 ml), 1 bottle or balloon in a cardboard box, complete with a mechanical dosing pump);
- Concentrate for the preparation of a solution for infusion: colorless, transparent (in ampoules of 2, 5 or 10 ml, 5 ampoules in blisters, 1, 2 or 10 packages in a cardboard 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 the sublingual spray includes:
- Active ingredient: nitroglycerin - 0.4 mg;
- Auxiliary components: 95% ethanol (as a 1% solution).
The composition of 1 ml of the concentrate for the preparation of the infusion solution includes:
- Active ingredient: nitroglycerin - 1 mg;
- Auxiliary components: dextrose, sodium chloride, potassium dihydrogen phosphate, water for injection.
Pharmacological properties
Pharmacodynamics
Nitroglycerin is a peripheral vasodilator that predominantly acts on the venous vessels. Its effect is mainly due to a decrease in myocardial oxygen demand due to a decrease in preload (a decrease in blood flow to the right atrium and expansion of peripheral venous vessels) and afterload (a 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. Expansion of the coronary vessels helps to improve 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 the blood supply to the subendocardial layers, and a regression of symptoms characteristic of pulmonary edema. Nitroglycerin is characterized by a central inhibitory effect on the sympathetic vascular tone and suppression of the vascular component responsible for the formation of pain. It also provokes the expansion of the 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, gall bladder, urinary tract.
The use of sublingual forms usually allows you to stop an attack of angina pectoris 1.5 minutes after oral administration, and the antianginal effect lasts for 30-60 minutes.
Pharmacokinetics
Nitroglycerin is rapidly and almost completely absorbed from the surface of the mucous membranes of the oral cavity. When taken sublingually, it immediately enters 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 blood plasma is determined after 4-5 minutes. The metabolism of a substance is carried out rather 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 glycerin.
The drug has a very large volume of distribution (1.2 (3.3 l / kg). The degree of binding to blood plasma proteins is 60%. Nitroglycerin is excreted in the urine in the form of metabolites (less than 1% of the dose taken 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 plasma half-life varies from 2.5 to 4.4 minutes (with infusion, from 1 to 3 minutes). Circulating nitroglycerin strongly binds to erythrocytes and accumulates in the walls of blood vessels.
Indications for use
Indications for the use of Nitroglycerin are:
- Angina pectoris (relief 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 effectiveness and safety of the use of Nitroglycerin for this age group of patients have not been established);
- Hypersensitivity to drug components.
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 when taking measures to maintain end diastolic pressure (sublingual spray);
- Severe arterial hypotension with systolic blood pressure below 90 mm Hg. Art. (sublingual spray);
- Constrictive pericarditis (sublingual spray);
- Angina pectoris associated with hypertrophic obstructive cardiomyopathy (sublingual spray);
- Acute myocardial infarction and chronic heart failure with low left ventricular filling pressure (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);
- Concomitant 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 impairment;
- Closed-angle glaucoma;
- Recent head injuries;
- Intracranial hypertension;
- Cardiac tamponade (sublingual tablets and infusion solution);
- Hepatic impairment (sublingual tablets and infusion solution), severe hepatic impairment (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 left ventricular filling pressure (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 shock, except in 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);
- Cerebral hemorrhage (infusion solution);
- Severe cerebral atherosclerosis (infusion solution);
- Pregnancy and lactation (for all forms of the drug);
- Elderly age (infusion solution).
Instructions for the use of Nitroglycerin: method and dosage
Sublingual tablets
To prevent complications, Nitroglycerin is recommended to be taken as directed by a doctor.
Nitroglycerin tablets are taken (sublingually) under the tongue, holding in the mouth until completely absorbed, without swallowing.
Nitroglycerin should be taken immediately when the first signs of an angina attack appear or before the expected physical activity or emotional stress. Single dose - 1 tablet. With stable angina pectoris, the effect can come from a lower dose, in this case the rest of the tablet, which did not have time to dissolve, is recommended to be spit out. In most cases (in 75% of patients), improvement is noted within the first 3 minutes of using Nitroglycerin.
If the angina attack is not stopped within 5 minutes, you should take another 1 tablet.
If there is no therapeutic effect after taking 2 tablets of Nitroglycerin, you should immediately consult a doctor.
Sublingual spray
Injected into or under the tongue, preferably in a sitting position, while holding the breath. After spraying, the spray is not swallowed immediately, but is held by closing the mouth for a few seconds.
To avoid complications, Nitroglycerin should be used as directed by a physician.
When the first signs of an angina attack appear, 1-2 doses of a spray are administered (depending on the 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 taking 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 package before use. Hold the bottle upright when spraying.
Infusion solution
The rate of intravenous injection 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 to control the rhythm of administration.
Administration of Nitroglycerin using a conventional fluid transfer system ensures dosing accuracy by counting the number of drops of fluid being transferred. Before the introduction, the nitroglycerin solution is preliminarily diluted in 0.9% sodium chloride solution or 5% glucose (dextrose) solution to a concentration of 0.01%. Do not use other solvents.
It is advisable to use glass and polyethylene tubes, since the active substance is absorbed on the walls of the 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 an 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 concentration 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, low blood pressure; rarely (especially in case of overdose) - cyanosis, orthostatic collapse, increased symptoms of angina pectoris (paradoxical reaction to nitrates); sometimes - collapse with loss of consciousness and bradyarrhythmia;
- Local reactions: burning under the tongue, flushing of the skin;
- 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, seizures, fever, shortness of breath, reflex tachycardia, lowering blood pressure (below 90 mm Hg), 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 2.65X10 -3 XE (grain units).
During therapy, a significant decrease in blood pressure and the development of dizziness may occur with a sharp transition to an upright position from a lying or sitting position, as well as in hot weather, while exercising or drinking alcohol.
With the preservation or significant severity of blurred vision or dryness of the oral mucosa, 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 concurrent administration of validol.
With frequent attacks of angina pectoris, it is recommended to use prolonged nitroglycerin drugs.
During the use of Nitroglycerin, the use of alcoholic beverages is strictly prohibited.
The sublingual spray contains alcohol, which is important for lactating and pregnant women, patients with functional liver disorders, epilepsy, traumatic brain injury and other diseases of the central nervous system, as well as alcohol abuse.
The infusion solution contains glucose (dextrose), which should 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 observation of the patient's condition.
In order to prevent an increase in the frequency of angina attacks, it is recommended to avoid abrupt withdrawal of the drug.
To prevent an undesirable decrease in blood pressure, the rate of administration of the Nitroglycerin infusion solution must be selected individually. A decrease in blood pressure can be observed not only during the selection of 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 who have undergone previous treatment 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 an increased concentration of attention and fast psychomotor reactions.
Drug interactions
With the simultaneous use of Nitroglycerin with some drugs, the following effects may occur:
- Vasodilators, antihypertensive drugs, angiotensin-converting enzyme inhibitors, phosphodiesterase-5 inhibitors, blockers of "slow" calcium channels, tricyclic antidepressants, ethanol, diuretics, beta-blockers, monoamine oxidase inhibitors, procainamide: an increase in the hypotensive effect
- Dihydroergotamine: an increase in its content in the blood and an increase in blood pressure;
- Heparin: decrease in its effectiveness;
- Acetylsalicylic acid: increasing the level of nitroglycerin in the blood and enhancing its action.
Analogs
Analogues of Nitroglycerin are: Nirmin, Nit-ret, Nitradisk, Nitroxoline, Nitrosorbide, Nitromint, Nitrocor, Nitrong forte, Nitro, Nitro pol infus, Angiolingval, Nitroglycerol, Nitroject, Anginin, Angibidts, Angisedin, Nitrogin, Nitrocardiol, Nitroglin, Nitrostat, Nitrozell, Nitrosprint, Nitrospray, Trinitroglycerol, Trinitrin, Trinitrol, Sustonit, Sustak Forte, Perlinganit.
Terms and conditions of storage
Store in a dark place, out of reach of children.
Shelf life:
- Sublingual tablets: 2 years at temperatures up to 25 ° C;
- Sublingual spray: 2 years at temperatures up to 15 ° C;
- Concentrate for solution for infusion: 3 years at a temperature of 5-25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nitroglycerin
According to reviews, Nitroglycerin turns out to be an indispensable drug for patients with angina pectoris. Especially often it is taken by elderly patients. The drug is fast acting and stops heart attacks almost immediately after administration. However, there are reports that mention adverse reactions, mainly dizziness and intense headache.
Price for Nitroglycerin in pharmacies
The approximate price of Nitroglycerin in the form of sublingual tablets is 48-66 rubles (the package contains 40 pcs.). You can buy metered-dose sublingual spray for 80-127 rubles (designed for 200 doses). The cost of a concentrate for preparing a solution for infusion varies from 540 to 624 rubles (the package contains 10 ampoules).
Nitroglycerin: prices in online pharmacies
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Drug name Price Pharmacy |
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Nitroglycerin 0.5 mg capsules sublingual 40 pcs. RUB 14 Buy |
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Nitroglycerin 0.5 mg tablets sublingual 40 pcs. 42 RUB Buy |
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Nitroglycerin 0.5 mg sublingual tablets 40 pcs. RUB 48 Buy |
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Nitroglycerin 0.5 mg tablets sublingual 40 pcs. RUB 49 Buy |
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Nitroglycerin tablets sublingual. 0.5mg 40 pcs. RUB 51 Buy |
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Nitroglycerin 0.4 mg / dose 200 doses sublingual dosed spray 1 pc. 91 rbl. Buy |
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Nitroglycerin 1 mg / ml concentrate for preparation of solution for infusion 10 ml 10 pcs. RUB 590 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
