Nitroglycerin tabs 0.5mg #40

Instruction for Nitroglycerin

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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 cylinders of 200 doses (10 ml), 1 bottle or balloon in a cardboard box, complete with a mechanical dosing pump);
    Concentrate for the preparation of solution for infusion: colorless, transparent (in ampoules of 2, 5 or 10 ml, 5 ampoules in blisters, 1, 2 or 10 packs 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.

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 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 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 syndrome. It also provokes the expansion of the meningeal vessels, which causes a headache after taking it, and relaxes the smooth muscle cells 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 the 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 glycerol.
The drug is distinguished by a very large volume of distribution (1.2,33.3 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 half-life from blood plasma 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

    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 pectoris (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 the components of the drug.
Depending on the dosage form, additional absolute contraindications to the use of the drug 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 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, the drug should be used with caution after assessing the benefit / risk ratio:
    Hemorrhagic stroke;
    Severe anemia;
    Thyrotoxicosis;
    Severe renal failure;
    Angle-closure 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: method and dosage

To prevent complications, the drug 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 anticipated physical exertion 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.
In cases where there is no therapeutic effect after taking 2 tablets of the drug, you should immediately consult a doctor.

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, a decrease in 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, when 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, the drug, 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 by taking validol at the same time.
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, craniocerebral trauma 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, the drug 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 when the rate of administration of the solution is selected, but also later, against the background of initially stabilized blood pressure (monitoring 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 the drug, care must be taken when driving vehicles and performing potentially hazardous types of work that require increased concentration of attention and rapid 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;
    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 the drug in the blood and enhancing its action.

Terms and conditions of storage

Store in a dark place, out of reach of children.
Shelf life - 2 years at temperatures up to 25 ° C;

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.

Terms of sell

You can buy Nitroglycerin without a doctor's prescription.