Nitroglycerin, 0.5 mg, 40 pcs.

1 tablet contains

Active substance:

nitroglycerin 500 mcg

Nitroglycerin is an organic nitrogen-containing compound with a predominant venodilating effect. The effects of nitroglycerin are due to its ability to release nitric oxide from its molecule, which is a natural endothelial relaxing factor.

Nitric oxide increases the intracellular concentration of cyclic guanosine monophosphatase, which prevents the penetration of calcium ions into smooth muscle cells and causes them to relax. Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces venous return to the heart (preload) and the resistance of the systemic circulation (afterload). This reduces the work of the heart and myocardial oxygen demand. Expansion of coronary vessels improves coronary blood flow and promotes its redistribution in areas with reduced blood circulation, which increases oxygen delivery to the myocardium.

A decrease in venous return leads to a decrease in filling pressure, an improvement in blood supply to the subendocardial layers, a decrease in pressure in the pulmonary circulation, and a regression of symptoms in pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic vascular tone, inhibiting the vascular component of the formation of pain. Nitroglycerin also relaxes smooth muscle cells of the bronchi, urinary tract, gallbladder, bile ducts, esophagus, small and large intestines, and their sphincters. The action of Nitroglycerin with sublingual application begins quickly, the effect develops within 1-1.5 minutes and lasts about 30 minutes.

 Pharmacokinetics

Nitroglycerin spray is rapidly and completely absorbed from the oral cavity into the systemic circulation. Bioavailability is 100% with sublingual administration, since “primary” hepatic degradation of the drug is excluded. Cmax in blood plasma is reached after 4 minutes. The connection with blood plasma proteins is 60%.

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 by the kidneys in the form of metabolites. The total ground clearance is 25-30 l / min. After taking the drug under the tongue, T1 / 2 from the blood plasma is 2.5-4.4 minutes.

Circulating nitroglycerin is firmly bound to erythrocytes and accumulates in the walls of blood vessels. The main route of excretion of nitroglycerin is the extraction of metabolites with urine; less than 1% of the dose is excreted unchanged.

Angina pectoris (relief and prevention of seizures, including before exercise).

• collapse;
• shock;
• age up to 18 years;
• the simultaneous use of phosphodiesterase inhibitors of the fifth type PDE-5 (including sildenafil, vardenafil, tadalafil and other PDE-5 inhibitors);
• severe arterial hypotension (systolic blood pressure below 90 mm Hg);
• cardiogenic shock (if no measures are taken to maintain the end diastolic pressure);
• angina pectoris caused by hypertrophic obstructive cardiomyopathy;
• constrictive pericarditis;
• pericardial tamponade;
• acute myocardial infarction and chronic heart failure with low left ventricular filling pressure;
• severe stenosis of the aortic and / or mitral valve, primary pulmonary hypertension (since hyperemia of insufficiently ventilated alveolar zones can lead to hypoxia);
• any condition associated with increased intracranial pressure;
• hypersensitivity to nitrates.

From the side of the cardiovascular system: dizziness, headache, tachycardia, fever, decreased blood pressure; rarely (especially in case of overdose) - orthostatic collapse, cyanosis, due to a pronounced decrease in blood pressure, the drug can aggravate the symptoms of angina pectoris (a paradoxical reaction to nitrates). Collapse with bradyarrhythmia and loss of consciousness is sometimes observed.

From the digestive system: dryness of the oral mucosa, rarely - nausea, vomiting, abdominal pain.

From the side of the central nervous system: weakness, rarely - anxiety, psychotic reactions, lethargy, disorientation.

Allergic reactions: rarely - skin rash, itching, exfoliative dermatitis.

Others: rarely - blurred vision, hypothermia, methemoglobinemia.

Other vasodilators and antihypertensive drugs (beta-blockers, blockers of "slow" calcium channels, angiotensin-converting enzyme (ACE) inhibitors), antipsychotics, tricyclic antidepressants, monoamioxidase (MAO) inhibitors, phosphodiesterase inhibitors, including other type 5 inhibitors 5), procainamide and ethanol can enhance the hypotensive effect of Nitroglycerin.

Nitroglycerin enhances the effect of dihydroergotamine and reduces the effectiveness of heparin, nitroglycerin increases the concentration of dihydroergotamine in the blood serum, thereby enhancing its effect.

Taking acetylsalicylic acid increases the level of nitroglycerin in the blood and enhances its effect.

Nitroglycerin spray enhances the excretion of catecholamines and vanillin mandelic acid in the urine.

Indication of the features of the action of the drug at the first dose or at its withdrawal:

There is no information.

Sublingual.

Nitroglycerin is recommended to be taken as directed by your doctor.

The tablet is kept under the tongue until it is completely absorbed, without swallowing, immediately after the onset of pain - 0.5-1 mg per dose. In many patients with stable angina pectoris, the effect comes from a lower dose (1 / 2–1 / 3 tablets), therefore, if the pain quickly passes, the rest of the tablet that has not had time to dissolve is recommended to be spit out.

Usually the antianginal effect appears within 0.5–2 minutes; 75% of patients notice improvement within the first 3 minutes, and another 15% - within 4–5 minutes. In the absence of antianginal action, within the first 5 minutes you need to take another 1 tablet. nitroglycerin. If there is no therapeutic effect after taking 2-3 tablets (capsules), you should immediately call a doctor. The duration of action after sublingual administration is about 45 minutes.

With frequent attacks of angina pectoris, it is customary to prescribe prolonged nitroglycerin drugs. Tolerance to sublingual forms of nitroglycerin develops infrequently, nevertheless, when it occurs in some patients, the dose of the drug has to be gradually increased, bringing it to 2-3 tablets.

Symptoms: headache, decreased blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, facial flushing, vomiting and diarrhea, asthenia, increased drowsiness, feeling of heat. Extremely high doses (more than 20 mg / kg) lead to methemoglobinemia, cyanosis, dyspnea and tachypnea, orthostatic collapse.

Treatment:

• In mild cases, the patient is transferred to the "lying" position with raised legs.
• In severe cases, apply general methods of treatment of intoxication and shock (volume replacement, norepinephrine and / or dopamine). Epinephrine is contraindicated.

With the development of methemoglobinemia, the following antidotes and treatment methods can be used:

• Vitamin C - 1 g as sodium salt by mouth or intravenously.
• Oxygen therapy, hemodialysis, blood transfusion (exchange).

It should be used with caution in orthostatic hypotension, hemorrhagic stroke, severe renal and / or hepatic failure, thyrotoxicosis, alcohol abuse, epilepsy, traumatic brain injury, closed-angle glaucoma (risk of increased intraocular pressure), migraine, severe anemia.

Special attention and supervision is required in the treatment of patients prone to the development of orthostatic hypotension, as well as in the presence of increased intracranial pressure. Sensitivity to nitrates can vary greatly from patient to patient, which should be considered when choosing a dosage. Increasing the dose may cause drug tolerance (addiction).

The drug contains alcohol, which is important for patients with impaired liver function, alcohol abuse, epilepsy, traumatic brain injury and other diseases of the central nervous system, as well as for pregnant women and children. Nitroglycerin can increase the effects of other drugs. If blurred vision or dry mouth persists or is severe, treatment should be discontinued.

Drinking alcoholic beverages while using the drug is strictly prohibited.

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.

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