Nitroglycerin, 0.5 mg 40 pcs

Nitroglycerin is an organic nitrogen-containing compound with a predominant venodilator effect. The effects of nitroglycerin are due to its ability to release from its molecule nitric oxide, 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 the smooth muscle cells and causes them to relax. The relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces the venous return to the heart (preload) and the resistance of the great circle of circulation (postload). This reduces heart function and myocardial oxygen demand. Dilation of the coronary vessels improves coronary blood flow and helps redistribute it to areas with reduced blood flow, which increases oxygen delivery to the myocardium.

Decreasing venous return leads to decreased filling pressure, improved blood supply to the subendocardial layers, decreased pressure in the small circle of circulation and regression of symptoms in pulmonary edema. Nitroglycerin has a central inhibitory effect on sympathetic vascular tone, depressing the vascular component of pain syndrome formation. Nitroglycerin also relaxes smooth muscle cells of bronchi, urinary tract, gall bladder, bile ducts, esophagus, small and large intestine as well as their sphincters. The action of Nitroglycerin when used sublingually starts 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 bloodstream. Bioavailability is 100% when administered sublingually, since “primary” hepatic degradation of the drug is excluded. Cmax in plasma is reached after 4 minutes. The binding to plasma proteins is 60%.

It is quickly metabolized with the participation of nitrate reductase, with the formation of di- and mononitrates (only isosorbide-5-monononitrate is active), the final metabolite is glycerol. It is excreted by the kidneys as metabolites. Total clearance is 25-30 l/min. After drug administration under the tongue T1/2 from plasma is 2.5-4.4 minutes.

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

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Indications

Angina pectoris (relief and prevention of attacks, including before physical activity).

Pharmacological effect

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 resistance of the systemic circulation (afterload). This reduces the work of the heart and the myocardium’s need for oxygen. Dilatation of coronary vessels improves coronary blood flow and promotes its redistribution to areas with reduced blood circulation, which increases oxygen delivery to the myocardium.

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

Pharmacokinetics

Nitroglycerin spray is quickly and completely absorbed from the oral cavity into the systemic circulation. Bioavailability is 100% when taken sublingually, 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 quickly 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. Excreted by the kidneys in the form of metabolites. The total clearance is 25-30 l/min. After taking the drug sublingually, T1/2 from blood plasma is 2.5-4.4 minutes.

Circulating nitroglycerin is tightly bound to red blood cells and accumulates in the walls of blood vessels. The main route of elimination of nitroglycerin is the extraction of metabolites in the urine; less than 1% of the dose is excreted unchanged.

Special instructions

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

Particular attention and observation is required when treating patients prone to the development of orthostatic hypotension, as well as in the presence of increased intracranial pressure. Sensitivity to nitrates can vary greatly between patients, which should be taken into account when choosing dosage. Increasing the dose may cause tolerance to the drug (addiction).

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

The consumption of alcoholic beverages while using the drug is strictly prohibited.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Nitroglycerine

Composition

1 tablet contains

Active ingredient:

nitroglycerin 500 mcg

Contraindications

collapse;
shock;
age under 18 years;
simultaneous use of phosphodiesterase type five inhibitors PDE-5 (including sildenafil, vardenafil, tadalafil and other PDE-5 inhibitors);
severe arterial hypotension (systolic blood pressure below 90 mmHg);
cardiogenic shock (if measures are not taken to maintain end-diastolic pressure);
angina 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;
increased sensitivity to nitrates.

Side Effects

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

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

From the central nervous system: weakness, rarely – anxiety, psychotic reactions, lethargy, disorientation.

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

Other: rarely – blurred vision, hypothermia, methemoglobinemia.

Interaction

Other vasodilators and antihypertensive drugs (beta-blockers, slow calcium channel blockers, angiotensin-converting enzyme (ACE) inhibitors), antipsychotics, tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, phosphodiesterase type 5 inhibitors (including sildenafil and other PDE-5 inhibitors), procainamide and ethanol may increase 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 vanillinmandelic acid in the urine.

Indication of the characteristics of the action of the drug when first taken or when discontinued:

No information available.

Overdose

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

Treatment:

In mild cases, transfer the patient to the “lying” position with raised legs.
In severe cases, use general methods of treating intoxication and shock (replenishment of circulating blood volume, norepinephrine and/or dopamine). The use of epinephrine is contraindicated.

When methemoglobinemia develops, the following antidotes and treatment methods can be used:

Vitamin C – 1 g in the form of sodium salt orally or intravenously.
Oxygen therapy, hemodialysis, blood transfusion (exchange).

Storage conditions

In a place protected from light and out of reach of children at a temperature not exceeding 15 ° C, away from fire.

Manufacturer

Medisorb, Russia