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

Stenocardia (control and prevention of attacks, including before physical activity).

Active ingredient

Composition

1 tablet contains

The active ingredient:

Nitroglycerin 500 mcg

How to take, the dosage

Sublingual.

Nitroglycerin is recommended when prescribed by a doctor.

The tablet is held under the tongue until completely absorbed, without swallowing, immediately after pain occurs, 0.5-1 mg per dose. Many patients with stable angina pectoris have a smaller dose (1/2-1/3 of a tablet), so if the pain goes away quickly, it is recommended that the remainder of the tablet, which has not had time to dissolve, be spit out.

The antianginal effect is usually seen in as little as 0.5-2 minutes; 75% of patients report improvement within the first 3 minutes, and another 15% within 4-5 minutes. If there is no antianginal effect, 1 more tablet should be taken within the first 5 min. nitroglycerin. If there is no therapeutic effect after taking 2-3 tablets (capsules), it is necessary to call a doctor immediately. The duration of action after sublingual administration is about 45 minutes.

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

Interaction

Other vasodilators and hypotensive agents (beta-adrenoblockers, “slow” calcium channel blockers, angiotensin-converting enzyme (ACE) inhibitors), neuroleptics, tricyclic antidepressants, monoamine oxidase inhibitors (MAOIs), type 5 phosphodiesterase inhibitors (including sildenafil and other FDE-5 inhibitors), procainamide and ethanol may increase the hypotensive effect of Nitroglycerin.

Nitroglycerin increases the effect of dihydroergotamine and reduces the effectiveness of heparin, and nitroglycerin increases the serum concentration of dihydroergotamine, thereby increasing its effect.

The administration of acetylsalicylic acid increases the blood level of nitroglycerin and enhances its effects.

Nitroglycerin spray increases the excretion of catecholamines and vanillinic acid in the urine.

Particulars of the effect of the drug when first taken or when it is withdrawn:

No information available.

Special Instructions

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

Particular attention and monitoring is required during the therapy of patients prone to develop orthostatic hypotension and in the presence of elevated intracranial pressure. The sensitivity to nitrates can vary widely from patient to patient, which should be considered when choosing a 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, craniocerebral trauma and other central nervous system diseases, as well as for pregnant women and children. Nitroglycerin may increase the effects of other drugs. If blurred vision or dry mouth persist or are severe, treatment should be discontinued.

The consumption of alcoholic beverages during the use of the drug is strictly prohibited.

During treatment, it is necessary to refrain from driving and engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Side effects

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 may increase symptoms of angina pectoris (paradoxical reaction to nitrates). Collapse with bradyarrhythmia and loss of consciousness is sometimes observed.

Digestive system disorders: dry mucous membrane of the mouth, rarely – nausea, vomiting, abdominal pain.

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

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

Other: rare – blurred vision, hypothermia, methemoglobinemia.

Overdose

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

Treatment:

The following antidotes and treatments may be used if methemoglobinemia develops:

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