Nitroglycerin tablets 0.5 mg, 40 pcs. (Nytrohlytseryn)

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40 tablets

Pharmacological action

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 their relaxation. Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces venous return to the heart (preload) and resistance to a large circle of blood circulation (afterload). This reduces heart function and myocardial oxygen demand. The expansion of the coronary vessels improves coronary blood flow and contributes to its redistribution in the area with reduced blood circulation, which increases the delivery of oxygen to the myocardium.

Decreased venous return leads to lower filling pressure, improved blood supply to the subendocardial layers, decreased pressure in the pulmonary circulation and 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 the smooth muscle cells of the bronchi, urinary tract, gall bladder, bile ducts, esophagus, small and large intestines, as well as their sphincters. The action of Nitroglycerin with sublingual administration begins quickly, the effect develops within 1-1. 5 minutes and lasts approximately 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 the “primary” hepatic degradation of the drug is excluded. Cmax in plasma is reached after 4 minutes. Communication with 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 glycerin. It is excreted by the kidneys in the form of metabolites. The total 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. The circulating nitroglycerin is firmly bound to red blood cells and accumulates in the walls of blood vessels. The main route of nitroglycerin excretion is the extraction of metabolites with urine of less than 1% of the dose excreted unchanged.

Indications

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

Contraindications

collapse

shock

age up to 18 years old

simultaneous use of type 5 phosphodiesterase inhibitors PDE-5 (including sildenafil, vardenafil, tadalafil and other inhibitors with low blood pressure 90 PDF-5) mmHg. )

cardiogenic shock (if measures are not taken to maintain the final diastolic pressure)

angina pectoris caused by hypertrophic obstructive cardiomyopathy

constrictive pericarditis

tamponade of pericardium

acute low myocardial infarction and chronic heart pressure heart disease 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.

Use during pregnancy and lactation

Use of Nitroglycerin during pregnancy and while breastfeeding requires a careful comparison of risk and benefit and should be carried out under strict medical supervision.

Nitroglycerin excreted in breast milk not found.

Use in childhood

Contraindicated in children under 18 years of age.

Special instructions

Use with caution in case of 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 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 in different patients can vary greatly, 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 impaired liver function, 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.

Drinking alcohol while using the drug is strictly prohibited.

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

Composition

1 tablet contains

active substance: nitroglycerin 500 mcg

Dosage and Administration

Sublingual.

Nitroglycerin is recommended for medical use.

The tablet is kept under the tongue until 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 also occurs from a lower dose (1/2 to 1/3 tablets), therefore, if the pain goes away quickly, it is recommended to spit out the rest of the tablet that does not have time to resolve. Typically, an antianginal effect is evident after 0.5–2 minutes, 75% of patients report improvement within the first 3 minutes, and another 15% within 4–5 minutes. In the absence of antianginal action, during the first 5 minutes you need to take another 1 tablet. nitroglycerin. In the absence of a 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 preparations. Tolerance to sublingual forms of nitroglycerin develops infrequently, nevertheless, when it occurs in some patients, the dose of the drug must be gradually increased, bringing it to 2-3 tablets.

Side effects

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

From the digestive system: dry 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.

Drug interactions

Other vasodilators and antihypertensives (beta-blockers, slow calcium channel blockers, angiotensin converting enzyme (ACE) inhibitors), antipsychotics, tricyclic antidepressants, monoamine oxidase inhibitors (MAOs), type 5 phosphodiesterase inhibitors (including sildenafil and other PDE-5 inhibitors), 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.

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

Nitroglycerin Spray enhances urinary excretion of catecholamines and vanillin-mandelic acid.

Indication of the specific effects of the drug at the first dose or when it is withdrawn:

No information.

Overdose

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

Treatment: In mild cases - transfer of the patient to the position of "lying down" with raised legs.

In severe cases, use common methods of treatment of intoxication and shock (circulating blood volume, norepinephrine and / or dopamine). The use of epinephrine is contraindicated.

In the development of methemoglobinemia, the following antidotes and treatment methods can be used: Vitamin C - 1 g in the form of a sodium salt inside or intravenously.

Oxygen therapy, hemodialysis, blood transfusion.

Storage Conditions

In a dark place away from the fire and away from children at a temperature not exceeding 15 ° C.

active substance

Nitroglycerin

The dosage form of

tablet

Possible product names

Nitroglycerin tablets 0.5 mg, 40 pcs.

MEDISORB, Russia



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