Nitroglycerin, pills 0.5mg, 40pcs – Medisorb

Composition

1 tablet contains

Active ingredient:

nitroglycerin 500 mcg

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 of the large circle of blood circulation (afterload). This reduces the work of the heart and the need for oxygen in the myocardium. Dilation of the coronary vessels improves coronary blood flow and promotes its redistribution in areas with reduced blood circulation, which increases the delivery of oxygen 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 small circle of blood circulation, and a regression of symptoms in pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic tone of blood vessels, inhibiting the vascular component of pain syndrome formation. Nitroglycerin also relaxes the smooth muscle cells of the bronchi, urinary tract, gallbladder, bile ducts, esophagus, small and large intestines, and 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 rapidly and completely absorbed from the oral cavity into the systemic circulation. Bioavailability is 100% with sublingual use, since “primary” hepatic degradation of the drug is excluded. Cmax in blood plasma is reached after 4 minutes. Binding to 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 strongly 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.

Indications

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

Contraindications

• collapse;
• shock;
• the age of 18;
• simultaneous use of inhibitors of phosphodiesterase of the fifth type of PDE-5 (i. e. sildenafil, vardenafil, tadalafil and other of inhibitors PDE-5);
• severe arterial hypotension (systolic blood pressure below 90 mm Hg. calendar);
• cardiogenic shock (unless measures are 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 filling pressure of the left ventricle;
• severe stenosis of the aortic and/or mitral valve disease, primary pulmonary hypertension (as hyperemia insufficiently ventilated alveolar areas 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 (paradoxical reaction to nitrates). Sometimes there is a collapse with bradyarrhythmia and loss of consciousness.

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, pruritus, exfoliative dermatitis.

Other: rarely-blurred vision, hypothermia, methemoglobinemia.

Interaction

Other vasodilators and antihypertensive agents (beta-blockers, slow calcium channel blockers, angiotensin-converting enzyme (ACE) inhibitors), neuroleptics, tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, phosphodiesterase type 5 inhibitors (including sildenafil and other PDE-5 inhibitors), procainamide, and ethanol can be used to reduce blood pressure. 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 vanillinmindalic acid in the urine.

Indication of the characteristics of the drug’s action at the first dose or when it is canceled:

No information available.

How to take, course of use and dosage

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 reception. In many patients with stable angina, the effect comes from a lower dose (1/2-1/3 tablets), so if the pain passes quickly, the rest of the tablet, which has not had time to resolve, is recommended to spit out.

Usually, the antianginal effect manifests itself 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 an antianginal effect, you need to take another 1 tablet during the first 5 minutes. 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 use is about 45 minutes.

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

Overdose

Symptoms: headache, low blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, redness of the face, vomiting and diarrhea, asthenia, increased drowsiness, feeling hot. Extremely high doses (more than 20 mg/kg) lead to methemoglobinemia, cyanosis, dyspnoea 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 treatment of intoxication and shock (replenishment of the volume of circulating blood, norepinephrine and / or dopamine). The use of epinephrine is contraindicated.

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

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

Special instructions

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

Special attention and monitoring 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 may vary greatly from patient to patient, which should be taken into account when choosing the 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 pregnant women and children. Nitroglycerin may increase the effects of other medications. If blurred vision or dry mouth persists or is severe, treatment should be discontinued.

The use of alcoholic beverages during the use of 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 increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets

Storage conditions

In a place protected from light and inaccessible to children at a temperature not exceeding 15 °C, away from fire.

Active ingredient

Nitroglycerin

Dosage form

Tablets

Purpose

For adults

Indications

Angina