Nitroglycerin, capsules 0.5mg, 40pcs

Composition

Active ingredient:

nitroglycerin 0.5 mg;

Pharmacological action

Nitroglycerin is a venodilating agent from the group of nitrates. Nitrates are able to release nitric oxide from their molecule, which is a natural endothelial relaxing factor-a mediator of direct activation of guanylate cyclase. An increase in cGMP concentration leads to relaxation of smooth muscle fibers, mainly venules and veins. It has an antianginal and antispasmodic effect, relaxes the smooth muscles of the vascular walls, bronchi, gastrointestinal tract, biliary tract, ureters. When administered intravenously (iv), it has a rapid reduction in preload on the heart due to the expansion of peripheral veins.

Reduces blood flow to the right atrium, helps to reduce pressure in the small circle of blood circulation and regression of symptoms in pulmonary edema, reduces afterload, myocardial oxygen demand (by reducing preload, afterload and ventricular wall tension due to a decrease in heart volume). Promotes the redistribution of coronary blood flow in areas with reduced blood circulation.

It has a central inhibitory effect on the sympathetic tone of blood vessels, inhibiting the vascular component of pain syndrome formation. Causes dilation of meningeal vessels, which explains the headache when using it.

Pharmacokinetics

Once in the systemic circulation,60% is bound by plasma proteins. It is highly lipophilic and has a large volume of distribution (3.3-1.2 l / kg). It is rapidly metabolized in the liver by glutathione reductase, which acts on organic nitrates, with the formation of di-and mononitrates, the final metabolite is glycerol. It is excreted by the kidneys in the form of metabolites.

The total clearance is 30-78 l / min, the elimination half – life is 1-3 min. In addition, nitroglycerin is metabolized in red blood cells by enzymatic reactions that occur with the participation of sulfhydryl radicals, as well as when interacting with reduced hemoglobin.

Indications

Unstable angina, pulmonary edema, acute myocardial infarction (including those complicated by acute left ventricular failure); relief of angina attacks.

Contraindications

severe anemia; hyperthyroidism; the age of 18 years (safety not established); hypersensitivity to nitrates; cranial hypertension; cardiac tamponade; isolated mitral stenosis; constrictive pericarditis (state, accompanied by a decrease in filling pressure of the left ventricle); uncontrolled hypovolemia; heart failure with normal or low pulmonary artery pressure; collapse; hemorrhagic stroke; subarachnoid hemorrhage; recent head injury; toxic pulmonary edema, idiopathic hypertrophic subaortic stenosis; form-closure glaucoma with high intraocular pressure; stroke; shock; hypotension (SBP simultaneous treatment with sildenafil (Viagra); pregnancy; breastfeeding. With caution (comparing risk and benefit): severe renal insufficiency; hepatic insufficiency (risk of methemoglobinemia).

Side effects

Allergic reactions: rarely – skin rash, itching. Local reactions: hyperemia of the skin, itching of the skin, burning, allergic contact dermatitis.

From the cardiovascular system: dizziness, “nitrate” headache, tachycardia, skin hyperemia, fever, palpitation, decreased blood pressure, rarely (especially with overdose) – orthostatic collapse, cyanosis.

Gastrointestinal disorders: dry mouth, nausea, vomiting, abdominal pain.

From the central nervous system: rarely (especially in case of overdose) – anxiety, psychotic reactions, lethargy, disorientation.

Others: blurred vision, weakness, hypothermia, methemoglobinemia.

Interaction

use with dihydroergotamine can lead to an increase in its content in the blood and lead to an increase in blood pressure (increased bioavailability of dihydroergotamine).

Simultaneous use of nitroglycerin and heparin reduces the effectiveness of the latter (after discontinuation of the drug, a significant decrease in blood clotting may occur, which may require a reduction in the dose of heparin).

Concomitant use with vasodilators, antihypertensive agents, angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, slow calcium channel blockers, procainamide, tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, phosphodiesterase inhibitors, and ethanol increases the hypotensive effect.

How to take, course of use and dosage

Sublingual.

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

The tablet (capsule) 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 (capsule) within 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 (capsules).

Overdose

Symptoms: reflex tachycardia, headache, asthenia may develop, marked decrease in blood pressure (below 90 mm Hg) with orthostatic dysregulation, dizziness, increased drowsiness, fever, nausea, vomiting, collapse, cyanosis, methemoglobinemia, dyspnea and tachypnea when using high doses (more than 20 mg/kg).

Treatment: stop further use. Lower the headboard of the bed and lift the patient’s legs.

As a rule, blood pressure normalizes within 15-20 minutes after stopping the use of nitroglycerin, then you can continue the use after re-selecting the infusion rate.

Special instructions

While taking nitroglycerin, a significant decrease is possible Blood pressure and the appearance of dizziness during a sharp transition to an upright position from a “lying” or “sitting” position, when drinking alcohol, performing physical exercises and hot weather. Nitroglycerin, like all organic nitrates, becomes addictive with frequent use, and an increase in the dose is required.

When driving vehicles and operating mechanisms that require increased attention, it should be borne in mind that taking nitroglycerin can lead to a decrease in the speed of motor and mental reaction.

The severity of headache with nitroglycerin may be reduced by reducing its dose and / or taking validol at the same time.

Form of production

Capsules

Storage conditions

In a place protected from light and out of reach of children, away from fire, at a temperature of 5°C to 25°C.

Shelf life

3 years

Active ingredient

Nitroglycerin

Dosage form

Capsules

Description

For adults

Indications

Angina