Nitrolong - instructions for use, dose, side effects, contraindications

Excipients: ethylcellulose - 15.86 mg; cellacephate - 26.52 mg; paraffin liquid -3.38 mg; barium sulfate - 8.515 mg; egg powder - 2.08 mg; lactose monohydrate - 3.445 mg.

Capsule composition:

Capsule body: titanium dioxide - 2.0%, gelatin - up to 100%.

Capsule cap: titanium dioxide 3.0%, iron oxide red oxide 0.0857%, gelatin up to 100%.

Description:

Capsule number 2: the case is white opaque, the lid is light pink, opaque. The contents of capsules are micro-granules of spherical shape, yellow with a cream or grayish tinge, with a weak specific smell.

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.01.D.A.02 Nitroglycerine

Pharmacodynamics:

The preparation is a capsule containing microgranules of nitroglycerin.

Nitrates are capable of releasing the molecule from the nitrogen oxide, which is the natural endothelial relaxing factor - mediated direct activation of guanylate cyclase, involved in the formation of cyclic guanosine monophosphate (cGMP) from guanosine triphosphate. An increase in the concentration of cGMP leads to a relaxation of smooth muscle fibers (mainly venules and veins). Nitroglycerine limits reflex effects on blood vessels and the heart, carried through the sympathetic nerves; reduces the resistance of peripheral and coronary vessels; reduces venous return of blood to the heart; reduces the need for myocardium in oxygen; redistributes the blood flow in the myocardium in favor of the focus of ischemia; increases tolerance to physical exertion of patients with angina pectoris.

The effect develops within the first hour after ingestion and lasts up to 6 hours or more.

Pharmacokinetics:

Unlike nitroglycerin, taken under the tongue, nitroglycerine, taken orally, is subjected to intensive metabolism during the "primary passage" through the liver. It is rapidly metabolized with the participation of nitrate to form di- and mononitrate (only active isosorbide-5-monbnitrat), the final metabolite - glycerol. Bioavailability is no more than 10% compared with nitroglycerin taken under the tongue.

Due to the slow gradual release of prolonged action from special capsules, it gradually enters the portal system and is rapidly destroyed by glutathione reductase and only metabolites (approximately 40%) enter the systemic bloodstream. Connection with blood plasma proteins - 60%. It is excreted by the kidneys in the form of metabolites. The total clearance is 25-30 l / min., And the half-life is up to 40 min.

Indications:

Prevention of angina attacks, including patients who underwent myocardial infarction.

Contraindications:

- Hypersensitivity to nitrates or any other components of the drug;

- chronic heart failure with severe stenoses of aortic, mitral valves or hypertrophic obstructive cardiomyopathy;

- acute myocardial infarction with low filling pressure of the left ventricle;

- cardiac tamponade;

- constrictive pericarditis;

- severe arterial hypotension (systolic blood pressure (BP) less than 100 mm Hg, diastolic blood pressure (BP) less than 60 mm Hg);

- Acute circulatory disturbance (shock, collapse);

- toxic pulmonary edema;

- craniocerebral trauma;

- disturbance of cerebral circulation, hemorrhagic stroke;

- increased intracranial pressure;

- angle-closure glaucoma;

- simultaneous administration of inhibitors of phosphodiesterase type 5 (PDE-5) - sildenafil, tadalafil, vardenafil;

- age under 18 years (effectiveness and safety not established);

- lactose intolerance, lactase deficiency and glucose-galactose malabsorption (due to the presence of lactose in the composition).

Carefully:

Severe anemia, hyperthyroidism, atherosclerosis, severe renal failure, severe hepatic insufficiency (risk of methaemoglobinaemia), increased peristalsis of the gastrointestinal tract, malabsorption syndrome.

Pregnancy and lactation:

The use of Nitrolong during pregnancy is not recommended.

Nitrolong can be used in pregnancy only in those cases when the benefit of treatment for the mother exceeds the potential risk to the fetus.

It is not known whether nitroglycerine with breast milk, therefore, during treatment with Nitrolong, breastfeeding should be discontinued.

Dosing and Administration:

The drug should be taken on an empty stomach. The capsule is swallowed whole, not liquid, with a small amount of liquid.

Nitrolong is recommended only for the doctor's prescription.

Doses of the drug Nitrolong are determined depending on the severity of the disease.

The individual design scheme should include a 10-12-hour "non-nitric" period to prevent the development of tolerance to nitrates.

Patients usually take 1 or 2 capsules 2 times a day - in the morning and at noon.

Due to the admission of an evening dose, a 10-12-hour "non-nitric" period is provided.

If necessary, the use of the drug 3 times a day with the observance of 10-12-hour "non-nitrate" period.

In patients with a predominance of nocturnal angina pectoris, Nitrolong should be administered at noon and in the evening.

The maximum daily dose is 31.2 mg (not more than 6 capsules containing 5.2 mg of nitroglycerin).

Side effects:

Side effects are dose-dependent and in most cases are associated with the vasodilating effect of nitroglycerin.

From the side of the cardiovascular system: "nitrate" headache, dizziness, a feeling of heat,tachycardia, palpitations, swelling of the ankles and lower legs, orthostatic hypotension, marked decrease in blood pressure (especially in overdose), cyanosis, fainting, paradoxical bradycardia (with acute arterial hypotension and / or syncope), angina (paradoxical reaction to the drug) with severe coronary sclerosis arteries, hyperemia of the skin.

From the gastrointestinal tract: dryness of the oral mucosa, nausea, vomiting, abdominal pain.

From the central nervous system: drowsiness, increased fatigue, overdose - anxiety, psychotic reactions, general weakness.

On the part of the hematopoiesis system: thrombocytopenia, methemoglobinemia.

Allergic reactions: skin rash, itching.

From the skin: dermatitis allergic, dermatitis exfoliative.

Other: blurred vision, hypothermia, increased sweating, development of tolerance (including cross-over to other nitrates).

Overdose:

Symptoms: headache, marked decrease. AD (less than 90 mm Hg) with orthostatic dysregulation, reflex tachycardia; dizziness may develop; asthenia,increased drowsiness, a feeling of heat, nausea, vomiting; in more severe cases (taking more than 20 mg / kg of nitroglycerin), too, sweating, dryness of the oral mucosa, visual impairment and collapse may occur. With the development of methemoglobinemia, hypoxia can lead to cyanosis, metabolic acidosis, seizures, dyspnoea and tachypnea, coma.

Treatment: In case of an overdose, if the patient is conscious, vomiting is necessary. With a marked decrease in blood pressure, it is necessary to put the patient on his back, raise his legs and immediately call a doctor. Prescribe symptomatic means. In more severe cases, for the correction of blood pressure, infusion of liquids and phenylephrine, epinephrine and other vasodilators is performed.

With methemoglobinemia, depending on the degree of severity, the following antidotes are recommended:

1. Ascorbic acid: 1 g inside or in the form of sodium salt intravenously.

2. Oxygenotherapy, hemodialysis, exchange blood transfusion.

Interaction:

Simultaneous reception of Nitrolong and alcohol can cause an additional decrease in blood pressure and collapse.

The antihypertensive effect of Nitrolong can be enhanced by its simultaneoususe with "slow" calcium channel blockers, beta-blockers, antihypertensive drugs, procainamide, diuretics, monoamine oxidase (MAO) inhibitors, vasodilators, phenothiazines or tricyclic antidepressants.

With simultaneous admission with sildenafil, as well as with other inhibitors of PDE-5, there may be a sharp decrease in blood pressure, so the simultaneous use with these drugs is contraindicated (see section "Contraindications").

Against the background of the use of quinidine and procainamide, orthostatic collapse may occur.

Simultaneous use of nitroglycerin and dihydroergotamine may increase the bioavailability of dihydroergotamine.

Simultaneous use of nitroglycerin and heparin reduces the effectiveness of the latter, which may require an increase in the dose of heparin (after the drug can be reduced dose of heparin).

Long-term intake of isosorbide dinitrate with nitroglycerin reduces the effect of the latter.

Pharmacokinetic: adsorbents, astringents and enveloping agents reduce the absorption of nitroglycerin in the gastrointestinal tract.

Special instructions:

Nitrolong should not be used to stop angina attacks!

To do this, use high-speed forms of nitroglycerin (sublingual forms).

The withdrawal of the drug is required only with pronounced side effects.

Patients previously treated with organic nitrates (isosorbide dinitrate, isosorbide mononitrate) may require a higher dose of nitroglycerin to produce the desired hemodynamic effect.

Against the backdrop of the use of the drug Nitrolong, a significant reduction in blood pressure and the appearance of dizziness can occur with a sharp transition from the "lying" or "sitting" position to the standing position, with alcohol, exercise and hot weather, as well as increased angina with a sharp decrease in blood pressure, ischemia, until the development of myocardial infarction and sudden death (paradoxical "nitrate" reactions).

It is necessary to warn the patient about the possible occurrence of a headache (especially at the beginning of treatment), which is due to the mechanism of action of Nitrolong.

Severity of headache in the background of the use of the drug Nitrolong can be reduced by lowering its dose or by simultaneous intake of menthol-containing medicines (eg, Validol).

If blurred vision or dry mouth persists or is severe, treatment with Nitrolong should be discontinued.

When treating with Nitrolong at any time of the day, it is necessary to ensure the presence of a 12-hour "non-nitrate" period. This helps prevent the development of tolerance to nitrates.

The withdrawal of the drug after long-term treatment with large doses should be carried out gradually. A sharp cessation of therapy can cause an aggravation of the course of coronary heart disease.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Capsules of prolonged action, 5.2 mg.

Packaging:

10 capsules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered.

10, 20, 30, 40, 50 or 100 capsules are placed in a can of polyethylene terephthalate for medicines.

One bank or 1, 2, 3, 4 or 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-000403

Date of registration:28.02.2011

Expiration Date:28.02.2016

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp04.12.2016

Illustrated instructions

Instructions

Nitrolong (Nitrolong)