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

Excipients: lactose monohydrate 38.3 mg, povidone 25-2.6 mg, microcrystalline cellulose 16.0 mg, croscarmellose sodium 2.4 mg, magnesium stearate 0.7 mg.

Description:

Round, flat-cylindrical tablets of white or almost white color, with a risk and a facet.

Pharmacotherapeutic group:vasodilator - nitrate

ATX: & nbsp

C.01.D.A.02 Nitroglycerine

Pharmacodynamics:

Peripheral vasodilator with predominant effect on venous vessels. The effect of nitroglycerin is mainly related to a decrease in the demand for myocardium in oxygen due to a reduction in preload (the expansion of peripheral veins and a decrease in the flow of blood to the right atrium) and postnagruzki (a decrease in the total peripheral vascular resistance). Has a central inhibitory effect on the sympathetic tone of blood vessels, inhibits the vascular component of the formation of pain syndrome.It causes the expansion of meningeal vessels, which explains the headache when it is used.

When applying sublingual forms, the attack of angina pectoris usually stops after 1.5 minutes, the antianginal effect persists from 30 minutes to 60 minutes.

Pharmacokinetics:

Quickly and completely absorbed from the surface of the mucous membranes of the mouth. When admission under the tongue the effect of "primary passage" through the liver is excluded. When you take 1 tablet under the tongue bioavailability is approximately 100%, the time to reach the maximum concentration in the blood - 5 minutes. Has a very large volume of distribution. Connection with blood plasma proteins - 60%. 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, the half-life period is 4-5 min.

Indications:

Kupirovanie and short-term prophylaxis of attacks of a stenocardia.

Contraindications:

- Hypersensitivity to the active substance, other organic nitrates or excipients;

- shock, collapse;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- simultaneous administration of inhibitors of phosphodiesterase-5 (including sildenafil, vardenafil, tadalafil, udenafil);

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

- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);

- severe anemia;

- cerebral hemorrhage;

- hypertrophic obstructive cardiomyopathy;

- constrictive pericarditis;

- cardiac tamponade;

- severe hypovolemia;

- severe aortic and subaortic stenosis;

- severe mitral stenosis.

Carefully:

Hemorrhagic stroke; with diseases accompanied by increased intracranial pressure, acute myocardial infarction and chronic heart failure with low left ventricular filling pressure (risk of lowering blood pressure and tachycardia, which may increase ischemia); angle-closure glaucoma (risk of increased intraocular pressure); thyrotoxicosis; arterial hypotension (can aggravate the condition, causing a paradoxical bradycardia and attacks of angina pectoris),orthostatic hypotension; severe renal insufficiency; severe hepatic insufficiency (risk of development of methemoglobinemia); recently suffered head trauma; mitral and / or aortic stenosis, alcoholism, migraine, epilepsy.

Pregnancy and lactation:

For safety reasons, the drug Nitroglycerine can be used during pregnancy and during breastfeeding only strictly according to the doctor's prescription, after a thorough evaluation of the benefits to the mother and the possible risk to the fetus / child, since there is currently insufficient data on the effects of its use in pregnant and lactating women.

There are data on the penetration of nitrates into breast milk, but the exact content of nitroglycerin in breast milk has not been determined. A possible risk of methaemoglobinemia in infants has also been reported. Isolation of nitroglycerin in breast milk has not been studied, so caution should be exercised when using this medication during breastfeeding. If the nursing mother still takes the drug Nitroglycerine, it is necessary to stop breastfeeding and to establish observation of the child for the development of possible side effects from the use of the drug.

Dosing and Administration:

Nitroglycerin is recommended only for the doctor's prescription.

Nitroglycerin should be taken immediately at the first signs of an attack of angina: 1 tablet. Nitroglycerine Put under the tongue and keep under the tongue until completely dissolved, without swallowing. The usual dose of the drug is 1 tablet under the tongue.

If the attack of angina is not stopped within 5 minutes, it is necessary to take another Nitroglycerin pill.

In the absence of therapeutic effect after taking 2 tablets, you must call a doctor.

With frequent attacks of angina pectoris, it is advisable to use nitroglycerine drugs at prolonged form.

Side effects:

To assess the incidence of adverse events, the following criteria were used (according to the classification of the World Health Organization): Often (≥10% of prescriptions); often (≥1% and <10%); infrequently (≥0.1% and <1%); rarely (≥0.01% and <0.1%); rarely (<0,01%); frequency unknown (insufficient data to estimate the frequency of development).

From the central nervous system: Often - "nitrate" headache; often - drowsiness, dizziness (including postural), frequency unknown - troar, psychotic reactions, inhibition, disorientation.

Co side of the gastrointestinal tract: infrequently - nausea, vomiting; rarely - heartburn.

From the side of the cardiovascular system: often - tachycardia, sensation heart beat, orthostatic hypotension; infrequently - paradoxical amplification etcangina pectoris, collapse (sometimes accompanied by bradyarrhythmia and syncope); rarely - cyanosis; frequency unknown - arterial hypotension.

From the skin and subcutaneous tissues: infrequently - skin allergic reactions (including rash), "tides" of blood to the skin of the face; rarely - angioedema, Stevens-Johnson syndrome; frequency unknown exfoliative dermatitis.

General disorders: often - asthenia.

Other: infrequently - blurred vision; rarely - methemoglobinemia.

For organic nitrates, there have been cases of development of severe arterial hypotension, accompanied by nausea, vomiting, anxiety, pallor and increased sweating.

Prolonged use of the drug may cause transient hypoxemia due to the relativeredistribution of blood flow to hypoventilated alveolar sites (in patients with coronary heart disease can lead to myocardial hypoxia).

Overdose:

Symptoms: a marked decrease in blood pressure (below 90 mm Hg) with orthostatic dysregulation, severe dizziness, headache, fainting, shortness of breath, severe weakness, palpitations, fever, seizures, asthenia, drowsiness, heat.

At application of high doses - a collapse, a cyanosis, a methemoglobinemia, a dyspnea and tachypnea.

Treatment

In light cases: transfer of patients to the "lying" position with raised legs or with aboutthe head end of the bed.

In more severe cases: with a pronounced decrease in blood pressure - replenishment of the volume of circulating blood, in exceptional cases, to improve blood circulation, one can inject infusions of norepinephrine (noradrenaline) and / or dopamine.

The introduction of epinephrine (adrenaline) and related compounds is contraindicated!

With methemoglobinemia: ascorbic acid - 1 g inside or in the form of the sodium salt intravenously - 0.1-0.15 ml / kg 1% solution up to 50 ml.

Oxygenotherapy, hemodialysis, exchange blood transfusion.

If there is a stoppage of breathing and heart, start immediately RAnimation activities.

Interaction:

With simultaneous use with other vasodilators, antihypertensive drugs, incl. beta-blockers, slow calcium channel blockers, angiotensin-converting enzyme inhibitors, diuretics, and phosphodiesterase-5 inhibitors used to treat erectile dysfunction (for example. sildenafil), procainamide, neuroleptics, tricyclic antidepressants, monoamine oxidase inhibitors, and also ethanol, an increase in antihypertensive action is possible.

With the simultaneous use of the drug with dihydroergotamine, there may be an increase in the concentration of dihydroergotamine in the blood, which leads to an increase in the antihypertensive effect of the latter.

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

Saproterin (coenzyme synthetase nitric oxide) increases the risk of developing arterial hypotension due to the potentiation of the synthesis of additional amounts of nitric oxide.

Nitro compounds can reduce the therapeutic effect of norepinephrine (noradrenaline).

Barbiturates accelerate metabolism and reduce the concentration of nitro compounds in the blood plasma.

Patients who previously received organic nitrates (isosorbide dinitrate or isosorbide mononitrate) an increased dose of nitroglycerin may be required.

With simultaneous use with amiodarone, propranolol, BCCC (verapamil, nifedipine, etc.), it is possible to increase the antianginal effect.

Under the influence of beta-adrenostimulants, alpha-adrenoblockers (dihydroergotamine, etc.), it is possible to reduce the severity of antianginal action (tachycardia and excessive BP reduction).

Special instructions:

Tablets can not be chewed, because through the mucous membrane of the oral cavity in the systemic blood flow can enter an excessive amount of active substance.

When Nitroglycerin is taken, a significant reduction in blood pressure and the appearance of dizziness can occur with a sharp transition to the vertical position from the "lying" or "sitting" position; when drinking alcohol, doing physical exercises and three hot weather, as well as strengthening angina with a sharp drop in blood pressure; ischemia up to myocardial infarction (paradoxical nitrate reactions).

During the period of treatment, alcohol is not allowed.

If blurred vision is persistent or severe, treatment should be discontinued.

To reduce the risk of side effects, caution should be exercised when using drugs with pronounced antihypertensive and vasodilating properties at the same time; refrain from drinking alcohol, limit stay in rooms with a high ambient temperature (sauna, sauna, hot shower), avoid taking several tablets simultaneously or sequentially in a short time after the first intake.

The risk of developing methaemoglobinemia, manifested by cyanosis and the appearance of a brown shade of blood, increases with prolonged uncontrolled intake of Nitroglycerin, the intake of high doses of the drug by a patient with hepatic insufficiency. In case of development of cyanosis Nitroglycerine it is necessary to urgently cancel and call a doctor.

Uncontrolled use of the drug can lead to the development of tolerance, expressed in reducing the duration and severity of the effect and the need to increase the dose to achieve a therapeutic effect.After a break in treatment, sensitivity to nitrates is restored.

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

During the period of treatment and for some time after its termination, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions (risk of dizziness).

Form release / dosage:

Tablets are sublingual, 0.5 mg.

Packaging:

40 tablets per container polymer.

Each polymer container, together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 years and 6 months.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:P N014095 / 01

Date of registration:23.07.2008 / 10.08.2015

The owner of the registration certificate:TECHNOLOG, PAO TECHNOLOG, PAO Ukraine

Manufacturer: & nbsp

TECHNOLOG, PAO Ukraine

Information update date: & nbsp11.03.2016

Illustrated instructions

Instructions

Nitroglycerine (Nitroglycerin)