Nitrogranulong
Nitrogranulong: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Nitrogranulong
ATX code: C01DA02
Active ingredient: nitroglycerin (Nitroglycerin)
Producer: Technologist, PrJSC (Ukraine)
Description and photo update: 2019-09-07
Nitrogranulong is a nitrate group drug used to prevent angina attacks.
Release form and composition
Dosage form - tablets of prolonged action: biconvex, round, white or almost white, at the fracture a core stands out, surrounded by a denser continuous layer (in a cardboard box 5 blisters of 10 tablets or 1 container of 50 tablets and instructions for use of Nitrogranulong).
Composition of 1 tablet:
- active substance: nitroglycerin - 2.9 or 5.2 mg;
- auxiliary components: corn starch, titanium dioxide, polyethylene glycol 6000, gelatin, anhydrous colloidal silicon dioxide, potato starch, magnesium stearate, white sugar, povidone, talc, lactose monohydrate.
Pharmacological properties
Pharmacodynamics
Nitrogranulong is one of the antianginal drugs with prolonged efficacy. The active ingredient is nitroglycerin, an active vasodilator that affects arterial and venous vessels, belongs to the group of organic nitrates.
The mechanism of the therapeutic effect of nitroglycerin is associated with peripheral prolonged vasodilation. Due to the use of the drug, there is a decrease in the resistance of the coronary vessels along with the expansion of predominantly postcapillary venous vessels, which leads to a decrease in venous return to the heart.
In the case of using higher doses, nitroglycerin also promotes the expansion of precapillary arterioles that regulate peripheral vascular resistance, while a decrease in the load on the myocardium and a decrease in its oxygen demand is noted.
In patients with angina pectoris, Nitrogranulong increases exercise tolerance, promotes redistribution of coronary blood flow in areas with reduced blood circulation.
Pharmacokinetics
After oral administration, nitroglycerin is gradually absorbed in the small intestine. Its action develops in 30-60 minutes, the duration of the effect is from 4 to 6 hours.
The substance is largely destroyed in the liver, nitrate reductase takes part in the process (the first pass effect), and then it is biotransformed into nitric oxide (NO) in smooth muscle cells.
In comparison with nitroglycerin used under the tongue, the bioavailability of Nitrogranulong is no more than 10%. The metabolites are mono- and dinitrates (only isosorbide-5-mononitrate is active). The final metabolite is glycerin. T 1/2 (half-life) of metabolites - 4 hours. Binds to plasma proteins (60%).
The drug is excreted mainly in the form of metabolites, mainly by the kidneys.
Indications for use
Nitrogranulong is prescribed for the prevention of angina attacks in patients with coronary artery disease (ischemic heart disease), including in the postinfarction period.
Contraindications
Absolute:
- a recent head injury;
- hemorrhagic stroke;
- cerebral ischemia;
- cerebral hemorrhage;
- increased intracranial pressure;
- bradycardia (less than 50 beats / min);
- hypertrophic obstructive cardiomyopathy;
- arterial hypotension (in patients with systolic pressure below 90 mm Hg);
- aortic stenosis;
- collapse;
- shock;
- conditions that are accompanied by a decrease in filling pressure of the left ventricle, including isolated mitral stenosis, acute myocardial infarction, constrictive pericarditis;
- angle-closure glaucoma combined with high intraocular pressure;
- toxic pulmonary edema;
- cardiac tamponade;
- combination therapy with PDE-5 (phosphodiesterase-5) inhibitors, including sildenafil, tadalafil, vardenafil;
- rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (Nitrogranulong contains lactose);
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to the components of the drug, as well as nitrates.
Relative (Nitrogranulong tablets are prescribed under medical supervision after assessing the balance of benefits and risks):
- severe renal / hepatic impairment;
- uncontrolled hypovolemia;
- hyperthyroidism;
- severe anemia;
- severe cerebral atherosclerosis;
- heart failure in patients with normal or low pulmonary artery pressure;
- elderly age.
Nitrogranulong, instructions for use: method and dosage
Nitrogranulong is taken orally, on an empty stomach, with a small amount of liquid. It is impossible to chew and bite the pill, since an excess amount of nitroglycerin can enter the systemic circulation through the oral mucosa.
The dosage regimen is determined individually by the severity of the disease.
In order to prevent the development of tolerance, Nitrogranulong should be used with a break of 10-12 hours (nitrate-free interval).
The drug is taken 2 times a day - in the morning and after lunch. A single dose - 1-2 tablets: with a mild course of the disease - 2.9 mg, with a more severe course - 5.2 mg. According to the indications, Nitrogranulong can be taken 3 times a day, while the nitrate-free interval of 10-12 hours must be observed.
In patients who have attacks mainly at night, the drug should be taken in the afternoon and evening.
The maximum daily dose of Nitrogranulong is 30 mg.
Side effects
Basically, in the early stages of the use of Nitrogranulong, depending on the dose and most often as a result of the vasodilator effect, the following side reactions from organs and systems can be observed:
- immune system: allergic reactions, including skin rash, itching, urticaria, pallor and / or flushing of the skin, anaphylactic shock;
- cardiovascular system: tachycardia, orthostatic reactions, decreased blood pressure, paradoxical bradycardia (in patients with acute hypotension or syncope), methemoglobinemia, facial hyperemia, pallor, cyanosis;
- nervous system: blurred vision, nitrate headache (especially observed at the beginning of the course of treatment; with prolonged treatment, the severity of the symptom decreases), feeling of weakness, dizziness, anxiety, disorientation, lethargy, psychotic reactions;
- digestive system: nausea, abdominal pain, vomiting, xerostomia;
- others: weakness, fever, respiratory failure, irritability, hypothermia, exacerbation of glaucoma, visual impairment.
There is also information about isolated cases of the development of the following disorders: angioedema, asystole, complete blockade, exacerbation of coronary heart disease due to hypoxia.
With a sudden decrease in blood pressure, paradoxical nitrate reactions (in the form of increased symptoms of angina pectoris) can sometimes occur.
Overdose
The main symptoms of nitroglycerin overdose are a decrease in blood pressure (to a level below 90 mm Hg) in combination with orthostatic dysregulation, increased body temperature, severe dizziness, headache, heart palpitations, fainting, vomiting, nausea, severe weakness, chills, increased sweating, shortness of breath, drowsiness, arterial hypotension, feeling of heat.
In the case of using high doses (from 0.02 mg / kg), the development of collapse, methemoglobinemia, tachypnea, dyspnea, cyanosis of the lips, palms or nails is possible.
Therapy: gastric lavage, taking laxatives, activated carbon. The patient must be transferred to a horizontal position with raised legs.
Other possible activities:
- severe cases of overdose: the use of plasma substitutes, sympathomimetics, oxygen;
- methemoglobinemia: use of methylene blue.
special instructions
For the treatment of acute attacks of angina pectoris, Nitrogranulong should not be used.
During the period of taking the drug, drinking alcohol is unacceptable. A visit to the sauna, bath, hot shower is contraindicated.
With frequent use to organic nitrates, including nitroglycerin, tolerance (addiction) may develop, which requires an increase in dose.
When carrying out a long course in order to prevent tolerance, it is recommended to take Nitrogranulong intermittently during the day, or to use it simultaneously with calcium antagonists, angiotensin-converting enzyme inhibitors or diuretics. In the event of the development of tolerance, it is possible to temporarily (for several days) cancellation of Nitrogranulong and its replacement with antianginal drugs belonging to other pharmacotherapeutic groups.
You must inform your doctor about a previous reaction to taking medications of this group.
During the period of taking Nitrogranulong, with a sharp transition from a lying or sitting position to an upright position, when doing physical exercises in hot weather, while drinking alcohol, dizziness may appear and blood pressure may significantly decrease.
In cases where xerostomia or blurred vision persist for a long time, or have significant severity, Nitrogranulong is canceled.
The likelihood of developing methemoglobinemia increases with prolonged uncontrolled intake of nitroglycerin, as well as the use of the drug in high doses by patients with hepatic insufficiency. The main symptoms of methemoglobinemia are cyanosis, discoloration of the blood.
Influence on the ability to drive vehicles and complex mechanisms
During the period of taking Nitrogranulong, you should refuse to drive vehicles.
Application during pregnancy and lactation
Nitrogranulong is not prescribed during pregnancy / lactation.
Pediatric use
For patients under 18 years of age, Nitrogranulong tablets are contraindicated.
With impaired renal function
Due to the risk of methemoglobinemia in severe renal failure, Nitrogranulong should be used with caution.
For violations of liver function
Due to the risk of developing methemoglobinemia in severe hepatic insufficiency, the drug should be used with caution.
Use in the elderly
Nitrogranulong is prescribed with caution to elderly patients.
Drug interactions
- vasodilators, antihypertensive drugs, angiotensin-converting enzyme inhibitors, slow calcium channel blockers, diuretics, tricyclic antidepressants, monoamine oxidase inhibitors, ethanol and ethanol-containing drugs, β-adrenergic blockers, procainamides, quinidine, novocainamide enhancing drugs
- tadalafil, sildenafil, vardenafil (PDE-5 inhibitors): the combination is contraindicated, which is associated with the risk of developing uncontrolled arterial hypotension and cardiovascular complications that are life-threatening;
- atropine and other drugs that have an m-anticholinergic effect: the effect of nitroglycerin may decrease, which is associated with a decrease in its bioavailability and secretion;
- dihydroergotamine: simultaneous use can cause an increase in its plasma concentration in the blood and an increase in blood pressure (due to an increase in bioavailability);
- heparin: its anticoagulant effect may decrease (after discontinuation of the drug, a significant decrease in blood clotting is likely and, as a consequence, a decrease in the dose of heparin is necessary);
- corticosteroids, α-adrenergic agonists, pituitrin, histamine, central nervous system stimulants, snake and bee venom, sun rays: the antianginal effect of nitroglycerin decreases;
- phenobarbital: against the background of combination therapy, nitrate metabolism in the liver is activated;
- barbiturates: nitroglycerin metabolism is accelerated;
- salicylates: the level of nitroglycerin in the blood rises;
- acetylcysteine, captopril, unitiol (donors of sulfhydryl groups): with combined use, reduced sensitivity to nitroglycerin is restored.
Analogs
Nitrogranulong analogs are Deponit 10, Nirmin, Nitrosprey, Nitrosprint, Nitro, Gluconite, Nitro-dur, Sustonit, Nitroglycerin, Nitrocor, Nitroject, Nitrolong, Perlinganit, Nitromint, Trinitrolong, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C in original packaging. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nitrogranulong
In isolated reviews of Nitrogranulong, it is noted that with regular use of the drug by patients, including the elderly, blood pressure normalizes and heart function improves.
Price for Nitrogranulong in pharmacies
The price of Nitrogranulong is unknown, since the registration period has expired, the drug is not available in pharmacies.
The approximate cost of analogs:
- Nitroglycerin (40 sublingual capsules of 0.5 mg each) - 16 rubles;
- Nitroglycerin (10 ampoules of 10 ml each with a concentrate for the preparation of a solution for infusion 1 mg / ml) - 532 rubles;
- Nitrocor (40 sublingual tablets 0.5 mg each) - 62 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
