Nitromintum
Active material: Nitroglycerin
When ATH: C01DA02
CCF: Peripheral vasodilators. Antianginal drug
ICD-10 codes (testimony): i20, I50.1
When CSF: 01.06.01.01.01
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
Pharmaceutical form, composition and packaging
◊ Aerosol sublingual dosage in the form of colorless or almost colorless transparent solution was obtained.
| 1 dose | |
| nitroglycerin (as 1% solution) | 400 g |
Excipients: ethanol, propylene glycol.
10 g (180 doses) – aluminum cylinders (1) with a metering pump and a spray head – packs cardboard.
Pharmacological action
Peripheral vasodilator with a primary effect on the venous vessels, antianginal drug. Nitroglycerin – organic nitrogen compound with a primary action venodilatiruyuschim.
The effects of nitroglycerin due to its ability to release a molecule of nitric oxide, which is a natural endothelial relaxing factor. Nitric oxide activates the enzyme guanylate cyclase, which leads to increased intracellular levels of cGMP, This prevents the penetration of calcium ions into smooth muscle cells, causing their relaxation. Relaxation of smooth muscle of the vascular wall causes vasodilation, reducing venous return to the heart (preload) and resistance to systemic circulation (afterload). This reduces the work of the heart and myocardial oxygen demand. Expansion of coronary vessels improves coronary blood flow and promotes its redistribution in reduced blood supply, increasing oxygen delivery to the myocardium. Reducing venous return results in lower filling pressure, improve the blood supply to the subendocardial layers, reduce the pressure in the pulmonary circulation and the regression of symptoms with pulmonary edema. Nitroglycerin has a central inhibiting effect on sympathetic vascular tone, inhibiting the formation of vascular component of pain. Nitroglycerin also relaxes the smooth muscle cells of the bronchi, urinary tract, gallbladder, bile duct, esophagus, small and large intestines, and their sphincters.
Action Nitromintum® It begins quickly, effect develops over 1-1.5 minutes and lasts for about 30 m.
Pharmacokinetics
Absorption
Nitromintum® Spray rapidly and completely absorbed from the mouth into the systemic circulation. Bioavailability Nitromintum® is 100% if sublingual application, tk. In this case nitroglycerin is not metabolized in “first pass” through the liver. Cmax plasma levels achieved after 4 m.
Distribution
Binding to plasma proteins is 60%.
Circulating nitroglycerin strongly associated with the erythrocytes and accumulates in the vascular wall.
Metabolism
It is rapidly metabolized with the participation of nitrate, to form a di- and mononitrate (pharmacologically active only isosorbide-5-mononitrate), the final metabolite – glycerol.
Deduction
After receiving the drug under the tongue T1/2 from plasma is 2.5-4.4 m. Total clearance – 25-30 l / min.
Write mainly in the urine as metabolites, less 1% excreted unchanged.
Testimony
- Angina (relief and prevention of attacks, incl. before exercise);
- Acute left ventricular failure (in a combination therapy).
Dosage regimen
The drug is used sublingually.
Before the first use of the drug should be filled metering pump by removing the protective cap and pressing the dosing valve several times until the aerosol. After a long break in the use of the cylinder may need to be repeated filling pump. When using a balloon should be kept vertically, spray head up.
Each time the metering valve from the cylinder, provided with a mechanical pump, released 1 dose (400 mcg nitroglycerin) aerosol.
Shake the bottle before use is not required.
To relief of angina attack sublingually applied 400-800 g (1-2 dose), pressing the metering valve, preferably in a sitting position, with a single breath at intervals 30 sec; thereafter should close the mouth for a few seconds. If necessary, the drug is administered again, but not more 1.2 mg (3 dose) during 15 m.
To prevention of attack sublingually applied 400 g (1 dose) for 5-10 min to load.
At acute left ventricular failure, pulmonary edema sublingually applied 1.6 mg (4 dose) and more in a short time under the strict control of hemodynamics (systolic blood pressure should be more 100 mmHg.).
In case of insufficient therapeutic effect of the same dose can be repeated after 10 m.
In applying the drug in elderly patients correction dosing regime is not required.
Side effect
Cardio-vascular system: dizziness, headache, tachycardia, fever; decrease in blood pressure; rarely (especially in overdose) – Orthostatic hypotension, cyanosis.
From the digestive system: dry mouth; rarely – nausea, vomiting, stomach ache.
CNS: weakness, rarely – anxiety, psychotic reactions, lethargy, disorientation.
Allergic reactions: rarely – skin rash, itch.
Local reactions: dermahemia, burning sensation under the tongue.
Other: rarely – blurred vision, gipotermiя, metgemoglobinemiâ.
Contraindications
- Shock;
- Collapse;
- Up to 18 years;
- Hypersensitivity to nitroglycerin and other organic nitrate.
FROM caution use in patients with acute circulatory failure, accompanied by severe arterial hypotension (systolic blood pressure less than 90 mmHg.), if orthostatic hypotension, hemorrhagic stroke, acute myocardial infarction and congestive heart failure with low pressure filling of the left ventricle, hypertrophic cardiomyopathy, severe renal and / or hepatic insufficiency, severe anemia and thyrotoxicosis, alcoholism, epilepsy, traumatic brain injury, intracranial hypertension, angle-closure glaucoma (the risk of increased intraocular pressure), migraine.
Pregnancy and lactation
During pregnancy and lactation is possible to use the drug under strict medical supervision in cases, when the anticipated benefits of therapy to the mother outweighs the potential risk to the fetus or infant.
Unknown, whether nitroglycerin is released in breast milk.
Cautions
Nitromintum® increases the excretion of catecholamines and vanilinmindalnoy acid in the urine.
During the drug the patient should exclude alcohol.
Use in Pediatrics
The drug is contraindicated for use in children and adolescents under the age of 18 years, tk. Safety Data Nitromintum® in these patients is not enough.
Effects on ability to drive vehicles and management mechanisms
At the beginning of treatment should refrain from driving vehicles and Occupation potentially hazardous activities, require high concentration and speed of psychomotor reactions. In the future, the degree of limitation is determined individually for each patient.
Overdose
Symptoms: headache, decrease in blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, redness of the face, vomiting and diarrhea, asthenia, hypersomnia, feeling the heat. At extremely high doses (more 20 mg / kg) observed methemoglobinemia, cyanosis, dyspnea and tachypnea, Orthostatic hypotension.
Treatment: in mild cases – Transfer the patient in the supine position with raised legs; in severe cases - the holding of symptomatic and supportive therapy, aimed at the elimination of toxic and shock (incl. vospolnenie OCK, a norepinephrine (noradrenaline) and / or dopamine). The use of epinephrine (adrenaline) contraindicated.
With the development of methemoglobinemia can use the following antidotes and treatments:
1. Vitamin C – 1 g sodium salt PO / in.
2. Methylene blue / in a dose of up to 50 ml of 1% solution.
3. Toluidine blue in /, the first dose 2-4 mg / kg, then multiply by 2 mg / kg.
4. -Therapy, hemodialysis, transfusion (exchange) blood.
Drug Interactions
Other vasodilators and antihypertensives (beta-blockers, blockers slow calcium channels), ACE inhibitors, neuroleptics, tricyclic antidepressants, MAO inhibitors, phosphodiesterase inhibitors, procainamide and ethanol may increase the hypotensive effect Nitromintum®.
Nitrominta® dihydroergotamine and enhances the effect of reducing the effectiveness of heparin.
Conditions of supply of pharmacies
The drug is resolved to application as an agent Valium holidays.
Conditions and terms
List B. The drug should be stored in a dark and inaccessible to children at temperature from 15 ° to 25 ° C, away from heat sources. Shelf life - 3 year.
The product is flammable and explosive. An empty cylinder to throw into the fire. Do not store and use near open flame or while smoking.
