Nitromint aerosol 400mcg dose 180doz
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Active ingredients
Nitroglycerine
Release form
Spray
Composition
Nitroglycerin (in the form of a 1% solution) 400 mcg. Adjuvants: ethanol, propylene glycol. 10 g (180 doses) - metal lithographed cylinders (aluminum) (1) with a metering pump with a spray head - cardboard packs. with a protective cap with control of the first opening - packs cardboard.
Pharmacological effect
Peripheral vasodilator with a predominant effect on the venous vessels, antianginal drug. Nitroglycerin is an organic nitrogen-containing compound with a predominant venodilating action. The effects of nitroglycerin are due to the ability to release nitric oxide from its molecule, which is a natural endothelial relaxing factor. Nitric oxide activates the enzyme guanylate cyclase, which leads to an increase in the intracellular level of cGMP, which prevents the penetration of calcium ions into smooth muscle cells and causes their relaxation. The relaxation of the smooth muscles of the vascular wall causes dilation of the blood vessels, which reduces the venous return to the heart (preload) and the resistance of the pulmonary circulation (afterload). This reduces the work of the heart and myocardial oxygen demand. The expansion of the coronary vessels improves coronary blood flow and promotes its redistribution in areas with reduced blood supply, which increases the delivery of oxygen to the myocardium. A decrease in venous return leads to a decrease in filling pressure, an improvement in the blood supply to the subendocardial layers, a decrease in pressure in the pulmonary circulation and a regression of symptoms in pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic vascular tone, inhibiting the vascular component of the formation of pain. Nitroglycerin also relaxes the smooth muscle cells of the bronchi, urinary tract, gall bladder, bile ducts, esophagus, the thin and thick intestines, and their sphincters. Nitromint action begins quickly, the effect develops within 1-1.5 minutes and lasts about 30 minutes.
Pharmacokinetics
Suction: Nitromint; the aerosol is quickly and completely absorbed from the oral cavity into the systemic circulation.The bioavailability of Nitromint is 100% for sublingual use, because in this case, nitroglycerin is not metabolized during the first passage through the liver. Cmax in plasma is reached after 4 minutes. Distribution: Plasma protein binding is 60%. Circulating nitroglycerin is strongly associated with red blood cells and accumulates in the walls of blood vessels. Metabolism: It is rapidly metabolized with the participation of nitrate reductase, with the formation of di- and mononitrates (only isosorbid-5-mononitrate is pharmacologically active), the final metabolite is glycerin. Withdrawal: After taking the drug under the tongue T1 / 2 from blood plasma is 2.5-4.4 minutes. Overall clearance - 25-30 l / min. It is mainly excreted in the urine as metabolites, less than 1% is excreted unchanged.
Indications
Angina pectoris (stopping and prevention of seizures, including before exercise). Acute left ventricular failure (as part of combination therapy).
Contraindications
- shock.— collapse.– age up to 18 years old.– hypersensitivity to nitroglycerin and other organic nitrates. The drug should be used with caution in acute circulatory failure, accompanied by severe arterial hypotension (systolic blood pressure less than 90 mm Hg), orthostatic hypotension, hemorrhagic stroke, acute myocardial infarction and chronic heart failure with low filling pressure of the left ventricle, hypertrophic cardiomyopathy, severe renal and / or hepatic insufficiency Acute, severe anemia and thyrotoxicosis, alcoholism, epilepsy, traumatic brain injury, intracranial hypertension, angle-closure glaucoma (risk of increased intraocular pressure), migraine.
Dosage and administration
The drug is used sublingually. Before the first use of the drug, the dosing pump should be filled by removing the protective cap and pressing the dosing valve several times until an aerosol appears. After a long interruption in the use of the cylinder, it may be necessary to refill the pump. When using the cylinder should be held vertically, spray head up. Each time you press the metering valve from a cylinder equipped with a mechanical pump, 1 dose (400 μg of nitroglycerin) is released as an aerosol. Shake the container before use is not required.To relieve angina pectoris, 400-800 mcg (1-2 doses) are applied sublingually by pressing the dosing valve, preferably in a sitting position, with breath held at intervals of 30 seconds, then the mouth should be closed for a few seconds. If necessary, the drug is re-administered, but not more than 1.2 mg (3 doses) for 15 minutes. To prevent the development of an attack, 400 mcg is applied sublingually (1 dose) 5-10 minutes before the load. In acute left ventricular failure, developing pulmonary edema, 1.6 mg (4 doses) and more are applied sublingually in a short period of time with strict hemodynamic control (systolic blood pressure should be more than 100 mm Hg). With insufficient therapeutic effect, the same dose can be repeated after 10 minutes. When using the drug in elderly patients, the dosage regimen is not required