Overdose
Symptoms: weak or rapid heartbeat, increased body temperature, cyanosis of the lips, nails or palms, convulsions, dizziness, fainting, shortness of breath, a feeling of strong pressure in the throat, weakness.
Treatment: transfer the patient to a position with legs raised (to enhance venous return); for hypotension - intravenous administration of alpha-adrenergic receptor agonists (with the exception of epinephrine), for methemoglobinemia - administration of methylene blue (iv) and oxygen therapy, for headache - taking aspirin or drugs containing menthol.
Nitrospray sublingual dose dosed 0.4 mg/dose 200 doses bottle 1 pc. In Perm
Latin name
NITROSPRAY
International nonproprietary name
nitroglycerin (glyceryl trinitrate) (nitroglycerin)
Release form
Sublingual dosed aerosol.
Package
10 ml (200 doses) - polypropylene bottles (1) with a mechanical dosing pump complete with a spray nozzle - cardboard packs.
Description
Sublingual spray dosed in the form of a clear, colorless liquid.
pharmachologic effect
Peripheral vasodilator with a predominant effect on venous vessels, antianginal drug. 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 increases the intracellular concentration of cyclic guanosine monophosphatase, which prevents the penetration of calcium ions into smooth muscle cells and causes them to relax. Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces venous return to the heart (preload) and resistance of the systemic circulation (afterload). This reduces the work of the heart and the myocardium's need for oxygen. Dilatation of coronary vessels improves coronary blood flow and promotes its redistribution to areas with reduced blood supply, which increases oxygen delivery to the myocardium. A decrease in venous return leads to a decrease in filling pressure, improved blood supply to the subendocardial layers, a decrease in pressure in the pulmonary circulation and regression of symptoms of pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic tone of blood vessels, inhibiting the vascular component of the formation of pain. Nitroglycerin also relaxes the smooth muscle cells of the bronchi, urinary tract, gallbladder, bile ducts, esophagus, small and large intestines, as well as their sphincters.
Indications
relief and prevention of angina attacks.
Directions for use and doses
Nitrospray-ICN is taken sublingually, in a sitting position, while holding your breath. Relief of an attack of angina: 1-2 doses containing 0.4-0.8 mg of nitroglycerin (if necessary, again after no less than 30 seconds), a maximum of 3 doses at intervals of 5 minutes. Prevention of angina attacks: 1 dose 5-10 minutes before expected exercise or stress. The maximum single dose is 1.6 mg (4 doses), daily dose is 6.4 mg (16 doses).
Compound
1 dose of nitroglycerin (in the form of a 4% solution) 400 mcg Excipients: ethanol (rectified ethyl alcohol).
Contraindications
- shock; - vascular collapse; - acute myocardial infarction with hypotension; — arterial hypotension (systolic blood pressure below 90 mm Hg); - hemorrhagic stroke; - recent head injury; - constrictive pericarditis; — closed-angle form of glaucoma; - hypertrophic cardiomyopathy; - toxic pulmonary edema; - pregnancy; - lactation period (breastfeeding); - childhood; - hypersensitivity to nitroglycerin and other organic nitrates.
special instructions
Due to the increased risk of developing orthostatic reactions during the period of use of the drug, caution should be exercised when abruptly moving to a standing position from a lying or sitting position, during prolonged standing, when performing physical exercises, or in hot weather. Discontinuation of the drug should be done gradually and under the supervision of a physician. During the period of use of the drug, you should avoid drinking alcohol.
Side effects
From the side of the central nervous system: blurred vision, headache (especially at the beginning of the course of treatment, with continued therapy it decreases), dizziness, weakness, restlessness. From the cardiovascular system: arterial hypotension (including orthostatic), reflex tachycardia, facial hyperemia; rarely (with a sharp decrease in blood pressure) – increased symptoms of angina pectoris (paradoxical “nitrate” reactions). From the digestive system: dry mouth, nausea, vomiting. Dermatological reactions: dermatitis, skin rash.
Drug interactions
Other antihypertensive drugs, antidepressants, PDE inhibitors (sildenafil), ethanol may enhance the hypotensive effect of Nitrospray. In this case, the effectiveness of Nitrospray may decrease. When used simultaneously with Nitrospray, the anticoagulant effect of heparin may be reduced.
Storage conditions
List B. The drug should be stored in a place protected from light and out of reach of children at temperatures up to 30°C, away from open flame.
Precautionary measures
If after taking 3 doses within 15 minutes there is no relief of the attack, a doctor’s consultation or hospitalization of the patient is necessary. You should refrain from using the drug in pediatric practice, since the safety and effectiveness of its use in children have not been determined. Alcohol consumption should be avoided during therapy. To reduce headaches, simultaneous administration of acetylsalicylic acid or menthol-containing drugs is possible. The drug should be discontinued gradually.
Nitrospray sublingual dosage. 0.4 mg/dose 200 doses 10 ml
Description:
Information is absent.
Compound:
Information is absent.
Indications for use:
Prevention of angina attacks by prophylactic use of the drug before physical activity; - relief of angina attacks; - acute ventricular failure (including acute myocardial infarction).
Contraindications:
Hypersensitivity to organic nitrates; - closed-angle form of glaucoma; - severe arterial hypotension; -increased intracranial pressure caused by cerebral hemorrhage or trauma; simultaneous use of phosphodiesterase inhibitors. age under 18 years (lack of sufficient clinical data). With caution: acute myocardial infarction with low left ventricular filling pressure (risk of decreased blood pressure and tachycardia, which can increase ischemia), chronic heart failure with low left ventricular filling pressure, severe anemia, triotoxicosis, hypertrophic cardiomyopathy (possible increased frequency of angina attacks), severe renal failure, liver failure (risk of developing methemoglobinsmia)
Pharmacodynamics:
The effects of nitroglycerin are due to its ability to release nitric oxide from its molecule, which is a natural endothelial relaxing factor. Nitric oxide increases the intracellular concentration of cyclic guanosine monophosphatase, which prevents the penetration of calcium ions into smooth muscle cells and causes them to relax. Relaxation of the smooth muscles of the vascular wall causes vasodilation, which reduces venous return to the heart (neuload) and resistance of the systemic circulation (afterload). This reduces the work of the heart and the myocardium's need for oxygen. Dilatation of coronary vessels improves coronary blood flow and promotes its redistribution to areas with reduced blood circulation, which increases oxygen delivery to the myocardium. A decrease in venous return leads to a decrease in filling pressure, improved blood supply to the subendocardial layers, a decrease in pressure in the pulmonary circulation and regression of symptoms of pulmonary edema. Nitroglycerin has a central inhibitory effect on the sympathetic tone of blood vessels, inhibiting the vascular component of the formation of pain. Nitroglycerin relaxes the smooth muscle cells of the bronchi, urinary tract, gallbladder, bile ducts, esophagus, small and large intestines. The action begins quickly, the effect develops within 1-1.5 minutes and lasts approximately 30 minutes
Pharmacokinetics:
Nitroglycerin, when administered sublingually, is quickly and completely absorbed from the oral cavity into the systemic circulation. Bioavailability is 100% when taken sublingually, since “primary” hepatic degradation of the drug is excluded. The maximum concentration in blood plasma is reached after 4 minutes. The connection with blood plasma proteins is 60%. It is quickly metabolized with the participation of nitrate reductase, with the formation of di- and mononitrates (only isosorbide-5-moconitrate is active), the final metabolite is glycerol. Excreted by the kidneys in the form of metabolites. The total clearance is 25-30 l/min. After taking the drug sublingually, the half-life from blood plasma is 2.5-4.4 minutes. Circulating nitroglycerin is tightly bound to red blood cells and accumulates in the walls of blood vessels. The main route of elimination of nitroglycerin is the extraction of metabolites in the urine; less than 1% of the dose is excreted unchanged.
Side effects:
From the cardiovascular system: dizziness, headache, tachycardia, fever, decreased blood pressure; rarely (especially in case of overdose) - orthostatic collapse, cyanosis. From the digestive system: dry mouth. rarely - nausea, vomiting, abdominal pain. From the central nervous system: weakness, rarely - anxiety, psychotic reactions, lethargy, disorientation. Allergic reactions: rarely - skin rash, itching. Local reactions: skin hyperemia, burning sensation under the tongue. Others: rarely - blurred vision, hypothermia, methemoglobinemia.
Method of preparation or use:
It is recommended to take the drug as prescribed by a doctor to avoid complications. Relief of an attack of angina pectoris At the first attack of angina pectoris, use 1 or 2 doses under the tongue. If necessary, can be reapplied at 5-minute intervals. If after taking three doses within 15 minutes the attack does not stop, you should immediately consult a doctor. For preventive purposes, use 1 dose 5-10 minutes before the expected load or stress. Highest single dose: 4 doses. Highest daily dose: 16 doses. Rules for taking the drug: - sit down as soon as possible - remove the protective cap from the balloon, hold the balloon vertically - open your mouth and hold your breath for a few seconds - press the balloon once, directing the stream of the drug under the tongue - close your mouth and try not to swallow the drug At first use or after prolonged non-use, it is recommended to release one dose into the air to fill the aerosol chamber before direct use.
Leave order:
According to the form of prescription form 107-1/у
Storage conditions:
In a place protected from light, at a temperature not exceeding 30 °C. (away from fire)
Nitrospray
Nitrospray (active ingredient - nitroglycerin) is a peripheral vasodilator drug of the nitrate group, which has an antianginal (anti-ischemic) effect and is used to relieve and prevent angina symptoms. Affects mainly venous vessels. Nitrates are rightfully considered one of the most effective groups of antianginal drugs, which have extensive experience in using both for the prevention of angina attacks and for their relief. Recently, nitroglycerin preparations in aerosol form have become increasingly popular. One of these drugs is the domestic drug nitrospray. The high effectiveness of aerosols is due to the rapid onset of the therapeutic effect precisely at those moments when the speed of action is the most important pharmacological characteristic - when relieving angina attacks. The effects of nitrospray (as well as other nitroglycerin preparations) are due to the ability of the active substance to split off a molecule of nitric oxide, known as endogenous endothelium-relaxing factor. Nitric oxide increases the level of cyclic guanosine monophosphatase inside cells, which prevents the penetration of calcium ions into the smooth muscle cells of the vascular wall, causing them to relax. The result of relaxation of the smooth muscle “cocoon” of blood vessels is vasodilation, a decrease in preload (due to a decrease in venous return) and afterload (due to a decrease in the resistance of the systemic vessels) on the myocardium. Thus, the heart is largely unloaded and reduces its demand for oxygen consumption. Increasing the lumen of the coronary vessels normalizes coronary circulation and redistributes blood flow in favor of ischemic areas of the myocardium. The reduction in venous return already mentioned above entails a decrease in filling pressure in the cavities of the heart, improved blood circulation in the subendocardial layers of the myocardium, a decrease in pressure in the pulmonary circulation and the elimination of pulmonary edema.
Nitrospray has a direct inhibitory effect on sympathetic vascular tone, suppressing the vascular component of the formation of pain. In addition to this, the drug exhibits a relaxing effect on smooth muscle cells of the respiratory, digestive (including sphincters of the esophagus, small and large intestines) and urogenital tract, bile ducts and gallbladder. Nitrospray is quickly and completely absorbed from the surface of the mucous membranes at the site of application. The concentration of the active substance sufficient to realize the therapeutic effect is achieved in a few minutes. The half-life of nitroglycerin when taken orally is 4 hours, however, since nitrospray is produced in the form of an aerosol for sublingual (sublingual) use, this figure will be significantly lower - no more than 20 minutes. The manufacturer placed the drug in a can with a metering pump, each press of which releases 1 dose equivalent to 400 mcg of nitroglycerin. To relieve an angina attack at its first manifestations, it is recommended to take 1-2 doses of nitrospray on or under the tongue, holding your breath first. The interval between repeated injections should be at least 30 seconds. If necessary, several injections can be made at five-minute intervals, but not more than 1200 mcg within 15 minutes. For preventive purposes, nitrospray in the amount of 1 dose is administered 5-10 minutes before the expected physical activity or psycho-emotional stress. The maximum amount of the drug administered at a time should not exceed 1600 mcg. The maximum daily dose of nitrospey is 6400 mcg. Due to the increased risk of postural hypotension during the use of nitrospray, caution must be exercised when changing the position of the body in space. Discontinuation of the drug should not be abrupt due to the risk of rebound syndrome. Nitrospray is incompatible with alcohol.
