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.
Buy Nitrospray FST sublingual spray 04.mg/dose 200doses 10ml in pharmacies
Trade name of the drug:
Nitrospray
International nonproprietary or generic name:
nitroglycerine
Dosage form:
dosed sublingual spray
Compound:
Nitroglycerin solution 4% - 250 g (in terms of nitroglycerin) - 10 g Ethanol - up to 1000 g (rectified ethyl alcohol)
Description:
a clear, colorless liquid contained in a bottle with a mechanical dosing pump. The determination is carried out immediately after opening the bottle.
Pharmacotherapeutic group:
vasodilator - nitrate
Pharmacological properties
Nitroglycerin is an organic nitrogen-containing compound with a predominant venodilating effect.
Mechanism of action
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 (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 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-mononitrate 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.
Indications for use
- prevention of angina attacks through prophylactic use of the drug before physical activity; - relief of angina attacks; - acute left ventricular failure (including acute myocardial infarction).
Contraindications
- increased sensitivity 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).
Carefully:
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, thyrotoxicosis, hypertrophic cardiomyopathy (possible increased frequency of angina attacks), severe renal failure, liver failure (risk of developing methemoglobinemia).
Pregnancy and lactation
There is no data on the penetration of nitroglycerin into breast milk.
Use during pregnancy and breastfeeding requires careful comparison of risks and benefits and should be carried out under strict medical supervision.
Directions for use and doses
It is recommended to take the drug as prescribed by a doctor to avoid complications.
Relieving an attack of angina
At the first attack of angina, use 1 or 2 doses sublingually. 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:
- if possible, sit down - 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.
When using for the first time or after long-term non-use, it is recommended to release one dose into the air to fill the aerosol chamber before direct use.
Side effect
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.
Other: rarely - blurred vision, hypothermia, methemoglobinemia.
Overdose
Symptoms: headache, decreased blood pressure, orthostatic hypotension, reflex tachycardia, dizziness, facial flushing, vomiting and diarrhea, asthenia, increased drowsiness, feeling hot. Extremely high doses (more than 20 mg/kg) lead to methemoglobinemia, cyanosis, dyspnea and tachypnea, and orthostatic collapse.
Treatment: in mild cases, transfer the patient to a lying position with legs elevated.
In case of severe manifestations of overdose, general methods of treating intoxication and shock (replenishment of circulating blood volume, norepinephrine, and/or dopamine, etc.) should be used.
The use of epinephrine (adrenaline) is contraindicated.
When methemoglobinemia develops, the following antidotes and treatment methods can be used:
1. Vitamin C - 1 g in the form of sodium salt or intravenously. 2. Methylene blue intravenously in a dose of up to 50 ml of a 1% solution. 3. Toluidine blue intravenously, the first dose is 2-4 mg/kg, then repeatedly 2 mg/kg. 4. Oxygen therapy, hemodialysis, blood transfusion (exchange).
Interaction with other drugs
Other vasodilators and antihypertensive drugs (beta-blockers, slow calcium channel blockers), angiotensin-converting enzyme (ACE) inhibitors, antipsychotics, tricyclic antidepressants, monoamine oxidase inhibitors (MAO), procainamide and ethanol may enhance the hypotensive effect of nitroglycerin.
Nitroglycerin enhances the effect of dihydroergotamine and reduces the effectiveness of heparin.
Orthostatic collapse may occur against the background of quinidine and procainamide.
Concomitant use with phosphodiesterase type 5 (PDE 5) inhibitors - sildenafil, tadalafil, vardenafil - may enhance the drug's ability to lower blood pressure.
special instructions
Nitroglycerin enhances the excretion of catecholamines and vanillinmandelic acid in the urine.
The consumption of alcoholic beverages while using the drug is strictly prohibited.
Impact on driving and work requiring increased attention
At the beginning of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. In the future, the degree of restrictions is determined individually for each patient.
Release form
Sublingual spray dosed 0.4 mg/dose.
10 ml (200 doses) in polypropylene bottles equipped with mechanical dosing pumps, nozzles and protective caps.
The bottle along with instructions for use is placed in a cardboard pack.
Storage conditions
List B. In a dark place, away from fire, at a temperature not exceeding 30 °C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date indicated on the package.
Conditions for dispensing from pharmacies
Over the counter.
