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.
Nitrospray
Orally, sublingually, buccally, intravenously, transdermally, cutaneously.
Relief of angina pectoris. Sublingually (the tablet or capsule is kept under the tongue until completely absorbed, without swallowing), immediately after the onset of pain - 0.5-1 mg per dose. If necessary, to achieve a faster effect, the capsule should be immediately crushed with teeth; the capsule can be repeated after 30-40 minutes. In many patients with stable angina, the effect occurs with a smaller dose (1/2-1/3 tablets), therefore, if the pain goes away quickly, it is recommended to spit out the remainder of the tablet that has not had time to dissolve. Typically, the antianginal effect appears within 0.5-2 minutes; 75% of patients note improvement within the first 3 minutes, and another 15% within 4-5 minutes. If there is no antianginal effect, another 0.5 mg of nitroglycerin should be taken during the first 5 minutes. If there is no therapeutic effect after taking 2 tablets, you should immediately call a doctor. Duration of action after sublingual administration is about 45 minutes.
For frequent attacks of angina, it is advisable to prescribe prolonged forms of nitrates. If an angina attack develops during treatment with long-acting nitrates, nitroglycerin must be taken sublingually to stop the acute attack. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, if it occurs in some patients, the dose of the drug must be gradually increased, bringing it to 2-3 tablets.
To prevent angina pectoris, take it orally with water before meals. In mild cases - 1-2 tablets of 2.9 mg 2-3 times a day. In more severe cases - 1-2 tablets of 5.2 mg 2-3 times a day. The maximum daily dose is 34.8 mg. Due to the fact that the bioavailability of nitroglycerin from retard tablets is low, it is recommended, if well tolerated, to take 1-3 tablets at a time regularly 3-4 times a day or periodically, 30-40 minutes before the expected physical activity. If the therapeutic effect is insufficient, the dose can be gradually increased (but not more than 2 tablets per dose), and after the onset of a therapeutic effect, it can be reduced.
1% solution for sublingual use: relief of an attack - 1-2 drops sublingually or 2-3 drops applied to a small piece of sugar and keep it in the mouth, without swallowing, until completely absorbed.
Buccal: a plate with a selected dose of nitroglycerin is glued to the oral mucosa, usually in the upper gum area above the canines or small molars. To do this, simply press the plate with your finger against the oral mucosa for a few seconds. The action occurs almost immediately and lasts 3-4 hours or more. To prevent angina attacks, 1 mg films are used for 1-1.5 hours, and 2 mg films are used for 2-3 hours. If it is necessary to increase the flow of nitroglycerin into the blood (including during intense walking, climbing several floors), you should lick the film 2-3 times with your tongue without moving it from its place. If physical activity exceeds the period of resorption of the film, it is necessary to stick a new one on the opposite side of the gum.
Transdermal: treatment begins with the application of one TTC 5 patch (0.2 mg/h) per day. To maintain therapy, the daily dose can be increased by attaching an additional patch (0.2 mg/h) and/or TTC 10 (0.4 mg/h). The maximum daily dose is the application of 2 TTC 10 patches (0.8 mg/hour). For CHF, it is recommended to begin and carry out treatment in a hospital setting until the patient is transferred to the required maintenance dose. The optimal dose should be determined (taking into account the clinical response and possible side effects). In this case, you should strictly monitor the appearance of signs of overdose (decreased blood pressure and tachycardia).
Cutaneously (ointment): the initial dose is 2.5 cm of ointment. If the effect is insufficient, the dose is gradually increased to 5-10 cm. The maximum single dose is 15 cm. The ointment is used 2-3 times a day. The prescribed amount of ointment is squeezed onto the dosing paper scale, the paper is attached tightly to a hairless area of skin (in the area of the upper chest, abdomen, outer thigh).
Aerosol, spray for sublingual use: to relieve an attack of angina - 0.4-0.8 mg (1-2 doses), pressing the dosing valve, preferably in a sitting position, while holding your breath at intervals of 30 seconds; After this, you should close your mouth for a few seconds. If necessary, repeat administration, but not more than 1.2 mg (3 doses) over 15 minutes. To prevent the development of an attack - 0.4 mg (1 dose) 5-10 minutes before exercise. In case of acute LV failure, developing pulmonary edema - 1.6 mg (4 doses) or more in a short period of time (under strict medical supervision).
IV administration of nitroglycerin should be carried out with individual selection of the rate of administration of the drug. The solution is administered through an automatic dispenser or through a conventional IV system. The automatic dispenser allows you to administer even an undiluted 0.1% solution with precise dosing of the rhythm of administration and the total dose. Administration through a conventional fluid transfusion system ensures precise dosage selection by counting the number of drops. When using a polyvinyl chloride tube system, the active substance is absorbed and losses on the tube walls are up to 60% (it is advisable to use polyethylene and glass tubes). The solution quickly degrades in light, so the vials and transfusion system must be shielded with light-proof material.
Typically, an infusion solution with a concentration of 100 mcg/ml is used: the concentrated solution is diluted with 0.9% NaCl solution or 5% dextrose solution (other solvents should not be used). The solution is administered intravenously at an initial rate of 5 mcg/min. The rate of administration can be increased every 3-5 minutes by 5 mcg/min (depending on the effect and response of heart rate, central venous pressure and systolic blood pressure, which can be reduced by 10-25% of the original, but should not be lower than 90 mm Hg .st.). If no therapeutic effect is obtained at an injection rate of 20 mcg/min, a further increase in the injection rate should be 10-20 mcg/min. If a response occurs (in particular, a decrease in blood pressure), a further increase in the infusion rate is not carried out or is carried out at longer intervals.
To achieve a good effect, the rate of administration of a 0.01% nitroglycerin solution usually does not exceed 100 mcg/min (1 ml/min). If there is no effect from lower doses and the blood pressure is acceptable, the rate of administration of a 0.01% solution can reach 300 mcg/min (3 ml/min). Further increase in speed is not advisable.
The duration of treatment is determined by clinical indications and can be 2-3 days.
Nitroglycerin for intravenous administration, if necessary, can be re-administered at any time intervals.
