Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Nitroglycerin is a nitrogen-containing compound, a peripheral vasodilator with venodilating and antianginal effects .
The action of nitroglycerin is associated with the ability to release nitric oxide, which affects the endothelium, causing smooth muscle relaxation and vasodilation. As a result, preload (venous return) and afterload (resistance of the systemic vessels) are reduced. The load on the heart is reduced and the need for oxygen is reduced.
The simultaneous expansion of the coronary vessels significantly increases the delivery of oxygen to the heart muscle. A decrease in venous return leads to a decrease in pressure in the pulmonary circle, a decrease in the volume of the left ventricle and eliminates pulmonary edema .
Relaxes the smooth muscles of the gallbladder and ducts, bronchi, urinary tract, and intestines. The effect of the drug begins in 30-60 seconds and lasts from 10 to 30 minutes.
Pharmacokinetics
The aerosol is quickly absorbed from the oral cavity. Bioavailability 100%. Cmax in the blood is determined after 4 minutes. 60% binds to blood proteins. Binds to red blood cells.
Metabolized to form mononitrates and dinitrates. Metabolites are excreted by the kidneys. T1/2 is 2.5–4.5 minutes.
Contraindications
- shock;
- collaptoid states;
- increased sensitivity to nitrates;
- age up to 18 years.
Prescribed with caution for orthostatic hypotension , acute circulatory failure with blood pressure below 90 mm Hg. Art., hypertrophic cardiomyopathy , hemorrhagic stroke , severe renal and liver failure , anemia , epilepsy , acute myocardial infarction with a low degree of filling of the left ventricle, thyrotoxicosis , alcoholism, head injury, angle-closure glaucoma , migraine .
Special instructions for the use of the drug Nitromint
In case of migraine and angle-closure glaucoma, Nitromint aerosol should be used with extreme caution and under medical supervision. During pregnancy, it is necessary to carefully assess the benefit/risk ratio before prescribing the drug. Aerosol Nitromint increases the urinary excretion of catecholamines and vanillylmandelic acid, and also contains ethanol. Its use can be dangerous in case of liver disease, alcoholism, epilepsy, brain injury, central nervous system diseases, and in childhood. Nitromint aerosol should not be used while smoking or near an open flame. When using the aerosol, a temporary burning sensation in the mouth may occur. The use of an aerosol may cause dizziness; this should be borne in mind when driving vehicles and operating machinery, especially at the beginning of treatment. Drinking alcoholic beverages during treatment with Nitromint is strictly prohibited.
Instructions for use of Nitromint (Method and dosage)
The drug is sprayed under the tongue while holding the breath. Before first use, you need to fill the pump by pressing the valve until an aerosol appears. If the cylinder is not used often, the pump needs to be refilled.
When spraying the drug, the container is held vertically, head up. One click on the valve corresponds to 1 dose - 0.4 mg of nitroglycerin . There is no need to shake the container before use.
Aerosol Nitromint, instructions for use
During an attack of angina, the spray is sprayed in an amount of 1–2 doses (0.4–0.8 mg) in a sitting position, at intervals of 30 s. Then you need to close your mouth. Repeated administration - up to 3 doses in 15 minutes.
To prevent an attack, use 1 dose 10 minutes before exercise.
For pulmonary edema and left ventricular failure, use 4 doses or more in a short time, controlling blood pressure (systolic>100 mmHg).
In elderly people, the dosage regimen does not change.
Nitromint sublingual spray dosed 400 µg/dose 180 DOZES 10g
Compound
Active substance: nitroglycerin (in the form of a 1% solution) - 400 mcg. Excipients: ethanol, propylene glycol.
Pharmacokinetics
After oral administration, it is absorbed from the gastrointestinal tract and undergoes a “first pass” effect through the liver. When administered sublingually, this effect is absent, and therapeutic concentrations in the blood plasma are achieved within a few minutes. Metabolized in the liver with the participation of nitrate reductase. Of the nitroglycerin metabolites, dinitro derivatives can cause pronounced vasodilation; perhaps they determine the therapeutic effect of nitroglycerin (glyceryl trinitrate) when taken orally.
Plasma protein binding is 60%. T1/2 after oral administration - 4 hours, with sublingual administration - 20 minutes, after intravenous administration - 1-4 minutes. It is excreted primarily by the kidneys.
Indications for use
- Angina pectoris (relief and prevention of attacks, including before physical activity).
- Acute left ventricular failure (as an auxiliary therapy).
Contraindications
Hypersensitivity to organic nitrates, shock, collapse, age under 18 years (lack of sufficient clinical data).
Carefully:
Acute circulatory failure accompanied by severe arterial hypotension (systolic blood pressure below 90 mm Hg), orthostatic hypotension, hemorrhagic stroke, acute myocardial infarction and chronic heart failure with low left ventricular filling pressure, hypertrophic cardiomyopathy, severe renal and/or liver failure , severe anemia and thyrotoxicosis, alcoholism, epilepsy, traumatic brain injury, intracranial hypertension, angle-closure glaucoma (risk of increased intraocular pressure), migraine.
Directions for use and doses
Sublingual.
Before using the canister for the first time, fill the dosing pump by removing the protective cap and pressing the dosing valve several times until the spray appears. After a long period of not using the cylinder, it may be necessary to refill the pump.
When using, the can should be held vertically with the spray head facing up. Each press of the dosing valve releases one dose (0.4 mg of nitroglycerin) as a spray from a canister equipped with a mechanical pump.
There is no need to shake the container before 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 s; 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 left ventricular failure, developing pulmonary edema - 1.6 mg (4 doses) or more in a short period of time with strict control of the circulatory condition (systolic blood pressure should be above 100 mm Hg). If the therapeutic effect is insufficient, the same dose can be repeated after 10 minutes.
No change in dosage regimen is required when using the drug in elderly patients.
Storage conditions
At a temperature of 15-25°C, in a place protected from light, away from heat sources.
The cylinder is explosive and flammable! It is prohibited to throw an empty cylinder into a fire! It is prohibited to store and use the drug near an open fire or in a smoking area!
Keep the drug out of the reach of children!
Best before date
3 years. Do not use after the expiration date stated on the packaging.
special instructions
Use with caution in patients with severe cerebral atherosclerosis, cerebrovascular accidents, with a tendency to orthostatic hypotension, with severe anemia, in elderly patients, as well as with hypovolemia and severe impairment of liver and kidney function (parenterally).
With prolonged use, tolerance to the effects of nitrates may develop. To prevent the occurrence of tolerance, it is recommended to observe a 10-12 hour break in their use during each 24-hour cycle.
If an attack of angina occurs during cutaneous use of nitroglycerin (glyceryl trinitrate), it should be stopped by taking glyceryl trinitrate under the tongue.
During the treatment period, avoid drinking alcohol.
Description
Peripheral vasodilator. Antianginal drug.
Dosage form
Sublingual spray dosed in the form of a colorless or almost colorless transparent solution without sediment.
Use in children
Contraindicated under the age of 18 years (lack of sufficient clinical data).
Pharmacodynamics
Peripheral vasodilator with a predominant effect on venous vessels. Antianginal agent. The mechanism of action is associated with the release of the active substance nitric oxide in the smooth muscles of blood vessels. Nitric oxide causes activation of guanylate cyclase and increases cGMP levels, which ultimately leads to smooth muscle relaxation. Under the influence of glyceryl trinitrate, arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. This is partly due to reflex reactions, as well as the less intense formation of nitric oxide from active substance molecules in the walls of arterioles.
The effect of nitroglycerin (glyceryl trinitrate) is mainly associated with a decrease in myocardial oxygen demand due to a decrease in preload (dilation of peripheral veins and a decrease in blood flow to the right atrium) and afterload (decreased OPSS). Promotes the redistribution of coronary blood flow into ischemic subendocardial areas of the myocardium. Increases exercise tolerance in patients with coronary artery disease and angina pectoris. In heart failure, it helps to unload the myocardium mainly by reducing preload. Reduces pressure in the pulmonary circulation.
Side effects
From the cardiovascular system: dizziness, headache, tachycardia, skin hyperemia, feeling of heat, arterial hypotension; rarely (especially with overdose) - collapse, cyanosis.
From the digestive system: nausea, vomiting.
From the side of the central nervous system: rarely (especially in case of overdose) - anxiety, psychotic reactions.
Allergic reactions: rarely - skin rash, itching.
Local reactions: mild itching, burning, redness of the skin.
Other: methemoglobinemia.
Use during pregnancy and breastfeeding
The excretion of nitroglycerin into breast milk has not been established.
The use of Nitromint® during pregnancy and breastfeeding requires careful comparison of risks and benefits and should be carried out under strict medical supervision.
Interaction
- When used simultaneously with vasodilators, ACE inhibitors, calcium channel blockers, beta-blockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol, ethanol-containing drugs, the hypotensive effect of glyceryl trinitrate may be enhanced.
- When used simultaneously with beta-blockers and calcium channel blockers, the antianginal effect is enhanced.
- When used simultaneously with sympathomimetics, it is possible to reduce the antianginal effect of glyceryl trinitrate, which, in turn, can reduce the pressor effect of sympathomimetics (as a result, arterial hypotension is possible).
- With the simultaneous use of drugs with anticholinergic activity (including tricyclic antidepressants, disopyramide), hyposalivation and dry mouth develop.
- There is limited evidence that acetylsalicylic acid, used as an analgesic, increases the concentration of nitroglycerin (glyceryl trinitrate) in the blood plasma. This may be accompanied by increased hypotensive effect and headaches.
- A number of studies have observed a decrease in the vasodilating effect of nitroglycerin (glyceryl trinitrate) during long-term therapy with acetylsalicylic acid.
- It is believed that it is possible to enhance the antiplatelet effect of acetylsalicylic acid with the use of nitroglycerin (glyceryl trinitrate).
- When used simultaneously with nitroglycerin, the effect of acetylcholine, histamine, and norepinephrine decreases.
- Against the background of intravenous administration of nitroglycerin, the anticoagulant effect of heparin may be reduced.
- With simultaneous use, it is possible to increase the bioavailability of dihydroergotamine and reduce the antianginal effect of nitroglycerin (glyceryl trinitrate).
- When used simultaneously with novocainamide, the hypotensive effect and the development of collapse may be enhanced.
- When used simultaneously with rizatriptan, sumatriptan, the risk of developing coronary artery spasm increases; with sildenafil - the risk of developing severe arterial hypotension and myocardial infarction; with quinidine - orthostatic collapse is possible; with ethanol - severe weakness and dizziness.
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 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 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 orally 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).
Impact on the ability to drive vehicles and operate machinery
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.
Overdose
Overdose is manifested by symptoms: orthostatic hypotension , headache, sharp decrease in blood pressure, tachycardia , dizziness, vomiting, drowsiness, facial flushing, feeling of heat.
When taking high doses (20 mg/kg or more), methemoglobinemia , dyspnea , cyanosis , and collapse . Treatment: lay the patient down, placing the legs in an elevated position. In severe cases - administration of norepinephrine , replenishment of blood volume. Epinephrine is contraindicated.
Drug interactions Nitromint
Nitromint should be used with caution in combination with:
- antihypertensive drugs: β-adrenergic receptor blockers, calcium channel blockers - may increase the antihypertensive effect;
- tranquilizers (chlordiazepoxide, trimethocin, tofisopam) - may increase the antihypertensive effect;
- tricyclic antidepressants such as imipramine - may increase the antihypertensive effect;
- diuretics - the risk of developing hypotension;
- heparin - decreased effect of heparin;
- dihydroergotamine (the effect of dihydroergotamine increases).
It is not recommended to prescribe Nitromint in combination with sildenafil - there is a risk of developing hypotension. For patients who have previously used nitrates (isosorbide dinitrate, isosorbide mononitrate), Nitromint aerosol is prescribed in high doses (reduced effect of nitroglycerin due to binding to nitrates).
Interaction
Vasodilators , ACE inhibitors , beta-blockers , CCBs , antipsychotics , antidepressants , MAO inhibitors , Procainamide and phosphodiesterase inhibitors enhance the hypotensive effect of the drug.
Simultaneous administration of ACC and ethanol enhances the vasodilating effect.
Nitromint enhances the effect of the antiadrenergic drug Dihydroergotamine and reduces the effects of Heparin .
Analogs
Level 4 ATC code matches:
Nitrospray
Nitroglycerine
Efox
Monosan
Pectrol
Isoket
Erinite
Cardiket
Sustak Forte
Nitrosorbide
nitroglycerin preparations in tablets (regular and extended-release), in the form of spray, aerosol, ointment, transdermal patches and films for gluing to the gums: Nitroglycerin , Sustak , Sustonit , Nitrong , Nitroderm , Gluconit , Deponit 10 , Nitrocor , Nirmin , Nit-ret , Perlinganite , Trinitrolong, Nitradisk , Nitrospray-ICN , Nitrospray , Nitro , Nitrosprint .
Analogues and substitutes: what can you take instead?
Nitromint is a high-quality, fast-acting drug due to its release form in the form of a spray or aerosol. But sometimes it is not available in the pharmacy. If there is an urgent need to purchase some nitroglycerin, you can choose one of the Nitromint analogues:
Nitroglycerin - can be purchased in tablets or in aerosol form (Nitroglycerin-Aerosol);- Sustak – tablets with prolonged action (1 tablet – 6.4 mg of nitroglycerin);
- Nitrospray, Nitrospray-ICN, Nitrosprint - sublingual dosed sprays (1 injection dose - 0.4 mg of nitroglycerin);
- Nitro concentrate for intravenous infusion (in ampoules of 2 and 5 ml), prescribed only by a doctor in a hospital setting.
Reviews
Nitroglycerin in tablet form may not give the desired effect in a critical situation. When compared with sublingual tablets, the use of an aerosol is more effective - the onset of action is accelerated, the antianginal effect is more pronounced and the duration of an angina . In this connection, the drug in this release form is suitable for providing “first aid”. A number of patients prefer the aerosol form due to its ease of use.
There are negative reviews that are associated with the presence of adverse reactions. Nitromint spray, like all nitrates , causes a pulsating headache that lasts from 15 minutes to several hours in some patients. In elderly patients it is accompanied by dizziness. The occurrence of headache is noted after the first doses of the drug. It is more often observed when using long-acting drugs.
In order to reduce this side effect, it is recommended to use drugs with menthol (for example, Validol ) or NSAIDs ( Acetylsalicylic acid , Paracetamol ) together. Side effects such as heartburn , nausea and vomiting are much less common.
Nitromint price, where to buy
You can buy it in many pharmacies in Moscow and other cities.
The price of Nitromint spray 10 g (180 doses) ranges from 149 rubles. up to 170 rub.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Nitromint spray sublingual.
dosage 0.4 mg/dose 180 doses cylinder 10g ZAO Pharmaceutical Plant EGIS RUB 147 order
Pharmacy Dialogue
- Nitromint (aerial 180 doses) Egis
RUB 144 order
- Nitromint spray 180 dosesEgis
RUB 144 order
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Pharmacy24
- Nitromint 0.4 mg/dose 10 g aerosol ZAT FZ EGIS/VAT Pharmaceutical plant EGIS, Ugorshchina/Ugorshchina
99 UAH.order
PaniPharmacy
- Nitromint aerosol Nitromint aer. 1% 10g Hungary, Egis
132 UAH order
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Overdose of the drug Nitromint, symptoms and treatment
Symptoms: headache, severe arterial hypotension, tachycardia, dizziness, hot flashes, vomiting, diarrhea, methemoglobinemia. In case of excessive overdose, cyanosis, dyspnea and tachypnea and changes in blood counts (methemoglobinemia) may occur. Treatment: for collapse, intravenous infusion of 0.9% sodium chloride solution, norepinephrine and/or dopamine is indicated. For methemoglobinemia:
- intravenous administration of methylene blue (maximum 50 ml of 1% solution); ascorbic acid intravenously - 1 g in the form of a solution of sodium salt of ascorbic acid or in the form of tablets - 1 g orally;
- toluidine blue at an initial dose of 2–4 mg/kg body weight intravenously, then 2 mg/kg again;
- oxygen therapy, hemodialysis, blood transfusion, blood transfusion.