Description
Release form
Capsules.
Packaging
40 pcs.
Pharmacological action
Nitroglycerin is a venodilating agent from the group of nitrates. Nitrates are able to release nitric oxide from their molecule, which is a natural endothelial relaxing factor – a mediator of direct activation of guanylate cyclase. An increase in the concentration of cGMP leads to relaxation of smooth muscle fibers, mainly venules and veins. It has an antianginal and antispasmodic effect, relaxes the smooth muscles of the vascular walls, bronchi, gastrointestinal tract, bile ducts, and ureters. With intravenous (iv) administration, it has a rapid decrease in preload on the heart due to the expansion of peripheral veins.
Reduces blood flow to the right atrium, helps to reduce pressure in the pulmonary circulation and regress symptoms of pulmonary edema, reduces afterload, oxygen demand of the myocardium (by reducing preload, afterload and tension of the ventricle walls due to a decrease in heart volume). Promotes redistribution of coronary blood flow in the area with reduced blood circulation.
It has a central inhibitory effect on the sympathetic tone of blood vessels, inhibiting the vascular component of the formation of pain. It causes the expansion of meningeal vessels, which explains the headache during its use.
Pharmacokinetics
Getting into the systemic circulation, 60% is bound by plasma proteins. Highly lipophilic, has a large distribution volume (3.3-1.2 l / kg). It is rapidly metabolized in the liver by glutathione reductase, which acts on organic nitrates, with the formation of di- and mononitrates, the final metabolite is glycerin. It is excreted by the kidneys in the form of metabolites. The total clearance is 30-78 l / min, the half-life is 1-3 minutes. In addition, nitroglycerin is metabolized in red blood cells by enzymatic reactions that occur with the participation of sulfhydryl radicals, as well as with interaction with reduced hemoglobin.
Indications
Acute myocardial infarction (including complicated by acute left ventricular failure) unstable angina, pulmonary edema, relief of angina attacks.
Contraindications
hypersensitivity to nitrates
cranial hypertension
cardiac tamponade
isolated mitral stenosis
constrictive pericarditis (conditions, accompanied by a decrease in left ventricular filling pressure)
uncontrolled hypovolemia
heart failure with normal or low pressure in the pulmonary artery
collapse
hemorrhagic stroke
subarachnoid hemorrhage
recently suffered head trauma hypertrophic pulmonary arthritis pressure
severe anemia
hyperthyroidism
age up to 18 years (safety of use not found)
cerebrovascular accident
shock
arterial hypotension (sardlkp SBP concurrent use of sildenafil (Viagra)
pregnancy
breastfeeding period
Caution (comparing risk and benefit): severe renal failure, liver failure (risk of methemoglobinemia).
Pregnancy and lactation
Information not described.
Special instructions
While taking nitroglycerin, a significant decrease in blood pressure and dizziness may occur with a sharp transition to the upright position from the ² Ñlying ² Ñ or ² Ñsitting ² Ñ position, while drinking alcohol, performing physical exercises and hot weather. With frequent use, nitroglycerin, like all organic nitrates, is addictive, and a dose increase is required.
When driving vehicles and controlling mechanisms that require increased attention, it should be borne in mind that taking nitroglycerin can lead to a decrease in the speed of motor and mental reactions.
The severity of headache while taking nitroglycerin can be reduced by reducing its dose and / or by taking validol.
Composition
Active ingredient: nitroglycerin 0.5 mg.
Dosage and Administration
Sublingual.
Nitroglycerin is recommended for medical use.
A tablet (capsule) is kept under the tongue until it is completely absorbed, without swallowing, immediately after the onset of pain – 0.5 1 mg per dose. In many patients with stable angina pectoris, the effect also occurs from a lower dose (1/2 to 1/3 tablets), therefore, if the pain goes away quickly, it is recommended to spit out the rest of the tablet that does not have time to resolve. Typically, an antianginal effect is evident after 0.5 2 minutes, 75% of patients report improvement within the first 3 minutes, and another 15% within 4 5 minutes. In the absence of antianginal action, during the first 5 minutes you need to take another 1 tablet (capsule). nitroglycerin. In the absence of a therapeutic effect after taking 2-3 tablets (capsules), you should immediately call a doctor. The duration of action after sublingual administration is about 45 minutes. With frequent attacks of angina pectoris, it is customary to prescribe prolonged nitroglycerin preparations. Tolerance to sublingual forms of nitroglycerin develops infrequently, however, when it occurs in some patients, the dose of the drug must be gradually increased, bringing it to 2-3 tablets (capsules).
Side effects of the
From the cardiovascular system: dizziness, “nitrate” headache, tachycardia, skin hyperemia, fever, palpitations, decreased blood pressure, rarely (especially with an overdose) – orthostatic collapse, cyanosis.
From the gastrointestinal tract: dry mouth, nausea, vomiting, abdominal pain.
From the central nervous system: rarely (especially with an overdose) – anxiety, psychotic reactions, lethargy, disorientation.
Allergic reactions: rarely – skin rash, itching.
Local reactions: flushing of the skin, itching of the skin, burning, allergic contact dermatitis.
Other: blurred vision, weakness, hypothermia, methemoglobinemia.
Drug interaction
Simultaneous administration with vasodilators, antihypertensive agents, angiotensin converting enzyme inhibitors (ACEs), beta-adrenergic blockers, slow calcium channel blockers, procainamide, tricyclic antidepressant inhibitors, antioxidant inhibitors, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, antioxidants, and others. hypotensive effect.
Prescribing with dihydroergotamine can lead to an increase in its content in the blood and lead to an increase in blood pressure (increased bioavailability of dihydroergotamine).
The simultaneous administration of nitroglycerin and heparin reduces the effectiveness of the latter (after discontinuation of the drug, a significant decrease in blood coagulability is possible, which may require a reduction in the dose of heparin).
Overdose
Symptoms: severe BP (below 90 mmHg) with orthostatic dysregulation, reflex tachycardia, headache, may develop asthenia, dizziness, increased drowsiness, feeling hot, nausea, vomiting, more nausea 20 mg / kg) – collapse, cyanosis, methemoglobinemia, dyspnoea and tachypnoea.
Treatment: discontinue further administration. The headboard of the bed should be lowered and the patient’s feet should be raised. As a rule, The blood pressure is normalized within 15-20 minutes after discontinuation of nitroglycerin, then it is possible to continue the introduction, after a resumption of infusion rate.
Storage conditions
In a protected from light and out of reach of children, away from fire, at a temperature from 5 ° C to 25 ° C .
Shelf life
3 years.
Deystvuyushtee substance
nitroglycerin
drugstore conditions
drugstore
dosage form
capsules
Indications
Indications
Angina pectoris, Prevention of acute myocardial infarction rda
Lumi, Russia
