International name Aspirin (Acetylsalicylic acid)
Group affiliation: NSAIDs
Description of the active substance (INN): acetylsalicylic acid
Release form, composition and packing
Pill, tablet (for children), tablets coated with enteric shell, coated tablets, effervescent tablets
Pharmacological action
NSAID, has anti-inflammatory, analgesic and antipyretic effects associated with non-selective inhibition of activity TSOG1 and TSOG2 regulating the synthesis of Pg. As a result, are not formed Pg, providing formation of edema and giperalgezii. Reduction of Pg (mainly E1) in the center of thermoregulation leads to a reduction in body temperature due to expansion of vessels in the skin and increase perspiration. Analgesic effect is caused by both central and peripheral actions. Reduces the aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiplatelet effect lasts for 7 days after a single dose (more pronounced in males than in females). Reduces the mortality and risk of myocardial infarction in unstable angina.
Effective in the primary prevention of CVD, particularly myocardial infarction in men older than 40 years, and for secondary prevention of myocardial infarction. At a daily dose of 6 g or more inhibits the synthesis of prothrombin in the liver and increases the prothrombin time. Increases the fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Speeds up hemorrhagic complications during surgery, increases the risk of bleeding during therapy with anticoagulants. Stimulates the excretion of uric acid (violating its reabsorption in the renal tubules), but in high doses. TSOG1 blockade in the gastric mucosa leads to inhibition of gastroprotective Pg, which can cause ulceration of the mucous membrane and subsequent bleeding. Less irritating to the mucous membrane of the digestive tract have formulations containing buffering agents, enteric shell, as well as special "sparkling" form of tablets.
Statement
Rheumatism, rheumatoid arthritis, an infectious-allergic myocarditis, pericarditis, rheumatic chorea - currently not used. Febrile syndrome in infectious and inflammatory diseases. Pain syndrome (various origins): headache (including associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, lumbago, thoracic radicular syndrome, myalgia, arthralgia, algomenorrhea. As antiplatelet drugs (doses up to 300 mg / day): CHD, multiple cardiovascular risk factors, silent myocardial ischemia, unstable angina, myocardial infarction (to reduce the risk of another heart attack and death after myocardial infarction), repeated transient cerebral ischemia and ischemic stroke in men, prosthetic heart valves (the prevention and treatment of venous thromboembolism), balloon angioplasty and coronary stent (reducing the risk of re-stenosis and the treatment of secondary stratification of coronary artery), at neateroskleroticheskih lesions of coronary artery disease (Kawasaki), aortoarteriit (Takayasu's disease), valve mitral heart defects and atrial fibrillation, mitral valve prolapse (prevention of thromboembolism), recurrent pulmonary embolism, pulmonary infarction, acute thrombophlebitis, Dressler's syndrome.
In clinical immunology and allergy: a gradually increasing doses for long, "aspirin" desensitization and the formation of stable tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin triad."
Contraindications
Hypersensitivity;
erosive and ulcerative lesions of the gastrointestinal tract (in acute phase), gastrointestinal bleeding;
"Aspirin" triad (a combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS series of pyrazolone);
hemorrhagic diathesis (haemophilia, von Willebrand disease, telangiectasia, gipoprotrombinemiey, thrombocytopenia, thrombocytopenic purpura);
dissecting aortic aneurysm, portal hypertension;
vitamin K;
hepatic / renal failure;
pregnancy (I and III trimester), lactation;
deficiency of glucose-6-phosphate dehydrogenase, children's age (15 years - the risk of Reye's syndrome in children with hyperthermia against viral diseases). C care. Hyperuricemia, urate nefrourolitiaz, gout, liver disease, peptic ulcer and / or 12 duodenal ulcer (history), decompensated heart failure.
Side Effects
Nausea, decreased appetite, stomachodynia, diarrhea, allergic reactions (skin rash, angioedema, bronchospasm), abnormal liver function and / or kidney disease; thrombocytopenia, anemia, leukopenia, Reye syndrome (encephalopathy and acute fatty liver with rapid development of liver failure) , the formation of haptenic-based mechanism "aspirin" asthma and "aspirin triad" (the combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS pyrazolone series). With prolonged use - dizziness, headache, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, hypocoagulation, hemorrhage (including gastrointestinal), visual impairment, hearing loss, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with increasing creatinine in blood and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of heart failure, edema, increased activity of liver transaminases.
Overdose
Symptoms (a single dose of 150 mg / kg - acute poisoning is considered to be an easy 150-300 mg / kg - moderate, more than 300 mg / kg - heavy): salitsilizma syndrome (nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache, malaise, fever - a poor prognostic sign in adults). Severe poisoning - central genesis hyperventilation, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, seizures, anuria, bleeding. Initially, central hyperventilation leads to respiratory alkalosis - shortness of breath, dyspnea, cyanosis, cold clammy sweat, with the strengthening of intoxication increases respiratory paralysis and uncoupling of oxidative phosphorylation, causing respiratory acidosis.
In chronic overdose concentration determined in plasma are poorly correlated with the severity of intoxication. The greatest risk of developing chronic toxicity observed in elderly patients when administered within a few days more than 100 mg / kg / day. In children and elderly patients the initial signs salitsilizma not always visible, so it is expedient to periodically determine the concentration of salicylates in the blood: levels above 70 mg% indicates a moderate or severe poisoning, above 100 mg% - on extremely heavy, poor prognosis.
If poisoning moderate requiring hospitalization for 24 hours Treatment: provocation of vomiting, the appointment of activated charcoal and laxatives, constant monitoring of CBS and electrolyte balance, depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Raising reserve alkalinity increases excretion of ASA by alkalinization of urine. Alkalization of urine is shown at the level of salicylates than 40 mg% and provided intravenous infusion of sodium bicarbonate (88 mEq in 1 liter 5% dextrose solution at a rate of 10-15 ml / hr / kg) recovery BCC and the induction of diuresis is achieved by introducing sodium bicarbonate the same dose and dilution, which was repeated 2-3 times. Use caution in elderly patients who have an intense infusion of fluid can lead to pulmonary edema. Does not recommend the use of acetazolamide for alkalinization of urine (may cause acidemia and enhance toxic effects of salicylates). Hemodialysis is indicated for the level of salicylate over 100-130 mg% in patients with chronic poisoning - 40 mg% or less if indicated (refractory acidosis, progressive deterioration, severe CNS disease, pulmonary edema and renal failure). When pulmonary edema - a mixture of mechanical ventilation, oxygen enriched.
Dosing and Administration
Soluble tablets: inside, previously dissolved in a small amount of water - at 400-800 mg 2-3 times a day (not more than 6 g).
In acute rheumatism - 100 mg / kg / day in 5-6 receptions. Tablets containing ASA at doses above 325 mg (400-500 mg), designed for use as an analgesic and anti-inflammatory drugs, in doses 50-75-100-300-325 mg - in adults, especially as antiplatelet drugs. Inside, with a frenetic and pain for adults - 0.5-1 g / d (up to 3 g) were divided into 3 doses. Duration of treatment should not exceed 2 weeks. Effervescent tablets dissolved in 100-200 ml of water and taken orally after a meal, a single dose - 0.25-1 g, take 3-4 times a day. Duration of treatment - from a single dose of up to many months of the course. To improve the blood rheology - 0.15-0.25 g / day for several months.
Myocardial infarction, as well as for secondary prevention in patients with myocardial infarction - 40-325 mg 1 time a day (usually 160 mg). As an inhibitor of platelet aggregation - 300-325 mg / day for a long time.
At the dynamic cerebral circulatory disorders in men, cerebral embolism - 325 mg / day with gradual increase to a maximum of 1 g / day, for the prevention of relapse - 125-300 mg / day. For the prevention of thrombosis or occlusion of the aortic graft - 325 mg every 7 h after nasal gastric tube set, and then oral - 325 mg 3 times daily (usually in combination with dipyridamole, which overturned in a week, continuing long-term treatment ASA).
With active rheumatoid arthritis administered (currently not assigned) in a daily dose of 8.5 g for adults and 100-125 mg / kg - for teenagers (15-18 years), the multiplicity of applications - 4-5 times a day. After 1-2 weeks of treatment for children, reduce the dose to 60-70 mg / kg / day treatment for adults continue in the same dose, duration of treatment - up to 6 weeks. Cancellation produced gradually over 1-2 weeks.
Cautions
Duration of treatment (without consulting a doctor) must not exceed 7 days when administered as analgesic drugs and more than 3 days as antipyretic. Currently, the use of ASA as an anti-inflammatory drugs in a daily dose of 5-8 g is limited due to the high probability of adverse effects from the gastrointestinal tract (NSAID gastropathy). Before surgery to reduce bleeding during surgery and postoperative period should stop taking salicylates for 5-7 days and notify the physician. During long-term therapy is necessary to carry out blood tests and study fecal occult blood. Children should not be prescribed drugs containing ASA, as in the case of viral infection, they may increase the risk of Reye's syndrome.
Symptoms of Reye's syndrome are persistent vomiting, severe encephalopathy, liver enlargement.
Group affiliation: NSAIDs
Description of the active substance (INN): acetylsalicylic acid
Release form, composition and packing
Pill, tablet (for children), tablets coated with enteric shell, coated tablets, effervescent tablets
Pharmacological action
NSAID, has anti-inflammatory, analgesic and antipyretic effects associated with non-selective inhibition of activity TSOG1 and TSOG2 regulating the synthesis of Pg. As a result, are not formed Pg, providing formation of edema and giperalgezii. Reduction of Pg (mainly E1) in the center of thermoregulation leads to a reduction in body temperature due to expansion of vessels in the skin and increase perspiration. Analgesic effect is caused by both central and peripheral actions. Reduces the aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets. Antiplatelet effect lasts for 7 days after a single dose (more pronounced in males than in females). Reduces the mortality and risk of myocardial infarction in unstable angina.
Effective in the primary prevention of CVD, particularly myocardial infarction in men older than 40 years, and for secondary prevention of myocardial infarction. At a daily dose of 6 g or more inhibits the synthesis of prothrombin in the liver and increases the prothrombin time. Increases the fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). Speeds up hemorrhagic complications during surgery, increases the risk of bleeding during therapy with anticoagulants. Stimulates the excretion of uric acid (violating its reabsorption in the renal tubules), but in high doses. TSOG1 blockade in the gastric mucosa leads to inhibition of gastroprotective Pg, which can cause ulceration of the mucous membrane and subsequent bleeding. Less irritating to the mucous membrane of the digestive tract have formulations containing buffering agents, enteric shell, as well as special "sparkling" form of tablets.
Statement
Rheumatism, rheumatoid arthritis, an infectious-allergic myocarditis, pericarditis, rheumatic chorea - currently not used. Febrile syndrome in infectious and inflammatory diseases. Pain syndrome (various origins): headache (including associated with alcohol withdrawal syndrome), migraine, toothache, neuralgia, lumbago, thoracic radicular syndrome, myalgia, arthralgia, algomenorrhea. As antiplatelet drugs (doses up to 300 mg / day): CHD, multiple cardiovascular risk factors, silent myocardial ischemia, unstable angina, myocardial infarction (to reduce the risk of another heart attack and death after myocardial infarction), repeated transient cerebral ischemia and ischemic stroke in men, prosthetic heart valves (the prevention and treatment of venous thromboembolism), balloon angioplasty and coronary stent (reducing the risk of re-stenosis and the treatment of secondary stratification of coronary artery), at neateroskleroticheskih lesions of coronary artery disease (Kawasaki), aortoarteriit (Takayasu's disease), valve mitral heart defects and atrial fibrillation, mitral valve prolapse (prevention of thromboembolism), recurrent pulmonary embolism, pulmonary infarction, acute thrombophlebitis, Dressler's syndrome.
In clinical immunology and allergy: a gradually increasing doses for long, "aspirin" desensitization and the formation of stable tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin triad."
Contraindications
Hypersensitivity;
erosive and ulcerative lesions of the gastrointestinal tract (in acute phase), gastrointestinal bleeding;
"Aspirin" triad (a combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS series of pyrazolone);
hemorrhagic diathesis (haemophilia, von Willebrand disease, telangiectasia, gipoprotrombinemiey, thrombocytopenia, thrombocytopenic purpura);
dissecting aortic aneurysm, portal hypertension;
vitamin K;
hepatic / renal failure;
pregnancy (I and III trimester), lactation;
deficiency of glucose-6-phosphate dehydrogenase, children's age (15 years - the risk of Reye's syndrome in children with hyperthermia against viral diseases). C care. Hyperuricemia, urate nefrourolitiaz, gout, liver disease, peptic ulcer and / or 12 duodenal ulcer (history), decompensated heart failure.
Side Effects
Nausea, decreased appetite, stomachodynia, diarrhea, allergic reactions (skin rash, angioedema, bronchospasm), abnormal liver function and / or kidney disease; thrombocytopenia, anemia, leukopenia, Reye syndrome (encephalopathy and acute fatty liver with rapid development of liver failure) , the formation of haptenic-based mechanism "aspirin" asthma and "aspirin triad" (the combination of asthma, recurrent polyposis of the nose and paranasal sinuses and the intolerance of ASA and LS pyrazolone series). With prolonged use - dizziness, headache, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, hypocoagulation, hemorrhage (including gastrointestinal), visual impairment, hearing loss, tinnitus, bronchospasm, interstitial nephritis, prerenal azotemia with increasing creatinine in blood and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, aseptic meningitis, increased symptoms of heart failure, edema, increased activity of liver transaminases.
Overdose
Symptoms (a single dose of 150 mg / kg - acute poisoning is considered to be an easy 150-300 mg / kg - moderate, more than 300 mg / kg - heavy): salitsilizma syndrome (nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache, malaise, fever - a poor prognostic sign in adults). Severe poisoning - central genesis hyperventilation, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, seizures, anuria, bleeding. Initially, central hyperventilation leads to respiratory alkalosis - shortness of breath, dyspnea, cyanosis, cold clammy sweat, with the strengthening of intoxication increases respiratory paralysis and uncoupling of oxidative phosphorylation, causing respiratory acidosis.
In chronic overdose concentration determined in plasma are poorly correlated with the severity of intoxication. The greatest risk of developing chronic toxicity observed in elderly patients when administered within a few days more than 100 mg / kg / day. In children and elderly patients the initial signs salitsilizma not always visible, so it is expedient to periodically determine the concentration of salicylates in the blood: levels above 70 mg% indicates a moderate or severe poisoning, above 100 mg% - on extremely heavy, poor prognosis.
If poisoning moderate requiring hospitalization for 24 hours Treatment: provocation of vomiting, the appointment of activated charcoal and laxatives, constant monitoring of CBS and electrolyte balance, depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Raising reserve alkalinity increases excretion of ASA by alkalinization of urine. Alkalization of urine is shown at the level of salicylates than 40 mg% and provided intravenous infusion of sodium bicarbonate (88 mEq in 1 liter 5% dextrose solution at a rate of 10-15 ml / hr / kg) recovery BCC and the induction of diuresis is achieved by introducing sodium bicarbonate the same dose and dilution, which was repeated 2-3 times. Use caution in elderly patients who have an intense infusion of fluid can lead to pulmonary edema. Does not recommend the use of acetazolamide for alkalinization of urine (may cause acidemia and enhance toxic effects of salicylates). Hemodialysis is indicated for the level of salicylate over 100-130 mg% in patients with chronic poisoning - 40 mg% or less if indicated (refractory acidosis, progressive deterioration, severe CNS disease, pulmonary edema and renal failure). When pulmonary edema - a mixture of mechanical ventilation, oxygen enriched.
Dosing and Administration
Soluble tablets: inside, previously dissolved in a small amount of water - at 400-800 mg 2-3 times a day (not more than 6 g).
In acute rheumatism - 100 mg / kg / day in 5-6 receptions. Tablets containing ASA at doses above 325 mg (400-500 mg), designed for use as an analgesic and anti-inflammatory drugs, in doses 50-75-100-300-325 mg - in adults, especially as antiplatelet drugs. Inside, with a frenetic and pain for adults - 0.5-1 g / d (up to 3 g) were divided into 3 doses. Duration of treatment should not exceed 2 weeks. Effervescent tablets dissolved in 100-200 ml of water and taken orally after a meal, a single dose - 0.25-1 g, take 3-4 times a day. Duration of treatment - from a single dose of up to many months of the course. To improve the blood rheology - 0.15-0.25 g / day for several months.
Myocardial infarction, as well as for secondary prevention in patients with myocardial infarction - 40-325 mg 1 time a day (usually 160 mg). As an inhibitor of platelet aggregation - 300-325 mg / day for a long time.
At the dynamic cerebral circulatory disorders in men, cerebral embolism - 325 mg / day with gradual increase to a maximum of 1 g / day, for the prevention of relapse - 125-300 mg / day. For the prevention of thrombosis or occlusion of the aortic graft - 325 mg every 7 h after nasal gastric tube set, and then oral - 325 mg 3 times daily (usually in combination with dipyridamole, which overturned in a week, continuing long-term treatment ASA).
With active rheumatoid arthritis administered (currently not assigned) in a daily dose of 8.5 g for adults and 100-125 mg / kg - for teenagers (15-18 years), the multiplicity of applications - 4-5 times a day. After 1-2 weeks of treatment for children, reduce the dose to 60-70 mg / kg / day treatment for adults continue in the same dose, duration of treatment - up to 6 weeks. Cancellation produced gradually over 1-2 weeks.
Cautions
Duration of treatment (without consulting a doctor) must not exceed 7 days when administered as analgesic drugs and more than 3 days as antipyretic. Currently, the use of ASA as an anti-inflammatory drugs in a daily dose of 5-8 g is limited due to the high probability of adverse effects from the gastrointestinal tract (NSAID gastropathy). Before surgery to reduce bleeding during surgery and postoperative period should stop taking salicylates for 5-7 days and notify the physician. During long-term therapy is necessary to carry out blood tests and study fecal occult blood. Children should not be prescribed drugs containing ASA, as in the case of viral infection, they may increase the risk of Reye's syndrome.
Symptoms of Reye's syndrome are persistent vomiting, severe encephalopathy, liver enlargement.
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