Acetylsalicylic acid (When ATH N02BA01)

When ATH:
N02BA01

Characteristic.

White small needle-like crystals or light crystalline powder, odorless or with a faint odor, slightly acidic taste. It is soluble in water at room temperature, soluble in hot water, slightly soluble in ethanol, caustic solutions and carbon alkalis.

Pharmacological action.
Analgesic, pyretic, anti-inflammatory, antiagregatine.

Application.

CHD, the presence of several risk factors for coronary artery disease, silent myocardial ischemia, unstable angina, myocardial infarction (to reduce the risk of myocardial reinfarction and death after myocardial infarction), repeated transient cerebral ischemia and ischemic stroke in men, prosthetic heart valves (prevention and treatment of venous thromboembolism), ballonnaя koronarnaя angioplasty and stent installation (reducing the risk of restenosis and treatment of secondary stratification of coronary artery), as well as coronary artery neateroskleroticheskih (Kawasaki disease), aortoarteriit (Takayasu's disease), mitral valvular heart disease and atrial fibrillation, mitral valve prolapse (thromboembolism prophylaxis), recurrent pulmonary embolism, Dressler's syndrome, pulmonary infarction, acute thrombophlebitis. Fever in infectious and inflammatory diseases. Pain syndrome weak and average intensity of various origins, incl. thoracic radicular syndrome, lyumbago, migraine, headache, neuralgia, toothache, myalgia, arthralgia, algomenorrhea. In clinical immunology and allergy using a gradually increasing doses for a prolonged "aspirin" desensitization and the formation of persistent tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin" triad.

According to the testimony rheumatism, rheumatic chorea, rheumatoid arthritis, infectious-allergic myocarditis, Pericarditis is being applied very rarely.

Contraindications.

Hypersensitivity, incl. "Aspirinovaâ" triad, «Aspirinovaya» asthma; gyemorragichyeskii diatyez (hemophilia, von Willebrand disease, teleangioэktaziya), rasslaivaющaя aneurysm aortы, heart failure, acute and recurrent erosive and ulcerative diseases of the gastrointestinal tract, gastrointestinal bleeding, acute renal or hepatic failure, original gipoprotrombinemii, vitamin K deficiency, thrombocytopenia, tromboticheskaya trombotsitopenicheskaya purpura, deficiency of glucose-6-fosfatdegidrogenazы, pregnancy (I and III trimester), breast-feeding, childhood and adolescence up 15 years when used as antipyretic (the risk of Reye's syndrome in children with fever against the background of viral diseases).

Restrictions apply.

Hyperuricemia, nephrolithiasis, gout, gastric ulcer and duodenal ulcer (history), severe liver and kidney, bronchial asthma, COPD, nasal polyposis, uncontrolled hypertension.

Pregnancy and breast-feeding.

The use of high doses of salicylates in the I trimester of pregnancy is associated with increased incidence of fetal malformations (cleft palate, heart disease). In the II trimester salicylates can be given only with the evaluation of risks and benefits. Appointment of salicylates in the III trimester of pregnancy is contraindicated.

Salicylates and metabolites thereof in small amounts into breast milk. Accidental intake of salicylates during lactation is not accompanied by the development of adverse reactions in the child and does not require stopping breastfeeding. However, long-term use or administered high doses discontinue breastfeeding.

Side effects.

Cardio-vascular system and blood (hematopoiesis, hemostasis): thrombocytopenia, anemia, leukopenia.

From the digestive tract: NSAID-gastropathy (dyspepsia, epigastric pain, heartburn, nausea and vomiting, severe bleeding in the digestive tract), decreased appetite.

Allergic reactions: hypersensitivity reactions (bronchospasm, laryngeal edema and urticaria), based on the formation of hapten mechanism "aspirin" asthma and "aspirin" triad (eosinophilic rhinitis, recurrent nasal polyposis, gipyerplastichyeskii sinusitis).

Other: liver dysfunction and / or kidney, Reye's syndrome in children (encephalopathy and acute fatty liver with the rapid development of liver failure).

In the long-term use-Vertigo, headache, noise in ears, hearing loss, blurred vision, interstitial nephritis, Pre-renal azotemia, with higher levels of blood creatinine and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, blood disease, aseptic meningitis, increased symptoms of congestive heart failure, swelling, increase in aminotransferase levels in the blood.

Cooperation.

It increases the toxicity of methotrexate, reducing its renal clearance, effects of narcotic analgesics (Oxycodone, propoksyfen, codeine), oral antidiabetic drugs, geparina, anticoagulants, thrombolysis and platelet aggregation inhibitors, reduces the effect of urikozuricheskih HP (ʙenzʙromaron, sulfinpirazon), antihypertensives, diuretics (spironolactone, furosemid). Phenacetin, antihistamines, paracetamol, Caffeine increases the risk of side effects. Glucocorticoids, ethanol etanolsoderzhaschie drugs increase the negative impact on the gastrointestinal mucosa and increase clearance. Increases concentration of digoxin, ʙarʙituratov, lithium salts in plasma. Antacids, containing magnesium and / or aluminum, slow down and reduce absorption of acetylsalicylic acid. Myelotoxic drugs increase the expression gematotoksichnosti acetylsalicylic acid.

Overdose.

It may occur after a single dose or high-dose long-term use. If a single dose of less than 150 mg / kg, Acute poisoning is considered easy, 150-300 mg/kg — moderate, When using higher doses — heavy.

Symptoms: syndrome salitsilizma (nausea, vomiting, noise in ears, blurred vision, dizziness, Strong headache, general malaise, fever is a bad prognostic sign in adults). More severe poisoning — stupor, convulsions and coma, non-cardiogenic pulmonary edema, sharp dehydration, KHS violation (first is a respiratory alkalosis, then metabolic acidosis), renal failure and shock.

In chronic overdose concentration, determined in plasma, poorly correlated with the degree of severity of intoxication. The greatest risk of developing chronic intoxication indicated the elderly when taken within a few days more 100 mg / kg / day. Children and elderly patients initial symptoms are not always visible salitsilizma, therefore it is advisable to periodically determine the concentration of salicylates in the blood. Higher level 70 mg% indicates moderate or severe poisoning; higher 100 mg% — extremely difficult, prognostically unfavorable. Moderate poisoning requires hospitalization for at least 24 no.

Treatment: provocation of vomiting, the appointment of activated charcoal and laxatives, monitoring of acid-base balance and electrolyte balance; Depending on the State of metabolism — the introduction of sodium bicarbonate, sodium citrate or sodium lactate. Increased reserve alkalinity increases the excretion of acetylsalicylic acid by alkalinization of urine. Alkalization of urine salicylate levels shown in the above 40 mg%, is provided in/in infuziei sodium bicarbonate — 88 mEq in 1 l 5% glucose solution, at speeds of 10-15 mL/kg/h. Restore BCC and induction of diuresis (achieved by introducing hydrogen at the same dose and dilution, repeated 2-3 times); it should be understood, that intensive infusion fluid elderly patients may lead to pulmonary edema. We do not recommend the use of acetazolamide for urine alkalinization (It can cause acidemia and enhance the toxic effect of salicylates). Hemodialysis is shown at the level of salicylates a 100-130 mg%, and in patients with chronic poisoning — 40 mg% or less when indicated (refractory acidosis, progressive deterioration, severe CNS, pulmonary edema and renal failure). In oteke light-IVL mixture, oxygenated, Mode positive end-expiratory pressure; for the treatment of cerebral edema used hyperventilation and osmotic diuresis.

Dosing and Administration.

Inside, dosing regimen depends on indication for use. The usual dose for adults when used as antipyretic and pain means, 500-1000 mg/day (to 3 g), divided by 3 admission.

Myocardial infarction, and for secondary prevention in patients, myocardial infarction — 40-325 mg 1 once a day (more 160 mg). As a platelet aggregation inhibitor — in a dose of 300-325 mg/day, protractedly. At the dynamic circulatory disorders in men, cerebral tromboemboliah, incl. to prevent the recurrence of — 325 mg/day, with a gradual increase to a maximum of 1 g / day. For the prevention of thrombosis or occlusion of aortic shunt is on 325 mg every 7 h through intranasal installed gavage, then through the mouth to 325 mg 3 once a day (usually in combination with dipyridamole, which overturned in a 1 Sun, continued long-term treatment with acetylsalicylic acid).

Precautions.

Undesirable concomitant use with other NSAIDs and glucocorticoids. For 5-7 days before surgery is necessary to cancel an appointment (to reduce bleeding during surgery and postoperatively).

The likelihood of developing NSAID-gastropathy reduced by appointment after eating, the use of tablets with buffer additives or coated with a special enteric coating. The risk of bleeding complications is considered when applying the lowest doses <100 mg / day.

It should be taken into account, that predisposed patients aspirin (even in small doses) It reduces the excretion of uric acid from the body and can cause the development of an acute attack of gout.

During long-term therapy is recommended to regularly examine the blood and stool for occult blood. In this regard, there are cases of encephalopathy gepatogennoy not recommended for the relief of feverish syndrome in children.

Cooperation