Acetylsalicylic acid

Chemical name

2-(Ацетилокси)бензойна я acid

Gross

C9-H8-O4

Characteristics

White smaller needle crystals or easy crystalline powder, little is soluble in water at room temperature, soluble in hot water, easily soluble in alcohol, caustic solutions and hydrogen industry.

Of drugs

The drugs-analgezirutee, analgesic, anti-inflammatory, antiagregatine. Ingibiruet ziklooksigenzu and irreversibly inhibits ziklooksigenazny way metabolism arahidonova acid synthesis blocks NG (PGA_2, PGUD_2, Pgf_2alfa, PGE_2, etc.) and tromboksana. Decreases hyperemia, exudation, capillary permeability, activity gialuronidasy limited power to the inflammatory process by oppression of ATF. Affects podcorkove points thermal and pain sensitivity. Impact algogennoe bradikinina effect. Decreasing Thv2 in platelets leads to the suppression of irreversible aggregation increases receptacles. Significant inhibition skleivaemosti blood gills achieved at doses up to 30 mg. Increases fibrinoliticescuu plasma activity and reduces the concentration of vitamin K-zawisimah factors out (II, VII, IX, X). Does the withdrawal of uric acid because it violated reabsorbece in bone Pocek.posle intake of adequately absorbed. During the removals are presistemna off in the bowel wall and in the liver (deacetiliruetsa). Rezorbirovannaya part very quickly hydrolyses special esterazami, T_1/2 it is not more than 15-20 min. Inside the circuit (at 75-90% due to albuminom), and distributed in the tissues of anion salicylic acid. C_max achieved in 2 hours Serum levels salicilatov very variabelen. C blood plasma proteins acetylsalicylic acid virtually no contact. The newborn babies may salicilata Bilirubin out of the albuminom and promote bilirubinova encephalopathy. Salicilata easily penetrate into many tissues and body fluids, including in sinovialnuu, cerebrospinal, peritonealnuu fluid sinoviale casing. Diffusion in the joint cavity accelerated if giperemia and oedema, and slow in coagulation phase inflammation. In small quantities salicilata found in the brain tissue, traces in bile, sweat, faeces. If azidoza most salicilata becoming neionizirovannuu acid is diffuse in the tissue, including in the brain. Quickly pass through the placenta, in small quantities derived from breast milk. Biotransformation salicilatov occurs predominantly in the liver with the formation of four major metabolites found in many tissues and urine. Excretion salicilatov largely by active glands in the kidneys bone in the form of constant (60%) and in the form of metabolites. Return unchanged salicilata depends on the pH of urine (the urine podschelacivanii increasing ionizirovanie salicilatov degraded their reabsorbece and significantly increased excretion). Speed excretion depends on the dose, with the admission of small doses T_1/2 2-3 h, and the increase rate may increase to 15-30 hours The newborn off salicilatov is much slower than that of взрослых.Противовосп��лительный effect of acetylsalicylic acid occurs in 1-2 days reception (with the creation in the tissues of therapeutic salicilatov level, which is 150 µ g / ml), reaches its maximum concentration in 20 to 30 mg%, and a whole period of application. Acute inflammation completely destroyed in a few days, and chronic effects during growing for a longer time and is not always complete. Antiagregatine Effects (kept for a period of 7 days after a single admission) more for men than for women. When treating acute myocardial infarction optimal dose is 160 mg. Reduces rate and the risk of myocardial infarction during a lightning strokes. Effective in the primary prevention of cardiovascular diseases, particularly heart attacks in men older than 40 years, and secondary prevention of myocardial infarction. The daily dose of 900 mg and higher reduced frequency of ischaemic stroke, and mortality from, the frequency of recurrence of the brain

Indications

Disease, the existence of multiple risk factors disease, bezbolevaya myocardial ischaemia, unstable stenocardia, myocardial infarction (to reduce the risk of repeat heart attack and death after myocardial infarction), repeat tricky brain ischaemia and ischemic stroke among men, prosthetic heart valves (prevention and treatment tromboamboliy) koronarnaya balloon angioplasty and installation stenta (reducing the risk of re-stenosis and secondary treatment stratification of coronary artery), and the �еатеросклеротически�� lesion coronary arteries (Kawasaki disease), aortoarteriit (Takayasu disease), valve defects mitrale hearts and mertzatelnaya Already, prolapse mitral valve (prevention embolism), retidivirute pulmonary embolism artery pericardit, Dressler syndrome, rheumatism, trochaic Medicine, rheumatoid arthritis, progressive systemic sclerosis, �нфекционно-аллергиче ский myocarditis, fever and �нфекционно-воспалите льных diseases, pulmonary infarction, acute throm, koreshkovy chest syndrome, lumbago, migraines, headache, nevralgia, other pain syndromes low and moderate intensity. The Clinical Immunology and Allergology used in incremental doses for a prolonged "aspirinova" desencitization and a strong tolerance to NPVS in patients with aspirinova "asthma and" aspirinova "triad.

Contraindications

Hypersensitivity, incl. "aspirinova" triad, "aspirinova" asthma; diateza hemorrhagic (hemophilia, a disease Villebranda, teleangioektasia) rasslaivataya anevrizma arteries, heart failure, acute and retidivirute erosivno-azwenne tract disease, severe violations of the liver and kidney failure, severe kidney or liver failure, giperuriquemia, stone with a reference gipoprotrombinemia deficit vitamin C, B19, trombotical trombozitopenica purpura, pregnancy (I term) Breastfeeding (at the end of treatment), childhood and adolescence (before age 14).

Side-Effects

Noise in the ears, dizziness, hearing impairment, Npvs-gastropatia (neuralgia, pain in epigastralna area, heartburn, nausea and vomiting, severe bleeding in the digestive tract), thrombocytopenia, anemia, lakopenia, Rayee syndrome, the reactions гиперчувствительност и (bronhospazm, throat swelling and urticaria), the formation on the basis of gaptenovogo mechanism aspirinova "bronchial asthma and aspirinova Triad (eozinofilny rhinitis, recurrent nasal polyposis, giperplasticskie sinusita); in the long-term use : intersticialny jade, prerenalnaya azotemia with higher levels of blood creatinine and gipercalziemiei, finger necrosis, acute renal failure, principally syndrome, diseases of the blood, aseptic meningitis, increased symptoms of congestive heart failure and edema, raising aminotransferaz in blood.

Patient interaction

Do methotrexate toxicity, the effects of narcotic analgesics (oxicodona, propoksifena, codeine), protivodiabeticakih oral drugs heparin, anti proximity, and trombolitikov aggregation inhibitors platelets reduces - gipotenziveh funds. Phenacetin, antihistamines means acetaminophen, caffeine increases the risk of side effects, glukokortikoida-negative effect on the mucous membrane of blood and increased Cl.

Overdosing

Or it might be the one receiving a dose or long-term use. If a single dose of less than 150 mg / kg, acute poisoning is easy 150-300 mg / kg, moderate and heavy, with the use of higher Doz.simptoma : salicilizma syndrome (nausea, vomiting, noise in the ears, a general malaise, fever, a bad prognostic sign in adults). More heavy-poisoning stalemate, convulsions and coma, necardiogenny healthy lungs, severe dehydration, violations KHS (initially respiratory alkaloz, then metabolic acidosis), kidney failure and shock. The greatest risk of chronic intoxication noted in the elderly in recruitment in the next few days, more than 100 mg / kg / day for children and patients older elementary salicilizma signs are not always visible, so it is useful to determine the time salicilatov concentration in the blood. Figures above 70 mg / testifies to the moderate to severe poisoning; Above 100 mg% of the extremely grave, prognosticeski disadvantaged. When poisoning moderate require hospitalization for at least 24 C.lechenie : provocation vomiting, the appointment of activated charcoal and laxatives, oschelacivanie urine (show salicilatov level above 40 mg%, the in / in infuziei gidrocarbonata sodium-88 mekw in 1 L 5% glucose solution, with a speed of 10 to 15 ml / kg / h) BCC restoration and induction diureza (achieved by gidrocarbonata in the same dose and breeding repeat 2-3 times); it should be borne in mind that intensive cefuroxim older fluid could lead to 61 lungs. They are generally not recommended for azetozolamida oschelacivania urine (may cause azidemiu and strengthen toxic effect salicilatov). Haemodialysis shown in the more salicilatov 100-130 mg%, and in patients with chronic poisoning-40 mg% and less subject to the availability of evidence (refrakterny acidosis, progressive deterioration of, the heavy defeat CNS, black lungs and kidney failure). In oteke light-IVL mixture enriched oxygen, in a positive pressure at the end of expiration; For the treatment of brain oedema apply giperventilatia and osmoticeski diurez.

Precautions

During 5-7 days before surgery to remove admission (to minimize bleeding during the operation and aftercare period). Irritation at the lower gastrointestinal function after eating, the use of pills buffer additives or covered with a special kishechnorastvorima sheathing. During long-term therapy the best approach is to analyse blood and fluid into the hidden blood. In connection with the incidents occurring gepatogenna encephalopathy is not recommended for short-panic syndrome in children.

Dosing and Administration

Inside, 500-1000 mg / day (up to 3 g), could be used three times a day; Children 2-3 years, 100 mg / day, 4-6 years, 200 mg / day, 7-9 years, 300 mg / day, over 12 years, 250 mg twice a day, daily intake of not more than 750 Mg.pri myocardial infarct, and for secondary prevention in patients after myocardial infarction - 40-325 mg once a day (more often 160 mg). As an aggregation inhibitor platelets, in a daily dose of 325 mg, Dleytelno.pri dynamic human circulatory men tromboemboliah brain, including for the prevention of relapse-325 mg / day, with a steady increase up to 1000 mg / Sut.dla thrombosis prophylaxis or occluzii 34b88 aortalni shunt on the 325 mg every 6 hours, through the route jeludochny probe, and then, through the mouth to 325 mg three times a day (usually in combination with dipiridamolom, lifted after one week, while long-term care insurance acetylsalicylic acid). Answers to the slow release (325 mg) Designate in the same doses, as a standard pill.

Literature

1. M. Ridker, Manson J.A.E., Gaziano J. et al. Low-dose aspirin therapy for chronic stable angina : a randomized, placebo clinical trial, "Ann. Intern. Med-1991-V. 114-P. 835-839.2. Steering Committee of the Physician's Health Study Research Group Final report on the aspirin component of the ongoing Physician's Health Study / / New Engl. J. Med-1989 .- V. 321-P. 129-135.3. The Dutch TIA Study Group. A comparison of two doses of aspirin (30 mg vs. 283 mg a day) in patients after a transient ischemic attack or minor stroke / / New Engl. J. Med-1991-V. 325-P. 1261-1266.

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