Acetylsalicylic acid
Producer: JSC Borisovsky Plant of Medical Supplies Republic of Belarus
Code of automatic telephone exchange: N02BA01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 500 mg of acetylsalicylic acid in 1 tablet.
Excipients: potato starch, food citric acid, talc, stearic acid, silicon dioxide colloid anhydrous.
Pharmacological properties:
Pharmacodynamics. Acetylsalicylic acid renders antiinflammatory, analgeziruyushchy, febrifugal and anti-aggregation action. The mechanism of action is connected with irreversible inhibition of activity of cyclooxygenase I and II of types by its acetylation.
Acetylsalicylic acid reduces a hyperemia, exudation and permeability of capillaries in the inflammation center. Brakes activity of hyaluronidase, oppresses products of ATP, limiting power ensuring inflammatory process.
The antiinflammatory effect of acetylsalicylic acid develops in 1-2 days of regular reception (after creation in fabrics of constant therapeutic level of salicylates which makes 150-200 mkg/ml) and reaches a maximum at the level of salicylate of 200-300 mkg/ml. Weakens a rest pain and at the movement, reduces morning constraint and a swelling of joints, improves their function. At posttraumatic and postoperative inflammatory processes quickly stops both spontaneous pain, and the pain arising at the movement. Reduces inflammatory hypostasis in the field of a wound.
Acetylsalicylic acid has soothing effect, raises an excitation threshold of the painful centers of a thalamus. Eliminates the pains of weak and average intensity having, as a rule, somatic character: muscle, joints, sinews pains, nervous trunks, head and tooth hurt. At visceral pains (inflammations of internals, renal and hepatic gripes) concedes to opioid analgetics.
Acetylsalicylic acid reduces the increased body temperature, but does not influence normal body temperature. It is connected with its ability to reduce activity of the thermoadjusting center of a hypothalamus, to reduce influence on it of endogenous pyrogens, to strengthen a thermolysis.
Acetylsalicylic acid breaks reaction of pasting (aggregation) of thrombocytes and leads to some lengthening of a bleeding time. Anti-aggregation action remains within 7 days after a single dose and is more expressed at men, than at women.
When using as anti-aggregation means in doses of 160-300 mg/days reduces a lethality and risk of development of a myocardial infarction in patients with unstable stenocardia. It is effective at primary and secondary prevention of a myocardial infarction, especially at men 40 years are more senior.
For prevention of a stroke, passing disturbance of cerebral circulation, tromboembolic episodes after hirurugichesky interventions on vessels or invasive researches drug appoint 100-300 mg/days in a dose.
Pharmacokinetics. After intake it is quickly and rather fully absorbed. During absorption is exposed to intensive deacetylation in a wall of intestines and liver (the period of semi-elimination of not changed acetylsalicylic acid no more than 15-20 min.) with formation of salicylic acid. The maximum concentration of acetylsalicylic acid in a blood plasma is reached in 10-20 min. after reception, salicylic acid – in 0,3-2,0 h.
In plasma about 80% of atselisalitsilovy and salicylic acid are in the state connected with albumine. At the same time, even the form of medicine connected with protein keeps the biological activity. At newborn children salicylic acid can force out bilirubin from communication with albumine and promote development of encephalopathy. Easily gets into all fabrics and liquids of an organism, including into synovial, cerebrospinal and peritoneal fluid. In the presence of an inflammation and hypostasis penetration of salicylate into a cavity of a joint accelerates. In a proliferative phase of an inflammation, opposite – it is slowed down. In brain tissues salicylates are found in small amounts, in bile, sweat and excrements. At development of acidosis salicylic acid passes into not ionized form and its penetration into fabrics of a nervous system increases. Quickly passes through a placenta, comes to breast milk.
It is metabolized in a liver with formation of a salitsilurat, salitsilovofenolny glucuronide, gentisinic and gentizuronovy acids. It is excreted by kidneys by active canalicular secretion in not changed form (60%) and in the form of metabolites. Removal depends from рН urine: at its alkalifying increases, at acidulation – decreases.
Elimination of drug is nonlinear and kinetics indicators, depend on the size of the accepted dose.
Elimination of salicylates at children of the first year of life proceeds much more slowly, than at adults.
Indications to use:
- acute rheumatic fever, pseudorheumatism, pericardis, Dressler's syndrome, rheumatic chorea;
- a pain syndrome of weak and average intensity (including a headache, migraine, a dentagra, pains at an osteoarthrosis, arthritis, a menalgiya, альгодисменорея);
- the backbone diseases which are followed by a pain syndrome: lumbago, sciatica;
- a feverish syndrome at acute infectious, infectious воспа-лительных diseases;
- prevention of development of a myocardial infarction at an ischemic heart disease, existence of several risk factors of an ischemic heart disease, bezbolevy ischemia of a myocardium, unstable stenocardia;
- prevention of a repeated myocardial infarction at persons with a heart attack in the anamnesis;
- prevention of an ischemic stroke at persons with the tranzitorny ischemic attack, an ischemic stroke in the anamnesis (at men);
- decrease in risk of a repeated stenosis and secondary stratification of a coronary artery after balloon coronary angioplasty and installation of a stent;
- prevention of thromboembolisms at vasculites of coronary arteries (the disease of Kawasaki, aortoarteriit Takayasa), valve mitral heart diseases, a ciliary arrhythmia, a prolapse of the mitral valve.
Route of administration and doses:
Apply inside, it is more preferable between meals. The tablet is placed in 100 ml of boiled water (1/2 glasses) and, stirring slowly, try to obtain its disintegration then drink the received suspension.
The adult appoint 1-2 tablets 3 times a day. The maximum single dose - 2 tablets, the maximum daily dose - 6 tablets.
To children (at treatment of acute rheumatic fever, a pericardis, elimination of a pain syndrome) appoint at the rate of 20-30 mg/kg. At the age of 2 - 3 years of 100 mg/days. At the age of 4-6 years in a dose of 200 mg/days. At the age of 7-9 years in a dose of 300 mg/days. 12 years in a single dose of 250 mg (1/2 tablets) 2 times a day, the maximum daily dose of 750 mg are aged more senior.
At a myocardial infarction, and also for secondary prevention at persons of 40-325 mg of 1 times which transferred a heart attack in days, in the evening (usually 1/4-1/2 tablets).
As means for decrease in aggregation of thrombocytes and the prevention of tromboembolic episodes on 250-325 mg/days (1/2-3/4 tablets) during the long period.
At the tranzitorny ischemic attacks or cerebral tromboembolic episodes at men apply 250-325 mg/days (1/2-3/4 tablets) with gradual increase as much as possible up to 1000 mg/days.
For prevention of thrombosis or occlusion of the aortal shunt - on 325 mg (3/4 tablets) in each 7 h via the nazogastralny probe. Then inside in the same dose 3 times a day in combination with Dipiridamolum (in 1 week Dipiridamolum is cancelled).
As an antipyretic appoint at the body temperature more than 38,5 °C (patients with febrile spasms in the anamnesis - at a temperature have more than 37,5 °C) in a dose of 500-1000 mg.
Features of use:
Pregnancy and lactation. In pregnancy Ii Iiitrimestrakh reception of acetylsalicylic acid is contraindicated. At use in Iiitrimestre of pregnancy of acetylsalicylic acid in a dose more than 500 mg/days can occur premature closing of an arterial channel at a fruit, develop pulmonary hypertensia, dysfunction of kidneys up to emergence of a renal failure with an oligoamnios, lengthening of a bleeding time at mother and a fruit by the end of pregnancy. In Iitrimestr of pregnancy incidental use of acetylsalicylic acid is allowed. As salicylates get into breast milk in small amounts in need of their use in the period of a lactation it is necessary to separate the child from a breast.
Use in pediatrics. When using acetylsalicylic acid at children 15 years with a hyperthermia (fever) in combination with a viral infection or ORZ are younger the risk of development of a syndrome to Reja (damage of a brain and liver) is high. Therefore use of acetylsalicylic acid for this group of patients is contraindicated and can be carried out only in limited cases (treatment of acute rheumatic fever, a pericardis).
Use in the period of surgical interventions. In 5-7 days prior to the planned surgical intervention it is necessary to stop reception of acetylsalicylic acid for reduction of risk of development of bleeding during operation and the postoperative period.
Prolonged use of acetylsalicylic acid. In need of prolonged use of acetylsalicylic acid it is necessary to control a pattern of peripheral blood and to investigate kcal on the occult blood. Especially at persons with GIT erosive cankers, gastrointestinal bleedings in the anamnesis, renal failures and a liver.
Use at persons with pathology of bronchopulmonary system. At patients with bronchial asthma, polipozy a nose and at hay fever use of acetylsalicylic acid can provoke an exacerbation of a disease.
Side effects:
- nausea, loss of appetite, a stomach ache, erosive cankers of a GIT, bleeding in a GIT, a liver failure.
- allergic reactions, skin rash, Quincke's disease, "aspirinovy" asthma and "aspirinovy" triad (Fernon-Vidal's syndrome).
- intersticial nephrite, a papillary necrosis, a nephrotic syndrome, a renal failure (at prolonged use).
- thrombocytopenia, anemia, leukopenia.
- a syndrome to Reja (encephalopathy in combination with acute fatty dystrophy of a liver and hepatocellular insufficiency).
- strengthening of weight of heart failure, manifestation is hidden the proceeding forms of chronic heart failure (at prolonged use).
- dizziness, headache, vision disorders, sonitus, decrease in auditory acuity, aseptic meningitis.
- an accustoming headache after cancellation of acetylsalicylic acid against the background of the previous prolonged use.
Interaction with other medicines:
At simultaneous use increases toxicity of a methotrexate, valproic acid, barbituric drugs, effects of narcotic analgetics, peroral antidiabetic drugs, sulfanamide means (including co-trimoxazole), triiodothyronine, digoxin due to their replacement from communication with protein.
Increases risk of bleedings at simultaneous use with indirect anticoagulants, inhibitors of aggregation of thrombocytes, thrombolytic means.
Weakens effects of antihypertensives from group of APF inhibitors, loopback and potassium - saving diuretics due to braking of formation of prostaglandins in kidneys.
Glucocorticosteroids strengthen toxic effect of acetylsalicylic acid on mucous a stomach, increase clearance of acetylsalicylic acid and reduce its concentration in a blood plasma.
At simultaneous use with salts of lithium increases concentration of ions of lithium in plasma.
Weakens action of uricosuric means due to competitive removal of uric acid in nephron tubules.
Strengthens toxic effect of alcohol on a mucous membrane of digestive tract.
Contraindications:
- deficit glyukozo-6-fosfatdegidrogenazy;
- hypersensitivity to acetylsalicylic and salicylic acid;
- GIT erosive cankers in an aggravation phase;
- "aspirinovy" asthma and "aspirinovy" triad;
- hemorrhagic diathesis (angiohemophilia, Werlhof's disease, telangiectasias), prothrombinopenia, hemophilia;
- the stratifying aortic aneurysm;
- deficit of vitamin K;
- reception of a methotrexate in a dose of 15 mg/week and more;
- renal and liver failure;
- pregnancy I and III trimester, lactation;
- children's age up to 15 years in combination with a hyperthermia against the background of viral diseases.
Overdose:
Arises at reception of once high doses of acetylsalicylic acid (more than 100 mg/kg) or prolonged use of acetylsalicylic acid in the raised doses (salitsilizm).
At reception of acetylsalicylic acid in a dose of 150-200 mg/kg (or at the level of salicylates in plasma of 50-80 mg/dl) poisoning of easy severity develops. Emergence of a ring in ears, a hyperventilation owing to stimulation of a respiratory center, a respiratory alkalosis in connection with loss of CO2 is characteristic.
At reception of acetylsalicylic acid in a dose of 200-300 mg/kg (or at the level of salicylates in plasma of 80-110 mg/dl) poisoning of moderate severity develops. There are severe short wind, a hyperthermia owing to dissociation of oxidation and phosphorylation (a bad predictive sign at adults), a metabolic acidosis in connection with strengthening of anaerobic glycolysis.
At reception of acetylsalicylic acid in a dose of 300-500 mg/kg (or at the level of salicylates in plasma of 110-160 mg/dl) the serious poisoning develops. There is a collapse, a coma, spasms, a prothrombinopenia.
At reception of acetylsalicylic acid in a dose> 500 mg/kg (or at the level of salicylates in plasma> 160 mg/dl) extremely serious poisoning with renal and respiratory failure develops.
Measures of the help include drug withdrawal, provocation of vomiting or a gastric lavage with absorbent carbon and purpose of salt laxatives for prevention of absorption of drug in a stomach and intestines. Introduction of alkalizing means for maintenance of values рН urine at the level of 7,5-8,0. At the level of salicylates in plasma over 300 mg/l (2,2 mmol/l) at children and 500 mg/l (3,6 mmol/l) at adults are shown carrying out the forced alkaline diuresis (also 5% of glucose with a speed of 10-15 ml/kg/h with furosemide of 40-60 mg are provided with intravenous infusion of hydrosodium carbonate 88 ¼Ý¬ó/l). Carry out recovery of OTsK and correction of KShchS. At the level of salicylates more than 1000 mg/l, and also at refractory acidosis are shown carrying out a hemodialysis. At wet brain carrying out IVL is shown by the mix enriched with oxygen in the mode of positive pressure at the end of an exhalation. At wet brain carry out a hyperventilation in combination with administration of osmotic diuretics.
The specific antidote does not exist.
It is not recommended to use for urine alkalization acetazoleamide at treatment of intoxication in connection with a possibility of development of an acidemia and strengthening of toxic effect of salicylate on the patient's organism.
Storage conditions:
In the place protected from light and moisture, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 4 years. Not to use after the termination of a period of validity.
Issue conditions:
Without recipe
Packaging:
10 tablets in planimetric bezjyacheykovy packaging, on 1 planimetric bezjyacheykovy packaging together with a leaf insert in a pack. 10 tablets in a blister strip packaging, on 1, 2, 3 or 5 blister strip packagings together with a leaf insert in a pack from a cardboard. For treatment and prevention facilities: 390 planimetric bezjyacheykovy or 300 blister strip packagings together with 10 application instructions in a box from a cardboard.
