Active ingredient: Acetylsalicylic acid (Acetylsalicylic acid) Concentration of active ingredient (mg): 500
NSAIDs. It has anti-inflammatory, analgesic and antipyretic effects, as well as inhibits platelet aggregation. The mechanism of action is associated with inhibition of the activity of COX - the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The decrease in the content of prostaglandins (mainly E1) in the center of thermoregulation leads to a decrease in body temperature due to the expansion of blood vessels of the skin and an increase in sweating. The analgesic effect is due to both central and peripheral effects. Reduces aggregation, platelet adhesion and thrombus formation due to the suppression of the synthesis of thromboxane A2 in platelets. It reduces mortality and the risk of myocardial infarction with unstable angina. Effective in the primary prevention of diseases of the cardiovascular system and in the secondary prevention of myocardial infarction. At a daily dose of 6 g or more, it inhibits the synthesis of prothrombin in the liver and increases the prothrombin time. Increases plasma fibrinolytic activity and reduces the concentration of vitamin K-dependent coagulation factors (II, VII, IX, X). It increases hemorrhagic complications during surgical interventions, increases the risk of bleeding during therapy with anticoagulants. Stimulates the excretion of uric acid (violates its reabsorption in the renal tubules), but in high doses. COX-1 blockade in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which may lead to ulceration of the mucous membrane and subsequent bleeding.
When ingestion is rapidly absorbed mainly from the proximal small intestine and to a lesser extent from the stomach. The presence of food in the stomach significantly alters the absorption of acetylsalicylic acid. Metabolizes in the liver by hydrolysis to form salicylic acid, followed by conjugation with glycine or glucuronide.The concentration of salicylates in the blood plasma is variable. About 80% of salicylic acid is bound to plasma proteins. Salicylates easily penetrate into many tissues and body fluids, including in spinal, peritoneal and synovial fluids. In small quantities, salicylates are found in the brain tissue, traces - in the bile, sweat, feces. Rapidly crosses the placental barrier, is excreted in small amounts with breast milk. In newborns, salicylates can displace bilirubin from the albumin and contribute to the development of bilirubin encephalopathy. The penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. most of the salicylate is converted to non-ionized acid, which penetrates well into tissues, incl. into the brain. It is excreted mainly by active secretion in the tubules of the kidneys in unchanged form (60%) and in the form of metabolites. The excretion of unchanged salicylate depends on the urine pH (when alkalinization of urine increases, the ionization of salicylates increases, their reabsorption worsens and excretion increases significantly). T1 / 2 of acetylsalicylic acid is approximately 15 minutes. T1 / 2 salicylate when taken in low doses is 2-3 hours, with an increase in dose may increase to 15-30 hours. In newborns, the elimination of salicylate is much slower than in adults.
Rheumatism, rheumatoid arthritis, infectious-allergic myocarditis; fever in infectious and inflammatory diseases; pain syndrome of weak and medium intensity of various genesis (including neuralgia, myalgia, headache); prevention of thrombosis and embolism; primary and secondary prevention of myocardial infarction; prevention of cerebral circulatory disorders by ischemic type.
Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, gastrointestinal bleeding, aspirin triad, presence in the history of indications of urticaria, rhinitis, caused by taking acetylsalicylic acid and other NSAIDs, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, exfoliating anesthesia, antifogging, antifungal, antifungal nodulis, antifungalis, antifungal, antifoaming, antifoaming, antifoaming, antifoaming, antifoaming, antifoaming, antifooprostroma, isn’t your heart, and you will be in trouble, you will have to do it, you will have anatomy, you will have hemorrhagic diathesis; K, hepatic and / or renal failure, deficiency of glucose-6-phosphate dehydrogenase, Reye's syndrome, childhood uany), I and III trimesters of pregnancy, lactation, hypersensitivity to acetylsalicylic acid and other salicylates.
Do not exceed recommended doses.
Use during pregnancy and lactation
Contraindicated for use in the I and III trimesters of pregnancy. In the second trimester of pregnancy, a one-time admission is possible according to strict indications. It has a teratogenic effect: when applied in the first trimester, it causes splitting of the upper palate, in the third trimester it causes inhibition of labor activity (inhibition of prostaglandin synthesis), premature closure of the arterial duct in the fetus, pulmonary hyperplasia vessels and hypertension in the pulmonary circulation. Acetylsalicylic acid is excreted in breast milk, which increases the risk of bleeding in a child due to function of platelets, so do not use acetylsalicylic acid in the mother during lactation.
Dosage and administration
Inside Dosage regimen is individual. For adults, a single dose of acetylsalicylic acid varies from 40 mg to 1 g, daily - from 150 mg to 8 g; frequency of use - 2-6 times / day.
Nausea, vomiting, anorexia, epigastric pain, diarrhea; rarely - the occurrence of erosive and ulcerative lesions, bleeding from the gastrointestinal tract, abnormal liver function, dizziness, headache, reversible visual disturbances, tinnitus, aseptic meningitis, thrombocytopenia, anemia, hemorrhagic syndrome, lengthening of bleeding time, impaired kidney function; with prolonged use - acute renal failure, nephrotic syndrome, skin rash, angioedema, bronchospasm, aspirin triad.
Interaction with other drugs
With simultaneous use of antacids containing magnesium and / or aluminum hydroxide, slow down and reduce the absorption of acetylsalicylic acid. With simultaneous use of calcium channel blockers, means that limit calcium intake or increase the excretion of calcium from the body, the risk of bleeding increases. When used simultaneously with acetylsalicylic acid effect of heparin and indirect anticoagulants, hypoglycemic agents of sulfonylurea derivatives, insulins, methotrexate, phenytoin, valproic acid. When used simultaneously with GCS, the risk of ulcerogenic action and the occurrence of gastrointestinal bleeding increases. If used simultaneously, the effectiveness of diuretics (spironolactone, furosemide) decreases. If other NSAIDs are used simultaneously, the risk of side effects increases.Acetylsalicylic acid can reduce plasma concentrations of indomethacin, piroxicam. When used simultaneously with gold, acetylsalicylic acid can induce damage to the liver. With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) decreases. and alendronate sodium may develop severe esophagitis. With simultaneous use of griseofulvin, absorption of acetic acid may be impaired. ilsalicylic acid. A case of spontaneous hemorrhage into the iris is described when taking an extract of ginkgo biloba against the background of prolonged use of acetylsalicylic acid at a dose of 325 mg / day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation. With simultaneous use of dipyridamole, an increase in C max of salicylate in blood plasma and AUC is possible. If used simultaneously with acetylsalicylic acid, concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase. in high doses with carbonic anhydrase inhibitors, salicylate intoxication is possible. Acetylsalicylic acid in doses of less than 300 mg / day has a slight effect ie the effectiveness of captopril and enalapril. With the use of acetylsalicylic acid in high doses, it is possible to decrease the effectiveness of captopril and enalapril. With simultaneous use, caffeine increases the absorption rate, plasma concentration and bioavailability of acetylsalicylic acid. With simultaneous use, metoprolol may increase Cmax of salicylate in plasma. acetylsalicylic acid in high doses there is a risk of severe adverse reactions from the kidneys. With simultaneous use of phenylb tazon reduces urikozurii caused by simultaneous use of acetylsalicylic kislotoy.Pri ethanol can enhance the effect of acetylsalicylic acid on the digestive tract.
With caution used in patients with diseases of the liver and kidneys, with bronchial asthma, erosive and ulcerative lesions and bleeding from the gastrointestinal tract in history,with increased bleeding or with simultaneous anticoagulation therapy, decompensated chronic heart failure. Acetylsalicylic acid even in small doses reduces the excretion of uric acid from the body, which can cause an acute attack of gout in susceptible patients. When conducting long-term therapy and / or using acetylsalicylic acid in high doses, it is necessary to observe a doctor and regularly monitor hemoglobin levels. The use of acetylsalicylic acid as an anti-inflammatory agent in a daily dose of 5-8 g is limited due to the high probability of side effects from the gastrointestinal tract. Surgical intervention to reduce bleeding during surgery and in the postoperative period, you should cancel the reception of salicylates for 5-7 days. During prolonged therapy and it is necessary to carry out a complete blood count and examination of feces for occult blood. The use of acetylsalicylic acid in pediatrics is contraindicated because in the case of viral infection in children under the influence of acetylsalicylic acid increases the risk of developing Reye's syndrome. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, enlarged liver. The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an analgesic and more than 3 days as an antipyretic. During the period of treatment, the patient should refrain from alcohol.