Acetylsalicylic acid - instructions for use, reviews, analogs and forms of release (tablets 250 mg and 500 mg) drugs for the treatment of inflammatory diseases, temperature, headache and other pain in adults, children and pregnancy
In this article, you can read the instructions for using the drug Acetylsalicylic acid. There are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Acetylsalicylic acid in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Acetylsalicylic acid in the presence of existing structural analogs.Use for the treatment of inflammatory diseases, temperature, headache, dental and other pain in adults, children, as well as during pregnancy and lactation.
Acetylsalicylic acid - Non-steroidal anti-inflammatory drug. Has anti-inflammatory, analgesic and antipyretic effect, and also inhibits platelet aggregation. The mechanism of action is associated with oppression of the activity of COX, the main enzyme of arachidonic acid metabolism, which is the precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Reduction of the content of prostaglandins (mainly E1) in the center of thermoregulation leads to a decrease in body temperature due to the expansion of the vessels of the skin and increased sweating. The analgesic effect is due to both central and peripheral action. Reduces aggregation, platelet adhesion and thrombus formation by suppressing the synthesis of thromboxane A2 in platelets.
Reduces the mortality and 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.In a daily dose of 6 grams or more suppresses the synthesis of prothrombin in the liver and increases prothrombin time. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent clotting factors (2, 7, 9, 10). It increases hemorrhagic complications during surgical interventions, increases the risk of bleeding on the background of therapy with anticoagulants. Stimulates the excretion of uric acid (violates its reabsorption in the renal tubules), but in high doses. Blockage of COX-1 in the gastric mucosa leads to inhibition of gastroprotective prostaglandins, which can cause ulceration of the mucosa and subsequent bleeding.
Pharmacokinetics
When ingested quickly absorbed mainly from the proximal part of the small intestine and to a lesser extent from the stomach. The presence of food in the stomach significantly alters the absorption of acetylsalicylic acid. Metabolised in the liver by hydrolysis with the formation of salicylic acid, followed by conjugation with Glycine or glucuronide. The concentration of salicylates in the blood plasma is variable.
About 80% of salicylic acid binds to blood plasma proteins.Salicylates easily penetrate into many tissues and body fluids, including. in spinal, peritoneal and synovial fluid. In small amounts, salicylates are found in the brain tissue, traces - in bile, sweat, feces. Rapidly penetrates the placental barrier, in small quantities excreted in breast milk.
In newborns, salicylates can displace bilirubin from bonding with albumin and promote the development of bilirubin encephalopathy.
Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation.
It is excreted mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites.
Indications
- rheumatism;
- rheumatoid arthritis;
- infectious-allergic myocarditis;
- fever in infectious and inflammatory diseases;
- pain syndrome of mild and moderate intensity of various genesis (including neuralgia, myalgia, headache);
- prevention of thrombosis and embolism;
- primary and secondary prevention of myocardial infarction;
- prevention of cerebral circulation disorders by ischemic type;
- in gradually increasing doses for continued "aspirin" desensitization and the formation of persistent tolerance to NSAIDs in patients with "aspirin" asthma and "aspirin triad."
Forms of release
Tablets 250 mg and 500 mg.
Instructions for use and dosage
Individual. For adults, a single dose varies from 40 mg to 1 g, daily from 150 mg to 8 g; multiplicity of application - 2-6 times a day. Drink preferably milk or alkaline mineral water.
Side effect
- nausea, vomiting;
- anorexia;
- pain in epigastrium;
- diarrhea;
- occurrence of erosive-ulcerative lesions;
- bleeding from the gastrointestinal tract;
- dizziness;
- headache;
- reversible visual impairment;
- noise in ears;
- thrombocytopenia, anemia;
- hemorrhagic syndrome;
- prolonged bleeding time;
- impaired renal function;
- acute renal insufficiency;
- skin rash;
- angioedema;
- bronchospasm;
- "Aspirin triad" (combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and drugs of pyrazolone series);
- Reye's syndrome (Reynaud);
- increased symptoms of chronic heart failure.
Contraindications
- erosive and ulcerative lesions of the gastrointestinal tract in the phase of exacerbation;
- gastrointestinal bleeding;
- "aspirin triad";
- the presence in the anamnesis of indications for urticaria, rhinitis caused by the intake of acetylsalicylic acid and other NSAIDs;
- hemophilia;
- hemorrhagic diathesis;
- hypoprothrombinemia;
- exfoliating aortic aneurysm;
- portal hypertension;
- deficiency of vitamin K;
- hepatic and / or renal insufficiency;
- deficiency of glucose-6-phosphate dehydrogenase;
- Reye's syndrome;
- Children's age (under 15 years - the risk of developing Reye's syndrome in children with hyperthermia in the presence of viral diseases);
- 1 and 3 trimesters of pregnancy;
- lactation period;
- hypersensitivity to acetylsalicylic acid and other salicylates.
Application in pregnancy and lactation
Contraindicated in the use of 1 and 3 trimesters of pregnancy. In the 2nd trimester of pregnancy, one-time administration is possible on strict indications.
Has a teratogenic effect: when applied in 1 trimester leads to the development of cleavage of the upper sky, in the 3rd trimester - causes inhibition of labor (inhibition of prostaglandin synthesis), premature closure of the arterial duct in the fetus, hyperplasia of pulmonary vessels and hypertension in the small circulation.
Acetylsalicylic acid is excreted in breast milk, which increases the risk of bleeding in the child due to a violation of the function of platelets, so you should not use acetylsalicylic acid in the mother during lactation.
special instructions
They are used with caution in patients with liver and kidney disease, with bronchial asthma, erosive and ulcerative lesions and bleeding from the gastrointestinal tract in an anamnesis, with increased bleeding or concomitant anticonvolution 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 predisposed patients. When performing long-term therapy and / or using acetylsalicylic acid in high doses, it is necessary to observe the doctor and regularly check the level of hemoglobin.
The use of acetylsalicylic acid as an anti-inflammatory agent in a daily dose of 5-8 grams is limited due to the high likelihood of developing side effects from the gastrointestinal tract.
Before surgical intervention, to reduce bleeding during surgery and in the postoperative period, it is necessary to cancel the intake of salicylates for 5-7 days.
During prolonged therapy, a general blood test and examination of feces for latent blood should be performed.
The use of acetylsalicylic acid in pediatrics is contraindicated, since in the case of viral infection in children under the influence of acetylsalicylic acid, the risk of developing the Reye syndrome increases. Symptoms of Reye's syndrome are prolonged vomiting, acute encephalopathy, enlargement of the liver.
Duration of treatment (without consulting a physician) should not exceed 7 days with an appointment as an analgesic and more than 3 days as an antipyretic.
During treatment, the patient should refrain from drinking alcohol.
Drug Interactions
With simultaneous use of antacids containing magnesium and / or aluminum hydroxide, slow down and reduce the absorption of acetylsalicylic acid.
With the simultaneous use of calcium channel blockers, drugs that limit the intake of calcium or increase the excretion of calcium from the body, the risk of bleeding increases.
With simultaneous use with acetylsalicylic acid, the action of Heparin and indirect anticoagulants, hypoglycemic agents of sulfonylurea derivatives, insulins, methotrexate, phenytoin, valproic acid increases.
With simultaneous application with GCS, the risk of ulcerogenic action and the occurrence of gastrointestinal bleeding increases.
With simultaneous use, the effectiveness of diuretics (spironolactone, furosemide) decreases.
With the simultaneous use of other NSAIDs, the risk of side effects increases. Acetylsalicylic acid can reduce plasma concentrations of indomethacin, piroxicam.
When used simultaneously with gold preparations, acetylsalicylic acid can induce liver damage.
With the simultaneous use, the effectiveness of uricosuric agents decreases (including probenecid, sulfinpyrazone, benzbromarone).
With the simultaneous use of acetylsalicylic acid and alendronate sodium, the development of severe esophagitis is possible.
With the simultaneous use of griseofulvin, absorption of acetylsalicylic acid may be impaired.
A case of spontaneous hemorrhage into the iris was described when taking an extract of Ginkgo Biloba against the background of prolonged use of acetylsalicylic acid at a dose of 325 mg per day. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.
With simultaneous use with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in blood plasma increase.
With the simultaneous use of salicylates in high doses with inhibitors of carbonic anhydrase, intoxication with salicylates is possible.
Acetylsalicylic acid in doses less than 300 mg per day has a negligible effect on the efficacy of Captopril and enalapril. With the use of acetylsalicylic acid in high doses, a decrease in the efficacy of captopril and Enalapril is possible.
With simultaneous use of Caffeine increases the rate of absorption, concentration in the blood plasma and bioavailability of acetylsalicylic acid.
When pentazocine is used against the background of long-term use of acetylsalicylic acid in high doses, there is a risk of developing serious adverse reactions from the kidneys.
With simultaneous use of phenylbutazone reduces uricosuria caused by acetylsalicylic acid.
With the simultaneous use of ethanol can increase the effect of acetylsalicylic acid on the digestive tract.
Analogues of the drug Acetylsalicylic acid
Structural analogs for the active substance:
- Anopyrine;
- ASA cardio;
- Aspicor;
- Aspen;
- Aspen Cardio;
- Aspirin "York";
- Aspirin;
- Aspirin 1000;
- Aspirin Cardio;
- Acercar;
- Acentene;
- Acetylsalicylic acid Cardio;
- Acetylsalicylic acid MS;
- Acetylsalicylic acid-Lect;
- Acetylsalicylic acid-Rusfar;
- Acetylsalicylic acid-UBF;
- Acylpyrine;
- Acsbyrin;
- Bufferin;
- Zorex Morning;
- KardiASK;
- Collorite;
- Myristin;
- Plolidol 100;
- Plolidol 300;
- Taspir;
- Trombo ACC;
- Thrombopol;
- Walsh-Asalgin;
- Upsarin of the UPSA;
- Hack el-Payne.
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