Composition
One tablet contains: Active ingredient: Acetylsalicylic acid-0.5 GH Auxiliary substances: potato starch-0.083632 glytric acid monohydrate-0.000168 g zinc-0.0162 g
Pharmacological action
The drug has analgesic, antipyretic, anti-inflammatory effects, which is due to the inhibition of cyclooxygenases involved in the synthesis of prostaglandins. Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxaneA2.
Pharmacokinetics
When taken orally, the absorption is complete. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated). The absorbed part is rapidly hydrolyzed by non-specific plasma cholinesterases and albuminesterase, so the half-life is no more than 15-20 minutes.
It circulates in the body (by 75-90% due to albumin) and is distributed in the tissues in the form of salicylic acid anion.
The time to reach the maximum concentration is 2 hours. The serum concentration of salicylates is very variable. Salicylates easily penetrate many tissues and body fluids, including the cerebrospinal fluid, peritoneal fluid, and synovial fluid.
Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the nervous tissue, traces – in bile, sweat, feces. When acidosis occurs, most of the salicylic acid is converted to non-ionized acid, which penetrates well into tissues, including the brain. It passes quickly through the placenta and is excreted in small amounts in breast milk.
It is mainly metabolized in the liver. The metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. It is mainly excreted by active secretion in the renal tubules in the form of salicylic acid (60%) and in the form of metabolites. The excretion of salicylic acid depends on the pH of the urine (when the urine is alkalized, the ionization of salicylates increases, their reabsorption worsens and the excretion increases significantly). The rate of elimination depends on the dose: when taking small doses, the half-life is 2-3 hours, with an increase in the dose it can increase to 15-30 hours.
Indications
Treatment of moderate or mild pain: headache (including withdrawal symptoms), toothache, sore throat, back and muscle pain, joint pain, pain during menstruation.
Elevated body temperature in “colds” and other infectious and inflammatory diseases (in adults and children over 15 years of age).
Use during pregnancy and lactation
During pregnancy, the use of the drug is contraindicated.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.
Contraindications
– Hypersensitivity to acetylsalicylic acid and other NSAIDs or other components of the drug;
– erosive-ulcerative lesions of the gastrointestinal tract (GIT) (in the phase of exacerbation);
gastrointestinal hemorrhage;
hemorrhagic diathesis;
– the combined use of methotrexate in a dose of 15 mg per week or more;
– complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid;
– bronchial asthma induced by ingestion of salicylates and other NSAIDs;
– pregnancy (I and III trimester), lactation period;
– children’s age (under 15 years – when used as antipyretic).
The drug is not prescribed to children under 15 years of age with acute respiratory diseases caused by viral infections, because of the risk of developing Reye’s syndrome (encephalopathy and acute fatty liver with acute development of liver failure).
With caution – with concomitant anticoagulant therapy, gout, stomach and/or duodenal ulcer (in the anamnesis), including chronic or recurrent peptic ulcer disease, or episodes of gastrointestinal bleeding; with renal and/or hepatic insufficiency, glucose-6-phosphate dehydrogenase deficiency; hyperuricemia, bronchial asthma, chronic obstructive pulmonary disease, hay fever, nasal polyposis, drug allergy, concomitant use of methotrexate at a dose of less than 15 mg/week, pregnancy (II trimester).
Side effects
From the gastrointestinal tract: decreased appetite, abdominal pain, heartburn, nausea, vomiting, obvious (vomiting with blood, tarry stools) or hidden signs of gastrointestinal bleeding, which can lead to iron deficiency anemia, erosive and ulcerative lesions (including perforation) of the gastrointestinal tract, isolated cases-liver function disorders (increased liver transaminases), diarrhea.
From the central nervous system: dizziness, tinnitus (usually signs of overdose); with prolonged use – headache, visual impairment, decreased hearing acuity, aseptic meningitis.
From the cardiovascular system: with prolonged use – increased symptoms of chronic heart failure.
From the hematopoietic system: increased risk of bleeding due to the effect of acetylsalicylic acid on platelet aggregation, thrombocytopenia, anemia, leukopenia.
From the excretory system: impaired renal function; with prolonged use-interstitial nephritis, prerenal azotemia with increased blood creatinine and hypercalcemia, papillary necrosis, acute renal failure, nephrotic syndrome, edema.
Allergic reactions: skin rash, anaphylactic reactions, bronchospasm, angioedema.
Reye’s syndrome (encephalopathy and acute fatty liver disease with rapid development of liver failure).
If such symptoms occur, it is recommended to stop taking the drug and immediately consult your doctor.
Interaction
Shared application:
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with methotrexate at a dose of 15 mg per week or more increased hemolytic cytotoxicity of methotrexate (decreased renal clearance of methotrexate and methotrexate is substituted salicylates in connection with blood plasma proteins);
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anticoagulants, for example, with heparin: increased risk of bleeding due to inhibition of platelet function, damage to the mucosa of the gastrointestinal tract, displacing anticoagulants (oral) from the blood plasma;
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with other nonsteroidal anti-inflammatory drugs: as a result of synergistic interaction increases the risk of ulcers and bleeding of the stomach;
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with uricosuric drugs, such as benzbromarone: reduces uricosuric effect;
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digoxin: digoxin concentration increased because of the reduced renal excretion;
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with hypoglycemic drugs such as insulin: increased hypoglycemic effect of hypoglycemic drugs due to the hypoglycemic action of the acetylsalicylic acid;
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drugs of the group of thrombolytics: the risk of bleeding increases;
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with systemic corticosteroids, except hydrocortisone, used as replacement therapy in Addison’s disease: the use of corticosteroids reduces the level of salicylates in the blood by increasing excretion of the latter;
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with angiotensin-converting enzyme: reduced glomerular filtration due to the inhibition of prostaglandins and, as a consequence, reduced antihypertensive effect;
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with valproic acid: increases toxicity of valproic acid;
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ethanol (alcoholic beverages): increases the risk of damaging effects on the mucous membranes of the gastrointestinal tract and increases the risk of gastrointestinal bleeding;
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enhances the effects of narcotic analgesics, of thrombolytics and thrombocyte aggregation inhibitors, sulfonamides (including co-trimoxazole);
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increases the concentration of barbiturates, lithium salts in the plasma;
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antacids containing magnesium and/or aluminum, slow down and reduce the absorption of acetylsalicylic acid;
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myelotoxic drugs increase the manifestation gematotoksichnosti of the drug.
How to take, course of use and dosage
Inside, adults and children over 12 years of age: a single dose is 250-500 mg, the maximum single dose is 1.0 g (2 tablets of 500 mg), the maximum daily dose is 3.0 g (6 tablets of 500 mg), a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours.
Children (as an analgesic) aged from b to 12 years, with the exception of acute respiratory diseases caused by viral infections, due to the risk of developing Reye’s syndrome (encephalopathy and acute fatty liver with acute development of liver failure), a single dose is 250 mg per reception, take up to 2 times a day.
How to use: the drug should be taken after a meal, washed down with water, milk or alkaline mineral water.
Frequency and time of use: a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Regular adherence to the drug regimen allows you to avoid a sharp increase in temperature and reduce the intensity of pain.
The duration of treatment (without consulting a doctor) should not exceed 7 days when prescribed as an analgesic and more than 7 days – as an antipyretic.
Overdose
Symptoms: Moderate overdose: nausea, vomiting, tinnitus, hearing loss, headache, dizziness and confusion.These symptoms disappear when the dose of the drug is reduced.
Severe overdose: fever, hyperventilation, ketoacidosis, respiratory alkalosis, metabolic acidosis, coma, cardiogenic shock, respiratory failure, severe hypoglycemia.
Treatment: hospitalization, gastric lavage, use of activated charcoal, monitoring of acid-base balance, alkaline diuresis in order to obtain a urine pH between 7.5-8 (forced alkaline diuresis is considered achieved if the concentration of salicylate in the blood plasma is more than 500 mg/l (3.6 mmol/l) in adults or 300 mg / l (2.2 mmol/l) in children), hemodialysis, compensation for fluid loss, symptomatic therapy.
Special instructions
Acetylsalicylic acid may cause bronchospasm, an attack of bronchial asthma, or other hypersensitivity reactions. Risk factors include the presence of bronchial asthma, nasal polyps, fever, chronic bronchopulmonary diseases, and a history of allergies (allergic rhinitis, skin rashes).
Acetylsalicylic acid may increase the tendency to bleed due to its inhibitory effect on platelet aggregation. This should be taken into account when surgical procedures are needed, including minor interventions such as tooth extraction. Before surgery, to reduce bleeding during the operation and in the postoperative period, you should stop taking the drug for 5-7 days and inform the doctor.
Children should not be prescribed medications containing acetylsalicylic acid, because in the case of a viral infection, the risk of Reye’s syndrome increases. Symptoms of Reye’s syndrome include prolonged vomiting, acute encephalopathy, and enlarged liver.
If it is necessary to use the drug during lactation, breastfeeding should be discontinued.
In the treatment of vascular diseases, the daily dose of acetylsalicylic acid ranges from 75 to 300 mg
. Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.
There was no effect of taking the drug on driving a motor vehicle and other mechanisms.
Form of production
Tablets
Storage conditions
Store in a dry place, at a temperature not exceeding 25 ° C. Keep out of reach of children.
Shelf
life is 4 years.
Active ingredient
Acetylsalicylic acid
Dosage form
Tablets
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