INN: Acetylsalicylic acid
Manufacturer: Marbiopharm OJSC
Anatomical-therapeutic-chemical classification: Acetylsalicylic acid
Registration number in the Republic of Kazakhstan: No. RK-LS-5No. 020068
Registration period: 07.08.2013 - 07.08.2018
Instructions
Tradename
Acetylsalicylic acid
International nonproprietary name
Acetylsalicylic acid
Dosage form
Tablets, 500 mg
Compound
One tablet contains
active substance: acetylsalicylic acid - 500 mg
Excipients: potato starch, acid stearic acid, citric acid monohydrate, talc
Description
Flat-cylindrical tablets, white, chamfered and scored, slightly marbled
Pharmacotherapeutic group
Analgesics. Other analgesics and antipyretics. Salicylic acid and its derivatives. Acetylsalicylic acid
ATX code N02BA01
Pharmacological properties
Pharmacokinetics
After ingestion, acetylsalicylic acid is converted into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acids in the digestive tract occurs quickly and completely. The maximum level of concentration in blood plasma is achieved after 10-20 minutes (acetylsalicylic acid) or 45-120 minutes ( general level salicylates). The degree of binding of acids to plasma proteins depends on the concentration, which is 49-70% for acetyl salicylic acid and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized during the initial passage through the liver.
The drug penetrates the blood-brain barrier and is also detected in breast milk and synovial fluid.
Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. The biotransformation of salicylates occurs primarily in the liver with the formation of 4 main metabolites found in many tissues and urine. Excretion of salicylates is carried out mainly by active secretion in the renal tubules in unchanged form (60%) and in the form of metabolites. The rate of excretion depends on the dose - when taking small doses, the half-life is 2-3 hours, and with increasing doses it can increase to 15-30 hours. In newborns, the elimination of salicylates is much slower than in adults. The anti-inflammatory effect of the drug occurs after 1-2 days of administration (after creating a constant therapeutic level of salicylates in the tissues, which is approximately 150-300 mcg/ml), reaches a maximum at a concentration of 20-30 mg% and persists throughout the entire period of use.
Pharmacodynamics
Acetylsalicylic acid has anti-inflammatory, antipyretic, and analgesic effects.
The anti-inflammatory effect of acetylsalicylic acid is explained by its influence on the processes occurring at the site of inflammation: a decrease in capillary permeability, a decrease in hyaluronidase activity, limiting the energy supply of the inflammatory process by inhibiting the formation of ATP, etc.
The antipyretic effect is associated with the effect on the hypothalamic thermoregulation centers.
The analgesic effect is due to the effect on pain sensitivity centers and the ability of salicylates to reduce the algogenic effect of bradykinin.
One of the main mechanisms of action of acetylsalicylic acid is the inactivation (suppression of activity) of the enzyme cyclooxygenase (an enzyme involved in the synthesis of prostaglandins), as a result of which the synthesis of prostaglandins is disrupted. Impaired prostaglandin synthesis leads to loss of sensitivity of peripheral nerve endings to kinins and other inflammatory and pain mediators (transmitters). Due to the disruption of prostaglandin synthesis, the severity of inflammation and their pyrogenic (increasing body temperature) effect on the thermoregulation center decreases. In addition, the effect of prostaglandins on sensory nerve endings is reduced, leading to a decrease in their sensitivity to pain mediators. It also has an antiaggregation effect.
The antiplatelet effect of the drug is to reduce the ability of platelets and other shaped elements blood to aggregation and reduce the likelihood of thrombosis. The mechanism of this action is associated with blocking the cyclooxygenase pathway of arachidonic acid metabolism, inhibition of the enzymes thromboxane synthetase, phosphodiesterase, an increase in the concentration of cAMP in platelets, a decrease in the level of intracellular calcium, inhibition of the synthesis of prostaglandins and the endogenous (synthesized in the body) compound of the prostaglandin group (eicosanoids) - thromboxane A2, which is a very active proaggregation (promoting platelet aggregation) factor, increasing the concentration of adenosine in the blood, blockade of glycoprotein GP IIb/IIIa receptors. As a result, platelet aggregation is inhibited, their resistance to deformation increases, the rheological properties of blood are improved, thrombus formation is suppressed, and microcirculation is normalized. Significant inhibition of platelet adhesiveness is achieved at doses of up to 30 mg. Increases fibrinolytic activity of plasma and reduces the concentration of vitamin K-dependent blood clotting factors. Stimulates excretion in high doses uric acid, since its reabsorption in the kidney tubules is impaired.
Indications for use
acute rheumatic fever, rheumatoid arthritis, pericarditis, Dressler's syndrome, rheumatic chorea
pain syndrome weak and medium intensity (including headache, migraine, toothache, pain due to osteoarthritis, arthritis, menalgia, algodismenorrhea)
diseases of the spine accompanied by pain (lumbago, sciatica)
neuralgia, myalgia
increased body temperature with colds and other infectious and inflammatory diseases (in adults and children over 15 years old)
Directions for use and doses
Acetylsalicylic acid is taken orally, after meals, with plenty of liquid - water, milk or mineral water.
For fever and pain syndrome It is recommended to take 0.25 - 0.5 g / day (1/2-1 tablet) 3 - 6 times a day. The interval between doses should be at least 4 hours. Maximum single dose 1 g. The maximum daily dose is 3.0 g.
If pain or fever persists after taking acetylsalicylic acid for 5 days, you should stop treatment and consult a doctor.
Side effects
dizziness, tinnitus, hearing loss
NSAID gastropathy: pain in the epigastric region, heartburn, nausea, vomiting, severe bleeding in the gastrointestinal tract
thrombocytopenia, anemia, leukopenia
Reye/Reye syndrome (progressive encephalopathy: nausea and uncontrollable vomiting, respiratory distress, drowsiness, convulsions; fatty liver, hyperammonemia, increased levels of AST, ALT)
allergic reactions: laryngeal edema, bronchospasm, urticaria, “aspirin” bronchial asthma and “aspirin” triad (eosinophilic rhinitis, recurrent nasal polyposis, hyperplastic sinusitis)
With long-term use:
interstitial nephritis, prerenal azotemia with increased creatinine in the blood and hypercalcemia, acute renal failure, nephrotic syndrome
papillary necrosis
blood diseases (anemia, agranulocytosis, thrombocytopenic purpura)
aseptic meningitis
increased symptoms of congestive heart failure, edema
increased levels of aminotransferases in the blood.
Contraindications
-
pregnancy and lactation
children under 15 years of age.
hypersensitivity to any component of the drug, including “aspirin” asthma, “aspirin” triad
hemorrhagic diathesis (hemophilia, von Willebrand disease, telangioethasia, thrombocytopenic purpura)
dissecting aortic anervism
decompensated chronic heart failure
acute and recurrent erosive and ulcerative diseases gastrointestinal tract(including gastrointestinal bleeding)
renal and liver failure
initial hypoprothrombinemia, vitamin K deficiency, thrombocytopenia
Drug interactions
At joint use acetylsalicylic acid with valproic acid preparations, cephalosporins or anticoagulants increases the risk of bleeding. With simultaneous use of the drug and NSAIDs, the main and side effects the latter.
During treatment with the drug, the side effects of methotrexate are aggravated (when taking the latter more than 15 mg/week, acetylsalicylic acid is contraindicated).
When used simultaneously with oral hypoglycemic drugs - sulfonylurea derivatives - the hypoglycemic effect is enhanced.
When used simultaneously with glucocorticosteroids and alcohol consumption, the risk of gastrointestinal bleeding increases.
The drug weakens the effect of spironolactone, furosemide, antihypertensive and anti-gout drugs that promote the excretion of uric acid.
Purpose antacids during treatment with the drug (especially in doses of more than 3.0 g for adults) may cause a decrease in high stable levels of salicylate in the blood.
special instructions
Acetylsalicylic acid increases the risk of bleeding even when taking small doses and for several days after taking it. Before any surgical procedure, inform your doctor, surgeon, anesthesiologist or dentist that you are taking acetylsalicylic acid. 5-7 days before surgical intervention it is necessary to cancel the dose (to reduce bleeding during the operation and in postoperative period). During long-term therapy, it is recommended to regularly perform blood tests and examine stool for occult blood.
With simultaneous anticoagulant therapy with acetylsalicylic acid in small doses, the excretion of uric acid is reduced, which may be the cause of gout.
Use in pediatrics The drug acetylsalicylic acid should not be prescribed to children under 15 years of age with acute respiratory diseases caused by viral infections, with diseases accompanied by hyperthermia due to the risk of developing Reye/Reye syndrome).
Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms
There is no evidence of adverse effects on active attention, motor activity and reflexes.
Overdose
Csymptoms: dizziness, visual and hearing impairment, nausea, vomiting, increased breathing. Later, depression of consciousness occurs, up to coma, respiratory failure, disturbance acid-base balance(respiratory alkalosis, then metabolic acidosis), acute renal failure (ARF), shock. Deadly intoxication is possible when taking a dose of 200 to 500 mg/kg.
Acetylsalicylic acid- nonsteroidal anti-inflammatory drugs (NSAIDs) with analgesic, antipyretic and anti-inflammatory properties. The mechanism of its action is the irreversible inactivation of cyclooxygenase enzymes, which play important role during the synthesis of prostaglandins.
Acetylsalicylic acid is used orally in a dose of 0.3 to 1 g to relieve pain and conditions accompanied by fever, such as colds, to reduce fever and relieve pain in joints and muscles.
Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane 2.
Pharmacokinetics.
After oral administration, acetylsalicylic acid is quickly and completely absorbed from the gastrointestinal tract. During and after absorption, it is converted to the main active metabolite, salicylic acid. The maximum concentration of acetylsalicylic acid in the blood plasma is achieved after 10-20 minutes, salicylates - after 20-120 minutes.
Acetylsalicylic and salicylic acids are completely bound to blood plasma proteins and are quickly distributed in the body.
Salicylic acid crosses the placenta and is excreted into breast milk.
Salicylic acid is metabolized in the liver. Metabolites of salicylic acid are salicylic acid, salicylphenol glucuronide, salicylacyl glucuronide, gentisic and gentisic acid.
The kinetics of salicylic acid elimination depends on the dose, since metabolism is limited by the activity of liver enzymes. The half-life depends on the dose and increases from 2-3 hours when using low doses to 15 hours when using high doses. Salicylic acid and its metabolites are excreted from the body primarily by the kidneys.
Indications for use
Indications for use of tablets Acetylsalicylic acid are:- Treatment of mild and moderately severe, acute pain syndrome (headache, toothache, joint and muscle pain, back pain).
- Symptomatic treatment of fever and/or pain associated with colds.
Mode of application
Acetylsalicylic acid taken orally after meals with a sufficient amount of liquid.Acetylsalicylic acid should not be used for longer than 3-5 days without consulting a doctor.
Adults and children over 15 years old - 1-2 tablets once. Repeated use is possible after 4-8 hours. The maximum daily dose should not exceed 4 g (8 tablets).
Side effects
From the gastrointestinal tract. Dyspepsia, pain in the epigastric region and abdominal pain, heartburn; in some cases - inflammation of the gastrointestinal tract, erosive and ulcerative lesions of the gastrointestinal tract, which can in rare cases cause gastrointestinal bleeding and perforation with corresponding laboratory and clinical manifestations.Rarely - transient liver failure with increased levels of liver transaminases.
From the side of blood and lymphatic system. Due to its antiplatelet effect on platelets, acetylsalicylic acid may increase the risk of bleeding. Bleedings such as PERIOPERATIVE bleeding, hematomas, urogenital bleeding, nosebleeds, bleeding from the gums were observed; rarely or very rarely - serious bleeding such as gastrointestinal bleeding and cerebral hemorrhage (especially in patients with uncontrolled arterial hypertension and/or with the simultaneous use of antihemostatic agents), which in rare cases can be life-threatening.
Bleeding can lead to acute and chronic posthemorrhagic anemia / iron deficiency anemia(due to the so-called hidden microbleeding) with corresponding laboratory manifestations and clinical symptoms such as asthenia, pallor skin, hypoperfusion.
In patients with severe glucose-6-phosphate dehydrogenase deficiency, hemolysis and the development of hemolytic anemia have been reported.
From the outside immune system. In patients with individual hypersensitivity to salicylates, allergic reactions may develop, including symptoms such as rash, urticaria, itching, eczema, rhinitis, nasal congestion, decreased blood pressure. Severe hypersensitivity reactions, including anaphylactic shock, angioedema, non-cardiogenic pulmonary edema. In patients bronchial asthma possible increase in the incidence of bronchospasm; allergic reactions from minor to moderate degree, potentially affecting the skin, respiratory system, gastrointestinal tract and cardiovascular system.
From the outside nervous system. Headache, dizziness, hearing loss, ringing in the ears and confusion may be signs of overdose.
From the urinary system. There is evidence of renal dysfunction and the development of acute renal failure.
Contraindications
Contraindications to the use of the drug Acetylsalicylic acid are: hypersensitivity to acetylsalicylic acid, other salicylates or to any component of the drug; bronchial asthma caused by a history of taking salicylates or other NSAIDs; acute gastrointestinal ulcers; hemorrhagic diathesis; severe renal failure; severe liver failure; severe heart failure; combination with methotrexate at a dose of 15 mg/week or more (see Section "Interaction with other drugs and other types of interactions").Pregnancy
Acetylsalicylic acid can be used during pregnancy only if other drugs are not effective and only after assessing the risk/benefit ratio.Suppression of prostaglandin synthesis may adversely affect pregnancy and/or embryonic/ intrauterine development. Available data epidemiological studies indicate the risk of miscarriage and fetal malformations after the use of prostaglandin synthesis inhibitors at the beginning of pregnancy. The risk increases with increasing dose and duration of therapy. According to research, the connection between taking acetylsalicylic acid and increased risk miscarriage not confirmed.
An increased risk of gastroschisis cannot be excluded when using acetylsalicylic acid. On early stages Pregnancy (1-4 months) has not been associated with an increased risk of developing malformations.
During the first and second trimesters of pregnancy, drugs containing acetylsalicylic acid should not be prescribed unless clearly clinically necessary. In women who are likely to be pregnant, or during the first and second trimesters of pregnancy, the dose of drugs containing acetylsalicylic acid should be as low as possible, and the duration of treatment should be shorter.
In the third trimester of pregnancy, all prostaglandin synthesis inhibitors can affect the fetus as follows:
- cardiopulmonary toxicity (with premature closure ductus arteriosus and pulmonary hypertension)
- impaired renal function with the possible subsequent development of renal failure with oligohydramnios.
Prostaglandin synthesis inhibitors can affect the woman and fetus at the end of pregnancy as follows:
- possibility of prolonging bleeding time, antiplatelet effect that can occur even after very low doses
- inhibition of uterine contractions, which can lead to a delay or increase in the duration of labor.
Despite this, acetylsalicylic acid is contraindicated in the third trimester of pregnancy.
There are certain indications that drugs that inhibit prostaglandin synthesis may interfere with reproductive function in women due to their effect on ovulation. This phenomenon is reversible and disappears after discontinuation of treatment.
Salicylates and their metabolites pass into breast milk in small quantities.
Since no adverse reactions were observed in infants whose mothers took acetylsalicylic acid, it is usually not necessary to interrupt breastfeeding. With long-term use of the drug or use of acetylsalicylic acid in high doses, the issue of stopping breastfeeding should be decided.
Interaction with other drugs
Combinations are contraindicated:Application acetylsalicylic acid with methotrexate at a dose of 15 mg/week or more increases the hematological toxicity of methotrexate (reduction of renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates from binding to plasma proteins).
Combinations to use with caution
When using acetylsalicylic acid with methotrexate at a dose of less than 15 mg/week, the hematological toxicity of methotrexate increases (decreased renal clearance of methotrexate by anti-inflammatory agents and displacement of methotrexate by salicylates from binding to plasma proteins).
The simultaneous use of ibuprofen prevents the irreversible inhibition of platelets by acetylsalicylic acid. Treatment of patients at risk of cardiovascular disease with ibuprofen may limit the cardioprotective effect of acetylsalicylic acid.
With the simultaneous use of high doses of salicylates with NSAIDs (due to their mutually complementary effect), the risk of ulcers and gastrointestinal bleeding increases.
With the simultaneous use of acetylsalicylic acid and anticoagulants, the risk of bleeding increases.
Simultaneous use with uricosuric drugs, such as benzobromarone, probenecid, reduces the effect of uric acid excretion (due to competition, the excretion of uric acid by the renal tubules).
When used simultaneously with digoxin, the concentration of the latter in the blood plasma increases due to a decrease in renal excretion.
With the simultaneous use of high doses of acetylsalicylic acid and oral antidiabetic drugs of the group of sulfonylurea derivatives or insulin, the hypoglycemic effect of the latter is enhanced due to the hypoglycemic effect of acetylsalicylic acid and the displacement of sulfonylurea bound to blood plasma proteins.
Diuretics in combination with high doses of acetylsalicylic acid reduce glomerular filtration due to a decrease in the synthesis of prostaglandins in the kidneys.
Systemic glucocorticosteroids (with the exception of hydrocortisone, which is used for replacement therapy with Addison's disease).
When using acetylsalicylic acid simultaneously with corticosteroids, the level of salicylates in the blood decreases and the risk of overdose increases after the end of treatment, as well as the risk of developing gastrointestinal bleeding.
ACE inhibitors in combination with high doses of acetylsalicylic acid cause a decrease glomerular filtration due to inhibition of vasodilator prostaglandins and a decrease in the hypotensive effect.
Selective serotonin reuptake inhibitors. There is an increased risk of upper gastrointestinal bleeding due to the possibility of a synergistic effect.
When used simultaneously with valproic acid, acetylsalicylic acid displaces it from its connection with blood plasma proteins, increasing the toxicity of the latter.
Ethyl alcohol causes damage to the mucous membrane of the gastrointestinal tract and prolongs bleeding time due to the synergy of acetylsalicylic acid and alcohol.
Overdose
Salicylate toxicity (use of more than 100 mg/kg/day for more than 2 days can lead to toxicity) is possible due to chronic intoxication resulting from long-term therapy, as well as due to acute intoxication (overdose), which is potentially life-threatening and the causes of which may be be, for example, accidental use by children or overdose.Chronic intoxication with salicylates can be hidden, since its symptoms are nonspecific. Moderate chronic intoxication caused by salicylates, or salicylicism, usually occurs only after repeated use of large doses.
Symptoms Dizziness, ringing in the ears, deafness, increased sweating, nausea and vomiting, headache, confusion. Symptoms mentioned can be controlled by reducing the dose. Tinnitus is possible when the concentration of salicylates in the blood plasma is more than 150-300 mcg/ml. More serious adverse reactions are observed when plasma concentrations of salicylates exceed 300 mcg/ml.
Acute intoxication is indicated by a pronounced change in the acid-base balance, which depends on the patient’s age and the severity of intoxication. In children, the most common manifestation is metabolic acidosis. The severity of the condition cannot be assessed solely on the basis of the concentration of salicylates in the blood plasma. Absorption of acetylsalicylic acid may slow down due to delayed gastric release and the formation of stones in the stomach.
Due to the complex pathophysiological effects, signs and symptoms of salicylate poisoning may include:
Intoxication from mild to moderate - tachypnea, hyperpnea, respiratory alkalosis; increased sweating, nausea and vomiting.
Intoxication from moderate to severe - respiratory alkalosis, which is accompanied by compensatory metabolic acidosis, hyperpyrexia. From the outside respiratory system: from hyperpnea, non-cardiogenic pulmonary edema to respiratory arrest and asphyxia. From the outside of cardio-vascular system: from arrhythmia, arterial hypotension to cardiac arrest. Dehydration, oliguria to renal failure, impaired glucose metabolism, ketosis are also observed; gastrointestinal bleeding hematological changes - from platelet inhibition to coagulopathy. From the nervous system: toxic encephalopathy and depression of the central nervous system, manifested in the form of drowsiness, depression of consciousness up to the development of coma and convulsions.
Changes in laboratory and other indicators: alkalemia, alkaluria, acidemia, aciduria, changes in blood pressure, ECG changes, hypokalemia, hypernatremia, hyponatremia, changes in renal function, hyperglycemia, hypoglycemia (especially in children). Increased level ketone bodies, hypoprothrombinemia.
Treatment of intoxication caused by an overdose of acetylsalicylic acid is determined by the severity, clinical symptoms and is provided standard methods, which are used for poisoning (gastric lavage, taking activated carbon, forced diuresis). All measures taken should be aimed at accelerating the removal of the drug and restoring the electrolyte and acid-base balance. Depending on the state of acid-base balance and electrolyte balance, infusion of electrolyte solutions is carried out. In case of serious poisoning, hemodialysis is indicated.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C.Keep out of the reach of children.
Release form
Acetylsalicylic acid - tablets.Package:
10 tablets in a blister, 10 tablets in a strip.
10 tablets per blister, 2 blisters per pack.
Compound
1 tablet Acetylsalicylic acid contains acetylsalicylic acid (calculated as 100% substance) 500 mg.Excipients: microcrystalline cellulose, croscarmellose sodium, colloidal silicon dioxide (aerosil), magnesium stearate, lemon flavor, citric acid.
Additionally
Acetylsalicylic acid use with caution when:- hypersensitivity to analgesic, anti-inflammatory, antirheumatic drugs, as well as in the presence of allergies to other substances;
- history of gastrointestinal ulcers, including chronic or recurrent peptic ulcer or a history of gastrointestinal bleeding
- simultaneous use of anticoagulants;
- impaired renal function or circulatory disorders (such as renal vascular disease, congestive heart failure, dehydration, major surgery, sepsis or significant blood loss), since acetylsalicylic acid may further increase the risk of kidney damage and cause acute renal failure
- liver dysfunction.
In patients with allergic complications, including bronchial asthma, allergic rhinitis, hives, skin itching, swelling of the mucous membrane and nasal polyposis, as well as when they are combined with chronic infections respiratory tract and in patients with hypersensitivity to NSAIDs during treatment with acetylsalicylic acid, bronchospasm, an attack of bronchial asthma or other allergic reactions may develop.
At surgical operations(including dental) the use of drugs containing acetylsalicylic acid may increase the likelihood of the appearance/intensification of bleeding, which is due to inhibition of platelet aggregation for some time after the use of acetylsalicylic acid.
When using small doses of acetylsalicylic acid, the excretion of uric acid may be reduced. This may lead to gout in patients with reduced uric acid excretion.
In patients with glucose-6-phosphate dehydrogenase deficiency, acetylsalicylic acid can cause hemolysis or hemolytic anemia. Factors that increase the risk of hemolysis include, for example, the use of high doses of the drug, fever or acute infections.
Long-term use of analgesics can lead to headaches.
Frequent use of painkillers may cause temporary impairment of kidney function with the risk of developing kidney failure (analgesic nephropathy). The risk is especially high when several different analgesics are used simultaneously.
For patients with concomitant liver or kidney dysfunction, it is necessary to reduce the dose of the drug or increase the interval between applications.
The drug is used for children over 15 years of age.
You should not use drugs containing acetylsalicylic acid in children with acute respiratory viral infections (ARVI), accompanied or not accompanied by an increase in body temperature, without consulting a doctor. For some viral diseases, especially for flu type A, flu type B and chicken pox, there is a risk of developing Reye's syndrome, which is a very rare but life-threatening disease and requires immediate attention medical intervention. The risk may be increased if acetylsalicylic acid is used as a concomitant drug, but a cause-and-effect relationship has not been proven in this case. If these conditions are accompanied by prolonged vomiting, this may be a sign of Reye's syndrome.
Main settings
| Name: | ACETYLSALICYLIC ACID |
| ATX code: | N02BA01 - |
For one tablet:
active substance: acetylsalicylic acid - 500.0 mg;
Excipients: talc, calcium stearate, citric acid monohydrate, colloidal anhydrous silicon dioxide, potato starch.
Pharmacotherapeutic group
Other analgesics and antipyretics. Salicylic acid and its derivatives.
ATS code: N02BA01.
pharmachologic effect"type="checkbox">
pharmachologic effect
Acetylsalicylic acid belongs to the group of acidic NSAIDs with analgesic, antipyretic and anti-inflammatory properties. The mechanism of its action is based on the irreversible inhibition of type I and II cyclooxygenases - enzymes involved in the synthesis of prostaglandins. In doses from 0.3 g to 1.0 g it is used for mild treatment and moderate pain and elevated temperature, for example, for colds or flu, to reduce fever and treat joint and muscle pain. Acetylsalicylic acid also inhibits platelet aggregation by blocking the synthesis of thromboxane Ag in platelets. For this reason, it is used in some cardiovascular diseases, in doses of 75-300 mg per day.
Indications for use
Fever;
- pain syndrome of weak and moderate intensity of various origins.
Directions for use and doses
To reduce the irritant effect on the gastrointestinal tract, the drug should be taken after meals with water, milk or alkaline mineral water. For pain of mild to moderate intensity and febrile conditions for children over 15 years of age and the elderly, a single dose is 500 mg (1 tablet), for adults - 1000 mg (2 tablets). If necessary, the drug can be taken 3 times a day with an interval of at least 4 hours. The maximum daily dose for children over 15 years of age is 1500 mg (3 tablets), for adults
- 3000 mg (6 tablets). You should not take the drug for more than 5 days as an analgesic and for more than 3 days as an antipyretic without a doctor’s prescription.
Side effect
When estimating frequency adverse reactions The following "gradation" is used:
Very common: ≥ 1/10;
Often:< 1/10, ≥ 1/100;
Infrequently:< 1/100, ≥ 1/1000;
Rarely:< 1/1000, ≥ 1/10000;
Very rarely:< 1/10000;
Unknown: Frequency cannot be estimated due to lack of data.
From the blood and lymphatic system:
Rare and very rare- serious bleeding, such as cerebral hemorrhage, especially in patients with uncontrolled hypertension and/or concomitant treatment with anticoagulants, which in some cases can be life-threatening.
Hemolysis and hemolytic anemia in patients with severe glucose-6-phosphate dehydrogenase deficiency.
Nose bleed, bleeding gums, skin bleeding or bleeding from the urogenital tract with a possible prolongation of bleeding time.
These effects persist for 4-8 days from the moment you stop taking the drug.
From the gastrointestinal tract:
Rarely- heartburn, nausea, vomiting, epigastric pain; erosive and ulcerative lesions (in rare cases can lead to perforation), gastrointestinal bleeding, which can lead to iron deficiency anemia, inflammatory conditions of the gastrointestinal tract.
From the central nervous system:
Dizziness, headache, tinnitus, decreased hearing, confusion (usually a sign of overdose).
From the skin and subcutaneous tissue:
Infrequently: skin hypersensitivity reactions such as skin rashes.
Rarely: severe skin hypersensitivity reactions (before the development of exudative erythema multiforme).
From the immune system:
Rarely: hypersensitivity reactions from the respiratory tract, gastrointestinal tract and cardiovascular system, especially in patients with asthma. May be observed following symptoms: arterial hypotension, asthma attacks, rhinitis, nasal congestion, anaphylactic shock or Quincke's edema.
Disorders of the liver and biliary tract:
Very rarely: increased levels of liver enzymes.
Renal and urinary tract disorders:
Renal impairment and acute renal failure have been reported.
Contraindications
Hypersensitivity to substances included in the drug; erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase); gastrointestinal bleeding; “aspirin” triad; hemorrhagic diathesis (hemophilia, von Willibrand's disease, telangiectasia, hypoprothrombinemia, thrombocytopenia, thrombocytopenic purpura); bronchial asthma induced by taking salicylates and other NSAIDs; dissecting aortic aneurysm; severe heart failure; portal hypertension; vitamin K deficiency; taking methotrexate at a dose of 15 mg per week or more; liver/renal failure; glucose-6-phosphate dehydrogenase deficiency; childhood (up to 15 years - the risk of developing Reye's syndrome in children with hyperthermia due to viral diseases); I and III trimesters of pregnancy and lactation.
Overdose
Overdose in the elderly and children requires special attention, since therapeutic overdose or accidental poisoning can be fatal in these patient groups.
Symptoms
Moderate overdose: ringing in the ears, hearing loss, sweating, nausea, vomiting, headache, dizziness. Symptoms disappear when the dosage is reduced.
Severe overdose: high temperature, hyperventilation, ketosis, respiratory alkalosis, metabolic acidosis, coma, cardiovascular failure, respiratory failure, severe hypoglycemia.
Actions in case of overdose
The patient must be taken to the hospital immediately.
Treatment
- gastric lavage, use of activated carbon, monitoring of acid-base balance;
- forced alkaline diuresis should be carried out at a plasma concentration of salicylates of 500 mg/l (3.6 mmol/l) in adults and 300 mg/l (2.2 mmol/l) in children. For severe poisoning, hemodialysis is indicated. Compensation for water loss is necessary;
- symptomatic treatment.
Precautionary measures
Care should be taken in following cases:
- at hypersensitivity to other analgesics, anti-inflammatory and antirheumatic drugs, in the presence of other types of hypersensitivity;
- if you have a history of allergies (for example, skin reactions, itching, urticaria), asthma, hay fever, nasal polyposis, or chronic respiratory diseases;
- at simultaneous treatment anticoagulants;
- for gastric ulcer and/or duodenum, erosive gastritis and a tendency to gastrointestinal bleeding;
- in patients with impaired liver function;
- in patients with impaired renal function and cardiovascular system ( vascular diseases kidney disease, chronic heart failure, dehydration, sepsis or severe bleeding), since acetylsalicylic acid may increase the risk of renal dysfunction and acute renal failure;
- before operations (even before such minor ones as tooth extraction), this may increase the risk of bleeding;
- in patients with glucose-6-phosphate dehydrogenase deficiency, acetylsalicylic acid may cause hemolysis or hemolytic anemia. Hemolysis can be triggered by high doses, fever or acute infections.
With constant use of painkillers, headaches may occur, which lead to repeated use. medicines and, in turn, can prolong the headache.
Chronic use of pain medications can cause permanent kidney damage with the risk of kidney failure (analgesic nephropathy). The risk increases when taking a combination of different pain medications.
Acetylsalicylic acid, even in small doses, reduces the excretion of uric acid from the body, which can cause the development acute attack gout in predisposed patients.
Acetylsalicylic acid should be used in febrile children and adolescents only for medical reasons and only if other measures are not effective. The occurrence of prolonged vomiting when using acetylsalicylic acid may be one of the signs of a life-threatening condition - Reye's syndrome, which requires immediate treatment.
Use during pregnancy and lactation
Use is contraindicated in the 1st and 3rd trimester of pregnancy and during lactation.
It has a teratogenic effect: when used in the first trimester, it leads to the development of cleft palate; in the third trimester causes inhibition labor activity(inhibition of PO synthesis), premature closure of the ductus arteriosus in the fetus, pulmonary vascular hyperplasia and hypertension in the pulmonary circulation. In the second trimester of pregnancy, occasional use of acetylsalicylic acid is allowed. It is excreted in breast milk, which increases the risk of bleeding in the baby due to impaired platelet function. Breastfeeding should be stopped during treatment.
Tablets with a flat surface, white, with a chamfer and a score. Marbling is allowed on the surface of the tablets.
Pharmacotherapeutic group
Other analgesics and antipyretics. Salicylic acid and its derivatives.
Acetylsalicylic acid.
ATX code N 02B A01
Pharmacological properties"type="checkbox">
Pharmacological properties
Pharmacokinetics
P After ingestion, acetylsalicylic acid is converted into the main metabolite - salicylic acid. Absorption of acetylsalicylic and salicylic acids in the digestive tract occurs quickly and
fully. The maximum level of concentration in the blood plasma is reached after 10-20 minutes (acetylsalicylic acid) or 45-120 minutes (total level of salicylates). The degree of binding of acids to plasma proteins depends on the concentration, which is 49-70% for acetylsalicylic acid and 66-98% for salicylic acid. 50% of the administered dose of the drug is metabolized during the initial passage through the liver. Metabolites of acetylsalicylic and salicylic acids are the glycine conjugant of salicylic acid, gentisic acid and its glycine conjugant. The drug is excreted from the body in the form of metabolites, mainly by the kidneys. The half-life of acetylsalicylic acid is 20 minutes. The half-life of salicylic acid increases in proportion to the dose taken and is 2, 4 and 20 hours for doses of 0.5 g, 1 g and 5 g respectively. The drug penetrates the blood-brain barrier and is also detected in breast milk and synovial fluid.
Pharmacodynamics
The drug has antipyretic, analgesic and anti-inflammatory effects, and also reduces platelet aggregation. The main mechanism of action of acetylsalicylic acid is the inactivation of the enzyme cyclooxygenase, as a result of which the synthesis of prostaglandins, prostacyclins and thromboxane is disrupted. Due to a decrease in the production of prostaglandins, their pyrogenic effect on thermoregulation centers is weakened. In addition, the sensitizing effect of prostaglandins on sensory nerve endings is reduced, which reduces their sensitivity to pain mediators. Irreversible disturbances in the synthesis of thromboxane A2 in platelets cause the antiplatelet effect of the drug. Acetylsalicylic acid also blocks cyclooxygenases of endothelial cells, in which prostacyclin, which has antiplatelet activity, is synthesized. Cyclooxygenases of endothelial cells are less sensitive to the action of acetylsalicylic acid and, unlike a similar platelet enzyme, are blocked reversibly.
Indications for use
Pain syndrome of weak and moderate intensity of various etiologies (including inflammatory) genesis
Increased temperature (fever) due to influenza, colds (ARVI) and other infectious and inflammatory diseases
Directions for use and doses
Acetylsalicylic acid is taken orally, after meals, with plenty of water.
For pain and fever during infectious and inflammatory diseases, a single dose for adults and children over 15 years of age is 0.5 - 1 g. The maximum daily dose is 3 g. For older people, the maximum daily dose is 1 g.
The duration of treatment should not exceed 5 days as an analgesic and 3 days as an antipyretic.
In patients with concomitant impairment of liver and kidney function, it is necessary to reduce the dose or increase the interval between taking the drug.
Side effects
Tinnitus, dizziness, hearing loss, visual impairment
Nausea, abdominal pain, heartburn, vomiting
Anorexia
Reye/Reye syndrome (encephalopathy combined with acute fatty liver)
Hypersensitivity reaction (bronchospasm, skin rash, Quincke's edema, urticaria, aspirin-induced asthma)
Interstitial nephritis, prerenal azotemia with increased blood creatinine and hypercalcemia, acute renal failure, nephrotic syndrome
Papillary necrosis
Breathing problems
Drowsiness
Convulsions
Erosive and ulcerative lesions of the digestive tract, sometimes complicated by latent or clinically pronounced (melena) bleeding, liver failure
Increased symptoms of congestive heart failure
Thrombocytopenia, leukopenia, anemia
Aseptic meningitis
Increased aminotransferase levels
Contraindications
Hypersensitivity to acetylsalicylic and salicylic acid
Peptic ulcer of the stomach and duodenum
Increased tendency to bleed
Kidney disease, renal and/or liver dysfunction
Concomitant treatment with anticoagulants (except for low-dose heparin therapy with frequent and careful monitoring of blood clotting)
Glucose-6-phosphate dehydrogenase deficiency
Bronchial asthma
Chronic or recurrent dyspeptic symptoms
History of erosive and ulcerative lesions of the upper gastrointestinal tract
Gastrointestinal bleeding
- “aspirin” bronchial asthma and “aspirin” triad
Vitamin K deficiency, hypoprothrombinemia
Dissecting aortic aneurysm
Pregnancy period and lactation period
Portal hypertension
Taking methotrexate at a dose of 15 mg/week or more
Childhood and adolescence up to 15 years
Drug interactions
With the simultaneous use of acetylsalicylic acid and anticoagulants, the risk of bleeding increases. With the simultaneous use of acetylsalicylic acid and non-steroidal anti-inflammatory drugs, the therapeutic and side effects of the latter are enhanced. During treatment with acetylsalicylic acid, the side effects of methotrexate are aggravated. With the simultaneous use of acetylsalicylic acid and oral antidiabetic drugs from the group of sulfonylurea derivatives, the hypoglycemic effect of the latter is enhanced. When used simultaneously with corticosteroids, the risk of developing gastrointestinal bleeding. Acetylsalicylic acid weakens the effect of spironolactone, furosemide, antihypertensive drugs and agents that promote the removal of uric acid.
Prescribing antacids during treatment with acetylsalicylic acid (especially in doses exceeding 3 g of acetylsalicylic acid for adults and 1.5 g for children) can reduce high steady-state levels of salicylates in the blood.
special instructions
Special Warnings and Cautions
The drug is not prescribed to children and adolescents under 15 years of age with acute respiratory diseases caused by viral infections, with diseases accompanied by hyperthermia due to the risk of developing Reye/Rea syndrome.
In patients with allergic diseases, including bronchial asthma, allergic rhinitis, urticaria, itching, swelling of the mucous membrane and nasal polyposis, as well as when they are combined with chronic respiratory tract infections and in patients with hypersensitivity to non-steroidal anti-inflammatory drugs during treatment with acetylsalicylic acid, attacks may develop bronchial asthma.
Use during surgical interventions. Before any surgical procedure, inform your doctor, surgeon, anesthesiologist or dentist that you are taking acetylsalicylic acid. 5-7 days before the planned surgical intervention, it is necessary to stop taking acetylsalicylic acid to reduce the risk of bleeding during surgery and the postoperative period.
During the period of use of the drug you should refrain from drinking alcohol.
Use during pregnancy
Inhibition of prostaglandin synthesis may have negative effects on pregnancy and embryonic or fetal development. Data from epidemiological studies indicate an increased risk of developing defects and malformations when using synthesis inhibitors
prostaglandins on early periods pregnancy. It is believed that the risk increases with increasing dose and duration of treatment.
Animal studies have shown reproductive toxicity; therefore, the use of drugs containing acetylsalicylic acid during pregnancy is not indicated.
The action of any complex and multicomponent drug is based on the properties of each of its individual elements. And if a pharmaceutical novelty can be expensive, then very often it is possible to purchase separately the main component of the drug and use it exclusively, saving a considerable amount. Among such simple and effective substances, it is worth highlighting acetylsalicylic acid, known to everyone. The drug has been used for many years as a remedy for pain and inflammation, and during all this time many more ways to use it have been found. Let's consider all aspects of using the tool in more detail.
Acetylsalicylic acid - what is it?
Acetylsalicylic acid is a derivative of salicylic acid that is used for medical purposes as a non-steroidal anti-inflammatory drug and a product for preventing the aggregation of blood cells. The substance itself is represented by white needle-shaped crystals or fine white powder, which has no distinct odor and easily dissolves in water and alcohol at temperatures above room temperature. It is offered to patients in tablet form, usually at a dosage of 500 mg per tablet.
Composition and effect of the drug
As already mentioned, acetylsalicylic acid is a tablet form of the substance, which is nothing more than just a compressed block active substance with the addition of several additional components (namely, potato starch, citric and stearic acid, talc and anhydrous silicon dioxide). The drug belongs to the group of analgesics and antipyretics.
Acid has an effect on the body in several directions: it helps fight inflammatory processes, relieves the intensity of painful sensations, lowers temperature and prevents blood platelets from sticking together (the so-called anti-aggregation effect). The anti-inflammatory effect of the drug develops over 24-48 hours of regular use, and the product also noticeably weakens painful sensations at rest and during motor acts, has a positive effect on morning mobility and improves joint function, relieving their swelling. The drug is able to relieve even spontaneous pain, which can occur during movement or in the postoperative period. At the wound site, taking acetylsalicylic acid helps reduce the intensity of swelling and inflammation.
Why is the drug prescribed: indications
Considering all the properties of the drug in question, it is not surprising that there are many indications for its use:
- febrile syndrome;
- the need to prevent myocardial infarction in coronary artery disease;
- diseases of the musculoskeletal system, which are accompanied by pain;
- headache, dental, menstrual, muscle pain, neuralgia;
- prevention of blood clots;
- acute thrombophlebitis (inflammation of the walls of the vein and the formation of a blood clot blocking its lumen);
- rheumatoid arthritis;
- rheumatic fever and pericarditis.
Instructions for use and dosage
The instructions indicate that the tablets are intended to be taken orally. You need to drink them if there is an appropriate need after eating, drinking or plain water, or milk. The standard dosage for adults is 1-2 tablets up to 4 times a day (maximum 1000 mg at a time). The maximum daily dose is 6 tablets (that’s 3 grams of the substance), an overdose of the drug is very dangerous. However, it is not recommended to take the product for longer than two weeks in a row.
Regarding patients childhood, then the drug cannot be taken until two years of age; a single dose for a child over 2 years old is 100 mg, over 3 years old – 150 mg, and so on, 50 mg per 1 year of age until adult dosages are reached.
How to take for blood thinning
People often hear the expression “thick blood,” but you shouldn’t take it literally. Liquid plasma tissue is formed by red blood cells, platelets and white blood cells, and each of these elements has its own functions. The problem of blood thickening is caused by difficulties with platelets - under the influence of certain factors, they begin to clot more actively, and as a result, dangerous blood clots form.
Acetylsalicylic acid helps prevent platelets from sticking together in liquid tissue, thereby being used as an element in the prevention of thrombosis and how. The action of the drug is aimed at improving blood microcirculation, but at the same time, long-term use of it can result in problems with the digestive tract. Thus, only a doctor can prescribe this method. For prevention, a dose of 200-250 mg per day is usually prescribed (half a tablet for several months), and in emergency situations it can be increased three times.
How to take pills for headaches
Pain syndrome of mild to moderate intensity is one of the indications for using the product. If you are worried about a headache, then an adult can take half or a whole tablet. If the situation does not improve, it is allowed readmission after 4 hours and no more than 2 tablets at a time. The daily maximum dose remains the same – 6 tablets, no more.
Acetylsalicylic acid in cold tablets
Aspirin (this is the same as acetylsalicylic acid) can be used as part of the treatment of colds, but the drug will not help cope with the cause of the problem, it will only be useful as an element symptomatic treatment. So, the tablets will help cope with the temperature, and will also help relieve aching joints and headaches. Reception in such a situation is carried out according to standard recommendations.
How to use aspirin for fever
If you have hyperthermia, it is recommended to take 1-2 tablets at a time. If there is such a need, then you can take up to 4 times a day with an interval of at least 4 hours, but again, do not forget about the maximum daily dose 6 aspirin tablets for an adult. For fever, the child is given part of the tablet in accordance with the age recommendations described earlier. It is worth remembering that acid has an irritating effect on the digestive system, so it is recommended to take it only after meals - this way the impact will be minimal.
For a hangover
At hangover syndrome The ability of acid to thin the blood turns out to be useful, since drinking alcohol has the opposite effect - it increases the viscosity of liquid tissue. Thus, taking the pill helps to lower the pressure inside the skull, as well as relieve swelling, that is, their use as part of getting rid of a hangover is effective and possible.
It’s worth noting right away that it is strictly forbidden to take acid together with alcohol, as this can lead to stomach bleeding. For withdrawal symptoms, it is best to take an effervescent aspirin tablet (for example, Upsarin-Upsa), which must be dissolved in water. This additionally helps minimize the symptoms of dehydration.
For toothache
Aspirin cannot be called the most popular drug for toothache, but it is very successfully used for this purpose. It is worth understanding that the tablet will have a positive effect on the inflammatory process and will partially relieve pain, but if the sensations are too pronounced, then there may not be an analgesic result. During an attack of toothache, you can take 1-2 tablets after meals.
During menstruation
Women's periods are often accompanied by severe pain, and they have to be dealt with with the help of medications. The remedy in question may be useful in such a situation, but only if the pain syndrome is not too intense. So, to get the best results, it is recommended to take the tablets for 3-4 days, starting 2 days before the start of menstruation and drinking 1 tablet 2 times a day.
From pressure
It is worth understanding that aspirin is not a drug for blood pressure, since it does not directly affect it. But this remedy can be prescribed if there are complications hypertension to thin the blood, as mentioned earlier.
Use for acne on the face
Using aspirin tablets on the face is a common practice. The mask helps you listen inflammatory processes, get rid of acne, cleanse pores, remove excess sebum and slightly dry the oily surfaces of the face. To prepare the product, you need to crush 5 tablets of the drug and mix the resulting powder with a tablespoon of liquid honey and half a teaspoon of jojoba oil. The resulting composition is applied to the skin for a quarter of an hour, after which it is removed with warm water.
Aspirin during pregnancy and breastfeeding
The drug cannot be called harmless to the fetus. Thus, during the first trimester, taking such acid is associated with an increased likelihood of the baby developing various defects, including the formation of cleft palate. During the second trimester, admission is possible, but only in the presence of acute indications and with the permission of the doctor; in the last period of gestation, admission is completely prohibited.
As for breastfeeding, the substance can partially pass into breast milk, but usually does not cause any side effects in the child, so a one-time dose does not require stopping the feeding process. But using pills in the form of a course can lead to certain difficulties, so doctors usually recommend stopping feeding.
Contraindications and side effects
Despite its versatility in use, the drug in question has many limitations in use. Thus, it cannot be used in cases of hypersensitivity to the components of the composition, the acute phase of a gastrointestinal ulcer, bleeding in the digestive system, aortic aneurysm with dissection, vitamin K deficiency in the body, disruption of the normal functioning of the liver and kidneys, gout. As for use to reduce fever, tablets cannot be used for this purpose in children under 15 years of age if hyperthermia is a consequence of a viral disease (for example, influenza).
Side effects may occur when taking the drug, and they are quite serious, so this once again confirms that only the attending physician can prescribe therapy with such a drug. So, to the number possible consequences include:
- nausea and vomiting, strong pain in the abdominal area, stool liquefaction;
- the appearance or intensification of headaches, the appearance of tinnitus and dizziness;
- in the presence of bleeding, the time to stop it may be prolonged, since the drug reduces the degree of platelet aggregation;
- bronchospasm, Quincke's edema;
- the appearance of a rash on the skin;
- increased symptoms chronic diseases hearts;
- disruption of the normal functioning of the urinary system.
Analogs
It is necessary to clarify that acetylsalicylic acid is a substance that is part of many modern drugs as an active ingredient, and its separate tablet form is the most affordable option. In this case, it would be more appropriate to talk not about analogues, but about drugs that contain acid: Aspicard, Aspirin, Acecardol, Bufferin, Cardiopyrin, Thrombo ACC, Sanovasc, Upsarin-UPSA, Fluspirin, etc.
Video: what aspirin tablets help with
There is a lot of information about Aspirin regarding methods and options for its use for human health. But it is important to understand that this is not a universal medicine, and it only has a certain list of problems that it can cope with.
