Buy Acetylsalicylic acid pills 500 mg 20 pcs
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Acetylsalicylic acid

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2019-09-19
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Clinical Pharmacology

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 by suppressing the synthesis of thromboxane A2 in platelets.

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 suppresses 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.

Indications

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.

In clinical immunology and allergology: in gradually increasing doses for prolonged "aspirin" desensitization and the formation of stable tolerance to NSAIDs in patients with "aspirin" asthma and the "aspirin triad".

Composition

1 tablet contains:
active substance: acetylsalicylic acid 500 mg.
Excipients: potato starch, stearic acid, citric acid, talc.

Acetylsalicylic acid is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Acetylsalicylic acid Pharmstandard Russia pills
CardiASK Canonpharma Russia pills
Acecardol Synthesis AKOMP Russia pills
Thrombo ASS G.L.Farma GmbH Austria pills
Aspirin Bayer Pharma AG Germany effervescent pills
Trombopol Polpharma Poland pills
Aspicore Vertex Russia pills
Upsarin UPSA UPSA SAS France effervescent pills

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Acetylsalicylic acid

Dosage and Administration

Orally, adults and children over 12 years of age: a single dose is 0.25-0.5 g, the maximum single dose is 1.0 g (2 pills of 0.5 g each), the maximum daily dose is 3.0 g (6 pills of 0.5 g) a single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours. Children, with the exception of acute respiratory diseases caused by viral infections, due to the risk of Reye's syndrome (encephalopathy and acute fatty liver with acute development of liver failure): single dose for children aged 3 years - 0.125 g (1/2 tablet 250 mg), from the age of 6, can be prescribed in pills of 0.25 g per dose.

The drug should be taken after meals with water, milk or alkaline mineral water.
Frequency and time of admission: 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 intake mode allows you to avoid a sharp increase in temperature and reduce the intensity of the pain syndrome.
The duration of treatment (without consulting a physician) should not exceed 7 days when prescribed as an anesthetic and more than 3 days as an antipyretic.

Adverse reactions

On the part of the digestive system: nausea, vomiting, anorexia, epigastric pain, diarrhea; rarely - the occurrence of erosive and ulcerative lesions, bleeding from the gastrointestinal tract, abnormal liver function.

On the part of the central nervous system: with prolonged use, dizziness, headache, reversible visual impairment, tinnitus, aseptic meningitis are possible.

From the hematopoietic system: rarely - thrombocytopenia, anemia.

On the part of the blood coagulation system: rarely - hemorrhagic syndrome, prolongation of bleeding time.

On the part of the urinary system: rarely - impaired renal function; with prolonged use - acute renal failure, nephrotic syndrome.

Allergic reactions: rarely - skin rash, angioedema, bronchospasm, "aspirin triad" (a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid and pyrazolone drugs).

Other: in some cases - Reye's syndrome; with prolonged use - increasing the symptoms of chronic heart failure.

Contraindications

Erosive and ulcerative gastrointestinal lesions in the acute phase, gastrointestinal bleeding, "aspirin triad", a history indication urticaria, rhinitis, caused by the intake of aspirin and other NSAIDs, hemophilia, hemorrhagic diathesis, hypoprothrombinemia, dissecting aortic aneurysm, portal hypertension, vitamin K deficiency, hepatic and / or renal failure, deficiency of glucose-6-phosphate dehydrogenase, Reye's syndrome, children age (up to 15 years old - the risk of Reye's syndrome in children with hyperthermia in the presence of viral illnesses tions), I and III trimesters of pregnancy, lactation, hypersensitivity to acetylsalicylic acid and other salicylates.

Drug interactions

With the 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, agents that limit calcium intake or increase the excretion of calcium from the body, the risk of bleeding increases.

With simultaneous use with acetylsalicylic acid, the effect of heparin and indirect anticoagulants, hypoglycemic agents of sulfonylurea derivatives, insulins, methotrexate, phenytoin, valproic acid, is enhanced.

With simultaneous use with corticosteroids increases the risk of ulcerogenic action and the occurrence of gastrointestinal bleeding.

With simultaneous use decreases the effectiveness of diuretics (spironolactone, furosemide).

With the simultaneous use of other NSAIDs increases the risk of side effects. Acetylsalicylic acid can reduce plasma concentrations of indomethacin, piroxicam.

When used simultaneously with gold preparations, acetylsalicylic acid may induce liver damage.

With simultaneous use, the effectiveness of uricosuric drugs (including probenecid, sulfinpyrazone, benzbromarone) decreases.

With simultaneous use of acetylsalicylic acid and alendronate sodium, the development of severe esophagitis is possible.

With the simultaneous use of griseofulvina possible violation of the absorption of acetylsalicylic acid.

The case of spontaneous hemorrhage into the iris when taking an extract of ginkgo biloba on the background of long-term use of acetylsalicylic acid at a dose of 325 mg / day is described. It is believed that this may be due to an additive inhibitory effect on platelet aggregation.

With the simultaneous use of dipyridamole may increase C max salicylate in the blood plasma and AUC.

With simultaneous use with acetylsalicylic acid, the concentrations of digoxin, barbiturates and lithium salts in the blood plasma increase.

With the simultaneous use of salicylates in high doses with carbonic anhydrase inhibitors, intoxication with salicylates is possible.

Acetylsalicylic acid in doses of less than 300 mg / day has a slight effect on the effectiveness of captopril and enalapril. When using acetylsalicylic acid in high doses, it is possible to reduce the effectiveness of captopril and enalapril.

With the simultaneous use of caffeine increases the rate of absorption, plasma concentration and bioavailability of acetylsalicylic acid.

With simultaneous use of metoprolol may increase the C max salicylate in the blood plasma.

When pentazocine is used during long-term administration of acetylsalicylic acid in high doses, there is a risk of severe adverse reactions from the kidneys.

With the simultaneous use of phenylbutazone reduces uricosuria caused by acetylsalicylic acid.

With simultaneous use of ethanol may enhance the effect of acetylsalicylic acid on the gastrointestinal tract.

Pregnancy and Lactation

Acetylsalicylic acid is contraindicated for use in I and III trimesters of pregnancy. In the II 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 the development of the upper palate splitting, in the third trimester it causes inhibition of labor activity (inhibition of prostaglandin synthesis), premature closure of the arterial duct in the fetus, hyperplasia of the pulmonary 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 dysfunction of platelets, so you should not use acetylsalicylic acid in the mother during lactation.

Special instructions

It is used with caution 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 while conducting anticoagulant 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 the use of acetylsalicylic acid in high doses requires the supervision of a physician and regular monitoring of 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 likelihood of side effects from the gastrointestinal tract.

Before surgery, to reduce bleeding during surgery and in the postoperative period, salicylates should be discontinued for 5-7 days.

During prolonged therapy it is necessary to carry out a general blood test 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 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 drinking alcohol.

Overdosage

Symptoms (single dose less than 150 mg / kg - acute poisoning is considered mild, 150-300 mg / kg - moderate, more than 300 mg / kg - severe): syndrome of salicilism (nausea, vomiting, tinnitus, blurred vision, dizziness, severe headache, malaise, fever - a bad prognostic sign in adults). Severe poisoning - central pulmonary hyperventilation, respiratory alkalosis, metabolic acidosis, confusion, drowsiness, collapse, convulsions, anuria, bleeding. Initially, central hyperventilation of the lungs leads to respiratory alkalosis - shortness of breath, asphyxiation, cyanosis, cold, sticky sweat; with increased intoxication, respiratory paralysis and dissociation of oxidative phosphorylation increase, causing respiratory acidosis.

In chronic overdose, the concentration determined in plasma correlates poorly with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly when taking more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicilism are not always visible, so it is advisable to periodically determine the concentration of salicylates in the blood: a level above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about the extremely severe, prognostically unfavorable. In case of moderate poisoning, hospitalization is required for 24 hours. Treatment: provocation of vomiting, administration of activated carbon and laxatives, constant monitoring of EC and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate, sodium citrate solution or sodium lactate. Increased reserve alkalinity enhances the excretion of ASA due to alkalization of urine. Alkalinization of urine is shown at the level of salicylates above 40 mg% and is provided by IV infusion of sodium bicarbonate (88 mEq per 1 l of 5% dextrose solution, at a rate of 10-15 ml / h / kg); the restoration of bcc and induction of diuresis are achieved by the introduction of sodium bicarbonate in the same doses and dilution, which is repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion can lead to pulmonary edema. The use of acetazolamide for alkalinization of urine is not recommended (it can cause acidemia and increase the toxic effect of salicylates). Hemodialysis is indicated at a salicylate level of more than 100-130 mg%, in patients with chronic poisoning - 40 mg% and lower if indicated (refractory acidosis, progressive deterioration of the condition, severe damage to the central nervous system, pulmonary edema, and renal failure). When pulmonary edema - mechanical ventilation mixture enriched with oxygen

  • Brand name: ACC
  • Active ingredient: Acetylcysteine
  • Manufacturer: Sandoz

Studies and clinical trials of Acetylsalicylic acid (Click to expand)

  1. Triphenyltin(IV) compounds with biologically active anionic groups: Crystal and molecular structures of the p-ethoxybenzoic acid, acetylsalicylic acid, phthalic acid and salicylaldehyde derivatives
  2. A population-based case–control teratologic study of acetylsalicylic acid treatments during pregnancy
  3. The influence of hydroxyethylcellulose on the diffusion of acetylsalicylic acid trihydromagnesium salt in aqueous solution
  4. Acetylsalicylic acid loading and release studies of the PMMA-g-polymeric oils/oily acids micro and nanospheres
  5. Thiolkatalysierte Hydrolyse von Acetylsalizylsäure. Hydrolysis of Acetylsalicylic Acid Catalyzed by Thiols
  6. Synthesis, Characterisation and Biological Evaluation of Copper and Silver Complexes based on Acetylsalicylic Acid
  7. Therapeutic effects of acetylsalicylic acid in giant cell arteritis
  8. Plasma and synovial fluid concentrations of acetylsalicylic acid in patients with rheumatoid arthritis
  9. The inhibitory effect of salicylate on the acetylation of human albumin by acetylsalicylic acid
  10. Urinary pH and plasma levels of salicylate after administration of different buffered acetylsalicylic acid formulations
  11. Comparison of two enteric-coated acetylsalicylic acid preparations by monitoring steady-state levels of salicylic acid and its metabolites in plasma and urine
  12. Acetylsalicylic acid metabolites in blood and urine after plain and enteric-coated tablets
  13. A pharmacokinetic approach to the establishment of biopharmaceutic characteristics of different acetylsalicylic acid formulations in man
  14. Comparison of developmental toxicology of aspirin (Acetylsalicylic Acid) in rats using selected dosing paradigms
  15. Rapid and sensitive determination of acetylsalicylic acid and salicylic acid in plasma using liquid chromatography–tandem mass spectrometry: application to pharmacokinetic study
  16. Determination of acetylsalicylic acid and its major metabolite, salicylic acid, in human plasma using liquid chromatography–tandem mass spectrometry: application to pharmacokinetic study of Astrix® in Korean healthy volunteers
  17. Profiles in altered metabolism. II—Accumulation of homogentisic acid in serum and urine following acetylsalicylic acid ingestion
  18. Heparin and coumadin versus acetylsalicylic acid for prevention of restenosis after coronary angioplasty
  19. ChemInform Abstract: Unexpected Transesterification of N-(Trifluoroacetyl) Doxorubicin with Acetylsalicylic Acid: Formation of 4′-O-Acetyl-N-(trifluoroacetyl) Doxorubicin.
  20. ChemInform Abstract: Synthesis of New Anthracycline Derivatives Containing Acetylsalicylic or Palmitic Acid Moiety.
  21. Seed loading effects on the mean crystal size of acetylsalicylic acid in a continuous-flow crystallization device
  22. Reversed-phase capillary electrochromatography for the simultaneous determination of acetylsalicylic acid, paracetamol, and caffeine in analgesic tablets
  23. Acetylsalicylic acid in the prevention of early stenosis and occlusion of transjugular intrahepatic portal-systemic stent shunts: A controlled study
  24. Acetylsalicylic acid inhibits hepatitis C virus RNA and protein expression through cyclooxygenase 2 signaling pathways

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