Description

Simple

A painkiller used to treat pain, fever, inflammation, and migraines, as well as reduce the risk of heart attacks, strokes, and other events.

Clinical

A salicylate used to treat pain, fever, inflammation, migraines, and reducing the risk of major adverse cardiovascular events.

Overview

Also known as _Aspirin_, acetylsalicylic acid (ASA) is a commonly used drug for the treatment of pain and fever due to various causes. Acetylsalicylic acid has both anti-inflammatory and antipyretic effects. This drug also inhibits platelet aggregation and is used in the prevention of blood clots stroke, and myocardial infarction (MI) [FDA label].

Interestingly, the results of various studies have demonstrated that long-term use of acetylsalicylic acid may decrease the risk of various cancers, including colorectal, esophageal, breast, lung, prostate, liver and skin cancer [15]. Aspirin is classified as a _non-selective cyclooxygenase (COX) inhibitor_ [11, 14] and is available in many doses and forms, including chewable ta... Read more

Pharmacology

Indication

**Pain, fever, and inflammation**

Acetylsalicylic acid (ASA), in the regular tablet form (immediate-release), is indicated to relieve pain, fever, and inflammation associated with many conditions, including the flu, the common cold, neck and back pain, dysmenorrhea, headache, tooth pain, sprains,... Read more

Pharmacodynamic

**Effects on pain and fever**

Acetylsalicylic acid disrupts the production of prostaglandins throughout the body by targeting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) [ Read more

Mechanism of action

Acetylsalicylic acid (ASA) blocks prostaglandin synthesis. It is non-selective for COX-1 and COX-2 enzymes [9, Read more

Absorption


Absorption is generally rapid and complete following oral administration but absorption may be variable depending on the route, dosage form, and other factors including but not limited to the rate of tablet dissolution, gastric contents, gastric emptying time, and gastric pH [FDA label].

**Deta... Read more

Protein binding

50% to 90% of a normal therapeutic concentration salicylate (a main metabolite of acetylsalicylic acid [FDA label]) binds plasma proteins, particularly albumin, while acetylsalicylic acid itself binds negligibly [FDA label]. Acetylsalicylic acid has the ability to bind to and acetylate many proteins... Read more

Volume of distribution

This drug is distributed to body tissues shortly after administration. It is known to cross the placenta. The plasma contains high levels of salicylate, as well as tissues such as spinal, peritoneal and synovial fluids, saliva and milk. The kidney, liver, heart, and lungs are also found to be rich i... Read more

Clearance

The clearance rate of acetylsalicylic acid is extremely variable, depending on several factors [6]. Dosage adjustments may be required in patient... Read more

Half life

The half-life of ASA in the circulation ranges from 13 - 19 minutes. Blood concentrations drop rapidly after complete absorption. The half-life of the salicylate ranges between 3.5 and 4.5 hours [FDA label].

Route of elimination

Excretion of salicylates occurs mainly through the kidney, by the processes of glomerular filtration and tubular excretion, in the form of free salicylic acid, salicyluric acid, and, additionally, phenolic and acyl glucuronides [FDA label].

Salicylate can be found in the urine soon after adminis... Read more

Toxicity

**Lethal doses**

Acute oral LD50 values have been reported as over 1.0 g/kg in humans, cats, and dogs, 0.92 g/kg - 1.48 g/kg in albino rats, 1.19 g/kg in guinea pigs, 1.1 g/kg in mice, and 1.8 g/kg in rabbit models [FDA label].

**Acute toxicity**

Salicylate toxicity is a problem that may de... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Renal Failure, Acute Canada
Varying Reports
Transient elevations in hepatic enzymes Canada
Varying Reports
Thirst Canada
Sweating Canada
Drowsiness Canada
Mental confusion Canada
Anaphylactic shock Canada
Anaphylaxis reactions Canada
Asthma Canada
Skin eruptions Canada
Pruritis Canada
Urticaria Canada
Anemia, Hemolytic Canada
Hemolysis Canada
Leukopenia Canada
Thrombocytopenia Canada
Anemia Canada
Purpura Canada
Hearing Loss Canada
Vertigo Canada
Tinnitus Canada
Serious bleeding Canada
Cerebrovascular hemorrhage Canada
Gingival Bleeding Canada
Urogenital bleeding Canada
Epistaxis Canada
Hematoma Canada
Perioperative hemorrhage Canada
Abdominal Pain Canada
Gastrointestinal inflammation Canada
Melena Canada
Hematemesis Canada
Heartburn Canada
Diarrhea Canada
Vomiting Canada
Nausea Canada
Gastric ulceration US
Increased risk of bleeding US
Renal Failure US
Clinical Trial
Renal Insufficiency US
Clinical Trial
Allergic Reaction US
Reye's syndrome US
Gastric Bleeding US
Cerebral Edema US
Clinical Trial
Agitation US
Clinical Trial
Coma US
Clinical Trial
Confusion US
Clinical Trial
Dizziness US
Clinical Trial
Headache US
Clinical Trial
Lethargy US
Clinical Trial

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Sex Group: female
  • Regions: Canada
  • Patient Conditions:
      • Name: Third trimester of pregnancy
      • Drugbank Id: DBCOND0108315
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Recommended Actions:
    • Avoid co-administration of methotrexate at doses of 15mg/week.
  • Regions: Canada
  • With Drugs:
      • Name: Methotrexate
      • Drugbank Id: DB00563
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: History of asthma
      • Drugbank Id: DBCOND0107635
  • Patient Conditions Associated With:
      • Name: NSAID use
      • Drugbank Id: DBCOND0021294
      • Related Concepts:
          • Name: Antiinflammatory therapy
          • Drugbank Id: DBCOND0025182
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: History of asthma
      • Drugbank Id: DBCOND0107635
  • Patient Conditions Associated With:
      • Name: Salicylate use
      • Drugbank Id: DBCOND0119122
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Congestive Heart Failure
      • Drugbank Id: DBCOND0029751
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Renal Failure
      • Drugbank Id: DBCOND0029445
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Severe hepatic disease
      • Drugbank Id: DBCOND0107692
      • Modification Of:
        • Base:
          • Name: Hepatic Disease
          • Drugbank Id: DBCOND0069929
        • Severity:
          • Includes:
            • severe
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Hepatic Failure
      • Drugbank Id: DBCOND0042778
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Hemorrhagic diathesis
      • Drugbank Id: DBCOND0102909
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Hypersensitivity:
    • true
    • Antipyretics
  • Regions: Canada
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Hypersensitivity:
    • true
    • analgesics
  • Regions: Canada
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: Acute gastrointestinal ulceration
      • Drugbank Id: DBCOND0128794
      • Modification Of:
        • Base:
          • Name: Gastrointestinal ulceration
          • Drugbank Id: DBCOND0096568
        • Severity:
          • Includes:
            • acute
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: Canada
  • Patient Conditions:
      • Name: History of gastrointestinal ulcers
      • Drugbank Id: DBCOND0119121
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Hypersensitivity:
    • true
    • Salicylates
  • Regions: Canada
  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Regions: US
  • Patient Conditions:
      • Name: Polyps, Nasal
      • Drugbank Id: DBCOND0052432
  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Regions: US
  • Patient Conditions:
      • Name: Rhinitis
      • Drugbank Id: DBCOND0014062
  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Regions: US
  • Patient Conditions:
      • Name: Asthma
      • Drugbank Id: DBCOND0013565
  • Route:
    • Oral
  • Dose Form:
    • Capsule
    • Tablet
  • Hypersensitivity:
    • true
    • NSAIDs
  • Regions: US
  • Route:
    • Oral
  • Dose Form:
    • Capsule
    • Tablet
  • Hypersensitivity:
    • true
  • Regions: US

Food Interactions

Avoid alcohol. Alcohol increases the risk of gastrointestinal bleeding.

Take after a meal. This reduces irritating gastrointestinal effects.

Take with a full glass of water.