Description

Simple

A pain medication used to reduce fever, pain, and inflammation.

Clinical

An NSAID and non-selective COX inhibitor used to treat mild-moderate pain, fever, and inflammation.

Overview

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.[7] The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.[8] Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.[9]

On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer _in vivo_ by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.[Read more

Pharmacology

Indication

Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.[ Read more

Pharmacodynamic

Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is a... Read more

Mechanism of action

The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the ar... Read more

Absorption

It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.[ Read more

Protein binding

Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.[ Read more

Volume of distribution

The apparent volume of distribution of ibuprofen is of 0.1 L/kg.[25]

Clearance

The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.[ Read more

Half life

The serum half-life of ibuprofen is 1.2-2 hours.[10] In patients with a compromised liver function, the h... Read more

Route of elimination

Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.[ Read more

Toxicity

The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinni... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Epigastric Pain US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Heartburn US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3-9%
  • Clinical Trial
    Abdominal Cramps US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Fullness of GI tract US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Abdominal distress US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Indigestion US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Nausea and vomiting US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Decreased appetite US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Fluid retention US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Nervousness US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Tinnitus US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Gastric ulcer with bleeding or perforation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Scotomata US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Diminished vision US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Amblyopia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hearing Loss US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Alopecia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Stevens-Johnson Syndrome US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Erythema multiforme US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Eosinophilia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Thrombocytopenic Purpura US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Thrombocytopenia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hemolytic Anemia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Aplastic Anemia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Agranulocytosis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Changes in color vision US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Abnormal Liver Function Tests US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pancreatitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hepatitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Jaundice US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Melena US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Gastritis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Duodenal ulcer with bleeding or perforation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Gastrointestinal Hemorrhage US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Vesiculobullous eruptions US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Aseptic meningitis with fever and coma US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Regions: US
    • With Therapies:
        • Name: Coronary artery bypass graft (CABG) surgery
        • Drugbank Id: DBCOND0107829
    • Hypersensitivity:
      • aspirin
      • Anti-Inflammatory Agents, Non-Steroidal
    • Regions: US

    Food Interactions

    Avoid alcohol.

    Take with food. Food reduces irritation.