Ibuprofen

Mechanism of action

COX-1 / COX-2 inhibitor

In plain language

Blocks an enzyme called cyclooxygenase that the body uses to make prostaglandins — chemical signals that cause pain, swelling, and fever — so fewer of these signals get made.

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ClinicalPlain language

How it works

Ibuprofen is a nonselective NSAID that inhibits both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), the enzymes that convert arachidonic acid into prostaglandins. By lowering prostaglandin synthesis, it reduces the mediators that sensitize nerve endings to pain, drive local vasodilation and vascular permeability during inflammation, and act on the hypothalamus to raise body temperature during fever. COX-2 inhibition accounts for most of the analgesic, anti-inflammatory, and antipyretic effect, while COX-1 inhibition — which also normally protects gastric mucosa and supports platelet aggregation — underlies the drug's characteristic GI and bleeding-related side effects. This dual, non-selective COX inhibition is the basis for both ibuprofen's clinical benefit and its adverse-effect profile.

Therapeutic applications

Per FDA-approved labeling, ibuprofen is indicated for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis, for relief of mild to moderate pain, and for treatment of primary dysmenorrhea. Over-the-counter formulations carry additional labeling for temporary relief of minor aches from headache, toothache, backache, muscular aches, and the common cold, minor pain of arthritis, and for temporary reduction of fever.

Class

Small molecule

Therapeutic area

Analgesic / Anti-inflammatory

Source

PubChem CID 3672 ↗FDA label (DailyMed) ↗