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Cited by 1,225Inflammatory mediators and NSAID effectsAntiplatelet Therapy and Cardiovascular DiseasesEicosanoids and Hypertension Pharmacology

The mechanism of action of aspirin

Vane, J.R, Botting, R.M·2003·Thrombosis Research
DOI 10.1016/s0049-3848(03)00379-7
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Abstract

The therapy of rheumatism began thousands of years ago with the use of decoctions or extracts of herbs or plants such as willow bark or leaves, most of which turned out to contain salicylates. Following the advent of synthetic salicylate, Felix Hoffman, working at the Bayer company in Germany, made the acetylated form of salicylic acid in 1897. This drug was named "Aspirin" and became the most widely used medicine of all time. In 1971, Vane discovered the mechanism by which aspirin exerts its anti-inflammatory, analgesic and antipyretic actions. He proved that aspirin and other non-steroid anti-inflammatory drugs (NSAIDs) inhibit the activity of the enzyme now called cyclooxygenase (COX) which leads to the formation of prostaglandins (PGs) that cause inflammation, swelling, pain and fever. However, by inhibiting this key enzyme in PG synthesis, the aspirin-like drugs also prevented the production of physiologically important PGs which protect the stomach mucosa from damage by hydrochloric acid, maintain kidney function and aggregate platelets when required. This conclusion provided a unifying explanation for the therapeutic actions and shared side effects of the aspirin-like drugs. Twenty years later, with the discovery of a second COX gene, it became clear that there are two isoforms of the COX enzyme. The constitutive isoform, COX-1, supports the beneficial homeostatic functions, whereas the inducible isoform, COX-2, becomes upregulated by inflammatory mediators and its products cause many of the symptoms of inflammatory diseases such as rheumatoid and osteoarthritis.

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Crossref · 10.1016/s0049-3848(03)00379-7

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34 of 34 references verified0 citation errors · 0 not checkable

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  • Aspirin was used for about 70 years for its antipyretic, analgesic, and anti-inflammatory clinical effects, but its pharmacological mechanisms were not understood until later.

    “aspirin was used for about 70 years for its antipyretic, analgesic, and anti-inflammatory clinical effects, but its pharmacological mechanisms were not understood until later [93, 94].”

    From Ethics and governance of trustworthy medical artificial intelligence (2023) · cites this paper as [94]

  • Many drugs used in clinics may not be fully understood initially.

    “Many of the drugs used in clinics may not be fully understood initially.”

    From Ethics and governance of trustworthy medical artificial intelligence (2023) · cites this paper as [94]

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Authors
Vane, J. R., & Botting, R. M.
Affiliations
William Harvey Research Institute (GB)
Venue
Thrombosis Research
Publisher
Elsevier BV
Published
2003-06
Volume
110
Issue
5-6
Pages
255-258
ISSN
0049-3848 (ISSN-L)
DOI
10.1016/s0049-3848(03)00379-7
OpenAlex
W2037182281
Cited by
1,225
References
34
Citations by year
2026: 48 · 2025: 82 · 2024: 87 · 2023: 99 · 2022: 84 · 2021: 71 · 2020: 78 · 2019: 62 · 2018: 68 · 2017: 61 · 2016: 65 · 2015: 53 · 2014: 56 · 2013: 50 · 2012: 36
FWCI
2.27
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Thrombosis Research (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Pharmacology › Inflammatory mediators and NSAID effects
  • Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Antiplatelet Therapy and Cardiovascular Diseases
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Eicosanoids and Hypertension Pharmacology
Keywords
aspirin, mechanism of action, salicylates, cyclooxygenase, cyclooxygenase-1, cyclooxygenase-2, prostaglandins, nonsteroidal anti-inflammatory drugs, anti-inflammatory activity, analgesia, fever reduction, gastroprotection, platelet aggregation, rheumatism, history of aspirin
MeSH terms
Animals, Anti-Inflammatory Agents, Non-Steroidal, Aspirin, Humans, Inflammation, Isoenzymes, Membrane Proteins, Pain, Platelet Aggregation Inhibitors, Prostaglandin-Endoperoxide Synthases, Prostaglandins, Thrombosis, Cyclooxygenase Inhibitors, Analgesics, Non-Narcotic, Cyclooxygenase 1, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors

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