Diclofenac

Diclofenac
Clinical data
Trade namesCataflam, Voltaren, Zipsor, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa689002
License data
Pregnancy
category
Routes of
administration
By mouth, rectal, intramuscular, intravenous, topical
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only) / S3 / S2
  • CA: ℞-only[4]
  • UK: POM (Prescription only) / P / GSL
  • US: WARNING[3]Rx-only / OTC[5]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein bindingMore than 99%
MetabolismLiver, oxidative, primarily by CYP2C9, also by CYP2C8, CYP3A4, as well as conjugative by glucuronidation (UGT2B7) and sulfation;[9] no active metabolites exist
Onset of actionWithin 4 hours (gel),[6] 30 min (non-gel)[7]
Elimination half-life1.2–2 h (35% of the drug enters enterohepatic recirculation)
Excretion35% bile, 65% urine[8]
Identifiers
  • [2-(2,6-Dichloroanilino)phenyl]acetic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.035.755 Edit this at Wikidata
Chemical and physical data
FormulaC14H11Cl2NO2
Molar mass296.15 g·mol−1
3D model (JSmol)
  • O=C(O)Cc1ccccc1Nc2c(Cl)cccc2Cl
  • InChI=1S/C14H11Cl2NO2/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19/h1-7,17H,8H2,(H,18,19) checkY
  • Key:DCOPUUMXTXDBNB-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Diclofenac (pronounced /dˈklfənæk/[1] or /dɪklɒˈfɛnæk/[10]), sold under the brand name Voltaren, among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammatory diseases such as gout.[7] It is taken by mouth or rectally in a suppository, used by injection, or applied to the skin.[7][11] Improvements in pain last for as much as eight hours.[7] It is also available in combination with misoprostol in an effort to decrease stomach problems.[12]

Common side effects include abdominal pain, gastrointestinal bleeding, nausea, dizziness, headache, and swelling.[7] Serious side effects may include heart disease, stroke, kidney problems, and stomach ulceration.[12][7] Use is not recommended in the third trimester of pregnancy.[7] It is likely safe during breastfeeding.[12] Diclofenac is believed to work by decreasing the production of prostaglandins, like other drugs in this class.[13]

In 2021, diclofenac was the 61st most commonly prescribed medication in the United States, with more than 11 million prescriptions.[14][15] It is available as its acid or in two salts, as either diclofenac sodium or potassium.[12]

It is also widely used for livestock; such use was responsible for the Indian vulture crisis, during which in a few years 95% of the country's vulture population was killed, and in many countries agricultural use is now forbidden.[16][17][18][19]

  1. ^ a b Cite error: The named reference tn was invoked but never defined (see the help page).
  2. ^ "Diclofenac Use During Pregnancy". Drugs.com. 16 January 2000. Retrieved 18 February 2024.
  3. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  4. ^ "Product monograph brand safety updates". Health Canada. 6 June 2024. Retrieved 8 June 2024.
  5. ^ "FDA Approves Three Drugs for Nonprescription Use Through Rx-to-OTC Switch Process". Food and Drug Administration. 14 February 2020. Retrieved 18 February 2024. Public Domain This article incorporates text from this source, which is in the public domain.
  6. ^ "How Long Does It Take for Voltaren Gel to Work?". YouDrugstore. Retrieved 18 February 2024.
  7. ^ a b c d e f g "Diclofenac epolamine Monograph for Professionals". Drugs.com. Retrieved 18 February 2024.
  8. ^ Williams BS, Buvanendran A (1 January 2011). "Nonopioid analgesics: NSAIDs, COX-2 inhibitors, and acetaminophen". In Benzon HT, Raja SN, Liu SS, Fishman SM (eds.). Essentials of Pain Medicine (3 ed.). W.B. Saunders. pp. 130–139. doi:10.1016/b978-1-4377-2242-0.00026-2. ISBN 978-1-4377-2242-0. Archived from the original on 10 January 2023. Retrieved 10 January 2023.
  9. ^ Sayyad M (23 August 2018). "Diclofenac Oral Uses, Dosage, Side Effects And Composition". Medicine Reviews Agency. Archived from the original on 24 August 2018. Retrieved 18 February 2024.
  10. ^ O'Toole MT, ed. (2017). Mosby's Dictionary of Medicine, Nursing & Health Professions (10th ed.). Elsevier. p. 536. ISBN 978-0-323-22205-1.
  11. ^ Chung CH (2017). "The use of Injectable Nonsteroidal Anti-Inflammatory Drugs in Local Accident & Emergency Practice". Hong Kong Journal of Emergency Medicine. 9 (2): 65–71. doi:10.1177/102490790200900201. S2CID 74032271.
  12. ^ a b c d British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. pp. 1033–1035. ISBN 978-0-85711-298-9.
  13. ^ Mosby's Drug Reference for Health Professions. Elsevier Health Sciences. 2017. p. 398. ISBN 978-0-323-56682-7.
  14. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  15. ^ "Diclofenac – Drug Usage Statistics". ClinCalc. Retrieved 18 February 2024.
  16. ^ Cuthbert RJ, Taggart MA, Prakash V, Chakraborty SS, Deori P, Galligan T, et al. (2014). "Avian scavengers and the threat from veterinary pharmaceuticals". Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences. 369 (1656): 20130574. doi:10.1098/rstb.2013.0574. PMC 4213586. PMID 25405963.
  17. ^ Cite error: The named reference Moreno2021 was invoked but never defined (see the help page).
  18. ^ European Medicines Agency, Committee for Medicinal Products for Veterinary Use, Opinion of the Committee pursuant to Article 30(3) of Regulation (EC) No 726/2004 on the risk to vultures and other necrophagous bird populations in the European Union in connection with the use of veterinary medicinal products containing the substance diclofenac (PDF), EMA/CVMP/761582/2014, archived (PDF) from the original on 7 July 2022, retrieved 16 April 2022
  19. ^ McKie R (11 April 2021). "Rare European vultures being poisoned by livestock drug". The Guardian. Archived from the original on 16 April 2022. Retrieved 16 April 2022. ...diclofenac has already been banned in India, Pakistan, Nepal and Bangladesh

© MMXXIII Rich X Search. We shall prevail. All rights reserved. Rich X Search