User:Mr. Ibrahem/Diclofenac

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Mr. Ibrahem/Diclofenac
Clinical data
Trade namesCataflam, Voltaren, others[1]
AHFS/Drugs.comSystemic: Monograph
Topical: Monograph
MedlinePlusa689002
License data
Pregnancy
category
Routes of
administration
By mouth, rectal, intramuscular, intravenous (renal- and gallstones), topical
Legal status
Legal status
  • AU: S2 (Pharmacy medicine) – S4
  • UK: POM (Prescription only) (P for topical formulation)
  • US: ℞-only / OTC[3]
  • ℞-only in most preparations/countries, limited OTC in some countries, manufacture and veterinary use is banned in India, Nepal, and Pakistan due to imminent extinction of local vultures
Pharmacokinetic data
Protein bindingMore than 99%
MetabolismLiver, oxidative, primarily by CYP2C9, also by CYP2C8, CYP3A4, as well as conjugative by glucuronidation (UGT2B7) and sulfation;[6] no active metabolites exist
Onset of actionWithin 4 hours (gel),[4] 30 min (non-gel)[5]
Elimination half-life1.2–2 hr (35% of the drug enters enterohepatic recirculation)
Excretion40% biliary 60% urine
Identifiers
  • [2-(2,6-Dichloroanilino)phenyl]acetic acid
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, 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.[5] It is taken by mouth, rectally in a suppository, used by injection, or applied to the skin.[5][8] Improvements in pain last for as much as eight hours.[5] It is also available in combination with misoprostol in an effort to decrease stomach problems.[9]

Common side effects include abdominal pain, gastrointestinal bleeding, nausea, dizziness, headache, and swelling.[5] Serious side effects may include heart disease, stroke, kidney problems, and stomach ulceration.[9][5] Use is not recommended in the third trimester of pregnancy.[5] It is likely safe during breastfeeding.[9] It is believed to work by decreasing the production of prostaglandin.[10] It blocks both cycloxygenase-1 (COX-1) and cycloxygenase-2 (COX-2).[5]

Diclofenac was patented in 1965 by Ciba-Geigy; it came into medical use in the United States in 1988.[5][11] It is available as a generic medication.[5] The wholesale cost in the developing world is generally less than US$2 per month as of 2015.[12] In the United States the wholesale cost of this amount is typically less than US$9 as of 2018.[13] In 2017, it was the 94th most commonly prescribed medication in the United States, with more than eight million prescriptions.[14][15] It is available as both a sodium and a potassium salt.[9]

References[edit]

  1. ^ "Diclofenac". Drugs.com. Archived from the original on 22 December 2018. Retrieved 22 December 2018.
  2. ^ a b "Diclofenac Use During Pregnancy". Drugs.com. 16 January 2000. Archived from the original on 29 July 2020. Retrieved 15 February 2020.
  3. ^ "FDA Approves Three Drugs for Nonprescription Use Through Rx-to-OTC Switch Process". U.S. Food and Drug Administration (FDA). 14 February 2020. Archived from the original on 15 February 2020. Retrieved 14 February 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  4. ^ "How Long Does It Take for Voltaren Gel to Work?". YouDrugstore. Archived from the original on 30 July 2020. Retrieved June 1, 2020.
  5. ^ a b c d e f g h i j "Diclofenac epolamine Monograph for Professionals". Drugs.com. AHFS. Archived from the original on 18 September 2020. Retrieved 22 December 2018.
  6. ^ Mujib sayyad (August 23, 2018). "Diclofenac Oral Uses, Dosage, Side Effects And Composition". Medicine Reviews Agency. Archived from the original on August 24, 2018. Retrieved August 24, 2018.
  7. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 18 September 2020. Retrieved 1 September 2020.
  8. ^ Chung, CH (11 December 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.
  9. ^ a b c d British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. pp. 1033–1035. ISBN 978-0857112989.
  10. ^ Mosby's Drug Reference for Health Professions. Elsevier Health Sciences. 2017. p. 398. ISBN 9780323566827. Archived from the original on 28 August 2021. Retrieved 30 April 2020.
  11. ^ Fischer, Janos (2006). Analogue-based drug discovery. Wiley-VCH. p. 517. ISBN 978-3527312573.
  12. ^ "Diclofenac Sodium". International Medical Products Price Guide. Retrieved 4 December 2019.[dead link]
  13. ^ "NADAC as of 2018-12-19". Centers for Medicare and Medicaid Services. Archived from the original on 19 December 2018. Retrieved 22 December 2018.
  14. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  15. ^ "Diclofenac - Drug Usage Statistics". ClinCalc. Archived from the original on 12 March 2021. Retrieved 11 April 2020.