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Flunixin

Flunixin is a nonsteroidal anti-inflammatory drug (NSAID), analgesic, and antipyretic used in horses, cattle and pigs. It is often formulated as the meglumine salt. In the United States, it is regulated by the U.S. Food and Drug Administration (FDA), and may only be lawfully distributed by order of a licensed veterinarian. There are many trade names for the product.

Flunixin
Clinical data
AHFS/Drugs.comInternational Drug Names
ATCvet code
Identifiers
  • 2-[[2-Methyl-3-(trifluoromethyl)phenyl]amino]pyridine-3-carboxylic acid
CAS Number
  • 38677-85-9 Y
PubChem CID
  • 38081
ChemSpider
  • 34911 N
UNII
  • 356IB1O400
KEGG
  • D04215 Y
ChEBI
  • CHEBI:76138 N
ChEMBL
  • ChEMBL1652146 N
CompTox Dashboard (EPA)
  • DTXSID4048565
ECHA InfoCard100.115.991
Chemical and physical data
FormulaC14H11F3N2O2
Molar mass296.249 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC1=C(C=CC=C1NC2=C(C=CC=N2)C(=O)O)C(F)(F)F
  • InChI=1S/C14H11F3N2O2/c1-8-10(14(15,16)17)5-2-6-11(8)19-12-9(13(20)21)4-3-7-18-12/h2-7H,1H3,(H,18,19)(H,20,21) N
  • Key:NOOCSNJCXJYGPE-UHFFFAOYSA-N N
 NY (what is this?)  (verify)

Dosage and uses in horses edit

Flunixin is administered at a dose of 1.1 mg/kg.[1] The full analgesic and antipyretic effects usually occur 1–2 hours following treatment, but there is often an effective analgesic effect within approximately 15 minutes. Despite its short plasma half life of 1.6–2.5 hours, effects can persist for up to 30 hours,[2] with maximal effects occurring between 2 and 16 hours. This is likely due to accumulation of the drug at inflammatory foci. Flunixin is primarily eliminated by the kidneys.[3]

Because it targets the inflamed tissue, flunixin is mainly used for colic pain, musculoskeletal pain, and ocular pain.[4][5][6] It is also used as an antipyretic and to reduce the effects of endotoxemia.[7]

Side effects and precautions edit

Flunixin is labeled for no more than 5 days of consecutive use and prolonged use increases the risk of toxicity. In horses, this includes gastric ulcers,[8] right dorsal colitis,[9] and nephrotoxicity.[10]

Flunixin is a prohibited substance under International Federation for Equestrian Sports rules,[11] and its use is prohibited or restricted by many other equestrian organizations. At labeled dose (1.1 mg/kg) given IV, detection time was found to be 144 hours.[12] However, drug recycling from bedding contamination by treated horses has been shown to potentially increase the clearance time.[13]

Administration edit

Flunixin may be given orally as a paste or as granules in feed. It can also be used intramuscularly (IM) or intravenously (IV). However, it is very irritating to tissue and IM administration has been associated with myonecrosis in horses,[14] so IV administration is preferred.

Administration of phenylbutazone to a horse also receiving flunixin has been shown to increase the risk of toxicity without improving analgesia.[15][16] For this reason, concurrent administration with another NSAID is not recommended. Doubling the dose of flunixin produces no improvement in analgesia, while potentially increasing the risk of toxicity.[4]

In the US, the only labeled route for flunixin administration in cattle is intravenous and pour-on. This is not the case in other countries; for example, in the UK, Allevenix is licensed for IV and intramuscular use,[17] and a pour-on product also exists.[18]

In the US flunixin is not labelled for goat use, however, flunixin may be used in goats in an extra-label fashion under appropriate veterinary guidance. Flunixin administered subcutaneously to dairy goats may carry a milk withdraw recommendation of 36-60 hours.[19] Interestingly, when given subcutaneously to goats in that study, tissue injury, such as seen in horses with intramuscular administration, was not observed.

See also edit

References edit

  1. ^ McIlwraith CW, Frisbie DD, Kawcak CE (2001). "Nonsteroidal Anti-Inflammatory Drugs". Proc. AAEP. 47: 182–187.
  2. ^ May SA, Lees P (1996). "Nonsteroidal anti-inflammatory drugs". In McIlwraith CW, Trotter GW (eds.). Joint Disease in the Horse. Philadelphia: WB Saunders. pp. 223–237.
  3. ^ Soma LR, Behrend E, Rudy J, Sweeney RW (November 1988). "Disposition and excretion of flunixin meglumine in horses". American Journal of Veterinary Research. 49 (11): 1894–8. PMID 3247913.
  4. ^ a b Foreman JH, Bergstrom BE, Golden KS, Roark JJ, Coren DS, Foreman CR, Schumacher SA (December 2012). "Dose titration of the clinical efficacy of intravenously administered flunixin meglumine in a reversible model of equine foot lameness". Equine Veterinary Journal. Supplement. 44 (43): 17–20. doi:10.1111/j.2042-3306.2012.00655.x. PMID 23447872.
  5. ^ Jochle W, Moore JN, Brown J, Baker GJ, Lowe JE, Fubini S, Reeves MJ, Watkins JP, White NA (June 1989). "Comparison of detomidine, butorphanol, flunixin meglumine and xylazine in clinical cases of equine colic". Equine Veterinary Journal. Supplement. 21 (7): 111–6. doi:10.1111/j.2042-3306.1989.tb05668.x. PMID 9118091.
  6. ^ Hilton HG, Magdesian KG, Groth AD, Knych H, Stanley SD, Hollingsworth SR (2011). "Distribution of flunixin meglumine and firocoxib into aqueous humor of horses". Journal of Veterinary Internal Medicine. 25 (5): 1127–33. doi:10.1111/j.1939-1676.2011.0763.x. PMID 21781166.
  7. ^ Bryant CE, Farnfield BA, Janicke HJ (February 2003). "Evaluation of the ability of carprofen and flunixin meglumine to inhibit activation of nuclear factor kappa B". American Journal of Veterinary Research. 64 (2): 211–5. doi:10.2460/ajvr.2003.64.211. PMID 12602591.
  8. ^ Videla R, Andrews FM (August 2009). "New perspectives in equine gastric ulcer syndrome". The Veterinary Clinics of North America. Equine Practice. 25 (2): 283–301. doi:10.1016/j.cveq.2009.04.013. PMID 19580940.
  9. ^ McConnico RS, Morgan TW, Williams CC, Hubert JD, Moore RM (November 2008). "Pathophysiologic effects of phenylbutazone on the right dorsal colon in horses". American Journal of Veterinary Research. 69 (11): 1496–505. doi:10.2460/ajvr.69.11.1496. PMID 18980433.
  10. ^ Black HE (1986). "Renal toxicity of non-steroidal anti-inflammatory drugs". Toxicologic Pathology. 14 (1): 83–90. doi:10.1177/019262338601400110. PMID 3487106. S2CID 28865193.
  11. ^ "FEI Prohibited Substances List". 28 October 2013. Retrieved 23 January 2016.
  12. ^ "FEI List of Detection Times" (PDF). Retrieved 23 January 2016.
  13. ^ Popot MA, Garcia P, Bonnaire Y (December 2011). "Doping control in horses: housing conditions and oral recycling of flunixin by ingestion of contaminated straw". Journal of Veterinary Pharmacology and Therapeutics. 34 (6): 612–4. doi:10.1111/j.1365-2885.2011.01276.x. PMID 21995754.
  14. ^ Peek SF, Semrad SD, Perkins GA (January 2003). "Clostridial myonecrosis in horses (37 cases 1985-2000)". Equine Veterinary Journal. 35 (1): 86–92. doi:10.2746/042516403775467513. PMID 12553469.
  15. ^ Foreman JH, Ruemmler R (November 2011). "Phenylbutazone and flunixin meglumine used singly or in combination in experimental lameness in horses". Equine Veterinary Journal. Supplement. 43 (40): 12–7. doi:10.1111/j.2042-3306.2011.00485.x. PMID 22082440.
  16. ^ Reed SK, Messer NT, Tessman RK, Keegan KG (March 2006). "Effects of phenylbutazone alone or in combination with flunixin meglumine on blood protein concentrations in horses". American Journal of Veterinary Research. 67 (3): 398–402. doi:10.2460/ajvr.67.3.398. PMID 16506899.
  17. ^ "Allevinix 50 mg/ml solution for injection for cattle, pigs and horses". NOAH Compendium. National Office of National Health. Retrieved 19 April 2017.
  18. ^ "Finadyne Transdermal 50 mg/ml pour-on solution for cattle". NOAH Compendium. National Office of National Health. Retrieved 19 April 2017.
  19. ^ Smith JS, Marmulak TL, Angelos JA, Lin Z, Rowe JD, Carlson JL, Shelver WL, Lee EA, Tell LA (2020). "Pharmacokinetic Parameters and Estimated Milk Withdrawal Intervals for Domestic Goats (Capra Aegagrus Hircus) After Administration of Single and Multiple Intravenous and Subcutaneous Doses of Flunixin Meglumine". Frontiers in Veterinary Science. 7: 213. doi:10.3389/fvets.2020.00213. PMC 7248982. PMID 32509803.

External links edit

  • Flunixin meglumine 2007-09-27 at the Wayback Machine
  • Flunixin Meglumine For Veterinary Use
  • Flunixin licensing in the UK provided by Norbrook

flunixin, nonsteroidal, anti, inflammatory, drug, nsaid, analgesic, antipyretic, used, horses, cattle, pigs, often, formulated, meglumine, salt, united, states, regulated, food, drug, administration, only, lawfully, distributed, order, licensed, veterinarian, . Flunixin is a nonsteroidal anti inflammatory drug NSAID analgesic and antipyretic used in horses cattle and pigs It is often formulated as the meglumine salt In the United States it is regulated by the U S Food and Drug Administration FDA and may only be lawfully distributed by order of a licensed veterinarian There are many trade names for the product FlunixinClinical dataAHFS Drugs comInternational Drug NamesATCvet codeQM01AG90 WHO IdentifiersIUPAC name 2 2 Methyl 3 trifluoromethyl phenyl amino pyridine 3 carboxylic acidCAS Number38677 85 9 YPubChem CID38081ChemSpider34911 NUNII356IB1O400KEGGD04215 YChEBICHEBI 76138 NChEMBLChEMBL1652146 NCompTox Dashboard EPA DTXSID4048565ECHA InfoCard100 115 991Chemical and physical dataFormulaC 14H 11F 3N 2O 2Molar mass296 249 g mol 13D model JSmol Interactive imageSMILES CC1 C C CC C1NC2 C C CC N2 C O O C F F FInChI InChI 1S C14H11F3N2O2 c1 8 10 14 15 16 17 5 2 6 11 8 19 12 9 13 20 21 4 3 7 18 12 h2 7H 1H3 H 18 19 H 20 21 NKey NOOCSNJCXJYGPE UHFFFAOYSA N N N Y what is this verify Contents 1 Dosage and uses in horses 2 Side effects and precautions 3 Administration 4 See also 5 References 6 External linksDosage and uses in horses editFlunixin is administered at a dose of 1 1 mg kg 1 The full analgesic and antipyretic effects usually occur 1 2 hours following treatment but there is often an effective analgesic effect within approximately 15 minutes Despite its short plasma half life of 1 6 2 5 hours effects can persist for up to 30 hours 2 with maximal effects occurring between 2 and 16 hours This is likely due to accumulation of the drug at inflammatory foci Flunixin is primarily eliminated by the kidneys 3 Because it targets the inflamed tissue flunixin is mainly used for colic pain musculoskeletal pain and ocular pain 4 5 6 It is also used as an antipyretic and to reduce the effects of endotoxemia 7 Side effects and precautions editFlunixin is labeled for no more than 5 days of consecutive use and prolonged use increases the risk of toxicity In horses this includes gastric ulcers 8 right dorsal colitis 9 and nephrotoxicity 10 Flunixin is a prohibited substance under International Federation for Equestrian Sports rules 11 and its use is prohibited or restricted by many other equestrian organizations At labeled dose 1 1 mg kg given IV detection time was found to be 144 hours 12 However drug recycling from bedding contamination by treated horses has been shown to potentially increase the clearance time 13 Administration editFlunixin may be given orally as a paste or as granules in feed It can also be used intramuscularly IM or intravenously IV However it is very irritating to tissue and IM administration has been associated with myonecrosis in horses 14 so IV administration is preferred Administration of phenylbutazone to a horse also receiving flunixin has been shown to increase the risk of toxicity without improving analgesia 15 16 For this reason concurrent administration with another NSAID is not recommended Doubling the dose of flunixin produces no improvement in analgesia while potentially increasing the risk of toxicity 4 In the US the only labeled route for flunixin administration in cattle is intravenous and pour on This is not the case in other countries for example in the UK Allevenix is licensed for IV and intramuscular use 17 and a pour on product also exists 18 In the US flunixin is not labelled for goat use however flunixin may be used in goats in an extra label fashion under appropriate veterinary guidance Flunixin administered subcutaneously to dairy goats may carry a milk withdraw recommendation of 36 60 hours 19 Interestingly when given subcutaneously to goats in that study tissue injury such as seen in horses with intramuscular administration was not observed See also editClonixinReferences edit McIlwraith CW Frisbie DD Kawcak CE 2001 Nonsteroidal Anti Inflammatory Drugs Proc AAEP 47 182 187 May SA Lees P 1996 Nonsteroidal anti inflammatory drugs In McIlwraith CW Trotter GW eds Joint Disease in the Horse Philadelphia WB Saunders pp 223 237 Soma LR Behrend E Rudy J Sweeney RW November 1988 Disposition and excretion of flunixin meglumine in horses American Journal of Veterinary Research 49 11 1894 8 PMID 3247913 a b Foreman JH Bergstrom BE Golden KS Roark JJ Coren DS Foreman CR Schumacher SA December 2012 Dose titration of the clinical efficacy of intravenously administered flunixin meglumine in a reversible model of equine foot lameness Equine Veterinary Journal Supplement 44 43 17 20 doi 10 1111 j 2042 3306 2012 00655 x PMID 23447872 Jochle W Moore JN Brown J Baker GJ Lowe JE Fubini S Reeves MJ Watkins JP White NA June 1989 Comparison of detomidine butorphanol flunixin meglumine and xylazine in clinical cases of equine colic Equine Veterinary Journal Supplement 21 7 111 6 doi 10 1111 j 2042 3306 1989 tb05668 x PMID 9118091 Hilton HG Magdesian KG Groth AD Knych H Stanley SD Hollingsworth SR 2011 Distribution of flunixin meglumine and firocoxib into aqueous humor of horses Journal of Veterinary Internal Medicine 25 5 1127 33 doi 10 1111 j 1939 1676 2011 0763 x PMID 21781166 Bryant CE Farnfield BA Janicke HJ February 2003 Evaluation of the ability of carprofen and flunixin meglumine to inhibit activation of nuclear factor kappa B American Journal of Veterinary Research 64 2 211 5 doi 10 2460 ajvr 2003 64 211 PMID 12602591 Videla R Andrews FM August 2009 New perspectives in equine gastric ulcer syndrome The Veterinary Clinics of North America Equine Practice 25 2 283 301 doi 10 1016 j cveq 2009 04 013 PMID 19580940 McConnico RS Morgan TW Williams CC Hubert JD Moore RM November 2008 Pathophysiologic effects of phenylbutazone on the right dorsal colon in horses American Journal of Veterinary Research 69 11 1496 505 doi 10 2460 ajvr 69 11 1496 PMID 18980433 Black HE 1986 Renal toxicity of non steroidal anti inflammatory drugs Toxicologic Pathology 14 1 83 90 doi 10 1177 019262338601400110 PMID 3487106 S2CID 28865193 FEI Prohibited Substances List 28 October 2013 Retrieved 23 January 2016 FEI List of Detection Times PDF Retrieved 23 January 2016 Popot MA Garcia P Bonnaire Y December 2011 Doping control in horses housing conditions and oral recycling of flunixin by ingestion of contaminated straw Journal of Veterinary Pharmacology and Therapeutics 34 6 612 4 doi 10 1111 j 1365 2885 2011 01276 x PMID 21995754 Peek SF Semrad SD Perkins GA January 2003 Clostridial myonecrosis in horses 37 cases 1985 2000 Equine Veterinary Journal 35 1 86 92 doi 10 2746 042516403775467513 PMID 12553469 Foreman JH Ruemmler R November 2011 Phenylbutazone and flunixin meglumine used singly or in combination in experimental lameness in horses Equine Veterinary Journal Supplement 43 40 12 7 doi 10 1111 j 2042 3306 2011 00485 x PMID 22082440 Reed SK Messer NT Tessman RK Keegan KG March 2006 Effects of phenylbutazone alone or in combination with flunixin meglumine on blood protein concentrations in horses American Journal of Veterinary Research 67 3 398 402 doi 10 2460 ajvr 67 3 398 PMID 16506899 Allevinix 50 mg ml solution for injection for cattle pigs and horses NOAH Compendium National Office of National Health Retrieved 19 April 2017 Finadyne Transdermal 50 mg ml pour on solution for cattle NOAH Compendium National Office of National Health Retrieved 19 April 2017 Smith JS Marmulak TL Angelos JA Lin Z Rowe JD Carlson JL Shelver WL Lee EA Tell LA 2020 Pharmacokinetic Parameters and Estimated Milk Withdrawal Intervals for Domestic Goats Capra Aegagrus Hircus After Administration of Single and Multiple Intravenous and Subcutaneous Doses of Flunixin Meglumine Frontiers in Veterinary Science 7 213 doi 10 3389 fvets 2020 00213 PMC 7248982 PMID 32509803 External links editFlunixin meglumine Archived 2007 09 27 at the Wayback Machine Flunixin Meglumine For Veterinary Use Flunixin licensing in the UK provided by Norbrook Retrieved from https en wikipedia org w index php title Flunixin amp oldid 1182077087, 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