NSAIDs FPAs Flashcards
What do NSAIDs act on?
COX
What is COX1 and COX2 responsible for?
> CoX 1 is physiologic - PGs, thromboxane - GIT, kidney, platelets - muscosal protection, renal blood flow and hemostasis > COX 2 is inducible - PGs - inflame sites, macrophages, synovocytes - inflammation pain andfever
Where do coxibs act?
- COX 2 only
4 main clinical indications for NSAIDs?
- analgesic
- anti-inflammatory
- anti-pyretic
- anti-thrombotic
Which drugs must never be used in FPAs in the UK?
> Phenylbutazone - causes fata blood dyscrasias in humans - no safe determined minimum residue limit (MRL) > chloramphenicol > metronidazole > Benzyl-penicillin (Crystapen) > Metoclopramide > Lidocaine > Gentamicin/Amikacin
Which drug should not be given to camelids and ruminants?
> Phenylbutazone
- Not legal for FPAs
- oral powder not bioavailable in ruminant
- T1/2 in llamas
Which species have no NSAIDs and few drugs licensed specifically for them?
- goats, sheep, camelids
Outline levels of the cascade
- vet med for different psecies or differnet condition
- human med in UK or vet med authorised in a member state (If for an FPA then for an FPA in the other country) in accordance with an import certificate issued by the VMD
- medicine prepared extemporaneously
> FPAs can only be treated with meds containing pharmacologically active substances listed in the table of allowed substances in commission regulation EU
What are the minimum withdrawals for a drug used under the cascade (ie not stated specifically for that species/indication)?
- 7d eggs and milk
- 28d meat from poultry and mammals
- 500 degree days meat from fish
What should be done if treating off label@?
- informed consent from the owner written and signed
Which NSAIDs are lic in FPAs? Which animals?
- Meloxicam (cattle, pigs, horses)
- Flunixin (cattle, pigs, horses)
- Ketoprofen (Cattle, pigs, horses)
- Carprofen (Cattle, horses)
- Tolfenamic acid (Cattle, pigs)
Doses of flunixin meglumine? CLinical uses?
- Cattle IV only 2.2mg/kg SID
- Pigs (IV or IM) 2.2mg/kg SID
- Alpacas = Horse dose IV only 1.1mg/kg SID/BID
> clinical uses - visceral and ophthalmic pain
- systemic inflammation (mastitis, metritis)
- pain relief after elective Sx (castration, disbudding)
> v cortisol, ^ feed intake, ^ dialy weight gains `
What is the most commonly prescribed NSAID in FPAs?
> Meloxicam
- preferential COX2
- prolonged T1/2 esp in cattle
- pain relef after surgery
- now LIC “releife of post-op pain following dehorning calves”
- effective against: systemic inflam (toxic mastitis), visceral and ophthalmic pain, cattle lameness
Doses of Meloxicam on and off label?
> label
- Cattle 0.5mg/kg (SC or IV) once, or of label q3d, 5d milk withdrawal
- Pigs 0.4mg/kg IM once or PO SID
Off label
- sheep 0.5mg/kg SID/BID (T1/2 shorter than in cattle)
- goats 0.5mg/kg BID/TID (effective plasma conc for 8 hours)
- alpacas 0.5mg/kg SID IV or 1mg/kg PO q72hrs(oral dose lasted 3d in one study)
What is ketoprofen? Uses? Compared to other NSAIDs?
- non selective COX inhibitor
- short t1/2 (limits use, requires multiple OFF LABEL doses)
- some effect on cattle lameness
- some evidence for short term effects in toxic mastitis
- LIC to reduce udder oedema cattle
- NOT as effective for analgesia with elective Sx cf other NSAIDs
Labelled use of ketoprofen?
- cattle and pigs 3mg/kg IV/IM SID for 3d
- NO milk withdrawal! YAY
What is carprofen? Uses? Compared to other NSAIDs?
- non selective COX inhibitor in largies
- prolonged T1/2 in cattle (even greater in young
Labelled use of carprofen?
- cattle 1.4mg/kg IV/SQ once
- NO milk withdrawal YAY!
Which NSAID is not used commonly in cattle?
> Tolfenamic acid
- bovine respiratory disease and acute mastitis (anti-inflam)
Labelled use of tolfenamic acid?
- cattle 2mg/kg IV only in dairy cattle q48hrs [never IM] milk withdrawal 24hrs
- pigs 2mg/kg IM in neck once (used for tx of metritis-mastitis-agalactiae (MMA) syndrome
Adverse effects opotentially of NSAIDs?
- anomasal ulceration
- renal toxicity
- care w/ hepatic dz
Which NSAIDs are lic in horses?
- meloxicam
- flunixin
- phenylbutazone
- suxibuzone
- ketoprofen
- carprofen
- Firicoxib
- Vedaprofen
What is phenylbutazone used for in horses? Dose?
- non selective COX1/2
- no evidence for tissue specificity (bone v visceral pain)
- less analgesic than flunixin
> 4.4mg/kg IV SID
> 8.8mg/kg PO SID for 1d then 4.4mg/kg/day (can be split BID) then 2,2mg/kg/day
What is suxibuzone?
- pro-drug of phenylbutazone given orally
- more palatable
- more $$$
What is flulnixin meglumine used for in horses? Dose?
- non-selective COX1/2
- no evidence tissue specificity
- good analgesic
- effective against systemic inflammation
> 1.1mg/kg IV/PO SID
> clinically used BID
What is meloxicam used for in horses? LIC? Dose?
- COX2 preferential
- LIC: colic, acute and chronic musculo-skeletal disorders
- pharmacokinetics show BID dosing regimen would improve efficacy
- supposedly good for use in foals
> 0.6mg/kg IV once and 0.6mg/kg PO SID (label)
What is ketoprofen used for in horses? Dose?
- non selective
- suppose to also inhibit lipoxygenase (though no evidence for this action in horses)
> 2.2mg/kg IV SID
What is carprofen used for in horses? Dose?
- non selective
- LIC: musculoskeletal disorders and surgery
> 0.7 mg/kg IV SID or PO
What is firocoxib used for in horses? Dose?
- only LIC COX2 specific inhibitor in horses
- long T1/2 (takes 3d to reach steady plasma level and affect lameness levels, 7d to reach peak plasma levels)
- LIC: OA and reduction in lameness
- achieves high levels in the eye
> 0.09mg/kg IV SID or 0.1mg/kg PO SID
Adverse effects of NSAIDs in horses?
> GIT
- gastric and oral ulcers sign of toxicity (dose too high)
- ulceration small/large intestinal mucosa
- RDC (ridght dorsal colitis) at regular doses and short-term use -> hypoalbumenaemia, neutropenia, D+, colic [PGs have a cytoprotective effect in the mucosa esp PGE2 and PGI2)
renal
-papillary necrosis
- dehydration, colume depletion -> renal vasoconstriction -> PG synthesis and 2* compensatory vasodilation
Phlebitis
- perivascular injection -> sever phlebitis and tissue necrosis
Define detection time
- approx. period of time for which a drug or its metabolites can be detected in a horse’s system
Define withdrawl time
- decided by vet, based on detection time + safety margin
- safety margin d/t differences in size, metabolism, fitness, illness/dz
What is EHSLC?
- comprises the racing authoritis of frnace, Ireland, UK, Germant, Italy and Scandanavia
See lecture for detection times of lots of drugs!
~
