NSAIDs Flashcards
definition of peripherial sensitisation
at the site of inflammation you feel pain much better
where in the eicosanoids chain do glucocorticoids have their effect
at phospholipase A2 - they diminish the whole process - most potent
localisation of COX1
stomach, kidney, platelets
localisation of COX2
macrophages, fibroblasts
COX1 production
constitutive - all the time produced
COX2 production
inductive - at site of inflammation
COX1 effects in stomach
produces prostaglandins mainly PGE to protect stomach wall
- decr HCl
- incr mucus secretions
- incr perfusion
what substances inhibit COX3
paracetamol, metamizole
where is COX3 present
in CNS, mainly hypothalamus and thalamus
what effects does inhibiting COX3 have on the body
great antipyretic and analgesic effect
old, non selective NSAIDs
ketoprofen, aspirin
more selective COX2 inhibitors
meloxicam, carprofen
name two coxibs that are extremely selective
deracoxib, firocoxib
absorption of NSAIDs
- usually weak acids - non ionised forms have better transport through membranes
- depends on feed
distribution of NSAIDs
- extensive albumin binding - cannot enter milk
- hypoalbuminaemia
- interactions
- loading dose
metabolism of NSAIDs
mainly glucoronic acid conjugation - feline sensitivity
while there is no NSAIDs authorised for cats for more than one week, which one is actually safe long term
meloxicam
excretion NSAIDs
urine in both inactive and active forms
where in the body would you find GI ulceration as a side effect
stomach and duodenum
two causes of GI ulceration as a side effect
- local irritation - ion trapping of weak acids
- PGE decr
can this GI ulceration be avoided by injecting the drugs
no, bc the PGE decr can cause it anyway
how do we treat GI ulceration
proton pump inhibitors eg omeprazole
should we give NSAIDs to patients with dehydration
no hydrate the animal first - kidney damage
due to the kidney damage, which limitations should we put on usage of NSAIDs
- rehydrate first
- not during anaesthesia - only post operative
- not with preexisting renal disease
which dog breed is most prone to idiosyncratic reactions with carprofen
golden retrievers
how often is hepatotoxicity observed as a possible side effect
rarely
why shouldnt we use paracetamol in cats
leads to methaemoglobinemia - seriously toxic
when can the side effect of platelet aggregeation inhibiton be useful
during thrombosis
which NSAIDs are more prone to platelet aggregation inhibiton
aspirin, flunixin, tolfenamic acid, ketoprofen
why should we be careful when using NSAIDs in arthritis patients
bc they can cause proteoglycan synthesis inhibiton - damages cartilage
which NSAIDs are more prone to proteoglycan synthesis inhibition
aspirin, ketoprofen, ibuprofen, naproxen
why are NSAIDs not recommended for use during pregnancy, esp the first trimester
they can cause fetal damage, teratogenicity
which NSAID in particular is known to have no effect on cartilage
maloxicam
why should we be careful when using NSAIDs around the time of parturition
they can cause placenta retention
the time period when we should avoid using NSAIDs around parturition
48hrs before to 36hrs after
which drug can be used safely around parturition
maloxicam
groups of acidic active substances
- salicylates
- arilpropionic acids
- heteroaryl acetic acids
- anthranilic acids
- butylpyrazolidines
- oxicams
groups of non acidic active substances
- anilin derivatives
- pyrazolones
coxibs
- deracoxib
- firocoxib
- robenacoxib
- cimicoxib
- mavacoxib
salicylates
- acetylsalicilic acid
- Na salicylate
- sulfasalazine, mesalazine
arilpropionic acids
- ketoprofen
- vedaprofen
- carprofen
heteroaryl acetic acids
diclofenac
anthraanilic acids
- flunixin meglumine
- tolfenamic acid
butyl pyrazolidines
phenylbutazone
oxicams
- piroxicam
- meloxicam
anilin derivatives
paracetamol
pyrazolones
metamizole sodium
possible side effects from NSAIDs
- GI ulceration
- kidney damage
- hepatoxcity
- platelet aggregation inhibition
- methaemoglobinaemia
- proteoglycan synthesis inhibition
- fetal damage
- placenta retention
which species can acetylsalycilic acid be used in
dogs, farm animals, not cats
in which farm animals is acetylsalycilic acid usually used in
poultry, swine
Na salicylate is used in which species
only farm animals, added to water
which is safer, acetylsalycilic acid or Na salicylate
Na salicylate - ore COX2 selective
in which species are sulfasalazine and mesalazine used
dogs and humans
indication for sulfasalazine and mesalazine
chronic colitis
what does ketoprofen do to platelet aggregation
significantly inhibits
ketoprofen use in cats
short term safety, best antipyretic in cats, v short half life
in which form does vedoprofen come for horses
as an oral paste
vedaprofen can be used in which species
horses
is vedaprofen selective
yes, COX2 selective
possible idiosyncratic reaction from carprofen in golden retrievers
hepatopathy - be careful when you give with other hepatotoxic drugs
carprofen duration in cattle
4-5 days
why is the WP for milk carprofen 0 days
because high albumin binding
can carprofen be given lifelong
yes
loading carprofen dose ca
po,sc,iv 4.4mg/kg
maintainence dose carprofen ca
2.2mg/kg
can carprofen be used in exotics
yes
side effects carprofen
no cartilage damage, rare side effects - COX2 selective
diclofenac is toxic for which species
dogs, cats and birds
what does flunixin meglumine do to platelet aggregation
inhibits -causes bleeding
why is there a flunixin meglumine pour on solution in cattle
the half life is short - decr absorption lasts longer
why is flunixin meglumine useful for mastitis, enteritis and colic
its antiendotoxic
why is flunixin meglumine frequently used in Eq
its spasmolytic
is tolfenamic acid long term in cats
no, short term
what does tolfenamic acid do to platelet aggregation
inhibits
in which species is phenylbutazone still used
equine, as an ointment
indications for piroxicam
oncology, prostate and urinary bladder tumours - lot of side effects
meloxicam loading dose Car
0.2mg/kg SID
meloxicam can be given how
inj and PO
meloxicam maintainance dose Car
0.1mg/kg SID
meloxicam large animals loading dose
0.4mg/kg
meloxicam large animals maintainence dose
0.6mg/kg
why is meloxicam useful for mastitis, enteritis and colic
its antiendotoxic
which COX does paracetamol inhibit
COX3 - analgesic, antipyretic
effect of metamizole sodium in cats
CNS signs, excitation, salivation
paracetamol dose cats
NEVER GIVE
metamizole sodium dose
20-30mg/kg
metamizole sodium effect
not specific but mainly COX3
species you can use deracoxib in
dog
firocoxib can be used in which species
dog, horse
firocoxib selectivity
highly selective COX2
robenacoxib species
dog/cat
robenacoxib how can it be given
inj
mavacoxib half life
long, 5-7 days
mavacoxib duration of action
3-4weeks
bioavaliability of mavacoxib with food
80%
bioavaliability of mavacoxib without food
20%
mavacoxib percent of albumin binding
98%
first repeat of mavacoxib
after 2wks
second onwards repeat of mavacoxib
every 4wks
