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