NSAIDs Flashcards
what is the function of Prostaglandin E (PGE)
- increased mucous production
- decreases acid production
- increases regeneration rate of mucous membranes
- dilates vessels in the kidneys - kidney protection
- Increase renal blood flow
- Protect against kidney damage
What is the localisation of COX-1 isoenzyme?
stomach, kidney, platelets
Constituitive
always present
“house keeping enzyme”
What is the loaction is COX-2 isoenzyme?
Macrophages and fibroblasts
Inductive
want to inhibit in the case of inflmmation
what is the localisation of COX-3 isoenzymes?
Thalamus and hypothalamus
Fever effect
Antipiretic, analgesic
name some traditional non COX-2 selective NSAIDs?
Aspirin
Ketoprophen
Fluxinin
Piroxicam
name come preferential COX-2 selective NSAIDs?
Meloxicam
Caprofen
vedaprofen
name the most important NSAID used in horses?
Fluxinin
describe Coxibs?
very safe
COX-2 selective
name some coxibs?
Fibrocoxib
Robenacoxib
Deracoxib
Cimicoxib
Mavacoxib
describe the side effects of NSAIDs?
GI ulceration and bleeding
kidney damage (predisposing factors)
Liver damage
Platelet aggregation inhibition
Methaeoglobinaemia (paracetamol)
Problems during pregnancy
Cartilage damage
Name some COX-3 inhibitors?
Paracetamol
metamizole
acetaminophen
describe the indications of NSAIDs?
- Osteoarthritis, osteoarthrosis
- Infectious arthritis
- Myositis, tendinitis
- Fever
- Endotoxaemia
- GI and urinary tract spasm
- Colitis
name the NSAIDS best suited for treatment of E.coli mastitis, enteritis in small animals, in gram negative infection?
Meloxicam and fluxinin
Antiendotoxin
Name the drugs best used to release spasms of the SM in the equine gut during colic?
Fluxinin
Metamizole
Spasmolytic
Name the best NSAID used as a antineoplastic drug?
Piroxicam
how do we minimise the chance of gastric ulcers associated with NSAID treatment?
administer with food or within protective capsule
hypoalbuminaemia can increase the chance of side effects?
True
extensive albumin binding protects the body from the drug
what is the purpose of the loading dose?
to saturate the albumin with the drug
Is there a WP for milk with NSAIDs?
No
describe the metabolism of NSAIDs?
- mostly glucuronic acid conjugation
- Feline sensitivity
- missing the enzyme
- Often smaller dose required
describe the excretion?
in the urine in both active and inactive forms
describe how GI ulceration occurs?
- Local irritation ( ion trapping)
- Reduced PGE
- less protection of the gastric mucosa
which NSAIDs often have platelet aggregation inhibition as a common side effect?
Asprin
Fluxinin
Tolfenamic acid
Ketoprophen
which NSAIDs can cause cartilage damage by proteoglycan synthesis inhibition?
Asprin
Ibuprofen
ketoprofen
naproxen
name the salicylates?
Asprin
Sulfasalazine
Mesalazine
name the arilproprionic acids?
Ketoprofen
Vedaprofen
carprofen
describe the benifits of using carprofen?
no cartilage damage
rare side effects
COX-2 preferential
also for exotic animals
long action in cattle
name the Anthronilic acids?
Fluxinin meglumine
Tolfenamic acid
describe fluxinin?
widely used in Eq
thrombocyte aggregation inhibition
antiendotoxic
describe the benifit of tolfenamic acid?
safe short term in cats
name the Oxicams?
Meloxicam
Piroxicam
describe Meloxicam?
COX-2 preferential
Used in Large animals for E.coli mastitis - antiendotoxin
describe a useful feature of Piroxicam?
Antineoplastic
prostate tumours
urinary bladder tumours
name the Non-acidic NSAID substances?
Alinin derivatives
Pyrazolones
Name and describe an Alanin derivative?
Paracetamol
COX-3 selective
analgesic, anitpyretic (minor analgesic)
Never use in cats
name and describe a Pyrazolone?
Metamizole
Not specific but mainly COX-3
can be used in the case of horse colic however not as effective as fluxinin
why are the coxibs different from other NSAIDs?
Highly selective COX-2 inhibition
less damaging to GI tract
However can cause more damage to the cardiovascular system
