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24 Cards in this Set
- Front
- Back
How do the NSAIDs have their anti-inflammatory effect? |
Via inhibition of cyclo-oxygenase (COX) |
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What are the two isoforms of COX and how do they differ? |
COX-1 (Good COX) - involved in numerous protective roles in the body, PGE2, PGI2 COX-2 (Bad COX) - induced after pro-inflammatory insult to create mediators of inflammation. |
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Why do we use drugs to reduce inflammation which exists to remove noxious stimuli? |
Because inflammatory response can be overzealous. |
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What is the significance of COX selectivity of NSAIDs? |
Allows use of drugs with more targeted affects and helps to reduce the negative side effects. |
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What are the main side effects of the NSAIDs and what does it relate to? |
COX-1 inhibition: - GI tract - Platelets - Kidneys |
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What is the MOA of NSAID GI tract side effects? |
Inhibit PGE2 and PGI1 (good protoglandins) which are responsible for: - Inhibiting acid secretion - Increasing mucosal blood flow - Increasing mucus production Leads to erosion, ulceration and haemorrhage |
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What is the MOA of the NSAID platelet side effects? |
inhibits thromboxane (pro-platlet aggregator) irreversibly and PGI2 (anti-platelet aggregator) temporarily. Leads to net decrease in platelet aggregation |
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What is the MOA of the NSAID kidney side effects? |
Inhibits good protaglandins: PGE2 - Increases salt and water excretion PGI2 - Increases salt and water excretion and increases renal vasodilation Causes increased water retention leading to hypertension and decreases renal blood flow leading to necrosis |
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What is relevant about NSAID pharmacokinetics? |
Good oral bioavailability Can readily be given as tablets Highly bound to blood protein would normally not leave blood and enter tissue unless their has been an increase in permeability (inflammation) |
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What are the main NSAIDs used in small animals? |
Meloxicam Carprofen The 'coxibs: Firocoxib, deracoxib, robenacoxib, mavacoxib |
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What is meloxicam's MOA and what is it used for? |
NSAID used for analgesia Suitable for exotic and cats due to lower concentration preparations available. |
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What is carprofen's MOA and what is it used for? |
NSAID used for analagesia |
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What are firocoxib and deracoxib's MOA and what are they used for? |
COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs. Only registered in dogs |
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What is robenacoxib's MOA and what is it used for? |
COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs. Registered in both cats and dogs and has good palatability. |
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What is mavacoxib's MOA and what is it used for? |
EXTREMELY LONG-ACTINGCOX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs. Long DOA (7 doses in 6 months) due to slow clearance Side-effects not as long acting as benefits. |
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What are the main NSAIDs used in horses? |
Phenylbutazone Flunixin Meloxicam (rarely used) |
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What is phenylbutazone's MOA and what is it used for? |
Non-selective NSAID for musculoskeletal analgesia Increased risk of side-effects due to lack of selectivity. |
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What is flunixin's MOA and what is it used for? |
Non-selective NSAID used for visceral analgesia. Increased risk of side-effects due to lack of selectivity. |
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What is meloxicam's significance in large animals? |
Rarely used but large animals although large animal preparation does exist. |
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What are the main NSAIDs used in production animals? |
Flunixin Tolfenamic acid Meloxicam |
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What is flunixin used for in production animals? |
Dairy cattle mastitis with well established withholding periods |
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What is tolfenamic acid's MOA and what is it used for? |
COX-1 sparing NSAID leading to decreased side-effects associated with non-selective NSAIDs. More expensive than flunixin so rarely used. Established withholding periods. |
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Why is phenylbutazone not routinely used in production animals? |
No established withholding periods. |
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What is the concern with using NSAIDs in sheep? |
None of the main drugs are registered in sheep and so have to be used off-label. Off-label use in production animals discouraged as withholding periods have not been established. |