NSAIDs Flashcards
What are indications for NSAID use?
- Mild-to-moderate pain
- Pain related to inflammation - particularly MSK
As an alternative or in addition to paracetamol
What inflammatory conditions are NSAIDs particularly useful for?
- RA
- Severe osteoarthritis
- Acute gout
What is the mechanism of action of NSAIDs?
Inhibits synthesis of prostaglandins from arachadonic acid by COX-1 and COX-2. The analgesic effects stem from COX-2 inhibition, which blocks COX-2 influence on the production of prostaglandins which cause inflammation and pain
What is cyclooxygenase?
Enzymes that produce prostaglandins
What is the function of COX-1?
COX-1 is the constitutive form. It stimulates prostaglandin synthesis that is essential to preserve integrity of the gastric mucosa; maintain renal perfusion (by dilating afferent glomerular arterioles); and inhibit thrombus formation at the vascular endothelium
What is the function of COX-2?
COX-2 is the inducible form, expressed in response to inflammatory stimuli. It stimulates production of prostaglandins that cause inflammation and pain
What are the side effects of COX-1 inhibition?
- Damage to gastric mucosa - PU
- Renal hypoperfusion - AKI
- Increased CV events risk - increased bleeding
What are side effects of COX-2 inhibition?
Inhibition of prostaglandin production - > inhibition of inflammation and pain
How do NSAIDs affect the kidneys?
COX-1 inhibition leads to constriction of the afferent glomerular arteriole -> AKI. Also causes acute interstitial nephritis
What are side effects of NSAIDs?
- GI toxicity/ulcers
- Renal impairment
- Increased CV tisk - Stroke/MI
- Hypersensitivity reactions
- Fluid retention
When do you need to be cautious when using NSAIDs?
Contraindicated:
- Severe renal impairment
- Heart Failure
- Liver Failure
- NSAID hypersensitivity
- Peptic ulcer disease
Cautioned use
- GI bleeding
- CV disease
What interactions do you need to be aware of when using NSAIDs?
Worsens GI ulceration:
- Low-dose aspirin
- Corticosteroids
GI bleeding:
- Anticoagulants
- SSRIS
Renal impairment:
- ACEi
- Diuretics
General bleeding risk
- Warfarin
How long does treatment with Naproxen take to reach full effect?
3 weeks
What advise would you give someone when giving them NSAIDs?
- Warn of indigestion and to seek medical advise if thise occurs
- Explain risk of long term use
- Advise to stop use if acutely unwell - risk of AKI
What are risk factors for GI complications with NSAID use?
- >65 years
- Previous peptic ulceration
- CVD
- Diabetes
- Concurrent therapy with GI side effects