non-steroidal anti-inflammatory drugs (NSAIDS) Flashcards
what is the MOA of NSAIDS
- COX enzyme inhibitor
- inhibits the cyclooxygenase (COX) and the prostaglandin synthesis pathway that is responsible for mediating information about pain to the brain
- not as much pain stimuli making it to the brain
what are normal effects from COX 1 pathway?
homeostasis of:
- GI blood flow
- renal system
- platelet aggregation
- macrophages
what are normal effects from COX 2 pathway?
- bronchodilation
- vasodilation
what are problems with cox inhibitors?
- multiple side effects
- frequent allergic reactions
- several require daily dosing for efficacy
- ceiling effects
- cox 2 have fewer complications BUT more specific cardiac effects
what are benefits of NSAIDS?
- analgesics
- anti inflammatory effects
- antipyretic effects
- not typically abused
- no respiratory depression
- absence of cognitive effects
- long duration of action
- have ceiling effects
what are effects of COX 2 inhibitors?
- risk of acute MI or CVA increases with prolonged use (prostaglandin protective mechanism)
- reduced side effects in comparison with NSAIDS as a class
- lack platelet effects
- decreased GI effects
when are NSAIDS contraindicated?
- allergic to aspirin
- renal failure (renal elimination)
- asthmatics have higher incidence of aspirin allergy and NSAID allergy (10%), especially if they also have nasal polyps (20%)
describe pharmacokinetics of NSAIDS
- well absorbed form GI tract (oral doses)
- CP450 metabolism
- 2% renally excreted unchanged
- conflicted studies on whether crosses BBB or not
what pts. typically benefit from NSAIDS?
- joint disease
- orthopedic surgery
- C-section
- Gyn procedures
- Big surgeries
- Back surgery
- arthritis
- musculoskeletal conditions
what pts. should NSAIDS not be used on?
- history of GI bleed
- renal injury/failure
- liver disease/malfunction
- bleeding disorders
- history of MI, esp. acute (within a year)
- ASA produces irreversible inactivation of platelets for the life of the platelet (7-10 days)- reasons should be stopped for a week prior to surgery
what are GI effects of NSAIDS?
- 15-30% incidence of ulcers with chronic use
* administer with H2 receptor antagonist (Pepcid, Prilosec)
what are coagulation effects of NSAIDS?
-COX 1 inhibitors cause platelet issues
what are cardiac effects of NSAIDS?
-increased risk of MI more with COX 2 inhibitors
-hypertension
prostaglandins improve HTN by relaxing vascular tone in arterial smooth muscle and also counteract responses to vasoconstrictive hormones
**so when prostaglandins are blocked, vasodilation is inhibited
*usually only a minor change in BP
what are renal effects of NSAIDS?
- little effect in healthy pts.
- renal medullary ischemia can occur d/t inhibition of prostaglandins
- renally impaired pts. may have a significant decrease in renal blood flow
- nephrotoxic if used chronically
- decreased GFR, Na+ retention leads to edema and HTN
what are hepatic effects of NSAIDS?
- may be hepatotoxic
- worse in chronically ill
- can lead to hepatic failure