مضادات الإلتهاب اللاستيروئيدية Anti-inflammatory Drugs

[dr.Hazem]

Diclofenac

More potent than indomethacin or naproxen
Ophthalmic, dermatologic, suppository and IM preparation are also available
Approved for long-term use: RA, OA and ankylosing spondylistis



Ketorolac

significant analgesic efficacy → used to replace morphine in mild to moderate postsurgical pain (IM).
use for > 5 days → peptic ulceration & renal impairment → withdrawal from some European markets.

[dr.Hazem]

Tolmetin and Nabumetone

As potent as aspirin in treatment of adult or juvenile RA or OA, but
They may have fewer side effects
Tolmetin is not used in Gout
Nabumetone May be < damaging to the stomach.
May cause pseudoporphyria & photosensitivity. 

Diflunisal

A diflurophenyl derivative of salicylic acid
It is not metabolized to salicylate and therefore can’t cause salicylate intoxication
3-4X more potent than ASA as analgesic and anti-inflammatory but has no antipyretic properties (does not cross BBB can’t relieve fever)

[dr.Hazem]

COX-2 Selective NSAIDs

The structural differences between COX-1 and COX-2 allowed for the development of selective COX-2 inhibitors

E.g. Celecoxib (Roficoxib and Valdecoxib withdrawn)

Differ from most of traditional NSAIDs that inhibit both COX-1 and COX-2
However, etodolac, meloxicam and numelsulide display some level of COX-2 selectivity

Lower risk of the development of GI bleeding
No significant effects on platelets

Relative selectivity Figure (41.11) in Lippincott (pp.504)

However, (like traditional NSAIDs) May cause renal insufficiency and increase risk of hypertension

However, for patients who require chronic use of NSAIDs and are at high risk for NSAID—related gastroduodenal toxicity, primary therapy with a COX-2 selective inhibitor is a reasonable option

Celecoxib

Selective for COX-2.
At in-vivo concentrations, does not inhibit COX-1
Inhibition of COX-2 is time-dependent and reversible
Readily absorbed from GIT (peak= 3 hrs)
Extensively metabolised by liver. Excreted by feces and urine
T1/2= 11 hrs (taken once daily)

Adverse effects:
The most common: Abdominal pain, diarrhea and dyspepsia

Less gastroduodenal ulcer than naproxen, diclofenac or ibuprofen

Kideny toxicity may occur (like with ither NSAIDs)

Celecoxib is contraindicated in patients allergic to sulfonamides

Selective COX-2 inhibitors should be avoided in patients with renal insufficiency, severe heart disease, volume depletion and/or hepatic failure

Patients with HX of anaphylactoid reactions to aspirin or nonselective NSAIDs may have similar effects..

[the-aspirant]

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[dr.Hazem]

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