NSAIDs (non aspirin) non-opioid analgesics, and gout drugs

Question 1

NSAIDs with analgesic and Marked anti-inflammatory action

Answer 1

Acetic acid derivatives

• Indomethacin - semmelweis says its slightly cox-1 selective. literally nobody else does.
• Diclofenac
• Bromfenac
• Sulindac

Enol acids

• Piroxicam
• Meloxicam - sliiiiiightyl COX2 selective, more antiinflamatory than analgesic.
• Tenoxicam

Pyrazolones

• Sulfinpyrazone
• Phenylbutazone
• Aminophenazone
• Methimazole

Question 2

What is the main difference between the oxicams and indomethacin or diclofenac

Answer 2

The acetic acid derivates are short acting. half life ~ 4 hours.

Piroxicam, Meloxicam, Tenoxicam are very long lasting half life ~50 hours.

Question 3

What are the effects of the pyrazolone NSAIDs, when are they used

Answer 3

They are mostly anti-pyretic and anti-inflammatory

Phenylbutazone is a very strong anti-inflammatory with severe NSAID side effects, and only used in very severe inflammation.

Question 4

What are the NSAIDs with analgesia and mild anti-inflammatory.

Answer 4

Priopionic acid derivatives:

• Ibuprofen - 2 hr half life
• Dexibuprofen
• Naproxen - Long half life, 14 hours
• Ketorolac - The only NSAID with parenteral formulations (sike, parecoxib too).

Fenamates:

• Mefenamic acid
• Fludenamic acid

Others: mild COX-2 Selectivity, mainly anti-inflammatory with weak analgesia.

• Nabumetone
• Nimesulide

Question 5

What are the NSAIDs with only analgesic effects and very weak or no anti-inflammatory effect

Answer 5

Paracetamol/Acetominophen (not really an NSAID)

• Selective COX inhibition in the brain. Doesn’t affect peripheral COX enzymes, nor does it affect inflammation AT ALL.
• May affect CNS cannabinoid receptors via some of its metabolites.

Phenacetin

• Prodrug version that is converted to Acetominophen.
• Not used in the US. Too toxic.

Coxims (Also not really NSAIDs)

• Celecoxib
• Etoricoxib - sulfonamide
• Parecoxib - Parenteral form.