drug therapy of inflammation

Question 1

acetylsalicylic acid

Answer 1

• Aspirin
• irreversibly acetylates COX1 and 2 (non-competitive inhibition)
• metabolite salicylic acid(salicylate) reversibly inhibits COX1 and 2
• antiplatelet at lowest dose, then analgesic and antipyretc at intermed dose then anti-inflammatory at highest dose
• often taken as baby asprin to prevent MI, CVA
• GI irritation**, nephrotoxicity, bleeding/anemia, hepatotoxicity, rare hypersensitivity reaction

Question 2

Diflunisal

Answer 2

• salicylate derivative
• reversibly inhibits COX1 and 2
• analgesic and antipyretic effects similar to aspirin, but weak anti-inflammatory effects
• fewer GI side effects and less platelet effects than aspirin
• longer t 1/2 so used for chronic tx of osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction,

Question 3

acetaminophen

Answer 3

• para-amino phenol
• Tylenol
• reversibly inhibits COX1 and 2
• weak anti-inflammatory effects
• analgesic and antipyretic effects similar to aspirin
• less GI side irritation, but hepatic toxicity with overdose

**aspirin has antiplatele, analgesic, anti-inflamm and antipyretic effects but has severe GI irritation

tylenol doesn’t have GI irritation but doesn’t have anti-inflammatory effects and can cause liver toxicity with overdose

Question 4

Indomethacin

Answer 4

• Indole
• reversibly inhibits COX1 and 2
• 10X more potent than aspirin but toxicity limits its use (thrombocytopenia, aplastic anemia and severe frontal headaches)
• analgesic, anti-inflammatory, anti-pyretic similar to aspirin
• less platelet effects than aspirin
• less GI irritation
• RA, ankylosing spondylitis, OA, acute gout

Question 5

Ibuprofren

Answer 5

• propionic acid derivative (“pro”)
• reversibly inhibits COX1 and 2
• anti-inflammatory tx of rheumatic disorders, OA, ankylosing spondylitis
• analgesia of postpartum pain, menstrual pain, oral, opthalmic sx
• GI irritation and hepatoxicity
• better tolerated than aspirin or indomethacin

Question 6

Naproxen

Answer 6

• propionic acid derivative (“pro”)
• Aleve
• reversibly inhibits COX1 and 2
• 20X more potent than aspirin
• anti-inflamm tx of rheumatic disorders, OA, ankylosing spondylitis
• analgesia of postpartum pain, menstrual pain and oral, opthalmic sx
• GI irritation and hepatoxicity
• better tolerated than aspirin or indomethacin
• **long t1/2 makes it useful for twice/day tx of arthritis

Question 7

Flurbiprofen and Oxaprozin

Answer 7

• propionic acid derivatives (“pro”)
• antiflammatory tx of rheumatic disorders, OA, ankylosing spondylitis
• analgesia for postpartum pain, menstrual pain, eye/opthalmic sx
• GI irritation, hepatoxocity
• better tolerated thatn aspirin or indomethacin
• oxaprozin has t1/2 = 50 hours (can be given once a day)

Question 8

piroxicam

Answer 8

• enolic acid
• long t1/2 (45 hours) makes it good chronic tx for RA or OA
• similar adverse effects as other NSAIDs

Question 9

Ketorolac

Answer 9

• Heteroaryl Acetic Acid
• reversibly inhibitis COX1 and 2
• injectable (IM) NSAID ** parenteral admin.
• for post-op pain; provides single-dose analgesic efficacy equal or better to standard opiods
• also used topically for inlamm conditions of eye

Question 10

Celecoxib(celebrex) and Etoricoxib

Answer 10

• COX 2 selective inhibs
• same anti-inflamm, anti-pyretic and analgesic effects as traditional NSAIDs but produce less GI toxicity
• no impact on platelet aggregation –> no cardioprotective effects like traditional NSAIDs
• increased risk for MI, stroke, thrombosis

** in theory COX2 inhibitors should be better NSAIDs bc COX2 is only induced during inflammation