Lecture 120 Flashcards
Ibuprofen undergoes metabolism by:
Hepatic metabolism (CYP2C19, 2C9)
Onset and duration of Ibuprofen
30-60 minutes; 6-8 hours
What happens if ibuprofen is taken before low-dose aspirin?
Ibuprofen blocks aspirin’s irreersible binding to platelet COX-1, reducing aspirin’s cardioprotective effect
Naproxen is metabolized by:
Hepatic metabolism (CYP2C9, 1A2)
Naproxen half-life
12-17 hours
Naproxen is prescribed to children older than 2 years to treat
Juvenile arthritis
Which two NSAIDs can interfere with aspirin’s antiplatelet effect?
Ibuprofen and naproxen
Distribution properties of indomethacin
Widely distributed, crosses BBB, and accumulates in synovial fluid
Indomethacin half-life
2.5-3.5 hours
Indomethacin is ____ more potent than aspirin
10-40 times
Which NSAID is used as a tocolytic?
Supress premature labor contractions
Indomethacin
Indomethacin is used to treat ____ in adults and children over 2 years old
Rheumatoid and other inflammatory disorders
Common intolerable side effects of indomethacin
Severe headache, dizziness, depression
Ketorolac half-life
2-9 hours
What is the primary use for ketorolac?
Short-term acute pain management (often in hospital)
What Boxed warning accompanies ketorolac?
Maximum 5 days systemic use due to significant bleeding risk that can occur at any time
Diclofenac half-life
1-2 hours
Which acetic acid derivative is somewhat COX-2 prefering but is still considered nonselective?
Diclofenac
Topical diclofenac is used for
joint/muscle pain and actinic keratosis
Adverse reactions unique to diclofenac
Possible hepatotoxicity, photosensitivity
Meloxicam half-life
15-24 hours
Meloxicam preferentially inhibits COX-2 over Cox-1 at higher/lower doses
Lower doses
How does the structure of Celecoxib contibute to its function?
Larger side chain fits COX-2 binding pocket but not COX-1’s
Celecoxib metabolism
Hepatic metabolism (CYP2C9)
