DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Naproxen Peak C p
1 hour 250 mg 5 mg/kg Peak anti-inflammatory More potent in vitro;
Protein binding 99% (less in elderly) 4 times/day twice/day effects may not be usually better
Metabolites 6-demethyl and other or 500 mg seen until 2-4 weeks tolerated; variably
metabolites twice/day of use prolonged t 1/2
t 1/2
14 hours Children: anti- Decreased protein binding may afford
inflammatory and delayed excretion cardioprotection in
increase risk of toxicity some individuals
in elderly
Fenoprofen Peak C p
2 hours 200 mg 4-6 times/day; 15% experience side
Protein binding 99% 300-600 mg 3-4 times/day effects; few
Metabolites Glucuronide, discontinue use
4-OH metabolite
2 hours
t 1/2
Ketoprofen Peak C p
1-2 hours Analgesia 25 mg 30% develop side
Protein binding 98% Anti- 3-4 times/day effects (usually GI,
Metabolites Glucuronide inflammatory 50-75 mg usually mild)
conjugates
3-4 times/day
2 hours
t 1/2
Flurbiprofen Peak C p
1-2 hours 200-300 mg/day in Available as a 0.03%
Protein binding 99% 2-4 divided doses ophthalmic solution
Metabolites Hydroxylates
and conjugates
6 hours
t 1/2
Oxaprozin Peak C p
3-4 hours 600-1800 mg/day Long t 1/2
allows for daily
Protein binding 99% administration; slow onset
Major Oxidates and of action; inappropriate
metabolites glucuronide for fever/acute analgesia
conjugates
t 1/2
40-60 hours
Enolic acid derivatives
Piroxicam Peak C p
3-5 hours 20 mg/day May inhibit activation Equipotent; perhaps
Protein binding 99% of neutrophils, activity of better tolerated
Metabolites Hydroxylates and proteoglycanase, 20% develop side
then conjugated collagenases effects; 5%
t 1/2
45-50 hours discontinue drug
(Continued )
CHAPTER 34
ANTI-INFLAMMATORY, ANTIPYRETIC, AND ANALGESIC AGENTS; PHARMACOTHERAPY OF GOUT
CHAPTER 34
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