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

Sulindac Peak C p
1-2 hours; 8 hours 150-200 mg twice/day 20% suffer GI side Efficacy comparable
(sulfoxide for sulfide metabolite; effects; 10% get CNS
prodrug) extensive enterohepatic side effects
circulation
Metabolites Sulfone and conjugates
(30%); sulindac and
conjugates (25%)
t 1/2
7 hours; 18 hours
for metabolite
Etodolac Peak C p
1 hour 200-400 mg 3-4 times/day Some COX-2 100 mg etodolac
(pyranocar- Protein binding 99% selectivity in vitro has similar efficacy
boxylic acid) Metabolites Hepatic metabolites to 650 mg of aspirin,
t 1/2
7 hours but may be better
tolerated
Tolmetin Peak C p
20-60 400-600 mg 20 mg/kg/day Food delays and Efficacy similar;
(heteroaryl Protein binding 99% 3 times/day for in 3-4 decreases peak 25-40% develop
acetate Metabolites Oxidized to carboxylic children (anti- divided doses absorption side effects; 5-10%
derivative) acid/other derivatives, inflammatory) May persist longer in discontinue drug
then conjugated
synovial fluid to give
t 1/2
5 hours a biological efficacy
longer than its plasma t 1/2
Ketorolac Peak C p
30-60 <65 years: 20 mg (orally), then Commonly given Potent analgesic,
(pyrrolizine Protein binding 99% 10 mg every 4-6 hours (not to parenterally (60 mg poor anticarboxylate)
Metabolites glucuronide exceed 40 mg/24 hours); >65 years: IM followed by 30 mg inflammatory
conjugate (90%) 10 mg every 4-6 hours (not to every 6 hours, or
t 1/2
4-6 hours exceed 40 mg/24 hours) 30 mg IV every 6 hours)
Available as ocular
preparation (0.25%);
1 drop every 6 hours
Diclofenac Peak C p
2-3 hours 50 mg 3 times/day or Available as topical gel, More potent; 20%
(phenylacetate Protein binding 99% 75 mg twice/day ophthalmic solution, and develop side effects,
derivatives) Metabolites Glucuronide and oral tablets combined 2% discontinue use,
sulfide with misoprostol 15% develop elevated
(renal 65%, First-pass effect; oral liver enzymes
bile 35%) bioavailability, 50%
1-2 hours
t 1/2
(Continued )
CHAPTER 34
ANTI-INFLAMMATORY, ANTIPYRETIC, AND ANALGESIC AGENTS; PHARMACOTHERAPY OF GOUT
CHAPTER 34
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