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

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SECTION IV
INFLAMMATION, IMMUNOMODULATION, AND HEMATOPOIESIS
Table 34–1
Classification and Comparison of Nonsteroidal Analgesics (Continued)
CLASS/DRUG
(SUBSTITUTION) PHARMACOKINETICS DOSING d COMMENTS COMPARED TO ASPIRIN
Fenamates (N-phenyl-anthranilates)
Mefenamic Peak C p
2-4 hours 500-mg load, then 250 mg Isolated cases of Efficacy similar;
acid Protein binding High every 6 hours hemolytic anemia GI side effects
Metabolites Conjugates of 3-hydroxy May have some (25%)
and 3-carboxyl
central action
metabolites (20%
recovered in feces)
3-4 hours
t 1/2
Meclofenamate Peak C p
0.5-2 hours 50-100 mg 4-6/day Efficacy similar;
Protein binding 99% (maximum of 400 mg/day) GI side effects
Metabolites Hepatic metabolism; (25%)
fecal and renal
excretion
t 1/2
2-3 hours
Flufenamic acid Not available in the U.S.
Propionic acid derivatives Intolerance of one does Usually better
not preclude use of tolerated
another propionate
derivative
Ibuprofen Peak C p
15-30 minutes Analgesia 200-400 mg every 10-15% discontinue Equipotent
Protein binding 99% Anti-inflammatory 4-6 hours due to adverse effects
Metabolites Conjugates of 300 mg/6-8 hours Children’s dosing
hydroxyl and or 400-800 mg Antipyretic: 5-10 mg/kg
carboxyl 3-4 times/day every 6 hours
metabolites
(max: 40 mg/kg/day)
t 1/2
2-4 hours Anti-inflammatory:
20-40 mg/kg/day in
3-4 divided doses