Bromfenac, a new nonsteroidal anti-inflammatory drug: relationship between the anti-inflammatory and analgesic activity and plasma drug levels in rodents.
Bromfenac [2-amino-3-(4-bromobenzoyl)benzenacetic acid, sodium salt sesquihydrate] exhibited potent analgesic and anti-inflammatory activity in mice and rats. In a mouse model of pain (acetylcholine abdominal constriction), bromfenac showed a rapid onset of activity (20 min) that persisted for at least 4 hr. In a rat model of inflammation (carrageenan foot edema), a single oral dose of bromfenac, 0.316 mg/kg, produced significant anti-inflammatory activity up to 24 hr after dosing. Bromfenac was readily absorbed after oral administration, peak plasma levels being achieved at the earliest time tested: 20 min in the mouse and 30 min in the rat. The plasma half-life of bromfenac in rats is less than 4 hr. Since the anti-inflammatory activity persisted for 20 to 24 hr in spite of its short plasma half-life, it appears that there is no direct correlation between duration of activity and plasma drug level.
Nolan
J C
JC
A. H. Robins Company, Department of Pharmacology, Richmond, Virginia.
Osman
M A
MA
Cheng
L K
LK
Sancilio
L F
LF
D000698:Analgesia; D000700:Analgesics / Q000097:blood / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood / Q000494:pharmacology*; D001577:Benzophenones / Q000097:blood / Q000494:pharmacology*; D001969:Bromobenzenes / Q000097:blood / Q000494:pharmacology*; D005260:Female; D006207:Half-Life; D051379:Mice; D008813:Mice, Inbred ICR
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001577:Benzophenones; D001969:Bromobenzenes; C053083:bromfenac