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Relationships between thromboxane production, platelet aggregability, and serum concentrations of ibuprofen or flurbiprofen
Author(s) -
Cox S R,
VanderLugt J T,
Gumbleton T J,
Smith R B
Publication year - 1987
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1987.66
Subject(s) - flurbiprofen , ibuprofen , platelet , thromboxane b2 , thromboxane , aspirin , platelet aggregation , pharmacology , chemistry , medicine , thromboxane a2
Arachidonate‐induced ex vivo platelet aggregations were performed before and after subjects received various doses of either ibuprofen or flurbiprofen. Both ibuprofen and flurbiprofen reduced the initial rate of thromboxane B 2 (TxB 2 ) production, but about 10% of control TxB 2 production was refractory to either drug. Aggregation was observed after TxB 2 concentrations exceeded a threshold of about 40 ng/ml. Once the threshold was achieved, aggregation and TxB 2 production occurred independently of either drug. Ibuprofen and flurbiprofen concentrations of about 3 and 0.2 μg/ml, respectively, inhibited aggregation during the 5‐minute testing period. A pharmacodynamic model was developed that predicts TxB 2 production, aggregation lag times, and percent aggregation as a function of the time course of drug concentrations in serum. Clinical Pharmacology and Therapeutics (1987) 41, 510–521; doi: 10.1038/clpt.1987.66