[Clinical study on the inhibitory effect of AA-2414 on platelet function in asthmatic patients].
We studied the effect of AA-2414, a TXA2 receptor antagonist, on platelet function in 12 asthmatic patients, 6 males and 6 females, whose mean age was 43.6 years. AA-2414 was orally administered to each patient at 20 mg/day for two weeks and then at 40 mg/day for the following two weeks. Platelet aggregation, plasma concentration of TXB2, and serum concentrations of AA-2414 and its metabolites were measured before and after the administration of each dose. Platelet aggregation induced by U-46619 (an analogue of PGH2), STA2 (a stable analogue of TXA2) and arachidonic acid with the administration of AA-2414 was significantly inhibited. The degree of this inhibition was proportional to the serum level of the drug. Plasma concentration of TXA2 tended to be lowered by administration of AA-2414, but it was not statistically significant. Eight (75.0%) of the 12 patients showed clinical improvement. In the cases where the drug was ineffective, the inhibition of platelet aggregation after administration of AA-2414 was less than in those cases where it was effective. We conclude that AA-2414 might exert its antiplatelet and antiasthmatic effects through antagonism of the TXA2 receptor. Investigation of the response to AA-2414 may be useful in assessing the clinical effect of this compound.
Hashizume
M
M
First Department of Internal Medicine, Kansai Medical University.
Kurokawa
D
D
Nishii
S
S
Yoshioka
F
F
Hada
S
S
Yasunaga
K
K
D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000368:Aged; D001249:Asthma / Q000097:blood* / Q000188:drug therapy; D016227:Benzoquinones; D006538:Heptanoic Acids; D006801:Humans; D008875:Middle Aged; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011809:Quinones / Q000008:administration & dosage / Q000494:pharmacology*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors; D017482:Receptors, Thromboxane; D013929:Thromboxane B2 / Q000097:blood
D016227:Benzoquinones; D006538:Heptanoic Acids; D010975:Platelet Aggregation Inhibitors; D011809:Quinones; D011982:Receptors, Prostaglandin; D017482:Receptors, Thromboxane; C060230:seratrodast; D013929:Thromboxane B2