Pyrazolopyridine derivative acts as a novel cyclooxygenase inhibitor: antiplatelet effect in aged patients with ischemic stroke.
OBJECTIVE
To examine the antiplatelet effect of a novel pyrazolopyridine derivative (KC-764) in geriatric patients with ischemic stroke.


METHODS
Randomized clinical trial of three graded dose levels.


METHODS
A geriatric clinic attached to a nursing home.


METHODS
Fifteen patients with a history of cerebral infarction with a mean age of 75 +/- 5 years (range, 65-83). Patients were divided into three groups and administered 10, 20, or 40 mg/day KC-764 for 8 weeks.


METHODS
Platelet aggregation induced by arachidonate, ADP, collagen and platelet-activating factor. Plasma or serum levels of thromboxane B2 and 6-ketoprostaglandin F1 alpha.


RESULTS
Platelet aggregation was inhibited by KC-764 administration and returned to the control level after discontinuation. Although plasma thromboxane B2 levels were markedly decreased, plasma 6-ketoprostaglandin F1 alpha was not affected. However, the dose of 10 mg/day was not sufficient to maintain an effective plasma level of KC-764. There were no side effects or changes in laboratory findings.


CONCLUSIONS
We confirmed that KC-764 at a dose of 20 to 40 mg/day is an effective antiplatelet agent and a good candidate for a trial to see if it is feasible for long-term use for the prevention of ischemic stroke in high-risk patients.
Satoh
K
K
Department of Pathological Physiology, Hirosaki University School of Medicine, Japan.
Yoshida
H
H
Imaizumi
T A
TA
Koyama
M
M
Hiramoto
M
M
Takamatsu
S
S
D015121:6-Ketoprostaglandin F1 alpha / Q000097:blood; D000284:Administration, Oral; D000368:Aged; D000369:Aged, 80 and over; D002545:Brain Ischemia / Q000188:drug therapy* / Q000517:prevention & control; D001643:Bridged Bicyclo Compounds / Q000097:blood / Q000627:therapeutic use*; D002561:Cerebrovascular Disorders / Q000188:drug therapy*; D002851:Chromatography, High Pressure Liquid; D016861:Cyclooxygenase Inhibitors / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D009539:Nicotinic Acids / Q000097:blood / Q000627:therapeutic use*; D010975:Platelet Aggregation Inhibitors / Q000627:therapeutic use*; D013929:Thromboxane B2 / Q000097:blood
D001643:Bridged Bicyclo Compounds; D016861:Cyclooxygenase Inhibitors; D009539:Nicotinic Acids; D010975:Platelet Aggregation Inhibitors; D013929:Thromboxane B2; D015121:6-Ketoprostaglandin F1 alpha; C074536:KC 764