Pyrazolopyridine derivative acts as a novel cyclooxygenase inhibitor: antiplatelet effect in aged patients with ischemic stroke

J Am Geriatr Soc. 1994 Jun;42(6):639-42. doi: 10.1111/j.1532-5415.1994.tb06863.x.

Abstract

Objective: To examine the antiplatelet effect of a novel pyrazolopyridine derivative (KC-764) in geriatric patients with ischemic stroke.

Design: Randomized clinical trial of three graded dose levels.

Setting: A geriatric clinic attached to a nursing home.

Patients: 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.

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

Main 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.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 6-Ketoprostaglandin F1 alpha / blood
  • Administration, Oral
  • Aged
  • Aged, 80 and over
  • Brain Ischemia / drug therapy*
  • Brain Ischemia / prevention & control
  • Bridged Bicyclo Compounds / blood
  • Bridged Bicyclo Compounds / therapeutic use*
  • Cerebrovascular Disorders / drug therapy*
  • Chromatography, High Pressure Liquid
  • Cyclooxygenase Inhibitors / therapeutic use*
  • Dose-Response Relationship, Drug
  • Humans
  • Nicotinic Acids / blood
  • Nicotinic Acids / therapeutic use*
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Thromboxane B2 / blood

Substances

  • Bridged Bicyclo Compounds
  • Cyclooxygenase Inhibitors
  • Nicotinic Acids
  • Platelet Aggregation Inhibitors
  • Thromboxane B2
  • 6-Ketoprostaglandin F1 alpha
  • KC 764