Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.4.21.5 (thrombin)
 33,306 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sulfinpyrazone and phenylbutazone block the aggregating action of collagen, antigen-antibody complexes, and gamma globulin-coated surfaces on blood platelets. These drugs do not block the action of ADP or thrombin. Inhibition of surface-induced aggregation appears to be the result of a decreased response of the platelets to surface stimuli, giving rise to diminished release of platelet constituents, such as ADP and serotonin. The intravenous infusion of these drugs produced results similar to those found in the in vitro experiments. Administration of phenylbutazone in doses sufficient to produce marked suppression of the platelet-collagen reaction impaired hemostatic plug formation at the ends of transected mesenteric vessels in rabbits. Since platelet function is considered a factor influencing platelet survival, the effect of phenylbutazone on platelet survival was examined. It was found that phenylbutazone prolonged platelet survival to more than twice the normal time and reduced platelet turnover by nearly 50%. These studies show that drugs which suppress platelet response to surface stimuli alter platelet function in vivo.
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PMID:Alteration of the response of platelets to surface stimuli by pyrazole compounds. 416 1

Platelet studies were performed during a controlled double-blind randomized clinical trial of sulfinpyrazone (Anturane Reinfarction Trial) in 41 patients who had recent myocardial infarction. Aggregation of platelet-rich plasma by thrombin (0.185, 0.246 U/ml), collagen, adenosine diphosphate, and adrenaline (0.23, 0.46, and 0.91 microgram/ml) was estimated after a 12 hour fast including abstinence from drugs and cigarette smoking. The tests were carried out 2 weeks after myocardial infarction and 6, 12, and 24 months later. At the last visit, washed platelet suspensions were also tested for aggregation to thrombin (0.03, 0.015 U/ml) +/- epinephrine (0.55 microgram/ml) and their production of malonyldialdehyde was estimated. A significant (p less than 0.02) reduction (50%) of the aggregation response of platelet-rich plasma to epinephrine was found in the group treated with sulfinpyrazone (n = 21) as compared with the placebo group (n = 20). Also, adrenaline evoked a milder (p less than 0.01) potentiation of aggregation by thrombin of the washed platelet suspensions in the sulfinpyrazone versus the placebo group. Other assays including platelet coagulant activity were not useful in discriminating between the 2 groups. It is concluded that sulfinpyrazone (200 mg 4 times daily) normalizes the platelet response to epinephrine; a relation with the drug-reported reduction of sudden death after myocardial infarction is suggested.
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PMID:Sulfinpyrazone decreases epinephrine-induced platelet aggregation after myocardial infarction. 675 59