The in-vitro and ex-vivo effects of chloroquine sulphate on platelet function: implications for malaria prophylaxis in patients with impaired haemostasis

J Trop Med Hyg. 1990 Apr;93(2):112-5.

Abstract

Platelet aggregation responses were studied in platelet-rich plasma from six healthy volunteers before and 2 and 6 h after ingestion of 600 mg chloroquine sulphate. Apart from a mild reduction in height of aggregation response to 1 microgram ml-1 collagen 2 h post-drug ingestion (mean percentage of pre-drug values +/- s.e.m. = 87.8% +/- 4.0%; P = 0.04), no significant differences were observed in platelet responses to ADP (1 and 5 microM) or collagen (1 and 4 micrograms ml-1) at 2 or 6 h post-chloroquine compared to the pre-drug values. In vitro, drug concentrations approximately 1000 times greater than those used therapeutically were required for 50% inhibition of platelet aggregation and ATP release in response to 5 microM ADP, 1 microgram ml-1 collagen and 4 micrograms ml-1 collagen (IC50 concentrations +/- s.e.m. for inhibition of aggregation = 98.5 +/- 3.7, 53.5 +/- 56.4 and 113.0 +/- 6.2 mg l-1 respectively; IC50s +/- s.e.m. for inhibition of ATP release = 0.9 +/- 0.2, 14.7 +/- 4.0 and 23.0 +/- 5.3 mg l-1 respectively). These data provide no cause for concern in using chloroquine for malaria prophylaxis in patients with impaired haemostasis.

MeSH terms

  • Adenosine Diphosphate / pharmacology
  • Adenosine Triphosphate / blood
  • Adult
  • Blood Coagulation Disorders / complications
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Chloroquine / pharmacology*
  • Chloroquine / therapeutic use
  • Collagen / pharmacology
  • Female
  • Humans
  • In Vitro Techniques
  • Malaria / complications
  • Malaria / prevention & control
  • Male
  • Platelet Aggregation / drug effects*

Substances

  • Adenosine Diphosphate
  • Chloroquine
  • Adenosine Triphosphate
  • Collagen