Inhibitory mechanisms of gabapentin, an antiseizure drug, on platelet aggregation

Chi Feng Pan, Ming Yi Shen, Chih Jen Wu, George Hsiao, Duen Suey Chou, Joen Rong Sheu

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Gabapentin (Neurontin) is an analogue of gamma-aminobutyric acid (GABA) that is effective against partial seizures. Gabapentin has been reported to modulate serotonin release from platelets, but the effects of gabapentin on platelet activation have not been explored. In this study, gabapentin concentration-dependently (60-240 μM) inhibited platelet aggregation in washed platelets stimulated by collagen (1 μg mL-1), ADP (20 μM) and arachidonic acid (60 μM). Gabapentin (120 and 240 μM) also concentration-dependently inhibited collagen (1 μg mL-1)-induced phosphoinositide breakdown, intracellular Ca2+ mobilization, thromboxane A2 formation, and p38 MAPK phosphorylation in human platelets. In conclusion, the most important findings of this study suggest that gabapentin inhibits platelet aggregation, at least in part, through the phospholipase C-inositol 1,4,5-trisphosphate-thromboxane A2-Ca 2+ pathway. Thus, it is possible that gabapentin treatment, alone or in combination with other antiplatelet drugs, may induce or potentiate inhibition of platelet aggregation, which may affect haemostasis in-vivo.

Original languageEnglish
Pages (from-to)1255-1261
Number of pages7
JournalJournal of Pharmacy and Pharmacology
Volume59
Issue number9
DOIs
Publication statusPublished - Sep 2007

Fingerprint

Platelet Aggregation
Pharmaceutical Preparations
Thromboxane A2
Blood Platelets
Collagen
Inositol 1,4,5-Trisphosphate
gabapentin
Platelet Aggregation Inhibitors
Platelet Activation
Type C Phospholipases
p38 Mitogen-Activated Protein Kinases
Phosphatidylinositols
Hemostasis
Arachidonic Acid
Adenosine Diphosphate
gamma-Aminobutyric Acid
Serotonin
Seizures
Phosphorylation

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

Cite this

Inhibitory mechanisms of gabapentin, an antiseizure drug, on platelet aggregation. / Pan, Chi Feng; Shen, Ming Yi; Wu, Chih Jen; Hsiao, George; Chou, Duen Suey; Sheu, Joen Rong.

In: Journal of Pharmacy and Pharmacology, Vol. 59, No. 9, 09.2007, p. 1255-1261.

Research output: Contribution to journalArticle

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