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The activation of human erythrocyte glutathione S – transferase (GST) by the antihistamines was also observed to be concentration – dependent i.e. higher concentrations produced greater activation of the enzyme. For instance, at cyproheptadine concentrations of 0.20mg% and 0.30mg%, red cell GST activity was increased by 4.99 folds (498.85%) and 6.98 folds (694.28%) respectively. Similarly, at the same concentrations (0.20mg% and 0.30mg%), klemastin activated human erythrocyte GST by 2.87 fold (387.36%) and 3.59 fold (359.20%) respectively, while chlorpheniramine produced activations of 7.82 fold (782.18%) and 8.93 fold (893.10%) respectively.
These results may point to a possible binding-deterioration of these drugs by the human erythrocyte GST.
Global Jnl Medical Sciences Vol.2(2) 2003: 141-144