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Diltiazem — a drug which defies its kinetics

SummaryDiltiazem is a calcium antagonist effective in the treatment of stable and unstable angina and mild to moderate systemic hypertension with a generally favourable side-effect profile. A number of published studies have attempted to formulate a therapeutic target range, but there appears to be little consensus of opinion. A minimum effective concentration of 40 ng/ml has been proposed by some authors whilst others have chosen 50 ng/ml and others upwards to 100 ng/ml. A review of the reports suggests that a trough concentration of above 50 ng/ml confers a better therapeutic outcome than does the lower concentrations. A number of modified release preparations enabling once a day dosing are available, all purporting to give adequate therapeutic concentrations. However, based on the above assumptions it would appear that those giving sustained concentrations above 50 ng/ml would be those of choice. Furthermore the benefits of once daily preparations lead to improved compliance and therefore improved therapeutic outcome and thus confirm that the modified preparations are the delivery of choice. Once chosen, it is advisable to maintain the same preparation in order to derive maximum clinical benefit.