Page 7
Features of the blockade of L-type voltage-gated Ca2+ channels evoked by verapamil and diltiazem
The manner in which inhibitors of Ca2+ influx block L-type voltage-gated Ca2+ channels helps to determine their tissue selectivity (click to see the selectivity spectrum).
Since these agents can only access their receptors (binding sites) when the channel pore is open, their blockade of the L-type channel exhibits use-dependency. The channel blockade evoked by these drugs occurs best when the channels are opening most frequently.
Since they do not inhibit the metabolism of bradykinin, they provide a useful alternative in patients who cannot tolerate the dry cough associated with the use of ACE inhibitors.
