Abstract
Several calcium channels (L, N, T, P, Q and R) were identified in humans. Of these channels, voltage-sensitive L-type and T-type calcium channels are mainly operative in cardiovascular system. There are five classes of calcium channel blocking drugs: phenylalkylamines, dihydropyridines, benzothiazepines, diphenylpiperazines, and a diarylaminopropylamine. Clinically available calcium channel blockers are dihydropyridines, benzothiazepines and phenylalkylamines. These calcium channel blockers (CCB) are selective and inhibit voltage–sensitive L-type slow calcium channels mediated calcium influx in cardiac myocytes and in smooth muscle by slowing the activation of the L-type calcium channel and also delay its recovery from inactivation. To show its effect, the drugs travel through the slow channel and bind to channel from the inner side of the membrane. They bind more effectively when the channels are in open and in inactivated state and reduce opening frequency of the channels. Verapamil and diltiazem block calcium channels in use (frequency)-dependent (effect is more apparent at faster rates) and in voltage-dependent fashion (more effective blockage in depolarized fibers).
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Tülümen, E., Borggrefe, M. (2020). Modulation of Calcium Handling: Calcium-Channel Modulators. In: Martínez-Rubio, A., Tamargo, J., Dan, G . (eds) Antiarrhythmic Drugs. Current Cardiovascular Therapy. Springer, Cham. https://doi.org/10.1007/978-3-030-34893-9_5
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