The Role of Local Anesthetic Effects in the Actions of Antiarrhythmic Drugs

Gintant, Gary A.; Hoffman, Brian F.

doi:10.1007/978-3-642-71110-7_7

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1987

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Cited by 6 publications

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“…Local anesthetic potency varies considerably between tissues and according to experimental conditions. 97,102 Regarding the active form of the local anesthetic molecule, it is assumed that the most active form is the cationic form,39,42 but why then are neutral drugs such as benzocaine (H2NC6H4C02C2H5) a powerful local anesthetic and anionic drugs such as phenobarbital…”

Section: Overviewmentioning

confidence: 99%

QSAR (quantitative structure-activity relationship) studies on local anesthetics

Gupta¹

1991

Chem. Rev.

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Section: Overviewmentioning

confidence: 99%

QSAR (quantitative structure-activity relationship) studies on local anesthetics

Gupta¹

1991

Chem. Rev.

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Progress and prospects for optimum antiarrhythmic drug design

Courtney¹

1987

Cardiovasc Drug Ther

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Different class I drugs slow down to differing degrees the rate at which sodium channel availability, hence excitability, recovers after action potentials. Drugs that produce longer recovery half-times generally produce greater proarrhythmic side effects. Increased lipid solubility may improve a drug's "potency" for blocking channels yet with implications for adverse effects. Drug action may be potentiated in depolarized and acidotic tissue via modulation of the recovery process. A knowledge of molecular properties of antiarrhythmic drugs helps to define these modes of interaction with the sodium channels and, hence, will help in future drug design. Prospects for improving our understanding of ionic events involved in the repolarization phase of cardiac action potentials are also outlined. The development of successful strategies for controlling reentrant arrhythmias will probably require a thorough understanding of both class I and class III drug actions at the level of the membrane ion channel.

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