Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

Hisakazu Ohtani; Erika Hanada; Michiko Hirota; Hitoshi Sato; Hajime Kotaki; Yasufumi Sawada; Hiroko Uemura; Haruaki Nakaya; Tatsuji Iga

doi:10.1211/0022357991773393

Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

Hisakazu Ohtani, Erika Hanada, Michiko Hirota, Hitoshi Sato, Hajime Kotaki, Yasufumi Sawada, Hiroko Uemura, Haruaki Nakaya, Tatsuji Iga

Research output: Contribution to journal › Article › peer-review

13 Citations (Scopus)

Abstract

We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (I(K)) and transient outward potassium current (I(to)) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and epinastine were found to inhibit I(K) with IC50 values of 5.96, 15.3 and 145 μM, respectively. I(to) was suppressed by epinastine with an IC50 value of 69.5 μM. The order of arrhythmogenicity, assessed by the inhibition of I(K), was ranked as terfenadine > ebastine > epinastine, consistent with that of the potencies of each drug for QT prolongation reported in rats.

Original language	English
Pages (from-to)	1059-1063
Number of pages	5
Journal	Journal of Pharmacy and Pharmacology
Volume	51
Issue number	9
DOIs	https://doi.org/10.1211/0022357991773393
Publication status	Published - 1999 Sept
Externally published	Yes

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science

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title = "Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes",

abstract = "We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (I(K)) and transient outward potassium current (I(to)) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and epinastine were found to inhibit I(K) with IC50 values of 5.96, 15.3 and 145 μM, respectively. I(to) was suppressed by epinastine with an IC50 value of 69.5 μM. The order of arrhythmogenicity, assessed by the inhibition of I(K), was ranked as terfenadine > ebastine > epinastine, consistent with that of the potencies of each drug for QT prolongation reported in rats.",

author = "Hisakazu Ohtani and Erika Hanada and Michiko Hirota and Hitoshi Sato and Hajime Kotaki and Yasufumi Sawada and Hiroko Uemura and Haruaki Nakaya and Tatsuji Iga",

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T1 - Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

AU - Ohtani, Hisakazu

AU - Hanada, Erika

AU - Hirota, Michiko

AU - Sato, Hitoshi

AU - Kotaki, Hajime

AU - Sawada, Yasufumi

AU - Uemura, Hiroko

AU - Nakaya, Haruaki

AU - Iga, Tatsuji

PY - 1999/9

Y1 - 1999/9

N2 - We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (I(K)) and transient outward potassium current (I(to)) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and epinastine were found to inhibit I(K) with IC50 values of 5.96, 15.3 and 145 μM, respectively. I(to) was suppressed by epinastine with an IC50 value of 69.5 μM. The order of arrhythmogenicity, assessed by the inhibition of I(K), was ranked as terfenadine > ebastine > epinastine, consistent with that of the potencies of each drug for QT prolongation reported in rats.

AB - We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (I(K)) and transient outward potassium current (I(to)) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and epinastine were found to inhibit I(K) with IC50 values of 5.96, 15.3 and 145 μM, respectively. I(to) was suppressed by epinastine with an IC50 value of 69.5 μM. The order of arrhythmogenicity, assessed by the inhibition of I(K), was ranked as terfenadine > ebastine > epinastine, consistent with that of the potencies of each drug for QT prolongation reported in rats.

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Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

Abstract

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