Cardiac actions of ciprofloxacin

Excerpt:


J Pharm Pharmacogn Res 6(2): 65-71, 2018. DOI: https://doi.org/10.56499/jppres17.292_6.2.65 Short Communication Ciprofloxacin, an antibiotic with cardiac actions on isolated rat hearts [Ciprofloxacina, un antibiótico con acciones cardiacas sobre corazones aislados de rata] Loipa Galán-Martínez*, Alberto D. Calderín-Pulido, Alicia Fleites-Vázquez, Julio L. Álvarez Laboratorio de Electrofisiología. Departamento de Investigaciones. Instituto de Cardiología y Cirugía Cardiovascular. Paseo y 17, … Continue reading Cardiac actions of ciprofloxacin

J Pharm Pharmacogn Res 6(2): 65-71, 2018.

DOI: https://doi.org/10.56499/jppres17.292_6.2.65

Short Communication

Ciprofloxacin, an antibiotic with cardiac actions on isolated rat hearts

[Ciprofloxacina, un antibiótico con acciones cardiacas sobre corazones aislados de rata]

Loipa Galán-Martínez*, Alberto D. Calderín-Pulido, Alicia Fleites-Vázquez, Julio L. Álvarez

Laboratorio de Electrofisiología. Departamento de Investigaciones. Instituto de Cardiología y Cirugía Cardiovascular. Paseo y 17, Vedado, cp 10400, La Habana, Cuba.

*E-mail: loipa@infomed.sld.cu

Abstract

Context: Ciprofloxacin is the most commonly used fluoroquinolone and is prescribed as the antibiotic of choice in the treatment of several microbial infections. Some clinical reports have suggested that ciprofloxacin may induce QT-interval prolongation and Torsades de Pointes arrhythmias. This drug is a weak inhibitor of a rapid component of the cardiac delayed rectifier potassium current IKr, but there are few electrophysiological data available to assess whether ciprofloxacin has the potency to provoke QT prolongation and subsequent Torsades de Pointes arrhythmias.

Aims: To evaluate the effect of ciprofloxacin on the contractile and electrical activity of isolated rat hearts.

Methods: The Langendorff technique was performed in rat hearts, and the effects of ciprofloxacin (0.001 - 100 μM) were measured on the cardiac force of contraction and on the RR, QRS and QTc intervals. The arrhythmogenic potential and the ventricular fibrillation threshold were evaluated with ciprofloxacin.

Results: Ciprofloxacin decreased the force of contraction of all hearts studied, in a concentration-dependent manner. The estimated IC50 for the inotropic negative effect was 0.15 ± 0.04 μM. Ciprofloxacin significantly prolonged the QRS complex, QTc and RR interval. Significant arrhythmic effects with ciprofloxacin were shown and the ventricular fibrillation threshold was decreased.

Conclusions: These results suggest that ciprofloxacin exerted effects on cardiac Na+, K+ and Ca2+ channels. The actions of ciprofloxacin require further studies at the cellular level. These conclusions may account for clinical data that have been reported previously.

Keywords: antibiotic; arrhythmia; ciprofloxacin; ECG; fluoroquinolones; QT prolongation.

Resumen

Contexto: La ciprofloxacina es la fluoroquinolona más comúnmente empleada como antibiótico de elección en el tratamiento de diversas infecciones microbianas. Algunos reportes clínicos han sugerido que la ciprofloxacina puede prolongar el intervalo QT y causar arritmias del tipo Torsión de Puntas. Este fármaco es un débil bloqueador del componente rápido de la corriente de potasio cardiaca rectificadora retardada IKr, pero hay pocos estudios electrofisiológicos que permitan explicar su potencia de acción para provocar la prolongación del intervalo QT y las consecuentes arritmias del tipo Torsión de Puntas.

Objetivos: Evaluar los efectos de ciprofloxacina sobre la actividad contráctil y eléctrica de corazones aislados de rata.

Métodos: Se llevó a cabo la técnica de Langendorff en los corazones de rata y se midieron los efectos de ciprofloxacina (0.001 – 100 μM) sobre la fuerza de contracción cardiaca y sobre los intervalos RR, QRS y QTc. Se evaluó el potencial arritmogénico y la variación del umbral de fibrilación ventricular con ciprofloxacina.

Resultados: La ciprofloxacina disminuyó la fuerza de contracción de todos los corazones estudiados de manera dependiente de la concentración. El valor de IC50 estimado para el efecto inotrópico negativo de ciprofloxacina fue de 0.15 ± 0.04 μM. El complejo QRS y los intervalos RR y QTc fueron prolongados significativamente con ciprofloxacina. Se observaron eventos arrítmicos con este compuesto y disminuyó significativamente el umbral de fibrilación ventricular.

Conclusiones: Estos resultados sugieren que la ciprofloxacina ejerce acciones sobre canales cardiacos de Na+, K+ y Ca2+, lo cual requiere la realización de otros estudios a nivel celular. Estas conclusiones pueden explicar los hallazgos clínicos reportados previamente.

Palabras Clave: antibiótico; arritmia; ciprofloxacina; ECG; fluoroquinolonas; QT prolongado.

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Citation Format: Galán-Martínez L, Calderín-Pulido AD, Fleites-Vázquez A, Álvarez JL (2018) Ciprofloxacin, an antibiotic with cardiac actions on isolated rat hearts. J Pharm Pharmacogn Res 6(2): 65–71. DOI: https://doi.org/10.56499/jppres17.292_6.2.65

© 2018 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

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