What question did this study set out to answer?

The aim is to evaluate the inhibitory effects of dronedarone on muscarinic K+ currents in guinea pig atrial cells compared to amiodarone.

December 1, 2000Journal of Cardiovascular Pharmacology

Inhibitory Effects of Dronedarone on Muscarinic K+ Current in Guinea Pig Atrial Cells

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Why the study?

Does dronedarone inhibit muscarinic K+ current more potently than amiodarone in guinea pig atrial cells?

Population

Single cells isolated from guinea pig atria

Comparison

Dronedarone (0.01, 0.1, and 1 microM) vs Amiodarone (0.1, 1, and 10 microM)

Design

Preclinical

Authors

EGEric GuillemareSanofi (France)AMAline MarionSanofi (France)DNDino NisatoSanofi (France)

Discussion

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Implication

Hypothesis-generating for dronedarone's atrial selectivity in AF; leaves open translation to human efficacy versus amiodarone.

Key Points

The aim is to evaluate the inhibitory effects of dronedarone on muscarinic K+ currents in guinea pig atrial cells compared to amiodarone.
Single cells from guinea pig atria were isolated for the patch-clamp technique.
Dronedarone and amiodarone were tested at varying concentrations (0.01 to 1 microM).
Effects on carbachol-induced K+ current were measured by the IC50 values.
Dronedarone inhibited I(K(ACh)) with an IC50 slightly above 10 nM, compared to amiodarone’s 1 microM.
At 0.01 and 0.1 microM, dronedarone reduced GTP-gamma-S induced K+ current by 28% and 58%, respectively.
Dronedarone is approximately 100 times more potent than amiodarone in inhibiting I(K(ACh)).

Structured PICO

Does dronedarone inhibit muscarinic K+ current more potently than amiodarone in guinea pig atrial cells?

Population

Single cells isolated from guinea pig atria

Intervention

Dronedarone (0.01, 0.1, and 1 microM)

Comparator

Amiodarone (0.1, 1, and 10 microM)

Outcome

Inhibition of the muscarinic acetylcholine receptor-operated K+ current (I(K(ACh))) activated by carbachol or GTP-gamma-Ssurrogate

Dronedarone is approximately 100 times more potent than amiodarone in inhibiting muscarinic K+ current in guinea pig atrial cells, which may contribute to its antiarrhythmic efficacy in atrial fibrillation.

Cite This Study

Guillemare et al. (2000) studied this question.

synapsesocial.com/papers/6a7153a41556b380a2271ffa https://doi.org/10.1097/00005344-200012000-00017

Topics

Persistent AF management Atrial fibrillation

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Inhibitory Effects of Dronedarone on Muscarinic K+ Current in Guinea Pig Atrial Cells

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

Topics

Inhibitory Effects of Dronedarone on Muscarinic K+ Current in Guinea Pig Atrial Cells

Discussion

Member takes

Implication

Key Points

Structured PICO

Cite This Study

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