Drug intelligence / Profile preview

propafenone + propranolol

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Propafenone + propranolol is a combination of two cardiac medications that can interact significantly when used together. Propafenone is a class 1c anti-arrhythmic agent that works as a potent sodium channel blocker, while propranolol is a highly lipid-soluble beta-receptor antagonist. When administered together, propafenone significantly increases propranolol plasma levels (by up to 213% for steady-state concentration) by inhibiting its metabolism, while propranolol does not significantly affect propafenone kinetics. This combination can produce additive effects on cardiac function, including reduced blood pressure and heart rate. Due to the potential for increased propranolol toxicity, this combination requires careful monitoring and potential dose adjustments.

02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)ADRB1 (β1)

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