Drug intelligence / Profile preview

ajmaline

Development stage
Phase 4
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Ajmaline is a class Ia antiarrhythmic alkaloid derived from the root of Rauwolfia serpentina and other plant sources. It is primarily used to manage various forms of tachycardias, including atrial fibrillation in patients with Wolff–Parkinson–White syndrome and well-tolerated monomorphic ventricular tachycardias. Ajmaline is also widely used as a diagnostic agent to unmask the type-1 Brugada syndrome electrocardiogram pattern. Its mechanism of action involves blocking sodium channels (notably the Nav 1.5 channel), which lengthens cardiac action potentials and slows conduction velocity, thereby stabilizing abnormal heart rhythms. Ajmaline also has additional effects on potassium (including hERG) and calcium channels, further prolonging repolarization and refractory periods[1][2][3][6].

Brand names
Gilurytmal
02

Targets

KCND3 (Potassium voltage-gated channel subfamily D member 3 with KChIP2 coexpression complex)KCNA5 (Ultra-rapid delayed rectifier potassium channel)KATP channel (ATP-sensitive potassium channel)KCNH2 (Voltage-gated potassium channel subfamily H member 2)SCN5A (Sodium channel protein type 5 subunit alpha)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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