Tocainide
Tocainide is a class Ib antiarrhythmic agent structurally related to lidocaine that blocks cardiac sodium channels in an activated/inactivated state-dependent manner, reducing the rate of rise of the action potential and shortening the effective refractory period in ventricular myocardium. It was used orally for life-threatening ventricular arrhythmias but was withdrawn from clinical use due to severe adverse effects including agranulocytosis, pulmonary fibrosis, and pulmonary edema. Unlike lidocaine, it is orally bioavailable due to its primary amine structure, but this did not outweigh its toxicity profile.
Molecular Weight
192.2600 g/mol
LogP
0.80
TPSA
55.10 Ų
Lipinski RO5
Pass
Pharmacokinetics (PK)
Pharmacodynamics (PD)
2D Structure
Cite this structure
Embed this structure
SMILES
Cc1cccc(C)c1NC(=O)C(C)N
InChI
InChI=1S/C11H16N2O/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12/h4-6,9H,12H2,1-3H3,(H,13,14)
Molecular Formula
C11H16N2O
HBD / HBA
2 / 2
Rotatable Bonds
2
Heavy Atoms
14
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
Tocainide is a class Ib antiarrhythmic agent structurally related to lidocaine that blocks cardiac sodium channels in an activated/inactivated state-dependent manner, reducing the rate of rise of the action potential and shortening the effective refractory period in ventricular myocardium. It was used orally for life-threatening ventricular arrhythmias but was withdrawn from clinical use due to severe adverse effects including agranulocytosis, pulmonary fibrosis, and pulmonary edema. Unlike lidocaine, it is orally bioavailable due to its primary amine structure, but this did …
Yes, Tocainide is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1762. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 38945. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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