Table 2.
Clinically available drugs that affect late INa. The blockers are in order of selectivity for late INa with concentrations for half block IC50 [6] and therapeutic concentrations [50]. For IC50 for drugs that increase late INa we report the concentration for half maximal increase from control for dofetilide [39] and the concentration to double late INa for Nilotonib [38]
| Drug | Ratio Late:Peak IC50 |
Late INa
IC50 μM |
Therapeutic concentration range μM |
|---|---|---|---|
| Block of late INa | |||
| Ranolazine | 38 - 61 | 7 | 0.4 - 6.1 |
| Amiodarone | 13 - 60 | 3 - 6.7 | 0.8 - 3.9 |
| Mexilitene | 9 - 51 | 3 - 5 | 3.4 - 9.5 |
| Lidocaine | 3 - 12 | 25 | 0.8 - 4.2 |
| Propranalol | 7 | 3 | 0.1 – 0.4 |
| Flecainide | 3 - 7 | 1.4 | 0.5 - 2.4 |
| Vernakalant | 3 - 5 | 30 | 7.2 - 14.3 |
| Quinidine | 1 | 12 | 9.3 - 24.7 |
| Increased Late INa | |||
| Dofetilide | .103 | .005-.023 | |
| Nilotinib | 1.0 | 1.7-62 | |