TABLE 3.
Comparative efficacy of antiepileptic drugs in rodent seizure models relative to KRM-II-81
| Assay | Efficacy | No Efficacy |
|---|---|---|
| Corneal kindlinga | ||
| KRM-II-81, 8.0 | Tpm, 50% protection at 58.9 | |
| Lev, 57.0 | ||
| Ltg, 37.1 | ||
| Pht, 66.9 | ||
| Cbz, 143.5 | ||
| Val, 728.0 | ||
| Mesial temporal lobeb | ||
| KRM-II-81, 15 | Val, 400 | |
| Lev, 800 | Ltg, 30 | |
| Cbz, 100 | ||
| Lamotrigine-insensitive kindlingc | ||
| Seizure severity | KRM-II-81, 5 | Etho, 200 |
| Cbz, 80 | Ltg, 50 | |
| Gpt, 150 | Pht, 40 | |
| Lev, 400 | Tpm, 300 | |
| Val, 135 | ||
| Lamotrigine-insensitive kindlingc | ||
| Seizure protection | KRM-II-81, 20 | Ltg, 50 |
| Cbz, 80 | Lev, 400 | |
| Etho, 200 | Pht, 40 | |
| Gbt, 300 | Tpm, 300 | |
| Val, 135 | ||
| Lamotrigine-insensitive kindlingc | ||
| Seizure duration | KRM-II-81, 10 | Etho, 200 |
| Cbz, 80 | Ltg, 50 | |
| Gbt, 300 | Lev, 400 | |
| Val, 135 | Pht, 40 | |
| Tpm, 300 | ||
| Kainate-induced chronic epilepsyd | ||
| Seizure burden | KRM-II-81, 20 × 3 | Ltg, 30 × 2 |
| Cbz, 30 × 3 | Pht, 10 × 2 | |
| Lev, 150 × 2 | Etho, 150 × 1 | |
| Gpt, 300 × 2 | Val, 300 × 2 | |
| Tpm, 300 × 2 | ||
| Kainate-induced chronic epilepsyd | ||
| Seizure freedom | KRM-II-81, 20 × 3 | Lev, 150 × 2 |
| Cbz, 30 × 3 | Ltg, 30 × 2 | |
| Gpt, 300 × 2 | Pht, 10 × 2 | |
| Tpm, 300 × 2 | Etho, 150 × 1 | |
| Val, 300 × 2 |
Cbz, carbamazepine; Etho, ethosuxamide; Gbt, gabapentin; Lev, leviteracetam; Ltg, lamotrigine; Pht, phenytoin; Tpm, topiramate; Val, valproate.
Doses are ED50 values in milligrams per kilogram. Data are from Rowley and White (2010) except for KRM-II-81 (present study).
Doses are minimal effective doses in milligrams per kilogram; Drugs in the no efficacy column are drugs that were active but only at doses with side effects. Data are from except for KRM-II-81 (present study).
Doses are minimal effective doses in milligrams per kilogram. Data are from Metcalf et al. (2019) except for KRM-II-81 (present study).
Doses are in milligram per kilogram × number of times per day dosed. Data are from Dr. K. S. Wilcox (personal communication) except for KRM-II-81 (present study).