Terfenadine is an antihistamine compound that is normally fully metabolized in the liver by the cytochrome P450 CYP3A4 subtype enzyme into the active form fexofenadine.
| Molecular Weight | 471.67 |
| Formula | C32H41NO2 |
| CAS Number | 50679-08-8 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Mayra Delgado-Ramrez, et al. Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels
[2] D W Aaronson. Effects of terfenadine on psychomotor performance. An overview
[3] J Soto, et al. Terfenadine-induced tremor
[4] R Jankowski, et al. Effect of terfenadine on nasal provocation
[5] H C Masheter. Terfenadine. The first nonsedating antihistamine
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