Verapamil hydrochloride (VPH) is an orally active L-type calcium channel inhibitor that eliminates calcium channel agonist-induced calcium inward flow and apoptosis. In addition, Verapamil HCl also inhibits voltage-dependent K(+) (Kv) channels, decreasing Kv current amplitude in a concentration-dependent manner, with an apparent K(d) value of 0.82 for inhibition of Kv channels. Verapamil hydrochloride is a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4.
| Molecular Weight | 491.06 |
| Formula | C27H38N2O4.HCl |
| CAS Number | 152-11-4 |
| Solubility (25°C) | Water 40 mg/mL DMSO 30 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
| 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.
[2] Syam Krishna, et al. Degradation of Verapamil hydrochloride in water by gliding arc discharge
[4] Victor Cohen, et al. Tarka® (trandolapril/verapamil hydrochloride extended-release) overdose
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