Drotaverine is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor, and it is also an L-type voltage-dependent calcium channel (L-VDCC) blocker, Drotaverine blocks the degradation of 3',5'-cyclic adenosine monophosphate. Inhibition of PDE4 leads to elevated levels of cAMP, leading to smooth muscle relaxation.
Drotaverin also acts as a cytostatic compound for several human tumor cell lines and nonmalignant mouse fibroblasts, and EC50 values as low as 3.0 μM were observed in SRB assays for HT-29 human colorectal carcinoma cells.
| Molecular Weight | 411.49 |
| Formula | C24H29NO5 |
| CAS Number | 54088-62-9 |
| Solubility (25°C) | DMSO (ultrasonic and warming) |
| 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.
[4] Ajay Shyam Kanbur, et al. Indian J Urol. Drotaverine-induced priapism
[5] Vyom Aggarwal. Indian Pediatr. Drotaverine for Recurrent Abdominal Pain in Children
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