Drotaverine
A03A - Drugs for functional bowel disorders
ATC A03AD02
Small molecule
Natural product
JFDA label: Dro Spaz
Mechanism of Action
Inhibitor of Phosphodiesterase 4 — Phosphodiesterase 4 inhibitor
| Target | Action | Gene / class |
|---|---|---|
| Phosphodiesterase 4 efficacy | INHIBITOR |
Indications
Off-label
- Bile Duct Diseases
- Digestive System Diseases
Pregnancy & Lactation
Lactation
Compatible
Hale L1
If a mother requires drotaverine, it is not a reason to discontinue breastfeeding.
Chemistry & Properties
| Formula | C24H31NO4 |
|---|---|
| Molecular weight | 397.52 g/mol |
| IUPAC name | (1Z)-1-[(3,4-diethoxyphenyl)methylidene]-6,7-diethoxy-3,4-dihydro-2H-isoquinoline |
| CAS | 14009-24-6 |
| PubChem CID | 1712095 |
| InChIKey | OMFNSKIUKYOYRG-MOSHPQCFSA-N |
| logP | 4.93 (XLogP 5.4) |
| Polar surface area | 48.95 Ų |
| H-bond acceptors / donors | 5 / 1 |
| Drug-likeness (QED) | 0.65 |
| Lipinski violations | 0 |
SMILES
CCOc1ccc(/C=C2\NCCc3cc(OCC)c(OCC)cc32)cc1OCCBiology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | Yes |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP1A2 | Substrate | — |
| CYP2B6 | Inhibitor | — |
| CYP2B6 | Substrate | — |
| CYP2C19 | Substrate | — |
| CYP2C8 | Inhibitor | — |
| CYP2C9 | Inhibitor | — |
| CYP2C9 | Substrate | — |
| CYP3A4 | Inhibitor | — |
| CYP3A4 | Substrate | — |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (3)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Dro Spaz | Tablet 40 mg | 20 tab | aburezeq drug store | 2.340 |
| Dro Spaz | Tablet 80 mg | 10 tab pack varies | aburezeq drug store | 2.630 |
| Dro Spaz | Tablet 80 mg | 20 tab pack varies | aburezeq drug store | 5.000 |