Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally.
Indication
Used in the treatment of functional bowel disorders and alleviating pain in renal colic.
Pharmacology
Drotaverine is a spasmolytic agent by inhibiting PDE4 in smooth muscle cells.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic
Absorption
Bioavailability is highly variable
Half Life
7 to 12 hours
Protein Binding
80 to 95%
References
•
Bolaji OO, Onyeji CO, Ogundaini AO, Olugbade TA, Ogunbona FA: Pharmacokinetics and bioavailability of drotaverine in humans. Eur J Drug Metab Pharmacokinet. 1996 Jul-Sep;21(3):217-21.
[Pubmed]