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drotaverine
- Development stage
- Phase 4
- Lead developer
- Chinoin
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Intramuscular
01
Overview
Drotaverine is a synthetic benzylisoquinoline derivative and antispasmodic drug primarily used to relieve smooth muscle spasms in the gastrointestinal and genitourinary tracts. It acts as a selective inhibitor of phosphodiesterase-4 (PDE4), leading to increased intracellular cyclic adenosine monophosphate (cAMP) levels and subsequent smooth muscle relaxation. Additionally, it inhibits voltage-dependent L-type calcium channel, further contributing to its spasmolytic effect. Drotaverine is structurally related to papaverine but exhibits greater antispasmodic potency. It is indicated for conditions such as gastrointestinal colic, biliary dyskinesia, menstrual pain (dysmenorrhea), and has been investigated for use in labor augmentation and other spastic disorders. The drug does not significantly affect the autonomic nervous system or penetrate the central nervous system[1][2][3][4][6][8].
- Brand names
- No-SpaDrotaverina
- Other names
- drotaverine hydrochlorideDrotaverin
02
Targets
LTCC (Voltage-gated calcium channel (L-type))PDE4A
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