Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H31NO4.ClH |
| Molecular Weight | 433.968 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCOC1=CC=C(\C=C2/NCCC3=C2C=C(OCC)C(OCC)=C3)C=C1OCC
InChI
InChIKey=JBFLYOLJRKJYNV-MASIZSFYSA-N
InChI=1S/C24H31NO4.ClH/c1-5-26-21-10-9-17(14-22(21)27-6-2)13-20-19-16-24(29-8-4)23(28-7-3)15-18(19)11-12-25-20;/h9-10,13-16,25H,5-8,11-12H2,1-4H3;1H/b20-13-;
Drotaverine, an antispasmodic drug, is a synthetic derivative of the natural isoquinoline alkaloid of Papaver somniferum, papaverine. It inhibits cyclic-3',5'-nucleotide-phophodiesterase (PDE) enzymes with concentration-dependent specificity, in addition, it behaves as a L-type voltage- operated calcium channel (L-VOCC) blocker. Drotaverin also acts as a cytostatic compound for several human tumor cell lines. Drotaverine is an effective medicine to treat spasm or twitches of the smooth muscles in the stomach and heart. It is used to relieve pain caused due to irritable bowel syndrome, headache, menstrual periods, and is also used to relieve cervical spasm during labor.
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. | 2010-12 |
|
| [Acute intermittent porphyria and oral contraception. Case report]. | 2006-03 |
|
| Pharmacokinetics and bioavailability of drotaverine in humans. | 1996-07-01 |
Patents
Sample Use Guides
The drug is administered for interior use. 1-2 tablets (0.04—0.08 g) 2—3 time a day. In children under 6 0.01—0.02 g 1—2 times a day, in children of 6—12 years old — 0.02 g 1—2 times a day. In children after 12 the adult dose.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27879007
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.
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NCI_THESAURUS |
C29704
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NCI_THESAURUS |
C29698
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DTXSID40243590
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SUB01843MIG
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6437861
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DB06751
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236960
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m4773
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100000087720
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C97980
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985-12-6
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24ZVH4C669
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ACTIVE MOIETY
SUBSTANCE RECORD