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Drotaverine

Clinical data
Routes of administration	Oral, intravenous
ATC code	A03AD02 (WHO)
Pharmacokinetic data
Bioavailability	Highly variable
Protein binding	80 to 95%
Metabolism	Hepatic
Elimination half-life	7 to 12 hours
Excretion	Fecal and renal
Identifiers
IUPAC name (Z)-1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline
CAS Number	985-12-6
PubChem CID	1712095
ChemSpider	1361582
UNII	98QS4N58TW
KEGG	D07879
ChEMBL	ChEMBL551978
CompTox Dashboard (EPA)	DTXSID60161227
ECHA InfoCard	100.110.916
Chemical and physical data
Formula	C24H31NO4
Molar mass	397.507 g/mol g·mol
3D model (JSmol)	Interactive image
SMILES O(c1ccc(cc1OCC)\C=C3\c2c(cc(OCC)c(OCC)c2)CCN3)CC
InChI InChI=1S/C24H31NO4/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/b20-13- Key:OMFNSKIUKYOYRG-MOSHPQCFSA-N
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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.

A few small 2003 studies found drotaverine to be nearly 80% effective in treating renal colic. It has also been studied in accelerating labor by speeding up cervical dilation, but the results have been conflicting. Drotaverine has been shown to be effective in paracervical block in managing pain during hysteroscopy and endometrial biopsy when administered together with mefenamic acid. IBS patients presenting with predominant diarrhea are more likely to benefit from Buscopan. Drotaverin has also been tested in combination with rimantadine for antiviral activity against A and B type influenza. Drotaverin has an adverse effects frequency of 0.9%, side effects being relatively uncommon.

Drotaverine in sold under brand name No-Spa (Chinoin Pharmaceutical and Chemical Works, Hungary, a member of the Sanofi-Aventis).

References

1. Stepaniuk AG, Stepaniuk NG, Stoliarchuk AA, Stepaniuk GI, Chernobrovyĭ VN (1998). "". Eksperimental'naia I Klinicheskaia Farmakologiia (in Russian). 61 (4): 17–9. PMID 9783101.{{cite journal}}: CS1 maint: multiple names: authors list (link)
2. Bolaji OO, Onyeji CO, Ogundaini AO, Olugbade TA, Ogunbona FA (1996). "Pharmacokinetics and bioavailability of drotaverine in humans". European Journal of Drug Metabolism and Pharmacokinetics. 21 (3): 217–21. doi:10.1007/BF03189716. PMID 8980918.{{cite journal}}: CS1 maint: multiple names: authors list (link)
3. Romics I, Molnár DL, Timberg G; et al. (2003). "The effect of drotaverine hydrochloride in acute colicky pain caused by renal and ureteric stones". BJU International. 92 (1): 92–6. doi:10.1046/j.1464-410X.2003.04262.x. PMID 12823389. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
4. Garmish OS, Zabashnyĭ SI, Smirnova EV, Kobeliatskiĭ IuIu (2003). "". Klinichna Khirurhiia (in Russian) (2): 47–50. PMID 12784437. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
5. Singh KC, Jain P, Goel N, Saxena A (2004). "Drotaverine hydrochloride for augmentation of labor". International Journal of Gynaecology and Obstetrics. 84 (1): 17–22. doi:10.1016/S0020-7292(03)00276-5. PMID 14698825. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
6. Madhu C, Mahavarkar S, Bhave S (2009). "A randomised controlled study comparing Drotaverine hydrochloride and Valethamate bromide in the augmentation of labour". Archives of Gynecology and Obstetrics. 282 (1): 11–5. doi:10.1007/s00404-009-1188-8. PMID 19644697. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
7. Gupta B, Nellore V, Mittal S (2008). "Drotaverine hydrochloride versus hyoscine-N-butylbromide in augmentation of labor". International Journal of Gynaecology and Obstetrics. 100 (3): 244–7. doi:10.1016/j.ijgo.2007.08.020. PMID 18031745. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
8. Sharma JB, Aruna J, Kumar P, Roy KK, Malhotra N, Kumar S (2009). "Comparison of efficacy of oral drotaverine plus mefenamic acid with paracervical block and with intravenous sedation for pain relief during hysteroscopy and endometrial biopsy". Indian Journal of Medical Sciences. 63 (6): 244–52. doi:10.4103/0019-5359.53394. PMID 19602758. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link) CS1 maint: unflagged free DOI (link)
9. Khalif IL, Quigley EM, Makarchuk PA, Golovenko OV, Podmarenkova LF, Dzhanayev YA (2009). "Interactions between symptoms and motor and visceral sensory responses of irritable bowel syndrome patients to spasmolytics (antispasmodics)". Journal of Gastrointestinal and Liver Diseases. 18 (1): 17–22. PMID 19337628. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
10. Zhilinskaya IN, Konovalova NI, Kiselev OI, Ashmarin IP (2007). "No-Spa and Remantadin are the novel complex preparations that inhibit effectively reproduction of the avian influenza viruses". Doklady Biological Sciences. 414 (1): 249–50. doi:10.1134/S0012496607030234. PMID 17668635.{{cite journal}}: CS1 maint: multiple names: authors list (link)
11. Tar A, Singer J (2002). "". Orvosi Hetilap (in Hungarian). 143 (11): 559–62. PMID 12583325. {{cite journal}}: Unknown parameter |month= ignored (help)

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