Drotaverine

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Drotaverine
File:Drotaverine.svg
Systematic (IUPAC) name
(Z)-1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline
Clinical data
Routes of
administration
Oral, intravenous
Pharmacokinetic data
Bioavailability Highly variable
Protein binding 80 to 95%
Metabolism Hepatic
Biological half-life 7 to 12 hours
Excretion Fecal and renal
Identifiers
CAS Number 985-12-6
ATC code A03AD02 (WHO)
PubChem CID 1712095
Chemical data
Formula C24H31NO4
Molar mass 397.507 g/mol[[Script error: No such module "String".]]
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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.[citation needed] Drotaverine has been shown to possess dose-dependant analgesic effects in animal models.[1] One small study has shown drotaverine to be eliminated mainly non-renally.[2]

A few small 2003 studies found drotaverine to be nearly 80% effective in treating renal colic.[3][4] It has also been studied in accelerating labor by speeding up cervical dilation, but the results have been conflicting.[5][6][7] Drotaverine has been shown to be effective in managing pain during hysteroscopy and endometrial biopsy when administered together with mefenamic acid.[8] IBS patients presenting with predominant diarrhea are more likely to benefit from Buscopan.[9] Drotaverin has also been tested in combination with rimantadine for antiviral activity against A and B type influenza.[10] Drotaverin has an adverse effects frequency of 0.9%, side effects being relatively uncommon.[11]

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

References

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pl:Drotaweryna ru:Дротаверин
  1. Stepaniuk AG, Stepaniuk NG, Stoliarchuk AA, Stepaniuk GI, Chernobrovyĭ VN (1998). "[The characteristics of the analgesic action of nitrosorbide and no-shpa]". Eksperimental'naia I Klinicheskaia Farmakologiia (in Russian). 61 (4): 17–9. PMID 9783101. 
  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. 
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  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: 249–50. doi:10.1134/S0012496607030234. PMID 17668635. 
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