Drotaverine

Drotaverine
Clinical data
Trade names	No-Spa, Doverin
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral, intravenous, intramuscular
ATC code	A03AD02 (WHO) ;
Legal status
Legal status	OTC (tablets), ℞-only (solution for injection) (RU)[1];
Pharmacokinetic data
Bioavailability	Highly variable (~65%), peak at 45–60 min
Protein binding	95–98%
Metabolism	Hepatic
Elimination half-life	7–16 hours
Excretion	>50% in urine and ~30% in bile[1]
Identifiers
	IUPAC name (Z)-1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline;
CAS Number	14009-24-6 ;
PubChem CID	1712095;
DrugBank	DB06751 ;
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−1
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, used to enhance cervical dilation during childbirth.[2]^:283

It is structurally related to papaverine, is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects.[3]

It is available in Asian and Central and Eastern European countries under several brand names.[4]

An article from 2013 described the effects from overdose (in a 19-year-old woman) as including vomiting, seizures and fatal cardiac toxicity.[5]

In 2016, the young Russian chess player Ivan Bukavshin died of a massive overdose (or poisoning) of the drug, which was originally thought to be a stroke.[6] his doses was 17 mg/kg in the blood stream.

Counterfeits

In Israel the product is known under the brand name "No-Spa" by the general public[7] which did not receive a permit to be distributed by the health ministry,[8] However due to high demand local medical counterfeiters had managed to smuggle No-Spa tablets during the years.[8]

In 2008 the Israeli health organization warned consumers from counterfeit No-SPA pills after a smuggler had been arrested at the Ben Gurion Airport with several thousand pills.[9][10]

In 2011 Israeli patent and trade mark office declined the use of the No-SPA.[7]

References

"Инструкция по применению препарата Но-шпа^® // No-Spa^® (tablets) Full Prescribing Information". National Register of Drugs (in Russian). Chinoin Pharmaceutical and Chemical Works. pp. 3–8.
Padubidri V and Anand E. Title Textbook of Obstetrics. BI Publications Pvt Ltd, 2006 ISBN 9788172252236
"The DrugBank database: Drotaverine". DrugBank Version 4.1. The Metabolomics Innovation Centre. Retrieved 9 August 2014.
Drotaverine - Drugs.com Drugs.com international listings for drotaverine Page accessed June 28, 2015
Drotaverine overdose (case report) Reactions Weekly, Volume 1481 (1), page 17.
Silence, lack of will, indifference (Russian, Chess-News)
NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office,11 July 2007
Health Ministry: Fake drug had been smuggled NRG, 11 March 2009
Health Ministry: Counterfeit NO-SPA pills had been smuggled and are considered a health risk, Globes
"משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa".

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[PI-1] "Инструкция по применению препарата Но-шпа^® // No-Spa^® (tablets) Full Prescribing Information". National Register of Drugs (in Russian). Chinoin Pharmaceutical and Chemical Works. pp. 3–8.

[2] Padubidri V and Anand E. Title Textbook of Obstetrics. BI Publications Pvt Ltd, 2006 ISBN 9788172252236

[drugbank-3] "The DrugBank database: Drotaverine". DrugBank Version 4.1. The Metabolomics Innovation Centre. Retrieved 9 August 2014.

[4] Drotaverine - Drugs.com Drugs.com international listings for drotaverine Page accessed June 28, 2015

[5] Drotaverine overdose (case report) Reactions Weekly, Volume 1481 (1), page 17.

[6] Silence, lack of will, indifference (Russian, Chess-News)

[study-7] NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office,11 July 2007

[smuggler-8] Health Ministry: Fake drug had been smuggled NRG, 11 March 2009

[9] Health Ministry: Counterfeit NO-SPA pills had been smuggled and are considered a health risk, Globes

[10] "משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa".