Drotaverine

Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, used to enhance cervical dilation during childbirth.[2]: 283 [3]

Not to be confused with doravirine.
Drotaverine
Clinical data
Trade namesNo-Spa, Doverin
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral, intravenous, intramuscular
ATC code
Legal status
Legal status
  • OTC (tablets), ℞-only (solution for injection) (RU)[1]
Pharmacokinetic data
BioavailabilityHighly variable (~65%), peak at 45–60 min
Protein binding95–98%
MetabolismHepatic
Elimination half-life7–16 hours
Excretion>50% in urine and ~30% in bile[1]
Identifiers
  • (Z)-1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.110.916
Chemical and physical data
FormulaC24H31NO4
Molar mass397.515 g·mol−1
3D model (JSmol)
  • O(c1ccc(cc1OCC)\C=C3\c2c(cc(OCC)c(OCC)c2)CCN3)CC
  • 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- Y
  • Key:OMFNSKIUKYOYRG-MOSHPQCFSA-N Y
 NY (what is this?)  (verify)

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

It is available in Asian and Central and Eastern European countries under several brand names.[5] Most known brand is No-Spa by Hungarian plant Chinoin (owned by Sanofi).

An article from 2013 described the effects from overdose (in a 19-year-old woman) as including vomiting, seizures and fatal cardiac toxicity.[6]

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.[7] 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[8] which did not receive a permit to be distributed by the health ministry,[9] however due to high demand local medical counterfeiters have managed to smuggle No-Spa tablets over the years.[9]

In 2008 the Israeli health organization warned consumers against counterfeit No-SPA pills after a smuggler had been arrested at the Ben Gurion Airport with several thousand pills.[10][11]

In 2011 Israeli patent and trade mark office declined the use of the No-SPA.[8]

References
  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, Anand E (2006). Title Textbook of Obstetrics. BI Publications Pvt Ltd. ISBN 9788172252236.
  3. Singh KC, Jain P, Goel N, Saxena A (January 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. S2CID 43824027.
  4. "The DrugBank database: Drotaverine". DrugBank Version 4.1. The Metabolomics Innovation Centre. Retrieved 9 August 2014.
  5. Drotaverine - Drugs.com Drugs.com international listings for drotaverine Page accessed June 28, 2015
  6. Drotaverine overdose (case report) Reactions Weekly, Volume 1481 (1), page 17.
  7. Silence, lack of will, indifference (Russian, Chess-News)
  8. NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office,11 July 2007
  9. Health Ministry: Fake drug had been smuggled NRG, 11 March 2009
  10. Health Ministry: Counterfeit NO-SPA pills had been smuggled and are considered a health risk, Globes
  11. "משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa".
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