Jump to content

Drotaverine

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by DMacks (talk | contribs) at 03:15, 22 June 2020 (Remove malformatted |molecular_weight= when infobox can autocalculate it, per Wikipedia talk:WikiProject Pharmacology#Molecular weights in drugboxes (via WP:JWB)). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

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 Edit this at Wikidata
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- checkY
  • Key:OMFNSKIUKYOYRG-MOSHPQCFSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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[specify] and Central and Eastern European[specify] 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

  1. ^ a b "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
  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)
  7. ^ a b NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office,11 July 2007
  8. ^ a b 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".
Retrieved from "https://en.wikipedia.org/w/index.php?title=Drotaverine&oldid=963838731"