Drotaverine

Source: Wikipedia, the free encyclopedia.
Not to be confused with doravirine.
Drotaverine
intramuscular
ATC code
Legal status
Legal status
  • OTC (tablets), Rx-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
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 (

spasms in the gastrointestinal tract, urinary system, and gall bladder.[2][3][4][5]

It is structurally related to papaverine, and is a selective inhibitor of phosphodiesterase-4, and has no anticholinergic effects.[6]

It is available in Asia,[specify] Central and Eastern Europe (Poland,[7] Hungary,[8] Estonia,[9] Latvia,[10] Lithuania[11]) under several brand names.[12] A popular brand is No-Spa, distributed by the Hungarian plant Chinoin (owned by Sanofi). It is distributed by Sanofi as Но-Шпа (No-shpa) in Russia.[13]

Pharmacodynamics

Drotaverine hydrochloride has a

spasmolytic, myotropic, vasodilation, hypotensive action.[5]

Drotaverine decreases active ionized calcium supply binding to smooth muscle cells due to inhibition of

arterial blood pressure, increases cardiac output (minute volume of heart), and has some antiarrhythmic potential.[5]

Drotaverine decreases

vascular tone of cerebral blood vessels and increases blood-filling. Practically, Drotaverine does not influence the autonomic nervous system and does not penetrate into the central nervous system.[5]

Side effects

Possible side effects include: heating sensation, dizziness, headache (rarely), insomnia. May be observed: arrhythmia (rarely), hypotension, tachycardia, sweating, nausea.[5]

Overdose of Drotaverine potentially can cause atrioventricular (AV) block, cardiac arrest, paralysis of respiratory system.[5]

Counterfeits

In Israel the product is known under the brand name "No-Spa" by the general public[14] which did not receive a permit to be distributed by the health ministry,[15] however due to high demand local medical counterfeiters have managed to smuggle No-Spa tablets over the years.[15]

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.[16][17]

In 2011, the Israeli patent and trademark office declined the use of No-SPA.[14]

Risks

An article from 2013 described the effects from overdose (in a 19-year-old female) as including vomiting, seizures and fatal cardiac toxicity.[18]

In 2016, the young Russian chess player Ivan Bukavshin died of a massive overdose (or poisoning) of the drug, which was initially thought to be a stroke; the dose detected in his blood was 17 mg/kg.[19]

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. ISBN 9788172252236
    .
  3. S2CID 43824027
    .
  4. ^ "DROTAVERINE: Uses, Side Effects and Medicines | Apollo Pharmacy". www.apollopharmacy.in. Retrieved 2022-05-24.
  5. ^ a b c d e f "RUE Belmedpreparaty - pharmaceutical enterprise in the Republic of Belarus - DROTAVERINE HYDROCHLORIDE". RUE Belmedpreparaty - pharmaceutical enterprise in the Republic of Belarus. Archived from the original on 2022-08-17. Retrieved 2022-05-24.
  6. ^ "The DrugBank database: Drotaverine". DrugBank Version 4.1. The Metabolomics Innovation Centre. Retrieved 9 August 2014.
  7. ^ "No-Spa, 40 mg, tabletki, 20 szt". doz.pl (in Polish). Retrieved 2023-01-09.
  8. ^ "DROTAVERIN-CHINOIN 40 mg tabletta 24 db - PATIKA24 Gyógyszer". www.patika24.hu (in Hungarian). Retrieved 2023-01-09.
  9. ^ "NO-SPA ÕHUKE POLÜMEERKATTEGA TBL 40MG N24 | BENU Veebiap". www.benu.ee (in Ewe). Retrieved 2023-01-09.
  10. ^ "NO-SPA 40 mg tabletes, 24 gab. - Piegāde visā Latvijā | Mēness aptieka". www.e-menessaptieka.lv (in Latvian). Retrieved 2023-01-09.
  11. ^ "Drotaverine - Vaistai.lt". vaistai.lt. Retrieved 2023-01-09.
  12. ^ Drotaverine - Drugs.com Drugs.com international listings for drotaverine Page accessed June 28, 2015
  13. ^ "Но-шпа — инструкция по применению, дозы, побочные действия, отзывы о препарате: таблетки, покрытые пленочной оболочкой,таблетки,раствор для внутривенного и внутримышечного введения, 20 мг/мл, 40 мг, 40 мг". РЛС® (in Russian). Retrieved 2023-10-26.
  14. ^ a b NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office, 11 July 2007
  15. ^ a b Health Ministry: Fake drug had been smuggled NRG, 11 March 2009
  16. ^ ניב, שי (2008-02-11). "חשש כי תרופה מזויפת בשם NO-SPA הוברחה לישראל ועשויה לגרום לסכנה בריאותית" [It is feared that a fake drug called NO-SPA has been smuggled into Israel and may cause a health hazard]. Globes (in Hebrew).
  17. ^ Bader, H (11 February 2008). "משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa" [The Ministry of Health warns against the use of an unapproved medicine called: No-Spa]. Israel National News (in Hebrew). Archived from the original on 10 March 2022.
  18. ^ Drotaverine overdose (case report) Reactions Weekly, Volume 1481 (1), page 17.
  19. ^ Silence, lack of will, indifference Archived 2016-12-18 at the Wayback Machine (Russian, Chess-News)
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