Drotaverine

Pharmacodynamics

Drotaverine hydrochloride has a spasmolytic, myotropic, vasodilation, hypotensive action.

Drotaverine decreases active ionized calcium supply binding to smooth muscle cells due to inhibition of phosphodiesterase and intracellular accumulation of cAMP. It has an apparent and prolonged action on smooth muscles of internal organs and blood vessels and it moderately decreases arterial blood pressure, increases cardiac output (minute volume of heart), and has some antiarrhythmic potential.

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.

Side effects

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

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

Counterfeits

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

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.

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

Risks

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

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.

References

References

1. "Инструкция по применению препарата Но-шпа // No-Spa (tablets) Full Prescribing Information". Chinoin Pharmaceutical and Chemical Works.
2. (2006). "Title Textbook of Obstetrics". BI Publications Pvt Ltd.
3. (January 2004). "Drotaverine hydrochloride for augmentation of labor". International Journal of Gynaecology and Obstetrics.
4. "DROTAVERINE: Uses, Side Effects and Medicines {{!}} Apollo Pharmacy".
5. "RUE Belmedpreparaty - pharmaceutical enterprise in the Republic of Belarus - DROTAVERINE HYDROCHLORIDE".
6. "No-Spa, 40 mg, tabletki, 20 szt.".
7. "DROTAVERIN-CHINOIN 40 mg tabletta 24 db - PATIKA24 Gyógyszer".
8. "NO-SPA ÕHUKE POLÜMEERKATTEGA TBL 40MG N24 {{!}} BENU Veebiap".
9. "NO-SPA 40 mg tabletes, 24 gab. - Piegāde visā Latvijā {{!}} Mēness aptieka".
10. "Drotaverine - Vaistai.lt".
11. Drotaverine - Drugs.com [https://www.drugs.com/international/drotaverine.html Drugs.com international listings for drotaverine] Page accessed June 28, 2015
12. "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".
13. [http://www.justice.gov.il/Units/RashamHaptentim/legalinfo/HaclatotRasham/TM%20202248%2023.1.2011.doc NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248], Israeli patent and trade mark office, 11 July 2007
14. [http://www.nrg.co.il/online/29/ART1/864/638.html Health Ministry: Fake drug had been smuggled] ''NRG'', 11 March 2009
15. ניב, שי. (2008-02-11). "חשש כי תרופה מזויפת בשם NO-SPA הוברחה לישראל ועשויה לגרום לסכנה בריאותית". Globes.
16. Bader, H. (11 February 2008). "משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa".
17. (2013). "Drotaverine overdose". Reactions Weekly.
18. [http://chess-news.ru/node/21958 Silence, lack of will, indifference] {{Webarchive. link. (2016-12-18 (Russian, Chess-News))