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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), Rx-only (solution for injection) (RU)
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
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	397.515 g·mol
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 and to relieve smooth muscle spasms in the gastrointestinal tract, urinary system, and gall bladder.

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

It is available in Asia, Central and Eastern Europe (Poland, Hungary, Estonia, Latvia, Lithuania) under several brand names. A popular brand is No-Spa, owned by Sanofi). It is distributed by Sanofi as Но-Шпа (No-shpa) in Russia.

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

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. p. 283. 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. "DROTAVERINE: Uses, Side Effects and Medicines | Apollo Pharmacy". www.apollopharmacy.in. Retrieved 2022-05-24.
5. ^ "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. ^ NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office, 11 July 2007
15. ^ 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". Reactions Weekly. 1481: 17. 2013. doi:10.1007/s40278-013-7608-3.
19. Silence, lack of will, indifference Archived 2016-12-18 at the Wayback Machine (Russian, Chess-News)

• Drugs acting on the gastrointestinal system and metabolism
• Norsalsolinol ethers
• Antispasmodics
• PDE4 inhibitors
• Sanofi