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Drotaverine Trade names No-Spa, Doverin AHFS /Drugs.com International Drug Names Routes of Oral, intravenous , intramuscular ATC code
Legal status
OTC (tablets), Rx-only (solution for injection) (RU [1]
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[1]
(Z
CAS Number PubChem CID DrugBank ChemSpider UNII KEGG ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.110.916 Formula C 24 H 31 N O 4 Molar mass −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
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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 .[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] [8] [9] [10] [11] [12] 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 [ edit ]
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 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.[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 [ edit ]
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 [ edit ]
In Israel the product is known under the brand name "No-Spa" by the general public[14] health ministry ,[15] [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]
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 [ edit ]
^ Padubidri V, Anand E (2006). Title Textbook of Obstetrics . BI Publications Pvt Ltd. p. 283. ISBN 9788172252236
^ 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 .
^ "DROTAVERINE: Uses, Side Effects and Medicines | Apollo Pharmacy" . www.apollopharmacy.in . Retrieved 2022-05-24 .
^ 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 .
^ "The DrugBank database: Drotaverine" . DrugBank Version 4.1 . The Metabolomics Innovation Centre. Retrieved 9 August 2014 .
^ "No-Spa, 40 mg, tabletki, 20 szt" . doz.pl (in Polish). Retrieved 2023-01-09 .
^ "DROTAVERIN-CHINOIN 40 mg tabletta 24 db - PATIKA24 Gyógyszer" . www.patika24.hu (in Hungarian). Retrieved 2023-01-09 .
^ "NO-SPA ÕHUKE POLÜMEERKATTEGA TBL 40MG N24 | BENU Veebiap" . www.benu.ee (in Ewe). Retrieved 2023-01-09 .
^ "NO-SPA 40 mg tabletes, 24 gab. - Piegāde visā Latvijā | Mēness aptieka" . www.e-menessaptieka.lv (in Latvian). Retrieved 2023-01-09 .
^ "Drotaverine - Vaistai.lt" . vaistai.lt . Retrieved 2023-01-09 .
^ Drotaverine - Drugs.com Drugs.com international listings for drotaverine Page accessed June 28, 2015
^ "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 .
^ a b NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248 , Israeli patent and trade mark office, 11 July 2007
^ a b Health Ministry: Fake drug had been smuggled NRG , 11 March 2009
^ 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).
^ 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.
^ "Drotaverine overdose" . Reactions Weekly . 1481 : 17. 2013. doi :10.1007/s40278-013-7608-3 .
^ Silence, lack of will, indifference Archived 2016-12-18 at the Wayback Machine (Russian, Chess-News)
R e t r i e v e d f r o m " https://en.wikipedia.org/w/index.php?title=Drotaverine&oldid=1232180214 " C a t e g o r i e s : ● D r u g s a c t i n g o n t h e g a s t r o i n t e s t i n a l s y s t e m a n d m e t a b o l i s m ● N o r s a l s o l i n o l e t h e r s ● A n t i s p a s m o d i c s ● P D E 4 i n h i b i t o r s ● S a n o f i H i d d e n c a t e g o r i e s : ● C S 1 R u s s i a n - l a n g u a g e s o u r c e s ( ru ) ● C S 1 P o l i s h - l a n g u a g e s o u r c e s ( pl ) ● C S 1 H u n g a r i a n - l a n g u a g e s o u r c e s ( hu ) ● C S 1 E w e - l a n g u a g e s o u r c e s ( ee ) ● C S 1 L a t v i a n - l a n g u a g e s o u r c e s ( lv ) ● C S 1 H e b r e w - l a n g u a g e s o u r c e s ( he ) ● W e b a r c h i v e t e m p l a t e w a y b a c k l i n k s ● A r t i c l e s w i t h s h o r t d e s c r i p t i o n ● S h o r t d e s c r i p t i o n m a t c h e s W i k i d a t a ● D r u g s w i t h n o n - s t a n d a r d l e g a l s t a t u s ● A r t i c l e s w i t h c h a n g e d C A S N o i d e n t i f i e r ● E C H A I n f o C a r d I D f r o m W i k i d a t a ● D r u g b o x e s w h i c h c o n t a i n c h a n g e s t o v e r i f i e d f i e l d s ● D r u g b o x e s w h i c h c o n t a i n c h a n g e s t o w a t c h e d f i e l d s ● A r t i c l e s n e e d i n g m o r e d e t a i l e d r e f e r e n c e s
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a d d i t i o n a l t e r m s m a y a p p l y . B y u s i n g t h i s s i t e , y o u a g r e e t o t h e T e r m s o f U s e a n d P r i v a c y P o l i c y . W i k i p e d i a ® i s a r e g i s t e r e d t r a d e m a r k o f t h e W i k i m e d i a F o u n d a t i o n , I n c . , a n o n - p r o f i t o r g a n i z a t i o n . ● P r i v a c y p o l i c y ● A b o u t W i k i p e d i a ● D i s c l a i m e r s ● C o n t a c t W i k i p e d i a ● C o d e o f C o n d u c t ● D e v e l o p e r s ● S t a t i s t i c s ● C o o k i e s t a t e m e n t ● M o b i l e v i e w
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