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| Clinical data | |
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| Trade names | No-Spa, Doverin |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral,intravenous,intramuscular |
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| Pharmacokinetic data | |
| Bioavailability | Highly variable (~65%), peak at 45–60 min |
| Protein binding | 95–98% |
| Metabolism | Hepatic |
| Eliminationhalf-life | 7–16 hours |
| Excretion | >50% in urine and ~30% in bile[1] |
| Identifiers | |
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| CAS Number | |
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| DrugBank |
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| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.110.916 |
| Chemical and physical data | |
| Formula | C24H31NO4 |
| Molar mass | 397.515 g·mol−1 |
| 3D model (JSmol) | |
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Drotaverine (INN, also known asdrotaverin) is anantispasmodic drug, used to enhancecervical dilation duringchildbirth and to relievesmooth musclespasms in thegastrointestinal tract,urinary system, andgall bladder.[2][3][4][5]
It is structurally related topapaverine, and is a selectiveinhibitor of phosphodiesterase-4, and has noanticholinergic effects.[6]
It is available inAsia,[specify]Central and Eastern Europe (Poland,[7] Hungary,[8] Estonia,[9] Latvia,[10] Lithuania[11]) under several brand names.[12] A popular brand isNo-Spa, owned bySanofi). It is distributed by Sanofi asНо-Шпа (No-shpa) in Russia.[13]
Drotaverine hydrochloride has aspasmolytic, myotropic,vasodilation,hypotensive action.[5]
Drotaverine decreases active ionized calcium supply binding to smooth muscle cells due to inhibition ofphosphodiesterase and intracellular accumulation ofcAMP. It has an apparent and prolonged action on smooth muscles of internal organs and blood vessels and it moderately decreasesarterial blood pressure, increasescardiac output (minute volume of heart), and has someantiarrhythmic potential.[5]
Drotaverine decreasesvascular tone ofcerebral blood vessels and increases blood-filling. Practically, Drotaverine does not influence theautonomic nervous system and does not penetrate into thecentral nervous system.[5]
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 causeatrioventricular (AV) block,cardiac arrest, paralysis of respiratory system.[5]
InIsrael 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 thehealth 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 theBen 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 playerIvan 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]