Chemistry:Drotaverine
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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 |
| Elimination half-life | 7–16 hours |
| Excretion | >50% in urine and ~30% in bile[1] |
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| Chemical and physical data | |
| Formula | C24H31NO4 |
| Molar mass | 397.515 g·mol−1 |
| 3D model (JSmol) | |
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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] 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 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
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 woman) 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
- ↑ 1.0 1.1 "Инструкция по применению препарата Но-шпа // No-Spa (tablets) Full Prescribing Information" (in ru). Chinoin Pharmaceutical and Chemical Works. pp. 3–8. http://grls.rosminzdrav.ru/InstrImgMZ.aspx?isNew=1&idReg=6198&page=4&isOld=1&t=.
- ↑ Title Textbook of Obstetrics. BI Publications Pvt Ltd. 2006. pp. 283. ISBN 9788172252236.
- ↑ "Drotaverine hydrochloride for augmentation of labor". International Journal of Gynaecology and Obstetrics 84 (1): 17–22. January 2004. doi:10.1016/s0020-7292(03)00276-5. PMID 14698825.
- ↑ "DROTAVERINE: Uses, Side Effects and Medicines | Apollo Pharmacy". https://www.apollopharmacy.in/salt/DROTAVERINE.
- ↑ 5.0 5.1 5.2 5.3 5.4 5.5 "RUE Belmedpreparaty - pharmaceutical enterprise in the Republic of Belarus - DROTAVERINE HYDROCHLORIDE" (in en). https://www.belmedpreparaty.com/product/anot.php?anat_id=395&lang_id=2.
- ↑ "The DrugBank database: Drotaverine". The Metabolomics Innovation Centre. http://www.drugbank.ca/drugs/DB06751.
- ↑ "No-Spa, 40 mg, tabletki, 20 szt." (in pl). https://www.doz.pl/apteka/p6349-No-Spa_40_mg_tabletki_20_szt..
- ↑ "DROTAVERIN-CHINOIN 40 mg tabletta 24 db - PATIKA24 Gyógyszer" (in hu). https://www.patika24.hu/drotaverin-chinoin-40-mg-tabletta-24-db.html.
- ↑ "NO-SPA ÕHUKE POLÜMEERKATTEGA TBL 40MG N24 | BENU Veebiap" (in ee). https://www.benu.ee:443/products-by-categories/hygiene-ee/no-spa-kaetud-tbl-40mg-n24.
- ↑ "NO-SPA 40 mg tabletes, 24 gab. - Piegāde visā Latvijā | Mēness aptieka" (in lv). https://www.e-menessaptieka.lv/no-spa-40-mg-tabletes-24-gab-1142207.
- ↑ "Drotaverine - Vaistai.lt". https://vaistai.lt/grupe/drotaverine.html.
- ↑ 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" (in ru). https://www.rlsnet.ru/drugs/no-spa-2216.
- ↑ 14.0 14.1 NO-SPA (also pronounced as No-SHPA) trade mark registration decision 202248, Israeli patent and trade mark office, 11 July 2007
- ↑ 15.0 15.1 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" (in he). Globes. https://www.globes.co.il/news/article.aspx?did=1000308494.
- ↑ Bader, H (11 February 2008). "משרד הבריאות מזהיר משימוש בתרופה לא מאושרת בשם: No-Spa" (in he). https://www.inn.co.il/flashes/209104.
- ↑ Drotaverine overdose (case report) Reactions Weekly, Volume 1481 (1), page 17.
- ↑ Silence, lack of will, indifference (Russian, Chess-News)
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