Arbidol
From Wikipedia, the free encyclopedia
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| Systematic (IUPAC) name | |
|---|---|
| 1-methyl-2-((phenylthio)methyl)-3-carbethoxy-4-((dimethylamino)methyl)-5-hydroxy-6-bromindole | |
| Identifiers | |
| CAS number | 131707-23-8 |
| ATC code | L03AX |
| PubChem | 9958103 |
| DrugBank | N/A |
| ChemSpider | 8133712 |
| Chemical data | |
| Formula | C22H28BrClN2O4S |
| Mol. mass | 531.89 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | N/A |
| Metabolism | N/A |
| Half life | 17–21 hours |
| Excretion | renal |
| Therapeutic considerations | |
| Pregnancy cat. |
N/A |
| Legal status |
N/A |
| Routes | oral |
Arbidol (Russian: Арбидол) (Chinese: 阿比朵尔) is an antiviral treatment for influenza infection used in Russia[1] and China. The drug is manufactured by Moscow-based Masterlek (Russian: Мастерлек). Its acceptance amongst the pharamecutical industry varies, although some Russian studies have shown it to be as effective as other available treatments.
Chemically, arbidol features an indole core, functionalized at all positions but one with different substituents. The drug inhibits viral entry into target cells, and also stimulates the immune response.
Arbidol is manufactured and made available as both tablets and capsules.
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[edit] Status
Testing of arbidol's efficacy has mainly occurred in China and Russia,[2][3] and it is well known in these two countries.[4]
The Russian tests showed the drug to be effective as other available treatments,[2] but it has yet to gain universal acceptance amongst the Western pharmaceutical industry. Some regions have welcomed arbidol, but it is not cost-effective option compared with other drugs,[citation needed] while others still maintain a level of suspicion over the validity of its safety and efficacy testing.[citation needed] Outbreaks of highly pathogenic avian influenza and the encroaching pandemic threat of H5N1 has seen the drug added to the arsenal of influenza treatments in several countries.[citation needed]
[edit] Mode of action
[edit] Biochemistry
Arbidol inhibits membrane fusion.[1]
Arbidol prevents contact between the virus and target host cells. Fusion between the viral capsid and the cell membrane of the target cell is inhibited. This prevents viral entry to the target cell, and therefore protects it from infection.[5]
Some evidence suggests that the drugs actions are more effective at preventing infections from RNA viruses than infections from DNA viruses.[6]
As well as specific antiviral action against both influenza A and influenza B viruses, Arbiodol exhibits modulatory effects on the immune system. The drug stimulates a humoral immune response, induces interferon-production, and stimulates the phagocytic function of macrophages.[7]
[edit] Clinical application
Arbidol is used primarily as an antiviral treatments for influenza. It is compared most with oseltamivir (Tamiflu, Roche).[citation needed].
The drug has also been investigated as a candidate drug for treatment of hepatitis C.[8]
[edit] Side effects
Side effects in children include sensitization to the drug. No known overdose cases have been reported and allergic reactions are limited to people with hypersensitivity. The LD50 is more than 4 g/kg.[9]
[edit] References
- ^ a b Leneva IA, Russell RJ, Boriskin YS, Hay AJ (February 2009). "Characteristics of arbidol-resistant mutants of influenza virus: implications for the mechanism of anti-influenza action of arbidol". Antiviral Res. 81 (2): 132–40. doi:. PMID 19028526. http://linkinghub.elsevier.com/retrieve/pii/S0166-3542(08)00431-2.
- ^ a b Leneva IA, Fediakina IT, Gus'kova TA, Glushkov RG (2005). "[Sensitivity of various influenza virus strains to arbidol. Influence of arbidol combination with different antiviral drugs on reproduction of influenza virus A]" (in English (Russian translation)). Терапевтический Архив (Therapeutic Archive) (Moscow, Russia: ИЗДАТЕЛЬСТВО "МЕДИЦИНА") 77 (8): 84–88. PMID 16206613. http://arbidol.org/arbidol-2005-works-as-well.html. Retrieved 2008-02-22.
- ^ Wang MZ, Cai BQ, Li LY, et al. (2004). "[Efficacy and safety of arbidol in treatment of naturally acquired influenza]" (in Chinese). Zhongguo Yi Xue Ke Xue Yuan Xaue Bao 26 (3): 289–93. PMID 15266832.
- ^ Boriskin YS, Leneva IA, Pécheur EI, Polyak SJ (2008). "Arbidol: a broad-spectrum antiviral compound that blocks viral fusion". Curr. Med. Chem. 15 (10): 997–1005. doi:. PMID 18393857. http://www.bentham-direct.org/pages/content.php?CMC/2008/00000015/00000010/0006C.SGM.
- ^ Boriskin YS, Pécheur EI, Polyak SJ (2006). "Arbidol: a broad-spectrum antiviral that inhibits acute and chronic HCV infection". Virol. J. 3: 56. doi:. PMID 16854226. http://www.virologyj.com/content/3//56.
- ^ Shi L, Xiong H, He J, et al. (2007). "Antiviral activity of arbidol against influenza A virus, respiratory syncytial virus, rhinovirus, coxsackie virus and adenovirus in vitro and in vivo". Arch. Virol. 152 (8): 1447–55. doi:. PMID 17497238.
- ^ Glushkov RG, Gus'kova TA, Krylova LIu, Nikolaeva IS (1999). "[Mechanisms of arbidole's immunomodulating action]" (in Russian). Vestn. Akad. Med. Nauk SSSR (3): 36–40. PMID 10222830.
- ^ Pécheur EI, Lavillette D, Alcaras F, et al. (2007). "Biochemical mechanism of hepatitis C virus inhibition by the broad-spectrum antiviral arbidol". Biochemistry 46 (20): 6050–9. doi:. PMID 17455911.
- ^ [1]
[edit] External links
- "Мастерлек" Pharmaceuticals, Moscow, Russia. Patent number № 2033157, Registry number № 003610/01.
- (Russian) Arbidol
- English published clinical studies and translations for Arbidol 1973–2009
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