Levamisole

• 产品号: DB00848
• CAS号: 14769-73-4
• 分子式: C11H12N2S
• 分子量: 204.29138

产品别名

• 标题: Levamisole
• IUPAC标准名: (6S)-6-phenyl-2H,3H,5H,6H-imidazo[2,1-b][1,3]thiazole
• IUPAC传统名: levamisole
• 商标名: Wormicid; Lepuron; LEVOMYSOL; Tetramisol; Ergamisol; Levamisol; Nilverm base; Tetramisole; Tramisol; Ketrax; Vermisol 150
• 别名: Phenyl imidothiazole; dl-Tetramisol; Levamisol [INN-Spanish]; L-Tetramisole; Levamisolum [INN-Latin]; Levamisole hydrochloride; dl-Tetramisole

产品登记号

• CAS号: 14769-73-4
• PubChem SID: 46509052
• PubChem CID: 26879

产品性质

• 疏水性(logP): 2.3
• 溶解度: 210 mg/mL

产品详细信息

详细说明 (English)

• Drug Groups: approved
• Description: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)
• Indication: For adjuvant treatment in combination with fluorouracil after surgical resection in patients with Dukes' stage C colon cancer. Also used to treat malignant melanoma and head/neck cancer.; Levamisole was originally used as an antihelminthic to treat worm infestations in both humans and animals.
• Pharmacology: Levamisole is a synthetic imidazothiazole derivative that has been widely used in treatment of worm infestations in both humans and animals. As an anthelmintic, it probably works by targeting the nematode nicotinergic acetylcholine receptor. As an immunomodulator, it appears that Levamisole is an immunostimulant which has been shown to increase NK cells and activated T-cells in patients receiving this adjuvantly along with 5FU for Stage III colon cancer.
• Toxicity: LD₅₀ = 40 mg/kg (Pigs, subcutaneous); LD₅₀ = 180 mg/kg (rat, oral)
• Affected Organisms: Humans and other mammals
• Biotransformation: Primarily hepatic (extensive) with both active and inactive metabolites.
• Absorption: Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.
• Half Life: 4.4-5.6 hours (biphasic)
• Protein Binding: 20-25%
• References: Grishchenko SV, Lavrukhina LA, Ketiladze ES, Krylov VF, Ershov FI: [Results of combined therapy using levamisole for patients with influenza complicated by pneumonia] Vopr Virusol. 1984 Mar-Apr;29(2):175-9. [Pubmed] ; Levamisole for corticosteroid-dependent nephrotic syndrome in childhood. British Association for Paediatric Nephrology. Lancet. 1991 Jun 29;337(8757):1555-7. [Pubmed] ; Van Belle H: Alkaline phosphatase. I. Kinetics and inhibition by levamisole of purified isoenzymes from humans. Clin Chem. 1976 Jul;22(7):972-6. [Pubmed]
• External Links: Wikipedia; RxList; Drugs.com

参考文献

• Grishchenko SV, Lavrukhina LA, Ketiladze ES, Krylov VF, Ershov FI: [Results of combined therapy using levamisole for patients with influenza complicated by pneumonia] Vopr Virusol. 1984 Mar-Apr;29(2):175-9. Pubmed
• Levamisole for corticosteroid-dependent nephrotic syndrome in childhood. British Association for Paediatric Nephrology. Lancet. 1991 Jun 29;337(8757):1555-7. Pubmed
• Van Belle H: Alkaline phosphatase. I. Kinetics and inhibition by levamisole of purified isoenzymes from humans. Clin Chem. 1976 Jul;22(7):972-6. Pubmed