Brands, Medical Use, Clinical Data
- Adjuvants, Immunologic
- Antinematodal Agents
- Antirheumatic Agents
Brands / Synonyms
; Ergamisol; Ketrax; L-Tetramisole; Lepuron; Levamisol; Levamisol [INN-Spanish]; Levamisole Tetramisole; Levamisolum [INN-Latin]; LEVOMYSOL; Nilverm base; Phenyl imidothiazole; Tetramisol; Tetramisole; Tramisol; Vermisol 150; Wormicid
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 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.
Mechanism of Action
The mechanism of action of levamisole as an antiparasitic agent appears to be tied to its agnositic activity towards the L-subtype nicotinic acetylcholine receptors in nematode muscles. This agonistic action reduces the capacity of the males to control their reproductive muscles and limits their ability to copulate. The mechanism of action of Levamisole as an anticancer drug in combination with fluorouracil is unknown. The effects of levamisole on the immune system are complex. The drug appears to restore depressed immune function rather than to stimulate response to above-normal levels. Levamisole can stimulate formation of antibodies to various antigens, enhance T-cell responses by stimulating T-cell activation and proliferation, potentiate monocyte and macrophage functions including phagocytosis and chemotaxis, and increase neutrophil mobility, adherence, and chemotaxis.
Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.
LD50 = 40 mg/kg (Pigs, subcutaneous); LD50 = 180 mg/kg (rat, oral)
Biotrnasformation / Drug Metabolism
Primarily hepatic (extensive) with both active and inactive metabolites.
ERGAMISOL® (levamisole hydrochloride) is contraindicated in patients with a known hypersensitivity
to the drug or its components.
ERGAMISOL® (levamisole hydrochloride) has been reported to produce "ANTABUSE"-like side effects
when given concomitantly with alcohol. Concomitant administration of phenytoin and ERGAMISOL® plus
fluorouracil has lead to increased plasma levels of phenytoin. The physician is advised to monitor plasma levels of
phenytoin and to decrease the dose if necessary.
Because of reports of prolongation of the prothrombin time beyond the therapeutic range in patients taking
concurrent levamisole and warfarin sodium, it is suggested that the prothrombin time be monitored carefully, and the
dose of warfarin sodium or other coumarin-like drugs should be adjusted accordingly, in patients taking both