Active ingredient: Levamisole - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Adjuvants, Immunologic
• Antinematodal Agents
• Antirheumatic Agents

Dosage Forms

• Tablet

Brands / Synonyms

dl-Tetramisol; dl-Tetramisole ; 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

Indications

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.

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.

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.

Absorption

Levamisole is rapidly absorbed (2 hours) from the gastrointestinal tract.

Toxicity

LD₅₀ = 40 mg/kg (Pigs, subcutaneous); LD₅₀ = 180 mg/kg (rat, oral)

Biotrnasformation / Drug Metabolism

Primarily hepatic (extensive) with both active and inactive metabolites.

Contraindications

ERGAMISOL^® (levamisole hydrochloride) is contraindicated in patients with a known hypersensitivity to the drug or its components.

Drug Interactions

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 drugs.