Introduction
Levamisole is an anthelmintic and immunomodulatory agent used primarily for the treatment of certain parasitic worm infections. It has also been studied and used as an adjunctive therapy in some immune-mediated diseases and cancers because of its immunomodulatory properties.
Although effective against helminth infections, levamisole is associated with serious adverse effects, including agranulocytosis, which has limited its clinical use in many countries. It has also been identified as an adulterant in illicit cocaine, contributing to significant toxic effects.
Uses
Levamisole is levamisole is a nicotinic receptor agonist used to treat helminth infections and some skin infections.
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.
Associated Conditions
Pharmacodynamics
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.
Protein Binding
20-25%
Half Life
4.4-5.6 hours (biphasic)
Toxicity
LD50 = 40 mg/kg (Pigs, subcutaneous); LD50 = 180 mg/kg (rat, oral)
Food Interactions
- Take on an empty stomach.
Dosage
- Age 1-4 year: 1 Tablets or 5 ml Syrup
- Age 5-15 year: 2 Tablets or 10 ml Syrup
- Age 16 year and over: 3 Tablets or 15 ml Syrup