Drug information of Levamisole


Drug group:

Levamisole is a cancer (antineoplastic) medication. Levamisole interferes with the growth of cancer cells and slows their growth and spread in the body. Levamisole is used in the treatment of colon cancer. Levamisole may also be used for purposes other than those listed in this medication guide.

Levamisole 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.

 Levamisole was withdrawn from the US and Canadian markets in 2000 and 2003, respectively, due to the risk of serious side effects and the availability of more effective replacement medications.

 Levamisole is also a medication used to treat parasitic worm infections.  Specifically it is used for ascariasis and hookworm infections. It is taken by mouth.

Mechanism of effect

The mechanism of action of  levamisole as an antiparasitic agent appears to be tied to its agonistic 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.  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 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.


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

Volume of distribution: Not Available

Protein binding: 20-25%

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

Route of elimination: Not Available

Half-life : 4.4-5.6 hours (biphasic)

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

Affected organisms: Humans and other mammals


Available Dosage Forms: Tablet

The dose of levamisole will be different for different patients. Follow your doctor's orders or the directions on the label.

  • Usual Adult Dose for Malignant Disease:

50 mg orally every 8 hours for 3 days (starting 7-30 days post-surgery). May be given as maintenance therapy for 3 days at 2 week intervals for 1 year.


  • The presence of other medical problems may affect the use of levamisole. Make sure you tell your doctor if you have any other medical problems, especially:
  • Infection—Levamisole may decrease your body's ability to fight infection
  • Do not use levamisole without first talking to your doctor if you have: liver disease; a seizure disorder; a bleeding or blood clotting disorder; or poor bone marrow function.

Points of recommendation

  • Take on an empty stomach.
  • If you vomit shortly after taking a dose of levamisole, check with your doctor. You will be told whether to take the dose again or to wait until the next scheduled dose.

Pregnancy level


Ask a Pharmacist

User's questions
    No comments yet.