levamisole

Action and Spectrum

Actions and Spectrum: 

Action: 

Immunomodulatory Activity: levamisole has been shown to stimulate the immune system, specifically the activity of specific white blood cells called neutrophils and lymphocytes. This immunomodulatory effect has led to its use as an adjuvant therapy in some instances of cancer and autoimmune disorders. 

Anticancer Activity (Experimental): levamisole has been investigated for its potential anticancer properties. It enhances immune responses against cancer cells and may directly affect tumor growth. However, its use in cancer treatment is not well-established and remains experimental. 

Spectrum: 

levamisole’s primary therapeutic use has been in the treatment of certain parasitic worm infections. It has been effective against roundworm infections, particularly Ascariasis. However, its usage has declined due to the development of other, more effective anthelmintic medications with fewer side effects. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Nausea 

metallic taste 

Diarrhea 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: levamisole must not be administered to individuals with a documented hypersensitivity or allergic response to the drug. Allergic responses can vary from minor skin eruptions to serious anaphylactic reactions. 

Agranulocytosis: levamisole has been linked to agranulocytosis, a condition where the bone marrow’s production of white blood cells (neutrophils) significantly decreases. Individuals with a history of agranulocytosis or those prone to blood disorders should avoid levamisole. 

Systemic Lupus Erythematosus (SLE): 

levamisole has been associated with triggering or exacerbating symptoms of autoimmune diseases like systemic lupus erythematosus. Individuals with SLE or other autoimmune disorders should avoid levamisole due to the potential for disease flare-ups. 

Pregnancy and Breastfeeding: The safety of levamisole during pregnancy and breastfeeding has not been established, and there may be potential risks to both the mother and the baby. It is generally recommended to avoid using Levamisole during these periods unless the potential benefits outweigh the risks. 

Children: levamisole’s safety and efficacy in pediatric patients have not been well established. Safer alternatives are usually preferred for treating parasitic infections in children. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

<b>Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

levamisole is an anthelmintic medication used for medicinal purposes to treat parasitic & bacterial infections. 

Pharmacodynamics:  

it’s believed to work by affecting the immune system and interfering with the metabolism of cells. It has immunomodulatory properties, meaning it can influence the functioning of the immune system.   

Pharmacokinetics: 

Absorption 

After oral administration, levamisole is absorbed through the gastrointestinal tract and enters the bloodstream. 

Distribution 

levamisole is distributed throughout the body and may accumulate in specific tissues. 

Metabolism 

levamisole undergoes metabolism primarily in the liver. The main metabolic pathways include: 

Oxidation: levamisole can undergo oxidative metabolism, primarily mediated by cytochrome P450 enzymes. This results in the formation of various metabolites, including hydroxylevamisole and aminorex-like compounds. 

Conjugation: Some metabolites, especially hydroxylevamisole, can undergo conjugation with glucuronic acid to form glucuronide conjugates. Conjugation is a process that makes these metabolites more water-soluble, aiding their excretion. 

Excretion and Elimination 

The metabolites of levamisole and a portion of the unchanged drug are excreted primarily through the kidneys in urine. The glucuronide conjugates and other metabolites are more water-soluble, facilitating their elimination from the body. 

Adminstartion

Administration:  

The administration is by oral route. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: levamisole 

Why do we use levamisole?  

Anthelminthic Treatment: levamisole was initially used to treat intestinal worm infections, specifically roundworms and hookworms.  

Immunomodulation in Autoimmune Diseases: levamisole has also been used as an immunomodulatory agent in certain autoimmune diseases, particularly in combination with other treatments. It was historically used to treat conditions like rheumatoid arthritis and lupus. Levamisole is thought to stimulate the immune system, potentially leading to a reduction in autoimmune activity. 

Chemotherapy Adjunct: There have been studies exploring the use of levamisole in conjunction with chemotherapy in certain types of cancer. It was thought to enhance the immune response against cancer cells and improve the effectiveness of chemotherapy.