The Levamisole Story

Effects of the Immunostimulant, Levamisole, on Opiate Withdrawal and Levels of Endogenous Opiate Alkaloids and Monoamine Neurotransmitters in Rat Brain

“…Levamisole was originally developed as a treatment for bacterial, helminthic, and viral diseases (Janssen 1976;Symens and Rosenthal 1977;Renoux 1980;Moertel et al 1990), but it is increasingly used as an immunostimulant. The results presented here demonstrate that systemic administration of levamisole reduced the symptoms of naltrexone-induced morphine withdrawal, produced a significant increase in the levels of endogenous morphine and codeine in brain and peripheral organs, and significantly altered the metabolism of the monoamine neurotransmitters in specific brain regions.…”

Immune-Mediated Agranulocytosis Caused by the Cocaine Adulterant Levamisole: A Case for Reactive Metabolite(s) Involvement

“…Apart from the formation of 1, in vitro incubations of [ 14 C]levamisole in human hepatocytes indicate the presence of several additional metabolites 3 to 8 (Fig. 1) (Janssen, 1976;Symoens et al, 1979;Roberts, 1994). With the exception of 3, which can arise from a cytochrome P450 (P450)-mediated imidazolidine ring dehydrogenation, the rate-limiting step in the formation of 4 to 8 appears to be mediated by a ring scission of the thiazolidine motif.…”

“…Levamisole was introduced as a broad spectrum veterinary anthelmintic in 1965 and anthelmintic in humans in 1966. Levamisole causes paralysis and passive elimination of worms, by inhibition of fumerate reductase in nematodes (Janssen, 1976 where parasitic infections are common, levamisole continues to be prescribed in humans (Albonico et al, 2003). Levamisole is also used to treat childhood nephrotic syndrome (excessive levels of protein in the urine) outside the United States (Hodson, 2003).…”

“…Levamisole is also used to treat childhood nephrotic syndrome (excessive levels of protein in the urine) outside the United States (Hodson, 2003). Serendipitous results on de novo pharmacology have been reported with levamisole, including apparent beneficial effects on host defense mechanism and enhanced immunologic protection against bacterial and viral pathogens (Janssen, 1976;Amery and Bruynseels, 1992). In the 1990s, several reviews about levamisole's efficacy as a human immune system modulator appeared in the literature, which focused on its potential beneficial effects in cancer treatment.…”

Effect of levamisole and azathioprine on the human mixed lymphocyte reaction (MLR).

“…Levamisole, the antihelminthic drug (Janssen, 1976), has been shown to enhance in vitro human lymphocyte responses to allogeneic cells (MLR) and mitogens (Sampson & Lui, 1976). It has also been found to reverse the inhibitory effect of azathioprine on rosette formation (Verhaegen et al, 1975(Verhaegen et al, , 1977 and antigen stimulated lymphocytes (Ivanyi, 1979) but its effect on the MLR has not been studied.…”