Tissue distribution and elimination of [3H]levamisole in the rat after oral and intramuscular administration

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Abstract
1. Total radioactivity and drug concentrations were determined in plasma, organs and excreta of male rats given a single oral or intramuscular dose (7.5 mg/kg) of [3H]levamisole. 2. The anthelmintic drug was distributed mostly within the digestive contents after oral administration and in kidneys and liver after intramuscular injection. 3. The parent drug accounted only for 32 to 45% of total radioactivity in plasma and it appeared metabolized in both urine and bile. 4. The urine (0-72h) contained 68-78% of the radioactive dose, as parent drug and other tritiated materials. The 4-hydroxylation of levamisole did not represent a major metabolic pathway of the drug in the rat.