Ivermectin binds avidly to plasma proteins

Abstract

Human pharmacokinetic data on the new anti-parasitic agent, ivermectin, are scanty. For the evaluation of its disposition a specific HPLC assay with sensitive fluorescence detection was developed. Applying equilibrium dialysis, plasma protein binding of ivermectin was measured in five healthy individuals and it averaged 93.2 +/- 4.4% (SD). Such strong binding should be taken into consideration, especially in patients with malnutrition or with diseases in which a decrease in plasma proteins and consequently a higher free fraction of ivermectin could be expected.

The Pharmacokinetics and Interactions of Ivermectin in Humans—A Mini-review

“…Ivermectin binds strongly to plasma proteins in healthy subjects (93.2%) (22). It was also high in onchocerciasis patients (93.1%), with a specific binding for serum albumin.…”

Ivermectin levels in human breast milk

“…kg -~ ivermectin. Ivermectin was analysed by high-pressure liquid chromatography (HPLC) following derivatization and fluorescent detection as previously described (Klotz et al 1990). There are two factors that determine the ivermectin exposure in infants: the amount reaching the infant through milk from the mother, and the infant's clearance capacity for ivermectin.…”

Treatment of Human Disseminated Strongyloidiasis with a Parenteral Veterinary Formulation of Ivermectin

“…For the first time in this situation, we documented ivermectin levels, which were below the average of those reported in normal subjects after oral administration (peak plasma concentration ‫ע[‬ SD], 48.5 ‫ע‬ 35.2 ng/mL) [16]. Ivermectin is highly bound to serum albumin [17]; thus, severe hypoalbuminemia may have contributed to a slower absorption from tissue edema, a larger volume of distribution, and an increased clearance of unbound drug. There was an accumulation of ivermectin and its metabolites after repeated doses and a sustained antiparasitic effect.…”