Semisynthetic anthelminthic agent. It binds selectively and with strong affinity to glutamate-gated chloride ion channels which occur in invertebrate nerve and muscle cells. This leads to increased permeability of cell membranes to chloride ions then hyperpolarization of the nerve or muscle cell, and death of the parasite.
Does not readily cross the blood-brain barrier
Protein Binding: ~ 93% primarily to albumin
Metabolism: Hepatic via CYP 3A4 (major); CYP2D6 (minor), and CYP2E1 (minor)
Avoid use or use with caution in pediatric patients < 2 years or < 15 kg due to increased risk for CNS effects (encephalopathy); monitor patients closely
Repeat treatment may be required in immunocompromised patients
Ivermectin has no activity against adult O. volvulus parasites