Ivermectin
Ivermectin. Macrocyclic lactone antiparasitic — opens parasite glutamate-gated chloride channels → flaccid paralysis. Used for strongyloidiasis… Oral half-life 35 h.
Macrocyclic lactone antiparasitic — opens parasite glutamate-gated chloride channels → flaccid paralysis. Used for strongyloidiasis, onchocerciasis, scabies, lice. P-glycoprotein efflux at the BBB protects mammals from CNS toxicity. CYP3A4 substrate.
PK: the half-life of 35.0 h is verbatim and stands (PMID:8839664, 25 onchocerciasis patients, single oral 150 micrograms/kg), though the paper does not state whether dosing was fasted or fed, which matters because food raises ivermectin exposure substantially. F 0.5 is dropped as UNSOURCEABLE rather than merely unsourced: there is no human intravenous ivermectin formulation, so an absolute bioavailability cannot exist. V 200 L is dropped as a value shared with unrelated drugs; the real human volumes are apparent and two-compartment, 89 L central and 234 L peripheral (PMID:30566757). ka 0.5 /h dropped, the source model using transit absorption with no single rate constant.
Pharmacokinetics
- Oral — t½ 35 h
Sources: PMID:8839664, PMID:30566757