Anthelmintic
A semisynthetic anthelminthic agent which 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.
藥動學
Absorption
Well absorbed in the fasting state; may be increased with a high-fat meal Distribution
1. Vd 3.1-3.5 L/kg in healthy volunteers; mean Vd 9.9 L/kg (range: 6.9 to 15.3 L/kg) in patients with onchocerciasis
2. High concentration in the liver and adipose tissue; does not readily cross the blood-brain barrier
3. Protein binding: ~93% primarily to albumin Metabolism
Hepatic via CYP3A4 (major), CYP2D6 (minor), and CYP2E1 (minor) Excretion
Feces; urine (<1%) Pharmacodynamics
1. Half-life elimination: 18 hours
2. Time to peak, serum: ~4 hours
禁忌症
Hypersensitivity to ivermectin or any component of the formulation
懷孕分類
The decision to use ivermectin during pregnancy should consider the specific indication (eg, onchocerciasis or Strongyloides infection) and the risk of disease progression in the absence of treatment. Although use in pregnancy is likely low risk, other agents are currently recommended for the treatment of pediculosis pubis or scabies in pregnant women.
哺乳分類
The decision to use ivermectin in a patient who is breastfeeding should consider the specific indication (eg, onchocerciasis or Strongyloides infection) and the risk of disease progression in the absence of treatment.
Onchocerciasis: 150 mcg/kg as a single dose; retreatment may be required every 3-12 months until asymptomatic Strongyloidiasis, intestinal: 200 mcg/kg/day for 1-2 days