Comparative Pharmacology
Head-to-head clinical analysis: HETRAZAN versus IVERMECTIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: HETRAZAN versus IVERMECTIN.
HETRAZAN vs IVERMECTIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Diethylcarbamazine (HETRAZAN) sensitizes microfilariae to phagocytosis by immobilizing them and altering their surface, making them more susceptible to destruction by host immune cells. It also has anthelminthic activity against adult worms.
Ivermectin is a macrocyclic lactone that binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate nerve and muscle cells, leading to increased chloride ion influx, hyperpolarization, and paralysis of the parasite. It also interacts with other ligand-gated chloride channels, such as those gated by gamma-aminobutyric acid (GABA). In mammals, these channels are largely confined to the central nervous system, but ivermectin does not readily cross the blood-brain barrier, providing a safety margin.
2 mg/kg orally three times daily after meals for 3 weeks (total dose 120 mg/kg per course). Maximum single dose: 10 mg/kg.
150–200 mcg/kg orally once, with repeat dose in 2 weeks for strongyloidiasis; for scabies, 200 mcg/kg orally once, repeat in 2 weeks if needed.
None Documented
None Documented
Clinical Note
moderateIvermectin + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Ivermectin."
Clinical Note
moderateIvermectin + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Ivermectin."
Clinical Note
moderateIvermectin + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Ivermectin."
Clinical Note
moderateIvermectin + Cyclosporine
Terminal elimination half-life is 8-12 hours in patients with normal renal function; may be prolonged in renal impairment.
Terminal elimination half-life is approximately 18 hours (range 12-24 hours) in healthy adults; prolonged in hepatic impairment.
Renal excretion of unchanged drug accounts for approximately 50-60% of elimination; the remainder is metabolized hepatically with metabolites excreted in urine. Fecal elimination is minimal (<5%).
Primarily fecal (≥90% as unchanged drug and metabolites); renal excretion is minimal (<1% of dose). Biliary excretion contributes to fecal elimination.
Category C
Category A/B
Anthelmintic
Anthelmintic
"The metabolism of Cyclosporine can be decreased when combined with Ivermectin."