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Ivermectin binds avidly to plasma proteins
U Klotz1, J E Ogbuokiri, P O Okonkwo
1Dr. Margarete-Fischer-Bosch Institut für Klinische Pharmakologie, Stuttgart, FRG.
European Journal of Clinical Pharmacology
|January 1, 1990
Summary
Human pharmacokinetic data for the anti-parasitic drug ivermectin is limited. This study found ivermectin strongly binds to plasma proteins, which is crucial for understanding its effects in certain patient groups.
Area of Science:
- Pharmacology
- Clinical Chemistry
Background:
- Human pharmacokinetic data for ivermectin, a novel anti-parasitic agent, is scarce.
- Understanding drug disposition is essential for effective therapeutic use.
Purpose of the Study:
- To evaluate the disposition of ivermectin in humans.
- To develop a sensitive analytical method for ivermectin quantification.
- To determine the plasma protein binding of ivermectin.
Main Methods:
- Development of a specific High-Performance Liquid Chromatography (HPLC) assay with fluorescence detection.
- Measurement of plasma protein binding using equilibrium dialysis in healthy individuals.
Main Results:
- A sensitive HPLC assay for ivermectin was successfully developed.
- Ivermectin exhibited strong plasma protein binding, averaging 93.2 +/- 4.4% (SD).
Conclusions:
- The high plasma protein binding of ivermectin is a key pharmacokinetic characteristic.
- This strong binding necessitates consideration in patients with conditions affecting plasma protein levels, such as malnutrition or liver disease, as it may alter the free fraction of the drug.