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Updated: May 26, 2026
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Published on: March 29, 2024
Decrease in brain distribution of fluvoxamine in experimental hyperlipidemic rats.
Keizo Fukushima1, Shinji Kobuchi, Masakazu Shibata
1Department of Clinical Pharmacokinetics, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Hyogo, Japan. keizo@pharm.kobegakuin.ac.jp
Summary
Fluvoxamine (FLV) shows affinity for plasma lipoproteins. Elevated lipoproteins may decrease FLV distribution to the brain, potentially attenuating its pharmacokinetic effects.
Area of Science:
- Pharmacology
- Biochemistry
- Toxicology
Background:
- Clinical studies suggest fluvoxamine (FLV) lowers plasma lipoprotein levels.
- Limited research exists on how plasma lipoproteins affect FLV pharmacokinetics.
Purpose of the Study:
- Investigate FLV affinity for plasma lipoproteins.
- Determine the impact of plasma lipoproteins on FLV biodistribution.
- Utilize a hyperlipidemic (HL) rat model for the study.
Main Methods:
- Hyperlipidemia induced in rats via Poloxamer-407 administration.
- In vitro analysis of FLV binding and distribution in plasma lipoproteins.
- In vivo pharmacokinetic and biodistribution studies of FLV in control and HL rats.
Main Results:
- FLV plasma protein binding increased from 83% in controls to 95% in HL rats.
- FLV recovery in triglyceride-rich lipoproteins was higher in HL rats.
- Area under the curve (AUC) for FLV was 3.9-fold greater in HL rats; brain distribution decreased by 80%.
Conclusions:
- FLV exhibits affinity for plasma lipoproteins.
- Elevated lipoproteins may reduce FLV brain biodistribution.
- Plasma lipoprotein levels might attenuate FLV's pharmacokinetic effects in the brain.
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