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Pharmacokinetics of pentachlorophenol in man
Archives of Toxicology
|February 1, 1986
Summary
Pentachlorophenol (PCP) has a long elimination half-life of approximately 17-20 days in humans, primarily due to high protein binding and tubular reabsorption. Alkalinizing the urine significantly increases PCP excretion.
Area of Science:
- Environmental Toxicology
- Human Pharmacology
- Pharmacokinetics
Background:
- Pentachlorophenol (PCP) is a widely used biocide with potential human health risks.
- Understanding PCP's metabolic fate and elimination in humans is crucial for risk assessment.
Purpose of the Study:
- To determine the elimination half-life and clearance of PCP in human volunteers.
- To investigate factors influencing PCP elimination, including plasma protein binding, tubular reabsorption, urinary pH, and enterohepatic circulation.
Main Methods:
- Oral administration of PCP and 13C-PCP to volunteers.
- Monitoring urinary and plasma PCP levels using gas chromatography-mass spectrometry (GC/MS).
- Investigating the effect of urinary alkalinization and analyzing bile for PCP presence.
Main Results:
- An elimination half-life of 17-20 days was determined for PCP in urine and blood.
- PCP clearance was found to be 0.07 ml/min, attributed to high plasma protein binding (>96%) and tubular reabsorption.
- Urinary alkalinization significantly increased daily PCP excretion.
- No significant accumulation of PCP in the enterohepatic circulation was observed.
Conclusions:
- PCP exhibits prolonged persistence in the human body due to pharmacokinetic factors.
- Urinary pH modification can enhance PCP elimination.
- The enterohepatic circulation does not appear to be a major reservoir for PCP in humans.