Intranasal and oral cocaine kinetics

Area of Science:

• Pharmacology
• Pharmacokinetics
• Toxicology

Background:

• Cocaine is a potent stimulant with significant abuse potential.
• Understanding cocaine pharmacokinetics is crucial for clinical and forensic toxicology.
• Previous studies have explored various routes of administration, but direct comparisons require further investigation.

Purpose of the Study:

• To compare the pharmacokinetic profiles of intranasal and oral cocaine administration.
• To determine the bioavailability and elimination half-life of cocaine via these routes.
• To investigate the dose-dependent kinetics of intranasal cocaine.

Main Methods:

• Seven subjects received intranasal cocaine (0.19-2.0 mg/kg) and oral cocaine (2.0-3.0 mg/kg).
• Plasma cocaine levels were measured over time.
• Pharmacokinetic parameters were analyzed using compartmental modeling.

Main Results:

• The mean elimination half-life (t 1/2) for intranasal cocaine was 75 ± 5 min, and for oral cocaine was 48 ± 3 min.
• Relative bioavailability was similar for both routes at a 2.0 mg/kg dose.
• Intranasal cocaine showed a linear increase in area under the concentration-time curve (AUC) with dose.

Conclusions:

• Intranasal and oral routes exhibit comparable bioavailability for cocaine.
• Elimination half-life differs significantly between intranasal and oral administration.
• Dose-proportional increases in exposure are observed with intranasal cocaine.