The pharmacokinetics of gabapentin in cats.

BACKGROUND

Gabapentin is the most commonly prescribed medication for the treatment of chronic musculoskeletal pain in cats. Despite this common and chronic usage, clinically relevant pharmacokinetic data is lacking.

OBJECTIVES

To evaluate the pharmacokinetics of clinically relevant dosing regimens of gabapentin in cats.

ANIMALS

Eight research-purpose mixed-breed cats.

METHODS

Cats were enrolled in a serial order, non-randomized pharmacokinetic study. Gabapentin was administered as an IV bolus (5 mg/kg), orally (10 mg/kg) as a single dose or twice daily for 2 weeks, or as a transdermal gel (10 mg/kg) in serial order. Serial blood samples were collected up to 48 hours. Plasma concentrations were determined using Ultra Performance Liquid Chromatography-Mass Spectrometry. Compartmental analysis was used to generate gabapentin time-concentration models.

RESULTS

After IV administration CL (median (range)) and terminal half-life were 160.67 mL/kg*hr (119.63-199.11) and 3.78 hours (3.12-4.47), respectively. The oral terminal half-life was 3.63 hours (2.96-4.77), and 3.72 hours (3.12-4.51) for single and repeated dosing. T and C , as predicted by the model were 1.05 hours (0.74-2.11), and 12.42 μg/mL (8.31-18.35) after single oral dosing, and 0.77 hours (0.58-1.64), and 14.78 μg/mL (9.70-18.41) after repeated oral dosing. Bioavailability after a single oral dose was 94.77% (82.46-122.83).

IMPORTANCE

Repeated oral dosing of gabapentin did not alter the drug's pharmacokinetics, making dose adjustments unnecessary with long-term treatment. As prepared, the transdermal route is an inappropriate choice for drug administration. These relevant data are important for future studies evaluating potential efficacy of the medication for treating chronic pain states in cats.