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Am J Vet Res. 2003 Aug;64(8):994-8.

Comparative bioavailability of fluoxetine after transdermal and oral administration to healthy cats.

Author information

1
Chicagoland Veterinary Behavior Consultants, 1042 Mountain Glen Way, Carol Stream, IL 60188, USA.

Abstract

OBJECTIVE:

To determine bioavailability, pharmacokinetics, and safety for transdermal (TD) and oral administration of fluoxetine hydrochloride to healthy cats.

ANIMALS:

12 healthy mixed-breed sexually intact 1- to 4-year-old purpose-bred cats.

PROCEDURE:

A single-dose pharmacokinetic study involving 3 groups of 4 cats each was conducted in parallel. Fluoxetine in a formulation of pluronic lecithin organogel (PLO gel) was applied to the hairless portion of the pinnae of cats at 2 dosages (5 or 10 mg/kg), or it was administered orally in capsules at a dosage of 1 mg/kg. Plasma samples were obtained and submitted for liquid chromatography-mass spectrometry-mass spectrometry analysis of fluoxetine and its active metabolite, norfluoxetine.

RESULTS:

Peak fluoxetine concentration (Cmax) was lower and time to Cmax longer for TD administration versus oral administration. Relative bioavailability of each dose administered via the TD route was 10% of the value for oral administration of the drug. Mean plasma elimination half-life after oral administration was 47 and 55 hours for fluoxetine and norfluoxetine, respectively.

CONCLUSIONS AND CLINICAL RELEVANCE:

This study provides evidence that fluoxetine in a 15% (wt:vol) PLO gel formulation can be absorbed through the skin of cats into the systemic circulation. However, the relative bioavailability for TD administration is approximately only 10% of that for the oral route of administration.

PMID:
12926591
[Indexed for MEDLINE]

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