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A liquid chromatography-tandem mass spectrometry (LC-MS-MS) method was developed for the quantitation of cetirizine in human plasma. Cetirizine and hydroxyzine (internal standard) were extracted from human plasma using a solid phase extraction procedure with Oasis HLB cartridges. Elution from a reverse phase Xterra MS C18 high-performance liquid chromatography (HPLC) column using a fast gradient was followed by MS-MS-multiple reaction monitoring (MRM). Cetirizine and the internal standard were ionised using the Turbolonspray(TM) interface operating in positive ion mode. The characteristic ion dissociation transitions m/z 389.3 --> 201.1 and m/z 375.3 --> 201.1 were monitored for cetirizine and internal standard respectively The limit of quantitation was 5 ng . mL(-1) using 250 muL of plasma. Inter and Intra batch precision expressed by relative standard deviation was less than 9%. The assay was robust, sensitive, and highly specific and there was no interference from human plasma observed. With a total run-time of 6 minutes, the method was suitable for supporting clinical studies and applied to the analysis of samples from a bioequivalence study.