|Values are valid only on day of printing.|
Paroxetine (Paxil and Paxil CR) is approved for treatment of depression. Paroxetine is completely absorbed. Metabolites of paroxetine are inactive. Paroxetine metabolism is carried out by cytochrome P450 (CYP) 2D6. Paroxetine can saturate CYP2D6 resulting in a nonlinear relationship between dose and serum concentration. Paroxetine clearance is significantly affected by reduced hepatic function, but only slightly by reduced renal function.
A typical adult paroxetine dose is 30 mg per day. Paroxetine is 100% bioavailable, 95% protein bound, and the apparent volume of distribution is 17 L/Kg. Time to peak serum concentration is 5 hours for the regular product and 8 hours for the controlled release product. The elimination half-life is 20 hours. Half-life is prolonged in the elderly and with cirrhosis.
Monitoring paroxetine therapy
Identifying noncompliance, although regular blood level monitoring is not indicated in most patients
Identifying states of altered drug metabolism when used in conjunction with CYP2D6 genotyping
Steady-state serum concentrations associated with optimal response to paroxetine are in the range of 30 to 120 ng/mL.
The most common toxicities associated with excessive serum concentration are asthenia, anticholinergic effects, anxiety, blurred vision, and changes in sexual function. Toxic range: > or =400 ng/mL.
No significant cautionary statements
1. Hiemke C, Baumann P, Bergemann N, et al: AGNP consensus guidelines for therapeutic drug monitoring in psychiatry: update 2011. Pharmacopsychiatry 2011;44:195-235
2. Tietz Textbook of Clinical Chemistry and Molecular Diagnostics. Edited by CA Burtis, ER Ashwood, DE Bruns. Elsevier, Mosby, Saunders, 2011