|Values are valid only on day of printing.|
Monitoring citalopram 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 CYP2C19 and CYP3A4-5 genotyping
Citalopram (Celexa) and S-citalopram (escitalopram, Lexapro) are approved for treatment of depression. Celexa is a racemic mixture containing equal amounts of R- and S-enantiomer. Metabolites of citalopram (N-desmethylcitalopram) are less active than citalopram and do not accumulate in serum to clinically significant concentration.
Citalopram metabolism is carried out by cytochrome P450 (CYP) 2C19 and 3A4-5. CYP 2D6 may play a minor role in citalopram metabolism. Citalopram is known to reduce CYP 2D6 activity. Citalopram clearance is significantly affected by reduced hepatic function, but only slightly by reduced renal function.
A typical Celexa dose administered to an adult is 40-mg per day. A typical Lexapro dose is 20-mg per day. Citalopram is 80% protein bound, and the apparent volume of distribution is 12 L/Kg. Bioavailability is 80% and protein binding is 56% for either form of the drug. Time to peak serum concentration is 4 hours, and the elimination half-life is 35 hours. Half-life is increased in the elderly. Dosage reductions may be necessary for patients who are elderly or have reduced hepatic function.
Steady-state serum concentrations associated with optimal response to citalopram are in the range of 50 to 100 ng/mL when the patient is administered the R,S-enantiomeric mixture (Celexa).
The most common toxicities associated with excessive serum concentration are fatigue, impotence, insomnia, and anticholinergic effects. The toxic range for citalopram is >220 ng/mL.
Test interpretation requires knowledge of which enantiomers (R, S- or S-) are prescribed; this assay does not distinguish the enantiomers.
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