Objective: To provide clinicians with a critical evaluation of citalopram,
a selective serotonin reuptake inhibitor (SSRI) that has been available in
Canada since March 1999. Data sources: Commercial searches (MEDLINE and Bib
lioTech) and an "in-house" search (InfoDrug) were used to find published En
glish-language references for clinical and preclinical publications. There
was no restriction of publication dates. Primary index terms used were: pha
rmacological properties, receptors, pharmacological selectivity, pharmacoki
netics, age-related pharmacokinetics, sex-related pharmacokinetics, renal d
ysfunction, hepatic dysfunction, cytochrome activity, drug interactions, ad
verse reactions, antidepressant switching, precautions, overdose, drug disc
ontinuation, children, geriatric, depression, combination therapy, placebo
control, refractory depression, anxiety disorders and medical disorders. St
udy selection: A total of 74 studies were reviewed. Twenty-one of these stu
dies specifically examined the clinical efficacy and tolerability of citalo
pram in depressive disorders as well as other disorders. In depressive diso
rders, clinical studies were required to have either placebo or active comp
arison controls for a minimum of 3 weeks. For other disorders, in the absen
ce of double-blind trials, open-label studies were included. Pharmacologica
l studies were limited to animal studies focusing on citalopram's selectivi
ty and receptor specificity, and positron emission tomography studies were
incorporated to include human pharmacological data. Pharmacokinetic studies
focused on the metabolism, safety and tolerability of citalopram, specific
ally with reference to adverse reactions, drug interactions and overdose in
addition to citalopram's effect on vulnerable populations, such as childre
n, the elderly and patients with metabolic diseases. Data extraction: Data
on clinical studies were summarized according to test measures, study durat
ion and outcome of study. Pharmacokinetic and pharmacodynamic studies were
summarized according to properties and interactions. Adverse reactions were
extracted to outline citalopram's safety profile. Data synthesis: Citalopr
am is an SSRI antidepressant with a more specific and selective pharmacolog
ical profile than other antidepressants of its class. It is well tolerated,
and drug interactions are not a significant concern. It is also reasonably
safe for populations vulnerable to pharmacokinetic effects, such as the el
derly and patients with metabolic diseases. In addition to its tolerability
, citalopram is effective in the treatment of major depression, other depre
ssive disorders and panic disorder. It has the potential to effectively tre
at other anxiety disorders and substance-use disorders; in addition, it may
be useful in several medical conditions. Conclusions: There is evidence to
support the role of citalopram as a well-tolerated and effective SSRI anti
depressant. There is a need for further evaluation of its role in psychiatr
ic disorders other than major depressive disorder.