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Chapter 17. Citalopram and S-Citalopram

Patrick H. Roseboom, Ph.D.; Ned H. Kalin, M.D.
DOI: 10.1176/appi.books.9781585623860.411382

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Excerpt

Citalopram (Celexa) and its pharmacologically active enantiomer, S-citalopram (Lexapro), are among the most selective serotonin (5-HT) reuptake inhibitors available. Both drugs are widely prescribed and have been shown in large-scale controlled trials to be effective in the treatment of depression; S-citalopram has also been shown in large-scale controlled trials to be effective in the treatment of anxiety disorders. In addition, both drugs are well tolerated in patients and show a low potential for pharmacokinetic drug interactions. Citalopram and S-citalopram have similar efficacy in the treatment of depression, with some studies suggesting a modest superiority of S-citalopram over citalopram in some measures of efficacy, including a possibly faster onset of therapeutic effect for S-citalopram. Antagonism of the effects of S-citalopram by R-citalopram has been invoked to explain the purported therapeutic differences between the two drugs. In addition, the affinity of citalopram for histamine receptors appears to reside in the R-enantiomer, suggesting that S-citalopram has a decreased potential for antihistaminergic side effects. Whether the postulated superiority of S-citalopram over citalopram is clinically meaningful in psychiatric practice requires further study.

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FIGURE 17–1. Chemical structure of citalopram.Asterisk (*) indicates chiral center.

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A possible explanation for the postulated modest superiority of S-citalopram over citalopram on some measures of antidepressant activity is
2.
Which of the following is a characteristic of citalopram’s pharmacokinetics?
3.
Treatment with citalopram was used in the first phase of the Sequenced Treatment Alternatives to Relieve Depression (STAR*D) trial. The primary outcome measure was depression remission, as measured by two rating scales. What remission rates were reported at study exit for citalopram?
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