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Citalopram

From Pharmacopedia

Experience

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1 provider report · avg efficacy 40.0/100 · avg side-effect burden 40.0/100 · 10 patients managed total

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Titration strategies

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Summary
Common uses
Major depressive disorder (FDA)0, Generalized anxiety disorder (off-label)0, Panic disorder (off-label)0, Obsessive-compulsive disorder (off-label)0, Posttraumatic stress disorder (off-label)0, Premenstrual dysphoric disorder (off-label)0, Menopausal vasomotor symptoms (off-label)0
Pharmacy
Starting dose
20 mg PO once daily; titrate to 40 mg/day after 1 week if tolerated. Elderly (>60) and hepatic impairment: 20 mg/day ceiling
Preparations
Tablets 10, 20, 40 mg; oral solution 10 mg/5 mL
US FDA Max
20 mg/day in adults >60 years per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60
Pharmacology
Routes
Oral
Onset
Antidepressant effect over 1-2 weeks; full clinical effect 4-6 weeks
Duration
24 hours (once-daily dosing)
Half-life
~35 hours[2]
Bioavailability
~80% (oral)[2]
Pregnancy
Observational signal for persistent pulmonary hypertension of the newborn (small absolute risk) and neonatal adaptation syndrome with third-trimester exposure.[citation needed]
Legal status
Rx-only in US. Carries the antidepressant Boxed Warning for suicidality in children, adolescents, and young adults[2]
Purported mechanism
Racemic mixture of R- and S-citalopram (the S-enantiomer is escitalopram, separately marketed as Lexapro). The S-enantiomer carries essentially all of the serotonin transporter (SERT) binding activity, while the R-enantiomer contributes the QT-prolonging liability that prompted the FDA's 2011 dose ceiling for adults over 60.0 CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response[1].

References

  1. CPIC Guideline for CYP2D6 and CYP2C19 Genotypes and Dosing of Selective Serotonin Reuptake Inhibitors, 2023. https://cpicpgx.org/guidelines/guideline-for-selective-serotonin-reuptake-inhibitors-and-cyp2d6-and-cyp2c19/
  2. 2.0 2.1 2.2 FDA Prescribing Information, Celexa (citalopram hydrobromide), Allergan/AbbVie, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020822s045lbl.pdf