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Celexa™ (Citalopram)                                                     Revised    6/10


History/ Background

Citalopram (also known as CelexaTM) is a selective serotonin reuptake inhibitor (SSRI) that was FDA-approved in 1998 for the treatment of depression.  It is a bicyclic phthalane derivative and structurally unrelated to tricyclic antidepressant drugs.  The selectivity for serotonin reuptake inhibition has been reported to be greater than other SSRI's including fluoxetine and paroxetine.

Mechanism of Action

Citalopram selectively inhibits the reuptake of neuronal serotonin 95-HT).  The mechanism of action of citalopram as an antidepressant is presumed to be linked to potentiation of serotonergic activity in the central nervous system resulting from its inhibition of CNS neuronal reuptake of serotonin.  Studies suggest that citalopram has no effects on norepinephrine and dopamine neuronal reuptake.

Kinetics

Citalopram is rapidly absorbed from the GI tract and has peak concentration is seen within 2 to 4 hours.  Food does not seem to affect its absorption.  The volume of distribution of citalopram is about 12 L/kg and it is approximately 80% protein bound.  Citalopram is metabolized mainly through the liver, with a mean terminal half-life of about 35 hours.

Clinical Presentation

Overdose of citalopram commonly causes CNS depression along with nausea and vomiting.  It has been reported to cause ECG changes, including tachydysrhythmia, widening of the QRS or prolongation of QTc.  Other toxicities, such seizures, hypotension, metabolic acidosis, hypokalemia, and syncope, have been noted after overdose.  Given its effect on serotonin levels, it is possible that citalopram may cause or contribute to serotonin syndrome.

Decontamination and Management

Establish and maintain an airway to ensure adequate ventilation and oxygenation.  Activated charcoal may be considred if ingestion occurred within the past one hour. 

There are no specific antidotes for ciralopram.  Provide good symptomatic and supportive care. Treat seizures with benzodiazepines, such as lorazepam, diazepam or midazolam.

This is not a treatment guideline and management may differ depending on the patient's history and other coingestions.  Call your Poison Control Center at 1-800-222-1222 if you have an overdose case for help and consulation.

References :

1. Pacher P, Ungvari Z, Nanasi P, et al. Speculations on difference between tricyclic and selective serotonin reuptake inhibitor antidepressants on their cardiac effects. Is there any? Current Medicinal Chemistry 1999; 6:469-480.
2. Rasmussen SL, Overo KF, Tanghoj P. Cardiac safety of citalopram: Prospective trials and retrospective analyses. J Clin Psychopharmacology 1999; 19(5):407-415.
3. Grundemar L, Wohlfart B, Lagersteedt C, et al. Symptoms and signs of severe citalopram overdose. Lancet 1997; 349: 1602.
4. Catalano G, Catalano MC, Epstein MA, et al. QTc interval prolongation associated with citalopram overdose: a case report and literature review. Clin Neuropharmacol 2001; May-June: 2-6.
5. Personne M, Sjoberg G, Persson H. Citalopram overdose: review of cases treated in Swedish hospitals. J Toxicol Clin Toxicol 1997; 35: 237-40.

6. Engebretsen, K.,Harris, C., Wood, J.Cardiotoxicity and late onset seizures with citalopram overdose.J Emergency Medicine 2003; 25 (2): 163-166.

7.Isbister, G., Bowe, S., Dawson, A., Whyte,I.Relative toxicity of selective serotonin reuptake inhibitors (SSRIs) in overdose. J Toxicol Clin Toxicol 2004; 42 (3), 277-285.

8. Kelly, C., Dhaun, N., Laing, W, et al. Comparative toxicology of citalopram and the newer antidepressants after overdose.J Toxicol Clin Toxicol 2004; 42 (1), 67-71.

9. Cuenca, P., Holt, K., Hoefle, J. Seizure secondary to citalopram overdose. .J Emergency Medicine 2004; 26 (2): 177-181.

10. US FDA website;

http://www.fda.gov/ohrms/dockets/ac/04/briefing/4006B1_07_Celexa-Label.pdf;

11. Nelson LS, Erdman AR, Booze LL, Cobaugh DJ, Chyka PA, Woolf AD, et al. Selective serotonin reuptake inhibitor poisoning: an evidence based consensus guideline for out-of-hospital managment.  Clin Toxicol 2007;45:315-332.

12. Editorial Staff: Citalopram. In: Klasco RK (Ed): DRUGDEX® System. Thompson Reuters, Greenwood Village, Colorado (Edition expires 12/2009)

 

 

 



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