Citalopram
Generic name: Citalopram
Sold under these brand names: Akarin, Celexa, Cipramil, Citrol, Cipraned , Citalopram, Seropram
Uses
It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia. The antidepressant effects may take one to four weeks to occur. It is taken by mouth.
Side Effects
Common side effects include nausea, trouble sleeping, sexual problems, shakiness, feeling tired, and sweating. Serious side effects include an increased risk of suicide in those under the age of 25, serotonin syndrome, glaucoma, and QT prolongation. It should not be used in someone on a MAO inhibitor. Antidepressant discontinuation syndrome may occur when stopped. There are concerns that use during pregnancy may harm the baby.
Pharmacokinetics
Citalopram is metabolized in the liver mostly by CYP2C19, but also by CYP3A4 and CYP2D6. Metabolites desmethylcitalopram and didesmethylcitalopram are significantly less energetic and their contribution to the overall action of citalopram is negligible. The half-life of citalopram is about 35 hours. Approximately 80% is cleared by the liver and 20% by the kidneys. The elimination process is slower in the elderly and in patients with liver or kidney failure. With once-daily dosing, steady plasma concentrations are achieved in about a week. Potent inhibitors of CYP2C19 and 3A4 might decrease citalopram clearance.
Administration
Citalopram is typically taken in one dose, either in the morning or evening. It can be taken with or without food. Its absorption does not increase when taken with food, but doing so can help prevent nausea. Nausea is often caused when the 5HT3 receptors actively absorb free serotonin, as this receptor is present within the digestive tract. The 5HT3 receptors stimulate vomiting. This side effect, if present, should subside as the body adjusts to the medication.
Overdose
Overdosage may result in vomiting, sedation, disturbances in heart rhythm, dizziness, sweating, nausea, tremor, and rarely amnesia, confusion, coma, or convulsions. Overdose deaths have occurred, sometimes involving other drugs, but also with citalopram as the sole agent. Citalopram and N-desmethylcitalopram may be quantified in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients or to assist in a medicolegal death investigation. Blood or plasma citalopram concentrations are usually in a range of 50-400 μg/l in persons receiving the drug therapeutically, 1000–3000 μg/l in patients who survive acute overdosage and 3–30 mg/l in those who do not survive. It is the most dangerous of SSRIs in overdose.
References
Citalopram Hydrobromide Monograph for Professionals”. Drugs.com. AHFS. Retrieved 23 December 2018.
“Celexa (citalopram hydrobromide) Tablets/Oral Solution” (PDF). Prescribing Information. Forest Laboratories, Inc.
Rang HP (2003). Pharmacology. Edinburgh: Churchill Livingstone. p. 187. ISBN978-0-443-07145-4.
Stahl SM (2011). The Prescriber’s Guide (Stahl’s Essential Psychopharmacology). Cambridge, UK: Cambridge University Press. ISBN978-0-521-17364-3.
Research, Center for Drug Evaluation and (24 August 2011). “Abnormal heart rhythms associated with high doses of Celexa (citalopram hydrobromide)”. Safety Communication.
Personne M, Sjöberg G, Persson H (1997). “Citalopram overdose–review of cases treated in Swedish hospitals”. Journal of Toxicology. Clinical Toxicology. 35 (3): 237–40. doi:10.3109/15563659709001206. PMID9140316
Luchini D, Morabito G, Centini F (December 2005). “Case report of a fatal intoxication by citalopram”. The American Journal of Forensic Medicine and Pathology. 26 (4): 352–4. doi:10.1097/01.paf.0000188276.33030.dd. PMID16304470
Taylor D, Paton C, Kapur S (2012). The Maudsley Prescribing Guidelines in Psychiatry (Taylor, The Maudsley Prescribing Guidelines). Hoboken, NJ, USA: Wiley-Blackwell. p. 588. ISBN9780470979693.
“Citalopram”. DrugBank. 17 August 2016. Retrieved 12 February 2017.
Final Labelling Citalopram https://www.fda.gov/ohrms/dockets/ac/04/briefing/4006b1_07_celexa-label.pdf