Citalopram HBr (Celexa®)

Citalopram in Brief
  • Generic name : Citalopram hydrobromide
  • Brand names: Celexa®, Cipramil®, Sipralexa, Seropram, Celepram
  • Therapeutic class: Antidepressant
  • Pharmacologic class: Selective serotonin reuptake inhibitor (SSRI)
  • FDA Approved: July 17, 1998
  • Chemical Formula: C20H22BrFN2
  • Pregnancy Category: C
  • Habit forming? No
  • Originally discovered: 1989, Denmark Denmark

History

Citalopram hydrobromide (Cipramil®) was originally created in 1989 by the pharmaceutical research-based company Lundbeck. Citalopram was under development for 15 years before it was finally introduced in Denmark 3.

H. Lundbeck A/S, founded in 1915, is a privately held international pharmaceutical company based in Copenhagen, Denmark. Lundbeck is engaged in the research and development, production, marketing and sale of drugs for the treatment of psychiatric and neurological disorders.

On March 27, 1998, American generics company, Forest Laboratories, entered into a strategic alliance with H. Lundbeck A/S covering United States marketing rights to central nervous system products developed by Lundbeck. Forest Laboratories does not engage in research itself, focusing instead on the development and sales of other companies products within the U.S. 3

Forest Laboratories introduced Cipramil® under the name Celexa® in September 1998.

FDA approved indications

  • depression

Off-label & Investigational uses

  • diabetic neuropathy 16
  • premature ejaculation 11
  • alcohol dependence 13, 17
  • panic disorder 18
  • social anxiety disorder (social phobias) 20
  • premenstrual dysphoric disorder 21
  • functional abdominal pain34 and irritable bowel syndrome (IBS) 22, 23, 24
  • seasonal affective disorder 4
  • compulsive sexual behavior (CSB) 8
  • anorexia nervosa 15
  • binge-eating disorder 25
  • bulimia nervosa 26
  • fibromyalgia 27
  • dementia
  • behavioural disturbances
  • hostility 33
  • obsessive-compulsive disorder (OCD) 2
  • chronic fatigue 30

Premature ejaculation
Citalopram has been found to significantly increase intravaginal ejaculatory latency time and number of intercourse episodes, and improve intercourse satisfaction 11.

Panic disorder
Citalopram (20-30 mg) can significantly decrease phobic symptoms in patients with panic disorder 18. Citalopram 20-30 mg is more effective than citalopram 40-60 mg 19.

Social anxiety disorder
Results of the study 20 suggest that citalopram (at a mean dose of 55 mg) may be a safe and effective treatment for generalized social anxiety disorder. It also may be effective for patients who have failed to tolerate or respond to a prior treatment trial.

Irritable bowel syndrome (IBS)
Selective serotonin reuptake inhibitors (SSRIs) are frequently used in the treatment of irritable bowel syndrome (IBS) although evidence of their efficacy is scarce. Results of the study suggest that Citalopram (20-40 mg/day) can significantly improve IBS symptoms. It can improve abdominal pain, bloating, impact of symptoms on daily life, and overall well being. The therapeutic effect is independent of effects on anxiety, depression, and colonic sensorimotor function 24.

Chronic fatigue
Citalopram 20 to 40 mg/day may improve fatigue, decrease headaches and muscle aches associated with fatigue for some individuals 30.


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Citalopram "pros" and "cons"

Citalopram may be appropriate for persons taking multiple medications because of its low potential for drug interactions and in elderly patients because of its tolerability.

Advantages:

  • Citalopram may be more tolerable than some other antidepressants, with relatively modest incidence of side effects 2
  • Low risk of withdrawal symptoms 2
  • Lower incidence of interactions - the only significant drug interaction is considered to be with MAOI 5, 6
  • Less likely than other SSRIs to cause sexual dysfunction 9, 10
  • Low rates of activating side effects (insomnia, anxiety, agitation)
  • Normalization of blood pressure
  • Safe in diverse populations
  • May be suitable antidepressant for fluoxetine (Prozac) intolerant patients 12
  • Analgesic effect 28
  • Potent anxiolytic 29

Disadvantages:

  • Concern about fatalities in overdose. Citalopram should be avoided in patients likely to take overdoses.
  • Overdose is associated with seizures and QT interval prolongation 32.
  • Because of the potential to increase the cardiac QT interval and the risk of torsade de pointes, citalopram dosage was recently restricted to maximum of 40 mg per day.
  • Risk of sexual side effects (decreased sexual desire, orgasmic dysfunction, ejaculatory dysfunction) 7
  • Risk for weight gain. May cause carbohydrate craving 14.
  • Citalopram has mild antihistamine properties which may be responsible for sedation, fatigue, and "emotional flattening" in some patients.

Mechanism of action

Citalopram hydrobromide is a highly selective and potent serotonin (5-hydroxytryptamine or 5-HT) reuptake inhibitor with minimal effects on the neuronal reuptake of norepinephrine and dopamine. The ability of citalopram to potentiate serotonergic activity in the central nervous system via inhibition of the neuronal reuptake of serotonin is thought to be responsible for its antidepressant action 1.

Time for Citalopram to clear out the system

The mean half-life is 35 hours. It may take 7 to 8 days to clear out of the system.

Onset of action

Citalopram hbr steady-state plasma levels are usually achieved in 1-2 weeks. Improvement in depression symptoms may be noticed in 1 to 4 weeks.

Weaning off Citalopram (Celexa)

Gradual reduction in the dose rather than abrupt cessation is recommended whenever possible. If intolerable symptoms occur following a decrease in the dose or upon discontinuation of treatment, then resuming the previous dose may be considered. Further dose decreasing may be undertaken at more gradual rate.

Citalopram & Alcohol

SSRI antidepressants present a low risk of fatal poisoning when taken in combination with alcohol 31. The clinical studies have shown that Citalopram does not potentiate the cognitive and motor effects of alcohol. However, concurrent use of alcohol and citalopram is not recommended because of possible added depressant effect.

Further reading

References

  • 1. U.S. FDA. Citalopram Prescribing Information.
  • 2. Pato MT. Beyond depression: citalopram for obsessive-compulsive disorder. Int Clin Psychopharmacol. 1999 May;14 Suppl 2:S19-26. PubMed
  • 3. Company history: 1975-1990.;Company history: 1990-2003. H. Lundbeck A/S
  • 4. Thorell LH, Kjellman B, Arned M, Lindwall-Sundel K, Walinder J, Wetterberg L. Light treatment of seasonal affective disorder in combination with citalopram or placebo with 1-year follow-up. Int Clin Psychopharmacol. 1999 May;14 Suppl 2:S7-11. PubMed
  • 5. Spina E, Scordo MG, D'Arrigo C. Metabolic drug interactions with new psychotropic agents. Fundam Clin Pharmacol. 2003 Oct;17(5):517-38. PubMed
  • 6. Syvalahti EK, Taiminen T, Saarijarvi S, Lehto H, Niemi H, Ahola V, Dahl ML, Salokangas RK. Citalopram causes no significant alterations in plasma neuroleptic levels in schizophrenic patients. J Int Med Res. 1997 Jan-Feb;25(1):24-32.
  • 7. Ekselius L, von Knorring L. Effect on sexual function of long-term treatment with selective serotonin reuptake inhibitors in depressed patients treated in primary care. J Clin Psychopharmacol. 2001 Apr;21(2):154-60.
  • 8.Wainberg ML, Muench F, Morgenstern J, Hollander E, Irwin TW, Parsons JT, Allen A, O'Leary A. A double-blind study of citalopram in the treatment of compulsive sexual behaviors in gay and bisexual men. J Clin Psychiatry. 2006 Dec;67(12):1968-73. PubMed
  • 9. Arias F, Padin JJ, Rivas MT, Sanchez A. Sexual dysfunctions induced by serotonin reuptake inhibitors. Aten Primaria. 2000 Oct 15;26(6):389-94. PubMed
  • 10. Mendels J, Kiev A, Fabre LF. Double-blind comparison of citalopram and placebo in depressed outpatients with melancholia. Depress Anxiety. 1999;9(2):54-60.
  • 11. Safarinejad MR, Hosseini SY. Safety and efficacy of citalopram in the treatment of premature ejaculation: a double-blind placebo-controlled, fixed dose, randomized study. Int J Impot Res. 2006 Mar-Apr;18(2):164-9
  • 12. Calabrese JR, Londborg PD, Shelton MD, Thase ME. Citalopram treatment of fluoxetine-intolerant depressed patients. J Clin Psychiatry. 2003 May;64(5):562-7.
  • 13. C A Naranjo, D M Knoke, and K E Bremner. Variations in response to citalopram in men and women with alcohol dependence. J Psychiatry Neurosci. 2000 May; 25(3): 269–275. PubMed
  • 14. Bouwer CD, Harvey BH. Phasic craving for carbohydrate observed with citalopram. Int Clin Psychopharmacol. 1996 Dec;11(4):273-8. PubMed
  • 15. Fassino S, Leombruni P, Daga G, Brustolin A, Migliaretti G, Cavallo F, Rovera G. Efficacy of citalopram in anorexia nervosa: a pilot study. Eur Neuropsychopharmacol. 2002 Oct;12(5):453-9. PubMed
  • 16. Sindrup SH, Bjerre U, Dejgaard A, Brosen K, Aaes-Jorgensen T, Gram LF. The selective serotonin reuptake inhibitor citalopram relieves the symptoms of diabetic neuropathy. Clin Pharmacol Ther. 1992 Nov;52(5):547-52. PubMed
  • 17. Naranjo CA, Bremner KE, Lanctot KL. Effects of citalopram and a brief psycho-social intervention on alcohol intake, dependence and problems. Addiction. 1995 Jan;90(1):87-99. PubMed
  • 18. Leinonen E, Lepola U, Koponen H, Turtonen J, Wade A, Lehto H. Citalopram controls phobic symptoms in patients with panic disorder: randomized controlled trial. J Psychiatry Neurosci. 2000 Jan;25(1):24-32. PubMed
  • 19. Wade AG, Lepola U, Koponen HJ, Pedersen V, Pedersen T. The effect of citalopram in panic disorder. Br J Psychiatry. 1997 Jun;170:549-53. PubMed
  • 20. Simon NM, Korbly NB, Worthington JJ, Kinrys G, Pollack MH. Citalopram for social anxiety disorder: an open-label pilot study in refractory and nonrefractory patients. CNS Spectr. 2002 Sep;7(9):655-7. PubMed
  • 21. Ravindran LN, Woods SA, Steiner M, Ravindran AV. Symptom-onset dosing with citalopram in the treatment of premenstrual dysphoric disorder (PMDD): a case series. Arch Womens Ment Health. 2007 Jun;10(3):125-7. PubMed
  • 22. Talley NJ, Kellow JE, Boyce P, Tennant C, Huskic S, Jones M. Therapy for Irritable Bowel Syndrome: A Double-Blind, Randomized, Placebo-Controlled Trial. Dig Dis Sci. 2007 May 15; PubMed
  • 23. Masand PS, Gupta S, Schwartz TL, Virk S, Hameed A, Kaplan DS. Open-label treatment with citalopram in patients with irritable bowel syndrome: a pilot study. Prim Care Companion J Clin Psychiatry. 2005;7(4):162-6. PubMed
  • 24. Tack J, Broekaert D, Fischler B, Oudenhove LV, Gevers AM, Janssens J. A controlled crossover study of the selective serotonin reuptake inhibitor citalopram in irritable bowel syndrome. Gut. 2006 Aug;55(8):1095-103.
  • 25. McElroy SL, Hudson JI, Malhotra S, Welge JA, Nelson EB, Keck PE. Citalopram in the treatment of binge-eating disorder: a placebo-controlled trial. J Clin Psychiatry. 2003 Jul;64(7):807-13. PubMed
  • 26. Milano W, Petrella C, Capasso A. Treatment of bulimia nervosa with citalopram: a randomized controlled trial. Biomed Res 2005;16:85–87.
  • 27. von Knorring L. Citalopram in patients with fibromyalgia--a randomized, double-blind, placebo-controlled study. Eur J Pain. 2000;4(1):27-35. PubMed
  • 28. Baraczka K, Janko' Z, Vargha K, Markus H. Clinical experiences with the analgesic effects of citalopram. Orv Hetil. 1997 Oct 12;138(41):2605-7. PubMed
  • 29. Fish EW, Faccidomo S, Gupta S, Miczek KA. Anxiolytic-like effects of escitalopram, citalopram, and R-citalopram in maternally separated mouse pups. J Pharmacol Exp Ther. 2004 Feb;308(2):474-80.
  • 30. Hartz AJ, Bentler SE, Brake KA, Kelly MW. The effectiveness of citalopram for idiopathic chronic fatigue. J Clin Psychiatry. 2003 Aug;64(8):927-35. PubMed
  • 31. Koski A, Vuori E, Ojanpera I. Newer antidepressants: evaluation of fatal toxicity index and interaction with alcohol based on Finnish postmortem data. Int J Legal Med. 2005 Nov;119(6):344-8. PubMed
  • 32. Kelly CA, Dhaun N, Laing WJ, Strachan FE, Good AM, Bateman DN. Comparative toxicity of citalopram and the newer antidepressants after overdose. J Toxicol Clin Toxicol. 2004;42(1):67-71.
  • 33. Kamarck TW, Haskett RF, Muldoon M, Flory JD, Anderson B, Bies R, Pollock B, Manuck SB. Citalopram intervention for hostility. J Consult Clin Psychol. 2009 Feb;77(1):174-88.
  • 34. Roohafza H, Pourmoghaddas Z, Saneian H, Gholamrezaei A. Citalopram for pediatric functional abdominal pain: a randomized, placebo-controlled trial. Neurogastroenterol Motil. 2014 Nov;26(11):1642-50.

Published: November 12, 2008
Last updated: February 01, 2017

Interesting facts

Citalopram molecule
  • Forest licenses the United States rights to Celexa from H. Lundbeck A/S, a privately held pharmaceutical company based in Copenhagen and the drug's originator.
  • The molecule is composed of two enantiomers - mirror images. They are called S-(+)-citalopram and R-(–)-citalopram.
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