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Citalopram (Celexa) Medical Facts
Citalopram (Celexa) in Brief
- Active ingredient: Citalopram hydrobromide
- Common brand names: Celexa, Cipramil, Sipralexa,
Seropram, Celepram
- Drug class: Antidepressant, Selective serotonin
reuptake inhibitor (SSRI)
- FDA Approved: July 17, 1998
- Chemical Formula:C20H22BrFN2
- Legal status: Prescription only
- Pregnancy Category: C
- Habit forming? No
- Originally discovered: 1989, Denmark

History
Citalopram (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
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
- 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
- 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 Celexa
(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 and symptoms (decrease
in headaches and muscle aches) associated with fatigue for some individuals
30.
Citalopram "pros" and "cons"
Citalopram (Celexa) may be appropriate medication in persons taking
multiple medications because of its low potential for drug interactions
and in elderly patients because of its tolerability.
- Advantages:
- well-tolerated
- minimal side-effects 2
- low risk of withdrawal symptoms 2
- lower incidence of drug interactions (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, 31
- potent anxiolytic 29
- Disadvantages:
- concern about fatalities in overdose (should be avoided in patients
likely to take overdoses)
- overdose is associated with seizures and QT interval prolongation
32
- risk of sexual side effects (decreased sexual desire, orgasmic
dysfunction, ejaculatory dysfunction) 7
- potential for weight gain
- may cause carbohydrate craving 14
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
Citalopram mean half-life is 35 hours. It may take 7 to 8 days to
clear out of the system.
Onset of action
Steady-state plasma levels are usually achieved in 1-2 weeks. As with
other SSRI antidepressants, 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
previously prescribed dose may be considered. Further dose decreasing
may be considered at more gradual rate.
Citalopram (Celexa) & Alcohol
SSRI antidepressants present a low risk of fatal poisoning when taken
in combination with alcohol 34.
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. Food and Drug Administration. Citalopram
U.S. 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, Wa*linder 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. PubMed
- 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. PubMed
- 8.Wainberg ML, Muench F, Morgenstern J, Hollander
E, Irwin TW, Parsons JT, Allen A, O'Leary A. A double-blind study
of citalopram versus placebo 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, Padi'n JJ, Rivas MT, Sa'nchez 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. PubMed
- 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. PubMed
- 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. PubMed
- 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, Br?sen
K, Aaes-J?rgensen 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, Lancto^t 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. Epub 2007 Apr 16. PubMed
- 22. Talley NJ, Kellow JE, Boyce P, Tennant C,
Huskic S, Jones M. Antidepressant Therapy (Imipramine and Citalopram)
for Irritable Bowel Syndrome: A Double-Blind, Randomized, Placebo-Controlled
Trial. Talley NJ, Kellow JE, Boyce P, Tennant C, Huskic S, Jones M.
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. Epub 2006 Jan 9. PubMed
- 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. Leombruni P, Amianto F, Delsedime N, Gramaglia
C, Abbate-Daga G, Fassino S. Citalopram versus fluoxetine for the
treatment of patients with bulimia nervosa: a single-blind randomized
controlled trial. Adv Ther. 2006 May-Jun;23(3):481-94. PubMed
- 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, Ma'rkus
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.
Epub 2003 Oct 30. PubMed
- 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. Aragona M, Bancheri L, Perinelli D, Tarsitani
L, Pizzimenti A, Conte A, Inghilleri M. Randomized double-blind comparison
of serotonergic (Citalopram) versus noradrenergic (Reboxetine) reuptake
inhibitors in outpatients with somatoform, DSM-IV-TR pain disorder.
Eur J Pain. 2005 Feb;9(1):33-8. 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.
PubMed
- 33. Rush AJ, Trivedi MH, Wisniewski SR, Stewart
JW, Nierenberg AA, Thase ME, Ritz L, Biggs MM, Warden D, Luther JF,
Shores-Wilson K, Niederehe G, Fava M; STAR*D Study Team. Bupropion-SR,
sertraline, or venlafaxine-XR after failure of SSRIs for depression.
N Engl J Med. 2006 Mar 23;354(12):1231-42. PubMed
- 34. 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.
Epub 2005 Mar 1. PubMed
Interesting facts
- 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.
- After unsuccessful treatment with an SSRI, approximately 25% of
patients have a remission of symptoms after switching to another
antidepressant (SSRI, bupropion (Wellbutrin) or venlafaxine (Effexor))
33.
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