- Generic name: Citalopram hydrobromide
- Trade name: Celexa
- Functional class: Antidepressant
- Chemical class: Selective serotonin reuptake inhibitor
- FDA approved: July 17, 1998
- Manufacturer: Forest Pharmaceuticals, Inc.
- Habit forming? No
- Pregnancy risk factor: C
Citalopram is in a class of antidepressants called
selective serotonin reuptake inhibitors. It is indicated
for the treatment of depression. Citalopramis is also effective in the treatment of certain eating disorders (e.g., anorexia nervosa, bulimia), anxiety, and panic disorders. It has the potential
to effectively treat substance use disorders.
Citalopram is generally sedating antidepressant, and it is considerably less activating than fluoxetine and sertraline. Citalopram represents a good balance of tolerability, efficacy, and cost.
Citalopram is effective in the treatment of moderate-to-severe
major depression, especially symptoms of depressed mood and melancholia,
with particularly robust effects at doses of 40 and 60 mg/day
- Steady state: reached in about 1 week.
- Metabolism: Citalopram is metabolized in the liver
by the cytochrome P450 enzyme system to demethylcitalopram,
didemethylcitalopram, citalopram N-oxide and a deaninated propionic
acid derivative. These metabolites are not thought to contribute
to the therapeutic action since both metabolites are less potent
serotonin reuptake inhibitors than the parent compound, are
present in lower concentrations and enter the brain less readily.
- Bioavailability: approximately 80%.
- Elimination half-life: 37 hours (range 30-42 hours).
The half-life of demethylcitalopram being 2 days and 4 days
- Excretion: eliminated primarily via the
liver (85%) and the remainder via the kidneys. Approximately
12% of the daily dose is excreted in urine as unchanged citalopram.
- Lower risk of drug interactions than with some other antidepressants
3. Citalopram does not significantly affect the metabolism of other drugs. Also, its metabolism is not affected by digoxin, lithium, warfarin, or carbamazepine.
- Probably safe for use on a long-term basis
- Causes less withdrawal symptoms than other SSRIs
- Absorption is not affected by food
- Low incidence of activating side effects
- Less likely than other antidepressants to cause sexual dysfunction
- Anxiolytic effects 15
- Suitable alternative for fluoxetine intolerant individuals
- Elicit relaxation of intestinal smooth muscle 16
- Risk of QT prolongation. Citalopram is not appropriate for people with risk factors for QT-prolongation, such as structural heart disease, bradycardia, hypokalaemia, hypomagnesaemia or hypocalcaemia.
- Weight gain and craving for carbohydrate 6.
- Sexual side effects.
- Citalopram should be used with caution in persons who are at risk of taking an overdose, especially those with cardiovascular disease.
- social anxiety disorder 11
- premature ejaculation 5
- premenstrual dysphoric disorder (PMDD) 12
- alcohol dependence 9
- binge-eating disorder 14
- anorexia nervosa 7
- diabetic neuropathy 8
- panic disorder 10
- irritable bowel syndrome 13
Mechanism of action
Citalopram represents a racemic mixture of two enantiomers - molecules that have the same atomic framework but different spatial arrangements.
Citalopram is an antidepressant that selectively inhibits serotonin
reuptake thereby potentiating serotonin neurotransmission. It
is the most selective serotonin reuptake inhibitor currently available
2. It has only minimal effects on norepinephrine and dopamine
neurotransmission with 3,400 times more serotonin (5-HT) activity
Citalopram also has mild antagonist actions at H1 histamine receptors.
Reviews, Discussions & Forums
- 1. Feighner JP, Over K. Multicenter study of citalopram
in moderate-to-severe depression.
J Clin Psychiatry. 1999 Dec;60(12):824-30. PubMed
- 2. 1. Milne RJ, Goa KL. Citalopram: its pharmacodynamic
and pharmacokinetic properties, and therapeutic potential in
depressive illness. Drugs. Mar 1991;41(3):450-477.
- 3. Lane RM. Pharmacokinetic drug interaction potential of
SSRIs. Int Clin Psychopharmacol.
1996 Dec;11 Suppl 5:31-61.
- 4. Arias F, Padi'n JJ, Rivas MT, Sa'nchez A. Sexual dysfunctions
induced by serotonin reuptake inhibitors. Aten Primaria. 2000
- 5. Safarinejad MR, Hosseini SY. Safety and efficacy of citalopram
in the treatment of premature ejaculation: a double-blind placebo-controlled,
randomized study. Int J Impot Res. 2006 Mar-Apr;18(2):164-9.
- 6. Bouwer CD, Harvey BH. Phasic craving for carbohydrate observed
with citalopram. Int Clin Psychopharmacol. 1996 Dec;11(4):273-8.
- 7. 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.
- 8. Sindrup SH, Bjerre U, Dejgaard A, Brsen K, Aaes-Jrgensen
T, Gram LF. Citalopram
relieves the symptoms of diabetic neuropathy. Clin Pharmacol
Ther. 1992 Nov;52(5):547-52.
- 9. 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
- 10. Leinonen E, Lepola U, Koponen H, Turtonen J, Wade A, Lehto
H. Citalopram controls phobic symptoms in patients with panic
disorder. J Psychiatry Neurosci.
2000 Jan;25(1):24-32. PubMed
- 11. 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.
- 12. Pearlstein T. Selective serotonin reuptake inhibitors
for premenstrual dysphoric disorder: the emerging gold standard?
- 13. Tack J, Broekaert D, Fischler B, Oudenhove LV, Gevers
AM, Janssens J. A controlled crossover study of the citalopram in irritable bowel syndrome.
Gut. 2006 Aug;55(8):1095-103.
- 14. McElroy SL, Hudson JI, Malhotra S, Welge JA, Nelson EB,
Keck PE. Citalopram in the treatment of binge-eating disorder. J Clin Psychiatry. 2003 Jul;64(7):807-13.
- 15. Izumi T, Inoue T, Kitaichi Y, Nakagawa S, Koyama T. Target
brain sites of the anxiolytic effect of citalopram. Eur J Pharmacol. 2006 Mar 18;534(1-3):129-32.
- 16. Tack J, Broekaert D, Corsetti M, Fischler B, Janssens J. Influence of acute serotonin reuptake inhibition on colonic sensorimotor function in man. Aliment Pharmacol Ther. 2006 Jan 15;23(2):265-74. PubMed
Written by HealthyStock.net, October 2009.
Last updated: May, 2015
- Citalopram was developed by the Danish pharmaceutical firm H.
Lundbeck A/S and is marketed in the U.S. by Forest Laboratories
under trade name Celexa.
- Citalopram is a highly selective inhibitor of serotonin reuptake
with a negligible affinity for other neurotransmitter receptors.
- Celexa appears to be safe to use on a long-term basis and may
cause less withdrawal than other antidepressants when use is stopped.
- Of all of the SSRIs Citalopram has the most favorable drug interactions profile because it has the least effect on the cytochrome P450 enzymes.