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Celexa (Citalopram)


  • Generic name: Citalopram hydrobromide
  • Trade name: Celexa
  • Pharmacologic category: Selective serotonin reuptake inhibitor
  • FDA approved: July 17, 1998
  • Manufacturer: Forest Pharmaceuticals, Inc.
  • Habit forming? No
  • Pregnancy risk factor: C
Medical uses

Celexa (Citalopram hydrobromide) is in a class of drugs called selective serotonin reuptake inhibitors. It is indicated for the treatment of depression. Citalopram has also been used to treat certain eating disorders (e.g., anorexia nervosa, bulimia). Citalopram is effective in the treatment of other depressive and panic disorders. It has the potential to effectively treat anxiety and substance use disorders.

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 1.

Nausea is the most common early side effect, however it is usually transient.

Pharmacological characteristics
  • 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.
  • Elimination half-life: 37 hours (range 30-42 hours). The half-life of demethylcitalopram being 2 days and 4 days for didemethylcitalopram.
  • 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.
Benefits
  • less risk of drug interactions than with some other antidepressants 3
  • probably safe to use on a long-term basis
  • causes less withdrawal symptoms than other SSRIs
  • absorption is not affected by food
  • fewer side effects than with other SSRIs
  • low incidence of activating side effects
  • less likely than other antidepressants to cause sexual dysfunction 4
  • anxiolytic effects 15
  • suitable alternative for fluoxetine intolerant individuals
  • elicit relaxation of intestinal smooth muscle 16
Concerns
  • craving for carbohydrate 6
  • weight gain
  • sexual side effects
Unlabeled uses
  • 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 than norepinephrine.

Citalopram also has mild antagonist actions at H1 histamine receptors.

Reviews, Discussions & Forums
References
  • 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 Oct 15;26(6):389-94.
  • 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. PubMed
  • 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): 269275. 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. 2002 Sep;7(9):655-7.
  • 12. Pearlstein T. Selective serotonin reuptake inhibitors for premenstrual dysphoric disorder: the emerging gold standard? Drugs. 2002;62(13):1869-85.
  • 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. PubMed
  • 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

Last updated: December 2013

Interesting facts

celexa


Citalopram
  • 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 has a chemical structure unrelated to that of other SSRIs. It 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.
  • Citalopram has been found to significantly reduce the symptoms of diabetic neuropathy and premature ejaculation.

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