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Celexa (Citalopram) Facts
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Basic information
- Generic name: Citalopram hydrobromide
- Brand/Trade names: Celexa
- Dosages: 10 mg, 20 mg, 40 mg tablets
- Pharmacologic category: Selective serotonin
reuptake inhibitor
- FDA approved: July 17, 1998
- Manufacturer: Forest Pharmaceuticals, Inc.
- Habit forming? No
- Pregnancy risk factor: C
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Medical uses
Celexa (Citalopram hydrobromide) is in a class of drugs called
selective serotonin reuptake inhibitors. This medication 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 disorders
and panic disorder. It has the potential to effectively treat
anxiety disorders 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
17.
Nausea is the most common early side effect, however it is usually
transient. Dosage reduction to 10 mg per day may alleviate early
nausea.
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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: Citalopram is 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.
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Benefits
- less risk of drug interactions than with some other antidepressants
3
- probably safe to use on a long-term basis
- cause 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
- has a moderate analgesic effect 16
- elicit relaxation of intestinal smooth muscle 18
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Concerns
- craving for carbohydrate [6]
- weight gain
- sexual side effects
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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]
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Mechanism of action
Citalopram is an antidepressant that selectively inhibits serotonin
reuptake thereby potentiating serotonin neurotransmission. Citalopram
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.
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Celexa Discussions Boards & Forums
- Celexa, Citalopram discussion: http://www.depressionforums.org/forums/index.php?showforum=55
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References
- 1. U.S. Food and Drug Administration. Celexa (Citalopram)
U.S. Prescribing Information. Available at (PDF format): Prescribing
Information
- 2. 1. Milne RJ, Goa KL. Citalopram. A review of 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
selective serotonin reuptake inhibitors. Int Clin Psychopharmacol.
1996 Dec;11 Suppl 5:31-61. PubMed
- 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. PubMed
- 5. 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
- 6. Bouwer CD, Harvey BH. Phasic craving for carbohydrate observed
with citalopram. Int Clin Psychopharmacol. 1996 Dec;11(4):273-8.
PubMed
- 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-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
- 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: randomized controlled trial. 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. PubMed
- 12. Pearlstein T. Selective serotonin reuptake inhibitors
for premenstrual dysphoric disorder: the emerging gold standard?
Drugs. 2002;62(13):1869-85. PubMed
- 13. 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
- 14. 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
- 15. Izumi T, Inoue T, Kitaichi Y, Nakagawa S, Koyama T. Target
brain sites of the anxiolytic effect of citalopram, a selective
serotonin reuptake inhibitor. Eur J Pharmacol. 2006 Mar 18;534(1-3):129-32.
Epub 2006 Feb 21. PubMed
- 16. 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
- 17. Feighner JP, Over? K. Multicenter, placebo-controlled,
fixed-dose study of citalopram in moderate-to-severe depression.
J Clin Psychiatry. 1999 Dec;60(12):824-30. PubMed
- 18. Pacher P, Ungvari Z, Kecskeme'ti V, Friedmann T, Furst
S. Serotonin reuptake inhibitors fluoxetine and citalopram relax
intestinal smooth muscle. Can J Physiol Pharmacol. 2001 Jul;79(7):580-4.
PubMed
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Interesting Celexa facts
- 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 little or no affinity for other neurotransmitter receptors.
- Celexa may also cause less drug interactions than some other antidepressants.
- 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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