Psychiatr. pro Praxi, 2003; 5: 230-234

Escitalopram - S-enantiomer citalopramu

prof. MUDr. Jaroslav Bouček CSc
Psychiatrická klinika FN a LF UP, Olomouc

Published: December 31, 2003  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Bouček J. Escitalopram - S-enantiomer citalopramu. Psychiatr. praxi. 2003;4(5):230-234.

Selektivní inhibitory zpětného vychytávání serotoninu (SSRI) široce v posledních 10 letech nahrazují starší tricyklické typy antidepresiv (AD) a spojením dobré účinnosti a příznivým profilem nežádoucích účinků se stávají léky první volby v léčbě depresí a anxiózních stavů (8, 12, 20, 31).

Citalopram je směsí R- a S-enantiomérů v poměru 50:50, přičemž S-enantiomér je aktivní látkou odpovědnou za vyvolání antidepresivního účinku. Escitalopram je více jak 2× potentnějším inhibitorem zpětného vychytávání serotoninu a byl proto uveden na trh jako nové AD ze skupiny SSRI pod obchodními názvy Cipralex firmou Lundbeck a Lexapro firmou Forest Laboratories.

U nás byl registrován 6. 11. 2002 jako escitalopram oxalát - potahované tablety 5, 10 a 20 mg.

Chemický název: (S)-1-[3-(dimetylamino) propyl]-1-(4-fluorofenyl)-1,3-dihydroisobenzofuron-5-karbonitril.

Download citation

References

  1. Baumann P, Larsen C. The pharmacokinetics of citalopram. Rev Contemp Pharmacotherapy 1995; 6: 287-295.
  2. Bergqvist PBF, Sánchez C. Escitalopram mediates the pharmacological activity of citalopram: in vivo studies. Nordic J Psych 2001; 55: 88-89.
  3. Burke WJ, Gergel I, Bose A. Fixed-dose trial of the single isomer SSRI escitalopram in depressed outpatients. J Clin Psychiatry. 2002 Apr; 63(4): 331-336. Go to original source... Go to PubMed...
  4. Davidson J, Bose A, Su G. Escitalopram in the treatment of generalized anxiety disorder. Int J Neuropsychopharmacol 2002; 5 (Suppl 1): 214.
  5. Davidson J, Bose A, Zheng H. Escitalopram in the treatment of generalized anxiety disorder: A double-blind, placebo controlled, flexible dose study. Poster presented at APA Annual Meeting, San Francisco, 2003. Go to original source...
  6. Drewes P, Thijssen I, Mengel H. A single dose, crossover pharmacokinetic study comparing racemic citalopram (40 mg) with the S-enantiomer of citalopram (escitalopram 20 mg) in healthy male volunteers. NCDEU Annual Meeting, Phoenix, Abstracts 2001: 91.
  7. Goodman WK, Bose A, Wang Q. Escitalopram 10 mg/day is effective in the treatment of generalized anxiety disorder. Poster presented at APA Annual Meeting, San Francisco, 2003.
  8. Gorman JM, Kent JM. SSRIs and SMRIs: broad spectrum of efficacy beyond major depression. J Clin Psychiatry. 1999; 60 (Suppl 4): 33-38; discussion 39.
  9. Gorman JM, Korotzer A, Su G. Efficacy comparison of escitalopram and citalopram in the treatment of major depressive disorder: Pooled analysis of placebo-controlled trials. CNS Spectrums 2002; 7 (Suppl.1): 40-44. Go to original source... Go to PubMed...
  10. Hakkarainen H, Reines EH. Escitalopram and citalopram: Safety comparison (Abstract). World J Biol Psychiatry 2001; 2 (Suppl.): 337.
  11. Hyttel J, Bogeso KP, Perregaard J, Sanchez C. The pharmacological effect of citalopram residues in the (S)-(+)-enantiomer. J Neural Transm Gen Sect. 1992; 88 (2): 157-160. Go to original source... Go to PubMed...
  12. Isaac M. Where are we going with SSRIs? Eur Neuropsychopharmacol. 1999; 9 (Suppl 3): 101-106. Go to original source... Go to PubMed...
  13. Joffe P, Larsen FS, Pedersen V, Ring-Larsen H, Aaes-Jorgensen T, Sidhu J. Single-dose pharmacokinetics of citalopram in patients with moderate renal insufficiency or hepatic cirrhosis compared with healthy subjects. Eur J Clin Pharmacol. 1998; 54 (3): 237-242. Go to original source... Go to PubMed...
  14. Kasper S, Loft H, Nil R. Escitalopram is efficacious and well tolerated in the treatment of social anxiety disorder. Nordic J Psych 2002; 56: 108.
  15. Lepola UM, Loft H, Reines EH. Escitalopram (10-20 mg/day) is effective and well tolerated in a placebo-controlled study in depression in primary care. Int Clin Psychopharmacol. 2003; 18 (4): 211-217. Go to original source... Go to PubMed...
  16. Lydiard RB. Effects of escitalopram on anxiety symptoms in depression. Poster presented at APA Annual Meeting, New Orleans, 2001.
  17. Moltke von LL, Greenblatt DJ, Giancarlo GM, Granda BW, Harmatz JS, Shader RI. Escitalopram (S-citalopram) and its metabolites in vitro: Cytochromes mediating biotransformation, inhibitory effects, and comparison to R-citalopram. Drug Metabol Disp 2001; 29: 1102-1109.
  18. Montgomery SA, Dürr-Pal N, Loft H, Nil R. Escitalopram prevents relapse in patients suffering from social anxiety disorder. Poster presented at APA Annual Meeting, San Francisco, 2003.
  19. Montgomery SA, Huusom AKT, Bothmer. Escitalopram: effective and better tolerated than venlafaxine XR in the treatment of depression. Nord J Psych 2003; 57 (2): 103. Go to original source...
  20. Montgomery SA, Judge R. Treatment of depression with associated anxiety: comparisons of tricyclic antidepressants and selective serotonin reuptake inhibitors. Acta Psychiatr Scand Suppl. 2000; 403: 9-16. Go to original source... Go to PubMed...
  21. Montgomery SA, Lader M, Bürger V, Stender K, Nil R. Escitalopram and paroxetine in fixed doses for the treatment of social anxiety disorder. Poster presented at SCNP Annual Meeting, Juan-Les-Pines, 2003.
  22. Ninan TP, Ventura D, Wang J. Escitalopram is effective and well tolerated in the treatment of severe depression. Poster presented at APA Annual Meeting, San Francisco, 2003.
  23. Owens MJ, Knight DL, Nemeroff CB. Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine. Biol Psychiatry. 2001; 50 (5): 345-350. Go to original source... Go to PubMed...
  24. Pirker W, Asenbaum S, Kasper S, Walter H, Angelberger P, Koch G, Pozzera A, Deecke L, Podreka I, Brucke T. Beta-CIT SPECT demonstrates blockade of 5HT-uptake sites by citalopram in the human brain in vivo. J Neural Transm Gen Sect. 1995; 100 (3): 247-256. Go to original source... Go to PubMed...
  25. Pollack MH, Bose A, Zheng H. Efficacy and tolerability of citalopram in the treatment of anxiety disorders. Poster presented at ADAA, Toronto, 2003. Go to original source...
  26. Rapaport MH, Bose A, Zheng H, Korotzer A. Escitalopram prevents relapse of depressive episodes (Abstract). In J Neuropsychopharmacol 2002; 5 (Suppl.): 146. Go to original source...
  27. Reines EH, Andersen HF, Colonna L. Escitalopram versus Citalopram: Well tolerated and more efficacious in long-term treatment of moderately depressed patients. Poster presented at SCNP Annual Meeting, Juan-Les-Pines, 2003.
  28. Sanchez C, Bergqvist PB, Brennum LT, Gupta S, Hogg S, Larsen A, Wiborg O. Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities. Psychopharmacology (Berl). 2003; 167 (4): 353-362. Epub 2003 Apr 26. Go to original source... Go to PubMed...
  29. Stahl S, Gergel I, Li D. Escitalopram in the treatment of panic disorder. Int J Neuropsychopharmacol 2002; 5 (Suppl 1): 217.
  30. Švestka J. Escitalopram - selektivní stereoizomer citalopramu. Psychiatrie 2003; 1: 38-45.
  31. Van Ameringen M, Mancini C. Pharmacotherapy of social anxiety disorder at the turn of the millennium. Psychiatr Clin North Am. 2001; 24 (4): 783-803. Go to original source... Go to PubMed...
  32. Wade A, Lemming OM, Hedegaard KB. Escitalopram 10 mg/day is effective and well tolerated in a placebo-controlled study in depression in primary care. Int Clin Psychopharmacol 2002; 17: 95-102. Go to original source... Go to PubMed...
  33. Wade A. Escitalopram is safe and well tolerated in long-term treatment of depression (Abstract). Int J Neuropsychopharmacol 2002; 5 (Suppl.): 147.




Psychiatry for Practice

Madam, Sir,
please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

I declare:

  1. that I have met the above instruction
  2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited


No

Yes

If your statement is not true, please be aware
that brings the risk of danger to their health or the health of others.