Peringatan Keamanan

Symptoms of overdose may include CNS effects (dizziness, convulsions, coma, somnolence), gastrointestinal distress (nausea, vomiting), and/or cardiac abnormalities (hypotension, tachycardia, ECG changes).L8513,L8516,L8522 There is no specific antidote for escitalopram overdose. Management of overdose should focus on monitoring for cardiac abnormalities and changes to vital signs as well as treatment with supportive measures as indicated. As escitalopram is highly distributed into tissue following oral administration, forced diuresis, dialysis, and other methods of extracting drug from plasma are unlikely to be beneficial.

Escitalopram

DB01175

small molecule approved

Deskripsi

Escitalopram is a selective serotonin re-uptake inhibitor (SSRI) and the S-enantiomer of racemic citalopram.A185420 It is used to restore serotonergic function in the treatment of depression and anxiety.L8513,L8516,L8522 Escitalopram is approximately 150 times more potent than citalopram’s R-enantiomer and is responsible for the vast majority of citalopram’s clinical activity, with some evidence suggesting that the R-enantiomer of racemic citalopram actively dampens the activity of escitalopram rather than existing simply as an inactive enantiomer.A39738,A185819 Amongst SSRIs, escitalopram exerts the highest degree of selectivity for the serotonin transporter (SERT) relative to other off-targets which may explain its lower rates of adverse effects as compared to other agents in this class.A185726 Escitalopram also differentiates itself from other SSRIs via allosteric action on its target - this may be the mechanism responsible for its observed superior efficacy and faster onset compared to other SSRIs.A185825,A185726,A185822

Struktur Molekul 2D

Berat 324.3919
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of escitalopram is 27-32 hours, though this is increased by approximately 50% in the elderly and doubled in patients with reduced hepatic function.[A185420,L8513,L8516,L8522] The elimination half-life of escitalopram's primary metabolite, S-desmethylcitalopram, is approximately 54 hours at steady state.[A39738]
Volume Distribusi Escitalopram appears to distribute extensively into tissues, with an apparent volume of distribution of approximately 12-26 L/kg.[L8513,L8516,L8522]
Klirens (Clearance) The oral plasma clearance of escitalopram is 600 mL/min, of which approximately 7% is due to renal clearance.[L8513,L8516,L8522]

Absorpsi

Absorption of escitalopram following oral administration is expected to be almost complete, with an estimated absolute bioavailability of approximately 80%. Tmax occurs after about 4-5 hours.L8513,L8516,L8522 Cmax and AUC appear to follow dose proportionality - at steady state, patients receiving 10mg of escitalopram daily had a Cmax of 21 ng/mL and a 24h AUC of approximately 360 ng*h/mL, while patients receiving 30mg daily had a roughly 3-fold increase in both Cmax and 24h AUC, comparatively.A39738

Metabolisme

The metabolism of escitalopram is mainly hepatic, mediated primarily by CYP2C19 and CYP3A4 and, to a lesser extent, CYP2D6. Oxidative N-demethylation by the CYP enzyme system results in S-desmethylcitalopram (S-DCT) and S-didesmethylcitalopram (S-DDCT) - these metabolites do not contribute to the pharmacologic activity of escitalopram, and exist in the plasma in small quantities relative to the parent compound (28-31% and <5%, respectively).L8513,L8516,L8522 There is also some evidence that escitalopram is metabolized to a propionic acid metabolite by monoamine oxidase A and B in the brain, and that these enzymes constitute the major route of escitalopram metabolism in the brain.A39738

Rute Eliminasi

After oral administration of escitalopram, approximately 8% of the total dose is eliminated in the urine as unchanged escitalopram and 10% is eliminated in the urine as S-desmethylcitalopram.L8513,L8516,L8522 The apparent hepatic clearance of escitalopram amounts to approximately 90% of the total dose.L8516

Farmakogenomik

3 Varian
CYP2C19 (rs4244285)

The presence of this polymorphism in CYP2C19 is associated with poor metabolism of escitalopram.

CYP2C19 (rs4986893)

The presence of this polymorphism in CYP2C19 is associated with reduced or poor metabolism of escitalopram.

SLC6A4 (rs25531)

The presence of this polymorphism in SLC6A4 may potentially be associated with increased risk of adverse events from escitalopram.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. The combined use of alcohol with psychotropic medications should be avoided.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1718 Data
Cyproheptadine The therapeutic efficacy of Escitalopram can be decreased when used in combination with Cyproheptadine.
Desmopressin The risk or severity of hyponatremia can be increased when Escitalopram is combined with Desmopressin.
Ioflupane I-123 Escitalopram may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Escitalopram.
Buprenorphine Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Hydrocodone Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Escitalopram can be increased when used in combination with Magnesium sulfate.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Orphenadrine Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Pramipexole Escitalopram may increase the sedative activities of Pramipexole.
Ropinirole Escitalopram may increase the sedative activities of Ropinirole.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Escitalopram.
Sodium oxybate Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Thalidomide Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Dabrafenib The serum concentration of Escitalopram can be decreased when it is combined with Dabrafenib.
Aclidinium The risk or severity of adverse effects can be increased when Escitalopram is combined with Aclidinium.
Mirabegron The risk or severity of urinary retention can be increased when Escitalopram is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Escitalopram is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Escitalopram.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Escitalopram.
Tiotropium The risk or severity of adverse effects can be increased when Escitalopram is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Escitalopram is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Escitalopram is combined with Umeclidinium.
Luliconazole The serum concentration of Escitalopram can be increased when it is combined with Luliconazole.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Escitalopram.
Esomeprazole The serum concentration of Escitalopram can be increased when it is combined with Esomeprazole.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Escitalopram.
Glycopyrronium The risk or severity of adverse effects can be increased when Escitalopram is combined with Glycopyrronium.
Boceprevir The serum concentration of Escitalopram can be decreased when it is combined with Boceprevir.
Simeprevir The serum concentration of Simeprevir can be decreased when it is combined with Escitalopram.
Telaprevir The serum concentration of Escitalopram can be decreased when it is combined with Telaprevir.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Escitalopram.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Escitalopram is combined with Botulinum toxin type A.
Glucagon Escitalopram may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Escitalopram may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Escitalopram is combined with Botulinum toxin type B.
Mirtazapine The risk or severity of serotonin syndrome can be increased when Mirtazapine is combined with Escitalopram.
Eluxadoline The risk or severity of constipation can be increased when Escitalopram is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Escitalopram is combined with Ramosetron.
Diamorphine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Escitalopram.
Desomorphine The risk or severity of serotonin syndrome can be increased when Desomorphine is combined with Escitalopram.
Carfentanil, C-11 The risk or severity of serotonin syndrome can be increased when Carfentanil, C-11 is combined with Escitalopram.
Iobenguane Escitalopram may decrease effectiveness of Iobenguane as a diagnostic agent.
Methyclothiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Methyclothiazide.
Chlorthalidone The risk or severity of hyponatremia can be increased when Escitalopram is combined with Chlorthalidone.
Bendroflumethiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Bendroflumethiazide.
Metolazone The risk or severity of hyponatremia can be increased when Escitalopram is combined with Metolazone.
Benzthiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Benzthiazide.
Hydroflumethiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Hydroflumethiazide.
Chlorothiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Chlorothiazide.
Trichlormethiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Trichlormethiazide.
Polythiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Polythiazide.
Quinethazone The risk or severity of hyponatremia can be increased when Escitalopram is combined with Quinethazone.
Cyclopenthiazide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Cyclopenthiazide.
Epitizide The risk or severity of hyponatremia can be increased when Escitalopram is combined with Epitizide.
Ethanol Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Escitalopram may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Escitalopram.
Ethchlorvynol The risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Escitalopram.
Succinylcholine The risk or severity of adverse effects can be increased when Succinylcholine is combined with Escitalopram.
Enflurane The risk or severity of adverse effects can be increased when Enflurane is combined with Escitalopram.
Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Escitalopram.
Butalbital The risk or severity of adverse effects can be increased when Butalbital is combined with Escitalopram.
Etomidate The risk or severity of adverse effects can be increased when Etomidate is combined with Escitalopram.
Talbutal The risk or severity of adverse effects can be increased when Talbutal is combined with Escitalopram.
Tolcapone The risk or severity of adverse effects can be increased when Tolcapone is combined with Escitalopram.
Thiethylperazine The risk or severity of adverse effects can be increased when Thiethylperazine is combined with Escitalopram.
Metocurine iodide The risk or severity of adverse effects can be increased when Metocurine iodide is combined with Escitalopram.
Secobarbital The risk or severity of adverse effects can be increased when Secobarbital is combined with Escitalopram.
Methocarbamol The risk or severity of adverse effects can be increased when Methocarbamol is combined with Escitalopram.
Metharbital The risk or severity of adverse effects can be increased when Metharbital is combined with Escitalopram.
Methohexital The risk or severity of adverse effects can be increased when Methohexital is combined with Escitalopram.
Entacapone The risk or severity of adverse effects can be increased when Entacapone is combined with Escitalopram.
Cisatracurium The risk or severity of adverse effects can be increased when Cisatracurium is combined with Escitalopram.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Escitalopram.
Thiopental The risk or severity of adverse effects can be increased when Thiopental is combined with Escitalopram.
Paramethadione The risk or severity of adverse effects can be increased when Paramethadione is combined with Escitalopram.
Dexmedetomidine The risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Escitalopram.
Dyclonine The risk or severity of adverse effects can be increased when Dyclonine is combined with Escitalopram.
Trimethobenzamide The risk or severity of adverse effects can be increased when Trimethobenzamide is combined with Escitalopram.
Rocuronium The risk or severity of adverse effects can be increased when Rocuronium is combined with Escitalopram.
Atracurium besylate The risk or severity of adverse effects can be increased when Atracurium besylate is combined with Escitalopram.
Riluzole The risk or severity of adverse effects can be increased when Riluzole is combined with Escitalopram.
Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Escitalopram.
Ethotoin The risk or severity of adverse effects can be increased when Ethotoin is combined with Escitalopram.
Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Escitalopram.
Propiomazine The risk or severity of adverse effects can be increased when Propiomazine is combined with Escitalopram.
Acetazolamide The risk or severity of adverse effects can be increased when Acetazolamide is combined with Escitalopram.
Phensuximide The risk or severity of adverse effects can be increased when Phensuximide is combined with Escitalopram.
Methylphenobarbital The risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Escitalopram.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Muscarinic acetylcholine receptor M1 CHRM1
Histamine H1 receptor HRH1
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2A HTR2A
Alpha-1 adrenergic receptors ADRA1A
5-hydroxytryptamine receptor 2C HTR2C
Alpha-2 adrenergic receptors ADRA2A
D(2) dopamine receptor DRD2
Sodium-dependent noradrenaline transporter SLC6A2
Sodium-dependent dopamine transporter SLC6A3

Referensi & Sumber

Synthesis reference: Robert Dancer, "Escitalopram hydrobromide and a method for the preparation thereof." U.S. Patent US20040167209, issued August 26, 2004.
Artikel (PubMed)
  • PMID: 15812262
    Moore N, Verdoux H, Fantino B: Prospective, multicentre, randomized, double-blind study of the efficacy of escitalopram versus citalopram in outpatient treatment of major depressive disorder. Int Clin Psychopharmacol. 2005 May;20(3):131-7.
  • PMID: 16834832
    Boulenger JP, Huusom AK, Florea I, Baekdal T, Sarchiapone M: A comparative study of the efficacy of long-term treatment with escitalopram and paroxetine in severely depressed patients. Curr Med Res Opin. 2006 Jul;22(7):1331-41.
  • PMID: 15367045
    Bielski RJ, Ventura D, Chang CC: A double-blind comparison of escitalopram and venlafaxine extended release in the treatment of major depressive disorder. J Clin Psychiatry. 2004 Sep;65(9):1190-6.
  • PMID: 17288694
    Nierenberg AA, Greist JH, Mallinckrodt CH, Prakash A, Sambunaris A, Tollefson GD, Wohlreich MM: Duloxetine versus escitalopram and placebo in the treatment of patients with major depressive disorder: onset of antidepressant action, a non-inferiority study. Curr Med Res Opin. 2007 Feb;23(2):401-16.
  • PMID: 15695064
    Chen F, Larsen MB, Sanchez C, Wiborg O: The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors. Eur Neuropsychopharmacol. 2005 Mar;15(2):193-8.
  • PMID: 17375980
    Rao N: The clinical pharmacokinetics of escitalopram. Clin Pharmacokinet. 2007;46(4):281-90. doi: 10.2165/00003088-200746040-00002.
  • PMID: 11454728
    von Moltke 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 Metab Dispos. 2001 Aug;29(8):1102-9.
  • PMID: 19773541
    Rudberg I, Reubsaet JL, Hermann M, Refsum H, Molden E: Identification of a novel CYP2C19-mediated metabolic pathway of S-citalopram in vitro. Drug Metab Dispos. 2009 Dec;37(12):2340-8. doi: 10.1124/dmd.109.029355. Epub 2009 Sep 22.
Menampilkan 8 dari 17 artikel.

Contoh Produk & Brand

Produk: 511 • International brands: 2
Produk
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  • Act Escitalopram ODT
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  • Ag-escitalopram
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International Brands
  • Cipralex
  • Esertia

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