Abstract:
:Escitalopram is the (S)-enantiomer of the racemic selective serotonin reuptake inhibitor antidepressant citalopram. Clinical studies have shown that escitalopram is effective and well tolerated in the treatment of depression and anxiety disorders. Following oral administration, escitalopram is rapidly absorbed and reaches maximum plasma concentrations in approximately 3-4 hours after either single- or multiple-dose administration. The absorption of escitalopram is not affected by food. The elimination half-life of escitalopram is about 27-33 hours and is consistent with once-daily administration. Steady-state concentrations are achieved within 7-10 days of administration. Escitalopram has low protein binding (56%) and is not likely to cause interactions with highly protein-bound drugs. It is widely distributed throughout tissues, with an apparent volume of distribution during the terminal phase after oral administration (V(z)/F) of about 1100L. Unmetabolised escitalopram is the major compound in plasma. S-demethylcitalopram (S-DCT), the principal metabolite, is present at approximately one-third the level of escitalopram; however, S-DCT is a weak inhibitor of serotonin reuptake and does not contribute appreciably to the therapeutic activity of escitalopram. The didemethyl metabolite of escitalopram (S-DDCT) is typically present at or below quantifiable concentrations. Escitalopram and S-DCT exhibit linear and dose-proportional pharmacokinetics following single or multiple doses in the 10-30 mg/day dose range. Adolescents, elderly individuals and patients with hepatic impairment do not have clinically relevant differences in pharmacokinetics compared with healthy young adults, implying that adjustment of the dosage is not necessary in these patient groups. Escitalopram is metabolised by the cytochrome P450 (CYP) isoenzymes CYP2C19, CYP2D6 and CYP3A4. However, ritonavir, a potent inhibitor of CYP3A4, does not affect the pharmacokinetics of escitalopram. Coadministration of escitalopram 20mg following steady-state administration of cimetidine or omeprazole led to a 72% and 51% increase, respectively, in escitalopram exposure compared with administration alone. These changes were not considered clinically relevant. In vitro studies have shown that escitalopram has negligible inhibitory effects on CYP isoenzymes and P-glycoprotein, suggesting that escitalopram is unlikely to cause clinically significant drug-drug interactions. The favourable pharmacokinetic profile of escitalopram suggests clinical utility in a broad range of patients.
journal_name
Clin Pharmacokinetjournal_title
Clinical pharmacokineticsauthors
Rao Ndoi
10.2165/00003088-200746040-00002subject
Has Abstractpub_date
2007-01-01 00:00:00pages
281-90issue
4eissn
0312-5963issn
1179-1926pii
4642journal_volume
46pub_type
杂志文章,评审abstract:OBJECTIVE:To determine the multiple dose pharmacokinetics of a new extended release (ER) capsule formulation of tolterodine, compared with the existing immediate release (IR) tablet, in healthy volunteers. DESIGN:Nonblind, randomised, 2-way crossover trial. PARTICIPANTS:19 healthy volunteers (7 females, 12 males), me...
journal_title:Clinical pharmacokinetics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003088-200140030-00006
更新日期:2001-01-01 00:00:00
abstract::In the treatment of patients with Parkinson's disease, apomorphine has an established place as a back-up therapy if other antiparkinsonian drugs, such as levodopa and oral dopamine agonists, have not controlled the existing response fluctuations. Apomorphine is a synthetic derivative of morphine, with a totally distin...
journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-199937030-00004
更新日期:1999-09-01 00:00:00
abstract:OBJECTIVE:To investigate the effect of concomitant administration of dairy products on the pharmacokinetics and tolerability of moxifloxacin. DESIGN:This was a single-centre, randomised, controlled, nonblinded, 2-way crossover study in healthy volunteers. PARTICIPANTS:12 healthy men (aged 25 to 46 years) were enrolle...
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pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003088-200140001-00005
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pub_type: 杂志文章,评审
doi:10.1007/s40262-017-0523-7
更新日期:2017-09-01 00:00:00
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doi:10.2165/00003088-200140040-00001
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pub_type: 临床试验,杂志文章
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
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更新日期:1996-03-01 00:00:00
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pub_type: 杂志文章
doi:10.2165/00003088-198510060-00004
更新日期:1985-11-01 00:00:00
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pub_type: 临床试验,杂志文章
doi:10.2165/00003088-200241070-00006
更新日期:2002-01-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,meta分析
doi:10.1007/s40262-016-0505-1
更新日期:2017-10-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-199835020-00003
更新日期:1998-08-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章
doi:10.2165/00003088-200140060-00006
更新日期:2001-01-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-199936030-00004
更新日期:1999-03-01 00:00:00
abstract:OBJECTIVE:To evaluate the effect of cilostazol administration on warfarin pharmacokinetics and pharmacodynamics following a single 25 mg dose of warfarin. DESIGN:A randomised double-blind 2-period crossover with healthy volunteers receiving either 100 mg cilostazol twice daily for 13 days or matching placebo twice dai...
journal_title:Clinical pharmacokinetics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003088-199937002-00009
更新日期:1999-01-01 00:00:00
abstract::Calcineurin inhibitors, the primary immunosuppressive therapy used to prevent alloreactivity of transplanted organs, have a narrow therapeutic index. Currently, treatment is individualized based on clinical assessment of the risk of rejection or toxicity guided by trough concentration monitoring. Advances in immune mo...
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pub_type: 杂志文章,评审
doi:10.1007/s40262-020-00923-w
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pub_type: 杂志文章,评审
doi:10.2165/00003088-199120060-00003
更新日期:1991-06-01 00:00:00
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pub_type: 杂志文章,随机对照试验
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pub_type: 杂志文章,多中心研究
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
doi:10.2165/00003088-199732040-00005
更新日期:1997-04-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2000-08-01 00:00:00
abstract::The pharmacokinetics and antihypertensive effects of felodipine, a new dihydropyridine calcium channel blocker, were studied in elderly hypertensive patients, 67 to 79 years of age and in young healthy subjects, 20 to 34 years of age following oral administration of 5 mg twice daily to steady-state. A single intraveno...
journal_title:Clinical pharmacokinetics
pub_type: 杂志文章
doi:10.2165/00003088-198814060-00004
更新日期:1988-06-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2004-01-01 00:00:00
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更新日期:2018-07-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
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更新日期:1984-01-01 00:00:00
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pub_type: 杂志文章,多中心研究,随机对照试验
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更新日期:2015-09-01 00:00:00
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journal_title:Clinical pharmacokinetics
pub_type: 杂志文章,评审
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更新日期:1990-09-01 00:00:00
abstract::Telithromycin is the first ketolide, which is a new class of antibacterial agents related to the macrolides that have structural modifications permitting dual binding to bacterial ribosomal RNA so that activity is retained against Streptococcus pneumoniae with macrolide-lincosamide-streptogramin(B) resistance. Clinica...
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更新日期:2005-01-01 00:00:00
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doi:10.1007/s40262-012-0009-6
更新日期:2012-12-01 00:00:00