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Escitalopram
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DRUG INFO Escitalopram
Drug Name:
Escitalopram
Indication: For the treatment of major depressive disorder and Generalized Anxiety Disorder (GAD).
Pharmacology: Escitalopram is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that escitalopram is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Escitalopram has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of escitalopram was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Escitalopram does not inhibit monoamine oxidase.
Mechanism Of Action: The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Escitalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.
Drug Category: Antidepressive Agents, Second-Generation; Serotonin Uptake Inhibitors; ATC:N06AB10
Brand Names/Synonyms: Escitalopram; Escitalopram Oxalate; Escitalopram [Inn]; Lexapro
Dosage Forms: TABLET
Absorption: The absolute bioavailability of citalopram is about 80% relative to an intravenous dose
Interactions:
DrugBank: Interactions for Escitalopram
Interactions for Escitalopram:
CNS Drugs - Given the primary CNS effects of escitalopram, caution should be used when it is taken in combination
with other centrally acting drugs.
Alcohol - Although LEXAPRO did not potentiate the cognitive and motor effects of alcohol in a clinical trial, as
with other psychotropic medications, the use of alcohol by patients taking LEXAPRO is not recommended. Monoamine
Oxidase Inhibitors (MAOIs) - See Contraindications and Warnings.
Drugs That Interfere With Hemostasis (NSAIDs, Aspirin, Warfarin, etc.)
Serotonin release by platelets plays an important role in hemostasis. Epidemiological studies of the case-control
and cohort design that have demonstrated an association between use of psychotropic drugs that interfere with
serotonin reuptake and the occurrence of upper gastrointestinal bleeding have also shown that concurrent use of an
NSAID or aspirin potentiated the risk of bleeding. Thus, patients should be cautioned about the use of such drugs
concurrently with LEXAPRO.
Cimetidine - In subjects who had received 21 days of 40 mg/day racemic citalopram, combined administration of 400
mg/day cimetidine for 8 days resulted in an increase in citalopram AUC and Cmax of 43% and 39%,
respectively. The clinical significance of these findings is unknown.
Digoxin - In subjects who had received 21 days of 40 mg/day racemic citalopram, combined administration of
citalopram and digoxin (single dose of 1 mg) did not significantly affect the pharmacokinetics of either citalopram
or digoxin.
Lithium - Coadministration of racemic citalopram (40 mg/day for 10 days) and lithium (30 mmol/day for 5 days) had
no significant effect on the pharmacokinetics of citalopram or lithium. Nevertheless, plasma lithium levels should be
monitored with appropriate adjustment to the lithium dose in accordance with standard clinical practice. Because
lithium may enhance the serotonergic effects of escitalopram, caution should be exercised when LEXAPRO and lithium
are coadministered.
Pimozide and Celexa - In a controlled study, a single dose of pimozide 2 mg co-administered with racemic
citalopram 40 mg given once daily for 11 days was associated with a mean increase in QTc values of approximately 10
msec compared to pimozide given alone. Racemic citalopram did not alter the mean AUC or Cmax of pimozide.
The mechanism of this pharmacodynamic interaction is not known.
Sumatriptan - There have been rare postmarketing reports describing patients with weakness, hyperreflexia, and
incoordination following the use of a selective serotonin reuptake inhibitor (SSRI) and sumatriptan. If concomitant
treatment with sumatriptan and an SSRI (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline, citalopram,
escitalopram) is clinically warranted, appropriate observation of the patient is advised.
Theophylline - Combined administration of racemic citalopram (40 mg/day for 21 days) and the CYP1A2 substrate
theophylline (single dose of 300 mg) did not affect the pharmacokinetics of theophylline. The effect of theophylline
on the pharmacokinetics of citalopram was not evaluated.
Warfarin - Administration of 40 mg/day racemic citalopram for 21 days did not affect the pharmacokinetics of
warfarin, a CYP3A4 substrate. Prothrombin time was increased by 5%, the clinical significance of which is
unknown.
Carbamazepine - Combined administration of racemic citalopram (40 mg/day for 14 days) and carbamazepine (titrated
to 400 mg/day for 35 days) did not significantly affect the pharmacokinetics of carbamazepine, a CYP3A4 substrate.
Although trough citalopram plasma levels were unaffected, given the enzyme-inducing properties of carbamazepine, the
possibility that carbamazepine might increase the clearance of escitalopram should be considered if the two drugs are
coadministered.
Triazolam - Combined administration of racemic citalopram (titrated to 40 mg/day for 28 days) and the CYP3A4
substrate triazolam (single dose of 0.25 mg) did not significantly affect the pharmacokinetics of either citalopram
or triazolam.
Ketoconazole - Combined administration of racemic citalopram (40 mg) and ketoconazole (200 mg) decreased the
Cmax and AUC of ketoconazole by 21% and 10%, respectively, and did not significantly affect the
pharmacokinetics of citalopram.
Ritonavir - Combined administration of a single dose of ritonavir (600 mg), both a CYP3A4 substrate and a potent
inhibitor of CYP3A4, and escitalopram (20 mg) did not affect the pharmacokinetics of either ritonavir or
escitalopram.
CYP3A4 and -2C19 Inhibitors - In vitro studies indicated that CYP3A4 and -2C19 are the primary enzymes
involved in the metabolism of escitalopram. However, coadministration of escitalopram (20 mg) and ritonavir (600 mg),
a potent inhibitor of CYP3A4, did not significantly affect the pharmacokinetics of escitalopram. Because escitalopram
is metabolized by multiple enzyme systems, inhibition of a single enzyme may not appreciably decrease escitalopram
clearance.
Drugs Metabolized by Cytochrome P4502D6 - In vitro studies did not reveal an inhibitory effect of
escitalopram on CYP2D6. In addition, steady state levels of racemic citalopram were not significantly different in
poor metabolizers and extensive CYP2D6 metabolizers after multiple-dose administration of citalopram, suggesting that
coadministration, with escitalopram, of a drug that inhibits CYP2D6, is unlikely to have clinically significant
effects on escitalopram metabolism. However, there are limited in vivo data suggesting a modest CYP2D6
inhibitory effect for escitalopram, i.e., coadministration of escitalopram (20 mg/day for 21 days) with the tricyclic
antidepressant desipramine (single dose of 50 mg), a substrate for CYP2D6, resulted in a 40% increase in
Cmax and a 100% increase in AUC of desipramine. The clinical significance of this finding is unknown.
Nevertheless, caution is indicated in the coadministration of escitalopram and drugs metabolized by CYP2D6.
Metoprolol - Administration of 20 mg/day LEXAPRO for 21 days in healthy volunteers resulted in a 50% increase in
Cmax and 82% increase in AUC of the beta-adrenergic blocker metoprolol (given in a single dose of 100 mg).
Increased metoprolol plasma levels have been associated with decreased cardioselectivity. Coadministration of LEXAPRO
and metoprolol had no clinically significant effects on blood pressure or heart rate.
Electroconvulsive Therapy (ECT) - There are no clinical studies of the combined use of ECT and escitalopram.
Concomitant Administration with Racemic Citalopram
Citalopram - Since escitalopram is the active isomer of racemic citalopram (Celexa), the two agents should not be
coadministered.
Chemical IUPAC Name: 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
Chemical Formula: C20H21FN2O
Half Life: 27-32 hours
Drug Type: Approved Drug
# Accession No: APRD00683
CAS Registry Number: 128196-01-0
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Escitalopram News (When available)
Forest Looks for a Spark 16 Jan 2006 TheStreet.com ...results. It has a big hit with Lexapro, a cousin of Celexa, but the latter's revenue has shriveled because of generic competition. ...
Forest Labs earnings expected lower Jan 12, 2006 MarketWatch The company also faces a threat to its other popular antidepressant, Lexapro from generic drugmaker Ivax. The companies will go ...
DrKW Reiterates Lundbeck At Add Jan 13, 2006 New Ratings Lundbeck's biggest problem is a court case against generic drug maker Ivax (IVX), which is challenging Lundbeck's patent on its popular antidepressant, Lexapro ...
Center files suit to stop faxes Jan 10, 2006 Akron Beacon Journal, ...did not have approval to ship faxes for its Lexapro drug to the Belden Village Pain and Wellness Center Inc., in violation of federal law, according to the suit ...
The antidepressants to watch in '06 Jan 4, 2006 CNN ...and Bear Sterns' Boris project that Cymbalta could reach $3 billion in annual sales by the end of the decade, bringing it neck in neck with competitor Lexapro. ...
Danish shares close lower, led by Danske Bank, Novo Nordisk ... Jan 3, 2006 Forbes ...extending its rise yesterday on reports that a US study has concluded that the use of anti-depressants -- including Lundbeck's Celexa and Lexapro -- does not ...
Eye On Stocks For Tuesday, Jan. 17 Jan 13, 2006 Forbes ..."While we remain concerned about risks to Lexapro growth in the mid-to-longer term, we feel that share repurchases & more licensing activity could limit ...
Morgan Stanley Cuts Lundbeck EPS Estimates Jan 13, 2006 New Ratings Cites likelihood of a fall in sales of antidepressant Lexapro as a result of changes to the US public health care system; a delay in the launch of bifeprunox ...
Antidepressants Don’t Increase Suicide Risk Jan 3, 2006 Christian Broadcasting Network, ...government-sponsored studies on some of the most popular antidepressants, such as Prozac, Zoloft, Celexa, and others, such as Paxil, Lexapro, Effexor, Remeron ...
New Study Suggests Cymbalta(R) Reduced Depression Symptoms at ... Dec 13, 2005 Market Wire (press release) IN -- (MARKET WIRE) -- 12/13/2005 -- Cymbalta® (duloxetine hydrochloride) reduced symptoms of depression at least as fast as Lexapro® (escitalopram) by the ...
New Study Suggests Cymbalta(R) Reduced Depression Symptoms At ... Dec 13, 2005 PR Newswire (press release), 13 /PRNewswire-FirstCall/ -- Cymbalta(R) (duloxetine hydrochloride) reduced symptoms of depression at least as fast as Lexapro(R) (escitalopram) by the end of ...
Suicide Drops With Antidepressant Use Jan 3, 2006 WebMD The 10 drugs identified by the FDA are Prozac, Paxil, Zoloft, Effexor, Celexa, Lexapro, Luvox, Remeron, Serzone, and Wellbutrin. ...
New Study Suggests Cymbalta Reduced Depression Symptoms At Least ... Dec 13, 2005 PharmaLive.com (press release), December 13, 2005 /PRNewswire-FirstCall/ -- Cymbalta(R) (duloxetine hydrochloride) reduced symptoms of depression at least as fast as Lexapro(R) (escitalopram ...
New Study Suggests Cymbalta (Duloxetine Hydrochloride) Reduced ... Dec 13, 2005 DG News INDIANAPOLIS, IN -- December 13, 2005 -- Cymbalta(R) (duloxetine hydrochloride) reduced symptoms of depression at least as fast as Lexapro(R) (escitalopram) by ...
Study Shows Cymbalta At Least as Fast as Leading Competitor in ... Dec 13, 2005 PharmaLive.com (press release), INDIANAPOLIS, December 13, 2005-- Cymbalta (duloxetine hydrochloride) reduced symptoms of depression at least as fast as Lexapro (escitalopram) by the end of ...
Forest Laboratories initiated with "hold" Dec 19, 2005 New Ratings ...mention that there is limited upside potential to the company’s share price, in view of the low product growth drivers and slowing sales growth of Lexapro. ...
Mylan Laboratories and Forest Laboratories Announce Nebivolol ... Jan 12, 2006 PharmaLive.com (press release), ...and Its Products Forest Laboratories' (www.frx.com) growing line of products includes: Lexapro(R) (escitalopram oxalate), an SSRI antidepressant indicated for ...
DemiDose(TM) Pill Splitter Allays Concern Over Dose Accuracy in ... Jan 11, 2006 PR Newswire (press release), Zocor - Levitra - Pravachol Mood Women's Health Antibiotic Allergy Migraine - Zyprexa - Fosamax - Levaquin - Zyrtec - Imitrex Oral - Lexapro - Prempro - Zoloft ...
Dover detective admits cocaine theft Jan 11, 2006 Dailyrecord.com, Avenue. Brennan had been prescribed the anti-depressant drug Lexapro and he had no alcohol in his system at the time of the crash. ...
LIFELONG HEALTH : Joyful Christmas season can also bring ... Dec 18, 2005 Arkansas Democrat-Gazette (subscription), ...medications. The most common are drugs called serotonin reuptake inhibitors (SSRIs), such as Prozac, Paxil, Zoloft, Lexapro and Celexa. ...
The Drug Dilemma Dec 28, 2005 ABC7Chicago.com, Antidepressants known as SSRIs pose the biggest problem. Those include drugs like Prozac, Paxil, Zoloft and Lexapro. Antihistamines ...
Danish shares higher midmorning, led by AP Moeller-Maersk ... Jan 3, 2006 Forbes ...rose 3.25 to 138, still lifted by news that a US study has concluded that the use of anti-depressants -- including Lundbeck's Celexa and Lexapro -- do not ...
Start of Medicare Part D going to be a bumpy ride Dec 30, 2005 San Mateo County Times, ...its list of accepted generic drugs a commonly prescribed "selective serotonin re-uptake inhibitor (SSRI)" called escitalopram , marketed under the name Lexapro ...
Seniors stranded without prescriptions Jan 5, 2006 BurlingtonFreePress.com, He gave her three days' worth of her Lipitor and Lexapro prescriptions, directions to call the state's toll-free help line immediately and a warning that she ...
David Lee Roth Jan 5, 2006 Audio Graphics, ...days. What we heard was an ego-deflated has-been rock star who came across like he was on a triple dose prescription of Lexapro. ...
Antidepressants (Eli Lilly & Co.'s Prozac) don't cause suicide ... Jan 3, 2006 EnjoyFrance.com, Pfizer Inc.'s Zoloft, GlaxoSmithKline Plc's Paxil, Solvay SA's Luvox, Biovail Corp.'s Wellbutrin, Forest Laboratories Inc.'s Celexa and Lexapro, Bristol-Myers ...
Herb Weisbaum: Some Encouraging News On Treating Depression Jan 5, 2006 KOMO, ...the risk of suicidal behavior was the lowest for patients taking 10 of the newest antidepressant, such as Prozac, Paxil, Zoloft, Celexa, Lexapro, and Wellbutrin ...
Subject: Jim Cramer's Action Alerts PLUS -- CEPH Jan 3, 2006 TheStreet.com (subscription), I went through a similar situation with Forest Labs (FRX:NYSE) in Celexa and Lexapro, and believe that Cephalon will be able to further protect its sleeping ...
Forest Laboratories, Inc. and Cypress Bioscience, Inc. to Commence ... Jan 5, 2006 Finanzen.net, Forest Laboratories' growing line of products includes: Lexapro(R) (escitalopram oxalate), an SSRI antidepressant indicated for the initial and maintenance ...
On January 30, He Nearly Killed Himself. On April 16, He Did. A 17 ... Jan 3, 2006 Village Voice, The poison had damaged his kidneys, so he could no longer take Depakote. Instead, a doctor gave him Lexapro, an antidepressant. ...
New Medicare prescription program brings higher co-pays, confusing ... Dec 28, 2005 San Jose Mercury News, He'll receive a larger-than-usual supply of Buspar, Lexapro and Seroquel, powerful psychiatric drugs that keep his schizophrenia and bipolar disorder in check. ...
Danish shares close lower, led by Danske Bank; Danisco higher ... Dec 13, 2005 Forbes Peer Eli Lilly said that, in a head-to-head study between its Cymbalta depression treatment and Lundbeck's Lexapro, Cymbalta showed just as fast a reduction in ...
Christmas Retrospective: Hit gifts in the Summers domicile Dec 26, 2005 Blogging Baby, It's pretty fun, but I'm currently weaning myself off Lexapro and the spinning and strobe lights are a little disturbing in my fragile state. ...
Drug stocks surge in mixed Europe Dec 19, 2005 Investor's Business Daily (subscription) 1.6%. Danish drugmaker H. Lundbeck (HLUKF), which is involved in patent dispute over Lexapro, rose 1.2% in Copenhagen. "For many ...
TOP 10: A Look Back at 2005 Dec 27, 2005 Phoenixville News, He said he was taking antidepressants Lexapro and Elavil, and admitted to Michaels that he has a dependency on OxyContin, a prescription painkiller. ...
Life's balance Jets coach Potter is battling depression Dec 15, 2005 Kansas.com, ...to him, ready to accept that he can't control the serotonin levels in his blood, ready to realize that 11 million others were taking the same Lexapro pills he ...
Judge dismisses suit filed against Conseco by 2 former directors Dec 14, 2005 Indianapolis Star, ...eight-week study of 684 patients found 48.7 percent responded to Cymbalta, compared with 45.3 percent of patients taking Forest Laboratories' Lexapro and 36.9 ...
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