Drug Name

Lexapro (Escitalopram)

Generic Name

Escitalopram Tablets (es-sye-TAL-oh-pram)

Looks like

Lexapro (escitalopram oxalate) is available as tablets or as an oral solution.

• Lexapro 5 mg-white, film-coated, round tablets
• Lexapro 10 mg-white, film-coated, round tablets
• Lexapro 20 mg-white, film-coated, round tablets

Dosage Form

Tablets

Route Of Administration

ORAL

Imprint Code

FL;5 / F;L;10 / F;L;20

Size

6mm / 7mm / 10mm

Alternatives

Anxiety
Xanax, Valium, Lorazepam, Cymbalta (Duloxetine), Ativan
Depression
Xanax, Zoloft, Prozac (Fluoxetine), Cymbalta (Duloxetine), Desyrel (Trazodone), Celexa (Citalopram)

Drug Uses

Treating depression or generalized anxiety disorder. It may also be used for other conditions as determined by your doctor.

Drug class

Lexapro is a selective serotonin reuptake inhibitor (SSRI). It works by restoring the balance of serotonin, a natural substance in the brain, which helps to improve certain mood problems.

Contains

Lexapro tablets are film-coated, round tablets containing escitalopram oxalate in strengths equivalent to 5 mg, 10 mg, and 20 mg escitalopram base. The 10 and 20 mg tablets are scored. The tablets also contain the following inactive ingredients: talc, croscarmellose sodium, microcrystalline cellulose/colloidal silicon dioxide, and magnesium stearate. The film coating contains hypromellose, titanium dioxide, and polyethylene glycol.

Lexapro oral solution contains escitalopram oxalate equivalent to 1 mg/mL escitalopram base. It also contains the following inactive ingredients: sorbitol, purified water, citric acid, sodium citrate, malic acid, glycerin, propylene glycol, methylparaben, propylparaben, and natural peppermint flavor.

Chemical formula

Lexapro (escitalopram oxalate) is an orally administered selective serotonin reuptake inhibitor (SSRI). Escitalopram is the pure S-enantiomer (single isomer) of the racemic bicyclic phthalane derivative citalopram. Escitalopram oxalate is designated S - (+) - 1 - [3 - (dimethyl - amino) propyl] - 1 - (p - fluorophenyl) - 5 - phthalancarbonitrile oxalate with the following structural formula:

The molecular formula is C20H21FN2O * C2H2O4 and the molecular weight is 414.40.

Mechanism of Action

The mechanism of antidepressant action of escitalopram, the S-enantiomer of racemic citalopram, is presumed to be linked to potentiation of serotonergic activity in the central nervous system (CNS) resulting from its inhibition of CNS neuronal reuptake of serotonin (5-HT). In vitro and in vivo studies in animals suggest that escitalopram is a highly selective serotonin reuptake inhibitor (SSRI) with minimal effects on norepinephrine and dopamine neuronal reuptake. Escitalopram is at least 100-fold more potent than the R-enantiomer with respect to inhibition of 5-HT reuptake and inhibition of 5-HT neuronal firing rate. Tolerance to a model of antidepressant effect in rats was not induced by long-term (up to 5 weeks) treatment with escitalopram. Escitalopram has no or very low affinity for serotonergic (5-HT1-7) or other receptors including alpha- and beta-adrenergic, dopamine (D1-5), histamine (H1-3), muscarinic (M1-5), and benzodiazepine receptors. Escitalopram also does not bind to, or has low affinity for, various ion channels including Na+, K+, Cl-, and Ca++ channels. Antagonism of muscarinic, histaminergic, and adrenergic receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular side effects of other psychotropic drugs.

How Taken

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Your doctor may occasionally change your dose to make sure you get the best results from the medication.

Take each dose with a full glass of water.

Try to take the medicine at the same time each day. Follow the directions on your prescription label.

To be sure you get the correct dose of liquid Lexapro, measure the liquid with a marked measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

It may take 4 weeks or longer before you start feeling better. Do not stop using Lexapro without first talking to your doctor. You may have unpleasant side effects if you stop taking this medication suddenly. Store Lexapro at room temperature away from moisture and heat.

Dosage and Administration

The recommended dose of Lexapro is 10 mg once daily. A fixed-dose trial of Lexapro demonstrated the effectiveness of both 10 mg and 20 mg of Lexapro, but failed to demonstrate a greater benefit of 20 mg over 10 mg. If the dose is increased to 20 mg, this should occur after a minimum of one week.

Lexapro should be administered once daily, in the morning or evening, with or without food.

Usual Starting Dose

The recommended starting dose of Lexapro is 10 mg once daily.

Missed Dose

Take the missed dose as soon as you remember. However, if it is almost time for the next regularly scheduled dose, skip the missed dose and take the next one as directed. Do not take extra medicine to make up the missed dose.

Overdose

Seek emergency medical attention if you think you have taken too much of this medication. Symptoms of an Lexapro overdose may include nausea, vomiting, tremor, sweating, rapid heartbeat, confusion, dizziness, seizures, and coma.

Storage

Store Lexapro at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. Keep Lexapro out of the reach of children and away from pets.

How Supplied

5 mg Tablets:
Bottle of 100 NDC # 0456-2005-01
White to off-white, round, non-scored, film-coated. Imprint "FL" on one side of the tablet and "5" on the other side.

10 mg Tablets:
Bottle of 100 NDC # 0456-2010-01
10 x 10 Unit Dose NDC # 0456-2010-63
White to off-white, round, scored, film-coated. Imprint on scored side with "F" on the left side and "L" on the right side. Imprint on the non-scored side with "10".

20 mg Tablets:
Bottle of 100 NDC # 0456-2020-01
10 x 10 Unit Dose NDC # 0456-2020-63
White to off-white, round, scored, film-coated. Imprint on scored side with "F" on the left side and "L" on the right side. Imprint on the non-scored side with "20".

Oral Solution:
5 mg/5 mL, peppermint flavor (240 mL) NDC # 0456-2101-08

What is the most important information I should know about Lexapro (Escitalopram)?

Do not take Lexapro together with a monoamine oxidase inhibitor (MAOI) such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate). You must wait at least 14 days after stopping an MAOI before you can take Lexapro. After you stop taking Lexapro, you must wait at least 14 days before you start taking an MAOI.
You may have thoughts about suicide when you first start taking an antidepressant, especially if you are younger than 24 years old. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

Call your doctor at once if you have any new or worsening symptoms such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself. SSRI antidepressants may cause serious or life-threatening lung problems in newborn babies whose mothers take the medication during pregnancy. However, you may have a relapse of depression if you stop taking your antidepressant during pregnancy. If you are planning a pregnancy, or if you become pregnant while taking Lexapro, do not stop taking the medication without first talking to your doctor.
It is dangerous to try and purchase Lexapro on the Internet or from vendors outside of the United States. Medications distributed from Internet sales may contain dangerous ingredients, or may not be distributed by a licensed pharmacy. Samples of Lexapro purchased on the Internet have been found to contain haloperidol (Haldol), a potent antipsychotic drug with dangerous side effects. For more information, contact the U.S. Food and Drug Administration (FDA) or visit www.fda.gov/buyonlineguide.

What should I discuss with my doctor before taking Lexapro (Escitalopram)?

It is dangerous to try and purchase Lexapro on the Internet or from vendors outside of the United States. Medications distributed from Internet sales may contain dangerous ingredients, or may not be distributed by a licensed pharmacy. Samples of Lexapro purchased on the Internet have been found to contain haloperidol (Haldol), a potent antipsychotic drug with dangerous side effects. For more information, contact the U.S. Food and Drug Administration (FDA) or visit www.fda.gov/buyonlineguide.

Do not use Lexapro if you are using an MAO inhibitor such as isocarboxazid (Marplan), tranylcypromine (Parnate), phenelzine (Nardil), rasagiline (Azilect), or selegiline (Eldepryl, Emsam). Serious and sometimes fatal reactions can occur when these medicines are taken with Lexapro. You must wait at least 14 days after stopping an MAO inhibitor before you can take Lexapro. After you stop taking Lexapro, you must wait at least 14 days before you start taking an MAOI.

Before taking Lexapro, tell your doctor if you are allergic to any drugs, or if you have:

• liver or kidney disease;
• seizures or epilepsy;
• bipolar disorder (manic depression); or
• a history of drug abuse or suicidal thoughts.

If you have any of these conditions, you may not be able to use Lexapro, or you may need a dosage adjustment or special tests during treatment.

You may have thoughts about suicide when you first start taking an antidepressant, especially if you are younger than 24 years old. Tell your doctor if you have worsening symptoms of depression or suicidal thoughts during the first several weeks of treatment, or whenever your dose is changed.

Your family or other caregivers should also be alert to changes in your mood or symptoms. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

FDA pregnancy category C. SSRI antidepressants may cause serious or life-threatening lung problems in newborn babies whose mothers take the medication during pregnancy. However, you may have a relapse of depression if you stop taking your antidepressant during pregnancy. If you are planning a pregnancy, or if you become pregnant while taking Lexapro, do not stop taking the medication without first talking to your doctor. Lexapro can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give Lexapro to anyone younger than 18 years old without the advice of of a doctor.

Absorption and Distribution

Following a single oral dose (20 mg tablet or solution) of escitalopram, peak blood levels occur at about 5 hours. Absorption of escitalopram is not affected by food.

The absolute bioavailability of citalopram is about 80% relative to an intravenous dose, and the volume of distribution of citalopram is about 12 L/kg. Data specific on escitalopram are unavailable.

The binding of escitalopram to human plasma proteins is approximately 56%.

Metabolism and Elimination

Following oral administrations of escitalopram, the fraction of drug recovered in the urine as escitalopram and S-demethylcitalopram (S-DCT) is about 8% and 10%, respectively. The oral clearance of escitalopram is 600 mL/min, with approximately 7% of that due to renal clearance.

Escitalopram is metabolized to S-DCT and S-didemethylcitalopram (S-DDCT). In humans, unchanged escitalopram is the predominant compound in plasma. At steady state, the concentration of the escitalopram metabolite S-DCT in plasma is approximately one-third that of escitalopram. The level of S-DDCT was not detectable in most subjects. In vitro studies show that escitalopram is at least 7 and 27 times more potent than S-DCT and S-DDCT, respectively, in the inhibition of serotonin reuptake, suggesting that the metabolites of escitalopram do not contribute significantly to the antidepressant actions of escitalopram. S-DCT and S-DDCT also have no or very low affinity for serotonergic (5-HT1-7) or other receptors including alpha- and beta-adrenergic, dopamine (D1-5), histamine (H1-3), muscarinic (M1-5), and benzodiazepine receptors. S-DCT and S-DDCT also do not bind to various ion channels including Na+, K+, Cl-, and Ca++ channels.

In vitro studies using human liver microsomes indicated that CYP3A4 and CYP2C19 are the primary isozymes involved in the N-demethylation of escitalopram.

Population Subgroups

Age - Escitalopram pharmacokinetics in subjects ≥ 65 years of age were compared to younger subjects in a single-dose and a multiple-dose study. Escitalopram AUC and half-life were increased by approximately 50% in elderly subjects, and Cmax was unchanged. 10 mg is the recommended dose for elderly patients.

Gender - In a multiple-dose study of escitalopram (10 mg/day for 3 weeks) in 18 male (9 elderly and 9 young) and 18 female (9 elderly and 9 young) subjects, there were no differences in AUC, Cmax, and half-life between the male and female subjects. No adjustment of dosage on the basis of gender is needed.

Reduced hepatic function - Citalopram oral clearance was reduced by 37% and half-life was doubled in patients with reduced hepatic function compared to normal subjects. 10 mg is the recommended dose of escitalopram for most hepatically impaired patients.

Reduced renal function - In patients with mild to moderate renal function impairment, oral clearance of citalopram was reduced by 17% compared to normal subjects. No adjustment of dosage for such patients is recommended. No information is available about the pharmacokinetics of escitalopram in patients with severely reduced renal function (creatinine clearance < 20 mL/min).

Drug-Drug Interactions

In vitro enzyme inhibition data did not reveal an inhibitory effect of escitalopram on CYP3A4, -1A2, -2C9, -2C19, and -2E1. Based on in vitro data, escitalopram would be expected to have little inhibitory effect on in vivo metabolism mediated by these cytochromes. While in vivo data to address this question are limited, results from drug interaction studies suggest that escitalopram, at a dose of 20 mg, has no 3A4 inhibitory effect and a modest 2D6 inhibitory effect.

Special Populations

Geriatric

Approximately 6% of the 1144 patients receiving escitalopram in controlled trials of Lexapro in major depressive disorder and GAD were 60 years of age or older; elderly patients in these trials received daily doses of Lexapro between 10 and 20 mg. The number of elderly patients in these trials was insufficient to adequately assess for possible differential efficacy and safety measures on the basis of age. Nevertheless, greater sensitivity of some elderly individuals to effects of Lexapro cannot be ruled out.

In two pharmacokinetic studies, escitalopram half-life was increased by approximately 50% in elderly subjects as compared to young subjects and Cmax was unchanged 10 mg/day is the recommended dose for elderly patients.

Of 4422 patients in clinical studies of racemic citalopram, 1357 were 60 and over, 1034 were 65 and over, and 457 were 75 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but again, greater sensitivity of some elderly individuals cannot be ruled out.

Pediatric

Safety and effectiveness in the pediatric population have not been established. One placebo-controlled trial in 264 pediatric patients with MDD has been conducted with Lexapro, and the data were not sufficient to support a claim for use in pediatric patients. Anyone considering the use of Lexapro in a child or adolescent must balance the potential risks with the clinical need.

Possible side effects

Get emergency medical help if you have any of these signs of an allergic reaction: skin rash or hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Call your doctor at once if you have any new or worsening symptoms such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

Call your doctor at once if you have any of these serious side effects:

• seizure (convulsions);
• tremors, shivering, muscle stiffness or twitching;
• problems with balance or coordination; or
• agitation, confusion, sweating, fast heartbeat.

Other less serious side effects are more likely to occur, such as:

• feeling nervous, restless, or unable to sit still;
• headache, trouble concentrating;
• drowsiness, dizziness;
• sleep problems (insomnia);
• nausea, diarrhea, heartburn;
• weight changes;
• decreased sex drive, impotence, or difficulty having an orgasm; or
• dry mouth, ringing in your ears.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.

What other drugs will affect Lexapro (Escitalopram)?

Talk to your doctor before taking any medicine for pain, arthritis, fever, or swelling. This includes aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), diclofenac (Voltaren), indomethacin, piroxicam (Feldene), nabumetone (Relafen), etodolac (Lodine), and others. Taking any of these drugs with Lexapro may cause you to bruise or bleed easily.

Before taking Lexapro, tell your doctor if you are using any of the following medicines:

• carbamazepine (Carbatrol, Tegretol);
• cimetidine (Tagamet);
• lithium (Lithobid, Eskalith);
• a blood thinner such as warfarin (Coumadin);
• any other antidepressants such as amitriptyline (Elavil), citalopram (Celexa), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), imipramine (Tofranil), nortriptyline (Pamelor), paroxetine (Paxil), or sertraline (Zoloft); or
• almotriptan (Axert), frovatriptan (Frova), sumatriptan (Imitrex), naratriptan (Amerge), rizatriptan (Maxalt), or zolmitriptan (Zomig).

If you are using any of these drugs, you may not be able to use Lexapro, or you may need dosage adjustments or special tests during treatment.

There may be other drugs not listed that can affect Lexapro. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

What should I avoid while taking Lexapro (Escitalopram)?

Do not take Lexapro together with citalopram (Celexa), isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), selegiline (Eldepryl, Emsam), or tranylcypromine (Parnate). Avoid drinking alcohol, which can increase some of the side effects of Lexapro.

Avoid using other medicines that make you sleepy (such as cold medicine, pain medication, muscle relaxers, medicine for seizures, other medication for depression or anxiety). They can add to sleepiness caused by Lexapro.

Lexapro can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert.

Contraindications

Concomitant use in patients taking monoamine oxidase inhibitors (MAOIs) is contraindicated.

Concomitant use in patients taking pimozide is contraindicated.

Lexapro is contraindicated in patients with a hypersensitivity to escitalopram or citalopram or any of the inactive ingredients in Lexapro.

Warnings

Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18-24) with major depressive disorder (MDD) and other psychiatric disorders. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.

The pooled analyses of placebo-controlled trials in children and adolescents with MDD, obsessive compulsive disorder (OCD), or other psychiatric disorders included a total of 24 short-term trials of 9 antidepressant drugs in over 4400 patients. The pooled analyses of placebo-controlled trials in adults with MDD or other psychiatric disorders included a total of 295 short-term trials (median duration of 2 months) of 11 antidepressant drugs in over 77,000 patients. There was considerable variation in risk of suicidality among drugs, but a tendency toward an increase in the younger patients for almost all drugs studied. There were differences in absolute risk of suicidality across the different indications, with the highest incidence in MDD. The risk differences (drug vs. placebo), however, were relatively stable within age strata and across indications.

No suicides occurred in any of the pediatric trials. There were suicides in the adult trials, but the number was not sufficient to reach any conclusion about drug effect on suicide.

It is unknown whether the suicidality risk extends to longer-term use, i.e., beyond several months. However, there is substantial evidence from placebo-controlled maintenance trials in adults with depression that the use of antidepressants can delay the recurrence of depression.

All patients being treated with antidepressants for any indication should be monitored appropriately and observed closely for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of a course of drug therapy, or at times of dose changes, either increases or decreases.

The following symptoms, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia (psychomotor restlessness), hypomania, and mania, have been reported in adult and pediatric patients being treated with antidepressants for major depressive disorder as well as for other indications, both psychiatric and nonpsychiatric. Although a causal link between the emergence of such symptoms and either the worsening of depression and/or the emergence of suicidal impulses has not been established, there is concern that such symptoms may represent precursors to emerging suicidality.

Consideration should be given to changing the therapeutic regimen, including possibly discontinuing the medication, in patients whose depression is persistently worse, or who are experiencing emergent suicidality or symptoms that might be precursors to worsening depression or suicidality, especially if these symptoms are severe, abrupt in onset, or were not part of the patient's presenting symptoms.

If the decision has been m