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Drug Notebook

Generic Name: escitalopram

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Lexapro
An SSRI antidepressant - treats Anxiety and Depression
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FDA Alerts

    Suicidality
  • Antidepressants may increase risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (18–24 years of age) with major depressive disorder and other psychiatric disorders; balance this risk with clinical need. Escitalopram is not approved for use in pediatric patients. (See Pediatric Use under Cautions.)
  • In pooled data analyses, risk of suicidality was not increased in adults >24 years of age and apparently was reduced in adults ≥65 years of age with antidepressant therapy compared with placebo.
  • Depression and certain other psychiatric disorders are themselves associated with an increased risk of suicide.
  • Appropriately monitor and closely observe all patients who are started on escitalopram therapy for clinical worsening, suicidality, or unusual changes in behavior; involve family members and/or caregivers in this process. (See Worsening of Depression and Suicidality Risk under Cautions.)

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escitalopram
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(EE si TAL o pram)

Drug Interactions

Extensively metabolized in the liver, principally by CYP2C19 and 3A4. Does not inhibit CYP1A2, 2C9, 2C19, 2E1, or 3A4 in vitro and exhibits only modest inhibition against CYP2D6.

Drugs Affecting Hepatic Microsomal Enzymes

Inhibitors of CYP2C19 and 3A4: clinically important pharmacokinetic interaction unlikely since escitalopram is metabolized by multiple enzyme systems.

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP2D6: potential pharmacokinetic (increased peak plasma concentrations and AUC of the substrate) interactions. Use with caution.

Drugs Affecting Hemostasis

Potential pharmacologic interaction (increased risk of bleeding) with drugs that affect coagulation; use with caution.

Drugs Associated with Serotonin Syndrome

Potential pharmacologic interaction (serotonin syndrome) with serotonergic agents. Avoid such use, or use with caution. (See Serotonin Syndrome under Cautions.)

Specific Drugs

Drug Interaction Comment
Alcohol Does not potentiate the cognitive and motor effects of alcohol Concomitant use not recommended
Antidepressants, tricyclics (TCAs) (e.g., desipramine, imipramine) Possible increased plasma TCA concentrations with TCAs that are substrates of CYP2D6 Use with caution
Carbamazepine Possible increased escitalopram clearance
Cimetidine Increased racemic citalopram AUC and peak plasma concentrations
Citalopram Therapeutic duplication; escitalopram is the more active isomer of racemic citalopram Concomitant use not recommended
CNS drugs Potentially additive CNS effects Use with caution
Digoxin Pharmacokinetic interaction unlikely
5-HT1 receptor agonists (“triptans”) Potentially life-threatening serotonin syndrome Observe carefully if used concomitantly, particularly during treatment initiation, dosage increases, or when another serotonergic agent is initiated
Isoniazid Possible serotonin syndrome
Ketoconazole Decreased peak plasma concentrations and AUC of ketoconazole
Linezolid Possible serotonin syndrome Use with caution
Lithium

Enhanced serotonergic effects of escitalopram

Pharmacokinetic interaction unlikely

 Use with caution
MAO inhibitors Possible serotonin syndrome or NMS

Concomitant use contraindicated

Allow at least 2 weeks to elapse between discontinuance of an MAO inhibitor and initiation of escitalopram, or vice versa

Metoprolol Increased plasma metoprolol concentrations possibly resulting in decreased cardioselectivity
NSAIAs (e.g., aspirin) Increased risk of bleeding Use with caution
Pimozide

Possible increased risk of QTc interval prolongation with racemic citalopram

Pharmacokinetic interactions unlikely with racemic citalopram

 Concomitant use contraindicated
Ritonavir Pharmacokinetic interactions unlikely
Sibutramine Possible serotonin syndrome Use with caution
Theophylline No effects evident on theophylline pharmacokinetics
Triazolam Pharmacokinetic interactions unlikely
Tryptophan and other serotonin precursors Possible serotonin syndrome Concomitant use not recommended
Warfarin

Possible increased PT and risk of bleeding

Pharmacokinetic interactions unlikely with racemic citalopram

 Use with caution

Pharmacokinetics

Absorption

Bioavailability

Well absorbed following oral administration, with peak plasma concentration usually attained within 5 hours.

Commercially available tablets and oral solution are bioequivalent.

Onset

Antidepressant effect usually occurs within 1–4 weeks.

Food

Food does not affect absorption.

Special Populations

In geriatric patients, AUC is increased approximately 50%.

Distribution

Extent

Crosses the placenta.

Distributed into breast milk.

Plasma Protein Binding

Approximately 56%.

Elimination

Metabolism

Extensively metabolized in the liver to less pharmacologically active metabolites by multiple enzyme systems, including CYP3A4 and CYP2C19.

Elimination Route

Eliminated principally in urine.

Half-life

27–32 hours.

Special Populations

In geriatric patients, half-life is increased by 50%.

Hepatic impairment decreases racemic citalopram oral clearance by 37% and doubles its half-life.

Mild to moderate renal impairment decreases racemic citalopram oral clearance by 17%. Pharmacokinetics not studied in patients with severe renal impairment (Clcr <20 mL/minute).

Stability

Storage

Oral

Solution and Tablets

25°C; excursions permitted to 15–30°C.

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Uses Dosage and Administration Cautions Drug Interactions Pharmacokinetics Stability Actions Advice to Patients Preparations
Related Learning
Centers
·As a Drug
Depression
Generalized Anxiety Disorder
Major Depression
Paranoid Personality Disorder
Personality Disorder
Phobias
Schizoaffective Disorder
Teenage Depression
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