Escitalopram

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[edit] BRAND NAMES

[edit] STRUCTURE

Escitalopram.jpg

S-enantiomer of racemic citalopram

[edit] MECHANISM OF ACTION

Escitalopram is a selective serotonin reuptake inhibitor (SSRI). It blocks the reuptake of serotonin into the presynaptic cell, increasing its level within the synaptic cleft. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs.

CYP3A4 and CYP2C19 are the primary enzymes involved in the metabolism of escitalopram

[edit] INDICATIONS

  • Acute and Maintenance Treatment of Major Depressive Disorder (MDD) in adults and adolescents aged 12-17 years (USA)/18 years (Europe). A major depressive episode implies a prominent and relatively persistent depressed or dysphoric mood that usually interferes with daily functioning (nearly every day for at least 2 weeks; it should include at least 4 of the following 8 symptoms: change in appetite, change in sleep, psychomotor agitation or retardation, loss of interest in usual activities or decrease in sexual drive, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, and a suicide attempt or suicidal ideation.
  • Acute Treatment of Generalized Anxiety Disorder (GAD) in adults. GAD is characterized by excessive anxiety and worry (apprehensive expectation) that is persistent for at least 6 months and which the person finds difficult to control. It must be associated with at least 3 of the following symptoms: restlessness or feeling keyed up or on edge, being easily fatigued, difficulty concentrating or mind going blank, irritability, muscle tension, and sleep disturbance. (USA and EUROPE)
  • Social anxiety disorder: A marked and persistent fear of one or more social or performance situations in which the person is exposed to unfamiliar people or to possible scrutiny by others. (EUROPE)
  • Panic disorder: unexpected discrete period of intense fear or discomfort, symptoms can include palpitations, sweating, trembling, sensations of shortness of breath, chest pain or discomfort, nausea or abdominal distress, feeling dizzy and fear of dying (EUROPE)

[edit] DOSAGE

  • Depression:Adults and Adolescents, the recommended dose is 10 mg once daily. Dosage may be increased up to max 20mg/day, after a minimum of one week for adults and 3 weeks for adolescents
  • Generalized Anxiety Disorder: Adults, the recommended starting dose is 10 mg/day. Dosage may be increased up to max 20mg/day, after a minimum of one week

The maximum dose should be limited to 10 mg/day in patients with hepatic impairment and in patients who are greater than 60 years of age because of expected higher exposures

Patients may notice improvement with escitalopram therapy in 1 to 4 weeks, they also should be advised to continue therapy as directed.

Discontinuing Escitalopram: A gradual dose reduction is recommended whenever possible

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to escitalopram or citalopram
  • It's use within 14 days of stopping an MAOI because of an increased risk of serotonin syndrome
  • Do not start Escitalopram in a patient who is being treated with linezolid or intravenous methylene blue
  • Concomitant use with pimozide (Orap®) because this can cause serious heart problems (QT prolongation)

[edit] WARNINGS AND PRECAUTIONS

  • FDA Black Box Warning for Escitalopram : Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of escitalopram or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. 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 in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. Escitalopram is not approved for use in pediatric patients less than 12 years of age
  • Abnormal heart rhythm (QTc interval prolongation): The potential for QT interval prolongation and Torsade de Pointes when using Citalopram in doses >40 mg/day were not observed with Escitalopram. (See Citalopram WARNINGS AND PRECAUTIONS
  • Serotonin Syndrome: Serotonin syndrome has been reported with SSRIs and SNRIs, including Escitalopram, both when taken alone, but especially when co-administered with other serotonergic agents (including Triptans, Tricyclic antidepressants, Fentanyl, Lithium, Tramadol, Tryptophan, Buspirone and St. John’s Wort). Serotonin syndrome symptoms may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).If such symptoms occur, discontinue Escitalopram and initiate supportive treatment. If concomitant use of Escitalopram with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome, particularly during treatment initiation and dose increases.
  • In clinical trials, cases of convulsion have been reported in association with Escitalopram treatment. Escitalopram should be introduced with care in patients with a history of seizure disorder.
  • Abnormal Bleeding: May increase the risk of bleeding. Use with NSAIDs, aspirin, warfarin, or drugs that affect coagulation may potentiate the risk of gastrointestinal or other bleeding
  • Hyponatremia: Hyponatremia has been reported with Escitalopram use, either alone or in combination with some diuretics (Hydrochlorothiazide, Furosemide). Hyponatremia appears to be the result of the syndrome of inappropriate antidiuretic hormone secretion (SIADH). Signs and symptoms include headache, new or increased seizure frequency, difficulty concentrating, memory impairment, confusion, weakness, and unsteadiness, which can lead to fall. Severe Hyponatremia may cause hallucination, syncope, seizure, coma, respiratory arrest, and death.
  • Interference with Cognitive and Motor Performance: Use caution when operating machinery

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Escitalopram should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Escitalopram is excreted in human breast milk. Caution should be exercised and breastfeeding infants should be observed for adverse reactions when Escitalopram is administered to a nursing woman

[edit] SIDE EFFECTS

Most commonly observed adverse reactions (incidence ≥ 5% and at least twice the incidence of placebo patients) are: insomnia, ejaculation disorder (primarily ejaculatory delay), nausea, sweating increased, fatigue and somnolence, decreased libido, and anorgasmia.

For more serious adverse effects (see WARNINGS AND PRECAUTIONS)

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antidepressants
Tricyclic antidepressants Amitriptyline (Elavil, Laroxyl)   Clomipramine (Anafranil)   Doxepin (Sinequan)   Imipramine (Tofranil)   Nortriptyline (Aventyl, Pamelor)   Trimipramine (Surmontil)
Selective serotonin reuptake inhibitors (SSRIs) Citalopram (Celexa, Seropram)   Escitalopram (Cipralex, Lexapro)   Fluoxetine (Prozac)   Fluvoxamine (Luvox, Maveral)   Paroxetine (Paxil, Seroxat)   Sertraline (Zoloft)
Serotonin–norepinephrine reuptake inhibitors (SNRIs) Desvenlafaxine (Pristiq)   Duloxetine (Cymbalta, Xeristar)   Venlafaxine (Efexor, Effexor)
Serotonin antagonists and reuptake inhibitors (SARIs) Trazodone (Desyrel, Oleptro)
Norepinephrine reuptake inhibitors (NRIs) Maprotiline (Ludiomil)   Reboxetine (Edronax)
Norepinephrine-dopamine reuptake inhibitors (NDRIs) Bupropion (Wellbutrin)
Noradrenergic and specific serotonergic antidepressants (NaSSAs) Mianserin (Lantanon)   Mirtazapine (Remeron)
Norepinephrine-dopamine disinhibitors (NDDIs) Agomelatine (Valdoxan, Thymanax)
Monoamine oxidase inhibitors Nonselective Tranylcypromine (Parnate)
Monoamine oxidase inhibitors B-Selective Selegiline (Transdermal) (Emsam)
Others 5-Hydroxytryptophan   S-Adenosyl methionine   Hypericum (St John's wort)