Trade Names:Lexapro- Tablets 5 mg- Tablets 10 mg- Tablets 20 mg- Solution, oral 5 mg per 5 mLCipralex (Canada)
Inhibits the CNS neuronal uptake of serotonin, potentiating serotonergic activity.
T max is approximately 5 h. Absolute bioavailability is approximately 80%.
Vd is approximately 12 L/kg. Approximately 56% is protein bound.
Metabolized in the liver to 2 metabolites (minimally active); CYP3A4 and CYP2C19 are involved in N-demethylation.
The mean terminal half-life is approximately 27 to 32 h. Approximately 8% is recovered in urine as escitalopram and 10% as a metabolite. Cl is 600 mL/min (approximately 7% caused by renal Cl).
No dosage adjustment for patients with mild to moderate renal impairment. No data on patients with CrCl less than 20 mL/min.Hepatic Function Impairment
Cl of escitalopram is decreased and half-life is prolonged in patients with reduced hepatic function.Elderly
AUC and half-life increased approximately 50%.Children
No dosage adjustment is needed in adolescent patients.Gender
Pharmacokinetics similar in men and women.
Major depressive disorder (MDD); generalized anxiety disorder (GAD).
Panic disorder; posttraumatic stress disorder.
Concurrent use of MAOIs or within 14 days of discontinuing MAOI treatment; coadministration of pimozide; hypersensitivity to escitalopram or citalopram.
PO Start with 10 mg once daily. Dosage may be increased to 20 mg once daily after 1 wk.Major Depressive DisorderAdults
PO Start with 10 mg once daily. The dose may be increased to 20 mg after 1 wk. However, 20 mg has not shown a clinical benefit over 10 mg.Children 12 yr of age and older
PO Start with 10 mg once daily. The dose may be increased to 20 mg after 3 wk.Elderly/Hepatic Function ImpairmentAdults
PO 10 mg/day.
Store at controlled room temperature (59° to 86°F).
Risk of serotonin syndrome may be increased. If coadministration is clinically warranted, carefully observe the patient, particularly when starting treatment or during dose increases.Alcohol
May potentiate the effects of alcohol; use of alcohol is not advised.Aspirin, NSAIDs (eg, ibuprofen), warfarin
Risk of bleeding may be increased. Use with caution and carefully monitor the patient.Beta-blockers (eg, metoprolol, propranolol)
Excessive beta-blockade (eg, bradycardia) may occur, increasing the risk of cardiac and CNS toxicity. Use with caution.Buspirone, opioid analgesics (eg, meperidine), sibutramine, SNRIs (eg, duloxetine), St. John's wort, sympathomimetics (eg, amphetamine), tramadol
The risk of serotonin syndrome may be increased. Closely monitor patients. Serotonin syndrome requires immediate medical attention, including withdrawal of the serotonergic agent and supportive care.Carbamazepine
Consider the possibility of decreased escitalopram serum concentrations and reduced efficacy. If an interaction is suspected, adjust the escitalopram dose as needed.Cimetidine
Serum levels may be increased by cimetidine. The clinical importance is unknown. If an interaction is suspected, it may be necessary to adjust the escitalopram dose.Citalopram
Escitalopram is the active isomer of racemic citalopram; do not coadminister these two agents.CNS drugs
Use with caution.Cyproheptadine
May decrease the pharmacologic effect of escitalopram. If there is a decrease in the efficacy of escitalopram, consider discontinuing cyproheptadine.Drugs metabolized by CYP2D6 (eg, desipramine)
Serum levels may be increased by escitalopram. Use with caution.Ketoconazole
Plasma concentrations may be reduced by escitalopram, decreasing therapeutic effect of ketoconazole. Observe the clinical response of the patient.Linezolid
The risk of serotonin syndrome may be increased. Because linezolid is an MAOI, allow at least 14 days after stopping linezolid before giving escitalopram.Lithium
Serotonergic effects of escitalopram may be enhanced. Elevated lithium concentrations and neurotoxicity may occur. Use with caution. Monitor lithium plasma concentrations and adjust the lithium dose as needed.L-tryptophan
The risk of symptoms related to central and peripheral toxicity (eg, agitation, dizziness, headache, restlessness, sweating) may be increased. Coadministration is not recommended.MAOIs (eg, phenelzine)
Coadministration is contraindicated. Allow at least 14 days to elapse between discontinuing an MAOI and starting escitalopram. Similarly, allow at least 14 days after stopping escitalopram before starting an MAOI.Methylene blue
Risk of neurologic adverse reactions, including serotonin syndrome, may be increased. Avoid concurrent use.Omeprazole
Escitalopram plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions. Monitor the patient. If an interaction is suspected, it may be necessary to adjust the escitalopram dose.Pimozide
Concurrent use is contraindicated with escitalopram.
None well documented.
Hypertension, palpitation (at least 1%); atrial fibrillation, bradycardia, cardiac failure, cerebrovascular accident, deep vein thrombosis, flushing, hypertensive crisis, hypotension, MI, orthostatic hypotension, phlebitis, QT prolongation, syncope, tachycardia, thrombosis, torsades de pointes, ventricular arrhythmia, ventricular tachycardia (postmarketing).
Headache (24%); insomnia (14%); somnolence (13%); fatigue (8%); decreased libido, dizziness (7%); abnormal dreaming, decreased appetite, lethargy (3%); paresthesia, yawning (2%); impaired concentration, increased appetite, irritability, light-headedness, migraine (at least 1%); abnormal gait, acute psychosis, aggression, akathisia, anger, asthenia, choreoathetosis, delirium, delusion, dysarthria, dyskinesia, dystonia, extrapyramidal disorder, fall, hypoesthesia, nightmare, NMS, paranoia, seizures, serotonin syndrome, tardive dyskinesia, tonic-clonic seizures, visual hallucinations (postmarketing).
Increased sweating (8%); rash (at least 1%); erythema multiforme, necrolysis, photosensitivity, Stevens-Johnson syndrome, TEN, urticaria (postmarketing).
Rhinitis (5%); blurred vision, nasal congestion, tinnitus (at least 1%); diplopia, glaucoma, nystagmus (postmarketing).
Diabetes mellitus, hyperprolactinemia (postmarketing).
Nausea (18%); diarrhea (14%); dry mouth (9%); constipation, indigestion (6%); vomiting (3%); abdominal pain, flatulence, toothache (2%); abdominal cramp, gastroenteritis, heartburn (at least 1%); GI hemorrhage, pancreatitis, rectal hemorrhage (postmarketing).
Ejaculation disorder (14%); anorgasmia (6%); impotence (3%); menstrual disorder (2%); menstrual cramps, urinary frequency, UTI (at least 1%); acute renal failure, priapism, spontaneous abortion (postmarketing).
Agranulocytosis, anemia, aplastic anemia, decreased prothrombin, ecchymosis, hemolytic anemia, idiopathic thrombocytopenia purpura, increased INR, leukopenia, thrombocytopenia (postmarketing).
Fulminant hepatitis, hepatic failure, hepatic necrosis, hepatitis (postmarketing).
Allergic reaction, anaphylaxis, angioedema (postmarketing).
Increased weight (at least 1%); hyperglycemia, hypoglycemia, hypokalemia, hyponatremia, SIADH (postmarketing).
Neck/shoulder pain (3%); arthralgia, jaw stiffness, limb pain, myalgia (at least 1%); myoclonus, rhabdomyolysis (postmarketing).
Sinusitis (3%); bronchitis, coughing, sinus congestion, sinus headache (at least 1%); dyspnea, epistaxis, pulmonary embolism (postmarketing).
Influenza-like symptoms (5%); allergy, chest pain, fever, hot flushes (at least 1%).
Compared with placebo, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants for MDD and other psychiatric disorders. Appropriately monitor and closely observe patients of all ages who are started on antidepressant therapy for clinical worsening, suicidality, or unusual changes in behavior. Advise families and caregivers of the need for close observation and communication with the prescriber.
Ensure that therapy is periodically reviewed to determine if it needs to be continued without change or if a dose change (eg, increase, decrease, discontinuation) is indicated. Monitor for clinical worsening, suicidality, and unusual changes in behavior, especially during the first few months of therapy or at times of increases or decreases in dose. The following symptoms may represent precursors to suicidality and should be reported to the health care provider immediately if noted or suspected: aggressiveness, agitation, anxiety, hostility, hypomania, impulsivity, insomnia, irritability, mania, panic attacks, and psychomotor restlessness. Frequently assess patient for response to treatment.
Category C .
Category D if taken in the second half of pregnancy (per Briggs' Drugs in Pregnancy and Lactation ).
Excreted in breast milk.
Safety and efficacy not established for treatment of GAD. Safety and effectiveness not established in children younger than 12 yr of age for the treatment of MDD.
The number of elderly patients studied was insufficient to assess difference in safety and efficacy based on age. Greater sensitivity of some elderly patients cannot be ruled out.
Use with caution in patients with severe renal impairment.
May impair judgement, thinking, or motor skills.
Bleeding episodes have been reported in patients treated with drugs that interfere with serotonin reuptake.
Use with caution in patients with concurrent systemic illness.
When discontinuing treatment, taper the dose to avoid adverse reactions. If treatment is to be discontinued or the dose reduced, gradually taper dose and monitor patient for withdrawal symptoms (eg, abnormal skin sensations, agitation, anxiety, confusion, dizziness, dysphoric mood, irritability, nausea, sweating). If significant withdrawal symptoms develop, reinstitute previous dosing schedule and attempt a less rapid tapering regimen after patient has stabilized.
Cases of hyponatremia or SIADH have been reported.
May activate hypomania or mania.
Not indicated for bipolar depression. Therefore, prior to starting treatment in patients with depressive symptoms, determine if patient is at risk for bipolar disorder.
Have been reported. Use with caution in patients with history of seizures.
Life-threatening serotonin syndrome or NMS-like reactions may occur, particularly with coadministration of serotonergic drugs.
Acute renal failure (rare), coma, dizziness, ECG changes (including QTc prolongation and very rare cases of torsades de pointes), hypotension, insomnia, nausea, seizures, sinus tachycardia, somnolence, vomiting.
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