LEXAPRO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LEXAPRO (LEXAPRO).
Selective serotonin reuptake inhibitor (SSRI); inhibits serotonin reuptake at the presynaptic neuron, potentiating serotonergic activity.
| Metabolism | Primarily hepatic via CYP3A4 and CYP2C19; active metabolite S-desmethylcitalopram. |
| Excretion | Primarily renal (approx. 80% as metabolites, 8% as unchanged drug); biliary/fecal elimination accounts for ~15%. |
| Half-life | 27-32 hours (mean ~30 h); steady state reached in ~1 week; linear kinetics at therapeutic doses. |
| Protein binding | Approximately 56% bound to plasma proteins (mainly albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | 12-26 L/kg (mean ~20 L/kg); extensive extravascular distribution consistent with high lipophilicity. |
| Bioavailability | Oral: approximately 80% (range 60-90%) after a single dose; food does not significantly affect absorption. |
| Onset of Action | Oral: 1-2 weeks for initial therapeutic effect; full effect may require 4-6 weeks. No IV formulation. |
| Duration of Action | 24 hours with once-daily dosing; sustained receptor occupancy due to long half-life; washout period >2 weeks recommended before switching MAOIs. |
10 mg orally once daily; may increase to 20 mg once daily after at least 1 week.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment for mild to moderate impairment. Not recommended for severe impairment (CrCl <20 mL/min). |
| Liver impairment | For Child-Pugh class A or B: 10 mg orally once daily. Use caution in severe impairment (Child-Pugh class C); limited data. |
| Pediatric use | Adolescents 12-17 years: 10 mg orally once daily. Children <12 years: not approved. |
| Geriatric use | Initial 5 mg orally once daily; maximum 10 mg once daily. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LEXAPRO (LEXAPRO).
| Breastfeeding | Escitalopram is excreted into human breast milk with a milk-to-plasma ratio (M/P) of approximately 2.0. Infant serum levels are typically low, but some cases of adverse effects such as irritability, feeding problems, and sleep disturbance have been reported. The American Academy of Pediatrics considers escitalopram compatible with breastfeeding, but caution is advised, especially in premature or compromised infants. |
| Teratogenic Risk | First trimester: Epidemiologic studies have shown a small increased risk of congenital cardiac defects (primarily ventricular septal defects) with exposure, with an absolute risk of approximately 1-2%. Second/third trimester: Late pregnancy exposure may increase risk for persistent pulmonary hypertension of the newborn (PPHN) and serotonin syndrome in the neonate. Third trimester use may lead to neonatal adaptation syndrome including irritability, respiratory distress, and feeding difficulties. |
■ FDA Black Box Warning
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
| Serious Effects |
["Concurrent use of MAOIs or within 14 days of discontinuing MAOI","Concomitant use of pimozide","Hypersensitivity to escitalopram or citalopram","QT prolongation or congenital long QT syndrome (for citalopram, caution for escitalopram)"]
| Precautions | ["Suicidality risk in young adults","Serotonin syndrome","QT prolongation","Hyponatremia","Bleeding risk","Activation of mania/hypomania","Seizure risk","Abrupt discontinuation syndrome"] |
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| Fetal Monitoring | Monitor maternal mental health status, and watch for signs of serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability). For the fetus, monitor growth and well-being with serial ultrasound assessments, particularly in the third trimester. Neonates exposed in utero should be observed for adaptation syndrome symptoms and PPHN (pulse oximetry screening). |
| Fertility Effects | Animal studies show no impairment of fertility; however, human data are limited. SSRIs may affect sperm quality and libido. Escitalopram can cause sexual dysfunction (delayed ejaculation, anorgasmia) which may impact fertility indirectly. No specific adverse effects on female fertility have been reported. |