Escitalopram Oxalate (escitalopram oxalate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Escitalopram, the S-enantiomer of citalopram, is a selective serotonin-reuptake inhibitor (SSRI) and an antidepressant.
Escitalopram is the pure S-enantiomer of the racemic bicyclic phthalane derivative citalopram. Escitalopram is at least 100-fold more potent with respect to the inhibition of the reuptake of serotonin (5-hydroxytryptamine (5-HT)) and inhibition of the 5-HT neuronal firing rate than the R-enantiomer.
Like other SSRIs, escitalopram's antidepressant effect is believed to involve potentiation of serotonin activity in the CNS. Escitalopram appears to have little or no effect on reuptake of other neurotransmitters such as norepinephrine and dopamine. In vitro studies have demonstrated escitalopram possesses little or no affinity for alpha- or beta-adrenergic, dopamine D1-5, histamine H1-3, GABA, muscarinic M1-5, or 5-HT1-7 receptors or various ion channels (e.g., calcium, chloride, potassium, sodium channels).
Single- and multiple-dose escitalopram pharmacokinetics are linear and dose-proportional over a dosage range of 10-30 mg daily. Steady state plasma concentrations are achieved within approximately 1 week with once-daily dosing. The extent of accumulation of escitalopram in plasma at steady state in young healthy subjects was 2.2-2.5 times the plasma concentrations seen after a single dose.
The absolute bioavailability of racemic citalopram is about 80% relative to an IV dose. Escitalopram oxalate tablet and oral solution dosage forms are bioequivalent. After a single 20 mg oral dose of escitalopram oxalate tablets or solution, time to achieve peak plasma concentrations is about 5 hours.
After administration of a single oral dose of 15 mg escitalopram oxalate capsules to healthy volunteers, time to achieve peak plasma concentrations was about 4.5 hours under fasting conditions and 5 hours under fed conditions. Absorption of escitalopram is not affected by food.
Escitalopram is about 56% protein bound. The mean terminal half-life is approximately 27-32 hours. The biotransformation of escitalopram is mainly hepatic.
About 7% of the oral clearance of escitalopram is renal.
Escitalopram is metabolized principally by the hepatic cytochrome P-450 (CYP) 2C19 and 3A4 isoenzymes. The principal metabolites are less potent inhibitors of serotonin reuptake, suggesting metabolites do not substantially contribute to the antidepressant activity of escitalopram. Following oral administration, about 8% of escitalopram and 10% of its principal metabolite were recovered in the urine.
USES: This medication is used to treat certain mental/mood disorders (such as depression, anxiety). Escitalopram belongs to a class of drugs known as selective serotonin reuptake inhibitors (SSRIs). It works by helping to restore the balance of a certain natural substance (serotonin) in the brain.
Generic name: escitalopram oxalate
Pronunciation: (ES-sye-TAL-oh-pram)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Escitalopram Oxalate
Indications
The following indications are listed for Escitalopram Oxalate:
- Anxiety With Depression
- Generalized Anxiety Disorder
- Major Depressive Disorder
Also known as: Anxiety Associated With Depression, Major Unipolar Illness, Mixed Anxiety And Depressive Disorder, Unipolar Mood Disorder.
Dosing
Dosage of escitalopram oxalate is expressed in terms of escitalopram.
Escitalopram oxalate is administered orally, as tablets, oral solution, or capsules, once daily in the morning or evening without regard to meals. Commercially available escitalopram oxalate tablets and oral solution are bioequivalent.
Swallow escitalopram oxalate capsules whole; do not open, crush, or chew.
Store escitalopram oxalate tablets and capsules at 20-25degreesC (excursions permitted between 15-30degreesC).
Store escitalopram oral solution at 20-25degreesC.
No dosing information is available for this tab.
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Drug interactions
In vitro studies showed cytochrome P-450 (CYP) isoenzymes 3A4 and 2C19 are the primary enzymes involved in the metabolism of escitalopram.
In vitro data did not reveal an inhibitory effect of escitalopram on CYP3A4, 1A2, 2C9, 2C19, and 2E1 isoenzymes. While in vivo data are limited, drug interaction studies suggest a 20 mg dose of escitalopram has no 3A4 inhibitory effect and a modest 2D6 inhibitory effect.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Concurrent or recent (i.e., within 14 days) therapy with monoamine oxidase inhibitors (MAOIs), including linezolid and IV methylene blue.
*Concomitant use with pimozide.
*Known hypersensitivity to escitalopram, citalopram, or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in >=5% of patients receiving escitalopram and with an incidence of at least twice that of placebo include insomnia, nausea, increased sweating, sexual dysfunction (ejaculation disorder, decreased libido, anorgasmia), fatigue, and somnolence.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of escitalopram have not been established in pediatric patients younger than 12 years of age with major depressive disorder. In an open-label study of 24 weeks' duration in 118 pediatric patients 7-11 years of age with major depressive disorder, the safety findings were consistent with the known safety and tolerability profile for escitalopram.
Safety and effectiveness have been established in pediatric patients >=12 years of age for the treatment of major depressive disorder. Based on data from controlled studies in adults and in pediatric patients, the safety of escitalopram was similar to that of adults with major depressive disorder.
Safety and efficacy of escitalopram have not been established in pediatric patients younger than 7 years of age with generalized anxiety disorder.
Safety and effectiveness have been established in pediatric patients >=7 years of age for the treatment of generalized anxiety disorder. Based on data from controlled studies in adults and in pediatric patients, the safety of escitalopram was similar to that of adults with generalized anxiety disorder.
An increased risk of suicidal thoughts and behaviors was observed in pediatric patients treated with antidepressants.
Decreased appetite and weight loss have been observed in association with the use of SSRIs. Therefore, regular monitoring of weight and growth should be performed in children and adolescents treated with an SSRI such as escitalopram.
A National Pregnancy Registry for Antidepressants is available that monitors pregnancy outcomes in females exposed to antidepressants during pregnancy. Clinicians are encouraged to register patients by calling the National Pregnancy Registry for Antidepressants at 1-844-405-6185 or by visiting online at https://womensmentalhealth.org/clinical-and-research-programs/pregnancyregi stry/antidepressants/.
Data from published observational studies found exposure to SSRIs (including escitalopram), particularly in the month before delivery, has been associated with a less than 2-fold increase in the risk of postpartum hemorrhage.
Available epidemiologic data with escitalopram in pregnant females have not established a drug-associated risk of major birth defects or miscarriage.
Infants exposed to SSRIs during pregnancy, particularly later in pregnancy, may have an increased risk of persistent pulmonary hypertension of the newborn (PPHN); exposure may also increase the risk of poor neonatal adaptation. There are risks associated with untreated depression in pregnancy.
In animal reproductive studies, both escitalopram and racemic citalopram, when administered at doses greater than human therapeutic doses, have been shown to have adverse effects on embryo/fetal and postnatal development, including fetal structural abnormalities. In a rat embryo/fetal development study, oral administration of escitalopram during the period of organogenesis resulted in decreased fetal body weight and associated delays in ossification at doses approximately >=55 times the maximum recommended human dose (MRHD) of 20 mg daily on a mg/m2 basis; maternal toxicity (clinical signs and decreased body weight gain and food consumption) was present at dosages of 56, 112, and 150 mg/kg daily. No malformations were observed at any of the doses tested (as high as 73 times the MRHD). When rats were treated with escitalopram during pregnancy and through weaning, slightly increased offspring mortality and growth retardation were noted at approximately 23 times the MRHD; slight maternal toxicity was also seen at this dose. Slightly increased mortality of offspring was seen at dosages of 24 mg/kg daily.
Females who discontinue antidepressants during pregnancy are more likely to experience a relapse of major depression than females who continue antidepressants. Consider the risk of untreated depression when discontinuing or changing treatment with antidepressant medication during pregnancy and postpartum.
Neonates exposed to serotonergic antidepressants (e.g., SSRIs, serotonin norepinephrine reuptake inhibitors (SNRIs)) late in the third trimester of pregnancy have developed complications that have sometimes been severe and required prolonged hospitalization, respiratory support, and enteral nutrition. Such complications can arise immediately upon delivery. Clinical findings reported in the neonates have included respiratory distress, cyanosis, apnea, seizures, temperature instability, feeding difficulty, vomiting, hypoglycemia, hypotonia, hypertonia, hyperreflexia, tremor, jitteriness, irritability, and constant crying. These features appear to be consistent with either a direct toxic effect of serotonergic antidepressants or, possibly, a drug withdrawal syndrome. In some cases, the clinical picture was consistent with serotonin syndrome.
Escitalopram and its metabolite are distributed into human milk. In a study of 8 nursing mothers receiving daily doses of escitalopram of 10-20 mg daily, exclusively breast-fed infants received about 3.9% of the maternal weight-adjusted dose of escitalopram and 1.7% of the maternal weight-adjusted dose of its metabolite. There are no data on the effects of escitalopram or its metabolites on milk production.
Excessive sedation, restlessness, agitation, poor feeding, and poor weight gain have been reported in infants exposed to escitalopram through breast milk; infants who are exposed should be monitored for these symptoms. Consider developmental and health benefits of breast-feeding along with the mother's clinical need for escitalopram and the potential for adverse effects on the breast-fed infant from exposure to escitalopram or from the underlying maternal condition.
For elderly patients, the recommended dosage of escitalopram oxalate tablets and oral solution is 10 mg daily.
As escitalopram oxalate capsules are only available in a 15 mg dose strength, use is not recommended in geriatric patients. Escitalopram oxalate capsules are not indicated in geriatric patients.
Approximately 6% of patients studied in clinical trials of escitalopram for major depressive disorder and generalized anxiety disorder were 60 years of age or older. Experience in geriatric patients in these trials was insufficient to determine possible differential efficacy and safety measures on the basis of age; however, increased sensitivity cannot be ruled out.
In 2 pharmacokinetic studies, the mean AUC and elimination half-life of escitalopram were increased by approximately 50% in geriatric individuals compared with younger individuals, but peak escitalopram concentrations were unchanged. The manufacturers recommend a dosage of escitalopram in geriatric patients of 10 mg once daily. Use of escitalopram oxalate capsules is not recommended in geriatric patients because the recommended dosage in these patients cannot be achieved with the dosage strength available for escitalopram capsules.
SSRIs and SNRIs, including escitalopram, have been associated with clinically important hyponatremia in geriatric patients, who may be at greater risk for this adverse effect.
ICD codes
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Last reviewed · Source: First Databank (FDB) drug data
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