Name: | Escitalopram |
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Name (isomeric): | DB01175 |
Drug Type: | small molecule |
Description: | S-enantiomer of citalopram. |
Synonyms: |
Escitalopram Oxalate
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Brand: | Cipralex, Lexapro |
Category: | Antidepressive Agents, Second-Generation, Serotonin Uptake Inhibitors |
CAS number: | 128196-01-0 |
Indication: | Labeled indications include major depressive disorder (MDD) and generalized anxiety disorder (GAD). Unlabeled indications include treatment of mild dementia-associated agitation in nonpsychotic patients. |
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Pharmacology: |
Escitalopram is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram ar...
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Mechanism of Action: |
The antidepressant, antiobsessive-compulsive, and antibulimic actions of escitalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Escitalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors. SSRIs bind...
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Absorption: | The absolute bioavailability of citalopram is about 80% relative to an intravenous dose. |
Protein binding: | ~56% |
Biotransformation: | Mainly hepatic. Escitalopram undergoes N-demethylation to S-demethylcitalopram (S-DCT) and S-didemethylcitalopram (S-DDCT). CYP3A4 and CYP2C19 are the enzymes responsible for this N-demethylation reaction. |
Route of elimination: | Following oral administrations of escitalopram, the fraction of drug recovered in the urine as escitalopram and S-demethylcitalopram (S-DCT) is about 8% and 10%, respectively. The oral clearance of escitalopram is 600 mL/min, with approximately 7% of that due to renal clearance. Escitalopram is metabolized to S-DCT and S-didemethylcitalopram (S-DDCT). |
Half Life: | 27-32 hours |
Clearance: | oral cl=600 mL/min [Following oral administrations] |
Toxicity: | Signs of overdose include convulsions, coma, dizziness, hypotension, insomnia, nausea, vomiting, sinus tachycardia, somnolence, and ECG changes (including QT prolongation). |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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