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Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. [ 7 ] [ 10 ] It is used to treat major depressive disorder , obsessive compulsive disorder , panic disorder , and social phobia . [ 7 ]
Serotonin. A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the action of the serotonin transporter (SERT).
Escitalopram and citalopram are used off-label with acceptable efficacy, while fluoxetine is not considered to be effective for this disorder. [22] The effect sizes of SSRIs in terms of improvement on the Liebowitz social anxiety scale in individual published trials of the drugs for social anxiety disorder have ranged from –0.029 to 1.214.
Evidence of the allosteric action of escitalopram on the serotonin transported is based on the observation that the R isomer of citalopram can decrease the potency and inhibit the effects of the S isomer, probably through an allosteric interaction between two distinct, non-overlapping binding sites for the two different isomers on the serotonin transporter.
Andersen et al. were able to generate a model of the (S)-citalopram binding site in human SERT by combining mutational analysis and comparative modeling where they found out that Asn-177 and Phe-341 where key determinants for (S)-citalopram potency and high affinity inhibition [47] in addition to Tyr-95, Asp-98, Ile-172 and Ser438 previously ...
Escitalopram is the (S)-enantiomer of citalopram (which exists as a racemate), hence the name es-citalopram. [9] Escitalopram was approved for medical use in the United States in 2002. [9] Escitalopram is rarely replaced by twice the dose of citalopram; escitalopram is safer and more effective. [11]
Citalopram is a racemic mixture (50/50), and the inhibition of 5-HT reuptake by citalopram is primarily due to the (S)-enantiomer. [1] Citalopram has no or very low affinity for 5-HT 1a 5-HT 2a, dopamine D 1 and D 2, α 1-, α 2-, and β-adrenergic, histamine H 1, gamma aminobutyric acid (GABA), muscarinic cholinergic, and benzodiazepine ...
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