Notice bibliographique
Résumé
Back to table of contents Previous article Next article Clinical & Research NewsFull AccessIsolating Isomers Enhances Antidepressant Efficacy, Study ShowsJim RosackJim RosackPublished Online:16 Aug 2002https://doi.org/10.1176/pn.37.16.0017aTwo research reports presented at the 23rd Collegium Internationale NeuroPsychopharmacologium Congress in Montreal in June indicate that isolation of active, single forms of molecules, called isomers, from mixed-isomer compounds can yield significant improvements in efficacy and in safety and tolerability profiles.The first report, about the antidepressant escitalopram (Lexapro), which was developed in Europe by Lundbeck and licensed to Forest Laboratories for marketing in the United States, indicates that the drug is more than twice as potent at increasing brain serotonin availability as its parent compound, citalopram (Celexa). Escitalopram is the S-isomer of citalopram, which is a compound that contains two isomers—or mirror-image forms (labeled the S and R isomers)—of the same molecule.Pharmacologists are finding that more often than not, one of the two isomers in mixed compounds is much more “active” than the other isomer, and is often responsible for therapeutic action of the compound, while the second isomer is often associated with secondary drug effects, which could manifest as side effects.The second research report indicates that when escitalopram (the compound’s generic name, simply indicating the chemical name, S-citalopram, phonetically) is administered along with the R-isomer, the ability of the S-isomer to increase serotonin levels actually declines, indicating that the R-isomer may be interfering with the active S-isomer’s ability to increase serotonin availability in the brain, according to Jack Gorman, M.D., the Lieber Professor and vice chair for research at the College of Physicians and Surgeons of Columbia University, who was involved in the studies.The mechanism by which the R-isomer affects the ability of the S-isomer to boost serotonin levels is still a mystery. However, pharmacologists at Lundbeck and Forest suspect that the two isomers are competing to bind with serotonin reuptake transporters. While the S-isomer is very potent at binding to and blocking the reuptake transporter, the R-isomer binds but may not as effectively disable reuptake.Overall, clinical trial data for escitalopram have been quite favorable, showing increased potency compared with citalopram. Previous studies have indicated that the new drug also has a reduced drug-interaction profile and is well tolerated, with few significant or serious side effects.A new drug application for escitalopram was submitted to the FDA in March 2001, and the agency issued an “approvable” letter for the new drug last January. A Forest spokesperson told Psychiatric News that final approval for marketing is expected within the “very near future.” ▪ ISSUES NewArchived
Récupéré en direct depuis OpenAlex et désinversé. Les résumés ne sont pas conservés dans cette base de données : les index inversés représentent 8,6 Go des 9,3 Go de texte de la base, et le serveur dispose de 13 Go libres.
Comment cette classification a été obtenuedéplier
Prédiction distillée sur la base complète
Imitation des enseignantsNi prévalence calibrée, ni vérité terrain. Validation humaine à venir. Apprise à partir de 10 348 étiquettes directes de Codex et de 10 348 étiquettes directes de Gemma. Le mode candidate est l'union des têtes enseignantes seuillées; le consensus est leur intersection. Ces sorties portent le statut machine_predicted_unvalidated et ne sont ni des étiquettes humaines ni des étiquettes directes de modèles de pointe.
Scores Codex et Gemma par catégorie
| Catégorie | Codex | Gemma |
|---|---|---|
| Métarecherche | 0,000 | 0,000 |
| Méta-épidémiologie (sens strict) | 0,000 | 0,000 |
| Méta-épidémiologie (sens large) | 0,000 | 0,000 |
| Bibliométrie | 0,000 | 0,000 |
| Études des sciences et des technologies | 0,000 | 0,000 |
| Communication savante | 0,000 | 0,000 |
| Science ouverte | 0,000 | 0,000 |
| Intégrité de la recherche | 0,000 | 0,000 |
| Charge utile insuffisante (le modèle a refusé de juger) | 0,001 | 0,000 |
Scores machine (provisoires)
Les deux têtes enseignantes du modèle étudiant, lues sur ce travail. Un score ordonne la base pour la relecture; il n'affirme jamais une catégorie, et le statut de validation accompagne chaque rangée tel quel.
Scores de référence d'un modèle non mature (critères de maturité non atteints, 7 itérations). Un score ordonne; il n'affirme jamais une catégorie.
score_only:v0-immature-baseline · tel quel depuis la passe de notation : score_only signifie que le nombre peut ordonner les travaux, et qu'aucune étiquette de catégorie n'en découleClassification
machine, non validéePrédiction automatique; un appel candidat d’une seule tête enseignante, pas un consensus.
Le détail, modèle par modèle et score par score, se trouve en fin de page sous « Comment cette classification a été obtenue ».