Sertralinum
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Natura chemica | |
---|---|
Formula chemica | C 17H 17Cl 2N |
Massa molaris | 306.229 g/mol |
PubChem | 68617 |
DrugBank | DB01104 |
Natura pharmacologica | |
Codex ATC | N06AB06 (WHO) |
Tempus semivitae biologicum | ~23–26 h |
Metabolismus | iecore (hepaticus): CYP2B6 |
Metabolitus | Desmethylo-sertralinum |
Excretio | renibus |
Ad usum therapeuticum | |
Applicatio | per os |
MedlinePlus | a697048 (Anglice) |
Sertralinum est substantia psychoanaleptica, antidepressiva et inhibitor reabsorptionis serotonini selectivus. Quae ad conturbationem obsessionem-compulsionem et phobias curandas adhibetur.
Historia recensere
Anno 1978 chemicus Willard Welsh societatis Pfizer mixturam Sertralini et enantiomerium eius fecit[1][2]. Intra unum mensem Welsh enantiomeres inactivos removit, ut Sertralinum primus inhibitor reabsorptionis Serotonini selectivus purus fuerit. Anno 1991 Sertralinum in mercatum introductum est.
Natura Sertralini recensere
Natura chemica recensere
Sertralinum est naphtylaminum cuius structura chemica (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-aminum et massa molaris 306.229 g/mol est. Codex ATC est N06AB06.
Natura pharmacologica recensere
Pharmacodynamica recensere
Sertralinum imprimis inhibitor reabsorptionis serotonini affinitate sui notate cum transportatro serotonini (SERT) est, Ki = 2.0 habens[3]. Novem mg/die sufficit ut transportatrorum dimidium serotonini impediatur[4].
Pharmacocinetica recensere
Tempus semivitae biologicum est circa 25 horae.[5] Sertralinum substratum cytochromatum, imprimis CYP2B6, minor CYP3A4 et CYP2C19, est[6]. Excretio est per urinas.
Usus Sertralini recensere
Toxicitas recensere
Effectus usu recensere
Reactiones adversae recensere
Nexus interni
Notae recensere
- ↑ Willard M. Welch (1995). Discovery and preclinical development of the serotonin reuptake inhibitor sertraline. Advances in Medicinal Chemistry 3: 113-148
- ↑ JJ Li (2009). Triumph of the heart. The Story of Statins. Oxford University Press. Pag. 135
- ↑ http://www.abcam.com/Sertraline-hydrochloride-ab141068.pdf
- ↑ Meyer JH, Wilson AA, Sagrati S, Hussey D, Carella A, Potter WZ, Ginovart N, Spencer EP, Cheok A, Houle S (2004). Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [11C]DASB positron emission tomography study. Am J Psych 161 (5): 826–35
- ↑ Fons.
- ↑ Obach R. S., Cox L. M., Tremaine L. M. (2005). "Sertraline is metabolized by multiple cytochrome P450 enzymes, monoamine oxidases, and glucuronyl transferases in human: an in vitro study". Drug Metab Dispos 33 (2): 262-70
- ↑ Shinkei Seishin Yakuri (1997). Neuropsychopharmacology. Bd. 19, S. 395
- ↑ Varela Piñón M., Adán-Manes J. (2017). "Selective Serotonin Reuptake Inhibitor-Induced Hyponatremia: Clinical Implications and Therapeutic Alternatives". Clinical neuropharmacology 40 (4): 177-9