Sertralinum
| |
| |
| Natura chemica | |
|---|---|
| Formula chemica | Formula:Chem |
| Massa molaris | 306.229 g/mol |
| PubChem | 68617 |
| DrugBank | DB01104 |
| Natura pharmacologica | |
| Codex ATC | Formula:ATC |
| Tempus semivitae biologicum | ~23–26 h |
| Metabolismus | iecore (hepaticus): CYP2B6 |
| Metabolitus | Desmethylo-sertralinum |
| Excretio | renibus |
| Ad usum therapeuticum | |
| Applicatio | per os |
| MedlinePlus | a697048 Formula:Ling |
Sertralinum est substantia psychoanaleptica, antidepressiva et inhibitor reabsorptionis serotonini selectivus. Quae ad conturbationem obsessionem-compulsionem et phobias curandas adhibetur.
Historia
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
Natura chemica
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
Pharmacodynamica
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
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
Toxicitas
Dosis letalis [7] 2800-7000 mg/kg homini (mus: 336) est.
Effectus usu
Reactiones adversae
Notae
- ↑ 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.
- ↑ Formula:Cite journal
- ↑ Shinkei Seishin Yakuri (1997). Neuropsychopharmacology. Bd. 19, S. 395
- ↑ Formula:Cite journal