Sertralinum

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Sertralinum
Sertralinum
Sertralinum
Natura chemica
Formula chemica C
17
H
17
Cl
2
N
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 | fontem 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 | fontem recensere]

Natura chemica[recensere | fontem 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 | fontem recensere]

Pharmacodynamica[recensere | fontem 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 | fontem 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 | fontem recensere]

Toxicitas[recensere | fontem recensere]

Dosis letalis [7] 2800-7000 mg/kg homini (mus: 336) est.

Effectus usu[recensere | fontem recensere]

Reactiones adversae[recensere | fontem recensere]

Crystal 128 up.png Commentatio principalis: Adversa drogae reactio

Nexus interni

Notae[recensere | fontem recensere]

  1. Willard M. Welch (1995). Discovery and preclinical development of the serotonin reuptake inhibitor sertraline. Advances in Medicinal Chemistry 3: 113-148
  2. JJ Li (2009). Triumph of the heart. The Story of Statins. Oxford University Press. Pag. 135
  3. http://www.abcam.com/Sertraline-hydrochloride-ab141068.pdf
  4. 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
  5. Fons.
  6. 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 
  7. Shinkei Seishin Yakuri (1997). Neuropsychopharmacology. Bd. 19, S. 395
  8. Varela Piñón M., Adán-Manes J. (2017). "Selective Serotonin Reuptake Inhibitor-Induced Hyponatremia: Clinical Implications and Therapeutic Alternatives". Clinical neuropharmacology 40 (4): 177-9