Sertralinum

compositum chemicum
Esculaap4.svg
Cave: notitiae huius paginae nec praescriptiones nec consilia medica sunt.
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.

HistoriaRecensere

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 SertraliniRecensere

Natura chemicaRecensere

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 pharmacologicaRecensere

PharmacodynamicaRecensere

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].

PharmacocineticaRecensere

Tempus semivitae biologicum   est circa 25 horae.[5] Sertralinum substratum cytochromatum, imprimis CYP2B6, minor CYP3A4 et CYP2C19, est[6]. Excretio est per urinas.

Usus SertraliniRecensere

ToxicitasRecensere

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

Effectus usuRecensere

Reactiones adversaeRecensere

  Commentatio principalis: Adversa drogae reactio

Nexus interni

NotaeRecensere

  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