Sertralinum

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**Sertralinum**
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

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, K_i = 2.0 habens^[3]. Novem mg/die sufficit ut transportatrorum dimidium serotonini impediatur^[4].

Pharmacocinetica

Tempus semivitae biologicum $t_{\frac {1}{2}}$ 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

Conferatur pagina principalis: Adversa drogae reactio.

Hyponatraemia^[8]

Nexus interni

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.
↑ 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

[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] ttp://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

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