Monograph
N06AB06 - Sertraline |
Propably not porphyrinogenic |
PNP |
Important Information
Risk for gastrointestinal adverse events in the form of nausea and diarrhoea motivates vigilance against insufficient intake of food, especially of carbohydrate.
Side effects
Common adverse reactions of sertraline that can be confused with an acute porphyric attack are diarrhoea, nausea, vomiting, constipation, abdominal pains and decreased appetite. These side effects may potentially be porphyrinogenic if leading to a decrease in carbohydrate intake.
Rationale
Sertraline is not suspected to be an inducer of CYP450 enzymes. Although sertraline has been reported to be a mechanism-based inhibitor of CYP3A4 in vitro, this was not found to be clinically relevant. No pharmacokinetic porphyrinogenic effects are thus suspected.
Chemical description
Naphthalenamine derivative
Therapeutic characteristics
Sertraline is a selective serotonin reuptake inhibitor (SSRI) indicated for the treatment of depression, panic disorder, obsessive compulsive disorder, social anxiety disorder and post-traumatic stress disorder. It is administered orally.
Metabolism and pharmacokinetics
Sertraline is metabolized by CYP3A4, 2C19 and 2B6, and the main pathway is demethylation to inactive desmethylsertraline (SPC).
In vitro, sertraline is reported to be an inhibitor of CYP2D6, 3A4 and 2B6, but only the inhibition of CYP2D6 is found to be clinically significant (DeVane 2002). Sertraline is classified as a weak inhibitor of CYP2D6 in vivo (FDA, Liston 2002). This drug possesses a secondary amine group, which is a common structure generating MI complexes causing mechanism-based inhibition (Fontana 2005). An in vitro study found that sertraline was a mechanism-based inhibitor of CYP3A4 (Masubuchi 2013). However, this was at concentrations much higher than plasma concentrations obtained in clinical use, and sertraline is not suspected to be an inhibitor of CYP3A4 in vivo (Preskorn 1997, Hassan 2000).
In vivo interaction studies also report that sertraline is not an inhibitor of CYP2C9 and 2C19 (SPC), and not an inducer of CYP3A4 (DeVane 2004).
Published experience
One case report of uneventful use in a patient with manifest AIP (Holroyd 1999).
IPNet drug reports
Uneventful use reported in 4 patients with acute porphyria.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Fontana E1, Dansette PM, et al. Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
Curr Drug Metab. 2005 Oct;6(5):413-54 |
|
| 2. | The Impact of Sertraline Co-Administration on the Pharmacokinetics of Olanzapine: A Population Pharmacokinetic Analysis of the STOP-PD.
Davies SJ, Mulsant BH, et al. Clin Pharmacokinet. 2015 May 14 |
25971243 |
| 3. | Comparative CYP3A4 inhibitory effects of venlafaxine, fluoxetine, sertraline, and nefazodone in healthy volunteers.
DeVane CL, Donovan JL, et al. J Clin Psychopharmacol. 2004 Feb;24(1):4-10. |
14709940 |
| 4. | Clinical pharmacokinetics of sertraline.
DeVane CL, Liston HL, et al. Clin Pharmacokinet. 2002;41(15):1247-66. |
|
| 5. | Dose-response evaluation of the interaction between sertraline and alprazolam in vivo.
Hassan PC, Sproule BA, et al. J Clin Psychopharmacol. 2000 Apr;20(2):150-8. |
10770452 |
| 6. | Psychotropic drugs in acute intermittent porphyria.
Holroyd S, Seward RL. Clin Pharmacol Ther. 1999 Sep;66(3):323-5. |
10511069 |
| 7. | Differential time course of cytochrome P450 2D6 enzyme inhibition by fluoxetine, sertraline, and paroxetine in healthy volunteers.
Liston HL, DeVane CL, et al. J Clin Psychopharmacol. 2002 Apr;22(2):169-73. |
11910262 |
| 8. | Time-dependent inhibition of CYP3A4 by sertraline, a selective serotonin reuptake inhibitor.
Masubuchi Y, Kawaguchi Y. Biopharm Drug Dispos. 2013 Nov;34(8):423-30. |
23929629 |
| 9. | Sertraline does not inhibit cytochrome P450 3A-mediated drug metabolism in vivo.
Preskorn SH, Alderman J, et al. Psychopharmacol Bull. 1997;33(4):659-65. |
|
| * | Summary of Product Characteristics | |
| 10. | The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Lustral).
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Tradenames
This list comprises raw data collected from different countries.
In some cases, a more comprehensive list of available drug packages is included.
Consequently, very similar terms may therefore appear multiple times.
Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors.
We strive to improve it continuously.
Asentra 100 mg filmomhulde tabletten · Asentra 50 mg filmomhulde tabletten · Sertraline Accord 100 mg filmomhulde tabletten · Sertraline Accord 50 mg filmomhulde tabletten · Sertraline Amarox 100 mg, filmomhulde tabletten · Sertraline Amarox 25 mg, filmomhulde tabletten · Sertraline Amarox 50 mg, filmomhulde tabletten · Sertraline Aurobindo 100 mg, filmomhulde tabletten · Sertraline Aurobindo 50 mg, filmomhulde tabletten · Sertraline BModesto 20 mg/ml, concentraat voor oplossing voor oraal gebruik · Sertraline ERC 20 mg/ml, concentraat voor oplossing voor oraal gebruik · Sertraline Krka 100 mg filmomhulde tabletten · Sertraline Krka 50 mg filmomhulde tabletten · Sertraline Mylan 100 mg, filmomhulde tabletten · Sertraline Mylan 50 mg, filmomhulde tabletten · Sertraline RIA 100 mg, filmomhulde tabletten · Sertraline RIA 50 mg, filmomhulde tabletten · Sertraline Sandoz 50 mg, filmomhulde tabletten · Sertraline SUN 50 mg, filmomhulde tabletten · Sertraline Viatris 100 mg, filmomhulde tabletten · Sertraline Viatris 20 mg/ml, concentraat voor oplossing voor oraal gebruik · Sertraline Viatris 25 mg, filmomhulde tabletten · Sertraline Viatris 50 mg, filmomhulde tabletten · Sertraline Xiromed 100 mg filmomhulde tabletten · Sertraline Xiromed 200 mg filmomhulde tabletten · Sertraline Xiromed 25 mg filmomhulde tabletten · Sertraline Xiromed 50 mg filmomhulde tabletten · Zoloft 100, filmomhulde tabletten 100 mg · Zoloft 20 mg/ml, concentraat voor oplossing voor oraal gebruik · Zoloft 25, filmomhulde tabletten 25 mg · Zoloft 50, filmomhulde tabletten 50 mg 
Serlain 100 mg compr. pellic. · Serlain 50 mg (PI Pharma) compr. pellic. · Serlain 50 mg compr. pellic. · Sertraline AB 100 mg compr. pellic. · Sertraline AB 50 mg compr. pellic. · Sertraline EG 100 mg (PI Pharma) compr. pellic. · Sertraline EG 100 mg compr. pellic. · Sertraline EG 50 mg (PI Pharma) compr. pellic. · Sertraline EG 50 mg compr. pellic. · Sertraline Sandoz 100 mg compr. pellic. · Sertraline Sandoz 50 mg compr. pellic. · Sertraline Teva 100 mg compr. pellic. · Sertraline Teva 50 mg compr. pellic. · Sertraline Viatris 100 mg compr. pellic. · Sertraline Viatris 50 mg compr. pellic. 
Altisben · ALTISBEN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Aremis · AREMIS 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · ASERIN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · ASERIN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · BESITRAN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · BESITRAN 20 mg/ml CONCENTRADO PARA SOLUCION ORAL · BESITRAN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · Semonic 150 mg Comprimidos Recubiertos con Pelicula · Semonic 200 mg Comprimidos Recubiertos con Pelicula · Sertralina · SERTRALINA ALMUS 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA ALMUS 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA ALTER 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA ALTER 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Apotex 100 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA ARISTO 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA AUROBINDO 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA AUROBINDO 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Aurovitas 50 mg Comprimidos Recubiertos con Pelicula efg · Sertralina Bluefish 100 mg Comprimidos Recubiertos con Pelicula efg · Sertralina Bluefish 50 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA CINFA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Cinfa 150 mg Comprimidos Recubiertos con Pelicula · Sertralina Cinfa 200 mg Comprimidos Recubiertos con Pelicula · SERTRALINA CINFA 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA CUVE 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA CUVE 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA DAVUR 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA DAVUR 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA KERN PHARMA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA KERN PHARMA 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA MABO 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA NORMON 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA NORMON 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA PENSA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA PENSA 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA PHARMA COMBIX 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA PHARMAGENUS 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA QUALIGEN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA QUALIGEN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Qualigen Farma100 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA SANDOZ 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA SANDOZ 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA SANDOZ FARMAC?UTICA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA SANDOZ FARMAC?UTICA 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA STADA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA SUN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA TARBIS 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA TARBIS 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Tarbis Farma 50 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA TECNIGEN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA TECNIGEN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Teva-Ratio 100 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA TEVAGEN 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA TEVAGEN 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Sertralina Viatris 100 mg Comprimidos Recubiertos con Pelicula efg · Sertralina Viatris 50 mg Comprimidos Recubiertos con Pelicula efg · SERTRALINA VIR PHARMA 100 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · SERTRALINA VIR PHARMA 50 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG 
Sertralina · Tatig · Zoloft 
ASENTRA 100 mg · ASENTRA 50 mg · SERLIFT 100 mg · SERLIFT 50 mg · SERTRALINA ARENA 100 mg · SERTRALINA ARENA 50 mg · SERTRALINA GEMAX PHARMA 50 mg · SERTRALINA GEMAX PHARMA100 mg · STIMULOTON 100 mg · STIMULOTON 50 mg · ZOLOFT 100 mg · ZOLOFT 20 mg/ml · ZOLOFT 50 mg 
Contulen · Lustral · Sertraline 
Sertralin 2care4 · Sertralin Accord · Sertralin Hexal · Sertralin KRKA · Sertralin Orion · Sertralin Teva · Sertralin Zentiva · Sertraline Medical Valley · Sertraline Orifarm · Sertramyl · Sertrix · Sertrone · Zoloft 
Sertralin Bluefish · Sertralin Hexal · Sertralin Zentiva · Sertraline Accord · Sertraline amarox · Sertraline arrow · Zoloft 
Apiolin · ApoSerta · Asentra · Asertin 100 · Asertin 50 · Miravil · Sastium · Sertagen · Sertralina Krka · Sertraline Medical Valley · Sertraline Medreg · Sertraline Zentiva · Sertranorm · Setaloft 100 mg · Setaloft 50 mg · Stimuloton · Zoloft · Zotral 
Serlain · Sertralin-Ratiopharm · Sertraline eg · Sertraline Viatris 
Sertral · Sertralin Bluefish · Sertralin Krka · Sertralin WH · Zoloft 
Sertralin Hexal · Sertralin Krka · Sertralin Orion · Sertralin ratiopharm · Sertraline Accord · Zoloft 
Asentra · Sertralin Actavis · Sertraline Accord · Sertraline Lannacher · Zoloft 
Asentra® · Sidata® · Zoloft®
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