Peringatan Keamanan

The LD50 of sertraline is >2000 mg/kg in rats according to the FDA label.L9061 One other references indicates an oral LD50 of in mice and rats of 419 - 548 mg/kg and 1327 - 1591mg/kg, respectively.MSDS

The most common signs and symptoms associated with a non-fatal sertraline overdose are somnolence, vomiting, tachycardia, nausea, dizziness, agitation, and tremor.L9016 No cases of fatal overdose with only sertraline have been reported. Most fatal cases are associated with the ingestion of sertraline with other drugs.A188499 Consequences of a sertraline overdose may include serotonin syndrome, hypertension, hypotension, syncope, stupor, coma, bradycardia, bundle branch block, QT-prolongation, torsade de pointes, delirium, hallucinations, and pancreatitis.L9016

Sertraline

DB01104

small molecule approved

Deskripsi

Sertraline is a popular antidepressant medication commonly known as a selective serotonin reuptake inhibitor (SSRI), and is similar to drugs such as Citalopram and Fluoxetine. Despite marked structural differences between compounds in this drug class, SSRIs exert similar pharmacological effects.

Several weeks of therapy with sertraline may be required before beneficial effects are noticed. Sertraline displays enhanced safety or tolerability than other classes of antidepressants, which frequently cause high levels of drowsiness, dizziness, blurred vision, and other undesirable effects.A1846,A187075,T28

Struktur Molekul 2D

Berat 306.23
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of sertraline is approximately 26 hours.[A1846,L9016] One reference mentions an elimination half-life ranging from 22-36 hours.[A187066]
Volume Distribusi Sertraline is widely distributed, and its volume of distribution is estimated to be more than 20L/kg.[A1846] Post-mortem studies in humans have measured liver tissue concentrations of 3.9–20 mg/kg for sertraline and between 1.4 to 11 mg/kg for its active metabolite, N-desmethyl-sertraline (DMS).[A187066] Studies have also determined sertraline distributes into the brain, plasma, and serum.[A187066]
Klirens (Clearance) In pharmacokinetic studies, the clearance of a 200mg dose of sertraline in studies of both young and elderly patients ranged between 1.09 ± 0.38 L/h/kg - 1.35 ± 0.67 L/h/kg.[A187066]

Absorpsi

Following once-daily administration of 50 to 200 mg for two weeks, the mean peak plasma concentrations (Cmax) of sertraline occurred between 4.5 to 8.4 hours after administration, and measured at 20 to 55 ?g/L.A1846,L9016 Steady-state concentrations are reached after 1 week following once-daily administration, and vary greatly depending on the patient.A187066,L9016 Bioavailability has been estimated to be above 44%. The area under the curve in healthy volunteers after a 100mg dose of sertraline was 456 ?g × h/mL in one study.A187066 Effects of food on absorption The effects of food on the bioavailability of the sertraline tablet and oral concentrate were studied in subjects given a single dose with and without food. For the tablet, AUC was slightly increased when sertraline was administered with food, the Cmax was 25% greater, and the time to peak plasma concentration was shortened by about 2.5 hours. For the oral concentrate preparation of sertraline, peak concentration was prolonged by approximately 1 hour with the ingestion of food.L9016

Metabolisme

Sertraline is heavily metabolized in the liver and has one major active metabolite. It undergoes N-demethylation to form N-desmethylsertraline, which is much less potent in its pharmacological activity than sertraline.A187066 In addition to N-demethylation, sertraline metabolism involves N-hydroxylation, oxidative deamination, and finally, glucuronidation.L9016 The metabolism of sertraline is mainly catalyzed by CYP3A4 and CYP2B6, with some activity accounted for by CYP2C19 and CYP2D6.A1846,L9022

Rute Eliminasi

Since sertraline is extensively metabolized, excretion of unchanged drug in the urine is a minor route of elimination, with 12-14% of unchanged sertraline excreted in the feces.A1846,A187066,L9016

Farmakogenomik

2 Varian
CYP2C19 (rs4244285)

The presence of this polymorphism in CYP2C19 is associated with poor metabolism of sertraline.

CYP2C19 (rs4986893)

The presence of this polymorphism in CYP2C19 is associated with reduced or poor metabolism of sertraline.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort.
  • 2. Take with or without food.

Interaksi Obat

1470 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Sertraline.
Cyproheptadine The therapeutic efficacy of Sertraline can be decreased when used in combination with Cyproheptadine.
Desmopressin The risk or severity of hyponatremia can be increased when Sertraline is combined with Desmopressin.
Ioflupane I-123 Sertraline may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Sertraline.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Sertraline.
Buprenorphine Sertraline may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Sertraline.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Hydrocodone Sertraline may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Magnesium sulfate The therapeutic efficacy of Sertraline can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Sertraline may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Orphenadrine Sertraline may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Sertraline may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Pramipexole Sertraline may increase the sedative activities of Pramipexole.
Ropinirole Sertraline may increase the sedative activities of Ropinirole.
Rotigotine Sertraline may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Sertraline.
Sodium oxybate Sertraline may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Sertraline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Sertraline.
Thalidomide Sertraline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Sertraline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Sertraline.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Sertraline resulting in a loss in efficacy.
Dabrafenib The serum concentration of Sertraline can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Sertraline can be increased when it is combined with Luliconazole.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Sertraline.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Sertraline.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Sertraline.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Sertraline.
Efavirenz The serum concentration of Sertraline can be decreased when it is combined with Efavirenz.
Disulfiram The risk or severity of adverse effects can be increased when Disulfiram is combined with Sertraline.
Aripiprazole The serum concentration of Aripiprazole can be increased when it is combined with Sertraline.
Aripiprazole lauroxil The serum concentration of Aripiprazole lauroxil can be increased when it is combined with Sertraline.
Darunavir The serum concentration of Sertraline can be decreased when it is combined with Darunavir.
Propafenone Sertraline may increase the QTc-prolonging activities of Propafenone.
Mirabegron The serum concentration of Sertraline can be increased when it is combined with Mirabegron.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Sertraline.
Mirtazapine Sertraline may increase the serotonergic activities of Mirtazapine.
Morphine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Sertraline.
Codeine The risk or severity of serotonin syndrome can be increased when Codeine is combined with Sertraline.
Hydromorphone The risk or severity of serotonin syndrome can be increased when Hydromorphone is combined with Sertraline.
Oxycodone The risk or severity of serotonin syndrome can be increased when Oxycodone is combined with Sertraline.
Butorphanol The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Sertraline.
Dextropropoxyphene The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Sertraline.
Pentazocine The risk or severity of serotonin syndrome can be increased when Pentazocine is combined with Sertraline.
Sufentanil The risk or severity of serotonin syndrome can be increased when Sufentanil is combined with Sertraline.
Nalbuphine The risk or severity of serotonin syndrome can be increased when Nalbuphine is combined with Sertraline.
Levorphanol The risk or severity of serotonin syndrome can be increased when Levorphanol is combined with Sertraline.
Remifentanil The risk or severity of serotonin syndrome can be increased when Remifentanil is combined with Sertraline.
Diphenoxylate The risk or severity of serotonin syndrome can be increased when Diphenoxylate is combined with Sertraline.
Oxymorphone The risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with Sertraline.
Dezocine The risk or severity of serotonin syndrome can be increased when Dezocine is combined with Sertraline.
Methadyl acetate The risk or severity of serotonin syndrome can be increased when Methadyl acetate is combined with Sertraline.
Dihydroetorphine The risk or severity of serotonin syndrome can be increased when Dihydroetorphine is combined with Sertraline.
Diamorphine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Sertraline.
Etorphine The risk or severity of serotonin syndrome can be increased when Etorphine is combined with Sertraline.
Dextromoramide The risk or severity of serotonin syndrome can be increased when Dextromoramide is combined with Sertraline.
Desomorphine The risk or severity of serotonin syndrome can be increased when Desomorphine is combined with Sertraline.
Carfentanil The risk or severity of serotonin syndrome can be increased when Carfentanil is combined with Sertraline.
Dihydrocodeine The risk or severity of serotonin syndrome can be increased when Dihydrocodeine is combined with Sertraline.
Alphacetylmethadol The risk or severity of serotonin syndrome can be increased when Alphacetylmethadol is combined with Sertraline.
Dihydromorphine The risk or severity of serotonin syndrome can be increased when Dihydromorphine is combined with Sertraline.
DPDPE The risk or severity of serotonin syndrome can be increased when DPDPE is combined with Sertraline.
Lofentanil The risk or severity of serotonin syndrome can be increased when Lofentanil is combined with Sertraline.
Opium The risk or severity of serotonin syndrome can be increased when Opium is combined with Sertraline.
Normethadone The risk or severity of serotonin syndrome can be increased when Normethadone is combined with Sertraline.
Piritramide The risk or severity of serotonin syndrome can be increased when Piritramide is combined with Sertraline.
Alphaprodine The risk or severity of serotonin syndrome can be increased when Alphaprodine is combined with Sertraline.
Meptazinol The risk or severity of serotonin syndrome can be increased when Meptazinol is combined with Sertraline.
Phenoperidine The risk or severity of serotonin syndrome can be increased when Phenoperidine is combined with Sertraline.
Phenazocine The risk or severity of serotonin syndrome can be increased when Phenazocine is combined with Sertraline.
Tilidine The risk or severity of serotonin syndrome can be increased when Tilidine is combined with Sertraline.
Carfentanil, C-11 The risk or severity of serotonin syndrome can be increased when Carfentanil, C-11 is combined with Sertraline.
Ethylmorphine The risk or severity of serotonin syndrome can be increased when Ethylmorphine is combined with Sertraline.
Ketobemidone The risk or severity of serotonin syndrome can be increased when Ketobemidone is combined with Sertraline.
Naltrexone The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Sertraline.
Bezitramide The risk or severity of serotonin syndrome can be increased when Bezitramide is combined with Sertraline.
Eluxadoline The risk or severity of serotonin syndrome can be increased when Eluxadoline is combined with Sertraline.
Nicomorphine The risk or severity of serotonin syndrome can be increased when Nicomorphine is combined with Sertraline.
Meperidine The risk or severity of serotonin syndrome can be increased when Meperidine is combined with Sertraline.
Alfentanil The risk or severity of serotonin syndrome can be increased when Alfentanil is combined with Sertraline.
Levacetylmethadol The risk or severity of serotonin syndrome can be increased when Levacetylmethadol is combined with Sertraline.
Benzhydrocodone The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Sertraline.
Fentanyl The risk or severity of serotonin syndrome can be increased when Fentanyl is combined with Sertraline.
Naloxegol The risk or severity of serotonin syndrome can be increased when Naloxegol is combined with Sertraline.
Iobenguane Sertraline may decrease effectiveness of Iobenguane as a diagnostic agent.
Methyclothiazide The risk or severity of hyponatremia can be increased when Sertraline is combined with Methyclothiazide.
Chlorthalidone The risk or severity of hyponatremia can be increased when Sertraline is combined with Chlorthalidone.
Bendroflumethiazide The risk or severity of hyponatremia can be increased when Sertraline is combined with Bendroflumethiazide.
Metolazone The risk or severity of hyponatremia can be increased when Sertraline is combined with Metolazone.
Benzthiazide The risk or severity of hyponatremia can be increased when Sertraline is combined with Benzthiazide.
Hydroflumethiazide The risk or severity of hyponatremia can be increased when Sertraline is combined with Hydroflumethiazide.
Indapamide The risk or severity of hyponatremia can be increased when Sertraline is combined with Indapamide.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent dopamine transporter SLC6A3
Sigma receptor PGRMC1
Sodium-dependent noradrenaline transporter SLC6A2
Equilibrative nucleoside transporter 4 SLC29A4

Referensi & Sumber

Synthesis reference: George J. Quallich, Michael T. Williams, "Process for preparing sertraline intermediates." U.S. Patent US4839104, issued February, 1977.
Artikel (PubMed)
  • PMID: 8573661
    Fabre LF, Abuzzahab FS, Amin M, Claghorn JL, Mendels J, Petrie WM, Dube S, Small JG: Sertraline safety and efficacy in major depression: a double-blind fixed-dose comparison with placebo. Biol Psychiatry. 1995 Nov 1;38(9):592-602.
  • PMID: 10211919
    Kronig MH, Apter J, Asnis G, Bystritsky A, Curtis G, Ferguson J, Landbloom R, Munjack D, Riesenberg R, Robinson D, Roy-Byrne P, Phillips K, Du Pont IJ: Placebo-controlled, multicenter study of sertraline treatment for obsessive-compulsive disorder. J Clin Psychopharmacol. 1999 Apr;19(2):172-6.
  • PMID: 10770145
    Brady K, Pearlstein T, Asnis GM, Baker D, Rothbaum B, Sikes CR, Farfel GM: Efficacy and safety of sertraline treatment of posttraumatic stress disorder: a randomized controlled trial. JAMA. 2000 Apr 12;283(14):1837-44.
  • PMID: 9307345
    Yonkers KA, Halbreich U, Freeman E, Brown C, Endicott J, Frank E, Parry B, Pearlstein T, Severino S, Stout A, Stone A, Harrison W: Symptomatic improvement of premenstrual dysphoric disorder with sertraline treatment. A randomized controlled trial. Sertraline Premenstrual Dysphoric Collaborative Study Group. JAMA. 1997 Sep 24;278(12):983-8.
  • PMID: 7859236
    Shelton RC: The role of sertraline in the management of depression. Clin Ther. 1994 Sep-Oct;16(5):768-82; discussion 767.
  • PMID: 1281075
    Murdoch D, McTavish D: Sertraline. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depression and obsessive-compulsive disorder. Drugs. 1992 Oct;44(4):604-24.
  • PMID: 12452737
    DeVane CL, Liston HL, Markowitz JS: Clinical pharmacokinetics of sertraline. Clin Pharmacokinet. 2002;41(15):1247-66. doi: 10.2165/00003088-200241150-00002.
  • PMID: 25155462
    Cooper JM, Duffull SB, Saiao AS, Isbister GK: The pharmacokinetics of sertraline in overdose and the effect of activated charcoal. Br J Clin Pharmacol. 2015 Feb;79(2):307-15. doi: 10.1111/bcp.12500.
Menampilkan 8 dari 18 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    46. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 573-574). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

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