Peringatan Keamanan

There are several published case reports of tianeptine intoxication and death L1435. An overdose of tianeptine can lead to opiod-like effects and lead to respiratory failure and death, due to its direct effect on the mu opioid receptor L1435. In addition, cardiotoxicity can result from an overdose of this medication L1435.

Tianeptine

DB09289

small molecule investigational

Deskripsi

Tianeptine is a drug used primarily in the treatment of major depressive disorder and has been studied in the treatment of irritable bowel syndrome (IBS) A31983. Structurally, it is classified as a tricyclic antidepressant (TCA), however, it possesses different pharmacological properties than typical tricyclic antidepressants A31969.

Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s L2946. Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in several other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S.

Struktur Molekul 2D

Berat 436.952
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 2.5 h [A33320]
Volume Distribusi 0.8 L/kg (0.77 +/- 0.31 L/kg) [A33320]
Klirens (Clearance) Rapidly cleared by the kidneys [L1429].

Absorpsi

Well absorbed, approximately 99% bioavailability A31998.

Metabolisme

Tianeptine is metabolized primarily by beta-oxidation of its heptanoic side chain A31992. The metabolism of tianeptine was studied after a one-time oral administration of radioisotopically (14C) labeled compound to healthy male volunteers. After 1 week, approximately 66% of the dose was eliminated by the kidneys (55% elimination during the first 24 hr). After 24h, unchanged drug 3% of the drug was found unchanged in the urine. Three major metabolites result from beta-oxidation of Tianeptine. The metabolite profiles of tianeptine in feces and plasma were found to be qualitatively similar to that in urine A31993.

Rute Eliminasi

Eliminated with bile as glucuronide and glutamine conjugates A32000.

Interaksi Makanan

2 Data
  • 1. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of tianeptine.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A metabolism, which may reduce serum levels of tianeptine.

Interaksi Obat

1723 Data
Modafinil The metabolism of Tianeptine can be increased when combined with Modafinil.
Armodafinil The metabolism of Tianeptine can be increased when combined with Armodafinil.
Valsartan Tianeptine may decrease the antihypertensive activities of Valsartan.
Ramipril Tianeptine may decrease the antihypertensive activities of Ramipril.
Esmolol Tianeptine may decrease the antihypertensive activities of Esmolol.
Betaxolol Tianeptine may decrease the antihypertensive activities of Betaxolol.
Remikiren Tianeptine may decrease the antihypertensive activities of Remikiren.
Torasemide Tianeptine may decrease the antihypertensive activities of Torasemide.
Guanadrel Tianeptine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Tianeptine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Tianeptine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Tianeptine may decrease the antihypertensive activities of Nitroprusside.
Atenolol Tianeptine may decrease the antihypertensive activities of Atenolol.
Minoxidil Tianeptine may decrease the antihypertensive activities of Minoxidil.
Timolol Tianeptine may decrease the antihypertensive activities of Timolol.
Treprostinil Tianeptine may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Tianeptine may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Tianeptine may decrease the antihypertensive activities of Prazosin.
Fosinopril Tianeptine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Tianeptine may decrease the antihypertensive activities of Trandolapril.
Metolazone Tianeptine may decrease the antihypertensive activities of Metolazone.
Benazepril Tianeptine may decrease the antihypertensive activities of Benazepril.
Labetalol Tianeptine may decrease the antihypertensive activities of Labetalol.
Cyclothiazide Tianeptine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Tianeptine may decrease the antihypertensive activities of Candoxatril.
Moexipril Tianeptine may decrease the antihypertensive activities of Moexipril.
Lisinopril Tianeptine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Tianeptine may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Tianeptine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Tianeptine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Tianeptine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Tianeptine may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Tianeptine may decrease the antihypertensive activities of Fenoldopam.
Chlorothiazide Tianeptine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Tianeptine may decrease the antihypertensive activities of Quinapril.
Telmisartan Tianeptine may decrease the antihypertensive activities of Telmisartan.
Hydrochlorothiazide Tianeptine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Tianeptine may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Tianeptine may decrease the antihypertensive activities of Deserpidine.
Diazoxide Tianeptine may decrease the antihypertensive activities of Diazoxide.
Bretylium Tianeptine may decrease the antihypertensive activities of Bretylium.
Terazosin Tianeptine may decrease the antihypertensive activities of Terazosin.
Acebutolol Tianeptine may decrease the antihypertensive activities of Acebutolol.
Nadolol Tianeptine may decrease the antihypertensive activities of Nadolol.
Epoprostenol Tianeptine may decrease the antihypertensive activities of Epoprostenol.
Bevantolol Tianeptine may decrease the antihypertensive activities of Bevantolol.
Practolol Tianeptine may decrease the antihypertensive activities of Practolol.
Polythiazide Tianeptine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Tianeptine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Tianeptine may decrease the antihypertensive activities of Saprisartan.
Spirapril Tianeptine may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Tianeptine may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Tianeptine may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Tianeptine may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Tianeptine may decrease the antihypertensive activities of Diethylnorspermine.
Bupranolol Tianeptine may decrease the antihypertensive activities of Bupranolol.
Temocapril Tianeptine may decrease the antihypertensive activities of Temocapril.
Indenolol Tianeptine may decrease the antihypertensive activities of Indenolol.
Trimazosin Tianeptine may decrease the antihypertensive activities of Trimazosin.
Rauwolfia serpentina root Tianeptine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Tianeptine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Tianeptine may decrease the antihypertensive activities of Angiotensin 1-7.
Talinolol Tianeptine may decrease the antihypertensive activities of Talinolol.
Imidapril Tianeptine may decrease the antihypertensive activities of Imidapril.
BQ-123 Tianeptine may decrease the antihypertensive activities of BQ-123.
Landiolol Tianeptine may decrease the antihypertensive activities of Landiolol.
Cicletanine Tianeptine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Tianeptine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Tianeptine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Tianeptine may decrease the antihypertensive activities of Guanoxan.
Delapril Tianeptine may decrease the antihypertensive activities of Delapril.
Vincamine Tianeptine may decrease the antihypertensive activities of Vincamine.
Linsidomine Tianeptine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Tianeptine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Tianeptine may decrease the antihypertensive activities of Tolonidine.
Endralazine Tianeptine may decrease the antihypertensive activities of Endralazine.
Esatenolol Tianeptine may decrease the antihypertensive activities of Esatenolol.
Cadralazine Tianeptine may decrease the antihypertensive activities of Cadralazine.
Cloranolol Tianeptine may decrease the antihypertensive activities of Cloranolol.
Cyclopenthiazide Tianeptine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Tianeptine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Tianeptine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Tianeptine may decrease the antihypertensive activities of Methoserpidine.
Epanolol Tianeptine may decrease the antihypertensive activities of Epanolol.
Guanoclor Tianeptine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Tianeptine may decrease the antihypertensive activities of Muzolimine.
Xipamide Tianeptine may decrease the antihypertensive activities of Xipamide.
Candesartan Tianeptine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Tianeptine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Tianeptine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Tianeptine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Tianeptine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Tianeptine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Tianeptine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Tianeptine may decrease the antihypertensive activities of Furosemide.
Amlodipine The metabolism of Tianeptine can be decreased when combined with Amlodipine.
Nimodipine Tianeptine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Tianeptine may decrease the antihypertensive activities of Nisoldipine.
Propranolol Tianeptine may decrease the antihypertensive activities of Propranolol.
Bisoprolol Tianeptine may decrease the antihypertensive activities of Bisoprolol.

Target Protein

Mu-type opioid receptor OPRM1
Sodium-dependent serotonin transporter SLC6A4
Glutamate receptor 1 GRIA1
5-hydroxytryptamine receptor 1A HTR1A
D(3) dopamine receptor DRD3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7774514
    Wilde MI, Benfield P: Tianeptine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depression and coexisting anxiety and depression. Drugs. 1995 Mar;49(3):411-39.
  • PMID: 12372016
    Kole MH, Swan L, Fuchs E: The antidepressant tianeptine persistently modulates glutamate receptor currents of the hippocampal CA3 commissural associational synapse in chronically stressed rats. Eur J Neurosci. 2002 Sep;16(5):807-16.
  • PMID: 22679908
    Sohn W, Lee OY, Kwon JG, Park KS, Lim YJ, Kim TH, Jung SW, Kim JI: Tianeptine vs amitriptyline for the treatment of irritable bowel syndrome with diarrhea: a multicenter, open-label, non-inferiority, randomized controlled study. Neurogastroenterol Motil. 2012 Sep;24(9):860-e398. doi: 10.1111/j.1365-2982.2012.01945.x. Epub 2012 Jun 11.
  • PMID: 17368617
    Reagan LP, Hendry RM, Reznikov LR, Piroli GG, Wood GE, McEwen BS, Grillo CA: Tianeptine increases brain-derived neurotrophic factor expression in the rat amygdala. Eur J Pharmacol. 2007 Jun 22;565(1-3):68-75. doi: 10.1016/j.ejphar.2007.02.023. Epub 2007 Feb 20.
  • PMID: 1660816
    Delbende C, Contesse V, Mocaer E, Kamoun A, Vaudry H: The novel antidepressant, tianeptine, reduces stress-evoked stimulation of the hypothalamo-pituitary-adrenal axis. Eur J Pharmacol. 1991 Sep 24;202(3):391-6.
  • PMID: 25759404
    Cooper CM, Whiting DA, Cowen PJ, Harmer CJ: Tianeptine in an experimental medicine model of antidepressant action. J Psychopharmacol. 2015 May;29(5):582-90. doi: 10.1177/0269881115573810. Epub 2015 Mar 10.
  • PMID: 2597170
    Fromenty B, Freneaux E, Labbe G, Deschamps D, Larrey D, Letteron P, Pessayre D: Tianeptine, a new tricyclic antidepressant metabolized by beta-oxidation of its heptanoic side chain, inhibits the mitochondrial oxidation of medium and short chain fatty acids in mice. Biochem Pharmacol. 1989 Nov 1;38(21):3743-51.
  • PMID: 1981739
    Grislain L, Gele P, Bertrand M, Luijten W, Bromet N, Salvadori C, Kamoun A: The metabolic pathways of tianeptine, a new antidepressant, in healthy volunteers. Drug Metab Dispos. 1990 Sep-Oct;18(5):804-8.
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Contoh Produk & Brand

Produk: 0 • International brands: 7
International Brands
  • Coaxil
  • Neptine — Hanmi South Korea
  • Salymbra
  • Stablon
  • Tatinol
  • Tianeurax
  • Zinosal

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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