Peringatan Keamanan

The most commonly reported adverse effects during clinical trials were nausea, diarrhea, and dry mouth. The FDA label includes a blackbox warning for the following risks and complications: serotonin syndrome, especially when combined with other serotonergic agents; increased risk of abnormal bleeding, especially when combined with NSAIDs, aspirin, or other drugs that affect coagulation; activation of mania/hypomania; hyponatremia; and suicidal thoughts and behaviour in children, adolescents, and young adults.

Vortioxetine

DB09068

small molecule approved investigational

Deskripsi

Vortioxetine is an antidepressant medication indicated for the treatment of major depressive disorder (MDD). It is classified as a serotonin modulator and stimulator (SMS) as it has a multimodal mechanism of action towards the serotonin neurotransmitter system whereby it simultaneously modulates one or more serotonin receptors and inhibits the reuptake of serotonin. More specifically, vortioxetine acts via the following biological mechanisms: as a serotonin reuptake inhibitor (SRI) through inhibition of the serotonin transporter, as a partial agonist of the 5-HT1B receptor, an agonist of 5-HT1A, and an antagonist of the 5-HT3, 5-HT1D, and 5-HT7 receptors. SMSs were developed because there are many different subtypes of serotonin receptors, however, not all of these receptors appear to be involved in the antidepressant effects of SRIs. Some serotonin receptors seem to play a relatively neutral or insignificant role in the regulation of mood, but others, such as 5-HT1A autoreceptors and 5-HT7 receptors, appear to play an oppositional role in the efficacy of SRIs in treating depression.

Struktur Molekul 2D

Berat 298.45
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean terminal half­life is approximately 66 hours
Volume Distribusi The apparent volume of distribution of vortioxetine is approximately 2600 L, indicating extensive extravascular distribution.
Klirens (Clearance) -

Absorpsi

The maximal plasma vortioxetine concentration (Cmax) after dosing is reached within 7 to 11 hours postdose. Absolute bioavailability is 75%. No effect of food on the pharmacokinetics was observed.

Metabolisme

Vortioxetine is extensively metabolized primarily through oxidation via cytochrome P450 isozymes CYP2D6, CYP3A4/5, CYP2C19, CYP2C9, CYP2A6, CYP2C8 and CYP2B6 and subsequent glucuronic acid conjugation. CYP2D6 is the primary enzyme catalyzing the metabolism of vortioxetine to its major, pharmacologically inactive, carboxylic acid metabolite, and poor metabolizers of CYP2D6 have approximately twice the vortioxetine plasma concentration of extensive metabolizers.

Rute Eliminasi

Following a single oral dose of 14C­labeled vortioxetine, approximately 59% and 26% of the administered radioactivity was recovered in the urine and feces, respectively as metabolites. Negligible amounts of unchanged vortioxetine were excreted in the urine up to 48 hours.

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Avoid St. John's Wort. When administered with vortioxetine, this herb may increase the risk of serotonin syndrome.
  • 3. Take with or without food.

Interaksi Obat

1965 Data
Ramipril Vortioxetine may decrease the antihypertensive activities of Ramipril.
Remikiren Vortioxetine may decrease the antihypertensive activities of Remikiren.
Guanadrel Vortioxetine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Vortioxetine may decrease the antihypertensive activities of Olmesartan.
Minoxidil Vortioxetine may decrease the antihypertensive activities of Minoxidil.
Prazosin Vortioxetine may decrease the antihypertensive activities of Prazosin.
Trandolapril Vortioxetine may decrease the antihypertensive activities of Trandolapril.
Benazepril Vortioxetine may decrease the antihypertensive activities of Benazepril.
Candoxatril Vortioxetine may decrease the antihypertensive activities of Candoxatril.
Moexipril Vortioxetine may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Vortioxetine may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Vortioxetine may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Vortioxetine may decrease the antihypertensive activities of Eprosartan.
Quinapril Vortioxetine may decrease the antihypertensive activities of Quinapril.
Deserpidine Vortioxetine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Vortioxetine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Vortioxetine may decrease the antihypertensive activities of Trimethaphan.
Bretylium Vortioxetine may decrease the antihypertensive activities of Bretylium.
Terazosin Vortioxetine may decrease the antihypertensive activities of Terazosin.
Cilazapril Vortioxetine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Vortioxetine may decrease the antihypertensive activities of Saprisartan.
Spirapril Vortioxetine may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Vortioxetine may decrease the antihypertensive activities of Dexpropranolol.
Diethylnorspermine Vortioxetine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Vortioxetine may decrease the antihypertensive activities of Temocapril.
Trimazosin Vortioxetine may decrease the antihypertensive activities of Trimazosin.
Rauwolfia serpentina root Vortioxetine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Vortioxetine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Vortioxetine may decrease the antihypertensive activities of Imidapril.
BQ-123 Vortioxetine may decrease the antihypertensive activities of BQ-123.
Dihydralazine Vortioxetine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Vortioxetine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Vortioxetine may decrease the antihypertensive activities of Guanoxan.
Delapril Vortioxetine may decrease the antihypertensive activities of Delapril.
Vincamine Vortioxetine may decrease the antihypertensive activities of Vincamine.
Guanoxabenz Vortioxetine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Vortioxetine may decrease the antihypertensive activities of Tolonidine.
Endralazine Vortioxetine may decrease the antihypertensive activities of Endralazine.
Cadralazine Vortioxetine may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Vortioxetine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Vortioxetine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Vortioxetine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Vortioxetine may decrease the antihypertensive activities of Guanoclor.
Tocopherylquinone Vortioxetine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Vortioxetine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Vortioxetine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Vortioxetine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Vortioxetine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Vortioxetine may decrease the antihypertensive activities of Quinaprilat.
Enalapril Vortioxetine may decrease the antihypertensive activities of Enalapril.
Captopril Vortioxetine may decrease the antihypertensive activities of Captopril.
Nimodipine Vortioxetine may decrease the antihypertensive activities of Nimodipine.
Carvedilol Vortioxetine may decrease the antihypertensive activities of Carvedilol.
Pinacidil Vortioxetine may decrease the antihypertensive activities of Pinacidil.
Aliskiren Vortioxetine may decrease the antihypertensive activities of Aliskiren.
Lacidipine Vortioxetine may decrease the antihypertensive activities of Lacidipine.
Niguldipine Vortioxetine may decrease the antihypertensive activities of Niguldipine.
Dexniguldipine Vortioxetine may decrease the antihypertensive activities of Dexniguldipine.
Amlodipine The metabolism of Vortioxetine can be decreased when combined with Amlodipine.
Azilsartan medoxomil Vortioxetine may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Vortioxetine may decrease the antihypertensive activities of Diazoxide.
Buprenorphine Vortioxetine 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 Vortioxetine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Vortioxetine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Vortioxetine.
Hydrocodone Vortioxetine 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 Vortioxetine.
Magnesium sulfate The therapeutic efficacy of Vortioxetine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Vortioxetine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Vortioxetine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Vortioxetine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Vortioxetine.
Orphenadrine Vortioxetine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Vortioxetine 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 Vortioxetine.
Pramipexole Vortioxetine may increase the sedative activities of Pramipexole.
Ropinirole Vortioxetine may increase the sedative activities of Ropinirole.
Rotigotine Vortioxetine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Vortioxetine.
Sodium oxybate Vortioxetine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Vortioxetine 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 Vortioxetine.
Thalidomide Vortioxetine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Vortioxetine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Yohimbine The therapeutic efficacy of Vortioxetine can be increased when used in combination with Yohimbine.
Dabrafenib The serum concentration of Vortioxetine can be decreased when it is combined with Dabrafenib.
Bethanidine Vortioxetine may decrease the antihypertensive activities of Bethanidine.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Vortioxetine.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Vortioxetine.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Vortioxetine.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Vortioxetine.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Vortioxetine.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Vortioxetine.
Guanabenz Vortioxetine may decrease the antihypertensive activities of Guanabenz.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Vortioxetine.
Tolazoline Vortioxetine may decrease the antihypertensive activities of Tolazoline.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Vortioxetine.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Vortioxetine.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Vortioxetine.
Omapatrilat Vortioxetine may decrease the antihypertensive activities of Omapatrilat.

Target Protein

Sodium-dependent serotonin transporter SLC6A4
5-hydroxytryptamine receptor 3A HTR3A
5-hydroxytryptamine receptor 7 HTR7
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 1A HTR1A
Beta-1 adrenergic receptor ADRB1
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21486038
    Bang-Andersen B, Ruhland T, Jorgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mork A, Stensbol TB: Discovery of 1-2-(2,4-dimethylphenylsulfanyl)phenylpiperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21. doi: 10.1021/jm101459g. Epub 2011 Apr 12.
  • PMID: 23428337
    Stenkrona P, Halldin C, Lundberg J: 5-HTT and 5-HT(1A) receptor occupancy of the novel substance vortioxetine (Lu AA21004). A PET study in control subjects. Eur Neuropsychopharmacol. 2013 Oct;23(10):1190-8. doi: 10.1016/j.euroneuro.2013.01.002. Epub 2013 Feb 18.
  • PMID: 23380522
    Mork A, Montezinho LP, Miller S, Trippodi-Murphy C, Plath N, Li Y, Gulinello M, Sanchez C: Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacol Biochem Behav. 2013 Apr;105:41-50. doi: 10.1016/j.pbb.2013.01.019. Epub 2013 Feb 1.
  • PMID: 22496396
    Hvenegaard MG, Bang-Andersen B, Pedersen H, Jorgensen M, Puschl A, Dalgaard L: Identification of the cytochrome P450 and other enzymes involved in the in vitro oxidative metabolism of a novel antidepressant, Lu AA21004. Drug Metab Dispos. 2012 Jul;40(7):1357-65. doi: 10.1124/dmd.112.044610. Epub 2012 Apr 11.

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