Peringatan Keamanan

The oral LD50 of trazodone is 690 mg/kg in rats.L7483

An overdose of trazodone may result in central nervous system, cardiac, respiratory effects. Signs and symptoms may include dyspnea, bradycardia, hypotension, mental status changes, lack of coordination, and coma, among others.L7486 In addition, an overdose may result in priapism, a persistent unrelievable penile tissue erection that may cause permanent damage if not treated promptly.A181198 No specific antidote exists for a trazodone overdose. If an overdose occurs, consider the possibility that trazodone may have been combined with other drugs. Contact a poison control center in case of overdose for the most current management guidelines.L3484 Dialysis does not accelerate trazodone clearance.A181177

Trazodone

DB00656

small molecule approved investigational

Deskripsi

Trazodone is triazolopyridine derivative from the serotonin receptor antagonists and reuptake inhibitors (SARIs) class of antidepressants.A181180 It is used in adults and has been shown to be comparable in efficacy to other drugs such as tricyclic antidepressants (TCAs), selective serotonin reuptake inhibitors (SSRIs), and serotonin-norepinephrine receptor inhibitor (SNRIs) in the treatment of depression.T646 A unique feature of this drug is that it does not promote the anxiety symptoms, sexual symptoms, or insomnia, which are commonly associated with SSRI and SNRI therapy.T646 Trazodone acts on various receptors, including certain histamine, serotonin, and adrenergic receptors, distinguishing it from other antidepressants that cover a narrow range of neurotransmitters.T646 It was initially granted FDA approval in 1981.L3484

Struktur Molekul 2D

Berat 371.864
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma elimination half-life was markedly prolonged (13.6 versus 6 hours) elderly volunteers in the fasted state when compared with younger volunteers.[A181177] Another study of 8 healthy individuals taking a single dose of trazodone indicated a terminal elimination half-life of 7.3 +/- 0.8 hr.[A181201] A two-phase pattern of trazodone elimination has been reported. Initially, the half-life is reported to range from 3 to 6 hours and the second phase of elimination to range from 5 to 9 hours.[L7547]
Volume Distribusi A single-dose pharmacokinetic study of 8 volunteers taking trazodone determined a volume of distribution of 0.84 +/- 0.16 L/kg.[A181201] The FDA medical review of trazodone reports a volume of distribution of 0.47 to 0.84 L/kg.[L7547]
Klirens (Clearance) A decrease in total apparent clearance (5.1 versus 10.8 L/h) was seen elderly volunteers in the fasted state when compared with younger volunteers.[A181177] Another pharmacokinetic study determined the total body clearance of trazodone to be 5.3 +/- 0.9 L/hr in 8 healthy patients taking a single dose of trazodone.[A181201]

Absorpsi

Trazodone is rapidly absorbed in the gastrointestinal tract after oral administration, with a bioavailability ranging from 63-91% A181177 and an AUC0?t of 18193.0 ng·h/mL.A181204 Food may impact absorption in a variable fashion, and may sometimes lead to decreases in the Cmax of trazodone.A181177,A181201 In the fed state in 8 healthy volunteers, the Cmax was measured to be 1.47 +/- 0.16 micrograms/mL, and in the fasted state, was measured at 1.88 +/- 0.42 micrograms/mL. The average Tmax after a single dose of 300 mg was 8 hours. Food may increase absorption by up to 20%.L7547

Metabolisme

Trazodone is heavily metabolized and activated in the liver by CYP3A4 enzyme to the active metabolite, m-chlorophenylpiperazine (mCPP).A987,A988 The full metabolism of trazodone has not been well characterized.L7483 Some other metabolites that have been identified are a dihydrodiol metabolite and carboxylic acid.A986

Rute Eliminasi

Less than 1% of an oral dose is excreted unchanged in the urine.L7483 In a pharmacokinetic study, about 60-70% of radiolabeled was excreted urine within 48 hours. Approximately 9-29% was found to be excreted in feces over a range of 60 to 100 hours.L7483 According to the FDA medical review, the kidneys are responsible for 70 to 75% of trazodone excretion. About 21% of trazodone is reported to be excreted by the fecal route and 0.13% of the parent drug is eliminated in the urine as unchanged drug.L7547

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Avoid St. John's Wort. The risk of serotonin syndrome may be increased.
  • 3. Take after a meal. Should be taken shortly after a light meal or snack.

Interaksi Obat

1760 Data
Desmopressin The risk or severity of hyponatremia can be increased when Trazodone is combined with Desmopressin.
Ioflupane I-123 Trazodone 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 Trazodone.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Trazodone.
Pimozide The risk or severity of QTc prolongation can be increased when Trazodone is combined with Pimozide.
Valsartan Trazodone may decrease the antihypertensive activities of Valsartan.
Ramipril Trazodone may decrease the antihypertensive activities of Ramipril.
Remikiren Trazodone may decrease the antihypertensive activities of Remikiren.
Torasemide Trazodone may decrease the antihypertensive activities of Torasemide.
Guanadrel Trazodone may decrease the antihypertensive activities of Guanadrel.
Olmesartan Trazodone may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Trazodone may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Trazodone may decrease the antihypertensive activities of Minoxidil.
Fosinopril Trazodone may decrease the antihypertensive activities of Fosinopril.
Trandolapril Trazodone may decrease the antihypertensive activities of Trandolapril.
Benazepril Trazodone may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Trazodone may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Trazodone may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Trazodone may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Trazodone may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Trazodone may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Trazodone may decrease the antihypertensive activities of Cryptenamine.
Perindopril Trazodone may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Trazodone may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Trazodone may decrease the antihypertensive activities of Fenoldopam.
Eprosartan Trazodone may decrease the antihypertensive activities of Eprosartan.
Quinapril Trazodone may decrease the antihypertensive activities of Quinapril.
Telmisartan Trazodone may decrease the antihypertensive activities of Telmisartan.
Deserpidine Trazodone may decrease the antihypertensive activities of Deserpidine.
Pentolinium Trazodone may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Trazodone may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Trazodone may decrease the antihypertensive activities of Diazoxide.
Cilazapril Trazodone may decrease the antihypertensive activities of Cilazapril.
Saprisartan Trazodone may decrease the antihypertensive activities of Saprisartan.
Spirapril Trazodone may decrease the antihypertensive activities of Spirapril.
Tienilic acid Trazodone may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Trazodone may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Trazodone may decrease the antihypertensive activities of Temocapril.
Nicorandil Trazodone may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Trazodone may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Trazodone may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Trazodone may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Trazodone may decrease the antihypertensive activities of Imidapril.
BQ-123 Trazodone may decrease the antihypertensive activities of BQ-123.
Dihydralazine Trazodone may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Trazodone may decrease the antihypertensive activities of Zofenopril.
Guanoxan Trazodone may decrease the antihypertensive activities of Guanoxan.
Delapril Trazodone may decrease the antihypertensive activities of Delapril.
Vincamine Trazodone may decrease the antihypertensive activities of Vincamine.
Guanoxabenz Trazodone may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Trazodone may decrease the antihypertensive activities of Tolonidine.
Endralazine Trazodone may decrease the antihypertensive activities of Endralazine.
Cadralazine Trazodone may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Trazodone may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Trazodone may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Trazodone may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Trazodone may decrease the antihypertensive activities of Guanoclor.
Muzolimine Trazodone may decrease the antihypertensive activities of Muzolimine.
Xipamide Trazodone may decrease the antihypertensive activities of Xipamide.
Candesartan Trazodone may decrease the antihypertensive activities of Candesartan.
Benazeprilat Trazodone may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Trazodone may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Trazodone may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Trazodone may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Trazodone may decrease the antihypertensive activities of Quinaprilat.
Furosemide Trazodone may decrease the antihypertensive activities of Furosemide.
Enalapril Trazodone may decrease the antihypertensive activities of Enalapril.
Captopril Trazodone may decrease the antihypertensive activities of Captopril.
Bosentan Trazodone may decrease the antihypertensive activities of Bosentan.
Irbesartan Trazodone may decrease the antihypertensive activities of Irbesartan.
Guanethidine Trazodone may decrease the antihypertensive activities of Guanethidine.
Hydralazine Trazodone may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Trazodone may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Trazodone may decrease the antihypertensive activities of Pinacidil.
Riociguat Trazodone may decrease the antihypertensive activities of Riociguat.
Macitentan Trazodone may decrease the antihypertensive activities of Macitentan.
Aliskiren Trazodone may decrease the antihypertensive activities of Aliskiren.
Selexipag Trazodone may decrease the antihypertensive activities of Selexipag.
Buthiazide Trazodone may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Trazodone may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Trazodone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Trazodone.
Hydrocodone Trazodone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Trazodone can be increased when used in combination with Magnesium sulfate.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Trazodone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Trazodone.
Paraldehyde Trazodone 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 Trazodone.
Pramipexole Trazodone may increase the sedative activities of Pramipexole.
Ropinirole Trazodone may increase the sedative activities of Ropinirole.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Trazodone.
Sodium oxybate Trazodone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Trazodone 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 Trazodone.
Thalidomide Trazodone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Trazodone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Trazodone.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Trazodone.
Phenmetrazine The risk or severity of hypertension can be increased when Trazodone is combined with Phenmetrazine.
Omapatrilat Trazodone may decrease the antihypertensive activities of Omapatrilat.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
Sodium-dependent serotonin transporter SLC6A4
5-hydroxytryptamine receptor 1A HTR1A
Histamine H1 receptor HRH1
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
5-hydroxytryptamine receptor 2C Htr2c

Referensi & Sumber

Artikel (PubMed)
  • PMID: 1365657
    Marek GJ, McDougle CJ, Price LH, Seiden LS: A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action. Psychopharmacology (Berl). 1992;109(1-2):2-11.
  • PMID: 1037253
    Jauch R, Kopitar Z, Prox A, Zimmer A: Pharmacokinetics and metabolism of trazodone in man (author's transl). Arzneimittelforschung. 1976;26(11):2084-9.
  • PMID: 9616194
    Rotzinger S, Fang J, Baker GB: Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metab Dispos. 1998 Jun;26(6):572-5.
  • PMID: 15978881
    Kalgutkar AS, Henne KR, Lame ME, Vaz AD, Collin C, Soglia JR, Zhao SX, Hop CE: Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4. Chem Biol Interact. 2005 Jun 30;155(1-2):10-20. Epub 2005 Apr 18.
  • PMID: 7673654
    Otani K, Yasui N, Kaneko S, Ishida M, Ohkubo T, Osanai T, Sugawara K, Fukushima Y: Trazodone treatment increases plasma prolactin concentrations in depressed patients. Int Clin Psychopharmacol. 1995 Jun;10(2):115-7.
  • PMID: 11817501
    Saletu-Zyhlarz GM, Abu-Bakr MH, Anderer P, Gruber G, Mandl M, Strobl R, Gollner D, Prause W, Saletu B: Insomnia in depression: differences in objective and subjective sleep and awakening quality to normal controls and acute effects of trazodone. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Feb;26(2):249-60.
  • PMID: 12930437
    Fink HA, MacDonald R, Rutks IR, Wilt TJ: Trazodone for erectile dysfunction: a systematic review and meta-analysis. BJU Int. 2003 Sep;92(4):441-6.
  • PMID: 29333613
    Davis JL, Schirmer J, Medlin E: Pharmacokinetics, pharmacodynamics and clinical use of trazodone and its active metabolite m-chlorophenylpiperazine in the horse. J Vet Pharmacol Ther. 2018 Jun;41(3):393-401. doi: 10.1111/jvp.12477. Epub 2018 Jan 14.
Menampilkan 8 dari 19 artikel.
Textbook
  • Justin J. Shin; Abdolreza Saadabadi. (2019). Trazodone, StatPearls. Stat Pearls.

Contoh Produk & Brand

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