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药品详细

Trazodone(曲唑酮)

化学结构式图
中文名
曲唑酮
英文名
Trazodone
分子式
C19H22ClN5O
化学名
2-{3-[4-(3-chlorophenyl)piperazin-1-yl]propyl}-2H,3H-[1,2,4]triazolo[4,3-a]pyridin-3-one
分子量
Average: 371.864
Monoisotopic: 371.151288058
CAS号
19794-93-5
ATC分类
N06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309)

生产厂家
  • Alvogen inc
  • American therapeutics inc
  • Apotex inc
  • Apothecon inc div bristol myers squibb
  • Labopharm inc
  • Matrix laboratories ltd
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Pliva inc
  • Quantum pharmics ltd
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. 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. Pubmed
  2. Jauch R, Kopitar Z, Prox A, Zimmer A: [Pharmacokinetics and metabolism of trazodone in man (author’s transl)] Arzneimittelforschung. 1976;26(11):2084-9. Pubmed
  3. 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. Pubmed
  4. 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. Pubmed
  5. 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. Pubmed
  6. 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. Pubmed
  7. 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. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Triazolopyridines
Substructures
  • Triazoles
  • Aliphatic and Aryl Amines
  • Pyridines and Derivatives
  • Triazolopyridines
  • Piperazines
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Pyridines
  • Heterocyclic compounds
  • Aromatic compounds
  • Cyanamides
  • Anilines
适应症
药理
Indication For the treatment of depression.
Pharmacodynamics Trazodone is an antidepressant and hypnotic chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. The mechanism of trazodone's antidepressant action in man is not fully understood. In animals, trazodone selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of trazodone in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. Trazodone is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system. In man, trazodone is well absorbed after oral administration without selective localization in any tissue. Since the clearance of trazodone from the body is sufficiently variable, in some patients trazodone may accumulate in the plasma.
Mechanism of action Trazodone binds at 5-HT2 receptor, it acts as a serotonin agonist at high doses and a serotonin antagonist at low doses. Like fluoxetine, trazodone's antidepressant activity likely results from blockage of serotonin reuptake by inhibiting serotonin reuptake pump at the presynaptic neuronal membrane. If used for long time periods, postsynaptic neuronal receptor binding sites may also be affected. The sedative effect of trazodone is likely the result of alpha-adrenergic blocking action and modest histamine blockade at H1 receptor. It weakly blocks presynaptic alpha2-adrenergic receptors and strongly inhibits postsynaptic alpha1 receptors. Trazodone does not affect the reuptake of norepinephrine or dopamine within the CNS.
Absorption Rapidly and almost completely absorbed following oral administration. Food may decrease the rate and extent of absorption.
Volume of distribution Not Available
Protein binding 89-95% bound to plasma proteins in vitro
Metabolism
Undergoes extensive hepatic metabolism via hydroxylation, N-dealkylation, N-oxidation and splitting of the pyridine ring. Cytochrome P450 (CYP) 3A4 catalyzes the formation of the major active metabolite, m-chlorophenylpiperazine (m-CPP). Metabolites may be further conjugated to glucuonic acid or glutathione. CYP2D6 is responsible for 4'-hydroxylation of m-CPP and the formation of at least one glutathione conjugates of m-CPP, a quinone imine-sulhydryl adduct. Oxotriazolopyridinpropionic acid, an inactive metabolite, and its conjugates account for about 20% of the total excreted oral dose. Less than 1% of the oral dose is excreted unchanged. Approximately 70-75% of the dose is eliminated in urine with the remainder being excreted in feces via biliary elimination.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Trazodone
4'-hydroxytrazodone glutathione Details
Trazodone
m-chlorophenylpiperazine (m-CPP) Details
Trazodone
triazolopropionic acid Details
Trazodone
triazolopyridinone epoxide Details
Trazodone
4'-hydroxytrazodone Details
Trazodone
    		Glutathione Details
    Trazodone
      		Glucuonic acid Details
      Trazodone
        		Oxotriazolopyridinpropionic acid Details
        Route of elimination Not Available
        Half life Undergoes biphasic elimination with an initial phase t1/2 α of 3-6 hours and a terminal phase t1/2 β of 5-9 hours.
        Clearance Not Available
        Toxicity LD50=96mg/kg (i.v. in mice)
        Affected organisms
        • Humans and other mammals
        Pathways Not Available
        理化性质
        Properties
        State solid
        Experimental Properties
        Property Value Source
        melting point 87 °C PhysProp
        water solubility Sparigly soluble Not Available
        logP 2.9 Not Available
        Predicted Properties
        Property Value Source
        water solubility 2.90e-01 g/l ALOGPS
        logP 2.68 ALOGPS
        logP 3.13 ChemAxon
        logS -3.1 ALOGPS
        pKa (strongest basic) 7.09 ChemAxon
        physiological charge 1 ChemAxon
        hydrogen acceptor count 4 ChemAxon
        hydrogen donor count 0 ChemAxon
        polar surface area 42.39 ChemAxon
        rotatable bond count 5 ChemAxon
        refractivity 105.88 ChemAxon
        polarizability 40.12 ChemAxon
        药物相互作用
        Drug Interaction
        Almotriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Aminoglutethimide The CYP3A4 inducer, Aminoglutethimide, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Aminoglutethimide is initiated, discontinued or dose changed.
        Amiodarone The CYP3A4 inhibitor, Amiodarone, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Amiodarone is initiated, discontinued or dose changed.
        Amitriptyline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Amoxapine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Amprenavir The protease inhibitor, Amprenavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Amprenavir is initiated, discontinued or dose changed.
        Aprepitant The CYP3A4 inhibitor, Aprepitant, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Aprepitant is initiated, discontinued or dose changed.
        Atazanavir The protease inhibitor, Atazanavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Atazanavir is initiated, discontinued or dose changed.
        Bosentan The CYP3A4 inducer, Bosentan, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Bosentan is initiated, discontinued or dose changed.
        Bromocriptine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Buspirone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Cabergoline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Carbamazepine The CYP3A4 inducer, Carbamazepine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Carbamazepine is initiated, discontinued or dose changed.
        Cimetidine The CYP3A4 inhibitor, Cimetidine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Cimetidine is initiated, discontinued or dose changed.
        Citalopram Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Clarithromycin The CYP3A4 inhibitor, Clarithromycin, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Clarithromycin is initiated, discontinued or dose changed.
        Clomipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Clotrimazole The CYP3A4 inhibitor, Clotrimazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Clotrimazole is initiated, discontinued or dose changed.
        Conivaptan The CYP3A4 inhibitor, Conivaptan, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Conivaptan is initiated, discontinued or dose changed.
        Cyclosporine The CYP3A4 inhibitor, Cyclosporine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Cyclosporine is initiated, discontinued or dose changed.
        Dabigatran etexilate P-Glycoprotein inducers such as trazodone may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
        Darunavir The protease inhibitor, Darunavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Darunavir is initiated, discontinued or dose changed.
        Delavirdine The CYP3A4 inhibitor, Delavirdine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Delavirdine is initiated, discontinued or dose changed.
        Desipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Dexamethasone The CYP3A4 inducer, Dexamethasone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Dexamethasone is initiated, discontinued or dose changed.
        Dextromethorphan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Dihydroergotamine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Diltiazem The CYP3A4 inhibitor, Diltizem, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Diltiazem is initiated, discontinued or dose changed.
        Donepezil Possible antagonism of action
        Doxepin Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Duloxetine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Efavirenz The CYP3A4 inhibitor and inducer, Efavirenz, may alter Trazodone efficacy/toxicity by altering Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Efavirenz is initiated, discontinued or dose changed.
        Eletriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Ergoloid mesylate Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Ergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Ergotamine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Erythromycin The CYP3A4 inhibitor, Erythromycin , may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Erythromycin is initiated, discontinued or dose changed.
        Escitalopram Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Etravirine The CYP3A4 inducer, Etravirene, may decrease Trazodone efficacy/toxicity by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Etravirine is initiated, discontinued or dose changed.
        Fluconazole The CYP3A4 inhibitor, Fluconazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Fluconazole is initiated, discontinued or dose changed.
        Fluoxetine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Fluvoxamine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Fosamprenavir The protease inhibitor, Fosamprenavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Fosamprenavir is initiated, discontinued or dose changed.
        Fosphenytoin The CYP3A4 inducer, Fosphenytoin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Fosphenytoin is initiated, discontinued or dose changed.
        Frovatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Furazolidone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Galantamine Possible antagonism of action
        Ginkgo biloba Increased effect and toxicity of both agents
        Haloperidol The CYP3A4 inhibitor, Haloperidol, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. The CYP2D6 inhibitor, Trazodone, may increase the efficacy of Haloperidol by decreasing Haloperidol metabolism and clearance. Monitor for changes in Trazodone and Haloperidol efficacy/toxicity if either agent is initiated, discontinued or dose changed.
        Imatinib The CYP3A4 inhibitor, Imatinib, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Imatinib is initiated, discontinued or dose changed.
        Imipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Indinavir The protease inhibitor, Indinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism via CYP3A4. Monitor for changes in Trazodone efficacy/toxicity if Indinavir is initiated, discontinued or dose changed.
        Isocarboxazid Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Isoniazid The CYP3A4 inhibitor, Isoniazid, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Isoniazid is initiated, discontinued or dose changed.
        Itraconazole The CYP3A4 inhibitor, Itraconazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Itraconazole is initiated, discontinued or dose changed.
        Ketoconazole The CYP3A4 inhibitor, Ketoconazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Ketoconazole is initiated, discontinued or dose changed.
        Lapatinib The CYP3A4 inhibitor, Lapatinib, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Lapatinib is initiated, discontinued or dose changed.
        Lidocaine The CYP3A4 inhibitor, Lidocaine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Lidocaine is initiated, discontinued or dose changed.
        Linezolid Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Lithium Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Lopinavir The protease inhibitor, Lopinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Lopinavir is initiated, discontinued or dose changed.
        Maprotiline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Meperidine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Methylergonovine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Metronidazole The CYP3A4 inhibitor, Metronidazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Metronidazole is initiated, discontinued or dose changed.
        Miconazole The CYP3A4 inhibitor, Miconazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Miconazole is initiated, discontinued or dose changed.
        Mirtazapine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Moclobemide Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Nafcillin The CYP3A4 inducer, Nafcillin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nafcillin is initiated, discontinued or dose changed.
        Naratriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Nefazodone Increased risk of serotonin syndrome. The CYP3A4 inhibitor, Nefazodone, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for symtpoms of sertonin syndrome and changes in Trazodone efficacy/toxicity if Nefazodone is initiated, discontinued or dose changed.
        Nelfinavir The protease inhibitor, Nelfinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nelfinavir is initiated, discontinued or dose changed.
        Nevirapine The CYP3A4 inducer, Nevirapine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Nevirapine is initiated, discontinued or dose changed.
        Nicardipine The CYP3A4 inhibitor, Nicardipine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Nicardipine is initiated, discontinued or dose changed.
        Norfloxacin The CYP3A4 inhibitor, Norfloxacin, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Norfloxacin is initiated, discontinued or dose changed.
        Nortriptyline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Oxcarbazepine The CYP3A4 inducer, Oxcarbazepine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Oxcarbazepine is initiated, discontinued or dose changed.
        Paroxetine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Pentobarbital The CYP3A4 inducer, Pentobarbital, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Pentobarbital is initiated, discontinued or dose changed.
        Pergolide Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Phenelzine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Phenobarbital The CYP3A4 inducer, Phenobarbital, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Phenobarbital is initiated, discontinued or dose changed.
        Phenytoin The CYP3A4 inducer, Phenytoin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Phenytoin is initiated, discontinued or dose changed.
        Posaconazole The CYP3A4 inhibitor, Posaconazole, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Posaconazole is initiated, discontinued or dose changed.
        Primidone The CYP3A4 inducer, Primidone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Primidone is initiated, discontinued or dose changed.
        Procarbazine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Promethazine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Protriptyline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Quinidine The CYP3A4 inhibitor, Quinidine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Quinidine is initiated, discontinued or dose changed.
        Rasagiline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Rifabutin The CYP3A4 inducer, Rifabutin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifabutin is initiated, discontinued or dose changed.
        Rifampin The CYP3A4 inducer, Rifampin, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifampin is initiated, discontinued or dose changed.
        Rifapentine The CYP3A4 inducer, Rifapentine, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Rifapentine is initiated, discontinued or dose changed.
        Ritonavir The protease inhibitor, Ritonavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Ritonavir is initiated, discontinued or dose changed.
        Rivastigmine Possible antagonism of action
        Rizatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        S-Adenosylmethionine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Saquinavir The protease inhibitor, Saquinavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Saquinavir is initiated, discontinued or dose changed.
        Selegiline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Sertraline Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Sibutramine Increased risk of serotonin syndrome. Avoid concomitant therapy.
        Sitaxentan The CYP3A4 inhibitor, Sitaxsenten, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Norfloxacin is initiated, discontinued or dose changed.
        St. John's Wort Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Tamoxifen Trazodone may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
        Tamsulosin Trazodone, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Trazodone is initiated, discontinued, or dose changed.
        Telithromycin The CYP3A4 inhibitor, Telithromycin, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Telithromycin is initiated, discontinued or dose changed.
        Tetracycline The CYP3A4 inhibitor, Tetracycline, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Tetracycline is initiated, discontinued or dose changed.
        Tipranavir The protease inhibitor, Tipranavir, may increase the efficacy/toxicity of Trazodone by inhibiting Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Tipranavir is initiated, discontinued or dose changed.
        Tramadol The use of two serotonin modulators, such as trazodone and tramadol, may increase the risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Tranylcypromine Increased risk of serotonin syndrome. Use caution during concomitant therapy and monitor for symptoms of serotonin syndrome.
        Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Triprolidine The CNS depressants, Triprolidine and Trazodone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
        Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
        Verapamil The CYP3A4 inhibitor, Verapamil, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Verapamil is initiated, discontinued or dose changed.
        Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of trazodone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of trazodone if voriconazole is initiated, discontinued or dose changed.
        Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and trazodone, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
        食物相互作用
        • Avoid alcohol.
        • Food decreases the rate and extent of absorption.

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