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DOXEPIN Drug Record

  • Summary
  • Interactions
  • Claims
  • DOXEPIN chembl:CHEMBL1628227 Approved

    Alternate Names:

    SINEQUAN
    ZONALON
    P-3693A
    SINEPIN
    DOXEPIN

    Drug Info:

    Drug Categories ethers, cyclic
    Drug Indications hypnotic
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antimigraine agent
    Drug Class antidepressive agents, tricyclic
    Year of Approval 1969
    Drug Class antipruritics
    Drug Groups investigational
    Drug Categories acid reducers
    Drug Categories adrenergic alpha-1 receptor antagonists
    Drug Categories adrenergic alpha-antagonists
    Drug Categories adrenergic antagonists
    Drug Categories agents producing tachycardia
    Drug Categories agents that produce hypertension
    Drug Categories agents that reduce seizure threshold
    Drug Categories anticholinergic agents
    Drug Categories antipruritics and local anesthetics
    Drug Categories antipruritics, incl. antihistamines, anesthetics, etc.
    Drug Categories combined inhibitors of serotonin/norepinephrine reuptake
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories dermatologicals
    Drug Categories dopamine antagonists
    Drug Categories drugs that are mainly renally excreted
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories histamine h1 antagonists
    Drug Categories histamine h2 antagonists
    Drug Categories hypnotics and sedatives
    Drug Categories muscarinic antagonists
    Drug Categories neurotoxic agents
    Drug Categories p-glycoprotein substrates
    Drug Categories potential qtc-prolonging agents
    Drug Categories qtc prolonging agents
    Drug Categories serotonergic drugs shown to increase risk of serotonin syndrome
    Drug Categories serotonin 5-ht1 receptor antagonists
    Drug Categories serotonin 5-ht2 receptor antagonists
    Drug Categories serotonin agents
    Drug Categories serotonin receptor antagonists
    Drug Categories tertiary amine tricyclic antidepressants
    Drug Categories tricyclics and other norepinephrine-reuptake inhibitors
    (5 More Sources)

    Publications:

    Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
    Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
    Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.
    de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem
    Tashiro et al., 2004, Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography., J Clin Pharmacol
    Tran et al., 1981, [3H]doxepin interactions with histamine H1-receptors and other sites in guinea pig and rat brain homogenates., Eur. J. Pharmacol.
    Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
    Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
    Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Singh et al., 2007, Novel therapeutic usage of low-dose doxepin hydrochloride., Expert Opin Investig Drugs
    Kano et al., 2004, Decreased histamine H1 receptor binding in the brain of depressed patients., Eur. J. Neurosci.
    Ehlert et al., 1990, The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart., J. Pharmacol. Exp. Ther.
    Beil et al., 1988, Interaction of antidepressants and neuroleptics with histamine stimulated parietal cell adenylate cyclase and H+ secretion., Pharmacology
    Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
    Kirchheiner J et al., 2002, Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers., Pharmacogenetics
    Duncan et al., 2007, Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin., Biochem. Pharmacol.
    Hicks JK et al., 2013, Clinical Pharmacogenetics Implementation Consortium guideline for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants., Clin Pharmacol Ther
  • DOXEPIN   HRH2

    Interaction Score: 0.26

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name Silenor (SO-101)

    PMIDs:
    2141000 2897127


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   HRH1

    Interaction Score: 0.21

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target
    Specific Action of the Ligand Antagonist

    PMIDs:
    3011460 22007643 15286093 7238574 19179941 6086881 2141000 7855217 11752352 17685877 15255990


    Sources:
    DTC TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • DOXEPIN   SLC6A2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    19179941 9537821


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • DOXEPIN   SLC6A4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    19179941 9537821


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • DOXEPIN   CHRM4

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    2141000 7855217 2329499


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   CHRM5

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    2141000 7855217 2329499


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   ADRA1D

    Interaction Score: 0.13

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    19179941 6086881 7855217


    Sources:
    DrugBank

  • DOXEPIN   HTR2B

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    309138 7855217


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   CHRM2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    2141000 7855217 2329499


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   CHRM1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    19179941 2141000 7855217 2329499


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   ADRA1B

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    19179941 6086881 7855217


    Sources:
    DrugBank

  • DOXEPIN   CHRM3

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    2141000 7855217 2329499


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   HTR2C

    Interaction Score: 0.07

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    309138 7855217


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   HRH4

    Interaction Score: 0.07

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • DOXEPIN   HTR2A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name Silenor (SO-101)
    Novel drug target Established target

    PMIDs:
    19179941 309138 7855217


    Sources:
    TdgClinicalTrial DrugBank

  • DOXEPIN   ADRA1A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    19179941 6086881 7855217


    Sources:
    DrugBank

  • DOXEPIN   HTR1A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    309138 7855217


    Sources:
    DrugBank

  • DOXEPIN   HTR6

    Interaction Score: 0.05

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • DOXEPIN   CYP2C19

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12360109 23486447


    Sources:
    FDA PharmGKB

  • DOXEPIN   KCNH2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    17560554


    Sources:
    PharmGKB DrugBank

  • DOXEPIN   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12360109


    Sources:
    PharmGKB

  • DOXEPIN   CYP1A2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DOXEPIN   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA

  • DOXEPIN   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • DrugBank: DB01142

    • Version: 5.1.7

    Alternate Names:
    Doxepine-75 - Cap Drug Brand
    Novo-doxepin Drug Brand
    Ntp-doxepin Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Groups investigational

    Publications:
    Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
    Beil et al., 1988, Interaction of antidepressants and neuroleptics with histamine stimulated parietal cell adenylate cyclase and H+ secretion., Pharmacology
    Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.

  • TEND: DOXEPIN

    • Version: 01-August-2011

    Alternate Names:
    DOXEPIN Primary Drug Name

    Drug Info:
    Drug Class antipruritics
    Year of Approval 1969
    Drug Class antidepressive agents, tricyclic

    Publications:

  • TdgClinicalTrial: DOXEPIN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antimigraine agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • DTC: DOXEPIN

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL1628227 ChEMBL Drug ID

    Drug Info:

    Publications:
    de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

  • PharmGKB: doxepin

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Kirchheiner J et al., 2002, Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers., Pharmacogenetics
    Hicks JK et al., 2013, Clinical Pharmacogenetics Implementation Consortium guideline for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants., Clin Pharmacol Ther

  • GuideToPharmacology: 135650208

    • Version: 29-September-2020

    Alternate Names:
    DOXEPIN GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • TTD: Doxepin

    • Version: 2020.06.01

    Alternate Names:
    D06FES TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1628227

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Doxepin

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21