DGIdb - PHENOBARBITAL Drug Record

PHENOBARBITAL chembl:CHEMBL40 Approved

Alternate Names:

PHENEMAL
NSC-128143
NOPTIL
PHENOBARBITONE
NSC-9848
LUMINAL
ESKABARB
PHENOBARBITAL
TALPHENO
PHENOBARBITAL CIV
NSC-128143-
SOLFOTON
PHENYLETHYLMALONYLUREA
FENOBARBITAL
PHENOBARBITAL SODIUM
PHENYLETHYLBARBITURSAEURE
5-ETHYL-5-PHENYL-2,4,6(1H,3H,5H)-PYRIMIDINETRIONE
PHENOBARBITURIC ACID
PHENYLETHYLBARBITURATE
PHENOBARBITOL
PHENYLETHYLBARBITURIC ACID
5-ETHYL-5-PHENYLPYRIMIDINE-2,4,6(1H,3H,5H)-TRIONE
5-ETHYL-5-PHENYLBARBITURIC ACID
5-ETHYL-5-PHENYL-PYRIMIDINE-2,4,6-TRIONE
LUMINAL®
5-PHENYL-5-ETHYLBARBITURIC ACID
PHENYLAETHYLBARBITURSAEURE
drugbank:01174
rxcui:8134
chembl:CHEMBL40
pubchem.compound:4763
chemidplus:50-06-6

Drug Info:

FDA Approval	Approved before 1982
Drug Class	small molecule
Drug Indications	Hypnotics and Sedatives
Drug Indications	Anticonvulsants
Drug Class	hypnotics and sedatives
Drug Class	anticonvulsants
Year of Approval	approved before 1982
Drug Categories	therapeutic uses
Drug Categories	pyrimidinones
Drug Categories	pyrimidines
Drug Categories	physiological effects of drugs
Drug Categories	pharmacologic actions
Drug Categories	p-glycoprotein/abcb1 substrates
Drug Categories	p-glycoprotein/abcb1 inducers
Drug Categories	neurotransmitter agents
Drug Categories	nervous system
Drug Categories	molecular mechanisms of pharmacological action
Drug Categories	methemoglobinemia associated agents
Drug Categories	metabolic side effects of drugs and substances
Drug Categories	hypnotics and sedatives
Drug Categories	heterocyclic compounds, 1-ring
Drug Categories	heterocyclic compounds
Drug Categories	gaba modulators
Drug Categories	gaba agents
Drug Categories	excitatory amino acid antagonists
Drug Categories	excitatory amino acid agents
Drug Categories	drug-related side effects and adverse reactions
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 cyp3a4 inducers (strong)
Drug Categories	cytochrome p-450 cyp3a inducers
Drug Categories	cytochrome p-450 cyp2e1 substrates
Drug Categories	cytochrome p-450 cyp2e1 inducers
Drug Categories	cytochrome p-450 cyp2c9 substrates
Drug Categories	cytochrome p-450 cyp2c9 inducers (strong)
Drug Categories	cytochrome p-450 cyp2c9 inducers
Drug Categories	cytochrome p-450 cyp2c8 inducers (strong)
Drug Categories	cytochrome p-450 cyp2c8 inducers
Drug Categories	cytochrome p-450 cyp2c19 substrates
Drug Categories	cytochrome p-450 cyp2c19 inducers
Drug Categories	cytochrome p-450 cyp2b6 inducers (strong)
Drug Categories	cytochrome p-450 cyp2b6 inducers
Drug Categories	cytochrome p-450 cyp2a6 inhibitors
Drug Categories	cytochrome p-450 cyp2a6 inducers
Drug Categories	cytochrome p-450 cyp1a2 inducers (strong)
Drug Categories	cytochrome p-450 cyp1a2 inducers
Drug Categories	combined inducers of cyp3a4 and p-glycoprotein
Drug Categories	chemically-induced disorders
Drug Categories	chemical actions and uses
Drug Categories	central nervous system depressants
Drug Categories	central nervous system agents
Drug Categories	barbiturates and derivatives
Drug Categories	barbiturates
Drug Categories	anticonvulsants
Drug Groups	approved
Drug Type	small molecule
Drug Categories	ugt2b7 inducers
Drug Categories	ugt1a1 inducers
Drug Categories	psycholeptics
Drug Categories	phenobarbital and similars
Drug Categories	p-glycoprotein substrates with narrow therapeutic index
Drug Categories	p-glycoprotein substrates
Drug Categories	p-glycoprotein inducers
Drug Categories	nicotinic antagonists
Drug Categories	narrow therapeutic index drugs
Drug Categories	enzyme inducing antiepileptic drugs
Drug Categories	cytochrome p-450 substrates
Drug Categories	cytochrome p-450 cyp3a7 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp3a7 inducers
Drug Categories	cytochrome p-450 cyp3a5 inducers (strong)
Drug Categories	cytochrome p-450 cyp3a5 inducers
Drug Categories	cytochrome p-450 cyp3a4 inducers
Drug Categories	cytochrome p-450 cyp3a inducers (strong)
Drug Categories	cytochrome p-450 cyp2e1 inducers (weak)
Drug Categories	cytochrome p-450 cyp2e1 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2c9 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2c8 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2c19 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp2c19 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp2c18 substrates
Drug Categories	cytochrome p-450 cyp2c18 inducers (strength unknown)
Drug Categories	cytochrome p-450 cyp1a2 inducers (strength unknown)
Drug Categories	cytochrome p-450 2c18 inducers
Drug Categories	bsep/abcb11 inducers
Drug Categories	anticholinergic agents
Drug Groups	investigational

(5 More Sources)

Publications:

Ma CL et al., 2014, Association of SCN1A, SCN2A and ABCC2 gene polymorphisms with the response to antiepileptic drugs in Chinese Han patients with epilepsy., Pharmacogenomics
Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics
Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Oxberry et al., 1984, Down regulation of prolactin receptors in the hamster ovary by the preovulatory gonadotropin surge., Biol. Reprod.
Osanai et al., 1997, Phenobarbital causes apoptosis in conditionally immortalized mouse hepatocytes depending on deregulated c-myc expression: characterization of an unexpected effect., Cancer Res.
Kobayashi K et al., 2004, Key structural features of ligands for activation of human pregnane X receptor., Drug Metab Dispos
Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.
Chen et al., 1992, Association between growth stimulation by phenobarbital and expression of cytochromes P450 1A1, 1A2, 2B1/2 and 3A1 in hepatic hyperplastic nodules in male F344 rats., Carcinogenesis
Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics
Talwar P et al., 2017, Genetic contribution of CYP1A1 variant on treatment outcome in epilepsy patients: a functional and interethnic perspective., Pharmacogenomics J
Grover S et al., 2010, Genetic polymorphisms in sex hormone metabolizing genes and drug response in women with epilepsy., Pharmacogenomics
Jin et al., 2010, The interaction of the neuroprotective compounds riluzole and phenobarbital with AMPA-type glutamate receptors: a patch-clamp study., Pharmacology
Brandt et al., 2006, The multidrug transporter hypothesis of drug resistance in epilepsy: Proof-of-principle in a rat model of temporal lobe epilepsy., Neurobiol. Dis.
Keangpraphun T et al., 2015, Association of ABCB1 C3435T polymorphism with phenobarbital resistance in Thai patients with epilepsy., J Clin Pharm Ther
Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics
Daniell, 1994, Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles., Pharmacology
Whiting, 2003, The GABAA receptor gene family: new opportunities for drug development., Curr Opin Drug Discov Devel
Macdonald et al., 1986, Anticonvulsant drugs: mechanisms of action., Adv Neurol
Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Nakaoka, 1990, Kinetic characteristics of UDP-glucuronosyltransferases towards a dithiol metabolite of malotilate in hepatic microsomes of rats and rabbits., Xenobiotica
Jonges et al., 1995, Effects of partial hepatectomy, phenobarbital and 3-methylcholanthrene on kinetic parameters of glucose-6-phosphate and phosphogluconate dehydrogenase in situ in periportal, intermediate and pericentral zones of rat liver lobules., Biochim. Biophys. Acta
Schuetz et al., 1990, Regulation of cytochrome P-450b/e and P-450p gene expression by growth hormone in adult rat hepatocytes cultured on a reconstituted basement membrane., J. Biol. Chem.
Hassan HE et al., 2013, Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone., Drug Metab Dispos
Manuyakorn W et al., 2013, Phenobarbital-induced severe cutaneous adverse drug reactions are associated with CYP2C19*2 in Thai children., Pediatr Allergy Immunol
Dildy-Mayfield et al., 1996, Anesthetics produce subunit-selective actions on glutamate receptors., J. Pharmacol. Exp. Ther.
Chaudhary et al., 1993, Effect of genetic obesity and phenobarbital treatment on the hepatic conjugation pathways., J. Pharmacol. Exp. Ther.
Tavoloni et al., 1983, Dose-related effects of phenobarbital on hepatic microsomal enzymes., Proc. Soc. Exp. Biol. Med.
Tanaka et al., 1997, Changes in glutamate receptors, c-fos mRNA expression and activator protein-1 (AP-1) DNA binding activity in the brain of phenobarbital-dependent and -withdrawn rats., Brain Res.
Horio et al., 1993, UDP glucuronosyltransferase gene expression is involved in the stimulation of ascorbic acid biosynthesis by xenobiotics in rats., J. Nutr.
Rico et al., 1992, Long-term influence of anticonvulsant agents on calcitonin, parathyroid hormone and osteocalcin., Eur. Neurol.
Romero et al., 2006, Chemical inducers of rodent glutathione s-transferases down-regulate human GSTA1 transcription through a mechanism involving variant hepatic nuclear factor 1-C., Mol. Pharmacol.

PHENOBARBITAL CHRNA4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

PHENOBARBITAL NR1I2

Interaction Types & Directionality:

agonist (activating)

activator (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Publications:

Kobayashi K et al., 2004, Key structural features of ligands for activation of human pregnane X receptor., Drug Metab Dispos

Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

PHENOBARBITAL GRIK2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

PHENOBARBITAL CHRNA7

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

PHENOBARBITAL GRIA2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Jin et al., 2010, The interaction of the neuroprotective compounds riluzole and phenobarbital with AMPA-type glutamate receptors: a patch-clamp study., Pharmacology

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

PHENOBARBITAL GRIN1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Publications:

Daniell, 1994, Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles., Pharmacology

PHENOBARBITAL GABRA1

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Whiting, 2003, The GABAA receptor gene family: new opportunities for drug development., Curr Opin Drug Discov Devel

Macdonald et al., 1986, Anticonvulsant drugs: mechanisms of action., Adv Neurol

PHENOBARBITAL GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
PHENOBARBITAL GABRA2

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
PHENOBARBITAL GABRA6

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
PHENOBARBITAL GABRA4

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
PHENOBARBITAL GABRA3

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
PHENOBARBITAL GRIA1

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

PHENOBARBITAL SCN2A

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ma CL et al., 2014, Association of SCN1A, SCN2A and ABCC2 gene polymorphisms with the response to antiepileptic drugs in Chinese Han patients with epilepsy., Pharmacogenomics

Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics

PHENOBARBITAL CYP3A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
PHENOBARBITAL PRL

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Oxberry et al., 1984, Down regulation of prolactin receptors in the hamster ovary by the preovulatory gonadotropin surge., Biol. Reprod.

PHENOBARBITAL BAX

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Osanai et al., 1997, Phenobarbital causes apoptosis in conditionally immortalized mouse hepatocytes depending on deregulated c-myc expression: characterization of an unexpected effect., Cancer Res.

PHENOBARBITAL CYP2D6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PHENOBARBITAL CYP1A2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Chen et al., 1992, Association between growth stimulation by phenobarbital and expression of cytochromes P450 1A1, 1A2, 2B1/2 and 3A1 in hepatic hyperplastic nodules in male F344 rats., Carcinogenesis

PHENOBARBITAL UGT2B15

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

PHENOBARBITAL CYP1A1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Talwar P et al., 2017, Genetic contribution of CYP1A1 variant on treatment outcome in epilepsy patients: a functional and interethnic perspective., Pharmacogenomics J

Grover S et al., 2010, Genetic polymorphisms in sex hormone metabolizing genes and drug response in women with epilepsy., Pharmacogenomics

PHENOBARBITAL ABCB1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Brandt et al., 2006, The multidrug transporter hypothesis of drug resistance in epilepsy: Proof-of-principle in a rat model of temporal lobe epilepsy., Neurobiol. Dis.

Keangpraphun T et al., 2015, Association of ABCB1 C3435T polymorphism with phenobarbital resistance in Thai patients with epilepsy., J Clin Pharm Ther

PHENOBARBITAL CYP2C9

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
PHENOBARBITAL UGT1A9

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics
PHENOBARBITAL UGT1A6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

PHENOBARBITAL CYP2B6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics

PHENOBARBITAL UGT1A5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Nakaoka, 1990, Kinetic characteristics of UDP-glucuronosyltransferases towards a dithiol metabolite of malotilate in hepatic microsomes of rats and rabbits., Xenobiotica

PHENOBARBITAL PGD

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Jonges et al., 1995, Effects of partial hepatectomy, phenobarbital and 3-methylcholanthrene on kinetic parameters of glucose-6-phosphate and phosphogluconate dehydrogenase in situ in periportal, intermediate and pericentral zones of rat liver lobules., Biochim. Biophys. Acta

PHENOBARBITAL TAT

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Schuetz et al., 1990, Regulation of cytochrome P-450b/e and P-450p gene expression by growth hormone in adult rat hepatocytes cultured on a reconstituted basement membrane., J. Biol. Chem.
PHENOBARBITAL NR1I3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Hassan HE et al., 2013, Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone., Drug Metab Dispos

PHENOBARBITAL CYP2C19

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Manuyakorn W et al., 2013, Phenobarbital-induced severe cutaneous adverse drug reactions are associated with CYP2C19*2 in Thai children., Pediatr Allergy Immunol

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PHENOBARBITAL GRIA3

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Dildy-Mayfield et al., 1996, Anesthetics produce subunit-selective actions on glutamate receptors., J. Pharmacol. Exp. Ther.

PHENOBARBITAL UGT1A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Chaudhary et al., 1993, Effect of genetic obesity and phenobarbital treatment on the hepatic conjugation pathways., J. Pharmacol. Exp. Ther.

Tavoloni et al., 1983, Dose-related effects of phenobarbital on hepatic microsomal enzymes., Proc. Soc. Exp. Biol. Med.

PHENOBARBITAL FOS

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Tanaka et al., 1997, Changes in glutamate receptors, c-fos mRNA expression and activator protein-1 (AP-1) DNA binding activity in the brain of phenobarbital-dependent and -withdrawn rats., Brain Res.

PHENOBARBITAL UGT1A10

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Horio et al., 1993, UDP glucuronosyltransferase gene expression is involved in the stimulation of ascorbic acid biosynthesis by xenobiotics in rats., J. Nutr.
PHENOBARBITAL PTH

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Rico et al., 1992, Long-term influence of anticonvulsant agents on calcitonin, parathyroid hormone and osteocalcin., Eur. Neurol.

PHENOBARBITAL GSTA1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Romero et al., 2006, Chemical inducers of rodent glutathione s-transferases down-regulate human GSTA1 transcription through a mechanism involving variant hepatic nuclear factor 1-C., Mol. Pharmacol.

PHENOBARBITAL MTHFR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB01174

Version: 5.1.7

Alternate Names:

PHENOBARBITAL DrugBank Drug Name

50-06-6 CAS Number

B-Donna Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

TEND: PHENOBARBITAL
- Version: 01-August-2011
Alternate Names:

PHENOBARBITAL Primary Drug Name

Drug Info:

Year of Approval approved before 1982

Drug Class anticonvulsants

Drug Class hypnotics and sedatives

Publications:
TdgClinicalTrial: PHENOBARBITAL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Anticonvulsants

Drug Indications Hypnotics and Sedatives

Drug Class small molecule

Publications:

NCI: PHENOBARBITAL

Version: 14-September-2017

Alternate Names:

C739 NCI drug code

Drug Info:

Publications:

Oxberry et al., 1984, Down regulation of prolactin receptors in the hamster ovary by the preovulatory gonadotropin surge., Biol. Reprod.

Rico et al., 1992, Long-term influence of anticonvulsant agents on calcitonin, parathyroid hormone and osteocalcin., Eur. Neurol.

Brandt et al., 2006, The multidrug transporter hypothesis of drug resistance in epilepsy: Proof-of-principle in a rat model of temporal lobe epilepsy., Neurobiol. Dis.

DTC: PHENOBARBITAL

Version: 02-September-2020

Alternate Names:

CHEMBL40 ChEMBL Drug ID

Drug Info:

Publications:

Hassan HE et al., 2013, Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone., Drug Metab Dispos

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PharmGKB: phenobarbital

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Keangpraphun T et al., 2015, Association of ABCB1 C3435T polymorphism with phenobarbital resistance in Thai patients with epilepsy., J Clin Pharm Ther

Haerian BS et al., 2013, SCN1A, SCN2A and SCN3A gene polymorphisms and responsiveness to antiepileptic drugs: a multicenter cohort study and meta-analysis., Pharmacogenomics

TTD: Phenobarbital
- Version: 2020.06.01
Alternate Names:

D0Y7RW TTD Drug ID

Drug Info:

Publications:
GuideToPharmacologyInteractions: 135650817
- Version: 20-July-2020
Alternate Names:

PHENOBARBITAL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL40
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

PHENOBARBITAL	DrugBank Drug Name
50-06-6	CAS Number
B-Donna	Drug Brand

PHENOBARBITAL Drug Record

PHENOBARBITAL chembl:CHEMBL40 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality: agonist (activating) activator (activating)

Interaction Info: Specific Action of the Ligand Agonist Endogenous Drug? False

Publications: Kobayashi K et al., 2004, Key structural features of ligands for activation of human pregnane X receptor., Drug Metab Dispos Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

Publications: Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol. Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

Publications: Daniell, 1994, Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles., Pharmacology

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name -

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name -

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Oxberry et al., 1984, Down regulation of prolactin receptors in the hamster ovary by the preovulatory gonadotropin surge., Biol. Reprod.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Osanai et al., 1997, Phenobarbital causes apoptosis in conditionally immortalized mouse hepatocytes depending on deregulated c-myc expression: characterization of an unexpected effect., Cancer Res.

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos. Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Nakaoka, 1990, Kinetic characteristics of UDP-glucuronosyltransferases towards a dithiol metabolite of malotilate in hepatic microsomes of rats and rabbits., Xenobiotica

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

agonist (activating)

activator (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Publications:

Kobayashi K et al., 2004, Key structural features of ligands for activation of human pregnane X receptor., Drug Metab Dispos

Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Interaction Types & Directionality:

antagonist (inhibitory)

Publications:

Daniell, 1994, Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles., Pharmacology

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Publications:

Oxberry et al., 1984, Down regulation of prolactin receptors in the hamster ovary by the preovulatory gonadotropin surge., Biol. Reprod.

Interaction Types & Directionality:

n/a

Publications:

Osanai et al., 1997, Phenobarbital causes apoptosis in conditionally immortalized mouse hepatocytes depending on deregulated c-myc expression: characterization of an unexpected effect., Cancer Res.

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Interaction Types & Directionality:

n/a

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality:

n/a

Publications:

Mazaleuskaya LL et al., 2015, PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses., Pharmacogenet Genomics

Interaction Types & Directionality:

n/a

Publications:

Faucette et al., 2004, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers., Drug Metab. Dispos.

Zanger UM et al., 2007, Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance., Pharmacogenomics

Interaction Types & Directionality:

n/a

Publications:

Nakaoka, 1990, Kinetic characteristics of UDP-glucuronosyltransferases towards a dithiol metabolite of malotilate in hepatic microsomes of rats and rabbits., Xenobiotica

Interaction Types & Directionality:

n/a

Publications:

Jonges et al., 1995, Effects of partial hepatectomy, phenobarbital and 3-methylcholanthrene on kinetic parameters of glucose-6-phosphate and phosphogluconate dehydrogenase in situ in periportal, intermediate and pericentral zones of rat liver lobules., Biochim. Biophys. Acta

Interaction Types & Directionality:

n/a

Publications:

Schuetz et al., 1990, Regulation of cytochrome P-450b/e and P-450p gene expression by growth hormone in adult rat hepatocytes cultured on a reconstituted basement membrane., J. Biol. Chem.

Interaction Types & Directionality:

n/a

Publications:

Hassan HE et al., 2013, Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone., Drug Metab Dispos

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Publications:

Dildy-Mayfield et al., 1996, Anesthetics produce subunit-selective actions on glutamate receptors., J. Pharmacol. Exp. Ther.

Interaction Types & Directionality:

n/a

Publications:

Chaudhary et al., 1993, Effect of genetic obesity and phenobarbital treatment on the hepatic conjugation pathways., J. Pharmacol. Exp. Ther.

Tavoloni et al., 1983, Dose-related effects of phenobarbital on hepatic microsomal enzymes., Proc. Soc. Exp. Biol. Med.

Interaction Types & Directionality:

n/a

Publications:

Tanaka et al., 1997, Changes in glutamate receptors, c-fos mRNA expression and activator protein-1 (AP-1) DNA binding activity in the brain of phenobarbital-dependent and -withdrawn rats., Brain Res.

Interaction Types & Directionality:

n/a

Publications:

Horio et al., 1993, UDP glucuronosyltransferase gene expression is involved in the stimulation of ascorbic acid biosynthesis by xenobiotics in rats., J. Nutr.

Interaction Types & Directionality:

n/a

Publications:

Rico et al., 1992, Long-term influence of anticonvulsant agents on calcitonin, parathyroid hormone and osteocalcin., Eur. Neurol.