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Identification
NamePrimidone
Accession NumberDB00794  (APRD00549)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

An antiepileptic agent related to the barbiturates; it is partly metabolized to phenobarbital in the body and owes some of its actions to this metabolite. Adverse effects are reported to be more frequent than with phenobarbital. (From Martindale, The Extra Pharmacopoeia, 30th ed, p309)

Structure
Thumb
Synonyms
5-Phenyl-5-ethyl-hexahydropyrimidine-4,6-dione
Desoxyphenobarbital
Mysoline
Primaclone
Primidon
Primidona
Primidone
Primidonum
External Identifiers
  • Rö 101
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mysolinetablet50 mg/1oralValeant Pharmaceuticals North America2009-06-24Not applicableUs
Mysolinetablet250 mg/1oralValeant Pharmaceuticals North America2009-06-24Not applicableUs
Mysoline 250mg Tabtablet250 mgoralElan Pharmaceuticals Inc1994-12-312004-08-05Canada
Mysoline Pediatric Chewable Tablets 125mgtablet125 mgoralElan Pharmaceuticals Inc1994-12-312004-08-05Canada
Mysoline Tab 125mgtablet125 mgoralAyerst Laboratories1963-12-311996-09-10Canada
Mysoline Tab 250mgtablet250 mgoralAyerst Laboratories1965-12-311997-08-15Canada
Primidonetablet125 mgoralAa Pharma Inc1977-12-31Not applicableCanada
Primidonetablet250 mgoralAa Pharma Inc1977-12-31Not applicableCanada
Primidone 125 Tabtablet125 mgoralPro Doc Limitee1982-12-311999-08-12Canada
Primidone 250 Tabtablet250 mgoralPro Doc Limitee1982-12-311999-08-12Canada
Sertan Tab 125mgtablet125 mgoralPharmascience Inc1983-12-312005-05-09Canada
Sertan Tab 250mgtablet250 mgoralPharmascience Inc1983-12-312005-05-09Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Primidonetablet50 mg/1oralMajor Pharmaceuticals2005-04-07Not applicableUs
Primidonetablet250 mg/1oralAmneal Pharmaceuticals2009-12-24Not applicableUs
Primidonetablet250 mg/1oralAmerican Health Packaging2007-06-14Not applicableUs
Primidonetablet50 mg/1oralGlobal Pharmaceuticals2008-02-12Not applicableUs
Primidonetablet250 mg/1oralMarlex Pharmaceuticals Inc2015-05-01Not applicableUs
Primidonetablet250 mg/1oralWatson Laboratories, Inc.2010-06-19Not applicableUs
Primidonetablet250 mg/1oralAv Pak2011-05-19Not applicableUs
Primidonetablet250 mg/1oralMajor Pharmaceuticals2005-04-07Not applicableUs
Primidonetablet50 mg/1oralAmneal Pharmaceuticals2009-12-24Not applicableUs
Primidonetablet50 mg/1oralLannett Company, Inc.2001-05-24Not applicableUs
Primidonetablet50 mg/1oralAv Pak2011-05-19Not applicableUs
Primidonetablet50 mg/1oralCardinal Health2001-05-242016-02-25Us
Primidonetablet250 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1978-12-01Not applicableUs
Primidonetablet50 mg/1oralSTAT Rx USA LLC2001-05-24Not applicableUs
Primidonetablet250 mg/1oralLannett Company, Inc.1978-12-01Not applicableUs
Primidonetablet50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2001-05-24Not applicableUs
Primidonetablet50 mg/1oralDr. Reddy's Laboratories Ltd2008-10-03Not applicableUs
Primidonetablet250 mg/1oralWest ward Pharmaceutical Corp2006-07-01Not applicableUs
Primidonetablet250 mg/1oralAv Kare, Inc.2008-04-24Not applicableUs
Primidonetablet250 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2006-07-01Not applicableUs
Primidonetablet250 mg/1oralDr. Reddy's Laboratories Ltd2008-10-03Not applicableUs
Primidonetablet50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2005-02-24Not applicableUs
Primidonetablet50 mg/1oralWest ward Pharmaceutical Corp2006-07-01Not applicableUs
Primidonetablet50 mg/1oralAv Kare, Inc.2008-04-24Not applicableUs
Primidonetablet250 mg/1oralQualitest Pharmaceuticals2005-02-24Not applicableUs
Primidonetablet50 mg/1oralPhysicians Total Care, Inc.2009-01-29Not applicableUs
Primidonetablet250 mg/1oralMajor Pharmaceuticals2009-12-24Not applicableUs
Primidonetablet50 mg/1oralAmerican Health Packaging2007-06-14Not applicableUs
Primidonetablet50 mg/1oralMc Kesson Contract Packaging2011-12-27Not applicableUs
Primidonetablet250 mg/1oralGlobal Pharmaceuticals2008-02-12Not applicableUs
Primidonetablet50 mg/1oralMarlex Pharmaceuticals Inc2015-05-01Not applicableUs
Primidonetablet50 mg/1oralQualitest Pharmaceuticals2005-02-24Not applicableUs
Primidonetablet250 mg/1oralPhysicians Total Care, Inc.2009-07-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LiskantinDesitin
MizodinUnia
MylepsinumNot Available
PridonaPsicofarma
PrimidApsen
PrysolineRekah
SertanAlkaloida
Brand mixturesNot Available
SaltsNot Available
Categories
UNII13AFD7670Q
CAS number125-33-7
WeightAverage: 218.2518
Monoisotopic: 218.105527702
Chemical FormulaC12H14N2O2
InChI KeyInChIKey=DQMZLTXERSFNPB-UHFFFAOYSA-N
InChI
InChI=1S/C12H14N2O2/c1-2-12(9-6-4-3-5-7-9)10(15)13-8-14-11(12)16/h3-7H,2,8H2,1H3,(H,13,15)(H,14,16)
IUPAC Name
5-ethyl-5-phenyl-1,3-diazinane-4,6-dione
SMILES
CCC1(C(=O)NCNC1=O)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as hydropyrimidines. These are compounds containing a hydrogenated pyrimidine ring (i.e containing less than the maximum bumber of double bonds.).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentHydropyrimidines
Alternative Parents
Substituents
  • Benzenoid
  • 1,3-diazinane
  • Monocyclic benzene moiety
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of epilepsy
PharmacodynamicsPrimidone is a barbiturate with anticonvulsant properties. Primidone, either alone or used concomitantly with other anticonvulsants, is indicated in the control of grand mal, psychomotor, and focal epileptic seizures. It may control grand mal seizures refractory to other anticonvulsant therapy. Primidone raises electro- or chemoshock seizure thresholds or alters seizure patterns in experimental animals. Primidone per se has anticonvulsant activity as do its two metabolites, phenobarbital and phenylethylmalonamide (PEMA). In addition to its anticonvulsant activity, Primidone potentiates that of phenobarbital in experimental animals.
Mechanism of actionPrimidone is a GABA receptor agonist. The mechanism of Primidone's antiepileptic action is not known.
Related Articles
Absorption90 to 100%
Volume of distributionNot Available
Protein binding70%
Metabolism

Hepatic

SubstrateEnzymesProduct
Primidone
PhenobarbitalDetails
Route of eliminationNot Available
Half life3-23 hours
ClearanceNot Available
ToxicitySymptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9907
Blood Brain Barrier+0.9642
Caco-2 permeable-0.5593
P-glycoprotein substrateSubstrate0.5222
P-glycoprotein inhibitor INon-inhibitor0.536
P-glycoprotein inhibitor IINon-inhibitor0.9048
Renal organic cation transporterNon-inhibitor0.8298
CYP450 2C9 substrateNon-substrate0.7961
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6863
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.924
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.7814
BiodegradationNot ready biodegradable0.982
Rat acute toxicity2.1941 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9912
hERG inhibition (predictor II)Non-inhibitor0.8735
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Xcel pharmaceuticals
  • Valeant pharmaceuticals international
  • Amneal pharmaceutical
  • Dr reddys laboratories ltd
  • Impax laboratories inc
  • Lannett co inc
  • Mutual pharmaceutical co inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral125 mg
Tabletoral250 mg
Tabletoral250 mg/1
Tabletoral50 mg/1
Prices
Unit descriptionCostUnit
Primidone powder10.56USD g
Mysoline 250 mg tablet6.52USD tablet
Mysoline 50 mg tablet1.26USD tablet
Primidone 250 mg tablet1.02USD tablet
Primidone 50 mg tablet0.51USD tablet
Apo-Primidone 250 mg Tablet0.09USD tablet
Apo-Primidone 125 mg Tablet0.06USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point281.5 °CPhysProp
water solubility500 mg/L (at 22 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP0.91HANSCH,C ET AL. (1995)
logS-2.64ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility1.04 mg/mLALOGPS
logP0.62ALOGPS
logP1.12ChemAxon
logS-2.3ALOGPS
pKa (Strongest Acidic)11.5ChemAxon
pKa (Strongest Basic)-6.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area58.2 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity59.04 m3·mol-1ChemAxon
Polarizability22.44 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (9.01 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General References
  1. Murphy K, Delanty N: Primary Generalized Epilepsies. Curr Treat Options Neurol. 2000 Nov;2(6):527-542. [PubMed:11096777 ]
  2. Kagitani-Shimono K, Imai K, Okamoto N, Ono J, Okada S: Unverricht-Lundborg disease with cystatin B gene abnormalities. Pediatr Neurol. 2002 Jan;26(1):55-60. [PubMed:11814737 ]
  3. Brown GM, Stone GH, Rathbone MP: Primidone and rapid cycling affective disorders. Lancet. 1993 Oct 9;342(8876):925. [PubMed:8105181 ]
  4. Schaffer LC, Schaffer CB, Caretto J: The use of primidone in the treatment of refractory bipolar disorder. Ann Clin Psychiatry. 1999 Jun;11(2):61-6. [PubMed:10440522 ]
  5. Young MC, Hughes IA: Loss of therapeutic control in congenital adrenal hyperplasia due to interaction between dexamethasone and primidone. Acta Paediatr Scand. 1991 Jan;80(1):120-4. [PubMed:2028784 ]
External Links
ATC CodesN03AA03
AHFS Codes
  • 28:12.04
PDB EntriesNot Available
FDA labelDownload (108 KB)
MSDSDownload (65.5 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Abiraterone can be decreased when it is combined with Primidone.
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Primidone.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Primidone.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Primidone.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Primidone.
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Primidone.
AldesleukinPrimidone may increase the hypotensive activities of Aldesleukin.
AliskirenPrimidone may increase the hypotensive activities of Aliskiren.
AmiloridePrimidone may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Primidone.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Primidone.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Primidone.
AmobarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Amobarbital.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Primidone.
Amyl NitritePrimidone may increase the hypotensive activities of Amyl Nitrite.
ApixabanThe serum concentration of Apixaban can be decreased when it is combined with Primidone.
ApraclonidinePrimidone may increase the hypotensive activities of Apraclonidine.
ApremilastThe serum concentration of Apremilast can be decreased when it is combined with Primidone.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Primidone.
ArtemetherThe serum concentration of the active metabolites of Artemether can be reduced when Artemether is used in combination with Primidone resulting in a loss in efficacy.
AtenololPrimidone may increase the hypotensive activities of Atenolol.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Primidone.
AzelastinePrimidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Azilsartan medoxomilPrimidone may increase the hypotensive activities of Azilsartan medoxomil.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Primidone.
BazedoxifeneThe serum concentration of Bazedoxifene can be decreased when it is combined with Primidone.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Primidone.
BenazeprilPrimidone may increase the hypotensive activities of Benazepril.
BendamustineThe serum concentration of Bendamustine can be decreased when it is combined with Primidone.
BendroflumethiazidePrimidone may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Primidone.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Primidone.
BoceprevirThe serum concentration of Boceprevir can be decreased when it is combined with Primidone.
BortezomibThe serum concentration of Bortezomib can be decreased when it is combined with Primidone.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Primidone.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Primidone.
BretyliumPrimidone may increase the hypotensive activities of Bretylium.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Primidone.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
BumetanidePrimidone may increase the hypotensive activities of Bumetanide.
BuprenorphinePrimidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Butabarbital.
ButalbitalThe metabolism of Butalbital can be increased when combined with Primidone.
ButethalThe risk or severity of adverse effects can be increased when Primidone is combined with Butethal.
CabozantinibThe serum concentration of Cabozantinib can be decreased when it is combined with Primidone.
CaffeineThe metabolism of Caffeine can be increased when combined with Primidone.
CanagliflozinPrimidone may increase the hypotensive activities of Canagliflozin.
CandesartanPrimidone may increase the hypotensive activities of Candesartan.
CannabidiolThe serum concentration of Cannabidiol can be decreased when it is combined with Primidone.
CaptoprilPrimidone may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Primidone.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Primidone.
CeritinibThe serum concentration of Ceritinib can be decreased when it is combined with Primidone.
ChloramphenicolThe metabolism of Primidone can be decreased when combined with Chloramphenicol.
ChlorothiazidePrimidone may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorthalidonePrimidone may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilPrimidone may increase the hypotensive activities of Cilazapril.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Primidone.
ClevidipinePrimidone may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Primidone.
ClonidinePrimidone may increase the hypotensive activities of Clonidine.
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Primidone.
CobicistatThe serum concentration of Cobicistat can be decreased when it is combined with Primidone.
CosyntropinCosyntropin may increase the hepatotoxic activities of Primidone.
CrizotinibThe serum concentration of Crizotinib can be decreased when it is combined with Primidone.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Primidone.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Primidone.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Primidone.
DapagliflozinPrimidone may increase the hypotensive activities of Dapagliflozin.
DasatinibThe serum concentration of Dasatinib can be decreased when it is combined with Primidone.
DesipramineThe metabolism of Desipramine can be increased when combined with Primidone.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Primidone.
DexamethasoneThe serum concentration of Dexamethasone can be decreased when it is combined with Primidone.
DexmedetomidinePrimidone may increase the hypotensive activities of Dexmedetomidine.
DexmethylphenidateThe serum concentration of the active metabolites of Primidone can be increased when Primidone is used in combination with Dexmethylphenidate.
DiclofenacThe serum concentration of Diclofenac can be decreased when it is combined with Primidone.
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Primidone.
DienogestThe serum concentration of Dienogest can be decreased when it is combined with Primidone.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Primidone.
DinutuximabPrimidone may increase the hypotensive activities of Dinutuximab.
DipyridamolePrimidone may increase the hypotensive activities of Dipyridamole.
DolutegravirThe serum concentration of Dolutegravir can be decreased when it is combined with Primidone.
DoxazosinPrimidone may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Primidone.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Primidone.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Primidone.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
DronabinolThe serum concentration of Dronabinol can be decreased when it is combined with Primidone.
DronedaroneThe serum concentration of Dronedarone can be decreased when it is combined with Primidone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Primidone.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Primidone.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Primidone.
EmpagliflozinPrimidone may increase the hypotensive activities of Empagliflozin.
EnalaprilPrimidone may increase the hypotensive activities of Enalapril.
EnalaprilatPrimidone may increase the hypotensive activities of Enalaprilat.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Primidone.
EplerenonePrimidone may increase the hypotensive activities of Eplerenone.
EprosartanPrimidone may increase the hypotensive activities of Eprosartan.
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Primidone.
Eslicarbazepine acetateThe serum concentration of Eslicarbazepine acetate can be decreased when it is combined with Primidone.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Primidone.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Primidone.
Etacrynic acidPrimidone may increase the hypotensive activities of Ethacrynic acid.
EthanolPrimidone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Ethinyl EstradiolThe therapeutic efficacy of Ethinyl Estradiol can be decreased when used in combination with Primidone.
EthoxzolamideThe risk or severity of adverse effects can be increased when Ethoxzolamide is combined with Primidone.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Primidone.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Primidone.
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Primidone.
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Primidone.
EverolimusThe serum concentration of Everolimus can be decreased when it is combined with Primidone.
ExemestaneThe serum concentration of Exemestane can be decreased when it is combined with Primidone.
FelbamateThe serum concentration of Primidone can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Primidone.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Primidone.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Primidone.
FludrocortisoneThe serum concentration of Fludrocortisone can be decreased when it is combined with Primidone.
FlunisolideThe metabolism of Flunisolide can be increased when combined with Primidone.
FluvoxamineThe metabolism of Fluvoxamine can be increased when combined with Primidone.
Folic AcidThe serum concentration of Primidone can be decreased when it is combined with Folic Acid.
FosinoprilPrimidone may increase the hypotensive activities of Fosinopril.
FosphenytoinThe metabolism of Primidone can be increased when combined with Fosphenytoin.
FurosemidePrimidone may increase the hypotensive activities of Furosemide.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Primidone.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Primidone.
GuanfacinePrimidone may increase the hypotensive activities of Guanfacine.
HeptabarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Heptabarbital.
HexobarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Hexobarbital.
HydralazinePrimidone may increase the hypotensive activities of Hydralazine.
HydrochlorothiazidePrimidone may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydrocodonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Primidone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Primidone.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Primidone.
IdelalisibThe serum concentration of Idelalisib can be decreased when it is combined with Primidone.
ImatinibThe serum concentration of Imatinib can be decreased when it is combined with Primidone.
ImipramineThe metabolism of Imipramine can be increased when combined with Primidone.
IndapamidePrimidone may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanPrimidone may increase the hypotensive activities of Irbesartan.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Primidone resulting in a loss in efficacy.
IsavuconazoniumThe serum concentration of the active metabolites of Isavuconazonium can be reduced when Isavuconazonium is used in combination with Primidone resulting in a loss in efficacy.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Primidone.
IsosorbidePrimidone may increase the hypotensive activities of Isosorbide.
Isosorbide DinitratePrimidone may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitratePrimidone may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprinePrimidone may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Primidone.
ItraconazoleThe serum concentration of Itraconazole can be decreased when it is combined with Primidone.
IvabradineThe serum concentration of Ivabradine can be decreased when it is combined with Primidone.
IvacaftorThe serum concentration of Ivacaftor can be decreased when it is combined with Primidone.
IxabepiloneThe serum concentration of Ixabepilone can be decreased when it is combined with Primidone.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Primidone.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Primidone.
LapatinibThe serum concentration of Lapatinib can be decreased when it is combined with Primidone.
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Primidone.
LeucovorinThe serum concentration of Primidone can be decreased when it is combined with Leucovorin.
LevobunololPrimidone may increase the hypotensive activities of Levobunolol.
LevomefolateThe serum concentration of the active metabolites of Primidone can be reduced when Primidone is used in combination with Levomefolate resulting in a loss in efficacy.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Primidone.
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Primidone.
LisinoprilPrimidone may increase the hypotensive activities of Lisinopril.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Primidone.
LosartanPrimidone may increase the hypotensive activities of Losartan.
LumefantrineThe serum concentration of Lumefantrine can be decreased when it is combined with Primidone.
LurasidoneThe serum concentration of Lurasidone can be decreased when it is combined with Primidone.
MacitentanThe serum concentration of MACITENTAN can be decreased when it is combined with Primidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Primidone.
MannitolPrimidone may increase the hypotensive activities of Mannitol.
MaravirocThe serum concentration of Maraviroc can be decreased when it is combined with Primidone.
MecamylaminePrimidone may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Primidone.
MefloquineThe therapeutic efficacy of Primidone can be decreased when used in combination with Mefloquine.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Primidone.
MetforminPrimidone may increase the hypotensive activities of Metformin.
MethadoneThe serum concentration of Methadone can be decreased when it is combined with Primidone.
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Primidone.
MethohexitalThe risk or severity of adverse effects can be increased when Primidone is combined with Methohexital.
MethotrimeprazinePrimidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethyclothiazidePrimidone may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaPrimidone may increase the hypotensive activities of Methyldopa.
MethylphenidateThe serum concentration of the active metabolites of Primidone can be increased when Primidone is used in combination with Methylphenidate.
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Primidone.
MetipranololPrimidone may increase the hypotensive activities of Metipranolol.
MetolazonePrimidone may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Primidone.
MetronidazoleThe serum concentration of Metronidazole can be decreased when it is combined with Primidone.
MetyrosinePrimidone may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Mifepristone can be decreased when it is combined with Primidone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Primidone.
MinoxidilPrimidone may increase the hypotensive activities of Minoxidil.
MoexiprilPrimidone may increase the hypotensive activities of Moexipril.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Primidone.
NadololPrimidone may increase the hypotensive activities of Nadolol.
NaloxegolThe serum concentration of Naloxegol can be decreased when it is combined with Primidone.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Primidone.
NesiritidePrimidone may increase the hypotensive activities of Nesiritide.
NetupitantThe serum concentration of Netupitant can be decreased when it is combined with Primidone.
NicardipineThe metabolism of Nicardipine can be increased when combined with Primidone.
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Primidone.
NilotinibThe serum concentration of Nilotinib can be decreased when it is combined with Primidone.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Primidone.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Primidone.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Primidone.
NitroglycerinPrimidone may increase the hypotensive activities of Nitroglycerin.
NitroprussidePrimidone may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Primidone.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Primidone.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Primidone.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Primidone.
OlmesartanPrimidone may increase the hypotensive activities of Olmesartan.
OrlistatThe serum concentration of Primidone can be decreased when it is combined with Orlistat.
OrphenadrinePrimidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Primidone.
PaliperidoneThe serum concentration of Paliperidone can be decreased when it is combined with Primidone.
PanobinostatThe serum concentration of Panobinostat can be decreased when it is combined with Primidone.
PapaverinePrimidone may increase the hypotensive activities of Papaverine.
ParaldehydePrimidone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Primidone is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Primidone.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Primidone.
PentobarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Pentobarbital.
PerampanelThe serum concentration of Perampanel can be decreased when it is combined with Primidone.
PerindoprilPrimidone may increase the hypotensive activities of Perindopril.
PethidinePrimidone may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PhenobarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Phenobarbital.
PhenytoinThe metabolism of Primidone can be increased when combined with Phenytoin.
PindololThe serum concentration of Pindolol can be decreased when it is combined with Primidone.
PirfenidoneThe serum concentration of Pirfenidone can be decreased when it is combined with Primidone.
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Primidone.
PramipexolePrimidone may increase the sedative activities of Pramipexole.
PraziquantelThe serum concentration of Praziquantel can be decreased when it is combined with Primidone.
PrazosinPrimidone may increase the hypotensive activities of Prazosin.
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Primidone.
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Propafenone can be decreased when it is combined with Primidone.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Primidone.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Primidone.
PyridoxineThe metabolism of Primidone can be increased when combined with Pyridoxine.
QuetiapinePrimidone may increase the hypotensive activities of Quetiapine.
QuinaprilPrimidone may increase the hypotensive activities of Quinapril.
QuinidineThe serum concentration of Quinidine can be decreased when it is combined with Primidone.
RamiprilPrimidone may increase the hypotensive activities of Ramipril.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Primidone.
RegorafenibThe serum concentration of Regorafenib can be decreased when it is combined with Primidone.
ReserpinePrimidone may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Primidone can be increased when combined with Rifabutin.
RifampicinThe metabolism of Primidone can be increased when combined with Rifampicin.
RifapentineThe metabolism of Primidone can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Primidone.
RiociguatPrimidone may increase the hypotensive activities of Riociguat.
RitonavirThe serum concentration of Ritonavir can be decreased when it is combined with Primidone.
RivaroxabanThe serum concentration of Rivaroxaban can be decreased when it is combined with Primidone.
RoflumilastThe serum concentration of Roflumilast can be decreased when it is combined with Primidone.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Primidone.
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Primidone.
RotigotinePrimidone may increase the sedative activities of Rotigotine.
RufinamideThe serum concentration of Rufinamide can be decreased when it is combined with Primidone.
SaquinavirThe serum concentration of Saquinavir can be decreased when it is combined with Primidone.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Primidone.
SecobarbitalThe risk or severity of adverse effects can be increased when Primidone is combined with Secobarbital.
SildenafilThe metabolism of Sildenafil can be increased when combined with Primidone.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Primidone.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Primidone.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Primidone.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Primidone.
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Primidone.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Primidone.
SpironolactonePrimidone may increase the hypotensive activities of Spironolactone.
SunitinibThe serum concentration of Sunitinib can be decreased when it is combined with Primidone.
SuvorexantThe serum concentration of Suvorexant can be decreased when it is combined with Primidone.
TadalafilThe serum concentration of Tadalafil can be decreased when it is combined with Primidone.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Primidone.
TasimelteonThe serum concentration of Tasimelteon can be decreased when it is combined with Primidone.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Primidone.
TelmisartanPrimidone may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Primidone.
TerazosinPrimidone may increase the hypotensive activities of Terazosin.
ThalidomidePrimidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Primidone.
TicagrelorThe serum concentration of the active metabolites of Ticagrelor can be reduced when Ticagrelor is used in combination with Primidone resulting in a loss in efficacy.
TimololThe serum concentration of Timolol can be decreased when it is combined with Primidone.
TizanidinePrimidone may increase the hypotensive activities of Tizanidine.
TofacitinibThe serum concentration of Tofacitinib can be decreased when it is combined with Primidone.
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Primidone.
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Primidone.
TorasemidePrimidone may increase the hypotensive activities of Torasemide.
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Primidone.
TrabectedinThe serum concentration of Trabectedin can be decreased when it is combined with Primidone.
TrandolaprilPrimidone may increase the hypotensive activities of Trandolapril.
TreprostinilThe serum concentration of Treprostinil can be decreased when it is combined with Primidone.
TriamterenePrimidone may increase the hypotensive activities of Triamterene.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Primidone.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Primidone.
Valproic AcidThe metabolism of Primidone can be decreased when combined with Valproic Acid.
ValsartanPrimidone may increase the hypotensive activities of Valsartan.
VandetanibThe serum concentration of Vandetanib can be decreased when it is combined with Primidone.
VemurafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Primidone.
VerapamilThe metabolism of Verapamil can be increased when combined with Primidone.
VilazodoneThe serum concentration of Vilazodone can be decreased when it is combined with Primidone.
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Primidone.
VorapaxarThe serum concentration of Vorapaxar can be decreased when it is combined with Primidone.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Primidone.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Primidone.
WarfarinThe metabolism of Warfarin can be increased when combined with Primidone.
ZaleplonThe serum concentration of Zaleplon can be decreased when it is combined with Primidone.
ZolpidemPrimidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Primidone.
Food Interactions
  • Avoid alcohol.
  • Avoid high doses of caffeine.
  • Take with food to reduce gastric irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. [PubMed:14579514 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  3. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  4. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  6. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  7. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA2
Uniprot ID:
P47869
Molecular Weight:
51325.85 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA3
Uniprot ID:
P34903
Molecular Weight:
55164.055 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA4
Uniprot ID:
P48169
Molecular Weight:
61622.645 Da
References
  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Transporter activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA5
Uniprot ID:
P31644
Molecular Weight:
52145.645 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA6
Uniprot ID:
Q16445
Molecular Weight:
51023.69 Da
References
  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  2. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ligand-gated ion channel activity
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions.
Gene Name:
CHRNA4
Uniprot ID:
P43681
Molecular Weight:
69956.47 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Toxic substance binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
Gene Name:
CHRNA7
Uniprot ID:
P36544
Molecular Weight:
56448.925 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ionotropic glutamate receptor activity
Specific Function:
Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and t...
Gene Name:
GRIA2
Uniprot ID:
P42262
Molecular Weight:
98820.32 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Kainate selective glutamate receptor activity
Specific Function:
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inacti...
Gene Name:
GRIK2
Uniprot ID:
Q13002
Molecular Weight:
102582.475 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
positive allosteric modulator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. ChEMBL Compound Report Card [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  3. The P450 Program [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23