You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NamePentobarbital
Accession NumberDB00312  (APRD01174)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236)

Structure
Thumb
Synonyms
5-Ethyl-5-(1-methyl-butyl)-pyrimidine-2,4,6-trione
5-Ethyl-5-(1-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
5-ethyl-5-(1-methylbutyl)barbituric acid
5-ethyl-5-(sec-pentyl)barbituric acid
Nembutal
Pentobarbital
Pentobarbitone
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nembutal Sodium Cap 100mgcapsule100 mgoralAbbott Laboratories, Limited1951-12-311997-08-18Canada
Nembutal Sodium Inj 50mg/mlsolution50 mgintramuscular; intravenousAbbott Laboratories, Limited1976-12-312008-06-06Canada
Nova Rectal Sup 25mgsuppository25 mgrectalSabex Inc1984-12-311999-08-12Canada
Nova Rectal Sup 50mgsuppository50 mgrectalSabex Inc1984-12-312001-08-02Canada
Novo-pentobarb 100mgcapsule100 mgoralNovopharm Limited1967-12-312005-08-10Canada
Pentobarbital Sodium Cap 50mgcapsule50 mgoralSands Pharm1972-12-311996-09-10Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nembutal Sodiuminjection50 mg/mLintramuscular; intravenousOak Pharmaceuticals, Inc. (Subsidiary of Akorn, Inc.)1973-09-19Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
NembutalLundbeck
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pentobarbital Sodium
Thumb
  • InChI Key: QGMRQYFBGABWDR-UHFFFAOYNA-M
  • Monoisotopic Mass: 248.113687095
  • Average Mass: 248.254
DBSALT000442
Categories
UNIII4744080IR
CAS number76-74-4
WeightAverage: 226.2722
Monoisotopic: 226.131742452
Chemical FormulaC11H18N2O3
InChI KeyInChIKey=WEXRUCMBJFQVBZ-UHFFFAOYSA-N
InChI
InChI=1S/C11H18N2O3/c1-4-6-7(3)11(5-2)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)
IUPAC Name
5-ethyl-5-(pentan-2-yl)-1,3-diazinane-2,4,6-trione
SMILES
CCCC(C)C1(CC)C(=O)NC(=O)NC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as barbituric acid derivatives. These are compounds containing a perhydropyrimidine ring substituted at C-2, -4 and -6 by oxo groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentBarbituric acid derivatives
Alternative Parents
Substituents
  • Barbiturate
  • Ureide
  • 1,3-diazinane
  • Urea
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the short-term treatment of insomnia.
PharmacodynamicsPentobarbital, a barbiturate, is used for the treatment of short term insomnia. It belongs to a group of medicines called central nervous system (CNS) depressants that induce drowsiness and relieve tension or nervousness. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Mechanism of actionPentobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Related Articles
AbsorptionBarbiturates are absorbed in varying degrees following oral, rectal, or parenteral administration.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

by hepatic microsomal enzyme system

Route of eliminationBarbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine, and less commonly, in the feces. Approximately 25 to 50 percent of a dose of aprobarbital or phenobarbital is eliminated unchanged in the urine, whereas the amount of other barbiturates excreted unchanged in the urine is negligible.
Half life5 to 50 hours (dose dependent)
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+0.9156
Blood Brain Barrier+0.9713
Caco-2 permeable-0.5926
P-glycoprotein substrateSubstrate0.5947
P-glycoprotein inhibitor INon-inhibitor0.6155
P-glycoprotein inhibitor IINon-inhibitor0.9218
Renal organic cation transporterNon-inhibitor0.923
CYP450 2C9 substrateNon-substrate0.7789
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateNon-substrate0.7066
CYP450 1A2 substrateNon-inhibitor0.9086
CYP450 2C9 inhibitorNon-inhibitor0.7484
CYP450 2D6 inhibitorNon-inhibitor0.9301
CYP450 2C19 inhibitorNon-inhibitor0.711
CYP450 3A4 inhibitorNon-inhibitor0.9522
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9276
Ames testNon AMES toxic0.6789
CarcinogenicityNon-carcinogens0.89
BiodegradationNot ready biodegradable0.9603
Rat acute toxicity3.2266 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9685
hERG inhibition (predictor II)Non-inhibitor0.8771
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ovation pharmaceuticals inc
  • Lannett co inc
  • Vitarine pharmaceuticals inc
  • Whiteworth towne paulsen inc
  • Anabolic inc
  • Elkins sinn div ah robins co inc
  • Everylife
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Parke davis div warner lambert co
  • L perrigo co
  • Purepac pharmaceutical co
  • Valeant pharmaceuticals international
  • Watson laboratories inc
  • Wyeth ayerst laboratories
  • Lundbeck inc
  • Nexgen pharma inc
Packagers
Dosage forms
FormRouteStrength
Injectionintramuscular; intravenous50 mg/mL
Capsuleoral100 mg
Solutionintramuscular; intravenous50 mg
Suppositoryrectal25 mg
Suppositoryrectal50 mg
Capsuleoral50 mg
Prices
Unit descriptionCostUnit
Pentobarbital sodium powder27.0USD g
Nembutal sodium 50 mg/ml via20.65USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point129.5 °CPhysProp
water solubility679 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.10HANSCH,C ET AL. (1995)
logS-2.52ADME Research, USCD
pKa8.11 (at 25 °C)SERJEANT,EP & DEMPSEY,B (1979)
Predicted Properties
PropertyValueSource
Water Solubility0.864 mg/mLALOGPS
logP2.16ALOGPS
logP1.89ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity58 m3·mol-1ChemAxon
Polarizability23.41 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.77 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Positivesplash10-004i-1290000000-90bfbd79bea4fe2b007bView in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Positivesplash10-0bti-1900000000-7e31dcdb272669c13101View in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Positivesplash10-01bc-9100000000-c9fe8276b8137dc73d20View in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Negativesplash10-004i-3980000000-84ea889a0fae4bed224bView in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Negativesplash10-0006-9500000000-c226fe2dfb4ee13e4ae8View in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Negativesplash10-000x-9500000000-cd4190b9c110ee5e4428View in MoNA
MSMass Spectrum (Electron Ionization)splash10-0a4l-6900000000-a65d8c67e006ad448814View in MoNA
References
Synthesis ReferenceNot Available
General References
  1. Knodell RG, Spector MH, Brooks DA, Keller FX, Kyner WT: Alterations in pentobarbital pharmacokinetics in response to parenteral and enteral alimentation in the rat. Gastroenterology. 1980 Dec;79(6):1211-6. [PubMed:6777235 ]
External Links
ATC CodesN05CA01
AHFS Codes
  • 28:24.04
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (50.3 KB)
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Pentobarbital.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Pentobarbital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Pentobarbital.
AcetazolamidePentobarbital may increase the hypotensive activities of Acetazolamide.
AldesleukinPentobarbital may increase the hypotensive activities of Aldesleukin.
AliskirenPentobarbital may increase the hypotensive activities of Aliskiren.
AmiloridePentobarbital may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Pentobarbital.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Pentobarbital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Pentobarbital.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Pentobarbital.
AmrinoneThe metabolism of Amrinone can be increased when combined with Pentobarbital.
Amyl NitritePentobarbital may increase the hypotensive activities of Amyl Nitrite.
ApraclonidinePentobarbital may increase the hypotensive activities of Apraclonidine.
AtenololPentobarbital may increase the hypotensive activities of Atenolol.
AzelastinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Azilsartan medoxomilPentobarbital may increase the hypotensive activities of Azilsartan medoxomil.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Pentobarbital.
BenazeprilPentobarbital may increase the hypotensive activities of Benazepril.
BendroflumethiazidePentobarbital may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BepridilThe metabolism of Bepridil can be increased when combined with Pentobarbital.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Pentobarbital.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Pentobarbital.
BretyliumPentobarbital may increase the hypotensive activities of Bretylium.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
BumetanidePentobarbital may increase the hypotensive activities of Bumetanide.
BuprenorphinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButalbitalThe metabolism of Butalbital can be increased when combined with Pentobarbital.
CaffeineThe metabolism of Caffeine can be increased when combined with Pentobarbital.
CanagliflozinPentobarbital may increase the hypotensive activities of Canagliflozin.
CandesartanPentobarbital may increase the hypotensive activities of Candesartan.
CaptoprilPentobarbital may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Pentobarbital.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Pentobarbital.
ChloramphenicolThe metabolism of Pentobarbital can be decreased when combined with Chloramphenicol.
ChlorothiazidePentobarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Pentobarbital.
ChlorthalidonePentobarbital may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilPentobarbital may increase the hypotensive activities of Cilazapril.
ClevidipinePentobarbital may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Pentobarbital.
ClonidinePentobarbital may increase the hypotensive activities of Clonidine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Pentobarbital.
DapagliflozinPentobarbital may increase the hypotensive activities of Dapagliflozin.
DesipramineThe metabolism of Desipramine can be increased when combined with Pentobarbital.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Pentobarbital.
DexmedetomidinePentobarbital may increase the hypotensive activities of Dexmedetomidine.
DiclofenamidePentobarbital may increase the hypotensive activities of Diclofenamide.
DicoumarolThe metabolism of Dicoumarol can be increased when combined with Pentobarbital.
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Pentobarbital.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Pentobarbital.
DinutuximabPentobarbital may increase the hypotensive activities of Dinutuximab.
DipyridamolePentobarbital may increase the hypotensive activities of Dipyridamole.
DoxazosinPentobarbital may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Pentobarbital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Pentobarbital.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Pentobarbital.
EmpagliflozinPentobarbital may increase the hypotensive activities of Empagliflozin.
EnalaprilPentobarbital may increase the hypotensive activities of Enalapril.
EnalaprilatPentobarbital may increase the hypotensive activities of Enalaprilat.
EplerenonePentobarbital may increase the hypotensive activities of Eplerenone.
EprosartanPentobarbital may increase the hypotensive activities of Eprosartan.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Pentobarbital.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Pentobarbital.
Etacrynic acidPentobarbital may increase the hypotensive activities of Ethacrynic acid.
EthanolPentobarbital 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 Pentobarbital.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Pentobarbital.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Pentobarbital.
FelbamateThe serum concentration of Pentobarbital can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Pentobarbital.
FlunarizineThe metabolism of Flunarizine can be increased when combined with Pentobarbital.
FosinoprilPentobarbital may increase the hypotensive activities of Fosinopril.
FurosemidePentobarbital may increase the hypotensive activities of Furosemide.
GabapentinThe metabolism of Gabapentin can be increased when combined with Pentobarbital.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Pentobarbital.
GuanfacinePentobarbital may increase the hypotensive activities of Guanfacine.
HydralazinePentobarbital may increase the hypotensive activities of Hydralazine.
HydrochlorothiazidePentobarbital may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydrocodonePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
ImipramineThe metabolism of Imipramine can be increased when combined with Pentobarbital.
IndapamidePentobarbital may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanPentobarbital may increase the hypotensive activities of Irbesartan.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Pentobarbital.
IsosorbidePentobarbital may increase the hypotensive activities of Isosorbide.
Isosorbide DinitratePentobarbital may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitratePentobarbital may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprinePentobarbital may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Pentobarbital.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Pentobarbital.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Pentobarbital.
LercanidipineThe metabolism of Lercanidipine can be increased when combined with Pentobarbital.
LevobunololPentobarbital may increase the hypotensive activities of Levobunolol.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Pentobarbital.
LisinoprilPentobarbital may increase the hypotensive activities of Lisinopril.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Pentobarbital.
LosartanPentobarbital may increase the hypotensive activities of Losartan.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
MannitolPentobarbital may increase the hypotensive activities of Mannitol.
MecamylaminePentobarbital may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone AcetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Pentobarbital.
MefloquineThe therapeutic efficacy of Pentobarbital can be decreased when used in combination with Mefloquine.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Pentobarbital.
MetforminPentobarbital may increase the hypotensive activities of Metformin.
MethazolamidePentobarbital may increase the hypotensive activities of Methazolamide.
MethotrimeprazinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethyclothiazidePentobarbital may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaPentobarbital may increase the hypotensive activities of Methyldopa.
MetipranololPentobarbital may increase the hypotensive activities of Metipranolol.
MetolazonePentobarbital may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Pentobarbital.
MetyrosinePentobarbital may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
MinoxidilPentobarbital may increase the hypotensive activities of Minoxidil.
MirtazapinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoexiprilPentobarbital may increase the hypotensive activities of Moexipril.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
NadololPentobarbital may increase the hypotensive activities of Nadolol.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Pentobarbital.
NesiritidePentobarbital may increase the hypotensive activities of Nesiritide.
NicardipineThe metabolism of Nicardipine can be increased when combined with Pentobarbital.
NicotineThe metabolism of Nicotine can be increased when combined with Pentobarbital.
NifedipineThe metabolism of Nifedipine can be increased when combined with Pentobarbital.
NimodipineThe metabolism of Nimodipine can be increased when combined with Pentobarbital.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Pentobarbital.
NitrendipineThe metabolism of Nitrendipine can be increased when combined with Pentobarbital.
NitroglycerinPentobarbital may increase the hypotensive activities of Nitroglycerin.
NitroprussidePentobarbital may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Pentobarbital.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Pentobarbital.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Pentobarbital.
OlmesartanPentobarbital may increase the hypotensive activities of Olmesartan.
OrphenadrinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PapaverinePentobarbital may increase the hypotensive activities of Papaverine.
ParaldehydePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Paroxetine.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
PerhexilineThe metabolism of Perhexiline can be increased when combined with Pentobarbital.
PerindoprilPentobarbital may increase the hypotensive activities of Perindopril.
PethidinePentobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PindololThe serum concentration of Pindolol can be decreased when it is combined with Pentobarbital.
PramipexolePentobarbital may increase the sedative activities of Pramipexole.
PrazosinPentobarbital may increase the hypotensive activities of Prazosin.
PrenylamineThe metabolism of Prenylamine can be increased when combined with Pentobarbital.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Pentobarbital.
PropacetamolThe metabolism of Propacetamol can be increased when combined with Pentobarbital.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Pentobarbital.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Pentobarbital.
PyridoxineThe metabolism of Pentobarbital can be increased when combined with Pyridoxine.
QuetiapinePentobarbital may increase the hypotensive activities of Quetiapine.
QuinaprilPentobarbital may increase the hypotensive activities of Quinapril.
RamiprilPentobarbital may increase the hypotensive activities of Ramipril.
ReserpinePentobarbital may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Pentobarbital can be increased when combined with Rifabutin.
RifampicinThe metabolism of Pentobarbital can be increased when combined with Rifampicin.
RifapentineThe metabolism of Pentobarbital can be increased when combined with Rifapentine.
RiociguatPentobarbital may increase the hypotensive activities of Riociguat.
RisedronateThe metabolism of Risedronate can be increased when combined with Pentobarbital.
RopinirolePentobarbital may increase the sedative activities of Ropinirole.
RotigotinePentobarbital may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Pentobarbital.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
SomatostatinThe risk or severity of adverse effects can be increased when Somatostatin is combined with Pentobarbital.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Pentobarbital.
SpironolactonePentobarbital may increase the hypotensive activities of Spironolactone.
SuvorexantPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
TelmisartanPentobarbital may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Pentobarbital.
TerazosinPentobarbital may increase the hypotensive activities of Terazosin.
ThalidomidePentobarbital 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 Pentobarbital.
TimololThe serum concentration of Timolol can be decreased when it is combined with Pentobarbital.
TizanidinePentobarbital may increase the hypotensive activities of Tizanidine.
TorasemidePentobarbital may increase the hypotensive activities of Torasemide.
TrandolaprilPentobarbital may increase the hypotensive activities of Trandolapril.
TriamterenePentobarbital may increase the hypotensive activities of Triamterene.
TrichlormethiazidePentobarbital may increase the orthostatic hypotensive activities of Trichlormethiazide.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Pentobarbital.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Pentobarbital.
Valproic AcidThe serum concentration of Pentobarbital can be increased when it is combined with Valproic Acid.
ValsartanPentobarbital may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Pentobarbital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Pentobarbital.
WarfarinThe metabolism of Warfarin can be increased when combined with Pentobarbital.
ZolpidemPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

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. Steinbach JH, Akk G: Modulation of GABA(A) receptor channel gating by pentobarbital. J Physiol. 2001 Dec 15;537(Pt 3):715-33. [PubMed:11744750 ]
  2. 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 ]
  3. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  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. 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 ]
  6. Davies DL, McCauley LD, Bolger MB, Alkana RL: Pressure-sensitive and -insensitive coupling in gamma-aminobutyric acid(A) receptors. Psychopharmacology (Berl). 2001 Oct;157(4):401-10. [PubMed:11605100 ]
  7. Rahman M, Zhu D, Lindblad C, Johansson IM, Holmberg E, Isaksson M, Taube M, Backstrom T, Wang MD: GABA-site antagonism and pentobarbital actions do not depend on the alpha-subunit type in the recombinant rat GABA receptor. Acta Physiol (Oxf). 2006 Aug;187(4):479-88. [PubMed:16866778 ]
  8. Feigenspan A, Weiler R: Electrophysiological properties of mouse horizontal cell GABAA receptors. J Neurophysiol. 2004 Nov;92(5):2789-801. Epub 2004 Jul 7. [PubMed:15240758 ]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  10. 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 ]
  11. 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]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated cation channel activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors (By similarity).
Components:
NameUniProt IDDetails
Glutamate receptor ionotropic, NMDA 1Q05586 Details
Glutamate receptor ionotropic, NMDA 2AQ12879 Details
Glutamate receptor ionotropic, NMDA 2BQ13224 Details
Glutamate receptor ionotropic, NMDA 2CQ14957 Details
Glutamate receptor ionotropic, NMDA 2DO15399 Details
Glutamate receptor ionotropic, NMDA 3AQ8TCU5 Details
Glutamate receptor ionotropic, NMDA 3BO60391 Details
References
  1. Daniell LC: Effect of anesthetic and convulsant barbiturates on N-methyl-D-aspartate receptor-mediated calcium flux in brain membrane vesicles. Pharmacology. 1994 Nov;49(5):296-307. [PubMed:7862741 ]

Enzymes

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. Lexicomp
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Lexicomp
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09