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Identification
NameButabarbital
Accession NumberDB00237  (APRD00752)
TypeSmall Molecule
GroupsApproved, Illicit
Description

Butabarbital (trade name Butisol) is a prescription barbiturate sleep aid. Butabarbital has a particularly fast onset of effects and short duration of action compared to other barbiturates, which makes it useful for certain applications such as treating severe insomnia and relieving anxiety before surgical procedures; however it is also relatively dangerous particularly when combined with alcohol, and so is now rarely used, although it is still prescribed in some Eastern European and South American countries. Its short duration of action gives butabarbital a high abuse potential, comparable to secobarbital. [Wikipedia]

Structure
Thumb
Synonyms
5-Ethyl-5-(1-methylpropyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Ethyl-5-(1-methylpropyl)barbituric acid
5-Sec-butyl-5-ethyl-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Sec-butyl-5-ethylbarbituric acid
5-Sec-butyl-5-ethylpyrimidine-2,4,6(1H,3H,5H)-trione
Butabarbital
Butisol
Secbutabarbital
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Butisol Sodiumtablet30 mg/1oralMeda Pharmaceuticals Inc.1939-08-01Not applicableUs
Butisol Sodium Tab 100mgtablet100 mgoralCarter Horner Corp.1982-12-312001-01-02Canada
Butisol Sodium Tab 15mgtablet15 mgoralCarter Horner Corp.1982-12-312001-01-02Canada
Butisol Sodium Tab 30mgtablet30 mgoralCarter Horner Corp.1982-12-312001-01-02Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ButalanNot Available
ButisolNot Available
Sarisol No. 2Not Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Butabarbital Sodium
Thumb
  • InChI Key: QORQZMBCPRBCAB-UHFFFAOYNA-M
  • Monoisotopic Mass: 234.098037031
  • Average Mass: 234.2275
DBSALT000312
Categories
UNIIP0078O25A9
CAS number125-40-6
WeightAverage: 212.2456
Monoisotopic: 212.116092388
Chemical FormulaC10H16N2O3
InChI KeyInChIKey=ZRIHAIZYIMGOAB-UHFFFAOYSA-N
InChI
InChI=1S/C10H16N2O3/c1-4-6(3)10(5-2)7(13)11-9(15)12-8(10)14/h6H,4-5H2,1-3H3,(H2,11,12,13,14,15)
IUPAC Name
5-(butan-2-yl)-5-ethyl-1,3-diazinane-2,4,6-trione
SMILES
CCC(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 short-term treatment of insomnia and anxiety disorders
PharmacodynamicsButabarbital, 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 actionButabarbital 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
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationBarbiturates are metabolized primarily by the hepatic microsomal enzyme system, and most metabolic products are excreted in the urine.
Half lifeNot Available
ClearanceNot Available
ToxicitySigns of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
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+0.9324
Blood Brain Barrier+0.9782
Caco-2 permeable-0.6013
P-glycoprotein substrateSubstrate0.5938
P-glycoprotein inhibitor INon-inhibitor0.617
P-glycoprotein inhibitor IINon-inhibitor0.961
Renal organic cation transporterNon-inhibitor0.9465
CYP450 2C9 substrateNon-substrate0.7719
CYP450 2D6 substrateNon-substrate0.9014
CYP450 3A4 substrateNon-substrate0.7098
CYP450 1A2 substrateNon-inhibitor0.8775
CYP450 2C9 inhibitorNon-inhibitor0.821
CYP450 2D6 inhibitorNon-inhibitor0.933
CYP450 2C19 inhibitorNon-inhibitor0.7828
CYP450 3A4 inhibitorNon-inhibitor0.9203
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9458
Ames testNon AMES toxic0.6458
CarcinogenicityNon-carcinogens0.8533
BiodegradationNot ready biodegradable0.9759
Rat acute toxicity3.6803 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.99
hERG inhibition (predictor II)Non-inhibitor0.9233
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Medpointe pharmaceuticals medpointe healthcare inc
  • Alpharma us pharmaceuticals division
  • Wockhardt eu operations (swiss) ag
  • Lannett co inc
  • Meda pharmaceuticals inc
  • Halsey drug co inc
  • Cm bundy co
  • Sandoz inc
  • Solvay pharmaceuticals
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Whiteworth towne paulsen inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Marshall pharmacal corp
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Tabletoral30 mg/1
Tabletoral100 mg
Tabletoral15 mg
Tabletoral30 mg
Prices
Unit descriptionCostUnit
Butisol sodium 50 mg tablet2.46USD tablet
Butisol sodium 30 mg tablet1.89USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point166.5 °CPhysProp
water solubility1360 mg/LNot Available
logP1.65WONG,O & MCKEOWN,RH (1988)
Predicted Properties
PropertyValueSource
Water Solubility1.39 mg/mLALOGPS
logP1.7ALOGPS
logP1.45ChemAxon
logS-2.2ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity53.4 m3·mol-1ChemAxon
Polarizability21.41 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
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
MSMass Spectrum (Electron Ionization)splash10-0a4l-6900000000-6e0cbc3d26c5541ad8ebView in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Butabarbital.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Butabarbital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Butabarbital.
AcetazolamideButabarbital may increase the hypotensive activities of Acetazolamide.
AldesleukinButabarbital may increase the hypotensive activities of Aldesleukin.
AliskirenButabarbital may increase the hypotensive activities of Aliskiren.
AmilorideButabarbital may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Butabarbital.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Butabarbital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Butabarbital.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Butabarbital.
AmrinoneThe metabolism of Amrinone can be increased when combined with Butabarbital.
Amyl NitriteButabarbital may increase the hypotensive activities of Amyl Nitrite.
ApraclonidineButabarbital may increase the hypotensive activities of Apraclonidine.
AtenololButabarbital may increase the hypotensive activities of Atenolol.
AzelastineButabarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Azilsartan medoxomilButabarbital may increase the hypotensive activities of Azilsartan medoxomil.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Butabarbital.
BenazeprilButabarbital may increase the hypotensive activities of Benazepril.
BendroflumethiazideButabarbital may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BepridilThe metabolism of Bepridil can be increased when combined with Butabarbital.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Butabarbital.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Butabarbital.
BretyliumButabarbital may increase the hypotensive activities of Bretylium.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
BumetanideButabarbital may increase the hypotensive activities of Bumetanide.
BuprenorphineButabarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButalbitalThe metabolism of Butalbital can be increased when combined with Butabarbital.
CaffeineThe metabolism of Caffeine can be increased when combined with Butabarbital.
CanagliflozinButabarbital may increase the hypotensive activities of Canagliflozin.
CandesartanButabarbital may increase the hypotensive activities of Candesartan.
CaptoprilButabarbital may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Butabarbital.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Butabarbital.
ChloramphenicolThe metabolism of Butabarbital can be decreased when combined with Chloramphenicol.
ChlorothiazideButabarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Butabarbital.
ChlorthalidoneButabarbital may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilButabarbital may increase the hypotensive activities of Cilazapril.
ClevidipineButabarbital may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Butabarbital.
ClonidineButabarbital may increase the hypotensive activities of Clonidine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Butabarbital.
DapagliflozinButabarbital may increase the hypotensive activities of Dapagliflozin.
DesipramineThe metabolism of Desipramine can be increased when combined with Butabarbital.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Butabarbital.
DexmedetomidineButabarbital may increase the hypotensive activities of Dexmedetomidine.
DiclofenamideButabarbital may increase the hypotensive activities of Diclofenamide.
DicoumarolThe metabolism of Dicoumarol can be increased when combined with Butabarbital.
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Butabarbital.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Butabarbital.
DinutuximabButabarbital may increase the hypotensive activities of Dinutuximab.
DipyridamoleButabarbital may increase the hypotensive activities of Dipyridamole.
DoxazosinButabarbital may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Butabarbital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Butabarbital.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Butabarbital.
EmpagliflozinButabarbital may increase the hypotensive activities of Empagliflozin.
EnalaprilButabarbital may increase the hypotensive activities of Enalapril.
EnalaprilatButabarbital may increase the hypotensive activities of Enalaprilat.
EplerenoneButabarbital may increase the hypotensive activities of Eplerenone.
EprosartanButabarbital may increase the hypotensive activities of Eprosartan.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Butabarbital.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Butabarbital.
Etacrynic acidButabarbital may increase the hypotensive activities of Ethacrynic acid.
EthanolButabarbital 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 Butabarbital.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Butabarbital.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Butabarbital.
FelbamateThe serum concentration of Butabarbital can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Butabarbital.
FlunarizineThe metabolism of Flunarizine can be increased when combined with Butabarbital.
FosinoprilButabarbital may increase the hypotensive activities of Fosinopril.
FurosemideButabarbital may increase the hypotensive activities of Furosemide.
GabapentinThe metabolism of Gabapentin can be increased when combined with Butabarbital.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Butabarbital.
GuanfacineButabarbital may increase the hypotensive activities of Guanfacine.
HydralazineButabarbital may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideButabarbital may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydrocodoneButabarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
ImipramineThe metabolism of Imipramine can be increased when combined with Butabarbital.
IndapamideButabarbital may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanButabarbital may increase the hypotensive activities of Irbesartan.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Butabarbital.
IsosorbideButabarbital may increase the hypotensive activities of Isosorbide.
Isosorbide DinitrateButabarbital may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitrateButabarbital may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprineButabarbital may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Butabarbital.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Butabarbital.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Butabarbital.
LercanidipineThe metabolism of Lercanidipine can be increased when combined with Butabarbital.
LevobunololButabarbital may increase the hypotensive activities of Levobunolol.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Butabarbital.
LisinoprilButabarbital may increase the hypotensive activities of Lisinopril.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Butabarbital.
LosartanButabarbital may increase the hypotensive activities of Losartan.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
MannitolButabarbital may increase the hypotensive activities of Mannitol.
MecamylamineButabarbital may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Butabarbital.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Butabarbital.
MetforminButabarbital may increase the hypotensive activities of Metformin.
MethazolamideButabarbital may increase the hypotensive activities of Methazolamide.
MethotrimeprazineButabarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethyclothiazideButabarbital may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaButabarbital may increase the hypotensive activities of Methyldopa.
MetipranololButabarbital may increase the hypotensive activities of Metipranolol.
MetolazoneButabarbital may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Butabarbital.
MetyrosineButabarbital may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
MinoxidilButabarbital may increase the hypotensive activities of Minoxidil.
MirtazapineButabarbital may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoexiprilButabarbital may increase the hypotensive activities of Moexipril.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
NadololButabarbital may increase the hypotensive activities of Nadolol.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Butabarbital.
NesiritideButabarbital may increase the hypotensive activities of Nesiritide.
NicardipineThe metabolism of Nicardipine can be increased when combined with Butabarbital.
NifedipineThe metabolism of Nifedipine can be increased when combined with Butabarbital.
NimodipineThe metabolism of Nimodipine can be increased when combined with Butabarbital.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Butabarbital.
NitrendipineThe metabolism of Nitrendipine can be increased when combined with Butabarbital.
NitroglycerinButabarbital may increase the hypotensive activities of Nitroglycerin.
NitroprussideButabarbital may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Butabarbital.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Butabarbital.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Butabarbital.
OlmesartanButabarbital may increase the hypotensive activities of Olmesartan.
OrphenadrineButabarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PapaverineButabarbital may increase the hypotensive activities of Papaverine.
ParaldehydeButabarbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Butabarbital is combined with Paroxetine.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Butabarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
PerhexilineThe metabolism of Perhexiline can be increased when combined with Butabarbital.
PerindoprilButabarbital may increase the hypotensive activities of Perindopril.
PethidineButabarbital 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 Butabarbital.
PramipexoleButabarbital may increase the sedative activities of Pramipexole.
PrazosinButabarbital may increase the hypotensive activities of Prazosin.
PrenylamineThe metabolism of Prenylamine can be increased when combined with Butabarbital.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Butabarbital.
PropacetamolThe metabolism of Propacetamol can be increased when combined with Butabarbital.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Butabarbital.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Butabarbital.
PyridoxineThe metabolism of Butabarbital can be increased when combined with Pyridoxine.
QuetiapineButabarbital may increase the hypotensive activities of Quetiapine.
QuinaprilButabarbital may increase the hypotensive activities of Quinapril.
RamiprilButabarbital may increase the hypotensive activities of Ramipril.
ReserpineButabarbital may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Butabarbital can be increased when combined with Rifabutin.
RifampicinThe metabolism of Butabarbital can be increased when combined with Rifampicin.
RifapentineThe metabolism of Butabarbital can be increased when combined with Rifapentine.
RiociguatButabarbital may increase the hypotensive activities of Riociguat.
RisedronateThe metabolism of Risedronate can be increased when combined with Butabarbital.
RopiniroleButabarbital may increase the sedative activities of Ropinirole.
RotigotineButabarbital may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butabarbital.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
SomatostatinThe risk or severity of adverse effects can be increased when Somatostatin is combined with Butabarbital.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Butabarbital.
SpironolactoneButabarbital may increase the hypotensive activities of Spironolactone.
SuvorexantButabarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
TelmisartanButabarbital may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Butabarbital.
TerazosinButabarbital may increase the hypotensive activities of Terazosin.
ThalidomideButabarbital 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 Butabarbital.
TimololThe serum concentration of Timolol can be decreased when it is combined with Butabarbital.
TizanidineButabarbital may increase the hypotensive activities of Tizanidine.
TorasemideButabarbital may increase the hypotensive activities of Torasemide.
TrandolaprilButabarbital may increase the hypotensive activities of Trandolapril.
TriamtereneButabarbital may increase the hypotensive activities of Triamterene.
TrichlormethiazideButabarbital may increase the orthostatic hypotensive activities of Trichlormethiazide.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Butabarbital.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Butabarbital.
Valproic AcidThe serum concentration of Butabarbital can be increased when it is combined with Valproic Acid.
ValsartanButabarbital may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Butabarbital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Butabarbital.
WarfarinThe metabolism of Warfarin can be increased when combined with Butabarbital.
ZolpidemButabarbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

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. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23