Identification

Name
Estazolam
Accession Number
DB01215  (APRD00955)
Type
Small Molecule
Groups
Approved, Illicit
Description

A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. [PubChem]

Structure
Thumb
Synonyms
  • 8-chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine
  • Estazolamum
External IDs
ABBOTT-47631
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Prosom Tab 1mgTablet1 mgOralAbbott1993-12-311997-08-18Canada
Prosom Tab 2mgTablet2 mgOralAbbott1993-12-311997-08-18Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EstazolamTablet2 mg/1OralRebel Distributors1997-08-19Not applicableUs
EstazolamTablet2 mg/1OralActavis Pharma Company1997-08-19Not applicableUs
EstazolamTablet1 mg/1OralGolden State Medical Supply1997-08-19Not applicableUs
EstazolamTablet2 mg/1OralMayne Pharma2016-08-03Not applicableUs
EstazolamTablet1 mg/1OralTeva1997-07-142018-01-31Us00093 0129 01 nlmimage10 4842a445
EstazolamTablet2 mg/1OralGolden State Medical Supply1997-08-19Not applicableUs
EstazolamTablet1 mg/1OralActavis Pharma Company1997-08-19Not applicableUs
EstazolamTablet2 mg/1OralTeva1997-07-142018-01-31Us00093 0130 01 nlmimage10 5142a895
EstazolamTablet1 mg/1OralMayne Pharma2016-08-03Not applicableUs
International/Other Brands
Esilgan (Takeda) / Eurodin (Takeda) / Nuctalon (Takeda) / ProSom
Categories
UNII
36S3EQV54C
CAS number
29975-16-4
Weight
Average: 294.738
Monoisotopic: 294.067224079
Chemical Formula
C16H11ClN4
InChI Key
CDCHDCWJMGXXRH-UHFFFAOYSA-N
InChI
InChI=1S/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2
IUPAC Name
12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene
SMILES
ClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1

Pharmacology

Indication

For the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.

Structured Indications
Pharmacodynamics

Estazolam, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.

Mechanism of action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit delta
potentiator
Human
AGamma-aminobutyric acid receptor subunit epsilon
potentiator
Human
AGamma-aminobutyric acid receptor subunit pi
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-3
potentiator
Human
AGABA-A receptor (anion channel)
positive allosteric modulator
Human
Absorption

Tablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested.

Volume of distribution
Not Available
Protein binding

93% protein bound, independant of concentration.

Metabolism

Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A).

Route of elimination

Estazolam is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.

Half life

The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.

Clearance
Not Available
Toxicity

Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe risk or severity of adverse effects can be increased when Estazolam is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Aceprometazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Estazolam is combined with Adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Estazolam is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Estazolam is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Estazolam is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Estazolam.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Estazolam is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Estazolam is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Estazolam is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Estazolam.Approved, Illicit, Investigational
Ambroxol acefyllinateThe therapeutic efficacy of Estazolam can be decreased when used in combination with Ambroxol acefyllinate.Experimental
AminophyllineThe therapeutic efficacy of Estazolam can be decreased when used in combination with Aminophylline.Approved
AmiodaroneThe serum concentration of Estazolam can be increased when it is combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Estazolam is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Estazolam is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Estazolam is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Estazolam is combined with Amperozide.Experimental
AprepitantThe serum concentration of Estazolam can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Estazolam is combined with Aripiprazole.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Estazolam is combined with Asenapine.Approved
AtazanavirThe serum concentration of Estazolam can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Estazolam can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Azaperone.Vet Approved
AzelastineEstazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Estazolam is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Estazolam is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Estazolam is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Estazolam is combined with Benzyl alcohol.Approved
BoceprevirThe serum concentration of Estazolam can be increased when it is combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Estazolam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Estazolam can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Estazolam is combined with Brexpiprazole.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Bromazepam.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Estazolam is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Estazolam is combined with Bromperidol.Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Bupivacaine.Approved, Investigational
BuprenorphineEstazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Estazolam.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Estazolam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Estazolam is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Estazolam is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Estazolam is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Estazolam.Approved, Illicit, Vet Approved
CanertinibThe risk or severity of adverse effects can be increased when Estazolam is combined with Canertinib.Investigational
CarbamazepineThe metabolism of Estazolam can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Carbinoxamine.Approved
CarbomycinThe serum concentration of Estazolam can be increased when it is combined with Carbomycin.Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Estazolam is combined with Carfentanil.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Estazolam is combined with Carisoprodol.Approved
CeritinibThe serum concentration of Estazolam can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Estazolam is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Estazolam is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Estazolam.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Estazolam.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Estazolam is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Cinchocaine.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Estazolam is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Estazolam can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Estazolam can be decreased when combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Estazolam is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Estazolam is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Estazolam is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Clonidine.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Estazolam is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Estazolam.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Estazolam is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Estazolam can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Estazolam is combined with Clozapine.Approved
CobicistatThe serum concentration of Estazolam can be increased when it is combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Estazolam.Approved, Illicit
ConivaptanThe serum concentration of Estazolam can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Estazolam can be decreased when combined with Crizotinib.Approved
CyclizineThe risk or severity of adverse effects can be increased when Estazolam is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Estazolam.Approved
CyclosporineThe metabolism of Estazolam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Estazolam is combined with Cyproheptadine.Approved
DabrafenibThe serum concentration of Estazolam can be decreased when it is combined with Dabrafenib.Approved
DantroleneThe risk or severity of adverse effects can be increased when Estazolam is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Estazolam is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dapoxetine.Investigational
DarunavirThe serum concentration of Estazolam can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Estazolam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Estazolam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Estazolam can be decreased when combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Estazolam is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Estazolam.Approved
DesipramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Estazolam is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Estazolam is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dexmedetomidine.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Estazolam is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Estazolam is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dezocine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Estazolam.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Estazolam is combined with Diethyl ether.Experimental
DifenoxinThe risk or severity of adverse effects can be increased when Estazolam is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Estazolam can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Estazolam can be decreased when combined with Diltiazem.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Estazolam is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Estazolam.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Estazolam.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Estazolam is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Estazolam is combined with Doxepin.Approved
DoxycyclineThe metabolism of Estazolam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Estazolam is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Illicit
DronedaroneThe metabolism of Estazolam can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Estazolam is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Estazolam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Estazolam is combined with Dyclonine.Approved
DyphyllineThe therapeutic efficacy of Estazolam can be decreased when used in combination with Dyphylline.Approved
EcgonineThe risk or severity of adverse effects can be increased when Estazolam is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Estazolam is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Estazolam is combined with Efavirenz.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Estazolam is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Estazolam is combined with Enflurane.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Estazolam is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Estazolam can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe serum concentration of Estazolam can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Estazolam is combined with Escitalopram.Approved, Investigational
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Estazolam.Approved
EthanolEstazolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethchlorvynol.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethyl chloride.Experimental
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Estazolam is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Estazolam is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Estazolam is combined with Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Estazolam is combined with Etorphine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Estazolam is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Estazolam is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Estazolam.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Estazolam is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Estazolam is combined with Flibanserin.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Fluanisone.Experimental
FluconazoleThe metabolism of Estazolam can be decreased when combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Estazolam is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Estazolam is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Estazolam.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Estazolam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Estazolam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Estazolam is combined with Fluspirilene.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Estazolam is combined with Fluticasone propionate.Approved
FluvoxamineThe metabolism of Estazolam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Estazolam can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Estazolam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Estazolam.Approved
FospropofolThe risk or severity of adverse effects can be increased when Estazolam is combined with Fospropofol.Approved, Illicit
Fusidic AcidThe serum concentration of Estazolam can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Estazolam.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Estazolam is combined with Gabapentin Enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Estazolam is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Estazolam is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Estazolam is combined with Glutethimide.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Estazolam is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Estazolam.Approved
HalothaneThe risk or severity of adverse effects can be increased when Estazolam is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Estazolam is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Estazolam is combined with Hexobarbital.Approved
HyaluronidaseThe therapeutic efficacy of Estazolam can be decreased when used in combination with Hyaluronidase.Approved, Investigational
HydrocodoneEstazolam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Estazolam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Iloperidone.Approved
ImatinibThe metabolism of Estazolam can be decreased when combined with Imatinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Estazolam is combined with Indalpine.Investigational, Withdrawn
IndinavirThe serum concentration of Estazolam can be increased when it is combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Estazolam is combined with Indiplon.Investigational
IsavuconazoniumThe metabolism of Estazolam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Estazolam.Approved, Vet Approved
IsradipineThe metabolism of Estazolam can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Estazolam can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Estazolam can be increased when it is combined with Ivacaftor.Approved
JosamycinThe serum concentration of Estazolam can be increased when it is combined with Josamycin.Approved
KetamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Ketobemidone.Approved
KetoconazoleThe serum concentration of Estazolam can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Estazolam can be increased when it is combined with Kitasamycin.Experimental
LamotrigineThe risk or severity of adverse effects can be increased when Estazolam is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Estazolam is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Estazolam is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Estazolam is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Estazolam is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Estazolam is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Estazolam is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Estazolam.Approved
LidocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Lidocaine.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Estazolam is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Estazolam is combined with Lofentanil.Illicit
LopinavirThe serum concentration of Estazolam can be increased when it is combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Estazolam is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Estazolam.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Lormetazepam.Approved
LovastatinThe metabolism of Estazolam can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Estazolam.Approved
LuliconazoleThe serum concentration of Estazolam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Estazolam can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Estazolam is combined with Maprotiline.Approved
MebicarThe risk or severity of adverse effects can be increased when Estazolam is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Estazolam is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Medetomidine.Vet Approved
MefloquineThe therapeutic efficacy of Estazolam can be decreased when used in combination with Mefloquine.Approved
MelatoninThe risk or severity of adverse effects can be increased when Estazolam is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Estazolam.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Estazolam is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Mesoridazine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Estazolam is combined with Metaxalone.Approved
MethadoneEstazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Estazolam is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Estazolam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Estazolam is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Estazolam.Approved
MethotrimeprazineEstazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Estazolam is combined with Methoxyflurane.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Estazolam is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Estazolam is combined with Methylecgonine.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Estazolam is combined with Methylphenobarbital.Approved
MetyrosineEstazolam may increase the sedative activities of Metyrosine.Approved
MianserinThe therapeutic efficacy of Estazolam can be decreased when used in combination with Mianserin.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Estazolam.Approved, Illicit
MifepristoneThe serum concentration of Estazolam can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Estazolam is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Investigational
MirtazapineEstazolam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Estazolam can be decreased when it is combined with Mitotane.Approved
MolindoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Estazolam.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Estazolam.Approved
NefazodoneThe serum concentration of Estazolam can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Estazolam can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Estazolam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Estazolam can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Estazolam can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Estazolam is combined with Nitrous oxide.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Estazolam is combined with Norflurane.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Estazolam is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Estazolam.Approved, Investigational
OlaparibThe metabolism of Estazolam can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Estazolam can be increased when it is combined with Oleandomycin.Vet Approved
OlopatadineThe risk or severity of adverse effects can be increased when Estazolam is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Estazolam is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Estazolam is combined with Opium.Approved, Illicit
OrlistatThe serum concentration of Estazolam can be decreased when it is combined with Orlistat.Approved, Investigational
OrphenadrineEstazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Estazolam is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Estazolam can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Estazolam.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Oxethazaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Estazolam is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Oxybuprocaine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Estazolam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Estazolam.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Estazolam can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Paliperidone.Approved
ParaldehydeEstazolam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Estazolam is combined with Paroxetine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Estazolam is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Estazolam.Approved, Vet Approved
PentobarbitalThe metabolism of Estazolam can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved
PerazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Estazolam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Estazolam.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Estazolam.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Estazolam is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Estazolam is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Estazolam can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Estazolam is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Estazolam.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Estazolam.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Estazolam is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Estazolam is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Estazolam is combined with Pomalidomide.Approved
PosaconazoleThe serum concentration of Estazolam can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleEstazolam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Estazolam.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Prilocaine.Approved
PrimidoneThe metabolism of Estazolam can be increased when combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Procaine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Estazolam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Estazolam.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Promethazine.Approved
PropanididThe risk or severity of adverse effects can be increased when Estazolam is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Proparacaine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Estazolam.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Estazolam is combined with Protriptyline.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Estazolam is combined with Proxibarbal.Experimental
PSD502The risk or severity of adverse effects can be increased when Estazolam is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Estazolam is combined with Quetiapine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Estazolam is combined with Ramelteon.Approved, Investigational
RanolazineThe metabolism of Estazolam can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Estazolam.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Estazolam.Approved
RifabutinThe metabolism of Estazolam can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Estazolam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Estazolam can be increased when combined with Rifapentine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Estazolam.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Estazolam is combined with Ritanserin.Investigational
RitonavirThe serum concentration of Estazolam can be increased when it is combined with Ritonavir.Approved, Investigational
RomifidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Romifidine.Vet Approved
RopiniroleEstazolam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Ropivacaine.Approved
RotigotineEstazolam may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Estazolam.Approved
SaquinavirThe serum concentration of Estazolam can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Estazolam.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Estazolam is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Estazolam is combined with Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Estazolam is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Estazolam is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Estazolam can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Estazolam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Estazolam can be increased when it is combined with Simeprevir.Approved
SolithromycinThe serum concentration of Estazolam can be increased when it is combined with Solithromycin.Investigational
St. John's WortThe serum concentration of Estazolam can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Estazolam can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Estazolam.Approved, Investigational
SulfisoxazoleThe metabolism of Estazolam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Estazolam is combined with Sulpiride.Approved
SultoprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Sultopride.Experimental
SuvorexantEstazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Estazolam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Estazolam is combined with Tasimelteon.Approved
TeduglutideThe serum concentration of Estazolam can be increased when it is combined with Teduglutide.Approved
TelaprevirThe serum concentration of Estazolam can be increased when it is combined with Telaprevir.Withdrawn
TelithromycinThe serum concentration of Estazolam can be increased when it is combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Estazolam.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Estazolam is combined with Tetrodotoxin.Investigational
ThalidomideEstazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe therapeutic efficacy of Estazolam can be decreased when used in combination with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Estazolam is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Estazolam is combined with Thiopental.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Estazolam.Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Estazolam is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Tiapride.Approved, Investigational
TiclopidineThe metabolism of Estazolam can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tilidine.Experimental
TizanidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tizanidine.Approved
TocilizumabThe serum concentration of Estazolam can be decreased when it is combined with Tocilizumab.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Estazolam is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Estazolam is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Estazolam.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Estazolam is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Estazolam is combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Estazolam is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Estazolam.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Estazolam is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Estazolam is combined with Trichloroethylene.Experimental
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Estazolam.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Estazolam is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Estazolam is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Triprolidine.Approved
TylosinThe serum concentration of Estazolam can be increased when it is combined with Tylosin.Vet Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Estazolam is combined with Valproic Acid.Approved, Investigational
VenlafaxineThe metabolism of Estazolam can be decreased when combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Estazolam is combined with Veralipride.Experimental
VerapamilThe metabolism of Estazolam can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Estazolam is combined with Vigabatrin.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Estazolam is combined with Vinyl ether.Experimental
VoriconazoleThe serum concentration of Estazolam can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Estazolam is combined with Vortioxetine.Approved
XenonThe risk or severity of adverse effects can be increased when Estazolam is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Estazolam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Estazolam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Estazolam.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Estazolam is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Estazolam is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Estazolam can be decreased when combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Estazolam is combined with Zolazepam.Vet Approved
ZolpidemEstazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Estazolam is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Estazolam.Approved
ZotepineThe risk or severity of adverse effects can be increased when Estazolam is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Estazolam is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

References

Synthesis Reference

Hester, J.B. Jr.; U.S. Patent 3,701,782; October 31, 1972; assigned to The Upjohn Co.

General References
  1. Watanabe S, Ohta H, Sakurai Y, Takao K, Ueki S: [Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants]. Nihon Yakurigaku Zasshi. 1986 Jul;88(1):19-32. [PubMed:3758874]
  2. Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. [PubMed:3089825]
  3. Usami N, Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A: Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5. [PubMed:11995921]
External Links
Human Metabolome Database
HMDB15346
KEGG Drug
D00311
KEGG Compound
C06981
PubChem Compound
3261
PubChem Substance
46507430
ChemSpider
3146
BindingDB
50240450
ChEBI
4858
ChEMBL
CHEMBL285674
Therapeutic Targets Database
DAP000930
PharmGKB
PA449502
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Estazolam
ATC Codes
N05CD04 — Estazolam

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentSleep Initiation and Maintenance Disorders1
4CompletedTreatmentPrimary Insomnia / Sleep Initiation and Maintenance Disorders1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral1 mg
TabletOral2 mg
Prices
Unit descriptionCostUnit
Prosom 2 mg tablet1.71USD tablet
Prosom 1 mg tablet1.53USD tablet
Estazolam 2 mg tablet0.96USD tablet
Estazolam 1 mg tablet0.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)228-229Hester, J.B. Jr.; U.S. Patent 3,701,782; October 31, 1972; assigned to The Upjohn Co.
water solubilityPractically insoluble (1.5 mg/L)Not Available
logP4.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0423 mg/mLALOGPS
logP1.72ALOGPS
logP2.09ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)18.4ChemAxon
pKa (Strongest Basic)4.97ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area43.07 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity94.44 m3·mol-1ChemAxon
Polarizability29.83 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9796
Caco-2 permeable+0.8427
P-glycoprotein substrateNon-substrate0.5939
P-glycoprotein inhibitor INon-inhibitor0.7883
P-glycoprotein inhibitor IIInhibitor0.7786
Renal organic cation transporterInhibitor0.7784
CYP450 2C9 substrateNon-substrate0.8367
CYP450 2D6 substrateNon-substrate0.9081
CYP450 3A4 substrateSubstrate0.674
CYP450 1A2 substrateInhibitor0.8989
CYP450 2C9 inhibitorInhibitor0.822
CYP450 2D6 inhibitorNon-inhibitor0.8586
CYP450 2C19 inhibitorInhibitor0.6571
CYP450 3A4 inhibitorNon-inhibitor0.6818
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8676
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7126
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.0584 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9752
hERG inhibition (predictor II)Non-inhibitor0.8944
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4u-4590000000-dbd088d66293b3b539c3
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as 1,2,4-triazolo[4,3-a][1,4]benzodiazepines. These are aromatic compounds containing a 1,4-benzodiazepine fused to and sharing a nitrogen atom with a 1,2,4-triazole ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,2,4-triazolo[4,3-a][1,4]benzodiazepines
Alternative Parents
Benzene and substituted derivatives / Aryl chlorides / Triazoles / Heteroaromatic compounds / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives
Substituents
1,2,4-triazolo[4,3-a][1,4]benzodiazepine / Aryl chloride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Azole / 1,2,4-triazole / Heteroaromatic compound / Ketimine / Propargyl-type 1,3-dipolar organic compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
triazoles, triazolobenzodiazepine (CHEBI:4858)

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...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
GABRG1
Uniprot ID
Q8N1C3
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight
53594.49 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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...
Gene Name
GABRG2
Uniprot ID
P18507
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight
54161.78 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
GABRG3
Uniprot ID
Q99928
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight
54288.16 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
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...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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...
Gene Name
GABRB2
Uniprot ID
P47870
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-2
Molecular Weight
59149.895 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-gated chloride 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...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor 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
GABRD
Uniprot ID
O14764
Uniprot Name
Gamma-aminobutyric acid receptor subunit delta
Molecular Weight
50707.835 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
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
GABRE
Uniprot ID
P78334
Uniprot Name
Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight
57971.175 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor 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. In the ute...
Gene Name
GABRP
Uniprot ID
O00591
Uniprot Name
Gamma-aminobutyric acid receptor subunit pi
Molecular Weight
50639.735 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor 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. Rho-1 GABA...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor 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. Rho-2 GABA...
Gene Name
GABRR2
Uniprot ID
P28476
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight
54150.41 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor 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
GABRR3
Uniprot ID
A8MPY1
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight
54271.1 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [PubMed:639854]
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. [PubMed:2889803]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:55