Identification

Name
Zopiclone
Accession Number
DB01198  (APRD00356)
Type
Small Molecule
Groups
Approved
Description

Zopiclone is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate like properties.

Structure
Thumb
Synonyms
  • (+-)-zopiclone
  • (±)-zopiclone
  • 6-(5-Chloro-2-pyridinyl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-yl 4-methyl-1-piperazinecarboxylate
  • Zopiclona
  • Zopiclone
  • Zopiclonum
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act ZopicloneTablet5 mgOralActavis Pharma Company2005-11-11Not applicableCanada
Act ZopicloneTablet7.5 mgOralActavis Pharma Company2005-11-11Not applicableCanada
Ava-zopicloneTablet5 mgOralAvanstra Inc2011-08-112014-08-21Canada
Ava-zopicloneTablet7.5 mgOralAvanstra Inc2011-09-092014-08-21Canada
Dom-zopicloneTablet5 mgOralDominion Pharmacal2009-05-25Not applicableCanada
Dom-zopicloneTablet7.5 mgOralDominion Pharmacal1999-11-23Not applicableCanada
Imovane - Tab 5mgTablet5.0 mgOralSanofi Aventis1998-02-10Not applicableCanada
Imovane 7.5 - Tab 7.5mgTablet7.5 mgOralSanofi Aventis1990-12-31Not applicableCanada
Ipg-zopicloneTablet3.75 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-zopicloneTablet7.5 mgOralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-zopicloneTablet5 mgOralApotex Corporation2002-06-04Not applicableCanada
Apo-zopiclone - Tab 7.5mgTablet7.5 mgOralApotex Corporation1996-09-19Not applicableCanada
International/Other Brands
Amoban / Imovane / Zimovane
Categories
UNII
03A5ORL08Q
CAS number
43200-80-2
Weight
Average: 388.808
Monoisotopic: 388.105066147
Chemical Formula
C17H17ClN6O3
InChI Key
GBBSUAFBMRNDJC-UHFFFAOYSA-N
InChI
InChI=1S/C17H17ClN6O3/c1-22-6-8-23(9-7-22)17(26)27-16-14-13(19-4-5-20-14)15(25)24(16)12-3-2-11(18)10-21-12/h2-5,10,16H,6-9H2,1H3
IUPAC Name
6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate
SMILES
CN1CCN(CC1)C(=O)OC1N(C(=O)C2=NC=CN=C12)C1=NC=C(Cl)C=C1

Pharmacology

Indication

For the short-term treatment of insomnia.

Structured Indications
Pharmacodynamics

Zopiclone is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.

Mechanism of action

Zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex. Both zopiclone and benzodiazepines act indiscriminately at the benzodiazepine binding site on α1, α2, α3 and α5 GABAA containing receptors as full agonists causing an enhancement of the inhibitory actions of GABA to produce the therapeutic (hypnotic and anxiolytic) and adverse effects of zopiclone.

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
UTranslocator protein
agonist
Human
Absorption

Rapidly absorbed following oral administration.

Volume of distribution
Not Available
Protein binding

Approximately 45%

Metabolism

Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance.

Route of elimination
Not Available
Half life

Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.

Clearance
Not Available
Toxicity

Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing.

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

References

Synthesis Reference

Thomas Jerussi, "Compositions comprising zopiclone derivatives and methods of making and using the same." U.S. Patent US20040147521, issued July 29, 2004.

US20040147521
General References
  1. Liu HJ, Sato K, Shih HC, Shibuya T, Kawamoto H, Kitagawa H: Pharmacologic studies of the central action of zopiclone: effects on locomotor activity and brain monoamines in rats. Int J Clin Pharmacol Ther Toxicol. 1985 Mar;23(3):121-8. [PubMed:2581904]
  2. Sato K, Hong YL, Yang MS, Shibuya T, Kawamoto H, Kitagawa H: Pharmacologic studies of central actions of zopiclone: influence on brain monoamines in rats under stressful condition. Int J Clin Pharmacol Ther Toxicol. 1985 Apr;23(4):204-10. [PubMed:2860074]
  3. Dundar Y, Dodd S, Strobl J, Boland A, Dickson R, Walley T: Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol. 2004 Jul;19(5):305-22. [PubMed:15252823]
  4. Blanchard JC, Julou L: Suriclone: a new cyclopyrrolone derivative recognizing receptors labeled by benzodiazepines in rat hippocampus and cerebellum. J Neurochem. 1983 Mar;40(3):601-7. [PubMed:6298365]
  5. Julou L, Bardone MC, Blanchard JC, Garret C, Stutzmann JM: Pharmacological studies on zopiclone. Pharmacology. 1983;27 Suppl 2:46-58. [PubMed:6142468]
External Links
Human Metabolome Database
HMDB15329
KEGG Drug
D01372
PubChem Compound
5735
PubChem Substance
46505233
ChemSpider
5533
BindingDB
50054136
ChEBI
32315
ChEMBL
CHEMBL135400
Therapeutic Targets Database
DAP000427
PharmGKB
PA10236
Drugs.com
Drugs.com Drug Page
Wikipedia
Zopiclone
ATC Codes
N05CF01 — Zopiclone
AHFS Codes
  • 28:24.92 — Miscellaneous Anxiolytics Sedatives and Hypnotics

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentParkinson's Disease (PD) / Sleeplessness1
1CompletedBasic ScienceHealthy Participants1
1CompletedPreventionSleeplessness1
1CompletedTreatmentPsychiatric Disorder NOS / Sleep Initiation and Maintenance Disorders1
1CompletedTreatmentSleeplessness2
2CompletedTreatmentInsomnia Chronic1
3CompletedTreatmentBalance1
3CompletedTreatmentHealthy Volunteers / Sleep Initiation and Maintenance Disorders1
3CompletedTreatmentObstructive Sleep Apnea (OSA)1
3CompletedTreatmentSleep1
3CompletedTreatmentSleeplessness1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4CompletedTreatmentFeeling Anxious1
4CompletedTreatmentSleeplessness1
4RecruitingSupportive CareSleep Apnea, Central / Ventricular Dysfunction1
4RecruitingTreatmentSleep / Sleeplessness1
Not AvailableCompletedDiagnosticCardiac Dysrhythmia / Chronic Obstructive / Hypercapnia / Hypoxemia / Pulmonary Diseases1
Not AvailableWithdrawnNot AvailableAutomobile Driving1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral5 mg
TabletOral5.0 mg
TabletOral7.5 mg
TabletOral3.75 mg
Prices
Unit descriptionCostUnit
Imovane 7.5 mg Tablet1.41USD tablet
Imovane 5 mg Tablet1.11USD tablet
Apo-Zopiclone 7.5 mg Tablet0.49USD tablet
Co Zopiclone 7.5 mg Tablet0.49USD tablet
Mylan-Zopiclone 7.5 mg Tablet0.49USD tablet
Novo-Zopiclone 7.5 mg Tablet0.49USD tablet
Nu-Zopiclone 7.5 mg Tablet0.49USD tablet
Pms-Zopiclone 7.5 mg Tablet0.49USD tablet
Ran-Zopiclone 7.5 mg Tablet0.49USD tablet
Ratio-Zopiclone 7.5 mg Tablet0.49USD tablet
Rhovane 7.5 mg Tablet0.49USD tablet
Sandoz Zopiclone 7.5 mg Tablet0.49USD tablet
Zopiclone 7.5 mg Tablet0.49USD tablet
Apo-Zopiclone 5 mg Tablet0.23USD tablet
Co Zopiclone 5 mg Tablet0.23USD tablet
Mylan-Zopiclone 5 mg Tablet0.23USD tablet
Novo-Zopiclone 5 mg Tablet0.23USD tablet
Pms-Zopiclone 5 mg Tablet0.23USD tablet
Ran-Zopiclone 5 mg Tablet0.23USD tablet
Ratio-Zopiclone 5 mg Tablet0.23USD tablet
Sandoz Zopiclone 5 mg Tablet0.23USD tablet
Zopiclone 5 mg Tablet0.23USD 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)178 °CPhysProp
water solubility0.151 mg/mL at 25 °CMEYLAN,WM et al. (1996)
logP0.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.885 mg/mLALOGPS
logP0.97ALOGPS
logP0.81ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)13.04ChemAxon
pKa (Strongest Basic)6.89ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area91.76 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity95.89 m3·mol-1ChemAxon
Polarizability37.67 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+0.9382
Caco-2 permeable+0.5805
P-glycoprotein substrateSubstrate0.6917
P-glycoprotein inhibitor IInhibitor0.6381
P-glycoprotein inhibitor IIInhibitor0.5
Renal organic cation transporterNon-inhibitor0.6785
CYP450 2C9 substrateNon-substrate0.7158
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.6775
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorInhibitor0.8995
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.689
Ames testAMES toxic0.5332
CarcinogenicityNon-carcinogens0.9174
BiodegradationNot ready biodegradable0.9941
Rat acute toxicity2.6411 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7838
hERG inhibition (predictor II)Non-inhibitor0.5688
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)MSsplash10-0007-6950000000-c1583a92e3cbc5066186
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
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00kb-0090000000-9d80e08080f406848221
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0092000000-977d45f9a516242be80f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0002-0090000000-397a508c11f66c161327
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014j-0090000000-abc6a676659114a83d08
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0790000000-74d7c73e854e61700433
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00lr-0920000000-2c17f6282d1031cb4d50
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0900000000-c0f92aba9374337ff737
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-003r-5900000000-46755df8b5cfb7f46bf9
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-9300000000-091d5434bc674d5bf9a4
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-9000000000-87365fa01fb0854897ca
13C NMR Spectrum1D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as cyclopyrrolones. These are compounds belonging to a family of pyridin-2-ylpyrrole based chemicals. The pyrrole is usually fused to a benzene, pyrimidine, or dithiin.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrrolopyrazines
Sub Class
Cyclopyrrolones
Direct Parent
Cyclopyrrolones
Alternative Parents
Piperazine carboxylic acids / 2-heteroaryl carboxamides / N-methylpiperazines / Pyridines and derivatives / Pyrazines / Aryl chlorides / Imidolactams / Tertiary carboxylic acid amides / Carbamate esters / Heteroaromatic compounds
show 9 more
Substituents
Cyclopyrrolone / Piperazine-1-carboxylic acid / 2-heteroaryl carboxamide / N-methylpiperazine / N-alkylpiperazine / Aryl chloride / Aryl halide / Imidolactam / Pyridine / Pyrazine
show 25 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
pyrrolopyrazine, monochloropyridine (CHEBI:32315)

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. Nutt DJ, Stahl SM: Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics. J Psychopharmacol. 2010 Nov;24(11):1601-12. doi: 10.1177/0269881109106927. Epub 2009 Nov 26. [PubMed:19942638]
  2. Hanson SM, Morlock EV, Satyshur KA, Czajkowski C: Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different. J Med Chem. 2008 Nov 27;51(22):7243-52. doi: 10.1021/jm800889m. [PubMed:18973287]
  3. Sanger DJ: The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents. CNS Drugs. 2004;18 Suppl 1:9-15; discussion 41, 43-5. [PubMed:15291009]
  4. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [PubMed:6135616]
  5. Ramerstorfer J, Furtmuller R, Vogel E, Huck S, Sieghart W: The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes. Eur J Pharmacol. 2010 Jun 25;636(1-3):18-27. doi: 10.1016/j.ejphar.2010.03.015. Epub 2010 Mar 19. [PubMed:20303942]
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. Nutt DJ, Stahl SM: Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics. J Psychopharmacol. 2010 Nov;24(11):1601-12. doi: 10.1177/0269881109106927. Epub 2009 Nov 26. [PubMed:19942638]
  2. Hanson SM, Morlock EV, Satyshur KA, Czajkowski C: Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different. J Med Chem. 2008 Nov 27;51(22):7243-52. doi: 10.1021/jm800889m. [PubMed:18973287]
  3. Ramerstorfer J, Furtmuller R, Vogel E, Huck S, Sieghart W: The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes. Eur J Pharmacol. 2010 Jun 25;636(1-3):18-27. doi: 10.1016/j.ejphar.2010.03.015. Epub 2010 Mar 19. [PubMed:20303942]
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. Nutt DJ, Stahl SM: Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics. J Psychopharmacol. 2010 Nov;24(11):1601-12. doi: 10.1177/0269881109106927. Epub 2009 Nov 26. [PubMed:19942638]
  2. Hanson SM, Morlock EV, Satyshur KA, Czajkowski C: Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different. J Med Chem. 2008 Nov 27;51(22):7243-52. doi: 10.1021/jm800889m. [PubMed:18973287]
  3. Ramerstorfer J, Furtmuller R, Vogel E, Huck S, Sieghart W: The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes. Eur J Pharmacol. 2010 Jun 25;636(1-3):18-27. doi: 10.1016/j.ejphar.2010.03.015. Epub 2010 Mar 19. [PubMed:20303942]
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. Nutt DJ, Stahl SM: Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics. J Psychopharmacol. 2010 Nov;24(11):1601-12. doi: 10.1177/0269881109106927. Epub 2009 Nov 26. [PubMed:19942638]
  2. Hanson SM, Morlock EV, Satyshur KA, Czajkowski C: Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different. J Med Chem. 2008 Nov 27;51(22):7243-52. doi: 10.1021/jm800889m. [PubMed:18973287]
  3. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [PubMed:6135616]
  4. Ramerstorfer J, Furtmuller R, Vogel E, Huck S, Sieghart W: The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes. Eur J Pharmacol. 2010 Jun 25;636(1-3):18-27. doi: 10.1016/j.ejphar.2010.03.015. Epub 2010 Mar 19. [PubMed:20303942]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Cholesterol binding
Specific Function
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in l...
Gene Name
TSPO
Uniprot ID
P30536
Uniprot Name
Translocator protein
Molecular Weight
18827.81 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. 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]
  3. Lalovic B, Phillips B, Risler LL, Howald W, Shen DD: Quantitative contribution of CYP2D6 and CYP3A to oxycodone metabolism in human liver and intestinal microsomes. Drug Metab Dispos. 2004 Apr;32(4):447-54. [PubMed:15039299]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. 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]
  3. Lalovic B, Phillips B, Risler LL, Howald W, Shen DD: Quantitative contribution of CYP2D6 and CYP3A to oxycodone metabolism in human liver and intestinal microsomes. Drug Metab Dispos. 2004 Apr;32(4):447-54. [PubMed:15039299]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 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 November 19, 2017 20:34