Zolpidem
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1992
- First approval year
- 1992
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Zolpidem
- Molecular weight
- 307.4
- Structure (SMILES)
- Cc1ccc(-c2nc3ccc(C)cn3c2CC(=O)N(C)C)cc1
- n n 6 trimethyl 2 p tolyl imidazo 1 2 a pyridine 3 acetamide
- N,N,6-TRIMETHYL-2-P-TOLYL-IMIDAZO(1,2-A)PYRIDINE-3-ACETAMIDE
- sanval
- Sanval
- zolpidem
- Zolpidem
- zolpidem [INN]
- ZOLPIDEM [MI]
- ZOLPIDEM [VANDF]
- Zolpidem [WHO-DD]
- zolpidem civ
- Zolpidem civ
- ZOLPIDEM CIV [USP-RS]
- zolpidem civ usp rs
- zolpidem inn
- zolpidem mi
- zolpidem vandf
- zolpidem who dd
- ATC classification codes
- N05CF02
Sources for recorded values
- CAS registry numbers
- 82626-48-0
- ChEMBL ID
- CHEMBL911
- InChIKey
- ZAFYATHCZYHLPB-UHFFFAOYSA-N
- PubChem compound IDs
- 5732
- RxNorm IDs (RxCUI)
- 39993
- FDA ingredient codes (UNII)
- 7K383OQI23
- Applicant
- COSETTE
- Approval date
- 16 Dec 1992
- Application number
- NDA019908
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- Pharmacology name
- zolpidem
- Type
- Synthetic organic
- Drug name stem
- -pidem
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- topical
- Action
- Positive
- Action type
- POSITIVE
- Target
- GABAA receptor α1 subunit
- Gene symbol
- GABRA1
- Protein identifier
- P14867
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Positive
- Action type
- POSITIVE
- Target
- GABAA receptor α3 subunit
- Gene symbol
- GABRA3
- Protein identifier
- P34903
- Median affinity
- 5.67
- Affinity units
- pKi
- Action
- Positive
- Action type
- POSITIVE
- Target
- GABAA receptor α2 subunit
- Gene symbol
- GABRA2
- Protein identifier
- P47869
- Median affinity
- 6.12
- Affinity units
- pKi
Open Targets mechanisms
- Mechanism
- GABA A receptor alpha-1/beta-1/gamma-2 positive allosteric modulator
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Target
- GABA A receptor alpha-1/beta-1/gamma-2
- Action type
- ALLOSTERIC MODULATOR
- Gene symbol
- GABRA1
- Protein identifier
- P14867
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Gene symbol
- GABRA1|GABRG2|GABRB3
- Protein identifier
- P14867|P18507|P28472
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Gene symbol
- GABRA1|GABRG2|GABRB2
- Protein identifier
- P14867|P18507|P47870
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Gene symbol
- GABRG2|GABRB3|GABRA3
- Protein identifier
- P18507|P28472|P34903
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Gene symbol
- GABRG2|GABRB3|GABRA2
- Protein identifier
- P18507|P28472|P47869
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- POSITIVE ALLOSTERIC MODULATOR
- Gene symbol
- GABRG2|GABRA3|GABRB2
- Protein identifier
- P18507|P34903|P47870
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Obesity
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001073
- Subject identifier
- D009765
- Condition
- Autistic Disorder
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003758
- Subject identifier
- D001321
- Condition
- Attention Deficit Disorder with Hyperactivity
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003888
- Subject identifier
- D001289
- Condition
- Substance-Related Disorders
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003890
- Subject identifier
- D019966
- Condition
- Sleep Initiation and Maintenance Disorders
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004698
- Subject identifier
- D007319
- Condition
- Anxiety
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005230
- Subject identifier
- D001007
- Condition
- Marijuana Abuse
- Highest recorded phase
- 1
- Condition identifier
- EFO:0007191
- Subject identifier
- D002189
- Condition
- Sleep Wake Disorders
- Highest recorded phase
- 3
- Condition identifier
- EFO:0008568
- Subject identifier
- D012893
- Condition
- Dementia
- Highest recorded phase
- 3
- Condition identifier
- HP:0000726
- Subject identifier
- D003704
- Condition
- Low Back Pain
- Highest recorded phase
- 1
- Condition identifier
- HP:0003419
- Subject identifier
- D017116
- Condition
- Dystonic Disorders
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0000477
- Subject identifier
- D020821
- Condition
- Depressive Disorder
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002050
- Subject identifier
- D003866
- Condition
- Schizophrenia
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0005090
- Subject identifier
- D012559
- Condition
- Parkinson Disease
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005180
- Subject identifier
- D010300
- Condition identifier
- EFO_0000246
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003888
- Highest recorded phase
- 3
- Condition identifier
- EFO_0003890
- Condition identifier
- EFO_0004698
- Condition identifier
- EFO_0007191
- Highest recorded phase
- 1
- Condition identifier
- EFO_0008568
- Highest recorded phase
- 3
- Condition identifier
- EFO_0022597
- Condition identifier
- GO_0030431
- Condition identifier
- HP_0001394
- Condition identifier
- HP_0002360
- Highest recorded phase
- 2
- Condition identifier
- HP_0002527
- Condition identifier
- HP_0003419
- Condition identifier
- HP_0003419
- Highest recorded phase
- 1
- Condition identifier
- HP_0030834
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000477
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001942
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002009
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002050
- Condition identifier
- MONDO_0004648
- Condition identifier
- MONDO_0004975
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004985
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005180
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005258
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005383
- Highest recorded phase
- 3
And 2 more, listed on the interactive page.
- Warning
- Black Box Warning
- Country
- United States
- Warning
- Black Box Warning
- Effect
- misuse
- Country
- United States
- Warning
- Black Box Warning
- Effect
- vascular toxicity
- Country
- United States
- Event
- abnormal behaviour
- Reports
- 166
- Reporting signal score
- 221.643
- Event
- abnormal sleep-related event
- Reports
- 53
- Reporting signal score
- 195.835
- Event
- aggression
- Reports
- 173
- Reporting signal score
- 201.678
- Event
- agitation
- Reports
- 233
- Reporting signal score
- 231.897
- Event
- altered state of consciousness
- Reports
- 151
- Reporting signal score
- 237.594
- Event
- amnesia
- Reports
- 339
- Reporting signal score
- 605.556
- Event
- anterograde amnesia
- Reports
- 33
- Reporting signal score
- 110.089
- Event
- anxiety
- Reports
- 239
- Reporting signal score
- 99.8729
- Event
- arthralgia
- Reports
- 17
- Reporting signal score
- 96.6896
- Event
- automatism
- Reports
- 30
- Reporting signal score
- 122.057
- Event
- bradyphrenia
- Reports
- 75
- Reporting signal score
- 153.997
- Event
- bradypnoea
- Reports
- 65
- Reporting signal score
- 175.914
- Event
- coma
- Reports
- 518
- Reporting signal score
- 1,117.52
- Event
- coma scale abnormal
- Reports
- 56
- Reporting signal score
- 122.823
- Event
- confusional state
- Reports
- 547
- Reporting signal score
- 657.251
- Event
- decorticate posture
- Reports
- 21
- Reporting signal score
- 92.7845
- Event
- delirium
- Reports
- 260
- Reporting signal score
- 420.024
- Event
- depressed level of consciousness
- Reports
- 186
- Reporting signal score
- 225.02
- Event
- diarrhoea
- Reports
- 72
- Reporting signal score
- 98.6941
- Event
- disorientation
- Reports
- 173
- Reporting signal score
- 222.536
- Event
- drug abuse
- Reports
- 907
- Reporting signal score
- 2,243.75
- Event
- drug dependence
- Reports
- 538
- Reporting signal score
- 1,449.44
- Event
- drug interaction
- Reports
- 291
- Reporting signal score
- 119.192
- Event
- drug tolerance
- Reports
- 48
- Reporting signal score
- 118.54
- Event
- drug use disorder
- Reports
- 87
- Reporting signal score
- 222.482
And 34 more, listed on the interactive page.
- NCT00283946
- NCT00374777
- NCT00425243
- NCT00440323
- NCT00630175
- NCT00999219
- NCT00318448
- NCT00494468
- NCT00608985
- NCT00784875
- NCT00940550
- NCT01463098
- NCT01779830
- NCT01804036
- NCT02139098
- NCT02839200
- NCT03056053
- NCT03158025
- NCT03160404
- NCT03375203
- NCT03885141
- NCT05615727
- NCT05764798
- NCT00893269
- NCT00976105
And 10 more, listed on the interactive page.
- Dose
- 5-10mg
- Route
- Oral
- How often
- Once daily
- Avoid use in severe hepatic impairment
- Do not readminister during the same night
- Effect slowed if taken with or immediately after a meal
- May need dose adjustment when combined with other CNS depressants
- Take only once per night
- Hydrogen bond acceptors
- 3
- Hydrogen bond donors
- 0
- Polar surface area
- 37.61
- Calculated partition coefficient (ALogP)
- 3.25
- Calculated partition coefficient (XLogP)
- 2.5
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 23
- Molecular formula
- C19H21N3O
- Monoisotopic mass
- 307.168462302
- Natural product
- Yes
- Recorded assays
- 1,940
- Active assays
- 377
- Confirmatory
- Other
- Screening
- Summary
- Sleep Aids, Pharmaceutical
- GABA-A Receptor Agonists
Distribution coefficient (LogD)
- Median
- 2.325
- Mean
- 2.325
- Minimum
- 2.3
- Maximum
- 2.35
- Unit
- unitless
- Assays
- 2
- Standard deviation
- 0.0353553
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Cardiac potassium channel inhibition
- Median
- 37,153.5
- Mean
- 37,153.5
- Minimum
- 37,153.5
- Maximum
- 37,153.5
- Unit
- nM
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- IC50
Solubility
- Median
- 260,000
- Mean
- 260,000
- Minimum
- 260,000
- Maximum
- 260,000
- Unit
- nM
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Oral bioavailability
- Median
- 72
- Mean
- 72
- Minimum
- 72
- Maximum
- 72
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (108)
- A 2-Part Single Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E2006
- A Comparison of Midazolam and Zolpidem as Oral Premedication in Children
- A Comparison of the Physiological and Behavioral Effects of Suvorexant and Zolpidem in Healthy Volunteers: A Randomized, Double-blind, Placebo Controlled Study
- A Double-blind, Group-comparison P-III Study With Zolpidem MR Using Placebo and Nitrazepam in Insomnia Patients
- A Double-blind, Group-comparison Study Using Zolpidem (Myslee) as a Comparative Drug in Patients With Insomnia
- A SMART Approach to Evaluating the Benefits of Common Prescription and OTC Medications for Insomnia
- A Study of FK199B to Compare Efficacy With Zolpidem by Polysomnography in Patients With Insomnia
- A Study of LY2624803 in Participants With Transient Insomnia
- A Study to Compare Efficacy and Safety of Zolpidem Modified Release Formulation Versus Zolpidem in Insomnia Patients
- A Study to Determine the Abuse Potential of Seltorexant Compared to Suvorexant and Zolpidem
- A Study to Determine the Abuse Potential of Single Oral Doses of Lemborexant Compared to Zolpidem, Suvorexant and Placebo in Healthy, Non-Dependent, Recreational Sedative Users
- A Study to Evaluate Efficacy and Safety of Zolpidem Modified Release Formulation in Insomnia Patients
- A Study to Evaluate the Efficacy, Safety, and Tolerability of JNJ-42847922 in Participants With Insomnia Disorder
- Almorexant (ACT 078573) in Adult Subjects With Chronic Primary Insomnia
- Alternative Dosing Regimens in the Pharmacotherapy of Insomnia
- An Efficacy Study of Compound LY2624803 in the Treatment of Patients With Chronic Insomnia
- Assess the Effect of Zolpidem, Silenor & Placebo on Arousability, Ataxia/Balance & Cognition in Healthy Volunteers
- Behavioral and Pharmacological Treatment for Insomnia
- Bioequivalence Study of Zolpidem 10 mg Tablets Under Fed Conditions
- Bioequivalence Study of Zolpidem 10mg Tablets Under Fasting Conditions
In development for (20)
- Alzheimer disease Phase 3
- Anxiety Phase 3
- Attention deficit-hyperactivity disorder Phase 3
- Autism Phase 2
- Autism spectrum disorder Phase 2
- Bipolar disorder Phase 3
- Cannabis dependence Phase 1
- Dementia Phase 3
- Depressive disorder Phase 3
- Drug dependence Phase 2
- Focal dystonia Phase 1
- Generalized anxiety disorder Phase 3
- Insomnia Phase 3
- Major depressive disorder Phase 1
- Obesity disorder Phase 1
- Panic disorder Phase 3
- Parkinson disease Phase 2
- Prostate adenocarcinoma Phase 1
- Schizophrenia Phase 3
- Sleep disorder Phase 3
Other linked conditions (1)
- Vascular dementia