zolpidem Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
hypnotics/sedatives, zolpidem derivatives	2870	82626-48-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ambien zolpidem zolpidem tartrate	An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA. Molecular weight: 307.40 Formula: C19H21N3O CLOGP: 3.03 LIPINSKI: 0 HAC: 4 HDO: 0 TPSA: 37.61 ALOGS: -3.99 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ambien
zolpidem
zolpidem tartrate

An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.

Molecular weight: 307.40
Formula: C19H21N3O
CLOGP: 3.03
LIPINSKI: 0
HAC: 4
HDO: 0
TPSA: 37.61
ALOGS: -3.99
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	23 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.47 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	72 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.54 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.08 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.70 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 16, 1992	FDA	SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Completed suicide	6348.28	45.82	1480	5373	19554	2331678
Toxicity to various agents	4111.95	45.82	1151	5702	31603	2319629
Drug abuse	2024.98	45.82	538	6315	11488	2339744
Intentional overdose	1376.21	45.82	393	6460	10928	2340304
Somnambulism	1360.20	45.82	245	6608	645	2350587
Amnesia	1266.42	45.82	335	6518	6918	2344314
Overdose	1137.90	45.82	388	6465	19519	2331713
Drug dependence	1054.33	45.82	244	6609	2801	2348431
Suicide attempt	986.50	45.82	304	6549	10978	2340254
Coma	968.11	45.82	285	6568	8771	2342461
Cardio-respiratory arrest	952.16	45.82	282	6571	8864	2342368
Somnolence	778.88	45.82	307	6546	23178	2328054
Cardiac arrest	769.73	45.82	270	6583	14660	2336572
Respiratory arrest	759.60	45.82	217	6636	5961	2345271
Fall	696.13	45.82	349	6504	46750	2304482
Confusional state	692.16	45.82	285	6568	24059	2327173
Intentional product misuse	619.20	45.82	205	6648	9284	2341948
Sopor	584.82	45.82	161	6692	3834	2347398
Poisoning	566.44	45.82	146	6707	2674	2348558
Insomnia	551.46	45.82	247	6606	25540	2325692
Loss of consciousness	496.39	45.82	209	6644	18558	2332674
Drug ineffective	459.58	45.82	354	6499	101270	2249962
Abnormal sleep-related event	457.70	45.82	75	6778	80	2351152
Road traffic accident	447.80	45.82	133	6720	4175	2347057
Hypotension	421.38	45.82	221	6632	32215	2319017
Intentional self-injury	418.43	45.82	125	6728	4002	2347230
Drug hypersensitivity	374.40	45.82	232	6621	46411	2304821
Abnormal behaviour	359.26	45.82	115	6738	4645	2346587
Sleep-related eating disorder	344.06	45.82	58	6795	84	2351148
Hallucination	288.08	45.82	112	6741	8036	2343196
Delirium	281.72	45.82	98	6755	5125	2346107
Tachycardia	274.69	45.82	133	6720	16276	2334956
Impaired driving ability	267.83	45.82	66	6787	993	2350239
Exposure via ingestion	265.95	45.82	62	6791	726	2350506
Agitation	264.87	45.82	115	6738	10936	2340296
Drug interaction	261.49	45.82	156	6697	29007	2322225
Drug withdrawal syndrome	259.79	45.82	99	6754	6722	2344510
Product substitution issue	257.62	45.82	91	6762	4978	2346254
Bradycardia	249.45	45.82	107	6746	9874	2341358
Disorientation	244.51	45.82	93	6760	6279	2344953
Withdrawal syndrome	236.86	45.82	77	6776	3260	2347972
Poisoning deliberate	230.78	45.82	60	6793	1131	2350101
Anxiety	222.19	45.82	141	6712	29218	2322014
Hallucination, visual	220.63	45.82	71	6782	2908	2348324
Mydriasis	210.87	45.82	64	6789	2155	2349077
Suicidal ideation	210.27	45.82	98	6755	10989	2340243
Unresponsive to stimuli	190.01	45.82	72	6781	4804	2346428
Accidental overdose	189.24	45.82	68	6785	3904	2347328
Death	180.92	45.82	191	6662	81277	2269955
Aggression	176.88	45.82	68	6785	4718	2346514
Depressed level of consciousness	168.68	45.82	75	6778	7529	2343703
Miosis	168.09	45.82	47	6806	1177	2350055
Vomiting	162.63	45.82	170	6683	71432	2279800
Electrocardiogram QT prolonged	154.08	45.82	71	6782	7743	2343489
Altered state of consciousness	153.99	45.82	58	6795	3802	2347430
Sleep talking	151.73	45.82	30	6823	146	2351086
Tremor	148.10	45.82	96	6757	20565	2330667
Dysarthria	145.68	45.82	64	6789	6238	2344994
Pneumonia aspiration	141.23	45.82	54	6799	3688	2347544
Disturbance in attention	135.51	45.82	59	6794	5626	2345606
Restlessness	134.25	45.82	55	6798	4508	2346724
Myocardial depression	131.05	45.82	23	6830	48	2351184
Mental status changes	130.02	45.82	57	6796	5525	2345707
Respiratory depression	129.66	45.82	44	6809	2126	2349106
Decorticate posture	126.85	45.82	21	6832	25	2351207
Depression	125.76	45.82	98	6755	28034	2323198
Memory impairment	125.67	45.82	73	6780	12850	2338382
Bradypnoea	124.75	45.82	30	6823	404	2350828
Ventricular hypokinesia	123.69	45.82	32	6821	590	2350642
Generalised tonic-clonic seizure	122.35	45.82	54	6799	5318	2345914
Coma scale abnormal	119.60	45.82	33	6820	785	2350447
Sleep disorder	118.72	45.82	56	6797	6433	2344799
Seizure	117.59	45.82	89	6764	24377	2326855
Prescription form tampering	113.43	45.82	23	6830	130	2351102
Hypothermia	106.89	45.82	38	6815	2110	2349122
Contusion	105.41	45.82	65	6788	12745	2338487
Sedation	103.93	45.82	42	6811	3320	2347912
Speech disorder	100.77	45.82	50	6803	6414	2344818
Victim of sexual abuse	92.18	45.82	18	6835	81	2351151
Dizziness	88.51	45.82	113	6740	58552	2292680
Drug tolerance	85.46	45.82	22	6831	397	2350835
Therapeutic response unexpected	85.31	45.82	38	6815	3821	2347411
Balance disorder	84.11	45.82	51	6802	9696	2341536
Depressed mood	83.37	45.82	41	6812	5157	2346075
Chemical submission	81.94	45.82	14	6839	23	2351209
Rhabdomyolysis	81.84	45.82	44	6809	6660	2344572
Feeling abnormal	79.90	45.82	70	6783	23511	2327721
Psychomotor retardation	78.26	45.82	22	6831	561	2350671
Acute respiratory distress syndrome	77.88	45.82	34	6819	3258	2347974
Metabolic acidosis	77.82	45.82	41	6812	5957	2345275
Nightmare	77.25	45.82	35	6818	3662	2347570
Homicide	76.59	45.82	16	6837	107	2351125
Bradyphrenia	76.46	45.82	25	6828	1074	2350158
Parasomnia	76.19	45.82	15	6838	71	2351161
Alcohol abuse	76.01	45.82	19	6834	303	2350929
Exposure during pregnancy	75.85	45.82	70	6783	25149	2326083
Irritability	75.15	45.82	41	6812	6386	2344846
Substance abuse	74.98	45.82	21	6832	528	2350704
Victim of chemical submission	74.72	45.82	14	6839	48	2351184
Eating disorder	72.23	45.82	29	6824	2252	2348980
Hepatic necrosis	72.20	45.82	24	6829	1086	2350146
Drug abuser	71.49	45.82	23	6830	938	2350294
Drop attacks	71.25	45.82	16	6837	156	2351076
Anterograde amnesia	70.84	45.82	15	6838	108	2351124
Condition aggravated	70.62	45.82	75	6778	31904	2319328
Cognitive disorder	70.42	45.82	37	6816	5344	2345888
Hallucination, auditory	66.42	45.82	27	6826	2165	2349067
Haematoma	66.41	45.82	35	6818	5086	2346146
Cardiogenic shock	66.40	45.82	28	6825	2463	2348769
Dyskinesia	65.73	45.82	34	6819	4755	2346477
Maternal exposure during pregnancy	64.63	45.82	51	6802	14812	2336420
Drug withdrawal convulsions	64.53	45.82	17	6836	337	2350895
Nausea	63.51	45.82	139	6714	112050	2239182
Drug-induced liver injury	61.77	45.82	30	6823	3669	2347563
Hypersensitivity vasculitis	60.87	45.82	22	6831	1280	2349952
Psychotic disorder	60.73	45.82	32	6821	4647	2346585
Hyperreflexia	60.68	45.82	20	6833	881	2350351
Electrocardiogram QRS complex prolonged	60.57	45.82	21	6832	1081	2350151
Mania	60.32	45.82	26	6827	2414	2348818
Drug screen positive	60.27	45.82	20	6833	900	2350332
Incorrect dose administered	59.60	45.82	41	6812	9654	2341578
Encephalopathy	58.65	45.82	31	6822	4530	2346702
Middle insomnia	58.17	45.82	22	6831	1455	2349777
Parkinsonism hyperpyrexia syndrome	56.93	45.82	10	6843	21	2351211
Head injury	56.40	45.82	29	6824	4005	2347227
Fatigue	55.95	45.82	112	6741	84761	2266471
Headache	55.49	45.82	108	6745	80071	2271161
Hypertension	54.84	45.82	61	6792	27300	2323932
Drug use disorder	54.54	45.82	15	6838	352	2350880
Hyponatraemia	54.25	45.82	44	6809	13281	2337951
Crying	54.05	45.82	29	6824	4367	2346865
Catatonia	53.78	45.82	18	6835	832	2350400
Syncope	52.96	45.82	48	6805	16827	2334405
Pulmonary congestion	52.08	45.82	22	6831	1943	2349289
Pancreatitis acute	51.85	45.82	27	6826	3826	2347406
Gait disturbance	51.73	45.82	54	6799	22491	2328741
Hypokalaemia	51.63	45.82	39	6814	10615	2340617
Vertigo	51.44	45.82	37	6816	9347	2341885
Cardiomegaly	51.05	45.82	23	6830	2373	2348859
Asthenia	50.60	45.82	77	6776	46849	2304383
Hangover	50.58	45.82	13	6840	233	2350999
Impaired work ability	50.44	45.82	21	6832	1789	2349443
Spleen congestion	50.34	45.82	10	6843	50	2351182
Weight increased	48.58	45.82	52	6801	22285	2328947
Acute kidney injury	48.46	45.82	58	6795	28064	2323168
Analgesic drug level increased	48.37	45.82	13	6840	279	2350953
Mental disorder	48.05	45.82	26	6827	3981	2347251
Leukocytosis	47.95	45.82	25	6828	3551	2347681
Product complaint	47.71	45.82	27	6826	4511	2346721
Hypokinesia	47.70	45.82	20	6833	1734	2349498
Hyperthermia	47.64	45.82	19	6834	1449	2349783
Blepharospasm	47.51	45.82	15	6838	575	2350657
Respiratory distress	47.24	45.82	28	6825	5101	2346131
Blood creatine phosphokinase increased	47.20	45.82	28	6825	5108	2346124
Asphyxia	47.07	45.82	17	6836	987	2350245
Aspiration	46.83	45.82	19	6834	1515	2349717
Acute pulmonary oedema	46.81	45.82	18	6835	1245	2349987
Oxygen saturation decreased	46.43	45.82	32	6821	7554	2343678
Logorrhoea	45.98	45.82	14	6839	475	2350757
Affective disorder	45.92	45.82	16	6837	836	2350396

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Completed suicide	3320.76	48.95	856	3734	15456	1726735
Toxicity to various agents	2090.91	48.95	683	3907	28458	1713733
Drug abuse	1471.67	48.95	440	4150	13249	1728942
Somnambulism	1211.94	48.95	218	4372	496	1741695
Amnesia	969.69	48.95	255	4335	4636	1737555
Intentional overdose	803.95	48.95	243	4347	7427	1734764
Drug dependence	753.04	48.95	193	4397	3134	1739057
Respiratory arrest	623.85	48.95	188	4402	5651	1736540
Confusional state	615.08	48.95	259	4331	21019	1721172
Cardio-respiratory arrest	592.54	48.95	202	4388	9091	1733100
Overdose	590.46	48.95	235	4355	16466	1725725
Somnolence	586.44	48.95	234	4356	16505	1725686
Suicide attempt	556.00	48.95	182	4408	7199	1734992
Cardiac arrest	513.82	48.95	210	4380	15720	1726471
Poisoning	490.58	48.95	130	4460	2402	1739789
Road traffic accident	480.47	48.95	138	4452	3475	1738716
Fall	409.05	48.95	211	4379	27003	1715188
Abnormal behaviour	404.00	48.95	138	4452	6204	1735987
Delirium	391.85	48.95	135	4455	6227	1735964
Intentional self-injury	377.14	48.95	107	4483	2566	1739625
Coma	374.37	48.95	135	4455	7127	1735064
Sopor	336.74	48.95	92	4498	1909	1740282
Insomnia	311.42	48.95	149	4441	16127	1726064
Impaired driving ability	290.51	48.95	64	4526	509	1741682
Hallucination	284.06	48.95	114	4476	8056	1734135
Intentional product misuse	267.32	48.95	106	4484	7252	1734939
Agitation	257.49	48.95	116	4474	10910	1731281
Abnormal sleep-related event	227.83	48.95	41	4549	91	1742100
Depressed level of consciousness	215.27	48.95	88	4502	6504	1735687
Drug interaction	213.48	48.95	140	4450	27818	1714373
Disorientation	213.31	48.95	83	4507	5386	1736805
Poisoning deliberate	205.32	48.95	52	4538	790	1741401
Sleep-related eating disorder	202.72	48.95	35	4555	54	1742137
Aggression	194.43	48.95	87	4503	8028	1734163
Drug ineffective	183.80	48.95	180	4410	63621	1678570
Altered state of consciousness	172.30	48.95	63	4527	3434	1738757
Anxiety	167.31	48.95	97	4493	15430	1726761
Withdrawal syndrome	165.90	48.95	55	4535	2233	1739958
Loss of consciousness	165.79	48.95	95	4495	14780	1727411
Tachycardia	160.69	48.95	88	4502	12540	1729651
Drug withdrawal syndrome	153.06	48.95	62	4528	4463	1737728
Mental status changes	135.48	48.95	62	4528	6013	1736178
Conduction disorder	129.48	48.95	31	4559	367	1741824
Hallucination, visual	128.76	48.95	47	4543	2545	1739646
Nightmare	121.80	48.95	46	4544	2741	1739450
Hypotension	114.75	48.95	99	4491	29555	1712636
Suicidal ideation	112.79	48.95	61	4529	8457	1733734
Parasomnia	108.87	48.95	21	4569	77	1742114
Exposure via ingestion	108.38	48.95	30	4560	650	1741541
Drug hypersensitivity	108.37	48.95	73	4517	15062	1727129
Irritability	106.43	48.95	51	4539	5481	1736710
Vomiting	105.86	48.95	106	4484	38209	1703982
Depression	101.99	48.95	73	4517	16596	1725595
Drug use disorder	100.08	48.95	26	4564	438	1741753
Death	99.96	48.95	155	4435	87288	1654903
Medication error	98.20	48.95	46	4544	4697	1737494
Ataxia	96.19	48.95	37	4553	2316	1739875
Restlessness	95.97	48.95	44	4546	4277	1737914
Automatism	92.03	48.95	17	4573	46	1742145
Suicidal behaviour	90.83	48.95	23	4567	348	1741843
Psychotic disorder	89.38	48.95	44	4546	5012	1737179
Miosis	89.29	48.95	31	4559	1447	1740744
Paranoia	84.54	48.95	33	4557	2148	1740043
Prescription form tampering	81.97	48.95	18	4572	140	1742051
Sleep disorder	79.78	48.95	38	4552	4025	1738166
Memory impairment	77.95	48.95	44	4546	6619	1735572
Dysarthria	76.15	48.95	40	4550	5219	1736972
Unresponsive to stimuli	75.07	48.95	38	4552	4591	1737600
Asphyxia	74.34	48.95	25	4565	1058	1741133
Incoherent	72.40	48.95	23	4567	811	1741380
Lethargy	69.64	48.95	42	4548	7142	1735049
Bradyphrenia	68.94	48.95	21	4569	643	1741548
Blood creatine phosphokinase increased	68.83	48.95	45	4545	8811	1733380
Homicide	68.68	48.95	18	4572	314	1741877
Product substitution issue	68.39	48.95	32	4558	3254	1738937
Anterograde amnesia	68.09	48.95	14	4576	76	1742115
Sedation	67.20	48.95	32	4558	3385	1738806
Accidental overdose	66.98	48.95	34	4556	4130	1738061
Skin laceration	66.69	48.95	27	4563	1934	1740257
Delusion	66.65	48.95	28	4562	2203	1739988
Rhabdomyolysis	66.45	48.95	48	4542	11042	1731149
Disturbance in attention	66.45	48.95	34	4556	4200	1737991
Electrocardiogram QT prolonged	65.88	48.95	37	4553	5508	1736683
Product administration error	65.33	48.95	30	4560	2923	1739268
Incorrect dose administered	63.38	48.95	40	4550	7369	1734822
Seizure	62.71	48.95	60	4530	20381	1721810
Initial insomnia	62.26	48.95	18	4572	458	1741733
Accidental exposure to product	61.66	48.95	32	4558	4069	1738122
Gun shot wound	61.45	48.95	17	4573	367	1741824
Metabolic acidosis	61.35	48.95	35	4555	5367	1736824
Drug tolerance	61.27	48.95	17	4573	371	1741820
Bradykinesia	60.82	48.95	18	4572	498	1741693
Abnormal dreams	60.76	48.95	25	4565	1866	1740325
Thinking abnormal	58.54	48.95	22	4568	1290	1740901
Mydriasis	58.34	48.95	22	4568	1302	1740889
Mania	57.86	48.95	25	4565	2108	1740083
Pneumonia aspiration	56.81	48.95	33	4557	5233	1736958
Balance disorder	56.37	48.95	34	4556	5778	1736413
Hypoglycaemia	56.27	48.95	39	4551	8399	1733792
Self-medication	55.88	48.95	18	4572	664	1741527
Head injury	55.46	48.95	27	4563	2997	1739194
Theft	53.00	48.95	11	4579	63	1742128
Tremor	52.98	48.95	45	4545	13086	1729105
Apnoea	52.90	48.95	21	4569	1428	1740763
Alcohol use	51.97	48.95	18	4572	833	1741358
Legal problem	51.74	48.95	11	4579	72	1742119
Drug withdrawal syndrome neonatal	51.67	48.95	17	4573	671	1741520
Encephalopathy	50.96	48.95	29	4561	4423	1737768
Personality change	50.66	48.95	19	4571	1107	1741084
Dependence	50.31	48.95	14	4576	309	1741882
Hyponatraemia	49.48	48.95	37	4553	8963	1733228
Hypokinesia	49.38	48.95	19	4571	1188	1741003

Pharmacologic Action:

Source	Code	Description
ATC	N05CF02	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine related drugs
CHEBI has role	CHEBI:35488	central nervous system depressant
CHEBI has role	CHEBI:51373	GABA agonist
CHEBI has role	CHEBI:35717	sedative
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018682	GABA Agents
MeSH PA	D018755	GABA Agonists
MeSH PA	D058785	GABA-A Receptor Agonists
MeSH PA	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D000068776	Sleep Aids, Pharmaceutical
FDA EPC	N0000175759	gamma-Aminobutyric Acid-ergic Agonist
FDA MoA	N0000000196	GABA A Agonists
FDA CS	M0018233	Pyridines
FDA PE	N0000175728	Central Nervous System Depression

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Initial insomnia	indication	59050008
Insomnia	indication	193462001
Suicidal thoughts	contraindication	6471006
Hallucinations	contraindication	7011001
Asthenia	contraindication	13791008
Alcohol intoxication	contraindication	25702006
Depressive disorder	contraindication	35489007
Aggressive behavior	contraindication	61372001
Substance abuse	contraindication	66214007
Sleep apnea	contraindication	73430006	DOID:0050847
Disease of liver	contraindication	235856003	DOID:409
Sleep automatism	contraindication	247962006
Severe chronic obstructive pulmonary disease	contraindication	313299006
Impaired cognition	contraindication	386806002
Memory impairment	contraindication	386807006
Attention deficit hyperactivity disorder	contraindication	406506008

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.73	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
1.75MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	7682628	Feb. 16, 2025	METHOD FOR TREATING INSOMNIA
3.5MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	7682628	Feb. 16, 2025	METHOD FOR TREATING INSOMNIA
10MG	EDLUAR	MYLAN SPECIALITY LP	N021997	March 13, 2009	RX	TABLET	SUBLINGUAL	9597281	April 6, 2027	METHOD OF TREATING INSOMNIA CHARACTERIZED BY DIFFICULTY WITH SLEEP ONSET
5MG	EDLUAR	MYLAN SPECIALITY LP	N021997	March 13, 2009	RX	TABLET	SUBLINGUAL	9597281	April 6, 2027	METHOD OF TREATING INSOMNIA CHARACTERIZED BY DIFFICULTY WITH SLEEP ONSET
1.75MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	7658945	April 15, 2027	METHOD FOR TREATING INSOMNIA
3.5MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	7658945	April 15, 2027	METHOD FOR TREATING INSOMNIA
1.75MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	8242131	Aug. 20, 2029	METHOD OF TREATING MIDDLE-OF-THE-NIGHT INSOMNIA
3.5MG	INTERMEZZO	PURDUE PHARMA	N022328	Nov. 23, 2011	DISCN	TABLET	SUBLINGUAL	8242131	Aug. 20, 2029	METHOD OF TREATING MIDDLE-OF-THE-NIGHT INSOMNIA
10MG	EDLUAR	MYLAN SPECIALITY LP	N021997	March 13, 2009	RX	TABLET	SUBLINGUAL	9265720	Feb. 25, 2031	METHOD OF TREATING INSOMNIA CHARACTERIZED BY DIFFICULTY WITH SLEEP ONSET
5MG	EDLUAR	MYLAN SPECIALITY LP	N021997	March 13, 2009	RX	TABLET	SUBLINGUAL	9265720	Feb. 25, 2031	METHOD OF TREATING INSOMNIA CHARACTERIZED BY DIFFICULTY WITH SLEEP ONSET
5MG/SPRAY	ZOLPIMIST	AYTU	N022196	Dec. 19, 2008	RX	SPRAY, METERED	ORAL	8236285	Aug. 7, 2032	TREATMENT OF TRANSIENT INSOMNIA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRA3_HUMAN GBRB3_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.42	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRB2_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	6.70	WOMBAT-PK	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1	Ion channel	P14867	GBRA1_HUMAN	ALLOSTERIC MODULATOR	Ki	7.68	IUPHAR	IUPHAR
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRB3_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	7.57	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRA2_HUMAN GBRB3_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.81	WOMBAT-PK	CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2	Ion channel	P18507 P34903 P47870	GBRA3_HUMAN GBRB2_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.16	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Km	3.70	WOMBAT-PK
Gamma-aminobutyric acid receptor subunit alpha-2	Ion channel	P47869	GBRA2_HUMAN		Ki	6.39	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-3	Ion channel	P34903	GBRA3_HUMAN		Ki	6.01	CHEMBL
GABA A receptor alpha-2/beta-2/gamma-2	Ion channel		GBRA2_RAT GBRB2_RAT GBRG2_RAT		Ki	6.81	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1	Ion channel		GBRA1_RAT		Ki	7.30	CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2	Ion channel		GBRA3_RAT GBRB2_RAT GBRG2_RAT		Ki	6.42	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-2	Ion channel		GBRA2_RAT		Ki	6.12	CHEMBL
CAAX prenyl protease 2	Unclassified		RCE1_YEAST		AC50	4.77	CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-5	Ion channel		GBRA5_RAT		Ki	7.46	CHEMBL
GABA A receptor alpha-6/beta-2/gamma-2	Ion channel		GBRA6_RAT GBRB2_RAT GBRG2_RAT		Ki	6.01	CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRA1_RAT GBRA2_RAT GBRA3_RAT GBRA4_RAT GBRA5_RAT GBRA6_RAT GBRB1_RAT GBRB2_RAT GBRB3_RAT GBRD_RAT GBRE_RAT GBRG1_RAT GBRG2_RAT GBRG3_RAT GBRP_RAT Q91ZM7_RAT		Ki	7.60	CHEMBL
GABA-A receptor; alpha-1/beta-2/gamma-2	Ion channel		GBRA1_RAT GBRB2_RAT GBRG2_RAT		Ki	7.72	CHEMBL
Translocator protein	Membrane receptor		TSPO_RAT		IC50	5.33	CHEMBL

External reference:

ID	Source
D000077334	MESH_DESCRIPTOR_UI
C0487782	UMLSCUI
D00706	KEGG_DRUG
7K383OQI23	UNII
5741	INN_ID
96231005	SNOMEDCT_US
4023596	VANDF
d00910	MMSL
39993	RXNORM
387569009	SNOMEDCT_US
004146	NDDF
CHEMBL911	ChEMBL_ID
DB00425	DRUGBANK_ID
CHEBI:10125	CHEBI
99294-93-6	SECONDARY_CAS_RN
5732	PUBCHEM_CID
CHEMBL1723343	ChEMBL_ID
CHEMBL3989820	ChEMBL_ID
4348	IUPHAR_LIGAND_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ambien	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5401	TABLET, FILM COATED	5 mg	ORAL	NDA	20 sections
Ambien	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5421	TABLET, FILM COATED	10 mg	ORAL	NDA	20 sections
Ambien	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5501	TABLET, COATED	6.25 mg	ORAL	NDA	20 sections
Ambien	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5521	TABLET, COATED	12.50 mg	ORAL	NDA	20 sections
Edluar	HUMAN PRESCRIPTION DRUG LABEL	1	0037-6010	TABLET	10 mg	ORAL	NDA	20 sections
Edluar	HUMAN PRESCRIPTION DRUG LABEL	1	0037-6050	TABLET	5 mg	ORAL	NDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0086	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0087	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0073	TABLET, FILM COATED	5 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0074	TABLET, FILM COATED	10 mg	ORAL	ANDA	20 sections
Zolpidem	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9962	TABLET	5 mg	ORAL	ANDA	19 sections
Zolpidem	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9963	TABLET	10 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0228-3481	TABLET, FILM COATED, EXTENDED RELEASE	6.25 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0228-3482	TABLET, FILM COATED, EXTENDED RELEASE	12.50 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8046	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8047	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8225	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8226	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
Zolpidem tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5315	TABLET, EXTENDED RELEASE	6.25 mg	ORAL	ANDA	20 sections
Zolpidem tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5316	TABLET, EXTENDED RELEASE	12.50 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5317	TABLET, COATED	5 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5318	TABLET, COATED	10 mg	ORAL	ANDA	20 sections
ZOLPIDEM TARTRATE	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6082	TABLET	5 mg	ORAL	ANDA	20 sections
ZOLPIDEM TARTRATE	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6083	TABLET	10 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0955-1702	TABLET, FILM COATED, EXTENDED RELEASE	6.25 mg	ORAL	NDA AUTHORIZED GENERIC	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	0955-1703	TABLET, FILM COATED, EXTENDED RELEASE	12.50 mg	ORAL	NDA AUTHORIZED GENERIC	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	10370-116	TABLET, FILM COATED, EXTENDED RELEASE	12.50 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	10370-117	TABLET, FILM COATED, EXTENDED RELEASE	6.25 mg	ORAL	ANDA	20 sections
ZOLPIDEM TARTRATE	HUMAN PRESCRIPTION DRUG LABEL	1	10544-040	TABLET	10 mg	ORAL	ANDA	20 sections
Zolpidem Tartrate	HUMAN PRESCRIPTION DRUG LABEL	1	10544-539	TABLET, FILM COATED	10 mg	ORAL	ANDA	20 sections