naltrexone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists related to normorphine	1765	16590-41-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: naltrexone cyclopropylmethylnoroxymorphone naltrel naltrexone hydrochloride naltrexone hydrochloride dihydrate naltrexone HCl	Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. Molecular weight: 341.41 Formula: C20H23NO4 CLOGP: 0.36 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 70 ALOGS: -2.05 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

naltrexone
cyclopropylmethylnoroxymorphone
naltrel
naltrexone hydrochloride
naltrexone hydrochloride dihydrate
naltrexone HCl

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

Molecular weight: 341.41
Formula: C20H23NO4
CLOGP: 0.36
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 70
ALOGS: -2.05
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	100 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	22 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	7.60 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	57 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.79 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.90 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 20, 1984	FDA	TEVA WOMENS

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
Injection site reaction	3616.37	22.30	1166	20154	52081	56218666
Alcoholism	2773.92	22.30	511	20809	1698	56269049
Injection site mass	2646.41	22.30	708	20612	16085	56254662
Injection site pain	1387.12	22.30	736	20584	116382	56154365
Injection site induration	994.05	22.30	285	21035	8330	56262417
Drug dependence	557.22	22.30	236	21084	22297	56248450
Therapeutic response shortened	453.23	22.30	160	21160	9226	56261521
Product administered at inappropriate site	346.89	22.30	97	21223	2573	56268174
Injection site swelling	262.43	22.30	178	21142	43400	56227347
Feeling abnormal	254.33	22.30	282	21038	133320	56137427
Withdrawal syndrome	251.46	22.30	128	21192	18334	56252413
Injection site abscess	244.45	22.30	61	21259	1025	56269722
Inadequate analgesia	153.94	22.30	52	21268	2619	56268128
Injection site warmth	152.16	22.30	84	21236	14159	56256588
Product dose omission issue	136.55	22.30	263	21057	204490	56066257
Needle issue	134.93	22.30	66	21254	8672	56262075
Inappropriate schedule of product administration	134.85	22.30	162	21158	83225	56187522
Alcohol use	130.95	22.30	43	21277	1982	56268765
Injection site nodule	129.01	22.30	49	21271	3470	56267277
Drug screen positive	122.56	22.30	47	21273	3417	56267330
Drug use disorder	122.28	22.30	51	21269	4618	56266129
Anxiety	115.36	22.30	237	21083	192935	56077812
Insomnia	108.26	22.30	230	21090	191630	56079117
Substance abuse	103.82	22.30	45	21275	4480	56266267
Body tinea	103.42	22.30	33	21287	1387	56269360
Injection site erythema	97.64	22.30	133	21187	77315	56193432
Depression	97.09	22.30	212	21108	179905	56090842
Lack of injection site rotation	96.40	22.30	23	21297	317	56270430
Product administration error	94.89	22.30	72	21248	20857	56249890
Inhibitory drug interaction	94.52	22.30	35	21285	2309	56268438
Alcohol poisoning	91.27	22.30	32	21288	1803	56268944
Injection site pruritus	89.17	22.30	94	21226	41837	56228910
Rheumatoid arthritis	85.67	22.30	20	21300	382584	55888163
Lack of administration site rotation	82.02	22.30	13	21307	10	56270737
Infection susceptibility increased	81.73	22.30	33	21287	2750	56267997
Injection site discomfort	81.39	22.30	37	21283	4123	56266624
Injection site cellulitis	75.74	22.30	25	21295	1171	56269576
Dependence	70.30	22.30	27	21293	1970	56268777
Tremor	68.00	22.30	145	21175	120944	56149803
Acute kidney injury	63.88	22.30	8	21312	240755	56029992
Necrosis ischaemic	63.65	22.30	20	21300	799	56269948
Injection site cyst	63.46	22.30	12	21308	47	56270700
Alcohol abuse	63.38	22.30	25	21295	1959	56268788
Glucose tolerance impaired	63.02	22.30	34	21286	5471	56265276
Injection site infection	59.12	22.30	23	21297	1737	56269010
Poor quality sleep	59.10	22.30	51	21269	17704	56253043
Euphoric mood	58.67	22.30	30	21290	4328	56266419
Imprisonment	57.27	22.30	14	21306	215	56270532
Systemic lupus erythematosus	55.93	22.30	3	21317	180075	56090672
Hospitalisation	55.65	22.30	101	21219	74899	56195848
Irritability	55.33	22.30	62	21258	29526	56241221
Impaired quality of life	54.26	22.30	36	21284	8438	56262309
Anaemia	54.14	22.30	17	21303	267494	56003253
Alcohol withdrawal syndrome	52.54	22.30	17	21303	747	56270000
Dyspnoea	51.71	22.30	91	21229	592486	55678261
Surgery	50.63	22.30	62	21258	32424	56238323
Pneumonia	50.44	22.30	48	21272	407050	55863697
Nausea	50.07	22.30	474	20846	763704	55507043
Pneumonia streptococcal	49.51	22.30	20	21300	1668	56269079
General physical health deterioration	49.36	22.30	4	21316	170006	56100741
Wrong technique in product usage process	49.21	22.30	83	21237	58085	56212662
Impaired work ability	48.79	22.30	42	21278	14530	56256217
Feeling drunk	47.87	22.30	25	21295	3767	56266980
Injection site necrosis	47.68	22.30	18	21302	1253	56269494
Beta haemolytic streptococcal infection	47.29	22.30	20	21300	1874	56268873
Injection site bruising	46.77	22.30	65	21255	38456	56232291
Pregnancy	46.63	22.30	60	21260	32973	56237774
Magnesium deficiency	45.35	22.30	14	21306	527	56270220
Treatment failure	44.36	22.30	6	21314	170386	56100361
Apathy	44.30	22.30	31	21289	7923	56262824
Hypotension	42.34	22.30	21	21299	250487	56020260
Headache	42.27	22.30	358	20962	558686	55712061
Drug intolerance	42.11	22.30	24	21296	264794	56005953
Purpura	41.21	22.30	33	21287	10329	56260418
Crying	40.21	22.30	45	21275	21395	56249352
Neutropenia	40.17	22.30	6	21314	158161	56112586
Malaise	40.01	22.30	257	21063	367603	55903144
Malabsorption from injection site	38.98	22.30	7	21313	19	56270728
Arthropathy	38.29	22.30	14	21306	200261	56070486
Condition aggravated	37.84	22.30	45	21275	344853	55925894
Oral herpes	37.81	22.30	45	21275	22845	56247902
Product use issue	37.30	22.30	12	21308	186029	56084718
Hyperammonaemia	36.59	22.30	23	21297	4917	56265830
Infusion related reaction	36.08	22.30	17	21303	208914	56061833
Detoxification	35.78	22.30	6	21314	9	56270738
Bone density decreased	35.25	22.30	33	21287	12727	56258020
Panic attack	35.10	22.30	41	21279	20406	56250341
Product preparation error	34.61	22.30	22	21298	4794	56265953
Mood altered	33.97	22.30	33	21287	13322	56257425
Rash	32.76	22.30	88	21232	492959	55777788
Fatigue	32.03	22.30	446	20874	788106	55482641
Injection site haematoma	31.67	22.30	23	21297	6229	56264518
Coronavirus infection	31.12	22.30	18	21302	3311	56267436
Toothache	30.94	22.30	36	21284	17844	56252903
Injection site irritation	30.82	22.30	20	21300	4516	56266231
Road traffic accident	30.76	22.30	45	21275	27882	56242865
Myoglobinuria	30.74	22.30	9	21311	282	56270465
Hyperlipidaemia	30.57	22.30	36	21284	18073	56252674
Atrial fibrillation	30.42	22.30	3	21317	108894	56161853
Hypersomnia	30.13	22.30	34	21286	16307	56254440
Adiposis dolorosa	30.09	22.30	9	21311	304	56270443
Skin disorder	29.86	22.30	43	21277	26266	56244481
Wound	29.56	22.30	8	21312	138796	56131951
Feeling of despair	29.50	22.30	15	21305	2138	56268609
Mass	29.47	22.30	30	21290	12809	56257938
Somnolence	29.23	22.30	131	21189	163282	56107465
Restless legs syndrome	29.12	22.30	34	21286	16913	56253834
Disease progression	29.11	22.30	3	21317	105170	56165577
Drug screen false positive	28.55	22.30	11	21309	809	56269938
Death of relative	28.32	22.30	8	21312	220	56270527
Decreased appetite	28.12	22.30	160	21160	219071	56051676
Food craving	28.11	22.30	13	21307	1506	56269241
Haemoglobin decreased	28.06	22.30	8	21312	134129	56136618
Oedema peripheral	27.96	22.30	15	21305	171239	56099508
Cold sweat	27.76	22.30	27	21293	10916	56259831
Intentional overdose	27.75	22.30	72	21248	68045	56202702
Dental operation	27.63	22.30	12	21308	1200	56269547
Stomatitis	27.60	22.30	6	21314	120804	56149943
Pyrexia	27.60	22.30	75	21245	418698	55852049
Caffeine consumption	27.52	22.30	4	21316	0	56270747
Therapeutic product effect decreased	27.43	22.30	15	21305	169437	56101310
Drug hypersensitivity	26.99	22.30	39	21281	275166	55995581
Restlessness	26.66	22.30	41	21279	26545	56244202
Suicidal ideation	26.63	22.30	64	21256	57678	56213069
Anger	26.29	22.30	27	21293	11645	56259102
Urinary tract infection	25.70	22.30	32	21288	240481	56030266
Injection site inflammation	25.54	22.30	16	21304	3400	56267347
Alanine aminotransferase increased	25.09	22.30	3	21317	93659	56177088
Snoring	24.85	22.30	16	21304	3565	56267182
Abnormal dreams	24.84	22.30	24	21296	9625	56261122
Drug withdrawal syndrome	24.71	22.30	39	21281	25818	56244929
Depressed mood	24.49	22.30	47	21273	36312	56234435
Cough	24.37	22.30	38	21282	259923	56010824
Product preparation issue	24.26	22.30	10	21310	878	56269869
Diaphragmatic paralysis	24.22	22.30	9	21311	599	56270148
Joint swelling	23.85	22.30	46	21274	289754	55980993
White blood cell count decreased	23.74	22.30	9	21311	125981	56144766
Swelling	23.48	22.30	34	21286	239737	56031010
Drug titration error	23.19	22.30	9	21311	675	56270072
Sepsis	23.19	22.30	12	21308	139828	56130919
Pulmonary embolism	23.13	22.30	6	21314	107118	56163629

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
Injection site reaction	5205.11	29.91	1259	19668	10392	31666025
Alcoholism	3012.85	29.91	644	20283	2755	31673662
Injection site pain	2789.79	29.91	991	19936	33643	31642774
Injection site mass	1439.52	29.91	395	20532	5469	31670948
Drug dependence	944.27	29.91	403	20524	22176	31654241
Feeling abnormal	639.21	29.91	422	20505	56580	31619837
Injection site induration	633.61	29.91	175	20752	2472	31673945
Therapeutic response shortened	582.78	29.91	197	20730	5640	31670777
Product administered at inappropriate site	445.22	29.91	123	20804	1737	31674680
Injection site swelling	384.81	29.91	169	20758	9918	31666499
Withdrawal syndrome	354.39	29.91	167	20760	11550	31664867
Needle issue	330.04	29.91	126	20801	5147	31671270
Product dose omission issue	299.47	29.91	358	20569	105228	31571189
Insomnia	274.50	29.91	325	20602	94511	31581906
Drug use disorder	245.02	29.91	94	20833	3889	31672528
Alcohol use	199.30	29.91	76	20851	3091	31673326
Lack of injection site rotation	192.42	29.91	39	20888	118	31676299
Injection site discomfort	186.52	29.91	59	20868	1358	31675059
Inappropriate schedule of product administration	166.65	29.91	186	20741	50637	31625780
Depression	163.49	29.91	247	20680	90568	31585849
Drug screen positive	161.40	29.91	69	20858	3783	31672634
Pain	154.74	29.91	364	20563	186395	31490022
Anxiety	147.65	29.91	236	20691	90797	31585620
Acute kidney injury	137.88	29.91	13	20914	279701	31396716
Injection site abscess	127.17	29.91	38	20889	718	31675699
Anaemia	123.17	29.91	4	20923	213518	31462899
Substance abuse	120.82	29.91	69	20858	7089	31669328
Product administration error	119.58	29.91	91	20836	15156	31661261
Alcohol poisoning	117.20	29.91	52	20875	3119	31673298
Headache	116.70	29.91	324	20603	183328	31493089
Malaise	112.72	29.91	303	20624	168208	31508209
Euphoric mood	106.76	29.91	56	20871	4864	31671553
Imprisonment	106.06	29.91	30	20897	463	31675954
Dependence	105.47	29.91	36	20891	1058	31675359
Drug withdrawal syndrome	103.06	29.91	91	20836	18659	31657758
Pneumonia	99.20	29.91	49	20878	335263	31341154
Nausea	98.94	29.91	433	20494	307514	31368903
Irritability	96.76	29.91	96	20831	22793	31653624
Apathy	94.93	29.91	57	20870	6425	31669992
Inadequate analgesia	83.25	29.91	39	20888	2654	31673763
Feeling drunk	82.15	29.91	34	20893	1717	31674700
Injection site erythema	79.09	29.91	70	20857	14392	31662025
Yawning	78.84	29.91	24	20903	484	31675933
Lack of administration site rotation	71.03	29.91	12	20915	6	31676411
Decreased appetite	70.72	29.91	242	20685	152975	31523442
Injection site nerve damage	70.38	29.91	12	20915	7	31676410
Injection site bruising	70.12	29.91	51	20876	7924	31668493
Road traffic accident	69.77	29.91	69	20858	16312	31660105
Alcohol withdrawal syndrome	68.58	29.91	28	20899	1365	31675052
Tremor	68.56	29.91	154	20773	76266	31600151
Sepsis	67.45	29.91	10	20917	151919	31524498
Injection site warmth	66.91	29.91	30	20897	1844	31674573
Thrombocytopenia	66.69	29.91	8	20919	142739	31533678
Condition aggravated	65.86	29.91	14	20913	163995	31512422
Atrial fibrillation	62.58	29.91	3	20924	113780	31562637
Fatigue	62.50	29.91	406	20521	334800	31341617
Injection site nodule	59.74	29.91	26	20901	1488	31674929
Toxicity to various agents	59.08	29.91	23	20904	181464	31494953
Dyspnoea	58.85	29.91	85	20842	343394	31333023
Emotional poverty	58.38	29.91	19	20908	480	31675937
Pyrexia	58.38	29.91	69	20858	303771	31372646
Renal failure	57.38	29.91	7	20920	123323	31553094
Feeling of despair	57.09	29.91	22	20905	920	31675497
Depressed mood	56.96	29.91	64	20863	17511	31658906
Platelet count decreased	54.62	29.91	5	20922	110430	31565987
Neutropenia	54.29	29.91	13	20914	140351	31536066
Hospitalisation	51.08	29.91	106	20821	49701	31626716
Injection site cellulitis	49.31	29.91	17	20910	515	31675902
Oedema peripheral	49.26	29.91	7	20920	109832	31566585
Hypotension	49.12	29.91	38	20889	204580	31471837
Respiratory failure	49.10	29.91	5	20922	101444	31574973
Injection site pruritus	48.61	29.91	37	20890	6157	31670260
Gait disturbance	47.32	29.91	135	20792	77360	31599057
Restlessness	46.90	29.91	67	20860	23294	31653123
Mood altered	46.83	29.91	41	20886	8305	31668112
Haemoglobin decreased	46.48	29.91	9	20918	112666	31563751
Cardiac failure	45.00	29.91	3	20924	85950	31590467
General physical health deterioration	44.86	29.91	10	20917	113425	31562992
Overdose	44.61	29.91	140	20787	84524	31591893
Blood creatinine increased	44.13	29.91	4	20923	89074	31587343
Anger	43.85	29.91	45	20882	11108	31665309
Pancytopenia	43.04	29.91	4	20923	87312	31589105
Coronavirus infection	42.87	29.91	28	20899	3655	31672762
Hypersomnia	42.17	29.91	44	20883	11075	31665342
Wrong technique in product usage process	41.50	29.91	77	20850	33266	31643151
Cardiac failure congestive	40.89	29.91	3	20924	79384	31597033
White blood cell count decreased	40.54	29.91	5	20922	87393	31589024
Toothache	39.59	29.91	32	20895	5809	31670608
Injection site inflammation	37.46	29.91	15	20912	695	31675722
Alcohol abuse	37.45	29.91	28	20899	4536	31671881
Substance use	37.15	29.91	14	20913	550	31675867
Mood swings	36.77	29.91	34	20893	7390	31669027
Abdominal pain upper	36.65	29.91	109	20818	63893	31612524
Panic attack	35.83	29.91	36	20891	8667	31667750
Sciatic nerve injury	35.76	29.91	9	20918	86	31676331
Death of relative	35.65	29.91	7	20920	17	31676400
Thinking abnormal	34.57	29.91	29	20898	5544	31670873
Product preparation error	34.55	29.91	19	20908	1813	31674604
Injection site scar	34.41	29.91	11	20916	262	31676155
Abnormal dreams	34.14	29.91	32	20895	7076	31669341
Injection site infection	33.24	29.91	15	20912	936	31675481
Product use in unapproved indication	33.18	29.91	12	20915	99159	31577258
Alanine aminotransferase increased	32.90	29.91	5	20922	74651	31601766
Myocardial infarction	32.77	29.91	17	20910	113437	31562980
Surgery	32.75	29.91	41	20886	12558	31663859
Energy increased	32.68	29.91	16	20911	1200	31675217
Libido decreased	31.55	29.91	25	20902	4411	31672006
Muscle spasms	31.50	29.91	108	20819	68210	31608207
Procedural pain	31.19	29.91	25	20902	4484	31671933
Mobility decreased	31.17	29.91	61	20866	27408	31649009
Substance use disorder	31.02	29.91	12	20915	507	31675910
Chromaturia	30.99	29.91	41	20886	13257	31663160
Pleural effusion	30.85	29.91	6	20921	74914	31601503
Pulmonary embolism	30.69	29.91	8	20919	81638	31594779
Urinary tract infection	29.93	29.91	7	20920	76862	31599555

FDA Adverse Event Reporting System (Geriatric)

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
Injection site reaction	7486.74	22.41	2155	34275	47697	70844317
Alcoholism	4546.70	22.41	909	35521	3536	70888478
Injection site pain	3620.22	22.41	1565	34865	116054	70775960
Injection site mass	3608.18	22.41	983	35447	17360	70874654
Injection site induration	1518.37	22.41	430	36000	8738	70883276
Drug dependence	1235.51	22.41	525	35905	36796	70855218
Therapeutic response shortened	769.74	22.41	278	36152	12560	70879454
Feeling abnormal	757.03	22.41	608	35822	141711	70750303
Product administered at inappropriate site	681.14	22.41	185	36245	3191	70888823
Injection site swelling	563.07	22.41	322	36108	42835	70849179
Withdrawal syndrome	524.69	22.41	256	36174	24648	70867366
Needle issue	405.79	22.41	167	36263	10748	70881266
Product dose omission issue	363.20	22.41	500	35930	216968	70675046
Insomnia	349.10	22.41	491	35939	217315	70674699
Injection site abscess	314.02	22.41	84	36346	1362	70890652
Inappropriate schedule of product administration	307.18	22.41	325	36105	107230	70784784
Drug use disorder	303.94	22.41	125	36305	8026	70883988
Alcohol use	287.73	22.41	103	36327	4524	70887490
Drug screen positive	260.84	22.41	102	36328	5738	70886276
Depression	239.70	22.41	393	36037	198581	70693433
Lack of injection site rotation	232.55	22.41	51	36379	333	70891681
Injection site discomfort	224.35	22.41	86	36344	4583	70887431
Anxiety	220.62	22.41	401	36029	219929	70672085
Injection site nodule	194.49	22.41	71	36359	3299	70888715
Injection site warmth	193.21	22.41	108	36322	13717	70878297
Inadequate analgesia	191.19	22.41	74	36356	4048	70887966
Product administration error	188.79	22.41	141	36289	29382	70862632
Acute kidney injury	171.97	22.41	21	36409	474603	70417411
Injection site erythema	156.31	22.41	190	36240	72734	70819280
Irritability	154.85	22.41	140	36290	38085	70853929
Anaemia	153.33	22.41	15	36415	403408	70488606
Alcohol poisoning	152.79	22.41	64	36366	4301	70887713
Euphoric mood	148.54	22.41	72	36358	6817	70885197
Imprisonment	138.75	22.41	36	36394	515	70891499
Lack of administration site rotation	137.83	22.41	22	36408	8	70892006
Substance abuse	135.15	22.41	76	36354	9761	70882253
Pneumonia	125.05	22.41	76	36354	596156	70295858
Dependence	123.66	22.41	46	36384	2254	70889760
Injection site cellulitis	116.69	22.41	40	36390	1542	70890472
Apathy	116.67	22.41	74	36356	11834	70880180
Headache	115.54	22.41	595	35835	579810	70312204
Drug withdrawal syndrome	115.49	22.41	111	36319	32604	70859410
Injection site pruritus	114.46	22.41	120	36310	39090	70852924
Nausea	112.39	22.41	784	35646	851304	70040710
Tremor	108.61	22.41	244	36186	155380	70736634
Feeling drunk	107.49	22.41	50	36380	4317	70887697
Malaise	101.22	22.41	465	35965	432467	70459547
Alcohol withdrawal syndrome	99.64	22.41	37	36393	1804	70890210
Condition aggravated	99.05	22.41	48	36382	427587	70464427
Dyspnoea	98.98	22.41	152	36278	769908	70122106
Decreased appetite	94.41	22.41	357	36073	304423	70587591
Fatigue	91.82	22.41	729	35701	823590	70068424
Body tinea	90.57	22.41	32	36398	1351	70890663
Thrombocytopenia	90.47	22.41	9	36421	239101	70652913
Injection site infection	90.16	22.41	35	36395	1929	70890085
General physical health deterioration	89.00	22.41	9	36421	236022	70655992
Pain	88.86	22.41	589	35841	628227	70263787
Rheumatoid arthritis	87.83	22.41	21	36409	291784	70600230
Injection site bruising	84.57	22.41	101	36329	37931	70854083
Hypotension	84.02	22.41	52	36378	404329	70487685
Anger	83.47	22.41	68	36362	16064	70875950
Wrong technique in product usage process	82.92	22.41	136	36294	68562	70823452
Atrial fibrillation	81.44	22.41	3	36427	184345	70707669
Yawning	80.89	22.41	29	36401	1278	70890736
Alcohol abuse	79.91	22.41	43	36387	5064	70886950
Emotional poverty	79.39	22.41	25	36405	735	70891279
Sepsis	78.90	22.41	15	36415	244530	70647484
Neutropenia	78.38	22.41	18	36412	257138	70634876
Mood altered	78.08	22.41	66	36364	16409	70875605
Injection site cyst	74.71	22.41	15	36415	59	70891955
Inhibitory drug interaction	73.77	22.41	37	36393	3770	70888244
Road traffic accident	73.67	22.41	90	36340	34592	70857422
Feeling of despair	73.57	22.41	33	36397	2618	70889396
Oedema peripheral	73.56	22.41	14	36416	228077	70663937
Injection site nerve damage	71.01	22.41	14	36416	49	70891965
Hypersomnia	70.55	22.41	69	36361	20695	70871319
Panic attack	70.52	22.41	71	36359	22048	70869966
Pyrexia	68.49	22.41	130	36300	606822	70285192
Disease progression	67.68	22.41	3	36427	156669	70735345
Infection susceptibility increased	67.06	22.41	32	36398	2925	70889089
Platelet count decreased	66.64	22.41	7	36423	178215	70713799
Pancytopenia	64.93	22.41	3	36427	151104	70740910
Toothache	64.03	22.41	62	36368	18368	70873646
Product preparation error	62.43	22.41	35	36395	4467	70887547
Poor quality sleep	60.66	22.41	63	36367	20286	70871728
Restlessness	59.99	22.41	90	36340	42038	70849976
Injection site irritation	59.80	22.41	31	36399	3384	70888630
Abnormal dreams	59.77	22.41	47	36383	10556	70881458
Urinary tract infection	58.94	22.41	27	36403	248742	70643272
Depressed mood	58.70	22.41	91	36339	43729	70848285
Blood creatinine increased	57.87	22.41	4	36426	142997	70749017
Malabsorption from injection site	57.87	22.41	10	36420	12	70892002
Haemoglobin decreased	57.47	22.41	17	36413	205142	70686872
Injection site haematoma	56.94	22.41	32	36398	4102	70887912
Somnolence	55.83	22.41	239	36191	215367	70676647
Renal impairment	55.53	22.41	5	36425	143932	70748082
Cardiac failure	55.34	22.41	5	36425	143536	70748478
Infusion related reaction	54.19	22.41	17	36413	197517	70694497
Necrosis ischaemic	53.68	22.41	20	36410	984	70891030
Restless legs syndrome	53.05	22.41	56	36374	18372	70873642
Gait disturbance	51.67	22.41	210	36220	184896	70707118
White blood cell count decreased	51.64	22.41	12	36418	170129	70721885
Impaired work ability	51.26	22.41	52	36378	16288	70875726
Pleural effusion	50.23	22.41	5	36425	132859	70759155
Alanine aminotransferase increased	49.83	22.41	8	36422	147472	70744542
Hospitalisation	49.41	22.41	122	36308	82446	70809568
Pulmonary embolism	49.32	22.41	10	36420	155857	70736157
Death of relative	48.98	22.41	13	36417	204	70891810
Renal failure	48.86	22.41	18	36412	189052	70702962
Stomatitis	48.16	22.41	5	36425	128506	70763508
Gastrointestinal haemorrhage	47.46	22.41	7	36423	137401	70754613
Chromaturia	46.67	22.41	59	36371	23469	70868545
Treatment failure	46.13	22.41	9	36421	144133	70747881
Drug screen false positive	45.97	22.41	18	36412	1015	70890999
Crying	45.00	22.41	55	36375	21144	70870870
Glucose tolerance impaired	44.59	22.41	33	36397	6773	70885241
Libido decreased	44.33	22.41	29	36401	4887	70887127
Drug intolerance	44.13	22.41	31	36399	225656	70666358
Hyponatraemia	43.50	22.41	14	36416	160073	70731941
Injection site inflammation	43.03	22.41	25	36405	3413	70888601
Mood swings	43.02	22.41	50	36380	18236	70873778
Suicidal ideation	42.88	22.41	104	36326	69492	70822522
Cold sweat	42.52	22.41	48	36382	16968	70875046
C-reactive protein increased	42.19	22.41	4	36426	110513	70781501
Sciatic nerve injury	42.13	22.41	14	36416	490	70891524
Detoxification	41.91	22.41	10	36420	99	70891915
Product use issue	41.88	22.41	20	36410	179917	70712097
Muscle spasms	41.58	22.41	173	36257	153873	70738141
Multiple organ dysfunction syndrome	41.24	22.41	4	36426	108511	70783503
Beta haemolytic streptococcal infection	40.73	22.41	20	36410	1947	70890067
Aspartate aminotransferase increased	40.48	22.41	8	36422	126970	70765044
Fall	40.31	22.41	107	36323	443989	70448025
Cough	39.94	22.41	66	36364	325311	70566703
Incorrect route of product administration	39.73	22.41	58	36372	26434	70865580
Maternal exposure during pregnancy	39.54	22.41	6	36424	115339	70776675
Impaired quality of life	38.75	22.41	34	36396	8882	70883132
Surgery	38.39	22.41	61	36369	29928	70862086
Cerebrovascular accident	38.19	22.41	13	36417	143457	70748557
Respiratory failure	37.40	22.41	20	36410	168715	70723299
Rash	37.16	22.41	136	36294	510426	70381588
Substance use	37.06	22.41	14	36416	716	70891298
Drug interaction	36.85	22.41	89	36341	381352	70510662
Magnesium deficiency	36.45	22.41	13	36417	564	70891450
Oedema	36.41	22.41	5	36425	103576	70788438
Pneumonia streptococcal	36.33	22.41	20	36410	2463	70889551
Food craving	36.15	22.41	17	36413	1504	70890510
Bradycardia	35.48	22.41	10	36420	124605	70767409
Influenza like illness	35.41	22.41	93	36337	65238	70826776
Abdominal pain	35.32	22.41	77	36353	342050	70549964
Therapeutic product effect incomplete	35.30	22.41	9	36421	119873	70772141
Product administered by wrong person	35.29	22.41	6	36424	6	70892008
Hyperhidrosis	34.90	22.41	147	36283	131439	70760575
Arthropathy	34.43	22.41	17	36413	150040	70741974
Toxicity to various agents	33.97	22.41	93	36337	382079	70509935
Thinking abnormal	33.59	22.41	36	36394	12015	70879999
Energy increased	33.54	22.41	20	36410	2864	70889150
Deep vein thrombosis	33.35	22.41	8	36422	111034	70780980
Injection site scar	33.22	22.41	13	36417	732	70891282
Myocardial infarction	32.99	22.41	24	36406	171621	70720393
Cardio-respiratory arrest	32.82	22.41	6	36424	100671	70791343
Decreased interest	32.75	22.41	21	36409	3420	70888594
Musculoskeletal discomfort	32.67	22.41	43	36387	17789	70874225
Hangover	32.28	22.41	17	36413	1916	70890098
Dental operation	32.16	22.41	14	36416	1034	70890980
Wheezing	32.05	22.41	5	36425	94165	70797849
Neutrophil count decreased	31.96	22.41	3	36427	83553	70808461
Dizziness	31.72	22.41	371	36059	463770	70428244
Injection site necrosis	31.72	22.41	15	36415	1344	70890670
Drug hypersensitivity	31.49	22.41	54	36376	262405	70629609
Pregnancy	31.30	22.41	49	36381	23732	70868282
Cardiac arrest	31.17	22.41	22	36408	159812	70732202
Substance use disorder	31.04	22.41	12	36418	654	70891360
Liquid product physical issue	30.48	22.41	13	36417	913	70891101
Product preparation issue	29.77	22.41	13	36417	967	70891047
Oral surgery	29.48	22.41	13	36417	990	70891024
Emotional disorder	29.18	22.41	35	36395	13191	70878823
Product use in unapproved indication	28.43	22.41	39	36391	207439	70684575
Bone density decreased	28.04	22.41	32	36398	11442	70880572
Feeling jittery	27.89	22.41	32	36398	11511	70880503
Migraine	27.79	22.41	91	36339	72147	70819867
Infection	27.51	22.41	41	36389	210744	70681270
Adiposis dolorosa	27.39	22.41	9	36421	304	70891710
Product physical consistency issue	27.16	22.41	11	36419	678	70891336
Injection site injury	27.01	22.41	11	36419	688	70891326
Exposure during pregnancy	26.98	22.41	6	36424	87711	70804303
Tachycardia	26.95	22.41	25	36405	158521	70733493
Neuropathy peripheral	26.74	22.41	16	36414	126880	70765134
Syringe issue	26.60	22.41	22	36408	5306	70886708
Rehabilitation therapy	26.56	22.41	14	36416	1581	70890433
Pruritus	26.47	22.41	90	36340	345470	70546544
Procedural pain	26.38	22.41	39	36391	17970	70874044
Leukopenia	26.11	22.41	11	36419	106549	70785465
Hypokalaemia	25.65	22.41	18	36412	131170	70760844
Mass	25.36	22.41	36	36394	15990	70876024
Stress	24.70	22.41	84	36346	67882	70824132
Abdominal pain upper	24.58	22.41	177	36253	193425	70698589
Acute myocardial infarction	24.51	22.41	4	36426	72883	70819131
Wound	24.50	22.41	10	36420	98722	70793292
Joint swelling	24.49	22.41	59	36371	253152	70638862
Acne	24.30	22.41	45	36385	24944	70867070
Intentional product use issue	24.14	22.41	16	36414	120126	70771888
Oral herpes	24.08	22.41	44	36386	24142	70867872
Caffeine consumption	24.06	22.41	4	36426	3	70892011
Heat stroke	24.01	22.41	13	36417	1550	70890464
Tachyphrenia	23.92	22.41	14	36416	1937	70890077
Hypoxia	23.91	22.41	9	36421	93335	70798679
Hepatitis C	23.65	22.41	31	36399	12776	70879238
Injection site indentation	23.58	22.41	7	36423	168	70891846
Anaphylactic reaction	23.32	22.41	5	36425	74969	70817045
Tooth disorder	23.14	22.41	43	36387	23895	70868119
Impaired healing	23.05	22.41	5	36425	74369	70817645
Osteoarthritis	22.95	22.41	5	36425	74142	70817872
Product reconstitution quality issue	22.87	22.41	7	36423	187	70891827
Constipation	22.73	22.41	61	36369	252377	70639637
Alcoholic hangover	22.64	22.41	4	36426	6	70892008
Overdose	22.60	22.41	157	36273	169588	70722426

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A08AA62	ALIMENTARY TRACT AND METABOLISM ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS Centrally acting antiobesity products
ATC	N02AA56	NERVOUS SYSTEM ANALGESICS OPIOIDS Natural opium alkaloids
ATC	N07BB04	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS DRUGS USED IN ADDICTIVE DISORDERS Drugs used in alcohol dependence
FDA MoA	N0000000154	Opioid Antagonists
MeSH PA	D000427	Alcohol Deterrents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D009292	Narcotic Antagonists
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
CHEBI has role	CHEBI:35488	central nervous system depressants
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:50137	mu-opioid receptor antagonists
CHEBI has role	CHEBI:78298	environmental contaminants
CHEBI has role	CHEBI:90755	antidote to opioid overdose
FDA EPC	N0000175691	Opioid Antagonist

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Alcoholism	indication	7200002
Severe pain	indication	76948002
Chronic pain	indication	82423001
Obesity	indication	414916001	DOID:9970
Prevention of opioid abuse	indication	426928008
Therapeutic opioid induced constipation	indication	136801000119102
Severe Pain with Opioid Tolerance	indication
Chronic Pain with Opioid Tolerance	indication
Neuropathic pain	off-label use	247398009
Suicidal thoughts	contraindication	6471006
Alcohol withdrawal delirium	contraindication	8635005
Chronic obstructive lung disease	contraindication	13645005	DOID:3083
Chronic disease of respiratory system	contraindication	17097001
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Hypercapnia	contraindication	29596007
Depressive disorder	contraindication	35489007
Acute hepatitis	contraindication	37871000
Disorder of gallbladder	contraindication	39621005	DOID:0060262
Gastrointestinal ulcer	contraindication	40845000
Hypothyroidism	contraindication	40930008	DOID:1459
Low blood pressure	contraindication	45007003
Gastrointestinal perforation	contraindication	51875005
Paralytic ileus	contraindication	55525008	DOID:8442
Acute nephropathy	contraindication	58574008
Hepatic failure	contraindication	59927004
Substance abuse	contraindication	66214007
Benign intracranial hypertension	contraindication	68267002	DOID:11459
Opioid dependence	contraindication	75544000	DOID:2559
Urethral stricture	contraindication	76618002
Decreased respiratory function	contraindication	80954004
Injury of head	contraindication	82271004
Cor pulmonale	contraindication	83291003	DOID:8515
Opioid withdrawal	contraindication	87132004
Disorder of biliary tract	contraindication	105997008	DOID:9741
Gastrointestinal obstruction	contraindication	126765001
Seizure disorder	contraindication	128613002
Drug-induced psychosis	contraindication	191483003	DOID:1742
Acute hepatic failure	contraindication	197270009
Acute pancreatitis	contraindication	197456007	DOID:2913
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Chronic diarrhea	contraindication	236071009
Benign prostatic hyperplasia	contraindication	266569009
Primary malignant neoplasm of gastrointestinal tract	contraindication	363745004
Macrocolon	contraindication	367495003
Eosinophilic asthma	contraindication	367542003	DOID:9498
Primary adrenocortical insufficiency	contraindication	373662000
Severe diarrhea	contraindication	409587002
Central nervous system depression	contraindication	418072004
Acute exacerbation of asthma	contraindication	708038006
Increased Creatine Phosphokinase	contraindication
Pain in Opioid Naive Patients	contraindication
Opioid Use Within Last 4 Hours in Narcotic-Dependent Patient	contraindication

🐶 Veterinary Drug Use

Species	Use	Relation
Cervidae	Antagonist to carfentanil citrate immobilization	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Trexonil	Wildlife Laboratories Inc.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.31	acidic
pKa2	7.66	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
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	11278544	April 21, 2024	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	7462626	July 20, 2024	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8815889	July 20, 2024	FOR EFFECT ON BLOOD GLUCOSE PARAMETERS IN PATIENTS WITH INSULIN RESISTANCE
100MG;4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
20MG;0.8MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
30MG;1.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
50MG;2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
60MG;2.4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
80MG;3.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
1.2MG;10MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
2.4MG;20MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
3.6MG;30MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
4.8MG;40MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
7.2MG;60MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
9.6MG;80MG	TROXYCA ER	PFIZER	N207621	Aug. 19, 2016	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8685443	July 3, 2025	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATMENT BY ORALLY ADMINISTERING A PLURALITY OF COMPOSITE SUBUNITS AS CLAIMED
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	9107837	June 4, 2027	USE OF NALTREXONE AND BUPROPION IN EXTENDED-RELEASE FORM FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
100MG;4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
100MG;4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
20MG;0.8MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
20MG;0.8MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
30MG;1.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
30MG;1.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
50MG;2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
50MG;2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
60MG;2.4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
60MG;2.4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
80MG;3.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	7682633	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
80MG;3.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8158156	June 19, 2027	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG TERM OPIOID TREATEMENT BY ORALLY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED.
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	10307376	Nov. 8, 2027	USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8318788	Nov. 8, 2027	USE OF NALTREXONE AND BUPROPION IN A LAYERED FORMULATION FOR CHRONIC WEIGHT MANAGEMENT FOR AFFECTING WEIGHT LOSS
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8722085	Nov. 8, 2027	USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	9125868	Nov. 8, 2027	USE OF NALTREXONE AND BUPROPION BASED ON AN ESCALATING DOSE SCHEDULE
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	11324741	May 29, 2029	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
380MG/VIAL	VIVITROL	ALKERMES	N021897	April 13, 2006	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	7919499	Oct. 15, 2029	PREVENTION OF RELAPSE TO OPIOID DEPENDENCE, FOLLOWING OPIOID DETOXIFICATION
380MG/VIAL	VIVITROL	ALKERMES	N021897	April 13, 2006	RX	FOR SUSPENSION, EXTENDED RELEASE	INTRAMUSCULAR	7919499	Oct. 15, 2029	TREATMENT OF ALCOHOL DEPENDENCE
100MG;4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
20MG;0.8MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
30MG;1.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
50MG;2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
60MG;2.4MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
80MG;3.2MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMBEDA	ALPHARMA PHARMS	N022321	Aug. 13, 2009	DISCN	CAPSULE, EXTENDED RELEASE	ORAL	8623418	Nov. 7, 2029	TREATMENT OF MODERATE TO SEVERE CHRONIC PAIN BY ADMINISTERING AN INTACT COMPOSITION AS CLAIMED
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	8916195	Feb. 2, 2030	USE OF NALTREXONE AND BUPROPION IN EXTENDED-RELEASE FORM FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	11033543	Jan. 10, 2031	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	9248123	Jan. 13, 2032	USE OF NALTREXONE AND BUPROPION FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY IN PATIENTS WITH MAJOR DEPRESSIVE DISORDER
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	10403170	June 5, 2033	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	11139056	June 5, 2033	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	9633575	June 25, 2033	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	10231964	July 2, 2034	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	10828294	July 2, 2034	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	10835527	July 2, 2034	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN	ANTAGONIST	Ki	7.99	WOMBAT-PK	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	ANTAGONIST	Ki	8.93	WOMBAT-PK	CHEMBL
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	ANTAGONIST	Ki	9.38	WOMBAT-PK	CHEMBL
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	6	DRUG MATRIX
Neuronal acetylcholine receptor subunit alpha-7	Ion channel	P36544	ACHA7_HUMAN		IC50	4.60	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.34	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_MOUSE		Ki	9.58	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_CAVPO		Ki	9.77	CHEMBL
Delta-type opioid receptor	GPCR		OPRD_MOUSE		Ki	7.91	CHEMBL
Delta-type opioid receptor	GPCR		OPRD_RAT		Ki	8.32	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_CAVPO		Ki	9.51	CHEMBL
Neuronal acetylcholine receptor subunit alpha-4	Ion channel		ACHA4_RAT		IC50	4.51	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_RAT		Ki	8.97	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_MOUSE		Ki	8.84	CHEMBL
Opioid receptor	GPCR		OPRD_RAT OPRM_RAT OPRK_RAT SGMR1_RAT		Ki	9.26	CHEMBL
Opioid receptors; mu and delta	GPCR		OPRD_MOUSE OPRM_MOUSE		Ki	9.06	CHEMBL

External reference:

ID	Source
4019853	VUID
N0000147939	NUI
D02095	KEGG_DRUG
16676-29-2	SECONDARY_CAS_RN
4018545	VANDF
4019853	VANDF
C0027360	UMLSCUI
CHEBI:7465	CHEBI
CHEMBL19019	ChEMBL_ID
CHEMBL1201149	ChEMBL_ID
D009271	MESH_DESCRIPTOR_UI
DB00704	DRUGBANK_ID
1639	IUPHAR_LIGAND_ID
3368	INN_ID
5S6W795CQM	UNII
5360515	PUBCHEM_CID
105069	RXNORM
11621	MMSL
20600	MMSL
5151	MMSL
d01406	MMSL
001615	NDDF
004662	NDDF
373546002	SNOMEDCT_US
64191009	SNOMEDCT_US
87617007	SNOMEDCT_US
850808-02-5	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NALTREXONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0406-1170	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
NALTREXONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0406-1170	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
NALTREXONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7036	TABLET, FILM COATED	50 mg	ORAL	ANDA	22 sections
EMBEDA	HUMAN PRESCRIPTION DRUG LABEL	2	16590-897	CAPSULE, EXTENDED RELEASE	0.80 mg	ORAL	NDA	14 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	16729-081	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42291-632	TABLET, FILM COATED	50 mg	ORAL	ANDA	25 sections
ContraveExtended-Release	HUMAN PRESCRIPTION DRUG LABEL	2	43063-772	TABLET, EXTENDED RELEASE	8 mg	ORAL	NDA	31 sections
ContraveExtended-Release	HUMAN PRESCRIPTION DRUG LABEL	2	43063-772	TABLET, EXTENDED RELEASE	8 mg	ORAL	NDA	31 sections
NALTREXONE HYDROCHLORIDE	Human Prescription Drug Label	1	47335-326	TABLET, FILM COATED	50 mg	ORAL	ANDA	22 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2866	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
ContraveExtended-Release	HUMAN PRESCRIPTION DRUG LABEL	2	50090-2945	TABLET, EXTENDED RELEASE	8 mg	ORAL	NDA	30 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3076	TABLET, FILM COATED	50 mg	ORAL	ANDA	28 sections
NALTREXONE HYDROCHLORIDE	Human Prescription Drug Label	1	50090-3929	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4925	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4925	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4926	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	51224-206	TABLET, FILM COATED	50 mg	ORAL	ANDA	28 sections
ContraveExtended-Release	HUMAN PRESCRIPTION DRUG LABEL	2	51267-890	TABLET, EXTENDED RELEASE	8 mg	ORAL	NDA	31 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53217-261	TABLET, FILM COATED	50 mg	ORAL	ANDA	25 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5574	TABLET, FILM COATED	50 mg	ORAL	ANDA	26 sections
Addex-1000	HUMAN PRESCRIPTION DRUG LABEL	1	57377-010	PELLET, IMPLANTABLE	1000 mg	SUBCUTANEOUS	Export only	4 sections
Addex-1000	HUMAN PRESCRIPTION DRUG LABEL	1	57377-010	PELLET, IMPLANTABLE	1000 mg	SUBCUTANEOUS	Export only	4 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62135-242	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63629-1046	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63629-1046	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63629-1047	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	63629-1047	TABLET, FILM COATED	50 mg	ORAL	ANDA	27 sections
Naltrexone Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	68071-2721	TABLET, FILM COATED	50 mg	ORAL	ANDA	23 sections
NALTREXONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	68084-291	TABLET, FILM COATED	50 mg	ORAL	ANDA	16 sections
NALTREXONE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	68084-291	TABLET, FILM COATED	50 mg	ORAL	ANDA	16 sections