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	3811.77	19.15	1221	21217	57303	63409281
Injection site mass	2738.71	19.15	733	21705	17923	63448661
Injection site pain	1479.51	19.15	777	21661	129023	63337561
Injection site induration	1057.26	19.15	299	22139	8927	63457657
Therapeutic response shortened	449.10	19.15	166	22272	11722	63454862
Product administered at inappropriate site	392.07	19.15	109	22329	3040	63463544
Injection site swelling	293.09	19.15	192	22246	47380	63419204
Feeling abnormal	264.83	19.15	293	22145	148099	63318485
Withdrawal syndrome	258.89	19.15	131	22307	19866	63446718
Injection site abscess	242.70	19.15	61	22377	1137	63465447
Injection site warmth	174.90	19.15	92	22346	15103	63451481
Inadequate analgesia	164.35	19.15	55	22383	2888	63463696
Needle issue	158.17	19.15	76	22362	10300	63456284
Body tinea	141.08	19.15	44	22394	1841	63464743
Injection site nodule	139.07	19.15	52	22386	3783	63462801
Drug screen positive	138.17	19.15	51	22387	3578	63463006
Product dose omission issue	137.49	19.15	274	22164	234039	63232545
Alcohol use	132.76	19.15	43	22395	2036	63464548
Inhibitory drug interaction	130.85	19.15	46	22392	2803	63463781
Inappropriate schedule of product administration	126.02	19.15	169	22269	103796	63362788
Anxiety	124.73	19.15	252	22186	217289	63249295
Insomnia	120.62	19.15	247	22191	215005	63251579
Injection site erythema	116.10	19.15	145	22293	83029	63383555
Infection susceptibility increased	114.17	19.15	44	22394	3477	63463107
Product administration error	108.48	19.15	78	22360	22319	63444265
Substance abuse	104.19	19.15	45	22393	4762	63461822
Depression	103.64	19.15	220	22218	196272	63270312
Injection site pruritus	103.41	19.15	102	22336	45014	63421570
Lack of injection site rotation	96.26	19.15	24	22414	432	63466152
Alcohol poisoning	95.90	19.15	33	22405	1886	63464698
Poor quality sleep	95.57	19.15	69	22369	19866	63446718
Injection site discomfort	92.74	19.15	41	22397	4589	63461995
Glucose tolerance impaired	90.71	19.15	45	22393	6532	63460052
Lack of administration site rotation	89.17	19.15	14	22424	11	63466573
Injection site cellulitis	84.42	19.15	27	22411	1227	63465357
Alcoholism	74.59	19.15	27	22411	1791	63464793
Impaired quality of life	73.69	19.15	51	22387	13732	63452852
Tremor	73.07	19.15	151	22287	132088	63334496
Impaired work ability	71.50	19.15	55	22383	17420	63449164
Injection site cyst	67.92	19.15	13	22425	60	63466524
Dependence	67.50	19.15	26	22412	2051	63464533
Alcohol abuse	66.67	19.15	26	22412	2120	63464464
Acute kidney injury	65.62	19.15	8	22430	263407	63203177
Purpura	65.31	19.15	44	22394	11341	63455243
Necrosis ischaemic	64.05	19.15	20	22418	840	63465744
Wrong technique in product usage process	63.07	19.15	93	22345	62247	63404337
Injection site infection	61.99	19.15	24	22414	1919	63464665
Euphoric mood	60.26	19.15	31	22407	4856	63461728
Surgery	58.90	19.15	68	22370	35844	63430740
Irritability	58.81	19.15	64	22374	31630	63434954
Systemic lupus erythematosus	58.28	19.15	4	22434	208914	63257670
Imprisonment	58.05	19.15	14	22424	218	63466366
Hospitalisation	56.49	19.15	105	22333	84976	63381608
Oral herpes	56.13	19.15	57	22381	26017	63440567
General physical health deterioration	55.76	19.15	4	22434	201398	63265186
Bone density decreased	55.47	19.15	44	22394	14568	63452016
Injection site necrosis	55.29	19.15	20	22418	1324	63465260
Injection site bruising	53.60	19.15	70	22368	41840	63424744
Dyspnoea	52.73	19.15	96	22342	661217	62805367
Anaemia	52.62	19.15	19	22419	293411	63173173
Alcohol withdrawal syndrome	52.37	19.15	17	22421	810	63465774
Product preparation error	51.20	19.15	30	22408	6062	63460522
Pregnancy	51.00	19.15	64	22374	36772	63429812
Feeling drunk	50.28	19.15	26	22412	4116	63462468
Hyperlipidaemia	50.01	19.15	47	22391	19524	63447060
Nausea	49.96	19.15	490	21948	853981	62612603
Treatment failure	49.67	19.15	6	22432	199037	63267547
Pneumonia streptococcal	49.49	19.15	20	22418	1791	63464793
Pneumonia	47.46	19.15	55	22383	456712	63009872
Beta haemolytic streptococcal infection	47.33	19.15	20	22418	2005	63464579
Drug intolerance	45.96	19.15	26	22412	308635	63157949
Skin disorder	45.27	19.15	54	22384	29453	63437131
Magnesium deficiency	45.06	19.15	14	22424	578	63466006
Apathy	43.43	19.15	31	22407	8763	63457821
Arthropathy	42.42	19.15	15	22423	234777	63231807
Crying	41.33	19.15	46	22392	23297	63443287
Panic attack	41.26	19.15	45	22393	22286	63444298
Infusion related reaction	40.56	19.15	18	22420	245503	63221081
Product use issue	39.99	19.15	14	22424	220506	63246078
Headache	39.79	19.15	369	22069	632872	62833712
Neutropenia	39.67	19.15	7	22431	174998	63291586
Drug screen false positive	39.55	19.15	14	22424	870	63465714
Malabsorption from injection site	39.46	19.15	7	22431	19	63466565
Malaise	37.88	19.15	264	22174	415690	63050894
Drug dependence	37.88	19.15	45	22393	24438	63442146
Hypotension	37.73	19.15	25	22413	272579	63194005
Mood altered	36.89	19.15	35	22403	14708	63451876
Rheumatoid arthritis	36.89	19.15	22	22416	253797	63212787
Hyperammonaemia	36.84	19.15	23	22415	5209	63461375
Suicidal ideation	36.48	19.15	73	22365	62348	63404236
Fatigue	36.28	19.15	475	21963	887553	62579031
Injection site haematoma	35.86	19.15	25	22413	6807	63459777
Toothache	34.28	19.15	38	22400	19161	63447423
Detoxification	34.18	19.15	6	22432	15	63466569
Condition aggravated	34.15	19.15	56	22382	402161	63064423
Injection site irritation	32.84	19.15	21	22417	4957	63461627
Hypersomnia	32.69	19.15	36	22402	18019	63448565
Disease progression	32.41	19.15	3	22435	122755	63343829
Intentional overdose	32.26	19.15	77	22361	74075	63392509
Wound	32.03	19.15	9	22429	163254	63303330
Rash	31.41	19.15	98	22340	560773	62905811
Myoglobinuria	31.08	19.15	9	22429	291	63466293
Adiposis dolorosa	30.70	19.15	9	22429	304	63466280
Coronavirus infection	30.61	19.15	19	22419	4259	63462325
Stomatitis	30.47	19.15	6	22432	138719	63327865
Atrial fibrillation	30.39	19.15	3	22435	116633	63349951
Substance use	30.02	19.15	10	22428	517	63466067
Oedema peripheral	29.59	19.15	15	22423	189496	63277088
Drug withdrawal syndrome	29.58	19.15	42	22396	27152	63439432
Feeling of despair	29.31	19.15	15	22423	2324	63464260
Cellulitis	29.29	19.15	79	22359	81879	63384705
Therapeutic product effect decreased	29.12	19.15	16	22422	193171	63273413
Mass	29.03	19.15	30	22408	13970	63452614
Somnolence	28.58	19.15	132	22306	178553	63288031
Haemoglobin decreased	28.58	19.15	8	22430	145477	63321107
Restless legs syndrome	28.57	19.15	34	22404	18497	63448087
Food craving	28.28	19.15	13	22425	1593	63464991
Anger	28.22	19.15	28	22410	12428	63454156
Road traffic accident	27.87	19.15	48	22390	36584	63430000
Caffeine consumption	27.79	19.15	4	22434	0	63466584
Product preparation issue	27.33	19.15	12	22426	1320	63465264
Injection site inflammation	27.32	19.15	17	22421	3826	63462758
Dental operation	27.27	19.15	12	22426	1327	63465257
Cold sweat	27.14	19.15	27	22411	12020	63454564
Restlessness	27.02	19.15	42	22396	29411	63437173
Death of relative	26.94	19.15	8	22430	283	63466301
Decreased appetite	26.85	19.15	166	22272	250886	63215698
Urinary tract infection	26.24	19.15	33	22405	264651	63201933
Alanine aminotransferase increased	26.19	19.15	3	22435	103767	63362817
Pyrexia	25.76	19.15	83	22355	470395	62996189
Swelling	25.60	19.15	36	22402	275342	63191242
Alopecia	25.06	19.15	51	22387	337485	63129099
Incorrect route of product administration	24.98	19.15	39	22399	27413	63439171
Joint swelling	24.76	19.15	49	22389	327617	63138967
Depressed mood	24.68	19.15	48	22390	40143	63426441
Diaphragmatic paralysis	24.60	19.15	9	22429	615	63465969
Abnormal dreams	24.49	19.15	24	22414	10492	63456092
Therapeutic product effect incomplete	24.33	19.15	7	22431	125049	63341535
Oedema	24.20	19.15	3	22435	97619	63368965
Injection site nerve damage	24.11	19.15	5	22433	37	63466547
Drug hypersensitivity	23.87	19.15	46	22392	310641	63155943
Pulmonary embolism	23.70	19.15	6	22432	116678	63349906
Snoring	23.52	19.15	16	22422	4186	63462398
White blood cell count decreased	23.27	19.15	10	22428	139094	63327490
Cough	22.79	19.15	43	22395	292700	63173884
Sepsis	22.61	19.15	13	22425	153110	63313474
Antidepressant discontinuation syndrome	22.59	19.15	5	22433	52	63466532
Drug titration error	22.18	19.15	9	22429	814	63465770
Impaired healing	21.36	19.15	5	22433	102537	63364047
Wheezing	21.27	19.15	4	22434	95591	63370993
Suicide attempt	21.04	19.15	58	22380	60860	63405724
Injection site indentation	20.60	19.15	6	22432	198	63466386
Pain	20.43	19.15	371	22067	740257	62726327
Yawning	19.83	19.15	9	22429	1071	63465513
Exposure during pregnancy	19.26	19.15	16	22422	155531	63311053
Maternal exposure during pregnancy	19.25	19.15	30	22408	220032	63246552

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	5480.39	28.73	1315	19556	11718	34924342
Injection site pain	2928.74	28.73	1032	19839	37973	34898087
Injection site mass	1500.71	28.73	410	20461	6216	34929844
Injection site induration	665.56	28.73	181	20690	2679	34933381
Feeling abnormal	655.07	28.73	429	20442	62806	34873254
Therapeutic response shortened	586.92	28.73	205	20666	7199	34928861
Product administered at inappropriate site	513.18	28.73	140	20731	2096	34933964
Needle issue	425.23	28.73	154	20717	6011	34930049
Injection site swelling	395.59	28.73	174	20697	11353	34924707
Withdrawal syndrome	360.69	28.73	167	20704	12288	34923772
Product dose omission issue	302.07	28.73	364	20507	119347	34816713
Insomnia	287.00	28.73	331	20540	103576	34832484
Injection site discomfort	214.19	28.73	66	20805	1544	34934516
Alcohol use	211.31	28.73	78	20793	3210	34932850
Lack of injection site rotation	184.63	28.73	40	20831	205	34935855
Depression	175.71	28.73	251	20620	96847	34839213
Drug screen positive	173.33	28.73	71	20800	3872	34932188
Pain	162.47	28.73	369	20502	204306	34731754
Inappropriate schedule of product administration	157.62	28.73	190	20681	62106	34873954
Anxiety	156.83	28.73	241	20630	99187	34836873
Acute kidney injury	135.47	28.73	13	20858	304975	34631085
Injection site abscess	135.28	28.73	40	20831	809	34935251
Product administration error	128.86	28.73	94	20777	16250	34919810
Substance abuse	125.82	28.73	70	20801	7571	34928489
Malaise	125.66	28.73	315	20556	185510	34750550
Headache	123.23	28.73	328	20543	200307	34735753
Anaemia	121.55	28.73	4	20867	233331	34702729
Alcohol poisoning	115.98	28.73	52	20819	3541	34932519
Drug withdrawal syndrome	114.82	28.73	95	20776	19739	34916321
Imprisonment	107.40	28.73	30	20841	491	34935569
Euphoric mood	104.85	28.73	56	20815	5585	34930475
Nausea	104.80	28.73	440	20431	339468	34596592
Dependence	103.31	28.73	35	20836	1115	34934945
Apathy	99.33	28.73	58	20813	6874	34929186
Irritability	98.78	28.73	96	20775	24594	34911466
Injection site erythema	93.79	28.73	77	20794	15822	34920238
Pneumonia	89.56	28.73	53	20818	362574	34573486
Inadequate analgesia	89.52	28.73	41	20830	2934	34933126
Feeling drunk	85.78	28.73	35	20836	1888	34934172
Lack of administration site rotation	84.95	28.73	14	20857	6	34936054
Alcoholism	83.41	28.73	39	20832	2926	34933134
Yawning	79.69	28.73	24	20847	518	34935542
Road traffic accident	79.63	28.73	73	20798	17377	34918683
Injection site bruising	75.56	28.73	53	20818	8610	34927450
Tremor	74.42	28.73	157	20714	82430	34853630
Decreased appetite	73.30	28.73	242	20629	166150	34769910
Injection site warmth	70.26	28.73	31	20840	2031	34934029
Alcohol withdrawal syndrome	69.56	28.73	28	20843	1458	34934602
Injection site nodule	69.54	28.73	29	20842	1654	34934406
Injection site nerve damage	66.94	28.73	12	20859	16	34936044
Fatigue	65.62	28.73	411	20460	370242	34565818
Sepsis	64.41	28.73	11	20860	166550	34769510
Thrombocytopenia	63.41	28.73	9	20862	156238	34779822
Depressed mood	62.49	28.73	67	20804	19250	34916810
Wrong technique in product usage process	61.96	28.73	91	20780	35895	34900165
Condition aggravated	61.80	28.73	19	20852	192177	34743883
Emotional poverty	60.88	28.73	20	20851	578	34935482
Feeling of despair	58.46	28.73	22	20849	955	34935105
Atrial fibrillation	57.57	28.73	4	20867	122389	34813671
Toxicity to various agents	57.29	28.73	24	20847	200338	34735722
Hospitalisation	56.93	28.73	113	20758	56789	34879271
Dyspnoea	56.73	28.73	86	20785	376696	34559364
Pyrexia	55.11	28.73	71	20800	332942	34603118
Platelet count decreased	53.28	28.73	5	20866	119712	34816348
Neutropenia	53.16	28.73	14	20857	156764	34779296
Overdose	52.80	28.73	146	20725	90913	34845147
Drug use disorder	52.08	28.73	32	20839	4159	34931901
Mood altered	52.04	28.73	43	20828	8909	34927151
Renal failure	51.85	28.73	8	20863	130549	34805511
Product preparation error	51.67	28.73	26	20845	2291	34933769
Injection site cellulitis	49.52	28.73	17	20854	564	34935496
Restlessness	49.10	28.73	68	20803	25414	34910646
Anger	49.00	28.73	47	20824	11837	34924223
Gait disturbance	48.85	28.73	136	20735	85004	34851056
Product physical consistency issue	48.60	28.73	17	20854	597	34935463
Oedema peripheral	48.36	28.73	7	20864	119805	34816255
Injection site pruritus	47.97	28.73	37	20834	6946	34929114
Drug dependence	47.22	28.73	65	20806	24152	34911908
Respiratory failure	47.10	28.73	5	20866	108567	34827493
Coronavirus infection	46.29	28.73	30	20841	4277	34931783
Hypotension	45.90	28.73	39	20832	221610	34714450
Hypersomnia	45.45	28.73	46	20825	12361	34923699
Haemoglobin decreased	44.47	28.73	9	20862	120763	34815297
General physical health deterioration	44.34	28.73	11	20860	128258	34807802
Cardiac failure	42.85	28.73	3	20868	91245	34844815
Pancytopenia	42.27	28.73	4	20867	95153	34840907
Blood creatinine increased	42.17	28.73	4	20867	94972	34841088
Injection site inflammation	41.94	28.73	17	20854	901	34935159
Product administered by wrong person	41.81	28.73	7	20864	4	34936056
Alcohol abuse	41.61	28.73	29	20842	4661	34931399
Toothache	39.90	28.73	32	20839	6356	34929704
White blood cell count decreased	39.88	28.73	5	20866	95440	34840620
Substance use	39.26	28.73	15	20856	679	34935381
Cardiac failure congestive	38.35	28.73	3	20868	83267	34852793
Panic attack	38.31	28.73	37	20834	9395	34926665
Mood swings	37.89	28.73	34	20837	7867	34928193
Abnormal dreams	37.12	28.73	33	20838	7545	34928515
Abdominal pain upper	36.93	28.73	110	20761	71380	34864680
Injection site infection	36.82	28.73	16	20855	1010	34935050
Thinking abnormal	36.76	28.73	30	20841	6107	34929953
Death of relative	36.36	28.73	7	20864	17	34936043
Sciatic nerve injury	35.60	28.73	9	20862	98	34935962
Heat stroke	34.47	28.73	15	20856	950	34935110
Procedural pain	34.19	28.73	26	20845	4780	34931280
Surgery	33.82	28.73	42	20829	14115	34921945
Injection site scar	33.74	28.73	11	20860	310	34935750
Energy increased	33.20	28.73	16	20855	1284	34934776
Muscle spasms	32.85	28.73	109	20762	74892	34861168
Libido decreased	32.51	28.73	25	20846	4671	34931389
Product use in unapproved indication	32.09	28.73	15	20856	117484	34818576
Mobility decreased	31.52	28.73	61	20810	30067	34905993
Drug screen false positive	31.43	28.73	13	20858	726	34935334
Chromaturia	31.40	28.73	41	20830	14479	34921581
Substance use disorder	30.77	28.73	13	20858	766	34935294
Myocardial infarction	30.76	28.73	17	20854	121068	34814992
Restless legs syndrome	30.64	28.73	31	20840	8323	34927737
Influenza like illness	30.21	28.73	57	20814	27577	34908483
Alanine aminotransferase increased	29.79	28.73	6	20865	80809	34855251
Somnolence	29.54	28.73	138	20733	110978	34825082
Urinary tract infection	29.45	28.73	7	20864	84074	34851986
Feeling jittery	29.23	28.73	22	20849	3981	34932079
Bradycardia	29.08	28.73	5	20866	75413	34860647

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	7767.91	21.29	2213	34707	52572	79654896
Injection site pain	3776.48	21.29	1610	35310	128228	79579240
Injection site mass	3691.00	21.29	999	35921	19185	79688283
Injection site induration	1583.62	21.29	441	36479	9378	79698090
Feeling abnormal	778.15	21.29	620	36300	158579	79548889
Therapeutic response shortened	766.08	21.29	285	36635	15578	79691890
Product administered at inappropriate site	717.13	21.29	195	36725	3770	79703698
Injection site swelling	597.65	21.29	333	36587	46799	79660669
Withdrawal syndrome	540.71	21.29	259	36661	26595	79680873
Needle issue	509.71	21.29	201	36719	12867	79694601
Insomnia	371.94	21.29	510	36410	244660	79462808
Product dose omission issue	369.63	21.29	511	36409	247026	79460442
Injection site abscess	316.89	21.29	85	36835	1555	79705913
Alcohol use	301.52	21.29	105	36815	4726	79702742
Inappropriate schedule of product administration	290.36	21.29	333	36587	133295	79574173
Drug screen positive	281.87	21.29	106	36814	5957	79701511
Injection site discomfort	257.28	21.29	95	36825	5071	79702397
Depression	253.25	21.29	399	36521	216391	79491077
Anxiety	236.26	21.29	417	36503	248095	79459373
Lack of injection site rotation	224.89	21.29	52	36868	498	79706970
Injection site warmth	213.49	21.29	114	36806	14693	79692775
Injection site nodule	208.66	21.29	75	36845	3705	79703763
Inadequate analgesia	197.42	21.29	76	36844	4553	79702915
Product administration error	194.59	21.29	142	36778	31704	79675764
Injection site erythema	180.12	21.29	201	36719	77996	79629472
Acute kidney injury	168.93	21.29	21	36899	519383	79188085
Irritability	162.51	21.29	142	36778	41002	79666466
Lack of administration site rotation	157.17	21.29	25	36895	12	79707456
Alcohol poisoning	156.43	21.29	65	36855	4756	79702712
Euphoric mood	150.81	21.29	73	36847	7653	79699815
Anaemia	149.64	21.29	16	36904	444999	79262469
Imprisonment	141.69	21.29	36	36884	527	79706941
Substance abuse	137.71	21.29	76	36844	10450	79697018
Drug withdrawal syndrome	131.46	21.29	117	36803	34601	79672867
Injection site cellulitis	126.39	21.29	42	36878	1636	79705832
Body tinea	126.18	21.29	43	36877	1811	79705657
Injection site pruritus	124.62	21.29	124	36796	42159	79665309
Dependence	122.29	21.29	45	36875	2377	79705091
Tremor	119.12	21.29	251	36669	169832	79537636
Nausea	118.66	21.29	802	36118	956394	78751074
Apathy	117.88	21.29	74	36846	12903	79694565
Headache	117.22	21.29	604	36316	653168	79054300
Pneumonia	113.85	21.29	84	36836	660162	79047306
Feeling drunk	111.88	21.29	51	36869	4668	79702800
Inhibitory drug interaction	105.18	21.29	48	36872	4405	79703063
Wrong technique in product usage process	103.19	21.29	148	36772	73727	79633741
Malaise	102.30	21.29	473	36447	489396	79218072
Fatigue	101.13	21.29	755	36165	928972	78778496
Alcohol withdrawal syndrome	100.20	21.29	37	36883	1974	79705494
Injection site bruising	97.12	21.29	107	36813	40895	79666573
Infection susceptibility increased	97.09	21.29	43	36877	3678	79703790
Pain	96.29	21.29	605	36315	703197	79004271
Dyspnoea	95.01	21.29	157	36763	856868	78850600
Decreased appetite	94.34	21.29	360	36560	342058	79365410
Alcoholism	93.86	21.29	42	36878	3681	79703787
Poor quality sleep	92.89	21.29	80	36840	22642	79684826
General physical health deterioration	92.17	21.29	10	36910	275228	79432240
Condition aggravated	89.92	21.29	61	36859	501063	79206405
Injection site infection	89.64	21.29	35	36885	2177	79705291
Anger	88.14	21.29	69	36851	17093	79690375
Thrombocytopenia	87.90	21.29	10	36910	265249	79442219
Alcohol abuse	87.88	21.29	45	36875	5318	79702150
Injection site cyst	83.79	21.29	17	36903	81	79707387
Yawning	82.58	21.29	29	36891	1337	79706131
Product preparation error	81.80	21.29	44	36876	5749	79701719
Mood altered	81.54	21.29	67	36853	17780	79689688
Panic attack	80.72	21.29	76	36844	24140	79683328
Emotional poverty	78.14	21.29	25	36895	862	79706606
Injection site nerve damage	75.87	21.29	15	36905	61	79707407
Hypotension	75.80	21.29	56	36864	440261	79267207
Neutropenia	75.46	21.29	20	36900	287690	79419778
Atrial fibrillation	75.20	21.29	4	36916	197882	79509586
Feeling of despair	74.89	21.29	33	36887	2788	79704680
Hypersomnia	74.18	21.29	71	36849	23015	79684453
Sepsis	74.02	21.29	17	36903	269411	79438057
Oedema peripheral	73.25	21.29	14	36906	252274	79455194
Disease progression	72.40	21.29	3	36917	184359	79523109
Road traffic accident	70.75	21.29	94	36826	43570	79663898
Impaired work ability	69.91	21.29	64	36856	19617	79687851
Toothache	69.11	21.29	64	36856	19906	79687562
Glucose tolerance impaired	68.20	21.29	44	36876	8040	79699428
Platelet count decreased	65.33	21.29	7	36913	194657	79512811
Pancytopenia	64.09	21.29	3	36917	165742	79541726
Restlessness	63.23	21.29	92	36828	46400	79661068
Injection site irritation	62.68	21.29	32	36888	3758	79703710
Pyrexia	62.27	21.29	139	36781	678570	79028898
Drug screen false positive	61.19	21.29	22	36898	1087	79706381
Abnormal dreams	61.03	21.29	47	36873	11365	79696103
Drug dependence	60.34	21.29	84	36836	40685	79666783
Depressed mood	60.30	21.29	92	36828	48388	79659080
Infusion related reaction	58.50	21.29	17	36903	230220	79477248
Injection site haematoma	58.10	21.29	33	36887	4794	79702674
Malabsorption from injection site	57.63	21.29	10	36910	15	79707453
Somnolence	57.49	21.29	241	36679	238740	79468728
Urinary tract infection	56.87	21.29	28	36892	274484	79432984
Blood creatinine increased	56.30	21.29	4	36916	155053	79552415
Restless legs syndrome	55.66	21.29	57	36863	20035	79687433
Haemoglobin decreased	55.34	21.29	17	36903	222102	79485366
Gait disturbance	54.46	21.29	215	36705	207291	79500177
Necrosis ischaemic	54.10	21.29	20	36900	1070	79706398
Product physical consistency issue	53.90	21.29	19	36901	886	79706582
Impaired quality of life	53.48	21.29	48	36872	14338	79693130
Renal impairment	52.12	21.29	6	36914	157777	79549691
Suicidal ideation	51.45	21.29	111	36809	76229	79631239
Hospitalisation	51.35	21.29	126	36794	94110	79613358
Treatment failure	50.46	21.29	9	36911	170477	79536991
Stomatitis	49.95	21.29	5	36915	146752	79560716
White blood cell count decreased	49.51	21.29	13	36907	188275	79519193
Alanine aminotransferase increased	49.40	21.29	8	36912	162562	79544906
Drug use disorder	49.28	21.29	37	36883	8614	79698854
Cardiac failure	48.46	21.29	7	36913	154835	79552633
Death of relative	48.29	21.29	13	36907	241	79707227
Chromaturia	47.31	21.29	59	36861	25687	79681781
Bone density decreased	46.62	21.29	43	36877	13304	79694164
Drug intolerance	46.17	21.29	33	36887	264086	79443382
Crying	45.90	21.29	55	36865	22988	79684480
Sciatic nerve injury	45.85	21.29	15	36905	556	79706912
Renal failure	45.55	21.29	18	36902	200950	79506518
Gastrointestinal haemorrhage	45.49	21.29	7	36913	147712	79559756
Product administered by wrong person	44.99	21.29	8	36912	15	79707453
Libido decreased	44.98	21.29	29	36891	5292	79702176
Pulmonary embolism	44.85	21.29	12	36908	171642	79535826
Injection site inflammation	44.69	21.29	26	36894	3950	79703518
Cold sweat	44.62	21.29	49	36871	18650	79688818
Mood swings	43.85	21.29	50	36870	19830	79687638
Surgery	43.33	21.29	64	36856	32702	79674766
Detoxification	42.85	21.29	10	36910	100	79707368
Muscle spasms	42.61	21.29	177	36743	174553	79532915
Product use issue	42.55	21.29	22	36898	209800	79497668
C-reactive protein increased	42.38	21.29	5	36915	129022	79578446
Product preparation issue	42.36	21.29	18	36902	1392	79706076
Pleural effusion	42.27	21.29	8	36912	145254	79562214
Substance use	42.21	21.29	16	36904	918	79706550
Rheumatoid arthritis	42.06	21.29	22	36898	208448	79499020
Hyponatraemia	41.86	21.29	15	36905	177833	79529635
Beta haemolytic streptococcal infection	41.48	21.29	20	36900	2077	79705391
Oral herpes	41.27	21.29	57	36863	27397	79680071
Multiple organ dysfunction syndrome	41.18	21.29	4	36916	120242	79587226
Syringe issue	40.54	21.29	29	36891	6269	79701199
Aspartate aminotransferase increased	39.57	21.29	8	36912	138633	79568835
Food craving	39.57	21.29	18	36902	1639	79705829
Influenza like illness	39.19	21.29	96	36824	71611	79635857
Incorrect route of product administration	38.87	21.29	63	36857	34866	79672602
Therapeutic product effect incomplete	38.75	21.29	9	36911	141636	79565832
Maternal exposure during pregnancy	38.72	21.29	8	36912	136530	79570938
Oedema	38.38	21.29	5	36915	119575	79587893
Dizziness	37.36	21.29	390	36530	526051	79181417
Hyperhidrosis	37.35	21.29	154	36766	151338	79556130
Wheezing	37.15	21.29	5	36915	116659	79590809
Pericarditis	36.95	21.29	3	36917	104233	79603235
Magnesium deficiency	36.78	21.29	13	36907	611	79706857
Arthropathy	36.76	21.29	18	36902	177093	79530375
Pneumonia streptococcal	36.40	21.29	20	36900	2725	79704743
Overdose	36.18	21.29	175	36745	184031	79523437
Cough	36.17	21.29	72	36848	366717	79340751
Thinking abnormal	35.84	21.29	37	36883	13124	79694344
Injection site necrosis	35.12	21.29	16	36904	1462	79706006
Fall	34.73	21.29	113	36807	487516	79219952
Purpura	34.69	21.29	44	36876	19483	79687985
Pregnancy	33.44	21.29	51	36869	26800	79680668
Cerebrovascular accident	33.43	21.29	15	36905	155277	79552191
Rash	33.42	21.29	146	36774	578212	79129256
Decreased interest	33.37	21.29	21	36899	3676	79703792
Injection site scar	33.12	21.29	13	36907	820	79706648
Abdominal pain	33.07	21.29	83	36837	389486	79317982
Energy increased	33.07	21.29	20	36900	3262	79704206
Bradycardia	32.64	21.29	11	36909	135546	79571922
Musculoskeletal discomfort	32.58	21.29	43	36877	19792	79687676
Hangover	32.53	21.29	17	36903	2095	79705373
Deep vein thrombosis	32.45	21.29	8	36912	120911	79586557
Respiratory failure	32.40	21.29	22	36898	180889	79526579
Dental operation	32.17	21.29	14	36906	1148	79706320
Drug interaction	31.83	21.29	93	36827	415090	79292378
Substance use disorder	31.62	21.29	13	36907	925	79706543
Cardio-respiratory arrest	31.51	21.29	6	36914	108504	79598964
Skin disorder	30.90	21.29	56	36864	33887	79673581
Injection site injury	30.75	21.29	12	36908	745	79706723
Product use in unapproved indication	30.34	21.29	43	36877	250316	79457152
Heat stroke	29.98	21.29	15	36905	1688	79705780
Neutrophil count decreased	29.98	21.29	4	36916	93955	79613513
Toxicity to various agents	29.78	21.29	98	36822	421442	79286026
Emotional disorder	29.74	21.29	35	36885	14352	79693116
Myocardial infarction	29.63	21.29	25	36895	184104	79523364
Cardiac arrest	29.41	21.29	22	36898	172074	79535394
Oral surgery	29.39	21.29	13	36907	1108	79706360
Liquid product physical issue	28.82	21.29	13	36907	1161	79706307
Rehabilitation therapy	28.60	21.29	15	36905	1862	79705606
Adiposis dolorosa	28.31	21.29	9	36911	304	79707164
Injection site indentation	28.09	21.29	8	36912	184	79707284
Hepatitis C	28.02	21.29	31	36889	11894	79695574
Feeling jittery	27.82	21.29	32	36888	12809	79694659
Pruritus	27.70	21.29	92	36828	394556	79312912
Hyperlipidaemia	27.60	21.29	46	36874	26047	79681421
Acne	27.52	21.29	47	36873	27143	79680325
Product reconstitution quality issue	27.42	21.29	8	36912	201	79707267
Migraine	27.38	21.29	96	36824	87397	79620071
Exposure during pregnancy	26.54	21.29	7	36913	101125	79606343
Drug hypersensitivity	25.89	21.29	63	36857	298853	79408615
Mass	25.85	21.29	36	36884	17436	79690032
Joint swelling	25.66	21.29	60	36860	288586	79418882
Injection site discolouration	25.57	21.29	24	36896	7590	79699878
Leukopenia	25.48	21.29	11	36909	116502	79590966
Wound	25.35	21.29	11	36909	116168	79591300
Intentional product use issue	25.28	21.29	20	36900	152092	79555376
Impaired healing	25.13	21.29	5	36915	87650	79619818
Tooth disorder	24.80	21.29	44	36876	26189	79681279
Caffeine consumption	24.48	21.29	4	36916	3	79707465
Tachyphrenia	24.44	21.29	14	36906	2066	79705402
Neuropathy peripheral	24.22	21.29	18	36902	141287	79566181
Abdominal pain upper	24.22	21.29	182	36738	223637	79483831
Infection	24.19	21.29	47	36873	241665	79465803
Hypokalaemia	23.86	21.29	19	36901	144021	79563447
Hypoxia	23.79	21.29	9	36911	103234	79604234
Stress	23.76	21.29	86	36834	79526	79627942
Procedural pain	23.49	21.29	40	36880	23044	79684424
Haematochezia	23.13	21.29	6	36914	87639	79619829
Alcoholic hangover	23.05	21.29	4	36916	6	79707462
Osteoarthritis	22.99	21.29	6	36914	87303	79620165
Nervousness	22.98	21.29	49	36871	33366	79674102
Acute myocardial infarction	22.93	21.29	4	36916	77032	79630436
Injection site paraesthesia	22.45	21.29	9	36911	600	79706868
Product compounding quality issue	22.21	21.29	5	36915	42	79707426
Tachycardia	22.06	21.29	30	36890	177738	79529730
Tooth extraction	21.50	21.29	26	36894	10969	79696499
Lower respiratory tract infection	21.46	21.29	17	36903	129203	79578265
Nightmare	21.45	21.29	41	36879	25820	79681648
Colitis	21.40	21.29	4	36916	73303	79634165

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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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 TREATMENT 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
850808-02-5	SECONDARY_CAS_RN
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

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
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	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	63629-1046	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