Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	1.402		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	3.784		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	18.323	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	20.989	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	55.670	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	80.440	%	High	1
herg	hERG pIC50	4.993	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	6.855	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	10.023	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	67.280	%	High	1
kinase-safety-class	ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,KDR,MAP2K6,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PRKDC,STK33,SYK,TEK,TGFBR1	27
kinase-selectivity-class	AXL,EIF2AK3,GRK2,MAP2K6,MAP3K14,TEK	6
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	1.824		High	1
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	6.252		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	70.469		High	1
mppb	Mouse plasma protein binding (% unbound)	67.120		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	19.231		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	0		High	1
pppb	Pig plasma protein binding (% unbound)	76.060	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.099	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	101.158	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	83.840	%	High	1
rppb	Rat plasma protein binding (% unbound)	53.680	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	944.061	uM	High	1

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	3551.48	19.39	1243	25779	90837	90510588
Injection site mass	2956.91	19.39	779	26243	21311	90580114
Injection site pain	1589.22	19.39	849	26173	172850	90428575
Injection site induration	1138.83	19.39	314	26708	10154	90591271
Product administered at inappropriate site	485.94	19.39	132	26890	4019	90597406
Therapeutic response shortened	409.94	19.39	178	26844	22701	90578724
Needle issue	335.93	19.39	134	26888	13800	90587625
Injection site swelling	333.74	19.39	213	26809	59626	90541799
Injection site abscess	317.20	19.39	76	26946	1378	90600047
Feeling abnormal	309.42	19.39	311	26711	166924	90434501
Withdrawal syndrome	292.25	19.39	140	26882	22384	90579041
Alcohol use	202.80	19.39	55	26967	1662	90599763
Injection site warmth	191.79	19.39	97	26925	17418	90584007
Inadequate analgesia	172.65	19.39	56	26966	3168	90598257
Wrong technique in product usage process	168.08	19.39	152	26870	71419	90530006
Drug screen positive	164.24	19.39	56	26966	3701	90597724
Injection site nodule	162.20	19.39	58	26964	4415	90597010
Product dose omission issue	156.80	19.39	298	26724	291389	90310036
Body tinea	147.03	19.39	45	26977	2103	90599322
Product administration error	142.12	19.39	92	26930	26331	90575094
Inhibitory drug interaction	137.69	19.39	47	26975	3116	90598309
Injection site erythema	137.53	19.39	158	26864	98344	90503081
Injection site pruritus	129.66	19.39	116	26906	53718	90547707
Anxiety	123.56	19.39	280	26742	309492	90291933
Substance abuse	123.39	19.39	50	26972	5356	90596069
Alcohol poisoning	122.18	19.39	38	26984	1874	90599551
Injection site cellulitis	121.95	19.39	36	26986	1485	90599940
Infection susceptibility increased	120.42	19.39	45	26977	3881	90597544
Inappropriate schedule of product administration	115.76	19.39	180	26842	149753	90451672
Poor quality sleep	113.56	19.39	78	26944	24615	90576810
Insomnia	106.82	19.39	277	26745	333197	90268228
Lack of injection site rotation	106.11	19.39	29	26993	902	90600523
Injection site discomfort	102.38	19.39	45	26977	5895	90595530
Tremor	100.72	19.39	171	26851	153002	90448423
Alcoholism	99.37	19.39	32	26990	1768	90599657
Lack of administration site rotation	98.76	19.39	17	27005	46	90601379
Glucose tolerance impaired	95.61	19.39	47	26975	7938	90593487
Systemic lupus erythematosus	94.36	19.39	3	27019	361893	90239532
Impaired work ability	93.51	19.39	63	26959	19263	90582162
Impaired quality of life	92.26	19.39	67	26955	23077	90578348
Alcohol abuse	91.60	19.39	31	26991	2002	90599423
Product preparation error	90.00	19.39	49	26973	10212	90591213
Suicidal ideation	89.10	19.39	110	26912	73745	90527680
Depression	84.47	19.39	238	26784	300363	90301062
Nausea	84.42	19.39	592	26430	1109724	89491701
General physical health deterioration	80.05	19.39	7	27015	355108	90246317
Surgery	76.51	19.39	80	26942	44807	90556618
Injection site infection	76.19	19.39	28	26994	2304	90599121
Purpura	75.90	19.39	50	26972	14728	90586697
Injection site cyst	75.49	19.39	15	27007	106	90601319
Euphoric mood	74.34	19.39	35	26987	5374	90596051
Dependence	71.58	19.39	26	26996	2069	90599356
Irritability	70.74	19.39	69	26953	35593	90565832
Injection site necrosis	68.07	19.39	23	26999	1478	90599947
Alcohol withdrawal syndrome	65.98	19.39	20	27002	904	90600521
Necrosis ischaemic	64.52	19.39	20	27002	975	90600450
Injection site bruising	60.03	19.39	76	26946	52231	90549194
Imprisonment	59.97	19.39	15	27007	327	90601098
Injection site haematoma	57.80	19.39	32	26990	6890	90594535
Stomatitis	57.79	19.39	7	27015	274691	90326734
Oral herpes	57.57	19.39	60	26962	33464	90567961
Bone density decreased	57.56	19.39	45	26977	17300	90584125
Arthropathy	57.13	19.39	19	27003	366223	90235202
Product physical consistency issue	56.95	19.39	18	27004	936	90600489
Feeling drunk	56.94	19.39	28	26994	4730	90596695
Hospitalisation	56.85	19.39	121	26901	127979	90473446
Drug dependence	56.78	19.39	56	26966	29271	90572154
Pineal gland cyst	56.43	19.39	13	27009	197	90601228
Cervicogenic headache	56.31	19.39	13	27009	199	90601226
Wound	56.29	19.39	11	27011	302969	90298456
Pneumonia	54.66	19.39	66	26956	637993	89963432
Impaired healing	54.47	19.39	4	27018	234195	90367230
Somnolence	54.28	19.39	161	26861	208923	90392502
Panic attack	54.14	19.39	52	26970	26313	90575112
Drug screen false positive	53.02	19.39	17	27005	926	90600499
Substance use	52.91	19.39	18	27004	1181	90600244
Hyperlipidaemia	52.44	19.39	48	26974	22868	90578557
Skin disorder	51.39	19.39	59	26963	36647	90564778
Drug withdrawal syndrome	50.39	19.39	52	26970	28671	90572754
Infusion related reaction	50.39	19.39	31	26991	416749	90184676
Thrombocytopenia	50.20	19.39	3	27019	208722	90392703
Pneumonia streptococcal	49.54	19.39	20	27002	2121	90599304
Treatment failure	48.75	19.39	15	27007	303913	90297512
Headache	48.20	19.39	429	26593	862317	89739108
Acute kidney injury	47.60	19.39	18	27004	320369	90281056
Dyspnoea	46.71	19.39	123	26899	880832	89720593
Beta haemolytic streptococcal infection	46.40	19.39	20	27002	2499	90598926
Crying	46.02	19.39	47	26975	25598	90575827
Rheumatoid arthritis	45.19	19.39	26	26996	362588	90238837
Magnesium deficiency	44.38	19.39	14	27008	723	90600702
Fatigue	44.13	19.39	531	26491	1153492	89447933
Product physical issue	44.09	19.39	25	26997	5635	90595790
Apathy	44.09	19.39	32	26990	11008	90590417
Migraine without aura	44.05	19.39	14	27008	741	90600684
Myoglobinuria	43.16	19.39	12	27010	398	90601027
Malabsorption from injection site	42.30	19.39	8	27014	42	90601383
Irritable bowel syndrome	41.91	19.39	6	27016	207442	90393983
Muscle injury	41.12	19.39	3	27019	176651	90424774
Product use issue	40.62	19.39	24	26998	329895	90271530
Toothache	40.36	19.39	41	26981	22189	90579236
Injection site irritation	40.06	19.39	24	26998	5991	90595434
Mood altered	39.40	19.39	36	26986	17108	90584317
Psoriatic arthropathy	38.96	19.39	10	27012	228325	90373100
Neutropenia	38.09	19.39	10	27012	224894	90376531
Joint swelling	38.05	19.39	57	26965	503243	90098182
Hypersomnia	37.80	19.39	39	26983	21492	90579933
Lower respiratory tract infection	37.36	19.39	14	27008	250645	90350780
C-reactive protein increased	37.22	19.39	5	27017	181384	90420041
Blister	36.75	19.39	15	27007	254983	90346442
Detoxification	36.12	19.39	6	27016	12	90601413
Febrile neutropenia	35.98	19.39	3	27019	158346	90443079
Hyperammonaemia	35.93	19.39	23	26999	6452	90594973
Pyrexia	35.89	19.39	91	26931	660394	89941031
Therapeutic product effect decreased	35.88	19.39	19	27003	277552	90323873
Suicide attempt	35.51	19.39	73	26949	75326	90526099
Swelling	35.15	19.39	44	26978	419014	90182411
Cellulitis	34.58	19.39	81	26941	91256	90510169
Drug hypersensitivity	34.56	19.39	53	26969	463556	90137869
Drug intolerance	34.50	19.39	50	26972	447541	90153884
Pregnancy	33.97	19.39	64	26958	61983	90539442
Anger	33.88	19.39	30	26992	13690	90587735
Blood cholesterol increased	33.82	19.39	10	27012	208002	90393423
Hepatic enzyme increased	33.36	19.39	35	26987	360701	90240724
Cold sweat	33.21	19.39	30	26992	14051	90587374
Intentional overdose	33.14	19.39	81	26941	93753	90507672
Injury	32.99	19.39	9	27013	197340	90404085
Disease progression	32.90	19.39	4	27018	156611	90444814
Adiposis dolorosa	32.19	19.39	9	27013	305	90601120
Syringe issue	32.05	19.39	18	27004	3984	90597441
Coronavirus infection	31.62	19.39	20	27002	5495	90595930
Oedema peripheral	31.40	19.39	19	27003	257896	90343529
Restless legs syndrome	31.25	19.39	36	26986	22434	90578991
No adverse event	31.05	19.39	65	26957	67917	90533508
Mental disorder	30.97	19.39	43	26979	32275	90569150
Malaise	30.90	19.39	288	26734	585698	90015727
Osteoarthritis	30.76	19.39	10	27012	195720	90405705
Anaemia	30.68	19.39	36	26986	352766	90248659
Mass	30.62	19.39	30	26992	15547	90585878
Stress	30.61	19.39	72	26950	81323	90520102
Abnormal dreams	30.59	19.39	26	26996	11231	90590194
Oedema	30.16	19.39	11	27011	200284	90401141
Product reconstitution quality issue	30.09	19.39	7	27015	111	90601314
Liver injury	30.01	19.39	7	27015	170560	90430865
Injection site inflammation	29.93	19.39	18	27004	4523	90596902
Wheezing	29.74	19.39	17	27005	238063	90363362
Hypersensitivity	29.30	19.39	57	26965	454620	90146805
Treatment noncompliance	29.12	19.39	54	26968	51673	90549752
Restlessness	29.09	19.39	44	26978	35676	90565749
Hypotension	28.51	19.39	33	26989	325364	90276061
Caffeine consumption	28.47	19.39	4	27018	0	90601425
Exposure during pregnancy	28.41	19.39	18	27004	238392	90363033
Emotional distress	28.22	19.39	44	26978	36618	90564807
Intentional self-injury	28.07	19.39	39	26983	29295	90572130
Food craving	27.87	19.39	13	27009	1954	90599471
Yawning	27.85	19.39	11	27011	1101	90600324
Sleep disorder due to general medical condition, insomnia type	27.75	19.39	3	27019	128691	90472734
Product administered by wrong person	27.27	19.39	6	27016	73	90601352
Acetonaemia	27.24	19.39	8	27014	324	90601101
Dental operation	26.92	19.39	12	27010	1624	90599801
Infection	26.39	19.39	42	26980	362052	90239373
Alopecia	26.25	19.39	69	26953	495002	90106423
Drug ineffective for unapproved indication	26.21	19.39	60	26962	66584	90534841
Maternal exposure during pregnancy	26.02	19.39	42	26980	360021	90241404
Dizziness	25.92	19.39	279	26743	589005	90012420
Product preparation issue	25.69	19.39	13	27009	2333	90599092
Snoring	25.49	19.39	17	27005	5109	90596316
Diaphragmatic paralysis	25.14	19.39	9	27013	687	90600738
Myalgia	24.99	19.39	111	26911	175014	90426411
Death of relative	24.88	19.39	8	27014	440	90600985
Feeling of despair	24.55	19.39	14	27008	3190	90598235
Atrial fibrillation	24.48	19.39	5	27017	133606	90467819
Depressed mood	24.08	19.39	49	26973	50173	90551252
Wrong technique in device usage process	23.50	19.39	17	27005	5818	90595607
Inflammation	23.40	19.39	12	27010	178580	90422845
Injection site nerve damage	23.27	19.39	5	27017	54	90601371
Pain	23.15	19.39	421	26601	995920	89605505
Lung disorder	22.95	19.39	8	27014	149875	90451550
Antidepressant discontinuation syndrome	22.80	19.39	6	27016	161	90601264
Disturbance in attention	22.64	19.39	46	26976	47063	90554362
White blood cell count decreased	22.24	19.39	11	27011	167098	90434327
Condition aggravated	22.04	19.39	97	26925	595448	90005977
Influenza like illness	21.77	19.39	63	26959	80548	90520877
Rash	21.56	19.39	144	26878	795956	89805469
Liquid product physical issue	21.21	19.39	10	27012	1540	90599885
Injection site granuloma	21.17	19.39	5	27017	85	90601340
Homeless	21.06	19.39	5	27017	87	90601338
Haemoglobin decreased	21.04	19.39	11	27011	161945	90439480
Contraindicated product prescribed	20.78	19.39	10	27012	1612	90599813
Discomfort	20.77	19.39	31	26991	274304	90327121
Chromaturia	20.63	19.39	27	26995	19160	90582265
Alanine aminotransferase increased	20.53	19.39	5	27017	118333	90483092
Eosinophilic pustular folliculitis	20.49	19.39	5	27017	98	90601327
Incorrect route of product administration	20.37	19.39	46	26976	50580	90550845
Acne	20.27	19.39	33	26989	28474	90572951
Drug titration error	20.12	19.39	9	27013	1228	90600197
Peripheral swelling	20.09	19.39	60	26962	413046	90188379
Injection site scar	19.98	19.39	9	27013	1248	90600177

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	5331.16	24.00	1325	23135	14396	42582479
Injection site pain	2833.23	24.00	1107	23353	56691	42540184
Injection site mass	1518.82	24.00	434	24026	8141	42588734
Needle issue	893.72	24.00	290	24170	8437	42588438
Injection site induration	668.74	24.00	188	24272	3299	42593576
Feeling abnormal	665.12	24.00	443	24017	69343	42527532
Product administered at inappropriate site	603.05	24.00	169	24291	2929	42593946
Therapeutic response shortened	547.57	24.00	227	24233	13327	42583548
Injection site swelling	405.82	24.00	197	24263	16776	42580099
Withdrawal syndrome	369.88	24.00	177	24283	14598	42582277
Insomnia	293.65	24.00	350	24110	117903	42478972
Product dose omission issue	263.68	24.00	380	24080	153985	42442890
Alcohol use	256.60	24.00	86	24374	2762	42594113
Wrong technique in product usage process	241.09	24.00	198	24262	42437	42554438
Drug screen positive	218.19	24.00	84	24376	4047	42592828
Injection site discomfort	215.96	24.00	72	24388	2274	42594601
Product administration error	202.57	24.00	128	24332	18215	42578660
Lack of injection site rotation	185.13	24.00	46	24414	485	42596390
Injection site abscess	181.35	24.00	52	24408	980	42595895
Depression	172.36	24.00	262	24198	111101	42485774
Anxiety	162.77	24.00	264	24196	118296	42478579
Pain	151.99	24.00	392	24068	244456	42352419
Drug withdrawal syndrome	145.16	24.00	111	24349	21438	42575437
Acute kidney injury	133.22	24.00	25	24435	367312	42229563
Product preparation error	127.95	24.00	60	24400	4718	42592157
Product physical consistency issue	127.19	24.00	39	24421	934	42595941
Anaemia	126.37	24.00	9	24451	280269	42316606
Malaise	125.73	24.00	334	24126	211822	42385053
Substance abuse	123.67	24.00	72	24388	8833	42588042
Inappropriate schedule of product administration	117.44	24.00	203	24257	95699	42501176
Nausea	112.31	24.00	487	23973	396312	42200563
Alcoholism	111.26	24.00	47	24413	2883	42593992
Injection site erythema	108.25	24.00	91	24369	20104	42576771
Headache	106.35	24.00	340	24120	239029	42357846
Euphoric mood	105.33	24.00	58	24402	6395	42590480
Irritability	102.33	24.00	102	24358	28026	42568849
Imprisonment	102.29	24.00	30	24430	614	42596261
Lack of administration site rotation	98.59	24.00	20	24440	73	42596802
Inadequate analgesia	97.67	24.00	44	24416	3153	42593722
Wrong technique in device usage process	97.33	24.00	42	24418	2715	42594160
Dependence	96.03	24.00	35	24425	1445	42595430
Pneumonia	93.73	24.00	64	24396	422085	42174790
Apathy	93.62	24.00	59	24401	8347	42588528
Alcohol withdrawal syndrome	89.28	24.00	33	24427	1418	42595457
Road traffic accident	88.11	24.00	79	24381	19014	42577861
Product physical issue	85.12	24.00	40	24420	3159	42593716
Alcohol poisoning	83.94	24.00	53	24407	7521	42589354
Feeling drunk	81.69	24.00	35	24425	2223	42594652
Tremor	80.34	24.00	174	24286	96755	42500120
Injection site warmth	79.03	24.00	36	24424	2647	42594228
Injection site bruising	76.78	24.00	59	24401	11466	42585409
Injection site nodule	76.54	24.00	33	24427	2128	42594747
Thrombocytopenia	73.15	24.00	11	24449	190268	42406607
Overdose	72.89	24.00	176	24284	105088	42491787
Yawning	71.96	24.00	24	24436	758	42596117
Injection site nerve damage	71.93	24.00	13	24447	20	42596855
Condition aggravated	71.73	24.00	30	24430	260724	42336151
Restlessness	71.39	24.00	86	24374	29163	42567712
Neutropenia	69.17	24.00	15	24445	199416	42397459
Decreased appetite	68.73	24.00	255	24205	192882	42403993
Injection site cellulitis	67.55	24.00	22	24438	644	42596231
Sepsis	67.12	24.00	16	24444	199318	42397557
Hospitalisation	64.52	24.00	136	24324	74194	42522681
Pyrexia	63.45	24.00	80	24380	393962	42202913
Alcohol abuse	62.27	24.00	35	24425	4014	42592861
Dyspnoea	62.23	24.00	99	24361	442522	42154353
Emotional poverty	62.15	24.00	21	24439	691	42596184
Product administered by wrong person	60.71	24.00	12	24448	37	42596838
Injection site infection	56.27	24.00	22	24438	1104	42595771
Depressed mood	55.83	24.00	68	24392	23316	42573559
Fatigue	55.52	24.00	433	24027	435208	42161667
Suicidal ideation	55.06	24.00	99	24361	48062	42548813
Feeling of despair	54.77	24.00	22	24438	1186	42595689
Atrial fibrillation	53.79	24.00	8	24452	139585	42457290
Platelet count decreased	53.26	24.00	8	24452	138573	42458302
Pancytopenia	49.63	24.00	5	24455	117738	42479137
Hypotension	49.54	24.00	45	24415	257586	42339289
Cardiac failure	49.34	24.00	3	24457	106853	42490022
General physical health deterioration	49.23	24.00	13	24447	151233	42445642
Coronavirus infection	49.23	24.00	33	24427	5181	42591694
Anger	48.79	24.00	48	24412	12970	42583905
Mood altered	48.75	24.00	44	24416	10674	42586201
Gait disturbance	48.73	24.00	145	24315	97855	42499020
Hypersomnia	47.68	24.00	50	24410	14568	42582307
Injection site pruritus	47.56	24.00	41	24419	9364	42587511
Drug dependence	47.08	24.00	70	24390	29024	42567851
Thinking abnormal	46.26	24.00	36	24424	7125	42589750
Renal failure	45.56	24.00	13	24447	143713	42453162
Haemoglobin decreased	43.85	24.00	11	24449	132460	42464415
Panic attack	43.79	24.00	42	24418	11003	42585872
Oedema peripheral	43.71	24.00	12	24448	136064	42460811
Respiratory failure	43.67	24.00	10	24450	128122	42468753
White blood cell count decreased	43.28	24.00	6	24454	110390	42486485
Substance use	40.83	24.00	20	24440	1731	42595144
Blood creatinine increased	40.80	24.00	7	24453	109996	42486879
Injection site inflammation	39.24	24.00	17	24443	1109	42595766
Toothache	38.22	24.00	33	24427	7550	42589325
Injection site scar	38.12	24.00	13	24447	440	42596435
Mood swings	37.74	24.00	35	24425	8791	42588084
Abnormal dreams	37.71	24.00	34	24426	8237	42588638
Death of relative	37.56	24.00	7	24453	14	42596861
Abdominal pain upper	37.11	24.00	118	24342	82491	42514384
Gastrointestinal haemorrhage	36.73	24.00	6	24454	97720	42499155
Syringe issue	36.72	24.00	34	24426	8522	42588353
Heat stroke	36.25	24.00	16	24444	1092	42595783
No adverse event	35.71	24.00	73	24387	38948	42557927
Surgery	35.36	24.00	47	24413	17569	42579306
Cardiac failure congestive	35.14	24.00	4	24456	85598	42511277
Needle track marks	34.86	24.00	8	24452	58	42596817
Libido decreased	33.74	24.00	26	24434	5072	42591803
Sciatic nerve injury	33.49	24.00	9	24451	132	42596743
Muscle spasms	33.40	24.00	117	24343	85927	42510948
Restless legs syndrome	33.36	24.00	34	24426	9580	42587295
Food craving	32.39	24.00	12	24448	519	42596356
Toxicity to various agents	32.33	24.00	51	24409	229085	42367790
Injection site movement impairment	32.32	24.00	5	24455	0	42596875
Energy increased	31.76	24.00	16	24444	1471	42595404
Chromaturia	31.08	24.00	42	24418	15947	42580928
Procedural pain	30.87	24.00	26	24434	5753	42591122
Hyponatraemia	30.66	24.00	10	24450	101452	42495423
Injection site haematoma	30.58	24.00	17	24443	1908	42594967
Pleural effusion	30.39	24.00	9	24451	97157	42499718
Product use in unapproved indication	30.06	24.00	37	24423	184419	42412456
Urinary tract infection	29.62	24.00	10	24450	99274	42497601
Hangover	29.57	24.00	14	24446	1124	42595751
Product reconstitution quality issue	29.49	24.00	9	24451	212	42596663
Drug screen false positive	29.43	24.00	13	24447	889	42595986
Constipation	29.23	24.00	30	24430	162261	42434614
Emotional disorder	28.87	24.00	26	24434	6288	42590587
Mobility decreased	28.77	24.00	63	24397	35243	42561632
Influenza like illness	28.46	24.00	59	24401	31781	42565094
Hyperhidrosis	28.42	24.00	115	24345	90397	42506478
Alcoholic hangover	28.38	24.00	5	24455	6	42596869
Detoxification	28.24	24.00	7	24453	73	42596802
Drug use disorder	27.89	24.00	32	24428	10301	42586574
Hypokalaemia	27.86	24.00	4	24456	71717	42525158
Feeling jittery	27.73	24.00	22	24438	4476	42592399
Myocardial infarction	27.13	24.00	19	24441	123990	42472885
Injected limb mobility decreased	26.51	24.00	5	24455	11	42596864
Deep vein thrombosis	26.22	24.00	6	24454	76951	42519924
Sluggishness	26.06	24.00	20	24440	3876	42592999
C-reactive protein increased	26.01	24.00	3	24457	63557	42533318
Intentional product use issue	25.70	24.00	5	24455	71828	42525047
Injection site cyst	25.40	24.00	5	24455	15	42596860
Pulmonary embolism	25.29	24.00	19	24441	119593	42477282
Dizziness	24.88	24.00	235	24225	249019	42347856
Neuropathy peripheral	24.49	24.00	14	24446	101839	42495036
Abdominal pain	24.46	24.00	45	24415	190426	42406449
Somnolence	24.17	24.00	151	24309	140954	42455921
Injection site hypoaesthesia	24.06	24.00	7	24453	139	42596736
Hypoglycaemia	24.06	24.00	3	24457	59851	42537024

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	7170.32	20.21	2237	40930	86833	110459299
Injection site pain	3859.60	20.21	1707	41460	176215	110369917
Injection site mass	3844.42	20.21	1038	42129	23575	110522557
Injection site induration	1648.69	20.21	453	42714	10930	110535202
Needle issue	1029.36	20.21	350	42817	17490	110528642
Feeling abnormal	859.06	20.21	646	42521	180065	110366067
Product administered at inappropriate site	824.15	20.21	224	42943	5169	110540963
Therapeutic response shortened	683.19	20.21	298	42869	29285	110516847
Injection site swelling	646.70	20.21	363	42804	61427	110484705
Withdrawal syndrome	584.34	20.21	272	42895	31108	110515024
Injection site abscess	415.16	20.21	106	43061	1900	110544232
Alcohol use	390.59	20.21	118	43049	4004	110542128
Product dose omission issue	372.23	20.21	538	42629	321244	110224888
Insomnia	345.06	20.21	552	42615	360038	110186094
Wrong technique in product usage process	342.27	20.21	279	42888	87069	110459063
Drug screen positive	335.53	20.21	117	43050	6293	110539839
Injection site discomfort	278.69	20.21	104	43063	6803	110539329
Product administration error	260.51	20.21	169	42998	37048	110509084
Inappropriate schedule of product administration	253.64	20.21	353	42814	203284	110342848
Anxiety	237.21	20.21	457	42710	344621	110201511
Injection site nodule	232.43	20.21	82	43085	4564	110541568
Injection site warmth	231.52	20.21	120	43047	17285	110528847
Lack of injection site rotation	223.66	20.21	58	43109	1108	110545024
Depression	218.96	20.21	421	42746	316914	110229218
Inadequate analgesia	217.90	20.21	80	43087	4997	110541135
Injection site erythema	203.64	20.21	216	42951	93960	110452172
Drug withdrawal syndrome	186.87	20.21	139	43028	37915	110508217
Irritability	183.58	20.21	151	43016	47658	110498474
Injection site cellulitis	179.30	20.21	55	43112	1965	110544167
Euphoric mood	171.97	20.21	79	43088	8748	110537384
Nausea	162.62	20.21	926	42241	1234764	109311368
Product physical consistency issue	161.62	20.21	47	43120	1393	110544739
Lack of administration site rotation	157.24	20.21	30	43137	120	110546012
Product preparation error	156.26	20.21	79	43088	10800	110535332
Tremor	150.13	20.21	277	42890	201955	110344177
Substance abuse	146.14	20.21	79	43088	12384	110533748
Alcohol poisoning	142.86	20.21	70	43097	8950	110537182
Imprisonment	141.93	20.21	37	43130	722	110545410
Injection site pruritus	137.20	20.21	132	43035	51126	110495006
Suicidal ideation	133.84	20.21	174	42993	93763	110452369
Acute kidney injury	131.94	20.21	42	43125	635388	109910744
Body tinea	131.79	20.21	44	43123	2071	110544061
Alcoholism	125.07	20.21	49	43118	3658	110542474
Dependence	124.54	20.21	45	43122	2684	110543448
Pneumonia	121.11	20.21	99	43068	876615	109669517
Product physical issue	120.31	20.21	52	43115	4984	110541148
General physical health deterioration	120.17	20.21	13	43154	425282	110120850
Alcohol withdrawal syndrome	119.68	20.21	41	43126	2089	110544043
Apathy	119.18	20.21	76	43091	16163	110529969
Feeling drunk	119.11	20.21	53	43114	5447	110540685
Alcohol abuse	118.10	20.21	51	43116	4878	110541254
Headache	114.18	20.21	659	42508	881718	109664414
Anaemia	112.05	20.21	37	43130	547049	109999083
Inhibitory drug interaction	111.41	20.21	49	43118	4898	110541234
Injection site infection	108.10	20.21	40	43127	2553	110543579
Injection site bruising	107.97	20.21	116	43051	51147	110494985
Poor quality sleep	106.34	20.21	88	43079	27989	110518143
Febrile neutropenia	106.09	20.21	4	43163	316763	110229369
Panic attack	104.02	20.21	88	43079	28852	110517280
Fatigue	103.27	20.21	818	42349	1215140	109330992
Infection susceptibility increased	100.46	20.21	44	43123	4354	110541778
Anger	96.83	20.21	71	43096	18936	110527196
Thrombocytopenia	92.82	20.21	13	43154	348872	110197260
Yawning	91.71	20.21	31	43136	1516	110544616
Pain	91.37	20.21	661	42506	954294	109591838
Restlessness	87.68	20.21	109	43058	56150	110489982
Dyspnoea	87.48	20.21	189	42978	1106683	109439449
Malaise	86.23	20.21	501	42666	671318	109874814
Injection site cyst	85.17	20.21	18	43149	132	110546000
Hypersomnia	84.17	20.21	77	43090	27984	110518148
Mood altered	83.05	20.21	68	43099	21307	110524825
Neutropenia	82.74	20.21	22	43145	374598	110171534
Emotional poverty	82.56	20.21	26	43141	1014	110545118
Somnolence	82.02	20.21	279	42888	297170	110248962
Wrong technique in device usage process	81.62	20.21	44	43123	6857	110539275
Injection site nerve damage	79.98	20.21	16	43151	86	110546046
Stomatitis	79.61	20.21	7	43160	270235	110275897
Condition aggravated	77.71	20.21	104	43063	734732	109811400
Impaired work ability	76.34	20.21	71	43096	26348	110519784
Syringe issue	75.98	20.21	47	43120	9478	110536654
Injection site haematoma	75.75	20.21	38	43129	5108	110541024
Disease progression	75.61	20.21	5	43162	244029	110302103
Toothache	75.25	20.21	67	43100	23508	110522624
Pyrexia	72.88	20.21	151	43016	898114	109648018
Glucose tolerance impaired	72.09	20.21	46	43121	9791	110536341
Decreased appetite	71.82	20.21	371	42796	475475	110070657
Feeling of despair	70.89	20.21	33	43134	3765	110542367
Drug dependence	70.20	20.21	92	43075	49928	110496204
Oedema peripheral	69.42	20.21	21	43146	328639	110217493
Infusion related reaction	67.76	20.21	32	43135	381130	110165002
Sepsis	67.20	20.21	22	43145	327324	110218808
Pancytopenia	65.82	20.21	4	43163	209609	110336523
Abnormal dreams	65.69	20.21	48	43119	12732	110533400
Pericarditis	63.66	20.21	6	43161	219108	110327024
C-reactive protein increased	63.22	20.21	6	43161	217913	110328219
Restless legs syndrome	63.22	20.21	62	43105	24564	110521568
Hypotension	61.83	20.21	68	43099	523781	110022351
Impaired healing	61.03	20.21	4	43163	196713	110349419
Drug screen false positive	60.33	20.21	22	43145	1347	110544785
Injection site irritation	59.93	20.21	32	43135	4892	110541240
Malabsorption from injection site	58.70	20.21	11	43156	39	110546093
Platelet count decreased	58.06	20.21	10	43157	230433	110315699
Atrial fibrillation	57.78	20.21	10	43157	229632	110316500
Depressed mood	56.43	20.21	92	43075	60717	110485415
Treatment failure	56.25	20.21	19	43148	277215	110268917
Arthropathy	56.13	20.21	21	43146	287501	110258631
Chromaturia	55.86	20.21	63	43104	29297	110516835
Wound	55.20	20.21	12	43155	234425	110311707
Maternal exposure during pregnancy	54.33	20.21	16	43151	254867	110291265
Substance use	53.79	20.21	24	43143	2482	110543650
Rheumatoid arthritis	53.48	20.21	25	43142	299588	110246544
Necrosis ischaemic	53.13	20.21	20	43147	1339	110544793
Renal impairment	52.57	20.21	6	43161	188439	110357693
Overdose	52.32	20.21	205	42962	233589	110312543
Detoxification	52.13	20.21	11	43156	80	110546052
Surgery	51.93	20.21	72	43095	41211	110504921
Cervicogenic headache	51.72	20.21	13	43154	218	110545914
Impaired quality of life	51.39	20.21	61	43106	29956	110516176
Oedema	50.99	20.21	10	43157	209966	110336166
Pineal gland cyst	50.96	20.21	13	43154	232	110545900
Wheezing	50.90	20.21	18	43149	255212	110290920
Cold sweat	50.20	20.21	52	43115	21979	110524153
Product administered by wrong person	49.47	20.21	11	43156	105	110546027
Libido decreased	49.16	20.21	30	43137	5905	110540227
Irritable bowel syndrome	49.04	20.21	4	43163	164211	110381921
Food craving	48.89	20.21	21	43146	1982	110544150
Crying	48.77	20.21	55	43112	25573	110520559
Lower respiratory tract infection	48.73	20.21	17	43150	243089	110303043
Blood creatinine increased	48.18	20.21	7	43160	182882	110363250
Bone density decreased	48.07	20.21	44	43123	15998	110530134
White blood cell count decreased	47.80	20.21	15	43152	229375	110316757
Gait disturbance	47.66	20.21	225	42942	277983	110268149
Mood swings	46.93	20.21	51	43116	22761	110523371
Death of relative	46.47	20.21	13	43154	334	110545798
Thinking abnormal	46.29	20.21	42	43125	15098	110531034
Type 2 diabetes mellitus	46.19	20.21	7	43160	177225	110368907
Urinary tract infection	45.97	20.21	36	43131	326246	110219886
Osteoarthritis	45.83	20.21	8	43159	182615	110363517
Hyperhidrosis	45.83	20.21	169	42998	187129	110359003
Cardiac failure	45.42	20.21	9	43158	187617	110358515
Dizziness	45.09	20.21	443	42724	697750	109848382
No adverse event	44.82	20.21	93	43074	73746	110472386
Injection site necrosis	44.71	20.21	19	43148	1747	110544385
Multiple organ dysfunction syndrome	44.47	20.21	4	43163	151706	110394426
Injection site inflammation	44.41	20.21	26	43141	4745	110541387
Haemoglobin decreased	44.00	20.21	21	43146	248706	110297426
Sciatic nerve injury	43.45	20.21	15	43152	782	110545350
Joint swelling	43.45	20.21	66	43101	442779	110103353
Inflammation	43.30	20.21	11	43156	193227	110352905
Product use issue	43.15	20.21	35	43132	311660	110234472
Migraine without aura	42.55	20.21	14	43153	629	110545503
Purpura	42.47	20.21	50	43117	24338	110521794
Influenza like illness	42.02	20.21	101	43066	88311	110457821
Drug hypersensitivity	41.42	20.21	71	43096	454019	110092113
Drug intolerance	41.42	20.21	59	43108	406453	110139679
Hyperkalaemia	41.42	20.21	3	43164	135793	110410339
Product reconstitution quality issue	41.35	20.21	12	43155	353	110545779
Lung disorder	40.82	20.21	10	43157	180037	110366095
Psoriatic arthropathy	40.76	20.21	13	43154	196748	110349384
Blister	40.52	20.21	19	43148	227357	110318775
Needle track marks	40.47	20.21	9	43158	86	110546046
Pleural effusion	40.04	20.21	10	43157	177699	110368433
Oral herpes	39.63	20.21	59	43108	36021	110510111
Product preparation issue	39.38	20.21	20	43147	2759	110543373
Blood cholesterol increased	38.65	20.21	12	43155	184773	110361359
Exposure during pregnancy	38.55	20.21	9	43158	167415	110378717
Hangover	38.37	20.21	19	43148	2483	110543649
Injection site scar	38.21	20.21	15	43152	1125	110545007
Beta haemolytic streptococcal infection	38.12	20.21	20	43147	2951	110543181
Hospitalisation	37.77	20.21	132	43035	142361	110403771
Energy increased	36.80	20.21	21	43146	3653	110542479
Infection	36.47	20.21	53	43114	362147	110183985
Tachyphrenia	36.46	20.21	18	43149	2338	110543794
Hyponatraemia	36.08	20.21	20	43147	217633	110328499
Magnesium deficiency	36.03	20.21	13	43154	772	110545360
Muscle injury	35.70	20.21	6	43161	140801	110405331
Intentional product use issue	35.36	20.21	27	43140	247879	110298253
Pneumonia streptococcal	35.10	20.21	20	43147	3469	110542663
Skin disorder	34.61	20.21	61	43106	42852	110503280
Gastrointestinal haemorrhage	34.17	20.21	11	43156	165507	110380625
Musculoskeletal discomfort	34.12	20.21	44	43123	23494	110522638
Feeling jittery	33.99	20.21	35	43132	14687	110531445
Stress	33.67	20.21	104	43063	105244	110440888
Heat stroke	33.61	20.21	16	43151	1919	110544213
Increased appetite	33.49	20.21	35	43132	14942	110531190
Neutrophil count decreased	33.36	20.21	4	43163	120937	110425195
Product leakage	33.15	20.21	15	43152	1603	110544529
Drug-induced liver injury	33.04	20.21	4	43163	120063	110426069
Rash	32.94	20.21	187	42980	820777	109725355
Hepatitis C	32.91	20.21	32	43135	12541	110533591
Incorrect route of product administration	32.41	20.21	75	43092	63986	110482146
Therapeutic product effect incomplete	32.40	20.21	24	43143	223781	110322351
Alopecia	32.37	20.21	58	43109	364695	110181437
Swelling	31.90	20.21	55	43112	350986	110195146
Road traffic accident	31.56	20.21	103	43064	107295	110438837
Drug use disorder	31.38	20.21	37	43130	18037	110528095
Emotional disorder	31.29	20.21	35	43132	16125	110530007
Dental operation	31.22	20.21	14	43153	1465	110544667
Decreased interest	31.20	20.21	21	43146	4887	110541245
Mental disorder	31.10	20.21	55	43112	38736	110507396
Renal failure	30.66	20.21	26	43141	226548	110319584
Myalgia	30.48	20.21	169	42998	222212	110323920
Alanine aminotransferase increased	30.29	20.21	17	43150	183756	110362376
Liquid product physical issue	30.16	20.21	14	43153	1586	110544546
Acne	30.13	20.21	50	43117	33470	110512662
Asthma	30.03	20.21	32	43135	250259	110295873
Adiposis dolorosa	29.79	20.21	9	43158	305	110545827
Hypoglycaemia	29.32	20.21	5	43162	116099	110430033
Liver injury	29.32	20.21	11	43156	150402	110395730
Injection site discolouration	29.31	20.21	26	43141	9077	110537055
Haematochezia	29.12	20.21	5	43162	115519	110430613
Muscle spasms	29.03	20.21	197	42970	277960	110268172
Rehabilitation therapy	29.02	20.21	15	43152	2146	110543986
Injection site injury	28.35	20.21	12	43155	1092	110545040
Oral surgery	28.09	20.21	13	43154	1463	110544669
Tooth disorder	27.85	20.21	45	43122	29464	110516668
Pruritus	27.54	20.21	125	43042	581435	109964697
Mass	27.37	20.21	36	43131	19594	110526538
Dyspnoea exertional	27.36	20.21	4	43163	104056	110442076
Leukopenia	27.18	20.21	12	43155	148779	110397353
Myoglobinuria	27.12	20.21	12	43155	1216	110544916
Hyperammonaemia	27.03	20.21	30	43137	13702	110532430
Colitis	26.75	20.21	4	43163	102319	110443813
Fibromyalgia	26.50	20.21	17	43150	170892	110375240
Disturbance in attention	26.48	20.21	68	43099	61927	110484205
Abdominal pain	26.29	20.21	107	43060	512882	110033250
Pulmonary embolism	26.20	20.21	27	43140	214447	110331685
Injection site indentation	26.07	20.21	8	43159	286	110545846
Cough	25.77	20.21	93	43074	461548	110084584
Cerebrovascular accident	25.52	20.21	20	43147	181264	110364868
Nervousness	25.46	20.21	49	43118	36802	110509330
Hyperlipidaemia	25.17	20.21	48	43119	35800	110510332
Caffeine consumption	25.16	20.21	4	43163	3	110546129
Hypertension	25.14	20.21	108	43059	509976	110036156
Fall	24.97	20.21	136	43031	603346	109942786
Aspartate aminotransferase increased	24.67	20.21	16	43151	159920	110386212
Hypokalaemia	24.60	20.21	21	43146	182427	110363705
Deep vein thrombosis	24.44	20.21	12	43155	139875	110406257
Coronavirus infection	24.44	20.21	24	43143	9521	110536611
Agitation	24.35	20.21	98	43069	112953	110433179
Treatment noncompliance	24.20	20.21	73	43094	72917	110473215
Hypersensitivity	24.16	20.21	79	43088	403919	110142213
Product use in unapproved indication	23.75	20.21	92	43075	447285	110098847
Injected limb mobility decreased	23.74	20.21	5	43162	36	110546096
Metabolic acidosis	23.69	20.21	5	43162	99739	110446393
International normalised ratio increased	23.61	20.21	3	43164	86769	110459363
Abnormal behaviour	23.48	20.21	49	43118	38990	110507142
Autoscopy	23.37	20.21	6	43161	110	110546022
Emotional distress	23.23	20.21	53	43114	44794	110501338
Product compounding quality issue	23.06	20.21	5	43162	42	110546090
Injection site haemorrhage	22.92	20.21	44	43123	32984	110513148
Hypoxia	22.80	20.21	11	43156	129504	110416628
Erythema	22.71	20.21	50	43117	291397	110254735
Obesity	22.58	20.21	8	43159	113343	110432789
Homeless	22.38	20.21	6	43161	131	110546001
Respiratory failure	22.16	20.21	31	43136	215301	110330831
Alcoholic hangover	22.11	20.21	4	43163	11	110546121
Muscle tightness	22.03	20.21	28	43139	14734	110531398
Eosinophilic pneumonia	22.00	20.21	20	43147	7207	110538925
Injection site paraesthesia	21.92	20.21	9	43158	759	110545373
Epilepsy	21.88	20.21	6	43161	100203	110445929
Sleep disorder due to general medical condition, insomnia type	21.84	20.21	7	43160	105636	110440496
Injection site hypersensitivity	21.78	20.21	13	43154	2458	110543674
Tooth extraction	21.58	20.21	26	43141	12965	110533167
Peripheral swelling	21.50	20.21	83	43084	403951	110142181
Rectal haemorrhage	21.36	20.21	10	43157	119823	110426309
Hepatic enzyme increased	21.14	20.21	60	43107	320832	110225300
Acetonaemia	20.95	20.21	8	43159	557	110545575
Cardiac arrest	20.58	20.21	28	43139	196725	110349407
Feeling of body temperature change	20.57	20.21	18	43149	6170	110539962
Injection site deformation	20.55	20.21	3	43164	0	110546132
Feeling of relaxation	20.50	20.21	6	43161	182	110545950
Joint range of motion decreased	20.47	20.21	11	43156	121821	110424311
Neuropathy peripheral	20.32	20.21	24	43143	179253	110366879

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	D009292	Narcotic Antagonists
MeSH PA	D018689	Sensory System Agents
FDA EPC	N0000175691	Opioid Antagonist
CHEBI has role	CHEBI:35488	central nervous system depressant
CHEBI has role	CHEBI:35703	xenobiotic
CHEBI has role	CHEBI:50137	μ-opioid receptor antagonist
CHEBI has role	CHEBI:78298	environmental contaminant
CHEBI has role	CHEBI:90755	antidote to opioid poisoning

Related Drugs by ATC class:

A08AA Centrally acting antiobesity products 15 drugs

bupropion cathine clobenzorex dexfenfluramine diethylpropion ephedrine etilamfetamine fenfluramine lorcaserin mazindol mefenorex phentermine show all 15 →

N02AA Natural opium alkaloids 8 drugs

codeine dihydrocodeine hydromorphone morphine naloxone nicomorphine oxycodone oxymorphone

N07BB Drugs used in alcohol dependence 4 drugs

acamprosate calcium carbimide disulfiram nalmefene

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	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	12048769	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
90MG;8MG	CONTRAVE	NALPROPION	N200063	Sept. 10, 2014	RX	TABLET, EXTENDED RELEASE	ORAL	11998542	July 2, 2034	FOR CHRONIC WEIGHT MANAGEMENT FOR TREATING OVERWEIGHT OR OBESITY

Orange Book exclusivity data (new drug applications)