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

Stem definition	Drug id	CAS RN
gabamimetic agents	1264	60142-96-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: gabapentin gabamox gabapen neurontin gabapentine	The mechanism by which gabapentin exerts its analgesic action is unknown, but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). In particular, gabapentin prevents pain-related responses in several models of neuropathic pain in rats or mice (e.g., spinal nerve ligation models, streptozocin-induced diabetes model, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formalin test). Gabapentin did not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase, acetic acid abdominal constriction test, footpad heat irradiation test). The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. Gabapentin exhibits antiseizure activity in mice and rats in both the maximal electroshock and pentylenetetrazole seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. Gabapentin was tested in radioligand binding assays at concentrations up to 100 uM and did not exhibit affinity for a number of other common receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine, alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2, opiate mu, delta or kappa, cannabinoid 1, voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin. In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels. Molecular weight: 171.24 Formula: C9H17NO2 CLOGP: -0.66 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 63.32 ALOGS: -1.60 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

gabapentin
gabamox
gabapen
neurontin
gabapentine

The mechanism by which gabapentin exerts its analgesic action is unknown, but in animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). In particular, gabapentin prevents pain-related responses in several models of neuropathic pain in rats or mice (e.g., spinal nerve ligation models, streptozocin-induced diabetes model, spinal cord injury model, acute herpes zoster infection model). Gabapentin also decreases pain-related responses after peripheral inflammation (carrageenan footpad test, late phase of formalin test). Gabapentin did not alter immediate pain-related behaviors (rat tail flick test, formalin footpad acute phase, acetic acid abdominal constriction test, footpad heat irradiation test). The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. Gabapentin exhibits antiseizure activity in mice and rats in both the maximal electroshock and pentylenetetrazole seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. Gabapentin was tested in radioligand binding assays at concentrations up to 100 uM and did not exhibit affinity for a number of other common receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine, alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2, opiate mu, delta or kappa, cannabinoid 1, voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites labeled with batrachotoxinin A 20-alpha-benzoate. Furthermore, gabapentin did not alter the cellular uptake of dopamine, noradrenaline, or serotonin. In vitro studies with radiolabeled gabapentin have revealed a gabapentin binding site in areas of rat brain including neocortex and hippocampus. A high-affinity binding protein in animal brain tissue has been identified as an auxiliary subunit of voltage-activated calcium channels.

Molecular weight: 171.24
Formula: C9H17NO2
CLOGP: -0.66
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 63.32
ALOGS: -1.60
ROTB: 3

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1.80	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	100 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	116.79 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.71 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.97 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.30 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 30, 1993	FDA	PFIZER PHARMS

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
Drug hypersensitivity	12337.89	22.71	3517	12628	43126	2298814
Completed suicide	5214.40	22.71	1531	14614	19503	2322437
Toxicity to various agents	3669.33	22.71	1307	14838	31447	2310493
Drug ineffective for unapproved indication	3149.74	22.71	694	15451	2272	2339668
Drug ineffective	2335.98	22.71	1339	14806	100285	2241655
Somnolence	1798.81	22.71	713	15432	22772	2319168
Drug abuse	1275.40	22.71	464	15681	11562	2330378
Dizziness	1201.33	22.71	722	15423	57943	2283997
Product use in unapproved indication	977.95	22.71	375	15770	10825	2331115
Confusional state	965.55	22.71	466	15679	23878	2318062
Cardio-respiratory arrest	954.33	22.71	349	15796	8797	2333143
Pain	891.55	22.71	611	15534	61246	2280694
Feeling abnormal	846.85	22.71	422	15723	23159	2318781
Drug intolerance	764.43	22.71	333	15812	13384	2328556
Respiratory arrest	742.77	22.71	262	15883	5916	2336024
Myoclonus	697.31	22.71	201	15944	2282	2339658
Overdose	692.84	22.71	349	15796	19558	2322382
Nausea	639.06	22.71	647	15498	111542	2230398
Condition aggravated	621.55	22.71	382	15763	31597	2310343
Cardiac arrest	615.65	22.71	294	15851	14636	2327304
Fall	578.85	22.71	423	15722	46676	2295264
Drug interaction	575.83	22.71	352	15793	28811	2313129
Tremor	541.90	22.71	300	15845	20361	2321579
Suicidal ideation	520.75	22.71	239	15906	10848	2331092
Product complaint	494.35	22.71	179	15966	4359	2337581
Fatigue	488.23	22.71	493	15652	84380	2257560
Coma	488.21	22.71	215	15930	8841	2333099
Intentional product misuse	475.38	22.71	214	15931	9275	2332665
Product use issue	466.22	22.71	228	15917	11941	2329999
Off label use	464.72	22.71	450	15695	73148	2268792
Intentional overdose	436.31	22.71	213	15932	11108	2330832
Sedation	436.07	22.71	151	15994	3211	2338729
Hallucination	434.48	22.71	192	15953	7956	2333984
Seizure	433.77	22.71	276	15869	24190	2317750
Weight increased	431.23	22.71	266	15879	22071	2319869
Rash	423.11	22.71	389	15756	59169	2282771
Accidental death	406.48	22.71	87	16058	232	2341708
Insomnia	405.89	22.71	270	15875	25517	2316423
Headache	400.11	22.71	432	15713	79747	2262193
Malaise	390.66	22.71	361	15784	55224	2286716
Depression	386.90	22.71	271	15874	27861	2314079
Poisoning	378.66	22.71	130	16015	2690	2339250
Balance disorder	377.34	22.71	184	15961	9563	2332377
Pain in extremity	368.05	22.71	311	15834	42229	2299711
Withdrawal syndrome	349.82	22.71	128	16017	3209	2338731
Vision blurred	330.33	22.71	193	15952	14475	2327465
Amnesia	326.71	22.71	152	15993	7101	2334839
Death	319.88	22.71	388	15757	81080	2260860
Anxiety	305.02	22.71	239	15906	29120	2312820
Gait disturbance	300.05	22.71	213	15932	22332	2319608
Memory impairment	298.78	22.71	173	15972	12750	2329190
Loss of consciousness	296.23	22.71	197	15948	18570	2323370
Depressed level of consciousness	292.58	22.71	143	16002	7461	2334479
Sopor	292.48	22.71	118	16027	3877	2338063
Paraesthesia	290.05	22.71	207	15938	21881	2320059
Dysarthria	286.69	22.71	133	16012	6169	2335771
Vomiting	284.07	22.71	343	15802	71259	2270681
Neuralgia	283.77	22.71	105	16040	2717	2339223
Hypoaesthesia	282.94	22.71	197	15948	20018	2321922
Acute kidney injury	281.49	22.71	224	15921	27898	2314042
Cognitive disorder	280.91	22.71	125	16020	5256	2336684
Respiratory depression	271.81	22.71	95	16050	2075	2339865
Intentional self-injury	265.06	22.71	111	16034	4016	2337924
Neuropathy peripheral	261.46	22.71	152	15993	11280	2330660
Agitation	252.90	22.71	147	15998	10904	2331036
Asthenia	251.24	22.71	263	15882	46663	2295277
Drug withdrawal syndrome	249.65	22.71	124	16021	6697	2335243
Dyskinesia	249.16	22.71	111	16034	4678	2337262
Fibromyalgia	246.82	22.71	99	16046	3201	2338739
Hallucination, visual	246.00	22.71	96	16049	2883	2339057
Suicide attempt	237.00	22.71	142	16003	11140	2330800
Lethargy	234.53	22.71	129	16016	8601	2333339
Vertigo	233.91	22.71	132	16013	9252	2332688
Speech disorder	232.09	22.71	116	16029	6348	2335592
Disorientation	221.87	22.71	112	16033	6260	2335680
Swelling	211.68	22.71	152	15993	16198	2325742
Disturbance in attention	209.94	22.71	104	16041	5581	2336359
Muscle spasms	209.72	22.71	169	15976	21397	2320543
Mental status changes	208.76	22.71	103	16042	5479	2336461
Pruritus	198.80	22.71	224	15921	43116	2298824
Muscular weakness	198.60	22.71	141	16004	14756	2327184
Dry mouth	197.34	22.71	113	16032	8140	2333800
Generalised tonic-clonic seizure	191.64	22.71	96	16049	5276	2336664
Hypotension	186.40	22.71	189	15956	32247	2309693
Arthralgia	186.04	22.71	242	15903	54043	2287897
Delirium	179.46	22.71	91	16054	5132	2336808
Oedema peripheral	179.34	22.71	161	15984	23602	2318338
Diarrhoea	178.45	22.71	298	15847	83266	2258674
Coordination abnormal	178.13	22.71	68	16077	1920	2340020
Back pain	177.41	22.71	182	15963	31477	2310463
Visual impairment	177.16	22.71	120	16025	11635	2330305
Exposure during pregnancy	174.98	22.71	163	15982	25056	2316884
Hyperhidrosis	174.00	22.71	132	16013	15290	2326650
Dysphagia	170.19	22.71	121	16024	12684	2329256
Ataxia	170.01	22.71	70	16075	2422	2339518
Peripheral swelling	169.11	22.71	137	16008	17460	2324480
Mental disorder	168.09	22.71	80	16065	3927	2338013
Sleep disorder	166.33	22.71	93	16052	6396	2335544
Weight decreased	166.04	22.71	167	15978	28204	2313736
Therapeutic product effect incomplete	164.67	22.71	110	16035	10421	2331519
Crying	164.01	22.71	81	16064	4315	2337625
Loss of personal independence in daily activities	163.64	22.71	86	16059	5225	2336715
Thinking abnormal	161.78	22.71	63	16082	1879	2340061
Constipation	160.14	22.71	145	16000	21484	2320456
Muscle twitching	159.70	22.71	69	16076	2696	2339244
Hypertension	158.17	22.71	160	15985	27201	2314739
Feeling drunk	156.28	22.71	49	16096	751	2341189
Abdominal discomfort	153.32	22.71	129	16016	17327	2324613
Mood altered	150.37	22.71	66	16079	2680	2339260
Drug dependence	150.13	22.71	68	16077	2977	2338963
Therapeutic response unexpected	149.62	22.71	73	16072	3786	2338154
Rhabdomyolysis	147.54	22.71	87	16058	6617	2335323
Euphoric mood	145.47	22.71	48	16097	873	2341067
Musculoskeletal stiffness	145.17	22.71	108	16037	12139	2329801
Exposure via ingestion	144.53	22.71	46	16099	742	2341198
Accidental overdose	141.70	22.71	71	16074	3901	2338039
Diplopia	138.71	22.71	67	16078	3398	2338542
Dyspnoea	138.46	22.71	258	15887	78475	2263465
Burning sensation	137.59	22.71	88	16057	7740	2334200
Abnormal behaviour	132.36	22.71	72	16073	4688	2337252
Encephalopathy	129.64	22.71	70	16075	4491	2337449
Swelling face	129.10	22.71	91	16054	9402	2332538
Mental impairment	128.29	22.71	57	16088	2383	2339557
Oedema	125.46	22.71	92	16053	10111	2331829
Anaphylactic reaction	122.71	22.71	89	16056	9616	2332324
Nightmare	119.98	22.71	62	16083	3635	2338305
Unresponsive to stimuli	117.15	22.71	67	16078	4809	2337131
Abdominal pain upper	116.42	22.71	123	16022	21977	2319963
Presbyacusis	115.22	22.71	23	16122	37	2341903
Joint swelling	113.28	22.71	107	16038	16712	2325228
Dry eye	113.22	22.71	61	16084	3895	2338045
Psychotic disorder	111.63	22.71	64	16081	4615	2337325
Gait inability	109.76	22.71	69	16076	5886	2336054
Nervous system disorder	109.09	22.71	55	16090	3061	2338879
Prescription drug used without a prescription	108.92	22.71	28	16117	197	2341743
Impaired driving ability	108.61	22.71	40	16105	1019	2340921
Psychomotor hyperactivity	107.83	22.71	47	16098	1875	2340065
Neck pain	107.48	22.71	75	16070	7622	2334318
Myalgia	107.46	22.71	121	16024	23212	2318728
Impaired work ability	107.24	22.71	46	16099	1764	2340176
Irritability	104.94	22.71	69	16076	6358	2335582
Renal impairment	104.20	22.71	82	16063	10010	2331930
Head injury	103.85	22.71	58	16087	3976	2337964
Catatonia	101.77	22.71	36	16109	814	2341126
Urticaria	100.28	22.71	119	16026	24142	2317798
Alanine aminotransferase increased	99.74	22.71	92	16053	13940	2328000
Hypersensitivity	99.63	22.71	117	16028	23476	2318464
Hypoglycaemia	99.28	22.71	74	16071	8333	2333607
Swollen tongue	98.70	22.71	62	16083	5281	2336659
Myocardial stunning	97.44	22.71	19	16126	25	2341915
Movement disorder	96.32	22.71	49	16096	2779	2339161
Medication error	95.69	22.71	64	16081	6067	2335873
Osteoarthritis	95.39	22.71	67	16078	6879	2335061
Pleural thickening	95.04	22.71	21	16124	68	2341872
Syncope	92.56	22.71	96	16049	16779	2325161
Therapeutic product effect decreased	91.12	22.71	78	16067	10711	2331229
Blood magnesium increased	91.11	22.71	23	16122	149	2341791
Gastrointestinal disorder	91.08	22.71	72	16073	8845	2333095
Respiratory failure	89.05	22.71	85	16060	13443	2328497
Nerve injury	88.95	22.71	35	16110	1073	2340867
Dysstasia	88.83	22.71	47	16098	2892	2339048
Abdominal pain	88.80	22.71	134	16011	34240	2307700
Nervousness	87.87	22.71	57	16088	5132	2336808
Pleural fibrosis	87.55	22.71	23	16122	178	2341762
Metabolic acidosis	87.39	22.71	60	16085	5938	2336002
Aggression	87.06	22.71	55	16090	4731	2337209
Blood potassium increased	86.49	22.71	42	16103	2154	2339786
Serotonin syndrome	85.99	22.71	49	16096	3491	2338449
Tachycardia	85.80	22.71	91	16054	16318	2325622
Contusion	85.29	22.71	81	16064	12729	2329211
Restless legs syndrome	85.15	22.71	42	16103	2229	2339711
Migraine	83.87	22.71	74	16071	10579	2331361
Epilepsy	83.60	22.71	53	16092	4586	2337354
Hypersomnia	83.51	22.71	42	16103	2324	2339616
Alopecia	82.91	22.71	103	16042	21898	2320042
Body height decreased	81.72	22.71	34	16111	1207	2340733
Treatment failure	81.65	22.71	62	16083	7177	2334763
Epigastric discomfort	80.03	22.71	27	16118	527	2341413
Renal failure	79.90	22.71	90	16055	17259	2324681
Emotional disorder	77.88	22.71	39	16106	2138	2339802
Deafness neurosensory	76.71	22.71	26	16119	515	2341425
Maternal exposure during pregnancy	75.18	22.71	81	16064	14782	2327158
Restlessness	74.51	22.71	49	16096	4514	2337426
Drug effective for unapproved indication	73.59	22.71	21	16124	228	2341712
Herpes zoster	73.47	22.71	66	16079	9659	2332281
Blood cholesterol increased	72.99	22.71	51	16094	5190	2336750
Intentional product use issue	72.10	22.71	44	16101	3558	2338382
Limb discomfort	72.09	22.71	43	16102	3336	2338604
Arthritis	72.07	22.71	66	16079	9902	2332038
Pyrexia	71.51	22.71	157	15988	53551	2288389
Abortion spontaneous	71.05	22.71	75	16070	13370	2328570
Blood creatinine increased	70.87	22.71	67	16078	10466	2331474
Neuroleptic malignant syndrome	70.71	22.71	36	16109	2044	2339896
Hyperreflexia	70.71	22.71	28	16117	873	2341067
Status epilepticus	70.31	22.71	38	16107	2440	2339500
Osteopenia	70.21	22.71	35	16110	1900	2340040
Drug screen positive	70.14	22.71	28	16117	892	2341048
Asterixis	69.85	22.71	20	16125	220	2341720
Poisoning deliberate	69.67	22.71	30	16115	1161	2340779
Hepatitis	68.67	22.71	53	16092	6284	2335656
Mood swings	68.18	22.71	41	16104	3228	2338712
Hypermobility syndrome	67.85	22.71	14	16131	29	2341911
Tinnitus	66.96	22.71	48	16097	5087	2336853
Aphasia	66.41	22.71	47	16098	4881	2337059
Altered state of consciousness	64.36	22.71	42	16103	3818	2338122
Wound	64.22	22.71	37	16108	2691	2339249
Urinary retention	63.85	22.71	41	16104	3626	2338314
Anorgasmia	62.54	22.71	18	16127	202	2341738
Drug diversion	62.54	22.71	18	16127	202	2341738
Aspartate aminotransferase increased	62.49	22.71	68	16077	12544	2329396
Electroencephalogram abnormal	62.46	22.71	25	16120	802	2341138
Myotonia	62.04	22.71	13	16132	30	2341910
Psychotic disorder due to a general medical condition	61.75	22.71	13	16132	31	2341909
Anger	61.68	22.71	35	16110	2472	2339468
Cyst	61.32	22.71	30	16115	1563	2340377
Hyponatraemia	61.12	22.71	69	16076	13256	2328684
Drug level increased	60.85	22.71	36	16109	2751	2339189
Dehydration	60.52	22.71	89	16056	22206	2319734
Oliguria	59.67	22.71	28	16117	1329	2340611
Infection	59.41	22.71	79	16066	17950	2323990
Congenital thrombocytopenia	58.71	22.71	10	16135	1	2341939
Blood alkaline phosphatase increased	58.70	22.71	49	16096	6496	2335444
Neurotoxicity	58.59	22.71	32	16113	2098	2339842
Urinary incontinence	58.50	22.71	41	16104	4192	2337748
Inadequate analgesia	58.01	22.71	22	16123	609	2341331
Asthma	57.80	22.71	62	16083	11252	2330688
Treatment noncompliance	57.17	22.71	45	16100	5489	2336451
Eosinophilic colitis	56.69	22.71	13	16132	52	2341888
Purpura senile	56.62	22.71	11	16134	14	2341926
Glaucoma	56.32	22.71	31	16114	2064	2339876
Dysphemia	56.09	22.71	20	16125	463	2341477
Decreased appetite	56.06	22.71	99	16046	28792	2313148
Blood creatine phosphokinase increased	55.74	22.71	43	16102	5093	2336847
Road traffic accident	55.55	22.71	40	16105	4268	2337672
Somatic symptom disorder	55.50	22.71	18	16127	309	2341631
Joint injury	54.73	22.71	32	16113	2392	2339548
Hyperkalaemia	54.68	22.71	45	16100	5848	2336092
Mania	54.53	22.71	32	16113	2408	2339532
Bradypnoea	54.32	22.71	19	16126	415	2341525
Delusion	53.98	22.71	30	16115	2035	2339905
Sacroiliitis	53.82	22.71	17	16128	267	2341673
Blood pressure increased	53.78	22.71	73	16072	16913	2325027
Skin lesion	53.34	22.71	38	16107	3987	2337953
Sciatica	53.18	22.71	30	16115	2095	2339845
Sleep apnoea syndrome	53.17	22.71	30	16115	2096	2339844
Depressed mood	53.12	22.71	42	16103	5156	2336784
Hallucination, auditory	52.31	22.71	30	16115	2162	2339778
Bedridden	52.24	22.71	26	16119	1406	2340534
Sensory loss	51.52	22.71	24	16121	1120	2340820
Chest pain	51.50	22.71	94	16051	28043	2313897
Tooth loss	50.68	22.71	25	16120	1326	2340614
Gamma-glutamyltransferase increased	50.62	22.71	42	16103	5520	2336420
Intervertebral disc protrusion	50.48	22.71	33	16112	3008	2338932
Blood glucose increased	50.26	22.71	60	16085	12230	2329710
Tooth disorder	50.25	22.71	37	16108	4086	2337854
Sensory disturbance	49.75	22.71	31	16114	2601	2339339
Panic attack	49.34	22.71	36	16109	3920	2338020
Incorrect dose administered	49.30	22.71	53	16092	9642	2332298
Diabetic neuropathy	49.18	22.71	18	16127	450	2341490
Heart rate increased	48.38	22.71	56	16089	11049	2330891
Sedation complication	48.17	22.71	14	16131	163	2341777
Wrong patient received product	48.06	22.71	15	16130	226	2341714
Hypokinesia	47.27	22.71	26	16119	1728	2340212
Pneumonia	47.24	22.71	127	16018	49169	2292771
Flatulence	47.18	22.71	37	16108	4488	2337452
Toxic epidermal necrolysis	47.09	22.71	32	16113	3112	2338828
Discomfort	47.04	22.71	39	16106	5120	2336820
Pneumonia aspiration	46.55	22.71	34	16111	3708	2338232
Cough	46.52	22.71	99	16046	33018	2308922
Hypoxia	46.51	22.71	42	16103	6185	2335755
Bradyphrenia	46.24	22.71	22	16123	1077	2340863
Electrocardiogram QRS complex prolonged	46.19	22.71	22	16123	1080	2340860
Dissociation	45.86	22.71	17	16128	441	2341499
Ankylosing spondylitis	45.54	22.71	19	16126	679	2341261
Tarsal tunnel syndrome	45.11	22.71	10	16135	33	2341907
Dystonia	44.42	22.71	27	16118	2167	2339773
Quality of life decreased	44.15	22.71	19	16126	734	2341206
Apnoea	43.87	22.71	23	16122	1388	2340552
Drug eruption	43.72	22.71	31	16114	3228	2338712
Diabetes mellitus	43.53	22.71	44	16101	7451	2334489
Sinus tachycardia	43.16	22.71	31	16114	3294	2338646
Oxygen saturation decreased	43.08	22.71	44	16101	7542	2334398
Blood sodium decreased	42.77	22.71	30	16115	3070	2338870
Skin abrasion	42.75	22.71	21	16124	1104	2340836
Focal dyscognitive seizures	42.75	22.71	17	16128	536	2341404
Eye movement disorder	42.71	22.71	21	16124	1106	2340834
Anion gap	42.67	22.71	12	16133	123	2341817
Urinary tract infection	42.62	22.71	90	16055	29852	2312088
Fear	42.48	22.71	28	16117	2588	2339352
Foetal exposure during pregnancy	42.36	22.71	37	16108	5215	2336725
Neutropenia	41.99	22.71	74	16071	21474	2320466
Affective disorder	41.90	22.71	19	16126	833	2341107
Product prescribing error	41.67	22.71	29	16116	2931	2339009
Adverse drug reaction	41.61	22.71	45	16100	8238	2333702
Bradycardia	41.26	22.71	49	16096	9932	2332008
Hypertonia	40.97	22.71	21	16124	1209	2340731
Anuria	40.97	22.71	24	16121	1800	2340140
Dysgeusia	40.83	22.71	45	16100	8414	2333526
Joint range of motion decreased	40.58	22.71	24	16121	1832	2340108
Brain injury	40.52	22.71	19	16126	900	2341040
Conversion disorder	39.94	22.71	15	16130	404	2341536
Trigeminal neuralgia	39.91	22.71	17	16128	640	2341300
Psychomotor skills impaired	39.83	22.71	15	16130	407	2341533
Rash pruritic	39.73	22.71	42	16103	7493	2334447
Premature delivery	39.63	22.71	29	16116	3171	2338769
Bipolar disorder	39.60	22.71	21	16124	1297	2340643
Pharyngeal oedema	39.56	22.71	30	16115	3463	2338477
Unevaluable event	39.00	22.71	45	16100	8846	2333094
Leukopenia	38.80	22.71	48	16097	10148	2331792
Electrocardiogram QT prolonged	38.47	22.71	42	16103	7772	2334168
Hostility	38.37	22.71	13	16132	257	2341683
Snoring	38.26	22.71	15	16130	455	2341485
Haemodialysis	38.17	22.71	24	16121	2045	2339895
Visual acuity reduced	38.13	22.71	35	16110	5263	2336677
Paralysis	38.12	22.71	23	16122	1821	2340119
Drug titration error	37.93	22.71	11	16134	127	2341813
Cholestasis	37.88	22.71	30	16115	3691	2338249
Increased appetite	37.86	22.71	21	16124	1419	2340521
Hepatocellular injury	37.69	22.71	31	16114	4024	2337916
Therapy non-responder	37.21	22.71	42	16103	8062	2333878
Visual field defect	36.85	22.71	21	16124	1495	2340445
Palpitations	36.67	22.71	60	16085	16396	2325544
Autonomic nervous system imbalance	36.40	22.71	14	16131	403	2341537
Stevens-Johnson syndrome	36.36	22.71	31	16114	4228	2337712
General physical health deterioration	36.28	22.71	55	16090	14084	2327856
Angioedema	36.00	22.71	42	16103	8354	2333586
Photophobia	35.96	22.71	24	16121	2265	2339675
Foot fracture	35.78	22.71	26	16119	2812	2339128
Inappropriate antidiuretic hormone secretion	35.77	22.71	24	16121	2285	2339655
Communication disorder	35.76	22.71	14	16131	423	2341517
Complex regional pain syndrome	35.75	22.71	13	16132	319	2341621
Spinal disorder	35.57	22.71	19	16126	1191	2340749
Lower limb fracture	35.56	22.71	23	16122	2058	2339882
Product substitution issue	35.53	22.71	33	16112	5036	2336904
Pollakiuria	35.51	22.71	29	16116	3727	2338213
Disease recurrence	35.51	22.71	28	16117	3423	2338517
Bone cyst	35.17	22.71	11	16134	167	2341773
Body dysmorphic disorder	35.09	22.71	8	16137	31	2341909
Rheumatoid arthritis	35.08	22.71	64	16081	19076	2322864
Walking aid user	34.77	22.71	16	16129	726	2341214
Eosinophilia	34.73	22.71	26	16119	2944	2338996
Middle insomnia	34.67	22.71	20	16125	1457	2340483
Incoherent	34.53	22.71	17	16128	898	2341042
Accidental poisoning	34.52	22.71	10	16135	115	2341825
Concussion	34.49	22.71	17	16128	900	2341040
Postmortem blood drug level abnormal	34.43	22.71	7	16138	13	2341927
Abnormal dreams	34.41	22.71	24	16121	2434	2339506
Poor quality sleep	34.26	22.71	22	16123	1945	2339995
Chorea	34.22	22.71	12	16133	264	2341676
Hypoxic-ischaemic encephalopathy	34.16	22.71	16	16129	756	2341184
Vertigo positional	34.14	22.71	13	16132	364	2341576
Personality change	34.07	22.71	17	16128	924	2341016
Facial pain	33.95	22.71	19	16126	1306	2340634
Stress	33.64	22.71	37	16108	6901	2335039
Economic problem	33.64	22.71	13	16132	379	2341561
Nystagmus	33.57	22.71	18	16127	1137	2340803
Pulmonary oedema	33.53	22.71	38	16107	7325	2334615
Abdominal distension	33.33	22.71	45	16100	10366	2331574
Exostosis	33.26	22.71	19	16126	1359	2340581
Hepatotoxicity	33.17	22.71	27	16118	3454	2338486
Human epidermal growth factor receptor decreased	33.16	22.71	7	16138	17	2341923
Tooth injury	32.98	22.71	11	16134	207	2341733
Dental caries	32.88	22.71	21	16124	1839	2340101
Transient ischaemic attack	32.73	22.71	34	16111	5944	2335996
Blister	32.64	22.71	36	16109	6735	2335205
Musculoskeletal discomfort	32.58	22.71	22	16123	2116	2339824
Full blood count abnormal	32.56	22.71	12	16133	306	2341634
Vestibular disorder	32.40	22.71	11	16134	219	2341721
Formication	32.36	22.71	16	16129	853	2341087
Blindness	32.26	22.71	27	16118	3591	2338349
Myoclonic epilepsy	32.03	22.71	11	16134	227	2341713
Menopause	31.95	22.71	12	16133	323	2341617
Resorption bone increased	31.85	22.71	11	16134	231	2341709
Petit mal epilepsy	31.84	22.71	15	16130	718	2341222
Epileptic encephalopathy	31.84	22.71	7	16138	22	2341918
Osteosclerosis	31.54	22.71	12	16133	335	2341605
Ankle fracture	31.43	22.71	22	16123	2243	2339697
Injury	31.06	22.71	33	16112	5921	2336019
Anion gap abnormal	31.03	22.71	8	16137	57	2341883
Apathy	30.98	22.71	18	16127	1329	2340611
Blood disorder	30.85	22.71	16	16129	944	2340996
Eczema	30.83	22.71	25	16120	3180	2338760
Malignant polyp	30.72	22.71	6	16139	8	2341932
Persecutory delusion	30.66	22.71	13	16132	484	2341456
Intervertebral disc degeneration	30.53	22.71	19	16126	1590	2340350
Mouth ulceration	30.42	22.71	27	16118	3885	2338055
Myocardial infarction	30.41	22.71	60	16085	18953	2322987
Back disorder	30.39	22.71	19	16126	1603	2340337
Lennox-Gastaut syndrome	30.33	22.71	7	16138	29	2341911
Gastrooesophageal reflux disease	30.17	22.71	40	16105	9055	2332885
Gingivitis	30.09	22.71	18	16127	1403	2340537
Atonic urinary bladder	29.95	22.71	7	16138	31	2341909
Stereotypy	29.85	22.71	9	16136	120	2341820
Liver function test abnormal	29.69	22.71	36	16109	7454	2334486
Hyperaesthesia	29.63	22.71	17	16128	1226	2340714
Mobility decreased	29.61	22.71	39	16106	8771	2333169
Glossodynia	29.61	22.71	20	16125	1925	2340015
Surgery	29.44	22.71	31	16114	5504	2336436
Toxic skin eruption	29.17	22.71	21	16124	2239	2339701
Cerebrovascular accident	29.08	22.71	61	16084	20125	2321815
Somnambulism	29.08	22.71	15	16130	875	2341065
Adverse event	29.04	22.71	36	16109	7623	2334317
Agranulocytosis	29.02	22.71	25	16120	3457	2338483
Brain death	28.94	22.71	13	16132	557	2341383
Eye pain	28.92	22.71	29	16116	4862	2337078
Cerebral vasoconstriction	28.85	22.71	11	16134	309	2341631
Arthropathy	28.73	22.71	35	16110	7281	2334659
Toe operation	28.57	22.71	9	16136	140	2341800
Toxicologic test abnormal	28.45	22.71	9	16136	142	2341798
Drug withdrawal syndrome neonatal	28.34	22.71	12	16133	445	2341495
Post procedural complication	28.33	22.71	23	16122	2931	2339009
Muscle rigidity	28.28	22.71	19	16126	1812	2340128
Product administration error	28.28	22.71	26	16119	3917	2338023
Paranoia	28.16	22.71	20	16125	2087	2339853
Haematuria	28.14	22.71	27	16118	4291	2337649
Pregnancy	27.98	22.71	36	16109	7913	2334027
Deafness	27.97	22.71	22	16123	2679	2339261
Homicidal ideation	27.87	22.71	12	16133	464	2341476
Hepatic enzyme increased	27.84	22.71	40	16105	9762	2332178
Hyperlipasaemia	27.77	22.71	8	16137	90	2341850
Scar	27.49	22.71	19	16126	1898	2340042
Lip swelling	27.44	22.71	28	16117	4793	2337147
Feeling jittery	27.36	22.71	19	16126	1913	2340027
Thirst	27.18	22.71	18	16127	1676	2340264
Incontinence	27.16	22.71	17	16128	1437	2340503
Blood potassium decreased	26.96	22.71	29	16116	5276	2336664
Major depression	26.87	22.71	15	16130	1026	2340914
Sepsis	26.79	22.71	56	16089	18432	2323508
Blood pressure decreased	26.68	22.71	38	16107	9198	2332742
Grip strength decreased	26.66	22.71	15	16130	1042	2340898
Muscle contractions involuntary	26.59	22.71	12	16133	520	2341420
Alcohol interaction	26.56	22.71	10	16135	271	2341669
Dysgraphia	26.38	22.71	12	16133	530	2341410
Strabismus	26.34	22.71	11	16134	394	2341546
Acute lung injury	26.33	22.71	9	16136	183	2341757
Face oedema	26.32	22.71	25	16120	3923	2338017
Feeling of body temperature change	26.27	22.71	13	16132	694	2341246
Dyspepsia	26.26	22.71	39	16106	9805	2332135
Substance abuse	26.23	22.71	12	16133	537	2341403
Musculoskeletal pain	26.20	22.71	41	16104	10789	2331151
Blood thyroid stimulating hormone normal	26.16	22.71	6	16139	24	2341916
Hypophagia	26.04	22.71	25	16120	3975	2337965
Drug tolerance	25.98	22.71	11	16134	408	2341532
Dementia	25.98	22.71	21	16124	2660	2339280
Hepatic necrosis	25.97	22.71	15	16130	1095	2340845
Dependence	25.93	22.71	11	16134	410	2341530
Cardiomegaly	25.86	22.71	20	16125	2376	2339564
Spinal pain	25.82	22.71	16	16129	1329	2340611
Hypothermia	25.55	22.71	19	16126	2129	2339811
Wrong product administered	25.42	22.71	16	16129	1366	2340574
Muscle tightness	25.27	22.71	18	16127	1887	2340053
Tenderness	25.16	22.71	18	16127	1900	2340040
Pituitary tumour benign	25.09	22.71	10	16135	317	2341623
Nerve compression	25.05	22.71	14	16131	960	2340980
Electrocardiogram PR prolongation	24.85	22.71	8	16137	134	2341806
Cyanosis	24.80	22.71	22	16123	3163	2338777
Crohn's disease	24.78	22.71	31	16114	6624	2335316
Skin discolouration	24.72	22.71	28	16117	5392	2336548
Hepatic steatosis	24.64	22.71	22	16123	3191	2338749
Phobia	24.58	22.71	8	16137	139	2341801
Oropharyngeal pain	24.32	22.71	41	16104	11477	2330463
Proctalgia	24.07	22.71	12	16133	651	2341289
Anal sphincter atony	24.04	22.71	7	16138	82	2341858
Onychalgia	23.91	22.71	8	16137	152	2341788
Aspiration	23.89	22.71	16	16129	1518	2340422
Haematemesis	23.76	22.71	24	16121	4058	2337882
Drug level above therapeutic	23.68	22.71	11	16134	510	2341430
Prescribed overdose	23.66	22.71	17	16128	1807	2340133
Stupor	23.60	22.71	12	16133	679	2341261
Thyroid disorder	23.53	22.71	16	16129	1557	2340383
Irritable bowel syndrome	23.51	22.71	17	16128	1824	2340116
Libido decreased	23.48	22.71	11	16134	520	2341420
Gastrointestinal pain	23.39	22.71	14	16131	1092	2340848
Blood chloride decreased	23.36	22.71	12	16133	694	2341246
Limb deformity	23.33	22.71	9	16136	261	2341679
Pre-existing condition improved	23.32	22.71	11	16134	528	2341412
Haemangioma of skin	23.31	22.71	7	16138	92	2341848
Gastritis	23.20	22.71	25	16120	4556	2337384
Nail disorder	23.05	22.71	14	16131	1122	2340818
Altered visual depth perception	23.03	22.71	7	16138	96	2341844
Vasculitic rash	22.94	22.71	8	16137	173	2341767
Hyperacusis	22.93	22.71	10	16135	399	2341541
Defaecation disorder	22.91	22.71	5	16140	15	2341925
Mydriasis	22.82	22.71	18	16127	2201	2339739
Cataract	22.77	22.71	28	16117	5880	2336060

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
Drug hypersensitivity	4584.87	27.12	1272	8153	13863	1723493
Completed suicide	2638.32	27.12	849	8576	15463	1721893
Toxicity to various agents	2357.50	27.12	905	8520	28236	1709120
Drug ineffective for unapproved indication	1599.94	27.12	363	9062	1466	1735890
Drug ineffective	1244.42	27.12	747	8678	63054	1674302
Drug abuse	886.51	27.12	365	9060	13324	1724032
Somnolence	874.06	27.12	383	9042	16356	1721000
Myoclonus	725.47	27.12	202	9223	2093	1735263
Confusional state	696.71	27.12	353	9072	20925	1716431
Cardio-respiratory arrest	597.68	27.12	247	9178	9046	1728310
Overdose	584.02	27.12	290	9135	16411	1720945
Respiratory arrest	532.70	27.12	200	9225	5639	1731717
Drug interaction	442.11	27.12	289	9136	27669	1709687
Dizziness	436.21	27.12	310	9115	34051	1703305
Product use in unapproved indication	433.87	27.12	198	9227	9224	1728132
Tremor	423.15	27.12	216	9209	12915	1724441
Pain	417.56	27.12	274	9151	26383	1710973
Cardiac arrest	392.09	27.12	219	9206	15711	1721645
Condition aggravated	389.71	27.12	241	9184	20909	1716447
Sedation	374.15	27.12	134	9291	3283	1734073
Mental status changes	364.88	27.12	154	9271	5921	1731435
Depression	345.62	27.12	205	9220	16464	1720892
Suicidal ideation	333.16	27.12	160	9265	8358	1728998
Fall	318.38	27.12	234	9191	26980	1710376
Hallucination	305.99	27.12	149	9276	8021	1729335
Seizure	302.34	27.12	203	9222	20238	1717118
Feeling abnormal	278.44	27.12	155	9270	11011	1726345
Depressed level of consciousness	273.45	27.12	129	9296	6463	1730893
Off label use	266.28	27.12	244	9181	38327	1699029
Coma	261.57	27.12	129	9296	7133	1730223
Insomnia	260.77	27.12	170	9255	16106	1721250
Intentional product misuse	256.99	27.12	128	9297	7230	1730126
Drug withdrawal syndrome	246.10	27.12	107	9318	4418	1732938
Agitation	245.07	27.12	142	9283	10884	1726472
Dysarthria	240.07	27.12	110	9315	5149	1732207
Gait disturbance	231.88	27.12	144	9281	12526	1724830
Product use issue	230.16	27.12	125	9300	8446	1728910
Anxiety	226.45	27.12	153	9272	15374	1721982
Withdrawal syndrome	214.20	27.12	80	9345	2208	1735148
Pain in extremity	213.71	27.12	158	9267	18314	1719042
Headache	213.06	27.12	205	9220	34171	1703185
Nausea	208.44	27.12	244	9181	50952	1686404
Drug intolerance	198.52	27.12	101	9324	5961	1731395
Product complaint	196.95	27.12	77	9348	2413	1734943
Accidental death	194.14	27.12	50	9375	370	1736986
Memory impairment	189.52	27.12	101	9324	6562	1730794
Intentional overdose	187.01	27.12	105	9320	7565	1729791
Fatigue	185.28	27.12	229	9196	50552	1686804
Vomiting	181.95	27.12	198	9227	38117	1699239
Delirium	179.70	27.12	96	9329	6266	1731090
Amnesia	179.33	27.12	88	9337	4803	1732553
Acute kidney injury	178.98	27.12	188	9237	34756	1702600
Dyskinesia	174.59	27.12	80	9345	3739	1733617
Aggression	173.55	27.12	102	9323	8013	1729343
Loss of consciousness	171.40	27.12	127	9298	14748	1722608
Asthenia	169.51	27.12	182	9243	34488	1702868
Vision blurred	164.85	27.12	100	9325	8323	1729033
Hypoaesthesia	162.86	27.12	105	9320	9730	1727626
Disorientation	161.43	27.12	85	9340	5384	1731972
Weight increased	158.51	27.12	109	9316	11248	1726108
Paraesthesia	157.04	27.12	105	9320	10346	1727010
Neuropathy peripheral	156.20	27.12	100	9325	9153	1728203
Drug dependence	156.18	27.12	71	9354	3256	1734100
Prescription drug used without a prescription	154.70	27.12	37	9388	193	1737163
Balance disorder	148.27	27.12	82	9343	5730	1731626
Muscle spasms	146.95	27.12	105	9320	11516	1725840
Lethargy	144.96	27.12	87	9338	7097	1730259
Euphoric mood	143.02	27.12	46	9379	799	1736557
Respiratory depression	141.52	27.12	59	9366	2188	1735168
Suicide attempt	140.23	27.12	86	9339	7295	1730061
Hypotension	140.15	27.12	153	9272	29501	1707855
Neuralgia	138.44	27.12	51	9374	1351	1736005
Nightmare	132.46	27.12	60	9365	2727	1734629
Poisoning	131.49	27.12	58	9367	2474	1734882
Hallucination, visual	123.81	27.12	56	9369	2536	1734820
Muscular weakness	123.59	27.12	90	9335	10159	1727197
Medication error	121.18	27.12	67	9358	4676	1732680
Abnormal behaviour	120.72	27.12	74	9351	6268	1731088
Death	119.44	27.12	252	9173	87191	1650165
Cognitive disorder	115.68	27.12	63	9362	4267	1733089
Ataxia	112.90	27.12	51	9374	2302	1735054
Poisoning deliberate	111.14	27.12	38	9387	804	1736552
Disturbance in attention	105.94	27.12	59	9366	4175	1733181
Oedema peripheral	104.13	27.12	97	9328	15453	1721903
Muscle twitching	102.42	27.12	44	9381	1758	1735598
Speech disorder	102.00	27.12	59	9366	4489	1732867
Swelling	101.93	27.12	69	9356	6927	1730429
Intentional self-injury	100.63	27.12	49	9376	2624	1734732
Syncope	99.94	27.12	91	9334	14078	1723278
Therapeutic product effect incomplete	99.68	27.12	62	9363	5386	1731970
Diplopia	99.43	27.12	48	9377	2522	1734834
Mental disorder	97.76	27.12	49	9376	2794	1734562
Respiratory failure	96.18	27.12	90	9335	14415	1722941
Erectile dysfunction	94.68	27.12	56	9369	4441	1732915
Burning sensation	94.62	27.12	50	9375	3185	1734171
Rash	94.52	27.12	144	9281	38549	1698807
Irritability	93.81	27.12	60	9365	5472	1731884
Coordination abnormal	93.21	27.12	39	9386	1458	1735898
Serotonin syndrome	92.78	27.12	47	9378	2741	1734615
Mood altered	92.40	27.12	43	9382	2079	1735277
Epilepsy	90.48	27.12	52	9373	3907	1733449
Sopor	88.53	27.12	41	9384	1960	1735396
Thinking abnormal	87.84	27.12	36	9389	1276	1736080
Bradypnoea	85.33	27.12	25	9400	312	1737044
Constipation	84.28	27.12	85	9340	14915	1722441
Electrocardiogram QRS complex prolonged	83.22	27.12	30	9395	745	1736611
Mental impairment	82.87	27.12	39	9386	1934	1735422
Foetal disorder	81.48	27.12	18	9407	61	1737295
Dysphagia	81.02	27.12	70	9355	10098	1727258
Alcohol interaction	80.95	27.12	24	9401	313	1737043
Urinary retention	80.46	27.12	54	9371	5341	1732015
Encephalopathy	79.75	27.12	50	9375	4402	1732954
Personality change	79.16	27.12	32	9393	1094	1736262
Hyperhidrosis	78.02	27.12	75	9350	12413	1724943
Impaired driving ability	76.16	27.12	26	9399	547	1736809
Road traffic accident	76.07	27.12	45	9380	3568	1733788
Unresponsive to stimuli	75.50	27.12	49	9376	4580	1732776
Therapeutic response unexpected	75.26	27.12	39	9386	2385	1734971
Obsessive-compulsive disorder	73.98	27.12	28	9397	800	1736556
Malaise	72.07	27.12	110	9315	29455	1707901
Anger	71.76	27.12	39	9386	2627	1734729
Tachycardia	69.90	27.12	71	9354	12557	1724799
Sleep disorder	68.70	27.12	44	9381	4019	1733337
Bradyphrenia	68.67	27.12	25	9400	639	1736717
Dyspnoea	68.38	27.12	148	9277	51911	1685445
Foetal exposure during pregnancy	68.02	27.12	52	9373	6307	1731049
Neutropenia neonatal	67.11	27.12	14	9411	33	1737323
Therapeutic product effect decreased	66.27	27.12	51	9374	6246	1731110
Urticaria	66.25	27.12	68	9357	12173	1725183
Peripheral swelling	65.77	27.12	56	9369	7915	1729441
Visual impairment	64.65	27.12	50	9375	6168	1731188
Sensory disturbance	64.46	27.12	29	9396	1295	1736061
Asterixis	63.78	27.12	19	9406	252	1737104
Intentional product use issue	62.88	27.12	36	9389	2683	1734673
Hyperreflexia	62.81	27.12	23	9402	598	1736758
Restlessness	61.44	27.12	42	9383	4279	1733077
Rhabdomyolysis	60.72	27.12	62	9363	11028	1726328
Myalgia	60.62	27.12	73	9352	15585	1721771
Anorgasmia	60.14	27.12	17	9408	185	1737171
Drug-induced liver injury	59.59	27.12	37	9388	3200	1734156
Sleep apnoea syndrome	59.34	27.12	32	9393	2122	1735234
Sweat gland disorder	58.63	27.12	13	9412	45	1737311
Hypertension	58.51	27.12	80	9345	19368	1717988
Nervous system disorder	58.12	27.12	33	9392	2421	1734935
Status epilepticus	58.05	27.12	31	9394	2015	1735341
Therapeutic product effect variable	57.52	27.12	15	9410	117	1737239
Pruritus	55.98	27.12	86	9339	23136	1714220
Abdominal discomfort	55.68	27.12	54	9371	9027	1728329
Movement disorder	55.11	27.12	28	9397	1642	1735714
Urinary incontinence	54.78	27.12	33	9392	2703	1734653
Generalised tonic-clonic seizure	54.40	27.12	38	9387	4008	1733348
Bradycardia	54.26	27.12	57	9368	10477	1726879
Oedema	53.64	27.12	47	9378	6901	1730455
Exposure via ingestion	53.63	27.12	21	9404	659	1736697
Actinic keratosis	53.12	27.12	20	9405	563	1736793
Dysmorphism	52.71	27.12	18	9407	379	1736977
Maternal exposure during pregnancy	52.46	27.12	21	9404	699	1736657
Feeling drunk	51.55	27.12	18	9407	406	1736950
Autonomic nervous system imbalance	51.42	27.12	18	9407	409	1736947
Gait inability	50.94	27.12	34	9391	3329	1734027
Quality of life decreased	50.32	27.12	19	9406	539	1736817
Dystonia	50.17	27.12	28	9397	1986	1735370
Premature baby	50.08	27.12	32	9393	2910	1734446
Aphasia	50.05	27.12	34	9391	3427	1733929
Muscle spasticity	49.88	27.12	25	9400	1424	1735932
Altered state of consciousness	49.73	27.12	34	9391	3463	1733893
Pneumonia aspiration	49.69	27.12	40	9385	5226	1732130
Myasthenia gravis	48.65	27.12	19	9406	592	1736764
Palpitations	48.45	27.12	44	9381	6770	1730586
Discomfort	48.19	27.12	30	9395	2606	1734750
Diabetic neuropathy	48.06	27.12	18	9407	499	1736857
Musculoskeletal stiffness	47.89	27.12	41	9384	5835	1731521
Nervousness	47.55	27.12	28	9397	2199	1735157
Phantom limb syndrome	47.23	27.12	11	9414	50	1737306
Vertigo	46.99	27.12	36	9389	4377	1732979
Heart rate increased	46.21	27.12	42	9383	6468	1730888
Diarrhoea	46.08	27.12	130	9295	53722	1683634
Hypoglycaemia	45.86	27.12	47	9378	8391	1728965
Pulmonary oedema	45.79	27.12	42	9383	6544	1730812
Paranoia	45.46	27.12	27	9398	2154	1735202
Hepatitis	45.40	27.12	37	9388	4918	1732438
Hypoxia	45.35	27.12	40	9385	5923	1731433
Hypotonia	45.14	27.12	24	9401	1546	1735810
Depressed mood	44.50	27.12	30	9395	2986	1734370
Opisthotonus	44.45	27.12	13	9412	161	1737195
Selective eating disorder	44.09	27.12	16	9409	405	1736951
Fibromyalgia	44.00	27.12	15	9410	314	1737042
Weight decreased	43.62	27.12	76	9349	22677	1714679
Antipsychotic drug level below therapeutic	43.39	27.12	13	9412	176	1737180
Increased appetite	43.27	27.12	20	9405	951	1736405
Chorea	43.25	27.12	14	9411	248	1737108
Tinnitus	42.93	27.12	30	9395	3165	1734191
Affective disorder	42.33	27.12	18	9407	700	1736656
Agranulocytosis	42.13	27.12	31	9394	3545	1733811
Arthralgia	41.97	27.12	76	9349	23368	1713988
Dry mouth	41.83	27.12	32	9393	3881	1733475
Renal tubular necrosis	40.98	27.12	25	9400	2094	1735262
Crying	40.87	27.12	22	9403	1453	1735903
Back pain	40.67	27.12	62	9363	16551	1720805
Bowen's disease	40.59	27.12	14	9411	304	1737052
Dependence	40.37	27.12	14	9411	309	1737047
Leukopenia	40.33	27.12	44	9381	8436	1728920
Talipes	40.18	27.12	15	9410	412	1736944
Accidental overdose	40.07	27.12	32	9393	4132	1733224
Hyponatraemia	39.88	27.12	45	9380	8955	1728401
Personality disorder	39.56	27.12	13	9412	242	1737114
Hypersensitivity	39.27	27.12	48	9377	10396	1726960
Hepatic steatosis	38.83	27.12	26	9399	2558	1734798
Chest pain	38.79	27.12	67	9358	19847	1717509
Decreased interest	38.15	27.12	14	9411	366	1736990
Trigeminal neuralgia	37.05	27.12	12	9413	213	1737143
Hypometabolism	36.95	27.12	8	9417	24	1737332
Blood creatinine increased	36.92	27.12	54	9371	13892	1723464
Mobility decreased	36.79	27.12	30	9395	3990	1733366
Hypoosmolar state	36.69	27.12	7	9418	8	1737348
Psychotic disorder	36.62	27.12	33	9392	5023	1732333
Incorrect dose administered	36.21	27.12	39	9386	7370	1729986
Drug effective for unapproved indication	36.18	27.12	11	9414	157	1737199
Pancytopenia	36.07	27.12	48	9377	11309	1726047
Dysaesthesia	35.88	27.12	14	9411	435	1736921
Tooth disorder	35.85	27.12	20	9405	1417	1735939
Abnormal dreams	35.78	27.12	22	9403	1869	1735487
Disinhibition	35.75	27.12	13	9412	331	1737025
Low birth weight baby	35.61	27.12	17	9408	870	1736486
Hypothermia	34.77	27.12	21	9404	1727	1735629
Renal failure	34.69	27.12	64	9361	19953	1717403
Gingival atrophy	34.68	27.12	7	9418	13	1737343
Akathisia	34.55	27.12	19	9406	1309	1736047
Paralysis	34.23	27.12	19	9406	1333	1736023
Drug tolerance	34.22	27.12	13	9412	375	1736981
Facial pain	34.09	27.12	13	9412	379	1736977
Metabolic encephalopathy	34.04	27.12	14	9411	500	1736856
Drug screen negative	33.99	27.12	9	9416	75	1737281
Accident	33.58	27.12	16	9409	815	1736541
Incoherent	33.53	27.12	16	9409	818	1736538
Hypokinesia	33.43	27.12	18	9407	1189	1736167
Restless legs syndrome	33.40	27.12	17	9408	1000	1736356
Self-medication	33.39	27.12	15	9410	667	1736689
Liver injury	33.34	27.12	21	9404	1861	1735495
Loss of personal independence in daily activities	33.34	27.12	23	9402	2376	1734980
Cholestasis	32.80	27.12	27	9398	3638	1733718
Drug level increased	32.55	27.12	24	9401	2753	1734603
Hepatotoxicity	32.48	27.12	25	9400	3059	1734297
Obesity	32.45	27.12	17	9408	1062	1736294
Therapy non-responder	32.42	27.12	34	9391	6232	1731124
Acute febrile neutrophilic dermatosis	32.30	27.12	12	9413	325	1737031
General physical health deterioration	32.16	27.12	49	9376	13069	1724287
Dysstasia	32.15	27.12	20	9405	1734	1735622
Emotional disorder	31.97	27.12	17	9408	1095	1736261
Impaired work ability	31.95	27.12	17	9408	1096	1736260
Mydriasis	31.87	27.12	18	9407	1306	1736050
Psychomotor skills impaired	31.69	27.12	12	9413	343	1737013
Drug level below therapeutic	31.51	27.12	13	9412	468	1736888
Abdominal pain	31.48	27.12	64	9361	21426	1715930
Nystagmus	31.41	27.12	16	9409	943	1736413
Injury	31.18	27.12	24	9401	2936	1734420
Suicidal behaviour	31.18	27.12	12	9413	359	1736997
Sciatica	31.17	27.12	15	9410	781	1736575
Arteriosclerosis coronary artery	30.76	27.12	20	9405	1872	1735484
Substance abuse	30.73	27.12	16	9409	987	1736369
Bradykinesia	30.63	27.12	13	9412	503	1736853
Nerve injury	30.63	27.12	13	9412	503	1736853
Pneumonia	30.58	27.12	102	9323	46080	1691276
Acute lung injury	30.39	27.12	10	9415	187	1737169
Conduction disorder	30.36	27.12	12	9413	386	1736970
Pulmonary hypoplasia	30.30	27.12	9	9416	118	1737238
Respiratory acidosis	30.12	27.12	14	9411	674	1736682
Cerebral infarction	30.09	27.12	30	9395	5179	1732177
Hyperkalaemia	30.07	27.12	38	9387	8509	1728847
Arrhythmia	29.98	27.12	32	9393	5984	1731372
Hypersomnia	29.76	27.12	19	9406	1724	1735632
Slow speech	29.71	27.12	10	9415	201	1737155
Distributive shock	29.63	27.12	9	9416	128	1737228
Thoracic vertebral fracture	29.53	27.12	10	9415	205	1737151
Bone metabolism disorder	29.50	27.12	7	9418	35	1737321
Liver function test abnormal	29.49	27.12	31	9394	5695	1731661
Pyrexia	29.42	27.12	101	9324	46299	1691057
Hepatitis cholestatic	29.23	27.12	17	9408	1304	1736052
Sedation complication	29.19	27.12	9	9416	135	1737221
Blood creatine phosphokinase increased	29.00	27.12	38	9387	8818	1728538
Product substitution issue	28.97	27.12	24	9401	3262	1734094
Precancerous skin lesion	28.83	27.12	9	9416	141	1737215
Gamma-glutamyltransferase increased	28.79	27.12	29	9396	5069	1732287
Renal impairment	28.78	27.12	45	9380	12269	1725087
Muscle rigidity	28.74	27.12	19	9406	1829	1735527
Lactic acidosis	28.64	27.12	29	9396	5100	1732256
Product prescribing error	28.63	27.12	21	9404	2389	1734967
Visual field defect	28.60	27.12	16	9409	1140	1736216
Rash maculo-papular	28.47	27.12	25	9400	3678	1733678
Psychomotor hyperactivity	28.33	27.12	19	9406	1874	1735482
Treatment noncompliance	28.30	27.12	29	9396	5172	1732184
Hepatic fibrosis	28.22	27.12	13	9412	613	1736743
Gingival disorder	28.05	27.12	10	9415	240	1737116
Left ventricular enlargement	28.02	27.12	7	9418	45	1737311
Incorrect route of product administration	27.86	27.12	24	9401	3441	1733915
Myocardial ischaemia	27.48	27.12	23	9402	3170	1734186
Blood sodium decreased	27.20	27.12	20	9405	2284	1735072

Pharmacologic Action:

Source	Code	Description
ATC	N03AX12	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics
FDA EPC	N0000175753	Anti-epileptic Agent
FDA PE	N0000008486	Decreased Central Nervous System Disorganized Electrical Activity
MeSH PA	D000700	Analgesics
CHEBI has role	CHEBI:35623	anticonvulsant
MeSH PA	D000927	Anticonvulsants
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D018692	Antimanic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018691	Excitatory Amino Acid Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D018689	Sensory System Agents
MeSH PA	D014149	Tranquilizing Agents

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Postherpetic neuralgia	indication	2177002
Restless legs	indication	32914008	DOID:0050425
Partial Epilepsy Treatment Adjunct	indication
Menopausal flushing	off-label use	198436008
Neuropathic pain	off-label use	247398009
Essential tremor	off-label use	609558009	DOID:4990
Acute postoperative pain	off-label use	107401000119105
Suicidal thoughts	contraindication	6471006
Depressive disorder	contraindication	35489007
Kidney disease	contraindication	90708001	DOID:557

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.02	acidic
pKa2	10.31	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
300MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8192756	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
300MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8252332	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
300MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8333992	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
600MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8192756	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
600MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8252332	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
600MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	8333992	Oct. 25, 2022	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
300MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	7438927	Feb. 26, 2024	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA
600MG	GRALISE	ALMATICA	N022544	Jan. 28, 2011	RX	TABLET	ORAL	7438927	Feb. 26, 2024	TREATMENT WITH GABAPENTIN, INCLUDING TREATMENT OF NEUROPATHIC PAIN, INCLUDING NEUROPATHIC PAIN ASSOCIATED WITH POSTHERPETIC NEURALGIA

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Voltage-dependent calcium channel subunit alpha-2/delta-1	Ion channel	P54289	CA2D1_HUMAN	MODULATOR	IC50	7.26	WOMBAT-PK	CHEMBL
Voltage-dependent calcium channel subunit alpha-2/delta-2	Ion channel	Q9NY47	CA2D2_HUMAN	MODULATOR	IC50	6.93	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Large neutral amino acids transporter small subunit 1	Transporter	Q01650	LAT1_HUMAN		IC50	4.52	WOMBAT-PK
Glutamate receptor ionotropic, NMDA 3A	Ion channel	Q8TCU5	NMD3A_HUMAN				WOMBAT-PK
Gamma-aminobutyric acid type B receptor subunit 2	GPCR	O75899	GABR2_HUMAN				WOMBAT-PK
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN				WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN				WOMBAT-PK
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN				WOMBAT-PK
Voltage-dependent calcium channel subunit alpha-2/delta-1	Ion channel		CA2D1_MOUSE		Ki	6.92	CHEMBL
Uncharacterized protein; Voltage-dependent calcium channel alpha-2 delta subunit	Ion channel		O77773_PIG		IC50	7.15	CHEMBL

External reference:

ID	Source
D000077206	MESH_DESCRIPTOR_UI
4020833	VUID
N0000148345	NUI
C0060926	UMLSCUI
D00332	KEGG_DRUG
6CW7F3G59X	UNII
5094	INN_ID
108402001	SNOMEDCT_US
4020833	VANDF
60712	MMSL
004415	NDDF
d03182	MMSL
4770	MMSL
25480	RXNORM
386845007	SNOMEDCT_US
3446	PUBCHEM_CID
CHEBI:42797	CHEBI
CHEMBL940	ChEMBL_ID
DB00996	DRUGBANK_ID
GBN	PDB_CHEM_ID
5483	IUPHAR_LIGAND_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0401	TABLET, FILM COATED	800 mg	ORAL	NDA	20 sections
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0513	TABLET, FILM COATED	600 mg	ORAL	NDA	20 sections
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0803	CAPSULE	100 mg	ORAL	NDA	20 sections
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0805	CAPSULE	300 mg	ORAL	NDA	20 sections
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0806	CAPSULE	400 mg	ORAL	NDA	20 sections
Neurontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-2012	SOLUTION	250 mg	ORAL	NDA	20 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2636	TABLET, FILM COATED	600 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2637	TABLET, FILM COATED	800 mg	ORAL	ANDA	19 sections
GABAPENTIN	HUMAN PRESCRIPTION DRUG LABEL	1	0440-5562	TABLET, FILM COATED	600 mg	ORAL	ANDA	12 sections
GABAPENTIN	HUMAN PRESCRIPTION DRUG LABEL	1	0440-5563	TABLET, FILM COATED	800 mg	ORAL	ANDA	12 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0440-7559	CAPSULE	300 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-1376	CAPSULE	100 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-1377	CAPSULE	400 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-1378	CAPSULE	300 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-6548	TABLET, FILM COATED	600 mg	ORAL	ANDA	18 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-6554	TABLET, FILM COATED	800 mg	ORAL	ANDA	13 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7762	CAPSULE	300 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7839	CAPSULE	400 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7844	CAPSULE	100 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7845	CAPSULE	300 mg	ORAL	ANDA	14 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7961	CAPSULE	100 mg	ORAL	ANDA	18 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7962	CAPSULE	300 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-7963	CAPSULE	400 mg	ORAL	ANDA	18 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8019	TABLET	600 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8095	CAPSULE	100 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8096	CAPSULE	300 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8097	CAPSULE	400 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8098	TABLET	600 mg	ORAL	ANDA	19 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8132	TABLET	800 mg	ORAL	ANDA	18 sections
Gabapentin	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8230	CAPSULE	100 mg	ORAL	ANDA	18 sections