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

Stem definitionDrug idCAS RN
gabamimetic agents 1264 60142-96-3

Description:

MoleculeDescription

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:

DoseUnitRoute
1.80 g O

ADMET properties:

PropertyValueReference
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 ┬ÁM/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:

DateAgencyCompanyOrphan
Dec. 30, 1993 FDA PFIZER PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 4.02 acidic
pKa2 10.31 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent calcium channel subunit alpha-2/delta-1 Ion channel MODULATOR IC50 7.26 WOMBAT-PK CHEMBL
Voltage-dependent calcium channel subunit alpha-2/delta-2 Ion channel MODULATOR IC50 6.93 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Large neutral amino acids transporter small subunit 1 Transporter IC50 4.52 WOMBAT-PK
Glutamate receptor ionotropic, NMDA 3A Ion channel WOMBAT-PK
Gamma-aminobutyric acid type B receptor subunit 2 GPCR WOMBAT-PK
Adenosine receptor A1 GPCR WOMBAT-PK
Alpha-2A adrenergic receptor GPCR WOMBAT-PK
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK
Voltage-dependent calcium channel subunit alpha-2/delta-1 Ion channel Ki 6.92 CHEMBL
Uncharacterized protein; Voltage-dependent calcium channel alpha-2 delta subunit Ion channel IC50 7.15 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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