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

Stem definitionDrug idCAS RN
diazepam derivatives 852 439-14-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RO-5-2807
  • diazepam
  • valium
A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.
  • Molecular weight: 284.74
  • Formula: C16H13ClN2O
  • CLOGP: 2.96
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 32.67
  • ALOGS: -4.37
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
10 mg O
10 mg P
10 mg R

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.06 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 2.01 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.38 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 42 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 15, 1963 FDA ROCHE

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
Toxicity to various agents 6311.78 39.04 1676 6686 31078 2318645
Completed suicide 5222.18 39.04 1323 7039 19711 2330012
Drug abuse 5168.55 39.04 1180 7182 10846 2338877
Overdose 1602.69 39.04 527 7835 19380 2330343
Coma 1599.48 39.04 440 7922 8616 2341107
Respiratory arrest 1557.13 39.04 398 7964 5780 2343943
Intentional overdose 1537.82 39.04 448 7914 10873 2338850
Cardiac arrest 1382.23 39.04 440 7922 14490 2335233
Cardio-respiratory arrest 1254.13 39.04 365 7997 8781 2340942
Somnolence 1238.89 39.04 454 7908 23031 2326692
Suicide attempt 1178.52 39.04 365 7997 10917 2338806
Poisoning 1008.27 39.04 241 8121 2579 2347144
Intentional product misuse 981.74 39.04 305 8057 9184 2340539
Death 933.58 39.04 544 7818 80924 2268799
Sopor 924.88 39.04 241 8121 3754 2345969
Drug dependence 764.27 39.04 196 8166 2849 2346874
Drug interaction 605.54 39.04 291 8071 28872 2320851
Respiratory depression 501.97 39.04 131 8231 2039 2347684
Drug hypersensitivity 487.49 39.04 295 8067 46348 2303375
Hypotension 486.67 39.04 260 8102 32176 2317547
Intentional self-injury 482.37 39.04 146 8216 3981 2345742
Depressed level of consciousness 466.09 39.04 165 8197 7439 2342284
Poisoning deliberate 436.48 39.04 104 8258 1087 2348636
Confusional state 430.35 39.04 218 8144 24126 2325597
Accidental overdose 406.80 39.04 127 8235 3845 2345878
Agitation 355.21 39.04 150 8212 10901 2338822
Fall 331.93 39.04 233 8129 46866 2302857
Tachycardia 322.26 39.04 158 8204 16251 2333472
Loss of consciousness 310.80 39.04 161 8201 18606 2331117
Seizure 308.09 39.04 175 8187 24291 2325432
Disturbance in attention 290.70 39.04 108 8254 5577 2344146
Drug ineffective 274.79 39.04 290 8072 101334 2248389
Exposure via ingestion 268.97 39.04 65 8297 723 2349000
Sedation 268.36 39.04 89 8273 3273 2346450
Bradypnoea 262.22 39.04 57 8305 377 2349346
Miosis 259.46 39.04 69 8293 1155 2348568
Anxiety 231.74 39.04 156 8206 29203 2320520
Drug withdrawal syndrome 230.40 39.04 96 8266 6725 2342998
Aggression 223.11 39.04 85 8277 4701 2345022
Drug withdrawal convulsions 216.70 39.04 47 8315 307 2349416
Condition aggravated 205.88 39.04 150 8212 31829 2317894
Depression 204.23 39.04 142 8220 27990 2321733
Restlessness 194.71 39.04 76 8286 4487 2345236
Suicidal ideation 191.62 39.04 98 8264 10989 2338734
Dysarthria 187.24 39.04 81 8281 6221 2343502
Altered state of consciousness 177.89 39.04 68 8294 3792 2345931
Disorientation 176.64 39.04 78 8284 6294 2343429
Vomiting 176.45 39.04 195 8167 71407 2278316
Electrocardiogram QT prolonged 173.63 39.04 82 8280 7732 2341991
Maternal exposure during pregnancy 172.60 39.04 101 8261 14762 2334961
Bradyphrenia 168.30 39.04 48 8314 1051 2348672
Toxic epidermal necrolysis 157.94 39.04 59 8303 3085 2346638
Status epilepticus 152.42 39.04 54 8308 2424 2347299
Treatment noncompliance 147.77 39.04 66 8296 5468 2344255
Hypotonia 146.83 39.04 48 8314 1682 2348041
Neuroleptic malignant syndrome 145.92 39.04 50 8312 2030 2347693
Substance abuse 145.61 39.04 37 8325 512 2349211
Schizophrenia 145.48 39.04 45 8317 1314 2348409
Serotonin syndrome 144.10 39.04 57 8305 3483 2346240
Exposure during pregnancy 139.25 39.04 108 8254 25111 2324612
Mydriasis 138.93 39.04 49 8313 2170 2347553
Accidental death 138.58 39.04 32 8330 287 2349436
Unresponsive to stimuli 136.12 39.04 60 8302 4816 2344907
Bradycardia 135.10 39.04 75 8287 9906 2339817
Hallucination 134.88 39.04 70 8292 8078 2341645
Withdrawal syndrome 133.27 39.04 53 8309 3284 2346439
Aspiration 131.96 39.04 43 8319 1491 2348232
Urinary retention 131.83 39.04 54 8308 3613 2346110
Respiratory failure 131.39 39.04 82 8280 13446 2336277
Cholestasis 131.07 39.04 54 8308 3667 2346056
Foetal exposure during pregnancy 125.56 39.04 58 8304 5194 2344529
Pneumonia aspiration 124.03 39.04 52 8310 3690 2346033
Hypothermia 121.51 39.04 44 8318 2104 2347619
Delirium 119.64 39.04 56 8306 5167 2344556
Dizziness 117.83 39.04 144 8218 58521 2291202
Psychomotor retardation 114.70 39.04 31 8331 552 2349171
Coma scale abnormal 113.09 39.04 33 8329 785 2348938
Insomnia 109.87 39.04 95 8267 25692 2324031
Psychotic disorder 109.75 39.04 51 8311 4628 2345095
Parkinsonism 104.86 39.04 36 8326 1469 2348254
Ataxia 104.47 39.04 41 8321 2451 2347272
Hyperhidrosis 102.81 39.04 74 8288 15348 2334375
Drug withdrawal syndrome neonatal 102.72 39.04 27 8335 430 2349293
Asphyxia 102.22 39.04 32 8330 972 2348751
Encephalopathy 101.68 39.04 48 8314 4513 2345210
Tremor 100.12 39.04 82 8280 20579 2329144
Respiratory acidosis 99.87 39.04 30 8332 791 2348932
Medication error 99.52 39.04 52 8310 6079 2343644
Syncope 96.85 39.04 74 8288 16801 2332922
Lethargy 95.17 39.04 57 8305 8673 2341050
Stevens-Johnson syndrome 92.42 39.04 44 8318 4215 2345508
Malaise 91.96 39.04 124 8238 55461 2294262
Hepatic steatosis 91.15 39.04 40 8322 3173 2346550
Myoclonus 90.72 39.04 37 8325 2446 2347277
Pulmonary oedema 90.60 39.04 52 8310 7311 2342412
Nausea 88.49 39.04 179 8183 112010 2237713
Respiratory distress 84.66 39.04 44 8318 5085 2344638
Social avoidant behaviour 83.71 39.04 24 8338 535 2349188
Abnormal behaviour 81.93 39.04 42 8320 4718 2345005
Pulmonary congestion 81.20 39.04 32 8330 1933 2347790
Alcohol poisoning 80.56 39.04 21 8341 323 2349400
Product use issue 80.18 39.04 58 8304 12111 2337612
Apnoea 80.15 39.04 29 8333 1382 2348341
Off label use 80.07 39.04 135 8227 73463 2276260
Respiratory disorder 79.72 39.04 39 8323 3965 2345758
Psychomotor hyperactivity 78.37 39.04 31 8331 1891 2347832
Metabolic acidosis 78.20 39.04 44 8318 5954 2343769
Pancreatic fibrosis 77.64 39.04 12 8350 2 2349721
Balance disorder 77.17 39.04 52 8310 9695 2340028
Pneumonia 75.50 39.04 106 8256 49190 2300533
Memory impairment 74.85 39.04 57 8305 12866 2336857
Headache 74.20 39.04 137 8225 80042 2269681
Sinus tachycardia 74.12 39.04 35 8327 3290 2346433
Visceral congestion 73.61 39.04 14 8348 41 2349682
Dehydration 73.16 39.04 71 8291 22224 2327499
Amnesia 72.98 39.04 45 8317 7208 2342515
Myocardial fibrosis 72.66 39.04 16 8346 113 2349610
Psychomotor skills impaired 71.71 39.04 20 8342 402 2349321
Hypertension 71.39 39.04 77 8285 27284 2322439
Drug level increased 70.42 39.04 32 8330 2755 2346968
Physical assault 70.39 39.04 17 8345 188 2349535
Speech disorder 69.90 39.04 42 8320 6422 2343301
Electrolyte imbalance 69.81 39.04 29 8333 2008 2347715
Acute kidney injury 69.64 39.04 77 8285 28045 2321678
Cyanosis 69.38 39.04 33 8329 3152 2346571
Muscle rigidity 69.34 39.04 28 8334 1803 2347920
Drug diversion 69.19 39.04 17 8345 203 2349520
Bradykinesia 68.63 39.04 21 8341 590 2349133
Gait disturbance 65.13 39.04 67 8295 22478 2327245
Alcohol use 64.66 39.04 19 8343 463 2349260
Oxygen saturation decreased 63.73 39.04 42 8320 7544 2342179
Generalised tonic-clonic seizure 63.57 39.04 37 8325 5335 2344388
Multiple organ dysfunction syndrome 63.45 39.04 42 8320 7599 2342124
Drug reaction with eosinophilia and systemic symptoms 62.65 39.04 37 8325 5481 2344242
Hyponatraemia 62.65 39.04 52 8310 13273 2336450
Extrapyramidal disorder 62.64 39.04 28 8334 2319 2347404
Feeling abnormal 62.62 39.04 67 8295 23514 2326209
Blood creatine phosphokinase increased 62.44 39.04 36 8326 5100 2344623
Sinus bradycardia 62.14 39.04 27 8335 2089 2347634
Cholelithiasis 60.93 39.04 37 8325 5766 2343957
Cholecystitis 60.67 39.04 27 8335 2213 2347510
Fatigue 60.42 39.04 130 8232 84743 2264980
Muscle spasms 60.32 39.04 63 8299 21503 2328220
Pyrexia 60.30 39.04 100 8262 53608 2296115
Spleen congestion 60.20 39.04 12 8350 48 2349675
Bezoar 59.67 39.04 15 8347 198 2349525
Mental status changes 59.66 39.04 36 8326 5546 2344177
Drug abuser 59.29 39.04 21 8341 940 2348783
Hyperthyroidism 59.12 39.04 26 8336 2071 2347652
Hepatocellular injury 59.04 39.04 32 8330 4023 2345700
Prescription drug used without a prescription 58.85 39.04 15 8347 210 2349513
Victim of child abuse 57.92 39.04 10 8352 13 2349710
Dermatitis exfoliative 57.63 39.04 22 8340 1219 2348504
Purpura senile 57.09 39.04 10 8352 15 2349708
Snoring 56.41 39.04 17 8345 453 2349270
Hypersomnia 56.12 39.04 26 8336 2340 2347383
Abdominal distension 56.08 39.04 44 8318 10367 2339356
Blister 55.69 39.04 37 8325 6734 2342989
Acidosis 55.44 39.04 23 8339 1587 2348136
Cardiac murmur 54.88 39.04 23 8339 1628 2348095
Dystonia 54.82 39.04 25 8337 2169 2347554
Aspartate aminotransferase increased 54.72 39.04 47 8315 12565 2337158
Catatonia 54.06 39.04 19 8343 831 2348892
Hyperthermia 54.04 39.04 22 8340 1446 2348277
Cognitive disorder 53.15 39.04 33 8329 5348 2344375
Drug screen positive 52.59 39.04 19 8343 901 2348822
Weight decreased 52.56 39.04 67 8295 28304 2321419
Dissociation 52.54 39.04 16 8346 442 2349281
Blood sodium decreased 52.31 39.04 27 8335 3073 2346650
Asthenia 52.15 39.04 87 8275 46839 2302884
Hypoxic-ischaemic encephalopathy 51.96 39.04 18 8344 754 2348969
Areflexia 51.69 39.04 17 8345 606 2349117
Impaired reasoning 51.18 39.04 9 8353 14 2349709
Hypokalaemia 50.95 39.04 42 8320 10612 2339111
Aortic valve calcification 50.67 39.04 11 8351 72 2349651
Brain oedema 50.51 39.04 24 8338 2286 2347437
Irritability 50.17 39.04 34 8328 6393 2343330
Decreased appetite 50.04 39.04 66 8296 28825 2320898
Drowning 49.74 39.04 12 8350 132 2349591
Body mass index decreased 49.40 39.04 10 8352 44 2349679
Hypernatraemia 49.38 39.04 18 8344 876 2348847
Gallbladder cholesterolosis 49.17 39.04 12 8350 139 2349584
Self-injurious ideation 48.99 39.04 16 8346 558 2349165
Obstructive airways disorder 48.58 39.04 20 8342 1353 2348370
Mental disorder 48.47 39.04 28 8334 3979 2345744
Patient uncooperative 47.67 39.04 9 8353 25 2349698
Product use in unapproved indication 47.09 39.04 41 8321 11159 2338564
Abdominal pain upper 47.06 39.04 56 8306 22044 2327679
Cardiomegaly 46.68 39.04 23 8339 2373 2347350
Pruritus 46.35 39.04 79 8283 43261 2306462
Panic attack 46.15 39.04 27 8335 3929 2345794
Hand deformity 45.97 39.04 18 8344 1068 2348655
Sudden death 45.86 39.04 21 8341 1839 2347884
Tarsal tunnel syndrome 45.56 39.04 9 8353 34 2349689
Judgement impaired 45.51 39.04 11 8351 122 2349601
Heart rate increased 45.38 39.04 40 8322 11065 2338658
Circulatory collapse 45.01 39.04 26 8336 3694 2346029
Erythema 44.37 39.04 58 8304 25101 2324622
Dyspnoea 44.30 39.04 110 8252 78623 2271100
Contusion 44.26 39.04 42 8320 12768 2336955
Pain 44.23 39.04 95 8267 61762 2287961
Hemiparesis 44.12 39.04 25 8337 3425 2346298
Facial nerve disorder 44.09 39.04 10 8352 82 2349641
Hyperchloraemia 43.88 39.04 10 8352 84 2349639
Hypotonia neonatal 43.81 39.04 12 8350 225 2349498
Mucosal erosion 43.56 39.04 12 8350 230 2349493
Hepatitis 43.54 39.04 31 8331 6306 2343417
Incorrect route of product administration 43.49 39.04 29 8333 5307 2344416
Aphasia 43.13 39.04 28 8334 4900 2344823
Drug use disorder 42.87 39.04 13 8349 354 2349369
Nightmare 42.51 39.04 25 8337 3672 2346051
Muscular weakness 42.50 39.04 44 8318 14853 2334870
Hepatic necrosis 42.11 39.04 17 8345 1093 2348630
Rhabdomyolysis 41.97 39.04 31 8331 6673 2343050
Left ventricular hypertrophy 41.83 39.04 15 8347 696 2349027
Akathisia 41.59 39.04 19 8343 1655 2348068
Road traffic accident 41.48 39.04 26 8336 4282 2345441
Tooth hypoplasia 41.43 39.04 8 8354 26 2349697
Drooling 41.42 39.04 15 8347 716 2349007
Hypercapnic coma 41.20 39.04 8 8354 27 2349696
Incontinence 40.90 39.04 18 8344 1436 2348287
Sleep disorder 40.61 39.04 30 8332 6459 2343264
Salivary hypersecretion 40.49 39.04 17 8345 1208 2348515
Premature baby 40.39 39.04 23 8339 3181 2346542
Renal failure 40.34 39.04 46 8316 17303 2332420
Developmental delay 40.32 39.04 12 8350 306 2349417
Epilepsy 39.72 39.04 26 8336 4613 2345110
Hallucination, auditory 39.62 39.04 20 8342 2172 2347551
Electroencephalogram abnormal 39.62 39.04 15 8347 812 2348911
Generalised anxiety disorder 39.53 39.04 11 8351 219 2349504
Hallucination, visual 39.21 39.04 22 8340 2957 2346766
Foetal death 39.18 39.04 19 8343 1893 2347830
Toxicologic test abnormal 39.17 39.04 10 8352 141 2349582

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
Toxicity to various agents 7725.34 45.54 2104 6018 27037 1711622
Drug abuse 6023.22 45.54 1492 6630 12197 1726462
Completed suicide 2379.05 45.54 757 7365 15555 1723104
Overdose 1826.85 45.54 625 7497 16076 1722583
Respiratory arrest 1433.55 45.54 407 7715 5432 1733227
Coma 1402.20 45.54 420 7702 6842 1731817
Somnolence 1175.89 45.54 453 7669 16286 1722373
Intentional overdose 1159.64 45.54 368 7754 7302 1731357
Cardiac arrest 1139.71 45.54 437 7685 15493 1723166
Drug dependence 1031.56 45.54 279 7843 3048 1735611
Poisoning 1008.33 45.54 259 7863 2273 1736386
Cardio-respiratory arrest 976.43 45.54 339 7783 8954 1729705
Death 917.52 45.54 657 7465 86786 1651873
Intentional product misuse 912.09 45.54 304 7818 7054 1731605
Accidental overdose 763.32 45.54 232 7890 3932 1734727
Suicide attempt 750.27 45.54 263 7859 7118 1731541
Drug interaction 535.23 45.54 309 7813 27649 1711010
Poisoning deliberate 510.91 45.54 121 8001 721 1737938
Substance abuse 439.80 45.54 111 8011 892 1737767
Respiratory depression 431.75 45.54 130 7992 2117 1736542
Agitation 410.64 45.54 191 7931 10835 1727824
Miosis 401.72 45.54 112 8010 1366 1737293
Depressed level of consciousness 392.19 45.54 159 7963 6433 1732226
Sopor 389.70 45.54 117 8005 1884 1736775
Pneumonia aspiration 372.59 45.54 144 7978 5122 1733537
Hypotension 367.50 45.54 249 7873 29405 1709254
Aggression 328.28 45.54 149 7973 7966 1730693
Loss of consciousness 306.60 45.54 173 7949 14702 1723957
Sedation 305.61 45.54 111 8011 3306 1735353
Intentional self-injury 304.65 45.54 104 8018 2569 1736090
Pulmonary oedema 276.01 45.54 124 7998 6462 1732197
Tachycardia 274.09 45.54 152 7970 12476 1726183
Dysarthria 272.47 45.54 115 8007 5144 1733515
Confusional state 266.24 45.54 180 7942 21098 1717561
Bradypnoea 265.91 45.54 60 8062 277 1738382
Prescription drug used without a prescription 237.15 45.54 51 8071 179 1738480
Electrocardiogram QT prolonged 202.73 45.54 95 8027 5450 1733209
Rhabdomyolysis 191.19 45.54 115 8007 10975 1727684
Unresponsive to stimuli 190.14 45.54 86 8036 4543 1734116
Coma scale abnormal 188.62 45.54 51 8071 548 1738111
Altered state of consciousness 186.13 45.54 78 8044 3419 1735240
Seizure 184.60 45.54 142 7980 20299 1718360
Accidental death 176.67 45.54 45 8077 375 1738284
Exposure via ingestion 173.12 45.54 49 8073 631 1738028
Anxiety 171.93 45.54 122 8000 15405 1723254
Abnormal behaviour 167.26 45.54 87 8035 6255 1732404
Asphyxia 167.03 45.54 53 8069 1030 1737629
Delirium 164.14 45.54 86 8036 6276 1732383
Visceral congestion 163.66 45.54 33 8089 76 1738583
Pulmonary congestion 162.62 45.54 59 8063 1746 1736913
Aspiration 160.58 45.54 59 8063 1811 1736848
Withdrawal syndrome 159.58 45.54 62 8060 2226 1736433
Brain oedema 158.47 45.54 61 8061 2135 1736524
Drug abuser 155.45 45.54 54 8068 1403 1737256
Drug use disorder 153.12 45.54 41 8081 423 1738236
Disturbance in attention 149.96 45.54 71 8051 4163 1734496
Drug withdrawal syndrome 148.48 45.54 72 8050 4453 1734206
Psychotic disorder 143.82 45.54 73 8049 4983 1733676
Drug ineffective 141.20 45.54 209 7913 63592 1675067
Alcohol abuse 138.43 45.54 40 8082 557 1738102
Disorientation 138.41 45.54 73 8049 5396 1733263
Restlessness 133.52 45.54 66 8056 4255 1734404
Insomnia 131.57 45.54 106 8016 16170 1722489
Metabolic acidosis 127.95 45.54 69 8053 5333 1733326
Logorrhoea 127.57 45.54 36 8086 458 1738201
Extrapyramidal disorder 123.04 45.54 52 8070 2325 1736334
Bradycardia 121.67 45.54 85 8037 10449 1728210
Neuroleptic malignant syndrome 121.39 45.54 56 8066 3092 1735567
Alcohol poisoning 117.35 45.54 34 8088 478 1738181
Arteriosclerosis coronary artery 110.09 45.54 45 8077 1847 1736812
Hypothermia 110.05 45.54 44 8078 1704 1736955
Bradyphrenia 108.63 45.54 34 8088 630 1738029
Drug screen positive 108.22 45.54 38 8084 1019 1737640
Salivary hypersecretion 103.20 45.54 40 8082 1425 1737234
Hepatocellular injury 101.73 45.54 50 8072 3181 1735478
Memory impairment 101.71 45.54 64 8058 6599 1732060
Suicidal ideation 101.30 45.54 70 8052 8448 1730211
Sinus tachycardia 100.61 45.54 46 8076 2486 1736173
Fall 100.46 45.54 115 8007 27099 1711560
Vomiting 98.43 45.54 135 7987 38180 1700479
Hyperhidrosis 93.84 45.54 78 8044 12410 1726249
Depression 93.13 45.54 88 8034 16581 1722078
Respiratory distress 92.69 45.54 55 8067 5102 1733557
Nystagmus 92.56 45.54 33 8089 926 1737733
Treatment noncompliance 92.26 45.54 55 8067 5146 1733513
Self-medication 91.36 45.54 30 8092 652 1738007
Hypoxia 90.31 45.54 57 8065 5906 1732753
Circulatory collapse 89.73 45.54 47 8075 3420 1735239
Drug diversion 87.63 45.54 23 8099 218 1738441
Serotonin syndrome 87.33 45.54 43 8079 2745 1735914
Hypotonia 86.78 45.54 36 8086 1534 1737125
Medication error 86.33 45.54 51 8071 4692 1733967
Accident 85.55 45.54 30 8092 801 1737858
Cardiomegaly 85.25 45.54 40 8082 2294 1736365
Gait disturbance 84.69 45.54 74 8048 12596 1726063
Blood creatine phosphokinase increased 82.99 45.54 63 8059 8793 1729866
Tension 80.40 45.54 23 8099 308 1738351
Hypoxic-ischaemic encephalopathy 79.73 45.54 29 8093 863 1737796
Drug withdrawal syndrome neonatal 79.20 45.54 27 8095 661 1737998
Foetal exposure during pregnancy 77.33 45.54 53 8069 6306 1732353
Drug withdrawal convulsions 74.99 45.54 21 8101 259 1738400
Psychomotor hyperactivity 73.97 45.54 34 8088 1859 1736800
Suicidal behaviour 73.46 45.54 22 8100 349 1738310
Thinking abnormal 72.22 45.54 30 8092 1282 1737377
Psychomotor skills impaired 70.07 45.54 21 8101 334 1738325
Dystonia 68.90 45.54 33 8089 1981 1736678
Mental status changes 67.71 45.54 48 8074 6027 1732632
Hallucination 67.59 45.54 54 8068 8116 1730543
Schizophrenia 65.40 45.54 32 8090 2014 1736645
Tremor 63.33 45.54 64 8058 13067 1725592
Self-injurious ideation 60.24 45.54 19 8103 361 1738298
Respiratory acidosis 60.12 45.54 22 8100 666 1737993
Apnoea 59.68 45.54 27 8095 1422 1737237
Generalised tonic-clonic seizure 59.55 45.54 38 8084 4008 1734651
Drug hypersensitivity 59.22 45.54 66 8056 15069 1723590
Drug level increased 58.90 45.54 33 8089 2744 1735915
Mydriasis 58.78 45.54 26 8096 1298 1737361
Tachypnoea 58.26 45.54 31 8091 2327 1736332
Alcohol interaction 58.24 45.54 18 8104 319 1738340
Sudden death 57.14 45.54 33 8089 2907 1735752
Acute kidney injury 57.09 45.54 100 8022 34844 1703815
Asthenia 56.36 45.54 99 8023 34571 1704088
Crystalluria 55.76 45.54 13 8109 71 1738588
Off label use 54.93 45.54 104 8018 38467 1700192
Catatonia 54.73 45.54 22 8100 863 1737796
Injury 54.29 45.54 32 8090 2928 1735731
Depressed mood 53.74 45.54 32 8090 2984 1735675
Ataxia 52.74 45.54 29 8093 2324 1736335
Poor quality sleep 51.64 45.54 23 8099 1167 1737492
Respiratory failure 51.23 45.54 60 8062 14445 1724214
Hepatic congestion 51.08 45.54 16 8106 297 1738362
Stupor 50.60 45.54 19 8103 619 1738040
Homicide 50.15 45.54 16 8106 316 1738343
Lethargy 50.07 45.54 43 8079 7141 1731518
Hyperthermia 49.75 45.54 25 8097 1666 1736993
Heart rate increased 49.55 45.54 41 8081 6469 1732190
Choking 48.11 45.54 21 8101 1015 1737644
Syncope 47.38 45.54 57 8065 14112 1724547
Patient restraint 46.92 45.54 9 8113 14 1738645
Encephalopathy 46.90 45.54 34 8088 4418 1734241
Delusion 45.92 45.54 26 8096 2205 1736454

Pharmacologic Action:

SourceCodeDescription
ATC N05BA01 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000777 Anesthetics
MeSH PA D018686 Anesthetics, Intravenous
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:35717 sedative
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D000927 Anticonvulsants
MeSH PA D000932 Antiemetics
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D011619 Psychotropic Drugs
FDA EPC N0000175694 Benzodiazepine
FDA CS M0002356 Benzodiazepines
MeSH PA D014149 Tranquilizing Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Alcohol withdrawal delirium indication 8635005
Anxiety indication 48694002
Sedation indication 72641008
Tetanus indication 76902006 DOID:11338
Epilepsy indication 84757009 DOID:1826
Alcohol withdrawal syndrome indication 191480000
Spasticity indication 221360009
Status epilepticus indication 230456007 DOID:1824
Induce Anterograde Amnesia indication
Preoperative Anxiety indication
Panic disorder off-label use 371631005 DOID:594
Cocaine-Associated Acute Ischemic Heart Disease off-label use
Disorder of lung contraindication 19829001 DOID:850
Alcohol intoxication contraindication 25702006
Depressive disorder contraindication 35489007
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Substance abuse contraindication 66214007
Sleep apnea contraindication 73430006 DOID:0050847
Decreased respiratory function contraindication 80954004
Open-angle glaucoma contraindication 84494001 DOID:1067
Myasthenia gravis contraindication 91637004 DOID:437
Hypoalbuminemia contraindication 119247004
Disease of liver contraindication 235856003 DOID:409
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.06 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 8927497 July 21, 2025 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER
5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 8927497 July 21, 2025 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER
7.5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 8927497 July 21, 2025 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER
10MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 9763876 March 27, 2029 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER
5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 9763876 March 27, 2029 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER
7.5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL 9763876 March 27, 2029 NASAL ADMINISTRATION OF DIAZEPAM FOR TREATMENT OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY IN PATIENTS 6 YEARS OF AGE AND OLDER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2023 NEW PRODUCT
5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2023 NEW PRODUCT
7.5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2023 NEW PRODUCT
10MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2027 INDICATED FOR THE ACUTE TX OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E. SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENT’S USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 6 YEARS OF AGE AND OLDER
5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2027 INDICATED FOR THE ACUTE TX OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E. SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENT’S USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 6 YEARS OF AGE AND OLDER
7.5MG/SPRAY VALTOCO NEURELIS INC N211635 Jan. 10, 2020 RX SPRAY NASAL Jan. 10, 2027 INDICATED FOR THE ACUTE TX OF INTERMITTENT, STEREOTYPIC EPISODES OF FREQUENT SEIZURE ACTIVITY (I.E. SEIZURE CLUSTERS, ACUTE REPETITIVE SEIZURES) THAT ARE DISTINCT FROM A PATIENT’S USUAL SEIZURE PATTERN IN PATIENTS WITH EPILEPSY 6 YEARS OF AGE AND OLDER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 7.14 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.85 WOMBAT-PK CHEMBL
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.70 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.94 WOMBAT-PK CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.96 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 8.00 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.20 WOMBAT-PK CHEMBL
GABA A receptor alpha-5/beta-3/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.20 WOMBAT-PK CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.71 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-2/gamma-3 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.67 WOMBAT-PK CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.65 WOMBAT-PK CHEMBL
Cytochrome P450 3A4 Enzyme Ki 4.42 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR ALLOSTERIC MODULATOR Ki 4.10 IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel Kd 7.64 CHEMBL
Adenosine receptor A3 GPCR IC50 7.92 CHEMBL
Translocator protein Membrane receptor Kd 6.67 CHEMBL
Cholinesterase Enzyme Ki 7.37 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 8.54 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 4.07 CHEMBL
GABA A receptor alpha-2/beta-2/gamma-2 Ion channel Ki 7.70 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-2 Ion channel Ki 7.82 CHEMBL
Thyrotropin-releasing hormone receptor GPCR ANTAGONIST Ki 5.15 IUPHAR
GABA-A receptor; alpha-1/beta-2/gamma-2 Ion channel Ki 7.92 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-1 Ion channel Ki 7.96 CHEMBL
Fatty acid-binding protein, liver Unclassified Ki 6.27 CHEMBL
Gamma-aminobutyric acid receptor subunit alpha-5 Ion channel Ki 8.01 CHEMBL
GABA-A receptor; anion channel Ion channel Ki 8 CHEMBL
GABA A receptor alpha-3/beta-2/gamma-2 Ion channel Ki 7.86 CHEMBL
Acetylcholinesterase Enzyme Ki 4.89 CHEMBL
GABA A receptor alpha-5/beta-3/gamma-2 Ion channel Ki 7.96 CHEMBL
GABA A receptor alpha-6/beta-2/gamma-2 Ion channel Ki 8.68 CHEMBL

External reference:

IDSource
D003975 MESH_DESCRIPTOR_UI
4017796 VUID
N0000146157 NUI
C0012010 UMLSCUI
D00293 KEGG_DRUG
387264003 SNOMEDCT_US
4573 MMSL
48546005 SNOMEDCT_US
4017796 VANDF
3322 RXNORM
001461 NDDF
d00148 MMSL
894 MMSL
CHEBI:49575 CHEBI
CHEMBL12 ChEMBL_ID
DB00829 DRUGBANK_ID
Q3JTX2Q7TU UNII
1295 INN_ID
3364 IUPHAR_LIGAND_ID
3016 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Diazepam Intensol HUMAN PRESCRIPTION DRUG LABEL 1 0054-3185 SOLUTION, CONCENTRATE 5 mg ORAL ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0054-3188 SOLUTION 5 mg ORAL ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6137 GEL 2.50 mg RECTAL NDA authorized generic 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6138 GEL 10 mg RECTAL NDA authorized generic 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0093-6139 GEL 20 mg RECTAL NDA authorized generic 13 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0004 TABLET 2 mg ORAL NDA 15 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0005 TABLET 5 mg ORAL NDA 15 sections
Valium HUMAN PRESCRIPTION DRUG LABEL 1 0140-0006 TABLET 10 mg ORAL NDA 15 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3925 TABLET 2 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3926 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0172-3927 TABLET 10 mg ORAL ANDA 14 sections
Diastat HUMAN PRESCRIPTION DRUG LABEL 1 0187-0658 GEL 10 mg RECTAL NDA 14 sections
Diastat HUMAN PRESCRIPTION DRUG LABEL 1 0187-0659 GEL 20 mg RECTAL NDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0271 TABLET 2 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0345 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0378-0477 TABLET 10 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-1273 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 15 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0409-3213 INJECTION, SOLUTION 5 mg INTRAMUSCULAR ANDA 13 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0527-1767 SOLUTION 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0527-1768 SOLUTION, CONCENTRATE 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-7799 TABLET 5 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-7800 TABLET 10 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0615-8049 TABLET 5 mg ORAL ANDA 12 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 0904-5880 TABLET 5 mg ORAL ANDA 15 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 10544-161 TABLET 10 mg ORAL ANDA 14 sections
Diazepam HUMAN PRESCRIPTION DRUG LABEL 1 11704-600 INJECTION 10 mg INTRAMUSCULAR NDA 14 sections
DIAZEPAM HUMAN PRESCRIPTION DRUG LABEL 1 12634-529 TABLET 5 mg ORAL ANDA 14 sections
DIAZEPAM HUMAN PRESCRIPTION DRUG LABEL 1 12634-698 TABLET 10 mg ORAL ANDA 14 sections
DIAZEPAM HUMAN PRESCRIPTION DRUG LABEL 1 16590-069 TABLET 2 mg ORAL ANDA 14 sections
DIAZEPAM HUMAN PRESCRIPTION DRUG LABEL 1 16590-070 TABLET 5 mg ORAL ANDA 14 sections