lormetazepam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 1608 848-75-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lormetazepam
  • methyllorazepam
  • N-Methyllorazepam
  • Molecular weight: 335.18
  • Formula: C16H12Cl2N2O2
  • CLOGP: 2.40
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 52.90
  • ALOGS: -4.31
  • ROTB: 1

Drug dosage:

DoseUnitRoute
1 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 75 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.12 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.90 hours Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,CDK5,EIF2AK3,GRK2,PDK1,PDK2,PDK4 7
kinase-selectivity-class AXL,EIF2AK3,GRK2,PDK4 4
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

None

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
Coma 677.78 27.57 281 11818 72351 90543997
Drug abuse 640.51 27.57 280 11819 82067 90534281
Poisoning deliberate 499.11 27.57 153 11946 16333 90600015
Somnolence 336.94 27.57 254 11845 208830 90407518
Intentional overdose 276.47 27.57 166 11933 93668 90522680
Drug dependence 268.01 27.57 112 11987 29215 90587133
Sopor 248.53 27.57 101 11998 24543 90591805
Toxicity to various agents 245.33 27.57 243 11856 287603 90328745
Drug interaction 211.06 27.57 220 11879 276233 90340115
Drug use disorder 208.79 27.57 67 12032 8276 90608072
Prescription form tampering 201.02 27.57 40 12059 687 90615661
Miosis 192.43 27.57 65 12034 9419 90606929
Suicide attempt 190.46 27.57 121 11978 75278 90541070
Depressed level of consciousness 171.95 27.57 112 11987 72672 90543676
Poisoning 155.55 27.57 63 12036 15154 90601194
Hypotension 151.39 27.57 201 11898 325196 90291152
Overdose 122.75 27.57 127 11972 157582 90458766
Serotonin syndrome 113.92 27.57 68 12031 37819 90578529
Altered state of consciousness 111.82 27.57 63 12036 31469 90584879
Intentional product misuse 109.96 27.57 93 12006 89511 90526837
Bradyphrenia 107.99 27.57 40 12059 7572 90608776
Electrocardiogram QT prolonged 105.31 27.57 83 12016 72373 90543975
Rhabdomyolysis 97.46 27.57 69 12030 51187 90565161
Vasoplegia syndrome 93.12 27.57 28 12071 2786 90613562
Fall 93.12 27.57 201 11898 481609 90134739
Hypothermia 92.45 27.57 44 12055 15531 90600817
Asphyxia 88.70 27.57 34 12065 7069 90609279
Substance use disorder 88.53 27.57 25 12074 1995 90614353
Pneumonia aspiration 79.88 27.57 56 12043 40884 90575464
Bradypnoea 79.26 27.57 28 12071 4630 90611718
Hyponatraemia 70.53 27.57 88 12011 133450 90482898
Respiratory acidosis 64.16 27.57 28 12071 8091 90608257
Drug ineffective 63.85 27.57 55 12044 1384243 89232105
Confusional state 60.01 27.57 148 11951 386057 90230291
Acute kidney injury 59.86 27.57 132 11967 320255 90296093
Mucosal erosion 59.51 27.57 18 12081 1827 90614521
Hypokalaemia 57.72 27.57 79 12020 131037 90485311
Hepatic cytolysis 57.32 27.57 41 12058 30875 90585473
Bradycardia 57.16 27.57 63 12036 83784 90532564
Pancreatic failure 54.39 27.57 16 12083 1476 90614872
Mydriasis 53.22 27.57 30 12069 14982 90601366
Lactic acidosis 53.06 27.57 48 12051 50415 90565933
Bradykinesia 52.31 27.57 23 12076 6765 90609583
Abdominal discomfort 51.71 27.57 3 12096 477325 90139023
Hypotonia neonatal 50.66 27.57 15 12084 1415 90614933
Renal failure 50.36 27.57 74 12025 130933 90485415
Pain 50.36 27.57 36 12063 996305 89620043
Rash 49.93 27.57 22 12077 796078 89820270
Metabolic acidosis 49.04 27.57 48 12051 55628 90560720
Substance abuse 47.17 27.57 20 12079 5386 90610962
Hypotonia 46.46 27.57 25 12074 11401 90604947
Victim of sexual abuse 46.45 27.57 12 12087 683 90615665
Neuroleptic malignant syndrome 45.11 27.57 27 12072 15069 90601279
Disorientation 44.50 27.57 41 12058 44073 90572275
Thymus disorder 44.30 27.57 10 12089 320 90616028
Drug intolerance 42.47 27.57 5 12094 447586 90168762
Eyelid myoclonus 41.86 27.57 8 12091 110 90616238
Alkalosis hypochloraemic 41.63 27.57 9 12090 235 90616113
Genital erosion 40.93 27.57 10 12089 453 90615895
Hepatic perfusion disorder 39.44 27.57 7 12092 62 90616286
Wrong patient 39.34 27.57 11 12088 846 90615502
Fatigue 38.81 27.57 59 12040 1153964 89462384
Hypoglycaemia 38.41 27.57 47 12052 69801 90546547
Hypergammaglobulinaemia 38.01 27.57 10 12089 611 90615737
Drug hypersensitivity 37.65 27.57 8 12091 463601 90152747
Neurological examination abnormal 37.61 27.57 9 12090 373 90615975
Sinus bradycardia 37.34 27.57 25 12074 16927 90599421
Hepatic enzyme increased 36.92 27.57 3 12096 360733 90255615
Eosinophilic pustular folliculitis 36.64 27.57 7 12092 96 90616252
Haemodynamic instability 35.08 27.57 21 12078 11718 90604630
Accidental exposure to product by child 34.55 27.57 11 12088 1322 90615026
Single umbilical artery 33.54 27.57 8 12091 327 90616021
Anterograde amnesia 33.45 27.57 9 12090 600 90615748
Hepatocellular injury 33.33 27.57 29 12070 28929 90587419
Cataplexy 33.13 27.57 11 12088 1509 90614839
Neutrophil toxic granulation present 32.79 27.57 7 12092 172 90616176
Mouth ulceration 32.49 27.57 33 12066 39941 90576407
Hyperthermia 32.22 27.57 19 12080 10316 90606032
Infection 32.07 27.57 5 12094 362089 90254259
Hyperammonaemia 31.57 27.57 16 12083 6459 90609889
Cardiogenic shock 31.22 27.57 26 12073 24442 90591906
Intentional self-injury 31.02 27.57 28 12071 29306 90587042
Cognitive disorder 30.79 27.57 42 12057 69365 90546983
Vertigo 30.60 27.57 42 12057 69769 90546579
Toxic epidermal necrolysis 30.43 27.57 29 12070 32499 90583849
Psychomotor retardation 29.86 27.57 14 12085 4775 90611573
Genital infection female 29.72 27.57 6 12093 111 90616237
Cholestatic liver injury 29.69 27.57 13 12086 3784 90612564
Shock 29.51 27.57 27 12072 28751 90587597
Hepatitis fulminant 29.21 27.57 13 12086 3932 90612416
Weight increased 28.69 27.57 10 12089 417917 90198431
Hypoaesthesia 28.61 27.57 4 12095 314206 90302142

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
Coma 505.28 23.46 222 6827 53332 42560954
Drug use disorder 325.74 23.46 104 6945 10229 42604057
Drug abuse 308.92 23.46 200 6849 104571 42509715
Miosis 231.07 23.46 86 6963 13360 42600926
Substance use disorder 136.82 23.46 46 7003 5299 42608987
Drug dependence 136.15 23.46 75 6974 29019 42585267
Intentional overdose 126.54 23.46 88 6961 51368 42562918
Poisoning deliberate 121.62 23.46 50 6999 10084 42604202
Somnolence 120.91 23.46 132 6917 140973 42473313
Sopor 96.52 23.46 46 7003 13156 42601130
Toxicity to various agents 77.66 23.46 137 6912 228999 42385287
Serotonin syndrome 74.94 23.46 49 7000 25796 42588490
Drug interaction 66.36 23.46 140 6909 266859 42347427
Overdose 58.16 23.46 79 6970 105185 42509101
Suicide attempt 53.68 23.46 51 6998 46049 42568237
Respiratory distress 52.03 23.46 48 7001 41772 42572514
Intentional self-injury 51.98 23.46 32 7017 15170 42599116
Respiratory depression 50.39 23.46 34 7015 18834 42595452
Self-injurious ideation 43.56 23.46 15 7034 1853 42612433
Pyramidal tract syndrome 42.92 23.46 10 7039 296 42613990
Poisoning 42.91 23.46 28 7021 14671 42599615
Drug ineffective 42.57 23.46 26 7023 630171 41984115
Toxic encephalopathy 41.18 23.46 21 7028 6932 42607354
Hypoventilation 39.70 23.46 17 7032 3785 42610501
Intentional product misuse 39.65 23.46 50 6999 61850 42552436
Mydriasis 39.30 23.46 22 7027 8748 42605538
Bradypnoea 37.34 23.46 17 7032 4376 42609910
Altered state of consciousness 35.25 23.46 33 7016 29226 42585060
Asphyxia 34.92 23.46 20 7029 8306 42605980
Respiratory acidosis 34.27 23.46 18 7031 6313 42607973
Rhabdomyolysis 32.10 23.46 51 6998 77968 42536318
Neuroleptic malignant syndrome 31.36 23.46 27 7022 21445 42592841
Hyperthermia 29.67 23.46 21 7028 12553 42601733
Confusional state 29.56 23.46 77 6972 167520 42446766
Pneumonia aspiration 28.24 23.46 38 7011 50040 42564246
Agitation 27.78 23.46 43 7006 64271 42550015
Prescription form tampering 27.07 23.46 8 7041 604 42613682
Self-destructive behaviour 25.97 23.46 7 7042 378 42613908
Blood triglycerides increased 25.29 23.46 21 7028 15875 42598411
Therapeutic hypothermia 25.29 23.46 4 7045 12 42614274
Hypothermia 25.21 23.46 19 7030 12496 42601790
Persecutory delusion 24.76 23.46 12 7037 3552 42610734
Multi-organ disorder 24.59 23.46 9 7040 1327 42612959
Withdrawal syndrome 24.51 23.46 20 7029 14755 42599531
Rash 23.95 23.46 8 7041 276946 42337340
Cardio-respiratory arrest 23.65 23.46 38 7011 58598 42555688
Circulatory collapse 23.49 23.46 24 7025 23612 42590674

FDA Adverse Event Reporting System (Geriatric)

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
Coma 1138.54 22.62 498 17907 117371 110453523
Drug abuse 788.26 22.62 442 17963 176969 110393925
Poisoning deliberate 577.25 22.62 202 18203 26129 110544765
Drug use disorder 483.49 22.62 161 18244 17913 110552981
Miosis 415.00 22.62 151 18254 21832 110549062
Somnolence 400.42 22.62 357 18048 297092 110273802
Intentional overdose 365.92 22.62 244 18161 132257 110438637
Sopor 324.64 22.62 146 18259 36400 110534494
Drug dependence 295.49 22.62 151 18254 49869 110521025
Toxicity to various agents 283.69 22.62 373 18032 480182 110090712
Drug interaction 234.96 22.62 348 18057 499835 110071059
Substance use disorder 219.27 22.62 71 18334 7219 110563675
Suicide attempt 214.54 22.62 160 18245 103234 110467660
Serotonin syndrome 180.29 22.62 116 18289 59037 110511857
Poisoning 175.11 22.62 89 18316 29016 110541878
Overdose 163.75 22.62 198 18207 233596 110337298
Depressed level of consciousness 147.06 22.62 133 18272 112145 110458749
Altered state of consciousness 134.94 22.62 96 18309 57530 110513364
Intentional product misuse 129.85 22.62 134 18271 132770 110438124
Rhabdomyolysis 115.09 22.62 120 18285 120281 110450613
Asphyxia 111.12 22.62 52 18353 14163 110556731
Drug ineffective 110.66 22.62 58 18347 1520482 109050412
Bradypnoea 107.97 22.62 44 18361 8605 110562289
Hypothermia 101.54 22.62 60 18345 26242 110544652
Pneumonia aspiration 100.04 22.62 93 18312 81140 110489754
Bradyphrenia 98.21 22.62 45 18360 11683 110559211
Respiratory acidosis 94.14 22.62 46 18359 13780 110557114
Hypotension 93.94 22.62 243 18162 523606 110047288
Mydriasis 89.36 22.62 52 18353 22105 110548789
Confusional state 87.72 22.62 221 18184 468459 110102435
Electrocardiogram QT prolonged 83.97 22.62 97 18308 108863 110462031
Intentional self-injury 79.95 22.62 59 18346 37370 110533524
Vasoplegia syndrome 79.47 22.62 31 18374 5408 110565486
Respiratory depression 74.17 22.62 53 18352 31948 110538946
Neuroleptic malignant syndrome 73.45 22.62 54 18351 34005 110536889
Fall 70.04 22.62 240 18165 603242 109967652
Hypokalaemia 67.37 22.62 114 18291 182334 110388560
Renal failure 61.52 22.62 124 18281 226450 110344444
Hyperthermia 60.56 22.62 40 18365 21232 110549662
Hyponatraemia 58.95 22.62 119 18286 217534 110353360
Rash 58.48 22.62 32 18373 820932 109749962
Hepatic cytolysis 58.26 22.62 58 18347 54995 110515899
Pain in extremity 57.07 22.62 7 18398 487111 110083783
Haemodynamic instability 55.56 22.62 39 18366 22849 110548045
Pain 53.80 22.62 48 18357 954907 109615987
Nasopharyngitis 53.48 22.62 3 18402 394358 110176536
Drug intolerance 49.74 22.62 5 18400 406507 110164387
Substance abuse 49.59 22.62 29 18376 12434 110558460
Hypersensitivity 49.35 22.62 5 18400 403993 110166901
Lactic acidosis 48.31 22.62 68 18337 92743 110478151
Mucosal erosion 48.10 22.62 18 18387 2806 110568088
Prescription form tampering 47.25 22.62 12 18393 509 110570385
Hyperglycaemia 46.77 22.62 64 18341 85026 110485868
Drug hypersensitivity 45.47 22.62 10 18395 454080 110116814
Pancreatic failure 43.75 22.62 16 18389 2338 110568556
Acute kidney injury 43.63 22.62 215 18190 635215 109935679
Bradykinesia 42.65 22.62 25 18380 10763 110560131
Victim of sexual abuse 41.99 22.62 11 18394 528 110570366
Arthralgia 41.73 22.62 41 18364 779591 109791303
Respiratory distress 41.21 22.62 54 18351 68820 110502074
Infusion related reaction 41.09 22.62 7 18398 381155 110189739
Withdrawal syndrome 40.69 22.62 37 18368 31343 110539551
Fatigue 40.61 22.62 89 18316 1215869 109355025
Persecutory delusion 40.05 22.62 20 18385 6271 110564623
Toxic encephalopathy 39.45 22.62 27 18378 15187 110555707
Cardiogenic shock 39.12 22.62 48 18357 57290 110513604
Metabolic acidosis 39.03 22.62 64 18341 99680 110471214
Parkinsonism 38.67 22.62 31 18374 22156 110548738
Weight increased 38.60 22.62 11 18394 419633 110151261
Eyelid myoclonus 38.51 22.62 8 18397 136 110570758
Tachycardia 38.30 22.62 103 18302 226542 110344352
Infection 38.29 22.62 7 18398 362193 110208701
Hepatic perfusion disorder 37.80 22.62 7 18398 63 110570831
Pneumonia 37.47 22.62 55 18350 876659 109694235
Disorientation 37.10 22.62 52 18353 70619 110500275
Sinus bradycardia 36.75 22.62 34 18371 29449 110541445
Anterograde amnesia 36.56 22.62 11 18394 877 110570017
Thymus disorder 36.40 22.62 10 18395 576 110570318
Hypotonia 36.30 22.62 26 18379 15719 110555175
Bradycardia 36.24 22.62 80 18325 155437 110415457
Hypoaesthesia 35.62 22.62 5 18400 314218 110256676
Wrong patient 34.73 22.62 12 18393 1487 110569407
Congestive cardiomyopathy 33.98 22.62 24 18381 14195 110556699
Neurological examination abnormal 33.65 22.62 10 18395 764 110570130
Cataplexy 33.58 22.62 11 18394 1158 110569736
Genital erosion 33.19 22.62 10 18395 801 110570093
Pyramidal tract syndrome 32.76 22.62 10 18395 837 110570057
Self-destructive behaviour 32.67 22.62 10 18395 845 110570049
Product dose omission issue 32.37 22.62 7 18398 321775 110249119
Urticaria 31.95 22.62 7 18398 318850 110252044
Eosinophilic pustular folliculitis 31.82 22.62 7 18398 158 110570736
Alkalosis hypochloraemic 31.60 22.62 9 18396 592 110570302
Hypergammaglobulinaemia 31.55 22.62 10 18395 948 110569946
Maternal exposure during pregnancy 31.52 22.62 3 18402 254880 110316014
Self-injurious ideation 31.21 22.62 15 18390 4331 110566563
Asthma 30.80 22.62 3 18402 250288 110320606
Agitation 30.80 22.62 62 18343 112989 110457905
Musculoskeletal stiffness 30.46 22.62 5 18400 279817 110291077
Cognitive disorder 30.07 22.62 53 18352 87458 110483436
Hypoventilation 30.05 22.62 18 18387 8063 110562831
Genital infection female 29.97 22.62 6 18399 84 110570810
Lower respiratory tract infection 29.69 22.62 3 18402 243103 110327791
Hepatocellular injury 29.20 22.62 39 18366 50603 110520291
Bladder dilatation 29.05 22.62 12 18393 2427 110568467
Neutrophil toxic granulation present 28.98 22.62 7 18398 241 110570653
Hepatic enzyme increased 28.43 22.62 9 18396 320883 110250011
Balance disorder 27.19 22.62 60 18345 116500 110454394
Mobility decreased 26.39 22.62 4 18401 237418 110333476
Cough 26.17 22.62 23 18382 461618 110109276
Cerebellar syndrome 25.96 22.62 15 18390 6287 110564607
Hyperammonaemia 25.68 22.62 20 18385 13712 110557182
Anticholinergic syndrome 25.47 22.62 13 18392 4267 110566627
Brain death 25.37 22.62 15 18390 6558 110564336
Loss of consciousness 25.28 22.62 81 18324 196225 110374669
Cardio-respiratory arrest 25.20 22.62 58 18347 115778 110455116
Lip erosion 25.03 22.62 10 18395 1856 110569038
Cholestasis 24.70 22.62 41 18364 64477 110506417
Vertigo 24.09 22.62 48 18357 86822 110484072
Hypoglycaemia 24.02 22.62 57 18348 116047 110454847
Drug reaction with eosinophilia and systemic symptoms 23.53 22.62 46 18359 82049 110488845
Dyspnoea 23.32 22.62 100 18305 1106772 109464122
White blood cell count decreased 23.04 22.62 5 18400 229385 110341509
Morbihan disease 23.03 22.62 4 18401 24 110570870
Product prescribing error 22.92 22.62 35 18370 51296 110519598
Accidental exposure to product by child 22.85 22.62 11 18394 3187 110567707
Hypomagnesaemia 22.62 22.62 38 18367 60332 110510562

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05CD06 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:35717 sedative

Related Drugs by ATC class:

N05CD Benzodiazepine derivatives 14 drugs
brotizolamcinolazepamdoxefazepamestazolamflunitrazepamflurazepamloprazolammidazolamnimetazepamnitrazepamquazepamremimazolam show all 14 →

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.75 acidic
pKa2 0.26 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01657 KEGG_DRUG
C0065185 UMLSCUI
CHEBI:52993 CHEBI
CHEMBL22097 ChEMBL_ID
DB13872 DRUGBANK_ID
C023842 MESH_SUPPLEMENTAL_RECORD_UI
13314 PUBCHEM_CID
7553 IUPHAR_LIGAND_ID
4339 INN_ID
GU56C842ZA UNII
28894 RXNORM
004099 NDDF
387570005 SNOMEDCT_US
96233008 SNOMEDCT_US

Pharmaceutical products:

None