lormetazepam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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 508.71 26.89 230 9412 64134 63415246
Drug abuse 485.55 26.89 231 9411 72287 63407093
Poisoning deliberate 334.12 26.89 106 9536 11112 63468268
Sopor 243.00 26.89 100 9542 22064 63457316
Drug dependence 220.27 26.89 96 9546 24387 63454993
Somnolence 208.29 26.89 190 9452 178495 63300885
Intentional overdose 185.39 26.89 124 9518 74028 63405352
Toxicity to various agents 171.78 26.89 199 9443 247051 63232329
Miosis 168.44 26.89 57 9585 7296 63472084
Drug interaction 156.71 26.89 183 9459 228948 63250432
Suicide attempt 154.93 26.89 103 9539 60815 63418565
Prescription form tampering 151.01 26.89 31 9611 547 63478833
Serotonin syndrome 115.23 26.89 65 9577 28617 63450763
Overdose 110.28 26.89 110 9532 114968 63364412
Vasoplegia syndrome 94.23 26.89 26 9616 1673 63477707
Rhabdomyolysis 92.09 26.89 66 9576 43885 63435495
Bradyphrenia 92.03 26.89 36 9606 6944 63472436
Depressed level of consciousness 90.19 26.89 75 9567 62003 63417377
Hypotension 89.05 26.89 153 9489 272451 63206929
Electrocardiogram QT prolonged 82.51 26.89 70 9572 59460 63419920
Confusional state 74.95 26.89 131 9511 236249 63243131
Fall 72.74 26.89 174 9468 392160 63087220
Asphyxia 71.47 26.89 29 9613 6152 63473228
Poisoning 68.77 26.89 36 9606 13664 63465716
Bradypnoea 67.67 26.89 24 9618 3526 63475854
Hypothermia 66.22 26.89 35 9607 13546 63465834
Pneumonia aspiration 65.83 26.89 49 9593 34491 63444889
Intentional product misuse 65.34 26.89 62 9580 60855 63418525
Respiratory acidosis 62.51 26.89 27 9615 6688 63472692
Hyponatraemia 61.13 26.89 80 9562 111820 63367560
Drug ineffective 53.92 26.89 48 9594 1044717 62434663
Bradykinesia 52.06 26.89 22 9620 5166 63474214
Hypokalaemia 51.77 26.89 71 9571 103733 63375647
Hypotonia neonatal 50.79 26.89 15 9627 1231 63478149
Bradycardia 49.03 26.89 58 9584 73169 63406211
Drug use disorder 46.26 26.89 20 9622 4964 63474416
Hypotonia 45.46 26.89 24 9618 9261 63470119
Thymus disorder 43.93 26.89 10 9632 291 63479089
Alkalosis hypochloraemic 43.88 26.89 9 9633 158 63479222
Substance abuse 43.67 26.89 19 9623 4788 63474592
Eosinophilic pustular folliculitis 42.71 26.89 7 9635 31 63479349
Rash 42.67 26.89 16 9626 560855 62918525
Eyelid myoclonus 41.25 26.89 8 9634 104 63479276
Wrong patient 40.89 26.89 9 9633 224 63479156
Disorientation 40.10 26.89 39 9603 39413 63439967
Acute kidney injury 39.51 26.89 108 9534 263307 63216073
Neurological examination abnormal 38.93 26.89 9 9633 281 63479099
Hypergammaglobulinaemia 38.48 26.89 10 9632 511 63478869
Pain 36.93 26.89 35 9607 740593 62738787
Victim of sexual abuse 35.78 26.89 10 9632 674 63478706
Altered state of consciousness 35.60 26.89 30 9612 25200 63454180
Mydriasis 34.72 26.89 22 9620 11934 63467446
Single umbilical artery 34.47 26.89 8 9634 254 63479126
Hepatic cytolysis 34.24 26.89 24 9618 15383 63463997
Cataplexy 33.80 26.89 11 9631 1245 63478135
Anterograde amnesia 33.26 26.89 9 9633 538 63478842
Hyperammonaemia 32.85 26.89 16 9626 5216 63474164
Cholestatic liver injury 32.78 26.89 13 9629 2597 63476783
Fatigue 31.78 26.89 54 9588 887974 62591406
Hepatocellular injury 31.51 26.89 29 9613 27352 63452028
Cardiogenic shock 30.98 26.89 24 9618 17908 63461472
Renal failure 30.64 26.89 60 9582 117592 63361788
Neuroleptic malignant syndrome 29.67 26.89 20 9622 12036 63467344
Genital infection female 29.66 26.89 6 9636 98 63479282
Sinus bradycardia 28.51 26.89 21 9621 14530 63464850
Lactic acidosis 28.42 26.89 32 9610 38255 63441125
Psychomotor retardation 27.85 26.89 13 9629 3857 63475523

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 340.99 23.63 157 5181 45521 34906072
Drug abuse 261.09 23.63 171 5167 98925 34852668
Drug dependence 114.00 23.63 61 5277 24156 34927437
Intentional overdose 101.62 23.63 70 5268 43604 34907989
Miosis 87.53 23.63 38 5300 9497 34942096
Poisoning deliberate 77.72 23.63 33 5305 7811 34943782
Somnolence 75.96 23.63 89 5249 111027 34840566
Toxicity to various agents 75.35 23.63 120 5218 200242 34751351
Respiratory distress 55.62 23.63 45 5293 35620 34915973
Drug use disorder 52.99 23.63 21 5317 4170 34947423
Sopor 52.68 23.63 29 5309 12107 34939486
Overdose 52.53 23.63 67 5271 90992 34860601
Suicide attempt 47.98 23.63 43 5295 39073 34912520
Drug interaction 47.96 23.63 106 5232 225840 34725753
Intentional self-injury 46.66 23.63 28 5310 13743 34937850
Pyramidal tract syndrome 46.56 23.63 10 5328 220 34951373
Serotonin syndrome 46.41 23.63 32 5306 19901 34931692
Hypoventilation 42.79 23.63 17 5321 3397 34948196
Bradypnoea 38.66 23.63 15 5323 2814 34948779
Hyperthermia 34.52 23.63 21 5317 10556 34941037
Respiratory depression 32.99 23.63 24 5314 16221 34935372
Rhabdomyolysis 32.88 23.63 46 5292 68117 34883476
Mydriasis 30.59 23.63 17 5321 7220 34944373
Persecutory delusion 29.40 23.63 12 5326 2568 34949025
Pneumonia aspiration 29.26 23.63 34 5304 41869 34909724
Asphyxia 28.74 23.63 16 5322 6819 34944774
Self-injurious ideation 26.87 23.63 10 5328 1674 34949919
Blood triglycerides increased 26.69 23.63 20 5318 14139 34937454
Withdrawal syndrome 26.66 23.63 19 5319 12436 34939157
Thrombocytopenic purpura 26.41 23.63 9 5329 1168 34950425
Drug ineffective 26.28 23.63 19 5319 456732 34494861
Hyperglycaemia 25.85 23.63 31 5307 39449 34912144
Squamous cell carcinoma 25.71 23.63 18 5320 11457 34940136
Impulse-control disorder 25.53 23.63 9 5329 1292 34950301

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 806.66 20.07 383 14039 100266 79629700
Drug abuse 600.22 20.07 370 14052 162321 79567645
Poisoning deliberate 376.91 20.07 138 14284 18690 79711276
Sopor 270.85 20.07 128 14294 32882 79697084
Intentional overdose 252.31 20.07 184 14238 105776 79624190
Drug dependence 242.36 20.07 127 14295 40642 79689324
Miosis 241.09 20.07 95 14327 15694 79714272
Somnolence 238.83 20.07 253 14169 238728 79491238
Toxicity to various agents 203.00 20.07 310 14112 421230 79308736
Suicide attempt 181.57 20.07 137 14285 82795 79647171
Drug interaction 162.42 20.07 278 14144 414905 79315061
Serotonin syndrome 149.26 20.07 96 14326 44931 79685035
Overdose 139.40 20.07 169 14253 184037 79545929
Rhabdomyolysis 107.72 20.07 112 14310 103019 79626947
Bradypnoea 97.94 20.07 38 14384 6014 79723952
Confusional state 92.79 20.07 188 14234 317809 79412157
Drug use disorder 91.27 20.07 40 14382 8611 79721355
Asphyxia 88.61 20.07 43 14379 11677 79718289
Pneumonia aspiration 87.11 20.07 82 14340 66885 79663081
Drug ineffective 86.67 20.07 44 14378 1080869 78649097
Bradyphrenia 83.35 20.07 40 14382 10600 79719366
Vasoplegia syndrome 81.54 20.07 29 14393 3601 79726365
Intentional product misuse 79.62 20.07 92 14330 95073 79634893
Respiratory acidosis 75.48 20.07 38 14384 11162 79718804
Depressed level of consciousness 75.15 20.07 90 14332 96562 79633404
Poisoning 74.26 20.07 50 14372 25222 79704744
Electrocardiogram QT prolonged 70.00 20.07 84 14338 90302 79639664
Intentional self-injury 65.26 20.07 51 14371 32368 79697598
Hypothermia 62.08 20.07 43 14379 22703 79707263
Mydriasis 61.86 20.07 39 14383 17604 79712362
Fall 55.74 20.07 204 14218 487425 79242541
Respiratory depression 54.60 20.07 43 14379 27587 79702379
Hyponatraemia 51.58 20.07 105 14317 177743 79552223
Hypokalaemia 51.56 20.07 93 14329 143947 79586019
Hypotension 50.96 20.07 185 14237 440132 79289834
Bradykinesia 44.75 20.07 24 14398 8019 79721947
Cardiogenic shock 44.57 20.07 46 14376 41868 79688098
Hyperthermia 44.36 20.07 32 14390 18005 79711961
Rash 44.04 20.07 25 14397 578333 79151633
Pain in extremity 43.35 20.07 7 14415 364531 79365435
Thymus disorder 42.32 20.07 10 14412 287 79729679
Persecutory delusion 40.11 20.07 19 14403 4890 79725076
Eyelid myoclonus 39.78 20.07 8 14414 105 79729861
Prescription form tampering 39.57 20.07 10 14412 382 79729584
Anterograde amnesia 38.38 20.07 11 14411 680 79729286
Hypotonia 36.70 20.07 25 14397 12845 79717121
Drug intolerance 36.53 20.07 3 14419 264116 79465850
Substance abuse 36.23 20.07 23 14399 10503 79719463
Pain 35.73 20.07 45 14377 703757 79026209
Neurological examination abnormal 35.40 20.07 10 14412 587 79729379
Pyramidal tract syndrome 35.40 20.07 10 14412 587 79729379
Respiratory distress 35.32 20.07 48 14374 58291 79671675
Wrong patient 35.23 20.07 9 14413 359 79729607
Cataplexy 35.11 20.07 11 14411 923 79729043
Hypersensitivity 33.60 20.07 4 14418 262235 79467731
Eosinophilic pustular folliculitis 33.34 20.07 7 14415 115 79729851
Hypergammaglobulinaemia 33.18 20.07 10 14412 737 79729229
Hepatic cytolysis 32.92 20.07 32 14390 27119 79702847
Alkalosis hypochloraemic 32.43 20.07 9 14413 495 79729471
Victim of sexual abuse 31.95 20.07 9 14413 523 79729443
Sinus bradycardia 31.07 20.07 30 14392 25217 79704749
Infusion related reaction 30.80 20.07 3 14419 230234 79499732
Acute kidney injury 30.60 20.07 179 14243 519225 79210741
Genital infection female 30.57 20.07 6 14416 69 79729897
Hypoventilation 30.53 20.07 18 14404 7206 79722760
Lactic acidosis 29.84 20.07 49 14373 70310 79659656
Pneumonia 29.72 20.07 46 14376 660200 79069766
Withdrawal syndrome 29.50 20.07 30 14392 26824 79703142
Arthralgia 28.54 20.07 37 14385 571766 79158200
Hyperglycaemia 28.51 20.07 48 14374 70287 79659679
Disorientation 28.37 20.07 45 14377 62731 79667235
Drug hypersensitivity 27.25 20.07 10 14412 298906 79431060
Neuroleptic malignant syndrome 27.07 20.07 29 14393 27530 79702436
Hepatocellular injury 27.07 20.07 38 14384 47555 79682411
Tachycardia 27.01 20.07 82 14340 177686 79552280
Fatigue 26.80 20.07 83 14339 929644 78800322
Product dose omission issue 26.76 20.07 6 14416 247531 79482435
Altered state of consciousness 26.44 20.07 36 14386 43786 79686180
Renal failure 26.25 20.07 88 14334 200880 79529086
Bradycardia 25.95 20.07 68 14354 135489 79594477
Faecaloma 25.03 20.07 19 14403 11545 79718421
Infection 23.94 20.07 7 14415 241705 79488261
White blood cell count decreased 23.80 20.07 3 14419 188285 79541681
Balance disorder 23.61 20.07 54 14368 98803 79631163
Anticholinergic syndrome 23.59 20.07 12 14410 3599 79726367
Hyperammonaemia 23.51 20.07 18 14404 11075 79718891
Cholestatic liver injury 22.71 20.07 13 14409 4928 79725038
Morbihan disease 22.69 20.07 4 14418 24 79729942
Generalised anxiety disorder 22.66 20.07 10 14412 2187 79727779
Congestive cardiomyopathy 22.55 20.07 18 14404 11762 79718204
Cough 22.43 20.07 20 14402 366769 79363197
Dyspnoea 22.28 20.07 80 14342 856945 78873021
Death 22.25 20.07 43 14379 566471 79163495
Gastroenteritis aeromonas 22.04 20.07 4 14418 29 79729937
Accidental poisoning 21.92 20.07 9 14413 1648 79728318
Xerophthalmia 21.41 20.07 7 14415 674 79729292
Hyperlactacidaemia 21.21 20.07 13 14409 5582 79724384
Blood pressure increased 21.15 20.07 6 14416 211354 79518612
Drug reaction with eosinophilia and systemic symptoms 21.10 20.07 40 14382 64204 79665762
Weight increased 21.05 20.07 12 14410 277374 79452592
Nystagmus 20.83 20.07 16 14406 9888 79720078
Loss of consciousness 20.58 20.07 72 14350 167871 79562095
Intellectual disability 20.34 20.07 8 14414 1312 79728654
Haemodynamic instability 20.16 20.07 20 14402 17362 79712604
Apraxia 20.12 20.07 10 14412 2857 79727109
Agitation 20.09 20.07 51 14371 99664 79630302

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:35717 hypnotics

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
CHEMBL399058 ChEMBL_ID
CHEMBL400001 ChEMBL_ID
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