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

Stem definition	Drug id	CAS RN
diazepam derivatives	1608	848-75-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
1	mg	O

ADMET properties:

Property	Value	Reference
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
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:

Source	Code	Description
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 level	Dissociation constant	Type (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:

ID	Source
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