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

Stem definition	Drug id	CAS RN
diazepam derivatives	1606	846-49-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ativan Wy 4036 Wy-4036 lorazepam	A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Molecular weight: 321.16 Formula: C15H10Cl2N2O2 CLOGP: 2.37 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 61.69 ALOGS: -4.26 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ativan
Wy 4036
Wy-4036
lorazepam

A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.

Molecular weight: 321.16
Formula: C15H10Cl2N2O2
CLOGP: 2.37
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 61.69
ALOGS: -4.26
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2.50	mg	O
2.50	mg	P
2.50	mg	SL

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	17 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.30 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	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)	0.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.08 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Sept. 30, 1977	FDA	VALEANT INTL

FDA Adverse Event Reporting System (Female)

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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
Sopor	2093.81	9.54	1291	290015	20873	63176843
Drug abuse	1256.05	9.54	1605	289701	70913	63126803
Completed suicide	595.15	9.54	1740	289566	143933	63053783
Suicide attempt	565.37	9.54	1008	290298	59910	63137806
Intentional overdose	450.86	9.54	1029	290277	73123	63124593
Somnolence	430.75	9.54	1792	289514	176893	63020823
Neuroleptic malignant syndrome	425.26	9.54	389	290917	11667	63186049
Intentional self-injury	421.60	9.54	554	290752	25133	63172583
Bradyphrenia	387.73	9.54	293	291013	6687	63191029
Agitation	380.83	9.54	845	290461	58912	63138804

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FDA Adverse Event Reporting System (Male)

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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
Sopor	859.15	10.31	579	152129	11557	34792666
Agitation	434.71	10.31	846	151862	56553	34747670
Neuroleptic malignant syndrome	433.08	10.31	460	152248	17474	34786749
Drug abuse	425.97	10.31	1168	151540	97928	34706295
Catatonia	334.77	10.31	231	152477	4794	34799429
Intentional self-injury	317.99	10.31	345	152363	13426	34790797
Bradyphrenia	301.96	10.31	213	152495	4585	34799638
Sedation	275.10	10.31	396	152312	20610	34783613
Psychotic disorder	273.22	10.31	428	152280	24024	34780199
Aggression	263.42	10.31	548	152160	38416	34765807

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FDA Adverse Event Reporting System (Geriatric)

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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
Sopor	2747.20	9.53	1775	364468	31235	79346910
Drug abuse	1495.34	9.53	2680	363563	160011	79218134
Completed suicide	828.54	9.53	2747	363496	243020	79135125
Neuroleptic malignant syndrome	798.55	9.53	798	365445	26761	79351384
Intentional self-injury	752.53	9.53	834	365409	31585	79346560
Agitation	695.56	9.53	1463	364780	98252	79279893
Suicide attempt	625.78	9.53	1257	364986	81675	79296470
Bradyphrenia	624.97	9.53	462	365781	10178	79367967
Somnolence	541.88	9.53	2354	363889	236627	79141518
Catatonia	529.63	9.53	387	365856	8369	79369776

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FDA Adverse Event Reporting System (Pediatric)

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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
Hypotonia neonatal	41.37	25.35	34	466	742	88550
Neonatal asphyxia	30.48	25.35	14	486	97	89195
Nasal congestion	26.02	25.35	9	491	25	89267

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Pharmacologic Action:

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Source	Code	Description
ATC	N05BA06	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
ATC	N05BA56	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
CHEBI has role	CHEBI:35717	hypnotics
FDA CS	M0002356	Benzodiazepines
FDA EPC	N0000175694	Benzodiazepine
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

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

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Disease	Relation	SNOMED_ID	DOID
Myoclonic seizure	indication	37356005
Atonic seizure	indication	42365007
Anxiety	indication	48694002
Absence seizure	indication	79631006
Lennox-Gastaut syndrome	indication	230418006
Status epilepticus	indication	230456007	DOID:1824
Panic disorder	indication	371631005	DOID:594
Sedation as Adjunct to Anesthesia	indication
Induce Anterograde Amnesia	indication
Delirium	off-label use	2776000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.09	acidic
pKa2	11.41	acidic
pKa3	0.63	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
1.5MG	LOREEV XR	ALMATICA	N214826	Feb. 16, 2022	RX	CAPSULE, EXTENDED RELEASE	ORAL	8999393	Jan. 8, 2034	ONCE DAILY TREATMENT OF ANXIETY DISORDER IN ADULTS
1MG	LOREEV XR	ALMATICA	N214826	Aug. 27, 2021	RX	CAPSULE, EXTENDED RELEASE	ORAL	8999393	Jan. 8, 2034	ONCE DAILY TREATMENT OF ANXIETY DISORDER IN ADULTS
2MG	LOREEV XR	ALMATICA	N214826	Aug. 27, 2021	RX	CAPSULE, EXTENDED RELEASE	ORAL	8999393	Jan. 8, 2034	ONCE DAILY TREATMENT OF ANXIETY DISORDER IN ADULTS
3MG	LOREEV XR	ALMATICA	N214826	Aug. 27, 2021	RX	CAPSULE, EXTENDED RELEASE	ORAL	8999393	Jan. 8, 2034	ONCE DAILY TREATMENT OF ANXIETY DISORDER IN ADULTS

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	IC50	8.46		WOMBAT-PK	CHEMBL
Fatty acid-binding protein, liver	Unclassified		FABPL_RAT		Ki	4.89		CHEMBL

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External reference:

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ID	Source
001460	NDDF
19225000	SNOMEDCT_US
202479	RXNORM
2104	MMSL
2809	INN_ID
3795	MMSL
387106007	SNOMEDCT_US
3958	PUBCHEM_CID
4017848	VUID
4017848	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0063	TABLET	0.50 mg	ORAL	NDA	20 sections
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0063	TABLET	0.50 mg	ORAL	NDA	20 sections
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0064	TABLET	1 mg	ORAL	NDA	20 sections
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0064	TABLET	1 mg	ORAL	NDA	20 sections
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0065	TABLET	2 mg	ORAL	NDA	20 sections
Ativan	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0065	TABLET	2 mg	ORAL	NDA	20 sections
Lorazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3532	SOLUTION, CONCENTRATE	2 mg	ORAL	ANDA	19 sections
Lorazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3532	SOLUTION, CONCENTRATE	2 mg	ORAL	ANDA	19 sections
Lorazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3425	TABLET	0.50 mg	ORAL	ANDA	21 sections
Lorazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3425	TABLET	0.50 mg	ORAL	ANDA	21 sections

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