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

Stem definition	Drug id	CAS RN
diazepam derivatives	1602	61197-73-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

loprazolam mesylate
loprazolam
loprazolam mesilate

Molecular weight: 464.91
Formula: C23H21ClN6O3
CLOGP: 0.43
LIPINSKI: 0
HAC: 9
HDO: 0
TPSA: 97.33
ALOGS: -3.71
ROTB: 3

Drug dosage:

Dose	Unit	Route
1	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1983	YEAR INTRODUCED

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	167.10	48.62	48	518	64316	63424140
Pyramidal tract syndrome	78.56	48.62	11	555	352	63488104
Hepatocellular injury	68.71	48.62	20	546	27361	63461095
Bundle branch block right	55.32	48.62	12	554	4986	63483470
Bradypnoea	53.50	48.62	11	555	3539	63484917
Somnolence	51.59	48.62	27	539	178658	63309798
Miosis	50.71	48.62	12	554	7341	63481115

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
Rhabdomyolysis	58.54	50.76	24	396	68139	34888372

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	191.33	37.21	65	985	100584	79642754
Miosis	90.45	37.21	24	1026	15765	79727573
Somnolence	78.71	37.21	45	1005	238936	79504402
Pyramidal tract syndrome	61.54	37.21	10	1040	587	79742751
Bradypnoea	58.53	37.21	14	1036	6038	79737300
Hepatocellular injury	53.58	37.21	21	1029	47572	79695766
Toxicity to various agents	53.36	37.21	44	1006	421496	79321842
Rhabdomyolysis	49.45	37.21	25	1025	103106	79640232

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CD11	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives

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

Disease	Relation	SNOMED_ID	DOID
Insomnia	indication	193462001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.28	Basic
pKa2	4.28	Basic
pKa3	2.6	Basic
pKa4	1.98	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN					WOMBAT-PK
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN					WOMBAT-PK
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN					WOMBAT-PK
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN					WOMBAT-PK

External reference:

ID	Source
D07326	KEGG_DRUG
C0077013	UMLSCUI
CHEBI:135754	CHEBI
CHEMBL2107448	ChEMBL_ID
DB13643	DRUGBANK_ID
4884	INN_ID
70111-54-5	SECONDARY_CAS_RN
759N8462G8	UNII
3033860	PUBCHEM_CID
235846	RXNORM
004097	NDDF
004098	NDDF
321119005	SNOMEDCT_US
395774003	SNOMEDCT_US
442011001	SNOMEDCT_US

Pharmaceutical products:

None