All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,JAK3,KIT,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1	55
kinase-selectivity-class	AXL,DYRK1B,MAPK7,PDK4,STK33,TTK	6
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

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	219.37	52.34	59	634	72573	90555181
Pyramidal tract syndrome	75.48	52.34	11	682	548	90627206
Hepatocellular injury	70.57	52.34	20	673	28938	90598816
Poisoning deliberate	61.81	52.34	16	677	16470	90611284
Bundle branch block right	56.09	52.34	12	681	5441	90622313

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	65.10	51.00	24	466	53530	42567315
Rhabdomyolysis	56.34	51.00	24	466	77995	42542850
Miosis	54.01	51.00	15	475	13431	42607414

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	264.15	40.64	83	1165	117786	110470265
Miosis	95.47	40.64	26	1222	21957	110566094
Somnolence	75.87	40.64	45	1203	297404	110290647
Pyramidal tract syndrome	59.58	40.64	10	1238	837	110587214
Toxicity to various agents	58.44	40.64	46	1202	480509	110107542
Bradypnoea	55.70	40.64	14	1234	8635	110579416
Hepatocellular injury	55.42	40.64	21	1227	50621	110537430
Rhabdomyolysis	49.39	40.64	25	1223	120376	110467675
Poisoning deliberate	48.17	40.64	16	1232	26315	110561736
Acute kidney injury	41.71	40.64	43	1205	635387	109952664

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

Related Drugs by ATC class:

N05CD Benzodiazepine derivatives 14 drugs

brotizolamcinolazepamdoxefazepamestazolamflunitrazepamflurazepamlormetazepammidazolamnimetazepamnitrazepamquazepamremimazolam show all 14 →

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
759N8462G8	UNII
3033860	PUBCHEM_CID
235846	RXNORM
004097	NDDF
004098	NDDF
321119005	SNOMEDCT_US
395774003	SNOMEDCT_US
442011001	SNOMEDCT_US
70111-54-5	SECONDARY_CAS_RN

Pharmaceutical products:

None