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

Stem definition	Drug id	CAS RN
diazepam derivatives	2240	2955-38-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: prazepam sedapran trepidan verstran prazene	A benzodiazepine that is used in the treatment of ANXIETY DISORDERS. Molecular weight: 324.81 Formula: C19H17ClN2O CLOGP: 3.93 LIPINSKI: 0 HAC: 3 HDO: 0 TPSA: 32.67 ALOGS: -4.91 ROTB: 3 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

prazepam
sedapran
trepidan
verstran
prazene

A benzodiazepine that is used in the treatment of ANXIETY DISORDERS.

Molecular weight: 324.81
Formula: C19H17ClN2O
CLOGP: 3.93
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 32.67
ALOGS: -4.91
ROTB: 3

Status: OFM

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

Drug dosage:

Dose	Unit	Route
30	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.08 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
None	FDA	PARKE DAVIS

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
Poisoning deliberate	394.06	37.57	99	3827	11119	63473977
Coma	311.74	37.57	125	3801	64239	63420857
Somnolence	181.21	37.57	121	3805	178564	63306532
Drug abuse	135.75	37.57	73	3853	72445	63412651
Altered state of consciousness	132.22	37.57	52	3874	25178	63459918
Suicide attempt	118.68	37.57	63	3863	60855	63424241
Intentional overdose	117.77	37.57	67	3859	74085	63411011
Drug dependence	102.63	37.57	43	3883	24440	63460656
Mydriasis	97.05	37.57	34	3892	11922	63473174
Toxicity to various agents	90.97	37.57	93	3833	247157	63237939
Hepatocellular injury	82.08	37.57	38	3888	27343	63457753
Hypotonia	77.63	37.57	27	3899	9258	63475838
Prothrombin time ratio decreased	64.64	37.57	13	3913	525	63484571
Sopor	64.05	37.57	30	3896	22134	63462962
Miosis	63.86	37.57	22	3904	7331	63477765
Electrocardiogram QT prolonged	61.68	37.57	41	3885	59489	63425607
Prescription form tampering	57.85	37.57	12	3914	566	63484530
Hypotension	57.29	37.57	77	3849	272527	63212569
Disturbance in attention	51.28	37.57	31	3895	38158	63446938
Respiratory acidosis	50.30	37.57	18	3908	6697	63478399
Overdose	41.63	37.57	43	3883	115035	63370061
Hypothermia	41.14	37.57	19	3907	13562	63471534
Vasoplegia syndrome	40.28	37.57	11	3915	1688	63483408
Hyperlactacidaemia	38.85	37.57	12	3914	2837	63482259
Prothrombin time shortened	38.53	37.57	11	3915	1984	63483112
Confusional state	38.20	37.57	59	3867	236321	63248775

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	212.71	35.76	84	1894	45594	34909359
Miosis	116.08	35.76	36	1942	9499	34945454
Somnolence	86.98	35.76	62	1916	111054	34843899
Drug abuse	81.47	35.76	57	1921	99039	34855914
Poisoning deliberate	80.44	35.76	26	1952	7818	34947135
Housebound	76.40	35.76	13	1965	225	34954728
Pneumonia aspiration	53.87	35.76	32	1946	41871	34913082
Bladder dilatation	47.60	35.76	12	1966	1480	34953473
Intentional overdose	40.18	35.76	27	1951	43647	34911306
Suicide attempt	37.96	35.76	25	1953	39091	34915862
Altered state of consciousness	36.12	35.76	20	1958	22873	34932080

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	491.92	29.65	207	5699	100442	79638040
Poisoning deliberate	435.16	29.65	124	5782	18704	79719778
Somnolence	259.81	29.65	181	5725	238800	79499682
Miosis	165.97	29.65	57	5849	15732	79722750
Altered state of consciousness	154.80	29.65	72	5834	43750	79694732
Suicide attempt	152.98	29.65	88	5818	82844	79655638
Drug abuse	146.13	29.65	110	5796	162581	79575901
Intentional overdose	135.54	29.65	89	5817	105871	79632611
Mydriasis	115.73	29.65	45	5861	17598	79720884
Hepatocellular injury	94.39	29.65	53	5853	47540	79690942
Toxicity to various agents	86.06	29.65	129	5777	421411	79317071
Respiratory acidosis	74.97	29.65	29	5877	11171	79727311
Drug dependence	74.37	29.65	43	5863	40726	79697756
Bladder dilatation	72.32	29.65	19	5887	2100	79736382
Housebound	63.88	29.65	13	5893	463	79738019
Hypotension	61.86	29.65	114	5792	440203	79298279
Electrocardiogram QT prolonged	59.42	29.65	51	5855	90335	79648147
Prothrombin time ratio decreased	55.28	29.65	13	5893	912	79737570
Disturbance in attention	53.74	29.65	38	5868	50763	79687719
Tachycardia	50.59	29.65	64	5842	177704	79560778
Sopor	50.26	29.65	31	5875	32979	79705503
Hypotonia	48.05	29.65	22	5884	12848	79725634
Pneumonia aspiration	42.40	29.65	37	5869	66930	79671552
Wrong patient received product	42.07	29.65	15	5891	4603	79733879
Overdose	41.21	29.65	59	5847	184147	79554335
Hyperkalaemia	38.73	29.65	45	5861	114353	79624129
Antipsychotic drug level increased	38.35	29.65	15	5891	5942	79732540
Confusional state	38.01	29.65	77	5829	317920	79420562
Vasoplegia syndrome	37.70	29.65	13	5893	3617	79734865
Fall	36.27	29.65	98	5808	487531	79250951
Drug ineffective	35.52	29.65	18	5888	1080895	78657587
Chronic actinic dermatitis	34.31	29.65	5	5901	21	79738461
Hypothermia	33.70	29.65	21	5885	22725	79715757
Retroplacental haematoma	32.62	29.65	6	5900	124	79738358
Prothrombin time shortened	31.37	29.65	11	5895	3217	79735265
Retinal vein occlusion	31.06	29.65	11	5895	3312	79735170
Cerebral haematoma	30.98	29.65	14	5892	7928	79730554
Limited symptom panic attack	30.66	29.65	5	5901	49	79738433
Gastrointestinal ischaemia	29.78	29.65	7	5899	490	79737992

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05BA11	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents

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

Disease	Relation	SNOMED_ID	DOID
Anxiety	indication	48694002
Insomnia	indication	193462001
Suicidal thoughts	contraindication	6471006
Disorder of lung	contraindication	19829001	DOID:850
Borderline personality disorder	contraindication	20010003	DOID:10930
Alcohol intoxication	contraindication	25702006
Shock	contraindication	27942005
Depressive disorder	contraindication	35489007
Substance abuse	contraindication	66214007
Psychotic disorder	contraindication	69322001
Sleep apnea	contraindication	73430006	DOID:0050847
Decreased respiratory function	contraindication	80954004
Kidney disease	contraindication	90708001	DOID:557
Hypoalbuminemia	contraindication	119247004
Disease of liver	contraindication	235856003	DOID:409
Sleep automatism	contraindication	247962006
Pregnancy, function	contraindication	289908002
Coma	contraindication	371632003
Porphyria	contraindication	418470004
Behavioral Disorders	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	2.89	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-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR				WOMBAT-PK	CHEMBL

External reference:

ID	Source
4018633	VUID
N0000146946	NUI
D00470	KEGG_DRUG
4018633	VANDF
C0032910	UMLSCUI
CHEBI:8362	CHEBI
CHEMBL969	ChEMBL_ID
DB01588	DRUGBANK_ID
D011222	MESH_DESCRIPTOR_UI
4890	PUBCHEM_CID
7275	IUPHAR_LIGAND_ID
1727	INN_ID
Q30VCC064M	UNII
8627	RXNORM
001459	NDDF
387417001	SNOMEDCT_US
74065006	SNOMEDCT_US

Pharmaceutical products:

None