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

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

Stem definition	Drug id	CAS RN
imidazopyrimidine or pyrazolopyrimidine derivatives, used as anxiolytics, sedatives, hypnotics	2857	151319-34-5

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: zaleplon sonata ZAL-846 CL 284,846 CL-284846

an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam Molecular weight: 305.34 Formula: C17H15N5O CLOGP: 1.80 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 74.29 ALOGS: -3.88 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.94 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	31 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.30 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	16 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.40 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.10 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.04 mg/mL	Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK5,CDK7,CDK9,CLK4,CSF1R,CSNK2A1,CSNK2A2,CSNK2A3,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,HIPK2,INSRR,IRAK1,ITK,JAK1,JAK2,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK15,MAPK7,MARK4,MET,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PIM3,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ULK1,ULK2	60
kinase-selectivity-class	CAMK2D,CDK9,CSNK2A2,DYRK1A,DYRK2,DYRK3,GSK3B,HIPK2,LRRK2,PIM3	10
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Aug. 13, 1999	FDA	PFIZER

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
Completed suicide	128.85	23.40	58	1477	145000	90481912
Somnambulism	35.66	23.40	10	1525	6218	90620694
Toxicity to various agents	35.24	23.40	33	1502	287813	90339099

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
Completed suicide	31.22	29.43	18	544	96447	42524326

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
Completed suicide	177.15	21.88	82	1616	242299	110345302
Somnambulism	36.35	21.88	10	1688	6395	110581206
Toxicity to various agents	35.31	21.88	40	1658	480515	110107086

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05CF03	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine related drugs
FDA MoA	N0000000196	GABA A Agonists
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D006993	Hypnotics and Sedatives
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators
FDA PE	N0000175728	Central Nervous System Depression
FDA EPC	N0000183360	gamma-Aminobutyric Acid A Receptor Agonist
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:35476	antipsychotic agent
CHEBI has role	CHEBI:35488	central nervous system depressant
CHEBI has role	CHEBI:35623	anticonvulsant
CHEBI has role	CHEBI:35717	sedative

Related Drugs by ATC class:

N05CF Benzodiazepine related drugs 3 drugs

eszopiclonezolpidemzopiclone

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

Disease	Relation	SNOMED_ID	DOID
Initial insomnia	indication	59050008
Disorders of initiating and maintaining sleep	indication	194437008
Depressive disorder	contraindication	35489007
Hepatic failure	contraindication	59927004
Sleep apnea	contraindication	73430006	DOID:0050847
Decreased respiratory function	contraindication	80954004
Sleep automatism	contraindication	247962006
Psychiatric Disturbance	contraindication
Chronic Obstructive Pulmonary Disease with Bronchospasms	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	3.81	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	POSITIVE ALLOSTERIC MODULATOR	EC50	5.79		WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	EC50	6.53		WOMBAT-PK	SCIENTIFIC LITERATURE

External reference:

ID	Source
4021177	VUID
N0000148625	NUI
D00530	KEGG_DRUG
4021177	VANDF
C0251504	UMLSCUI
CHEBI:10102	CHEBI
CHEMBL1521	ChEMBL_ID
DB00962	DRUGBANK_ID
C085665	MESH_SUPPLEMENTAL_RECORD_UI
5719	PUBCHEM_CID
4345	IUPHAR_LIGAND_ID
7312	INN_ID
S62U433RMH	UNII
261654	RXNORM
136698	MMSL
31278	MMSL
8288	MMSL
d04452	MMSL
007833	NDDF
116104009	SNOMEDCT_US
387012004	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0084	CAPSULE	5 mg	ORAL	ANDA	25 sections
Zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0085	CAPSULE	10 mg	ORAL	ANDA	25 sections
ZALEPLON	HUMAN PRESCRIPTION DRUG LABEL	1	21695-105	CAPSULE	10 mg	ORAL	NDA	24 sections
ZALEPLON	HUMAN PRESCRIPTION DRUG LABEL	1	21695-376	CAPSULE	5 mg	ORAL	NDA	24 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	29300-131	CAPSULE	5 mg	ORAL	ANDA	23 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	29300-132	CAPSULE	10 mg	ORAL	ANDA	23 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	33261-454	CAPSULE	10 mg	ORAL	ANDA	17 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	33261-486	CAPSULE	5 mg	ORAL	ANDA	17 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	42254-130	CAPSULE	5 mg	ORAL	ANDA	16 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	42254-147	CAPSULE	10 mg	ORAL	ANDA	16 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	42254-189	CAPSULE	5 mg	ORAL	ANDA	16 sections
ZALEPLON	HUMAN PRESCRIPTION DRUG LABEL	1	43063-505	CAPSULE	5 mg	ORAL	ANDA	26 sections
ZALEPLON	HUMAN PRESCRIPTION DRUG LABEL	1	43063-505	CAPSULE	5 mg	ORAL	ANDA	26 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	43063-783	CAPSULE	10 mg	ORAL	ANDA	23 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	43063-783	CAPSULE	10 mg	ORAL	ANDA	23 sections
Zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	43063-912	CAPSULE	10 mg	ORAL	ANDA	25 sections
Zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	43063-912	CAPSULE	10 mg	ORAL	ANDA	25 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	45865-541	CAPSULE	10 mg	ORAL	ANDA	24 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	50090-1564	CAPSULE	10 mg	ORAL	ANDA	23 sections
ZALEPLON	Human Prescription Drug Label	1	52959-957	CAPSULE	10 mg	ORAL	ANDA	23 sections
Sonata	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4431	CAPSULE	10 mg	ORAL	NDA	14 sections
Sonata	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5139	CAPSULE	5 mg	ORAL	NDA	14 sections
ZALEPLON	Human Prescription Drug Label	1	54868-5908	CAPSULE	10 mg	ORAL	ANDA	26 sections
ZALEPLON	Human Prescription Drug Label	1	54868-5909	CAPSULE	5 mg	ORAL	ANDA	26 sections
ZALEPLON	Human Prescription Drug Label	1	57237-239	CAPSULE	5 mg	ORAL	ANDA	26 sections
ZALEPLON	Human Prescription Drug Label	1	57237-240	CAPSULE	10 mg	ORAL	ANDA	26 sections
ZALEPLON	HUMAN PRESCRIPTION DRUG LABEL	1	61919-629	CAPSULE	10 mg	ORAL	ANDA	14 sections
zaleplon	HUMAN PRESCRIPTION DRUG LABEL	1	63629-3405	CAPSULE	10 mg	ORAL	ANDA	23 sections
ZALEPLON	Human Prescription Drug Label	1	65862-214	CAPSULE	5 mg	ORAL	ANDA	26 sections
ZALEPLON	Human Prescription Drug Label	1	65862-215	CAPSULE	10 mg	ORAL	ANDA	26 sections