zaleplon Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
imidazopyrimidine or pyrazolopyrimidine derivatives, used as anxiolytics, sedatives, hypnotics 2857 151319-34-5

Description:

MoleculeDescription

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: 1.43
  • 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:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 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) 0.94 ┬ÁM/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

Approvals:

DateAgencyCompanyOrphan
Aug. 13, 1999 FDA PFIZER

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 46.22 20.01 45 2185 145875 46537957
Somnambulism 23.86 20.01 9 2221 5028 46678804
Insomnia 23.75 20.01 34 2196 164890 46518942

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Insomnia 39.04 25.63 32 1243 93304 29857899
Anxiety 33.82 25.63 29 1246 89842 29861361
Depression 27.71 25.63 26 1249 90411 29860792

Pharmacologic Action:

SourceCodeDescription
ATC N05CF03 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine related drugs
FDA MoA N0000000196 GABA A Agonists
FDA PE N0000175728 Central Nervous System Depression
MeSH PA D000927 Anticonvulsants
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 D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35474 minor tranquilisers
CHEBI has role CHEBI:35488 cns depressants
CHEBI has role CHEBI:35623 antiepileptic
CHEBI has role CHEBI:35717 sedatives
FDA EPC N0000183360 gamma-Aminobutyric Acid A Receptor Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.81 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 6.53 WOMBAT-PK SCIENTIFIC LITERATURE
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR EC50 5.79 WOMBAT-PK CHEMBL

External reference:

IDSource
4021177 VUID
N0000148625 NUI
D00530 KEGG_DRUG
4021177 VANDF
C0288656 UMLSCUI
CHEBI:10102 CHEBI
CHEMBL1521 ChEMBL_ID
C085665 MESH_SUPPLEMENTAL_RECORD_UI
5719 PUBCHEM_CID
7312 INN_ID
S62U433RMH UNII
4345 IUPHAR_LIGAND_ID
DB00962 DRUGBANK_ID
261654 RXNORM
136698 MMSL
31278 MMSL
8288 MMSL
d04452 MMSL
007833 NDDF
116104009 SNOMEDCT_US
387012004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 42043-210 CAPSULE 5 mg ORAL ANDA 26 sections
Zaleplon HUMAN PRESCRIPTION DRUG LABEL 1 42043-211 CAPSULE 10 mg ORAL ANDA 26 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 43063-783 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 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
Zaleplon HUMAN PRESCRIPTION DRUG LABEL 1 66336-056 CAPSULE 5 mg ORAL ANDA 34 sections