praziquantel ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
anthelminthics (undefined group) 2241 55268-74-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • praziquantel
  • (+/-)-Praziquantel
  • azinox
  • cysticide
  • distocide
  • prazinon
  • pyquiton
  • saniquantrel
An anthelmintic used in most schistosome and many cestode infestations.
  • Molecular weight: 312.41
  • Formula: C19H24N2O2
  • CLOGP: 3.36
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 40.62
  • ALOGS: -2.91
  • ROTB: 1

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
3 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.40 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 240.07 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 7 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1982 FDA BAYER HLTHCARE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC P02BA01 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTHELMINTICS
ANTITREMATODALS
Quinoline derivatives and related substances
FDA EPC N0000175481 Anthelmintic
MeSH PA D000871 Anthelmintics
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000977 Antiparasitic Agents

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

DiseaseRelationSNOMED_IDDOID
Opisthorchiasis indication 1059007 DOID:13768
Infection by Schistosoma indication 10087007
Clonorchiasis due to C. Sinensis indication
Schistosomiasis due to S. Mekongi indication
Schistosomiasis due to S. Haematobium indication
Schistosomiasis due to S. Japonicum indication
Schistosomiasis due to S. Mansoni indication
Heart disease contraindication 56265001 DOID:114
Seizure disorder contraindication 128613002
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Ocular Cysticercosis contraindication




๐Ÿถ Veterinary Drug Use

SpeciesUseRelation
Cats Removal of cestodes, Dipylidium caninum Indication
Cats Removal of cestodes, Taenia taeniaeformis Indication
Dogs Removal of cestodes, Dipylidium caninum Indication
Dogs Removal of cestodes, Taenia pisiformis Indication
Dogs Removal of cestodes, Echinococcus granulosus Indication
Dogs Removal and control of cestode, Echinococcus multilocularis Indication
Horses Treatment and control of Tapeworms, Anoplocephala perfoliata Indication

๐Ÿถ Veterinary products

ProductApplicantIngredients
Droncit 5.68% Injectible Solution Elanco US Inc. 1
Droncit Canine Cestocide Tablets, Droncit Feline Cestocide Tablets, Praziquantel 34 (Rx), Tapeworm Dewormer for Cats (OTC), Tapeworm Dewormer for Dogs (OTC) Elanco US Inc. 1
Vercom Paste Anthelmintic Elanco US Inc. 2
Drontal Plus, Drontal Plus Taste Tabs, Quad Dewormer Elanco US Inc. 3
Drontal Tablets Elanco US Inc. 2
ZIMECTERIN Gold Paste Boehringer lngelheim Animal Health USA Inc. 2
Equimax Virbac AH Inc. 2
Quest Plus Gel Zoetis Inc. 2
Iverhart Max Virbac AH Inc. 3
Sentry HC Worm X Plus Virbac AH Inc. 2
Profender Elanco US Inc. 2
Panacur Plus Intervet Inc. 3
Sentinel Spectrum Intervet Inc. 3
INTERCEPTOR PLUS Elanco US Inc. 2
Duocare Boehringer lngelheim Animal Health USA Inc. 2
IVERHART MAX Chew Virbac AH Inc. 3
Centragard Boehringer lngelheim Animal Health USA Inc. 2
Prazitech Bimeda Animal Health Limited 1
Prazi-C Tablets (OTC), Praziquantel Tablets (Rx) Cronus Pharma Specialities India Private Limited 1
Praziquantel Injection Bimeda Animal Health Limited 1

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Bile salt export pump Transporter IC50 4.01 CHEMBL
High voltage-activated calcium channel beta subunit CavB1 Ion channel BLOCKER CHEMBL CHEMBL
High voltage-activated calcium channel beta subunit CavB2 Ion channel BLOCKER CHEMBL CHEMBL
Glutathione S-transferase class-mu 26 kDa isozyme Enzyme WOMBAT-PK

External reference:

IDSource
4018263 VUID
N0000146593 NUI
D00471 KEGG_DRUG
4018263 VANDF
C0032911 UMLSCUI
CHEBI:91583 CHEBI
PZQ PDB_CHEM_ID
CHEMBL976 ChEMBL_ID
DB01058 DRUGBANK_ID
D011223 MESH_DESCRIPTOR_UI
C078071 MESH_SUPPLEMENTAL_RECORD_UI
4891 PUBCHEM_CID
3895 INN_ID
6490C9U457 UNII
8628 RXNORM
5344 MMSL
72429 MMSL
d00349 MMSL
002962 NDDF
387310003 SNOMEDCT_US
55889005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PRAZIQUANTEL HUMAN PRESCRIPTION DRUG LABEL 1 49884-231 TABLET, FILM COATED 600 mg ORAL ANDA 22 sections
Biltricide HUMAN PRESCRIPTION DRUG LABEL 1 50419-747 TABLET, FILM COATED 600 mg ORAL NDA 23 sections
Biltricide HUMAN PRESCRIPTION DRUG LABEL 1 50419-747 TABLET, FILM COATED 600 mg ORAL NDA 23 sections
Biltricide HUMAN PRESCRIPTION DRUG LABEL 1 76413-146 TABLET, FILM COATED 600 mg ORAL NDA 20 sections