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praziquantel 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anthelminthics (undefined group) | 2241 | 55268-74-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anthelmintic used in most schistosome and many cestode infestations.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 7 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.709 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.026 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 70.469 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 34.356 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 16.220 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 32.770 | % | High | 1 |
| herg | hERG pIC50 | 4.538 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 16.634 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 134.276 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 19.600 | % | High | 1 |
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.455 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 131.826 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 15.130 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 8.710 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 28.760 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 128.825 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 71.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 17.480 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 606.736 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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 |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:35443 | anthelminthic drug |
Related Drugs by ATC class:
P02BA Quinoline derivatives and related substances 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| 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 |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 4018263 | VUID |
| N0000146593 | NUI |
| D00471 | KEGG_DRUG |
| 4018263 | VANDF |
| C0032911 | UMLSCUI |
| CHEBI:45267 | CHEBI |
| PZQ | PDB_CHEM_ID |
| CHEMBL976 | ChEMBL_ID |
| DB01058 | DRUGBANK_ID |
| D011223 | MESH_DESCRIPTOR_UI |
| 4891 | PUBCHEM_CID |
| C078071 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3895 | INN_ID |
| 6490C9U457 | UNII |
| 8628 | RXNORM |
| 5344 | MMSL |
| 72429 | MMSL |
| d00349 | MMSL |
| 002962 | NDDF |
| 387310003 | SNOMEDCT_US |
| 55889005 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PRAZIQUANTEL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49884-231 | TABLET, FILM COATED | 600 mg | ORAL | ANDA | 23 sections |
| Biltricide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-747 | TABLET, FILM COATED | 600 mg | ORAL | NDA | 24 sections |
| Biltricide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76413-146 | TABLET, FILM COATED | 600 mg | ORAL | NDA | 20 sections |