Substance
ID:933
Names and Identifiers
Synonyms
Praziquantel
IUPAC Traditional name
praziquantel
IUPAC name
2-cyclohexanecarbonyl-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolin-4-one
Brand Name
Biltricide
Properties
Physical Property
Solubility
400 mg/L
Hydrophobicity(logP)
2.5
Molecule Details
Drug Groups
approved
Description
An anthelmintic used in most schistosome and many cestode infestations. [PubChem]
Indication
For the treatment of infections due to all species of schistosoma.
Pharmacology
Praziquantel is an anthelmintic used in most schistosome and many cestode infestations. Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. The drug further causes vacuolization and disintegration of the schistosome tegument. The effect is more marked on adult worms compared to young worms. An increased calcium influx may play an important role. Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.
Biotransformation
renal
Absorption
Rapidly absorbed (80%)
Half Life
0.8-1.5 hours (in serum)
Protein Binding
80 to 85%
References
•
Doenhoff MJ, Cioli D, Utzinger J: Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis. Curr Opin Infect Dis. 2008 Dec;21(6):659-67.
[Pubmed]
•
McManus DP, Loukas A: Current status of vaccines for schistosomiasis. Clin Microbiol Rev. 2008 Jan;21(1):225-42.
[Pubmed]
External Links
Molecular Spectra
No Data Available
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References