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Praziquantel is a pyrazino-isoquinolein derivative from the thioxantonic group used as a broad anthelmintic spectrum. Specifically, it is known as a treatment of trematodes and cestodes infections such as schistosomiasis, taeniasis, and cysticercosis. 5 The efficacy of praziquantel in treating parasitic flatworms infection with low cost (~US$0.20 drug cost to treat a child) makes it an integral to WHO's plan to eliminate schistosomiasis by 2030. 6 , 7 Despite being approved since 1980, the exact mechanism of action is yet to be elucidated. 7
Praziquantel is an anthelmintic medication used to treat parasitic worm infections such as schistosomiasis, clonorchiasis, and opisthorchiasis
- Indication
- Associated Conditions
- Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose FormTreatment ofClonorchiasis••••••••••••••••••Treatment ofOpisthorchiasis••••••••••••••••••Treatment ofOpisthorchiasis••••••••••••••••••Treatment ofSchistosomiasis••••••••••••••••••Treatment ofSchistosomiasis••••••••••••••••••
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- Pharmacodynamics
In vitro studies on trematodes and cestodes have shown that praziquantel induces a rapid contraction of schistosomas by a specific effect on the permeability of the cell membrane. 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 Ca2+-influx may play an important role.9
Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is specific to trematodes and cestodes; nematodes (including filariae) are not affected.9
Praziquantel is active against schistosoma (for example, Schistosoma mekongi, Schistosoma japonicum, Schistosoma mansoni and Schistosoma hematobium), and infections due to the liver flukes, Clonorchis sinensis/Opisthorchis viverrini. Published in vitro data have shown a potential lack of efficacy of praziquantel against migrating schistosomulae.10
An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks.1
- Mechanism of action
Although the exact mechanism of action is unknown, praziquantel was hypothesized to target the β subunits of voltage-gated Ca2+ channels, particularly in Schistosoma mansoni and Schistosoma japonicum, due to the lack of two conserved serine residues in these subunits. This is supported by the finding that co-administration of calcium channel blockers like nicarpidine and nifedipine renders 50% of Schistosoma mansoni resistant to praziquantel.10,1
Increased exposure of antigens on the worm surface was also observed, but little research has been done to elucidate on the mechanism of action.1
TargetActionsOrganismA
Schistosome calcium ion (Ca2+) channelsother/unknown
Schistosoma- Absorption
After oral administration of praziquantel, about 80% of the dose is absorbed. In subjects with normal hepatic function who received 40 mg/kg of praziquantel under fasting conditions, the mean ± SD Cmax and AUC were 0.83 ± 0.52 µg/mL and 3.02 ± 0.59 µg/mL x hr. The Tmax was 1.48 ± 0.74 hours.10
- Volume of distribution
Following a single oral dose of 40 mg/kg of praziquantel in healthy volunteers, the volume of distribution was estimated to be 7695 ± 2716 L.4
- Protein binding
Approximately 80% of praziquantel is bound exclusively to albumin.3
- Metabolism
Praziquantel is rapidly metabolized by the cytochrome P450 enzyme system and undergoes a first-pass effect after oral administration.10
Additional reading:
CAS 124878-55-3 2-Iodo-1-Phenyl-Pentane-1-One with ...
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- Route of elimination
Approximately 80% of an oral dose of praziquantel is excreted in the kidneys, almost exclusively (greater than 99%) in the form of praziquantel metabolites.10
- Half-life
Following oral administration, the elimination half-life of praziquantel in serum ranges between 0.8 to 1.5 hours.10
- Clearance
Following a single oral dose of 40 mg/kg of praziquantel in healthy volunteers, the clearance was estimated to be 11.4 ± 2.8 L/kg/h.4
- Adverse Effects
- Toxicity
The acute toxicity of praziquantel is relatively low, as demonstrated by oral LD50 values ranging between 200 - 2976 mg/kg in various species.9
Published studies have not identified an association between praziquantel use during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies conducted in pregnant rats and rabbits no adverse developmental outcomes were observed with oral administration of praziquantel during organogenesis at approximately 0.65 times (rats) or 1.3 times (rabbits) the highest recommended human daily dose of 75 mg/kg/day, based on body surface area.10
Mutagenicity studies of praziquantel published in the scientific literature are inconclusive. Long-term oral carcinogenicity studies in rats and golden hamsters did not reveal any carcinogenic effect at doses up to 250 mg/kg/day (about half of the human daily dose based on body surface area). Praziquantel had no effect on fertility and general reproductive performance of male and female rats when given at oral doses ranging from 30 to 300 mg/kg body weight (up to 0.65 times the human daily dose based on body surface area).10
- Pathways
Not Available
- Pharmacogenomic Effects/ADRs
Not Available
Praziquantel is an anthelmintic agent with activity against a broad spectrum of trematodes and cestodes that is used predominantly in the therapy of schistosomiasis, liver flukes, and cysticercosis. Praziquantel therapy has been reported to cause serum aminotransferase elevations during therapy, but clinically apparent liver injury after its use is rare if it occurs at all.
Praziquantel (praz" i kown' tel) is a heterocyclic prazino-isoquinoline derivative with a broad spectrum of activity against several trematodes (Fasciola, Schistosoma) and cestodes (Taenia). Praziquantel is believed to act by interference with tegument calcium transport, resulting in paralysis of the parasitic worms with subsequent loss of adherence to tissue, degradation and expulsion. Praziquantel was approved for use in the United States in 1982 for schistosomiasis and subsequently for clonorchiasis. Praziquantel is also commonly used in veterinary medicine. Praziquantel is available for human use in tablets of 600 mg generically and under the brand name Biltricide. The typical dose for treating schistosomiasis in adults is 20 mg/kg (depending upon the species) three times over one day. The dose for treating clonorchiasis is 25 mg/kg three times over one day. Side effects are common but transient, and include abdominal discomfort, nausea, vomiting, vertigo, muscle aches, drowsiness, headaches and fatigue, some of the symptoms being due to its effects on the parasites. Serious adverse events include transient clinical deterioration, cardiac arrhythmias, hypersensitivity reactions and rash.
Hepatotoxicity
Praziquantel therapy has been associated with elevations in serum aminotransferase levels in up to 27% of patients, but these abnormalities were self-limiting. Praziquantel has been rarely associated with clinically apparent liver injury, which generally accompanied hypersensitivity reactions such as rash and fever. In a large retrospective survey from China, 2 of 25,000 treated patients were reported to have developed jaundice after praziquantel therapy, but no specific information about the two cases was provided. There have been few studies of long term therapy with praziquantel, and most controlled trials of this agent have used one day courses without serum aminotransferase monitoring. However, millions of people have been treated with praziquantel as a part of large scale control strategies in China where schistosomiasis Japonica is endemic. The combination of praziquantel preventive therapy and snail control has resulted in marked decreases in the prevalence of infection in the population with no evidence of significant toxicity. Thus, mild acute liver injury can accompany systemic hypersensitivity reactions to praziquantel, but both the allergic reaction and the liver injury tend to be short-lived and resolve rapidly even without specific therapy.
Likelihood score: D (possible rare cause of clinically apparent liver injury usually as a part of a systemic hypersensitivity reaction).
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