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Restrict the search for
praziquantel
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There is one exact (name or code) match for praziquantel
Status:
US Approved Rx
(1982)
Source:
NDA018714
(1982)
Source URL:
First approved in 1981
Source:
NADA111607
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Praziquantel, marketed as Biltricide, is an anthelmintic used in humans and animals for the treatment of tapeworms and flukes. Specifically, it is effective against schistosoma, Clonorchis sinensis the fish tape worm Diphyllobothrium latum. Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. 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. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis. Schistosome calcium ion channels are currently the only known target of praziquantel. The antibiotic rifampicin decreases plasma concentrations of praziquantel. Carbamazepine and phenytoin are reported to reduce the bioavailability of praziquantel. Chloroquine reduces the bioavailability of praziquantel. The drug cimetidine heightens praziquantel bioavailability.
Status:
US Approved Rx
(1982)
Source:
NDA018714
(1982)
Source URL:
First approved in 1981
Source:
NADA111607
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Praziquantel, marketed as Biltricide, is an anthelmintic used in humans and animals for the treatment of tapeworms and flukes. Specifically, it is effective against schistosoma, Clonorchis sinensis the fish tape worm Diphyllobothrium latum. Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. 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. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis. Schistosome calcium ion channels are currently the only known target of praziquantel. The antibiotic rifampicin decreases plasma concentrations of praziquantel. Carbamazepine and phenytoin are reported to reduce the bioavailability of praziquantel. Chloroquine reduces the bioavailability of praziquantel. The drug cimetidine heightens praziquantel bioavailability.
Status:
US Approved OTC
Source:
21 CFR 357.110 anthelmintic pyrantel pamoate
Source URL:
First approved in 1971
Class (Stereo):
CHEMICAL (ACHIRAL)
Pyrantel is an anthelmintic, which acts as an agonist of nicotinic receptors (AChRs) of nematodes and exerts its therapeutic effects by depolarizing their muscle membranes. It is used to treat a number of parasitic worm infections. This includes ascariasis, hookworm infections, enterobiasis (pinworm infection), trichostrongyliasis and trichinellosis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, headache and somnolence.
Status:
Investigational
Source:
INN:arpraziquantel [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Praziquantel, (-)- is oxopyrazinoisoquinoline derivative and a levorotated isomer of Praziquantel patented by Merck Patent G.m.b.H. as anthelmintics agent. In rabbits infested with S. japonicum, the therapeutic effect of Praziquantel, (-)-was greater than that of dl-praziquantel as rated by the number of the worms in tissues and by liver damage. Histopathological examination showed that liver egg granulomas in the levo-praziquantel group were fewer in no. and smaller in size and were predominantly composed of Pseudotubercles instead of eosinophilic abscesses. Levo-praziquantel is therapeutically superior to praziquantel, while dextro-praziquantel is almost ineffective.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Praziquantel, (+)- is the dextrorotated (+) isomer of Praziquantel. Praziquantel (PZQ) is the drug of choice against schistosomiasis. Since exposure of schistosomes to the drug is associated with calcium influx and muscular contraction, calcium channels have been suggested as the target. It is a specific pharmacological effect seen exclusively with the active levo-R(-)stereo isomer of the drug. Praziquantel, (+)- apparently contributes little to the therapeutic efficacy of Praziquantel. In vivo, single 400-mg/kg oral doses of Praziquantel, (-)- and Praziquantel, (+)- achieved worm burden reductions of 100 and 19%, respectively. Moreover, worms treated in vivo with Praziquantel, (+)- displayed an only transient hepatic shift and returned to the mesenteric veins within 24 h.
Status:
Possibly Marketed Outside US
Source:
NADA141275
(2007)
Source URL:
First approved in 2007
Source:
NADA141275
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Emodepside is a semi-synthetic product (originated by Astellas and out-licensed to Bayer for animal and human use); its precursor is synthesized by a fungus living in the leaves of Camellia japonica. It is a potent antihelminthic drug used in combination with praziquantel (as Profender®) and in combination with toltrazuril (as Procox®) for the treatment of parasitic worms in cats and dogs. Emodepside, a semi-synthetic derivative of PF1022A, belongs to a new class of anthelmintic drugs, the cyclooctadepsipeptides, and shows good efficacy against macrocyclic lactone-, levamisole- or benzimidazole-resistant nematode populations. Although putative receptors for emodepside have already been discovered, its mode of action is still not fully understood. It has being suggested that GABA(A)-receptor UNC-49 is associated with the emodepside mode of action. It has also being shown that Emodepside binds to a presynaptic latrophilin receptor in nematodes. The following presynaptic signal transduction occurs via activation of Gqalpha protein and phospholipase-Cbeta, which leads to mobilization of diacylglycerol (DAG). DAG then activates UNC-13 and synaptobrevin, two proteins which play an important role in presynaptic vesicle-functioning. This finally leads to the release of a currently unidentified transmitter. The transmitter (or modulator) exerts its effects at the postsynaptic membrane and induces a flaccid paralysis of the pharynx and the somatic musculature in nematodes.
