Praziquantel

312.41

312.41

259-559-6

757285

DTXSID9021182

QP54AA54|QP52AA51|P - Antiparasitic products, insecticides and repellents

29339900

40.6

2.5

Solid

1.1209 (rough estimate)

136 °C

1377℃

>110°(230°F)

Freely soluble in ethanol or dichloromethane. Slightly soluble in water;ethanol: soluble 5mg/mL

−20°C

Oral-rat LD50; 2840 mg/kg; Oral-Mouse LD50: 2454 mg/kg

Flammable; burning produces toxic nitrogen oxide fumes

176.5 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

1

11-34

16-26-36/37/39-45-24/25

UQ4150000

F,C

Ventilated, low temperature and dry

Stable at normal temperatures and pressures.

P201, P202, P261, P264, P270, P271, P273, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P308+P313, P312, P322, P330, P363, P405, P501

H302

|Warning|H302 (12.05%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P273, P301+P312, P330, and P501|Aggregated GHS information provided by 85 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

moderately toxic

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.

80 to 85%

For the treatment of infections due to all species of schistosoma.|FDA Label|For cats with, or at risk from mixed infestations by cestodes, nematodes and ectoparasites. The veterinary medicinal product is exclusively indicated when all three groups are targeted at the same time.EctoparasitesTreatment and prevention of infestations by fleas (Ctenocephalides felis). Elimination of fleas within 24 hours. One treatment prevents further infestations for at least one month.Prevention of environmental flea contamination by inhibiting the development of flea immature stages (eggs, larvae and pupae) for over a month.The product can be used as part of a treatment strategy for the control of flea allergy dermatitis (FAD).Treatment and prevention of infestations by ticks (Ixodes ricinus). Elimination of ticks within 48 hours. One treatment prevents further infestations for up to 3 weeks.Treatment of notoedric mange (Notoedres cati).CestodesTreatment of infestations with tapeworms (Dipylidium caninum, Taenia taeniaeformis, Echinococcus multilocularis, Joyeuxiella pasqualei (adult), and Joyeuxiella fuhrmanni (adult)).NematodesTreatment of infestations with gastrointestinal nematodes (L3, L4 larvae and adults of Toxocara cati, adults of Toxascaris leonina, L4 larvae and adults of Ancylostoma tubaeforme and Ancylostoma ceylanicum, and adults of Ancylostoma brazilienze).Treatment of infestations with feline lungworms (L3 larvae, L4 larvae and adults of Aelurostrongylus abstrusus, L4 larvae and adults of Troglostrongylus brevior).Treatment of infestations with vesical worms (Capillaria plica).Prevention of heartworm disease (Dirofilaria immitis larvae) for one month.|CatsFor cats suffering from, or at risk from, mixed parasitic infections caused by roundworms and tapeworms of the following species:Roundworms (Nematodes)Toxocara cati (mature adult, immature adult, L4 and L3);Toxocara cati (L3 larvae) – treatment of queens during late pregnancy to prevent lactogenic transmission to the offspring;Toxascaris leonina (mature adult, immature adult and L4);Ancylostoma tubaeforme (mature adult, immature adult and L4).Tapeworms (Cestodes)Dipylidium caninum (mature adult and immature adult);Taenia taeniaeformis (adult);Echinococcus multilocularis (adult).LungwormsAelurostrongylus abstrusus (adult).DogsFor dogs suffering from, or at risk from, mixed parasitic infections caused by roundworms and tapeworms of the following species:Roundworms (nematodes):Toxocara canis (mature adult, immature adult, L4 and L3);Toxascaris leonina (mature adult, immature adult and L4);Ancylostoma caninum (mature adult and immature adult);Uncinaria stenocephala (mature adult and immature adult);Trichuris vulpis (mature adult, immature adult and L4);Tapeworms (Cestodes):Dipylidium caninum;Taenia spp.;Echinococcus multilocularis (mature adult and immature);Echinococcus granulosus (mature adult and immature).|For cats with, or at risk from mixed infections by cestodes, nematodes and ectoparasites. The veterinary medicinal product is exclusively indicated when all three groups are targeted at the same time.

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.

Anthelmintic Agents

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.

Agents that kill parasitic worms. They are used therapeutically in the treatment of HELMINTHIASIS in man and animal. (See all compounds classified as Anthelmintics.)

Rapidly absorbed (80%)

renal

0.8-1.5 hours (in serum)

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.

Biltricide

Veterinary drugs -> Broadline -> EMA Drug Category|Avermectins, Eprinomectin, combinations, Antiparasitic products, insecticides and repellents -> Veterinary pharmacotherapeutic group|Veterinary drugs -> Profender -> EMA Drug Category|Antiparasitic products, insecticides and repellents -> Veterinary pharmacotherapeutic group|Veterinary drugs -> NexGard Combo -> EMA Drug Category|Eprinomectin, combinations, Avermectins, Antiparasitic products, insecticides and repellents -> Veterinary pharmacotherapeutic group|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients|Pharmaceuticals -> Animal Drugs -> Approved in Taiwan