吡喹酮（，或）為一種用於人類及動物的驅蟲藥，專門治療絛蟲及吸蟲。對於血吸蟲、中華肝吸蟲、廣節裂頭絛蟲特別有效，吡喹酮為世界衛生組織基本藥物標準清單上的藥物，為世界上對於基本公共衛生最重要的藥物之一。1970 年代由拜耳公司的藥學部研發成功。 醫療用途 吡喹酮可以用於治療人類、哺乳類，以及魚類的寄生蟲病。包含腸胃道或是外部的感染，以下為其適用疾病： 包蟲症：為包囊蟲幼蟲所引起的感染症。 豬囊尾蚴病：為豬肉絛蟲幼蟲感染腦部或肌肉所引起的疾病（但在腦囊蟲病則以阿苯達唑效果較佳） Feline caused in cats by gastrointestinal infection with adult tapeworms of the species used either alone or in combination with in cats and dogs whose gut is infected with the roundwormsnematodes or respectively use is often combined with pyrantel Schistosomiasis caused by trematodes of the genus SchistosomaAs of 2005 praziquantel is the primary treatment for human schistosomiasis for which it is usually effective in a single dose brought on by the Chinese liver fluke Clonorchis sinensis caused by infection with lung flukes mostly of the species Paragonimus westermani Fasciolopsiasis caused by intestinal fluke Fasciolopsis buski and other Trematoda infections of many fish species 副作用 The majority of side effects develop due to the release of the contents of the parasites as they are killed and the consequent host immune reaction The heavier the parasite burden the heavier and more frequent the side effects normally are Central nervous system Frequently occurring side effects are dizziness headache and malaise Drowsiness somnolence fatigue and vertigo have also been seen Almost all patients with cerebral cysticercosis experience CNS side effects related to the celldeath of the parasites headache worsening of preexisting neurological problems and These side effects may be lifethreatening and can be reduced by coadministration of corticosteroids It is strongly recommended that all patients with cerebral cysticercosis are hospitalized during treatment GI Tract Approximately 90 of all patients have abdominal pain or cramps with or without nausea and vomiting Diarrhea may develop and may be severe with colic Sweating fever and sometimes bloody stools may occur together with diarrhea Liver Asymptomatic and transient increases of liver enzymes AST and ALT are noted frequently up to 27 No case of symptomatic liver damage has ever been seen so far Sensitivity reactions Urticaria rash pruritus and in white blood cell counts Other locationsbody as a whole Lower back pain myalgia arthralgia fever sweating various cardiac arrhythmias and hypotension Drug interactions 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 Mechanism of action The mode of action is not exactly known at present but experimental evidence indicates praziquantel increases the permeability of the membranes of schistosome cells towards calcium ions The drug thereby induces contraction of the parasites resulting in paralysis in the contracted state The dying parasites are dislodged from their site of action in the host organism and may enter systemic circulation or may be destroyed by host immune reaction phagocytosis Additional mechanisms including focal disintegrations and disturbances of oviposition laying of eggs are seen in other types of sensitive parasites Another hypothesis concerning the mechanism of action of praziquantel has been recently reported The drug seems to interfere with adenosine uptake in cultured worms This effect may have therapeutical relevance given that the schistosome as the and the other praziquantelsensitive parasites is unable to synthesize purines such as adenosine de novo Bayers Animal Health Division website states Praziquantel is active against cestodes tapeworms Praziquantel is absorbed metabolized in the liver and excreted in the bile Upon entering the digestive tract from the bile cestocidal activity is exhibited Following exposure to praziquantel the tapeworm loses its ability to resist digestion by the mammalian host Because of this whole tapeworms including the scolices plural ofscolex are very rarely passed after administration of praziquantel In many instances only disintegrated and partially digested pieces of tapeworms will be seen in the stool The majority of tapeworms are digested and are not found in the feces Praziquantel is administered as a racemate but only the Renantiomer is biologically active the enantiomers may be separated using a resolution of an amine obtained from praziquantel Pharmacokinetics Praziquantel is well absorbed about 80 from the gastrointestinal tract However due to extensive firstpass metabolism only a relatively small amount enters systemic circulation Praziquantel has a serum halflife of 08 to 15 hours in adults with normal renal and liver function Metabolites have a halflife of 4 to 5 hours In patients with significantly impaired liver function Child Pugh classes B lld C the serum halflife is increased to 3 to 8 hours Praziquantel and its metabolites are mainly excreted renally within 24 hours after a single oral dose 70 to 80 is found in urine but less than 01 as the unchanged drug Praziquantel is metabolized through the cytochrome P450 pathway via CYP3A4 Agents that CYP3A4 such as phenytoin rifampin and azole antifungals will affect the metabolism of praziquantel Praziquantel has a particularly dramatic effect on patients with schistosomiasis Studies of those treated have shown that within six months of receiving a dose of praziquantel up to 90 of the damage done to internal organs due to schistosomiasis infection can be reversed History Praziquantel was developed in the laboratories for parasitological research of Bayer AG and Merck KGaA in Germany Elberfeld and Darmstadt in the mid 1970s 商品名 Biltricide Bayer 600 mg Tablets：人類使用 Cesol Merck Tablets Cestoved Vedco ：藥片或注射劑，獸醫使用 Cysticide Merck Tablets Distocide Shin Poong Pharm Co Ltd 600mg tablet：人類使用 Distoside Chandra Bhagat Pharma Pvt Ltd 600mg tablet：人類使用 Droncit Bayer ：獸醫使用 Drontal combination with Bayer：獸醫使用 DWorm Farnum for veterinary use note that DWorm also makes roundworm medicine containing piperidine which is not effective against tapeworms Fish Tapes Thomas Labs for aquarium use Kaicide Taiwan Milbemax combination with Novartis：獸醫使用 Popantel Jurox PraziPro Hikari ：水生動物飼養使用 PrazTastic NFPNational Fish Pharmaceuticals ：水生動物飼養使用 Pure Prazi COTS KoiChildren of the Sun Koi：水生動物飼養使用 PraziPure JKO Inc dba Kodama Koi Farm Kodama Koi Garden licensed by COTS Koi：水生動物飼養使用 Profender combination with Bayer ：獸醫使用 Tape Worm Tabs Trade Winds ：獸醫使用 Zentozide Berich Thailand Co 核准狀況 吡喹酮名列世界衛生組織基本藥物標準清單之中，是世界上對於基本公共衛生最重要的藥物之一。 在英國，吡喹酮並未獲准在人體上使用。但在必要時可以根據在患者實名的情況下進口。在英國吡喹酮可以作為獸用驅蟲藥銷售。 在美國，吡喹酮被 FDA 批准用於血吸蟲病及肝吸蟲病的治療，儘管它對其他種類的感染也有效。 參考文獻 Category 驅蟲藥 Category 世界衛生組織基本藥物 Category 胺類 Category 內醯胺類