Clinical data | |
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Pronunciation | /ˌpræzɪˈkwɒntɛl/ |
Trade names | Biltricide |
AHFS/Drugs.com | Monograph |
MedlinePlus | a608048 |
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Routes of administration | Human use: by mouth (tablets) |
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Pharmacokinetic data | |
Bioavailability | Relatively small |
Metabolism | Liver |
Elimination half-life | 0.8–1.5 hours (main metabolites: 4–5 hours) |
Excretion | Urine (mainly) |
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CAS Number | |
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CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.054.126 |
Chemical and physical data | |
Formula | C19H24N2O2 |
Molar mass | 312.413 g·mol−1 |
3D model (JSmol) | |
Melting point | 136 to 138 °C (277 to 280 °F) |
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Praziquantel (PZQ), sold under the brandname Biltricide among others, is a medication used to treat a number of types of parasitic worm infections in mammals, birds, amphibians, reptiles, and fish. [2] In humans specifically, it is used to treat schistosomiasis, clonorchiasis, opisthorchiasis, tapeworm infections, cysticercosis, echinococcosis, paragonimiasis, fasciolopsiasis, and fasciolosis. [2] It should not be used for worm infections of the eye. [3] It is taken by mouth. [2]
Side effects in humans may include poor coordination, abdominal pain, vomiting, headache, and allergic reactions. [3] While it may be used during pregnancy, it is not recommended for use during breastfeeding. [3] Praziquantel is in the anthelmintic class of medications. [2] It works partly by affecting the function of the worm's sucker. [2]
Praziquantel was approved for medical use in the United States in 1982. [2] It is on the World Health Organization's List of Essential Medicines. [4]
Praziquantel is used to treat diseases caused by infection with several types of internal/gastrointestinal, and external parasites, including:
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.[ citation needed ]
The WHO states praziquantel is safe during pregnancy. [14] Animal studies have failed to reveal evidence of fetal harm. Praziquantel is effective in reducing schistosomiasis during pregnancy. [15] Another trial found that treatment with praziquantel did not increase the rates of low birthweight, fetal death, or congenital anomalies. [16]
The antibiotic rifampicin decreases plasma concentrations of praziquantel. [17]
Carbamazepine and phenytoin are reported to reduce the bioavailability of praziquantel. [18] Chloroquine also reduces its bioavailability. [19]
The drug cimetidine heightens praziquantel bioavailability. [20] [21]
The drug's 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' muscle, 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.[ citation needed ]
Another hypothesis regarding the mechanism of action is that it interferes with adenosine uptake in worms. [22] This effect may have therapeutical relevance given that the schistosome, as the Taenia and the Echinococcus (other praziquantel-sensitive parasites), is unable to synthesize purines, such as adenosine, de novo.[ citation needed ]
Bayer's 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 of "scolex"), 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." [23]
Praziquantel is administered as a racemate, but only the (R)-enantiomer is biologically active; the enantiomers may be separated using a resolution of an amine obtained from praziquantel. [24]
Praziquantel is well absorbed (about 80%) from the gastrointestinal tract. However, due to extensive first-pass metabolism, only a relatively small amount enters systemic circulation. Praziquantel has a serum half-life of 0.8 to 1.5 hours in adults with normal renal and liver function. Metabolites have a half-life of 4 to 5 hours. In patients with significantly impaired liver function (Child-Pugh score B and C), the serum half-life is increased to 3 to 8 hours. Praziquantel and its metabolites are mainly excreted renally; within 24 h after a single oral dose, 70 to 80% is found in urine, but less than 0.1% as the unchanged drug. Praziquantel is metabolized through the cytochrome P450 pathway via CYP3A4. Agents that induce or inhibit CYP3A4 such as phenytoin, rifampin, and azole antifungals will affect the metabolism of praziquantel.[ citation needed ]
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. [9]
Praziquantel was developed in the laboratories for parasitological research of Bayer AG and Merck KGaA in Germany (Elberfeld and Darmstadt) in the mid-1970s.[ citation needed ]
Praziquantel is on the World Health Organization's List of Essential Medicines. [4]
Praziquantel is not licensed for use in humans in the UK, but it can be imported when necessary on a named-patient basis. [26] It is available in the UK as a veterinary anthelmintic.
Praziquantel is FDA approved in the US for the treatment of schistosomiasis and liver flukes, although it is effective in other infections. [27]
It may cause problems in dogs with MDR1 mutations. [29]
Schistosomiasis, also known as snail fever, bilharzia, and Katayama fever, is a disease caused by parasitic flatworms called schistosomes. The urinary tract or the intestines may be infected. Symptoms include abdominal pain, diarrhea, bloody stool, or blood in the urine. Those who have been infected for a long time may experience liver damage, kidney failure, infertility, or bladder cancer. In children, it may cause poor growth and learning difficulty.
Trematoda is a class of flatworms known as flukes or trematodes. They are obligate internal parasites with a complex life cycle requiring at least two hosts. The intermediate host, in which asexual reproduction occurs, is usually a snail. The definitive host, where the flukes sexually reproduce, is a vertebrate. Infection by trematodes can cause disease in all five traditional vertebrate classes: mammals, birds, amphibians, reptiles, and fish.
Cysticercosis is a tissue infection caused by the young form of the pork tapeworm. People may have few or no symptoms for years. In some cases, particularly in Asia, solid lumps of between one and two centimetres may develop under the skin. After months or years these lumps can become painful and swollen and then resolve. A specific form called neurocysticercosis, which affects the brain, can cause neurological symptoms. In developing countries this is one of the most common causes of seizures.
Helminthiasis, also known as worm infection, is any macroparasitic disease of humans and other animals in which a part of the body is infected with parasitic worms, known as helminths. There are numerous species of these parasites, which are broadly classified into tapeworms, flukes, and roundworms. They often live in the gastrointestinal tract of their hosts, but they may also burrow into other organs, where they induce physiological damage.
Hymenolepiasis is infestation by one of two species of tapeworm: Hymenolepis nana or H. diminuta. Alternative names are dwarf tapeworm infection and rat tapeworm infection. The disease is a type of helminthiasis which is classified as a neglected tropical disease.
Albendazole is a broad-spectrum anthelmintic and antiprotozoal agent of the benzimidazole type. It is used for the treatment of a variety of intestinal parasite infections, including ascariasis, pinworm infection, hookworm infection, trichuriasis, strongyloidiasis, taeniasis, clonorchiasis, opisthorchiasis, cutaneous larva migrans, giardiasis, and gnathostomiasis, among other diseases.
Taenia solium, the pork tapeworm, belongs to the cyclophyllid cestode family Taeniidae. It is found throughout the world and is most common in countries where pork is eaten. It is a tapeworm that uses humans as its definitive host and pigs as the intermediate or secondary hosts. It is transmitted to pigs through human feces that contain the parasite eggs and contaminate their fodder. Pigs ingest the eggs, which develop into larvae, then into oncospheres, and ultimately into infective tapeworm cysts, called cysticercus. Humans acquire the cysts through consumption of uncooked or under-cooked pork and the cysts grow into an adult worms in the small intestine.
Taenia saginata, commonly known as the beef tapeworm, is a zoonotic tapeworm belonging to the order Cyclophyllidea and genus Taenia. It is an intestinal parasite in humans causing taeniasis and cysticercosis in cattle. Cattle are the intermediate hosts, where larval development occurs, while humans are definitive hosts harbouring the adult worms. It is found globally and most prevalently where cattle are raised and beef is consumed. It is relatively common in Africa, Europe, Southeast Asia, South Asia, and Latin America. Humans are generally infected as a result of eating raw or undercooked beef which contains the infective larvae, called cysticerci. As hermaphrodites, each body segment called proglottid has complete sets of both male and female reproductive systems. Thus, reproduction is by self-fertilisation. From humans, embryonated eggs, called oncospheres, are released with faeces and are transmitted to cattle through contaminated fodder. Oncospheres develop inside muscle, liver, and lungs of cattle into infective cysticerci.
Schistosoma japonicum is an important parasite and one of the major infectious agents of schistosomiasis. This parasite has a very wide host range, infecting at least 31 species of wild mammals, including 9 carnivores, 16 rodents, one primate (human), two insectivores and three artiodactyls and therefore it can be considered a true zoonosis. Travelers should be well-aware of where this parasite might be a problem and how to prevent the infection. S. japonicum occurs in the Far East, such as China, the Philippines, Indonesia and Southeast Asia.
Paragonimus westermani is the most common species of lung fluke that infects humans, causing paragonimiasis. Human infections are most common in eastern Asia and in South America. Paragonimiasis may present as a sub-acute to chronic inflammatory disease of the lung. It was discovered by Coenraad Kerbert (1849–1927) in 1878.
Taenia pisiformis, commonly called the rabbit tapeworm, is an endoparasitic tapeworm which causes infection in lagomorphs, rodents, and carnivores. Adult T. pisiformis typically occur within the small intestines of the definitive hosts, the carnivores. Lagomorphs, the intermediate hosts, are infected by fecal contamination of grasses and other food sources by the definitive hosts. The larval stage is often referred to as Cysticercus pisiformis and is found on the livers and peritoneal cavities of the intermediate hosts. T. pisiformis can be found worldwide.
Taeniasis is an infection within the intestines by adult tapeworms belonging to the genus Taenia. There are generally no or only mild symptoms. Symptoms may occasionally include weight loss or abdominal pain. Segments of tapeworm may be seen in the stool. Complications of pork tapeworm may include cysticercosis.
Niclosamide, sold under the brand name Niclocide among others, is an anthelmintic medication used to treat tapeworm infestations, including diphyllobothriasis, hymenolepiasis, and taeniasis. It is not effective against other worms such as flukes or roundworms. It is taken by mouth.
Sparganosis is a parasitic infection caused by the plerocercoid larvae of the genus Spirometra including S. mansoni, S. ranarum, S. mansonoides and S. erinacei. It was first described by Patrick Manson in 1882, and the first human case was reported by Charles Wardell Stiles from Florida in 1908. The infection is transmitted by ingestion of contaminated water, ingestion of a second intermediate host such as a frog or snake, or contact between a second intermediate host and an open wound or mucous membrane. Humans are the accidental hosts in the life cycle, while dogs, cats, and other mammals are definitive hosts. Copepods are the first intermediate hosts, and various amphibians and reptiles are second intermediate hosts.
Oxamniquine, sold under the brand name Vansil among others, is a medication used to treat schistosomiasis due to Schistosoma mansoni. Praziquantel, however, is often the preferred treatment. It is given by mouth and used as a single dose.
A Schistosomiasis vaccine is a vaccine against Schistosomiasis, a parasitic disease caused by several species of fluke of the genus Schistosoma. No effective vaccine for the disease exists yet. Schistosomiasis affects over 200 million people worldwide, mainly in rural agricultural and peri-urban areas of the third world, and approximately 10% suffer severe health complications from the infection. While chemotherapeutic drugs, such as praziquantel, oxamniquine and metrifonate both no longer on the market, are currently considered safe and effective for the treatment of schistosomiasis, reinfection occurs frequently following drug treatment, thus a vaccine is sought to provide long-term treatment. Additionally, experimental vaccination efforts have been successful in animal models of schistosomiasis.
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may also be called vermifuges or vermicides. Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals.
Taenia asiatica, commonly known as Asian taenia or Asian tapeworm, is a parasitic tapeworm of humans and pigs. It is one of the three species of Taenia infecting humans and causes taeniasis. Discovered only in 1980s from Taiwan and other East Asian countries as an unusual species, it is so notoriously similar to Taenia saginata, the beef tapeworm, that it was for a time regarded as a slightly different strain. But anomaly arose as the tapeworm is not of cattle origin, but of pigs. Morphological details also showed significant variations, such as presence of rostellar hooks, shorter body, and fewer body segments. The scientific name designated was then Asian T. saginata. But the taxonomic consensus turns out to be that it is a unique species. It was in 1993 that two Korean parasitologists, Keeseon S. Eom and Han Jong Rim, provided the biological bases for classifying it into a separate species. The use of mitochondrial genome sequence and molecular phylogeny in the late 2000s established the taxonomic status.
Taenia hydatigena is one of the adult forms of the canine and feline tapeworm. This infection has a worldwide geographic distribution. Humans with taeniasis can infect other humans or animal intermediate hosts by eggs and gravid proglottids passed in the feces.
Gastropod-borne parasitic diseases (GPDs) are a group of infectious diseases that require a gastropod species to serve as an intermediate host for a parasitic organism that can infect humans upon ingesting the parasite or coming into contact with contaminated water sources. These diseases can cause a range of symptoms, from mild discomfort to severe, life-threatening conditions, with them being prevalent in many parts of the world, particularly in developing regions. Preventive measures such as proper sanitation and hygiene practices, avoiding contact with infected gastropods and cooking or boiling food properly can help to reduce the risk of these diseases.
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