Praziquantel

Medication

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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.[3] In humans specifically, it is used to treat schistosomiasis, clonorchiasis, opisthorchiasis, tapeworm infections, cysticercosis, echinococcosis, paragonimiasis, fasciolopsiasis, and fasciolosis.[3] It should not be used for worm infections of the eye.[4] It is taken by mouth.[3]

Side effects in humans may include poor coordination, abdominal pain, vomiting, headache, and allergic reactions.[4] While it may be used during pregnancy, it is not recommended for use during breastfeeding.[4] Praziquantel is in the anthelmintic class of medications.[3] It works partly by affecting the function of the worm's sucker.[3]

Praziquantel was approved for medical use in the United States in 1982.[3] It is on the World Health Organization's List of Essential Medicines.[5]

Medical uses

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Praziquantel is used to treat diseases caused by infection with several types of internal/gastrointestinal, and external parasites, including:

Side effects

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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]

• Central nervous system (CNS): 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 cell-death of the parasites (headache, worsening of pre-existing neurological problems, seizures, arachnoiditis, and meningism). These side effects may be life-threatening and can be reduced by coadministration of corticosteroids. All patients with cerebral cysticercosis are strongly recommended to be hospitalized during treatment.
• Gastrointestinal tract: About 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 been seen so far.
• Sensitivity reactions: Urticaria, rash, pruritus and eosinophilia in white blood cell counts
• Other locations/body as a whole: Lower back pain, myalgia, arthralgia, fever, sweating, various cardiac arrhythmias, and hypotension

Pregnancy

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The WHO states praziquantel is safe during pregnancy.[15] Animal studies have failed to reveal evidence of fetal harm. Praziquantel is effective in reducing schistosomiasis during pregnancy.[16] Another trial found that treatment with praziquantel did not increase the rates of low birthweight, fetal death, or congenital anomalies.[17]

Drug interactions

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The antibiotic rifampicin decreases plasma concentrations of praziquantel.[18]

Carbamazepine and phenytoin are reported to reduce the bioavailability of praziquantel.[19] Chloroquine also reduces its bioavailability.[20]

The drug cimetidine heightens praziquantel bioavailability.[21][22]

Mechanism of action

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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.[23] 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."[24]

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.[25]

Pharmacokinetics

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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.[10]

History

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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]

Society and culture

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Brand names

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Regulatory approval

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Praziquantel is on the World Health Organization's List of Essential Medicines.[5]

Praziquantel is not licensed for use in humans in the UK, but it can be imported when necessary on a named-patient basis.[27] 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.[28]

Veterinary medicine

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It may cause problems in dogs with MDR1 mutations.[30]

See also

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References

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What is this medication?

PRAZIQUANTEL (PRAZ i KWON tel) is an anti-infective. It is used to treat infections of some parasite worms.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Biltricide

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What should I tell my care team before I take this medication?

They need to know if you have any of these conditions:

•liver disease

•worm cysts in the eye

•an unusual or allergic reaction to praziquantel, other medicines, foods, dyes, or preservatives

•pregnant or trying to get pregnant

•breast-feeding

How should I use this medication?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food. Do not chew, crush, or melt this medicine in the mouth before swallowing. Tablets may be broken at score lines as directed. Take your medicine at regular intervals. Do not take your medicine more often than directed. Take all of your medicine as directed even if you think you are better. Do not skip doses or stop your medicine early.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 4 years of age for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

NOTE: This medicine is only for you. Do not share this medicine with others.

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What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.

What may interact with this medication?

•barbiturates like phenobarbital

•chloroquine

•cimetidine

•dexamethasone

•erythromycin

•grapefruit juice

•lumacaftor; ivacaftor

•medicines for fungal infections like ketoconazole and itraconazole

•rifampin

•some medicines for seizures like carbamazepine, phenytoin, fosphenytoin, oxcarbazepine

•St. John's Wort

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

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What should I watch for while using this medication?

Visit your doctor or health care professional to check that the infection is cleared. Tell your doctor if your symptoms do not improve or if they get worse.

You may get drowsy or dizzy. On the day of and on the day after treatment with this medicine, do not drive, use machinery, or do anything that needs mental alertness. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.

Practice good hygiene to prevent infection of others. Wash your hands, scrub your fingernails and shower often. Every day change and launder linens and undergarments. Scrub toilets often and keep floors clean.

What side effects may I notice from receiving this medication?

Side effects that you should report to your doctor or health care professional as soon as possible:

•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue

•bloody diarrhea

•breathing problems

•fast, irregular heartbeat

•fever

•seizures

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

•aches, pains

•dizzy, drowsy

•headache

•loss of appetite

•stomach upset, nausea

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medication?

Keep out of the reach of children.

Store at room temperature below 30 degrees C (86 degrees F). Store away from heat and direct light. Throw away any unused medicine after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

For more Reliable Praziquantel Apiinformation, please contact us. We will provide professional answers.