Praziquantel (Biltricide) - Uses, Dose, Brands, Side effects

Praziquantel (Biltricide) is an antihelminthic medicine that is used to treat most infections caused by cestodes and schistosomes.

Praziquantel Uses:

  • Helminths:

    • Treatment of infections in patients ≥1 year caused by the following species of Schistosoma:
      • Schistosoma mekongi,
      • S. japonicum,
      • S. mansoni,
      • S. hematobium) and the
      • liver flukes (Clonorchis sinensis/ Opisthorchis viverrini)
  • Off-Label Use of Praziquantel in Adults:

    • Neurocysticercosis, parenchymal;
    • Tapeworms

Praziquantel Dose in Adults

Praziquantel Dose in the Treatment of Schistosomiasis:

  • Oral: Dosage of 20 mg/kg 3 times a day for one day, spaced 4- to 6 hours apart.

Praziquantel Dose in the treatment of Clonorchiasis/ opisthorchiasis:

  • Oral: 3 times a day for 1 to 2 days at a dose of 25 mg/kg.

Praziquantel Dose in the treatment of parenchymal Neurocysticercosis (>2 viable cysts) (off-label):

  • Oral:
    • For 10 to 14 days, administer 50 mg/kg/day in three evenly spaced doses (in conjunction with albendazole); repeat the dose if 6-month follow-up imaging reveals persistent viable lesions.
  • Note:

    • Before beginning antiparasitic therapy, begin adjunctive corticosteroid therapy.
    • Patients with untreated hydrocephalus, calcified lesions, or cysticerci encephalitis should not get antiparasitic therapy; instead, an infectious disease specialist should be consulted for particular therapeutic advice.

Praziquantel Dose in the treatment of Tapeworms (off-label):

  • Oral: As a single stat dosage, administer 5 to 10 mg/kg (25 mg/kg for Hymenolepis nana).

Praziquantel Dose in Children:

  • Note: The period between doses is highly variable and depends on the patient's condition; intervals of 4 to 6 hours are recommended for doses given three times daily.

Praziquantel Dose in the Treatment of Flukes:

Clonorchiasis (Clonorchis sinensis or Chinese liver fluke); Opisthorchiasis (Opisthorchis viverrini or Southeast Asian liver fluke):

  • Children and Adolescents:

    • Oral: Dosage of 25 mg/kg For one to two days, 3 times per day at 4- to 6-hour intervals.

Fasciolopsiasis (Fasciolopsis buski [intestinal fluke]):

  • Children and Adolescents:

    • Oral: 3 doses of 25 mg/kg per day for one day.

Paragonimiasis (Paragonimus spp. or lung fluke]):

  • Children and Adolescents:

    • Oral: Dosage of 25 mg/kg 3 times every day for two to three days.

Praziquantel Dose in the treatment of Schistosomiasis (Bilharziasis):

Treatment (CDC 2018c; Red Book [AAP 2018]):

  • Note: Dosage of 25 mg/kg 3 times every day for two to three days.

Schistosoma japonicum and Schistosoma mekongi:

  • Children and Adolescents:

    • Oral: 20 mg/kg/dose 3 times a day for 1 day

Schistosoma mansoni, Schistosoma haematobium, and Schistosoma intercalatum:

  • Children and Adolescents:

    • Oral: 20 mg/kg/dose twice a day for 1 day

Control programs for endemic areas:

  • Infants, Children, and Adolescents:

    • Oral:
      • A single dose of 40 mg/kg has been used successfully to treat S. mansoni in the population that included infants (aged 5 months to 7 years) and urogenital S. haematobium in children aged 1 to 10; however, pharmacokinetic evidence indicates a decreased cure rate in young children and infants.
      • One argument is that younger patients may need higher dosages due to pharmacokinetic/dynamic variations.
      • For example, in young children, a single dose of 60 mg/kg was successfully utilised to treat S.mansoni in children between the ages of 3 and 8 in a hyperendemic location.

Praziquantel Dose in the Treatment of Tapeworms:

Praziquantel for the treatment of the intestinal (Adult) stage of Diphyllobothrium latum (fish tapeworm), Taenia saginata (beef tape worm), Taenia solium (pork tapeworm):

  • Children and Adolescents:

    • Oral: 5 to 10 mg/kg as a single stat dose

Praziquantel for the treatment of the intestinal stage (adult stage) of Dipylidium caninum:

  • Infants ≥6 months, Children, and Adolescents:

    • Oral: 5 to 10 mg/kg as a single stat dose

Praziquantel for the treatment of Hymenolepis nana (dwarf tapeworm):

  • Children and Adolescents:

    • Oral: 25 mg/kg as a single dose

Praziquantel for tissue stage (larva stage) of Neurocysticercosis (Taenia solium or pork tapeworm):

  • Children and Adolescents:

    • Oral: 50 mg/kg/day for 15 days.
    • Note: May be used in conjunction with antiseizure medication and/or corticosteroids.

Praziquantel Pregnancy Category: B

  • According to available data, there has been no evidence of an increase in maternal or fetal outcomes after the use of Praziquantel during Schistosoma treatment.
  • The World Health Organization recommends that pregnant women receive praziquantel in areas where soil-transmitted and schistosomiasis are common.
  • Neurocysticercosis non-emergent treatment may be delayed until after the pregnancy is over.

Praziquantel use during breastfeeding:

  • Breast milk contains Praziquantel.
  • One study found that breast milk concentrations of praziquantel 50mg/kg or three 20mg/kg doses were 1% after maternal use.
  • According to the manufacturer breastfeeding during therapy is a decision that should be made after considering the risks to infants and the benefits to mothers.
  • The World Health Organization considers that praziquantel is compatible with breastfeeding females.

Praziquantel Dose in Kidney Disease:

  • No dosage adjustment is necessary.

Praziquantel Dose in Liver Disease:

  • There are no dosage adjustments provided in the manufacturer's labeling.
  • However, total drug exposure in moderate-to-severe impairment is increased.

  • Occurrence and/or severity may be increased in patients with a high worm burden.

Side effects of Praziquantel

  • Central nervous system:

    • Dizziness
    • Headache
    • Malaise
  • Dermatologic:

    • Urticaria
  • Gastrointestinal:

    • Abdominal distress
    • Nausea
  • Miscellaneous:

    • Fever

Contraindications to Praziquantel:

  • Hypersensitivity to the primary drug
  • ocular cysticercosis;
  • a concomitant prescription with strong cytochrome P450 (CYP450) inducers, such as rifampin

Warnings and precautions

  • Cardiac arrhythmias:

    • During treatment, monitor patients suffering from arrhythmias;
    • Praziquantel administration has been linked to a variety of conditions including ectopic rhythms and ventricular fibrillation.
  • Effects on central nervous system:

    • Praziquantel could be used to treat central nervous system disorders such as paragonimiasis or schistosomiasis.
    • Think about whether patients who have previously experienced seizures or other symptoms that could point to central nervous system involvement, including subcutaneous nodules that could point to cysticercosis, are at a higher risk.
  • Hepatic impairment

    • Take care when you have moderate or severe hepatic impairment.
    • Praziquantel plasma concentrations could increase as a result of impaired liver drug metabolism.
  • Neurocysticercosis:

    • Use only as directed: By triggering an inflammatory reaction, antiparasitic therapy can make the symptoms of neurocysticercosis worse.
    • It is important to start adjunctive corticosteroid treatment before you begin antiparasitic therapies.
    • Untreated hydrocephalus, cysticerci, and calcified lesions should not be treated with antiparasitic treatment.
    • To exclude intraocular cysticerci, perform a funduscopic examination before initiating antiparasitic treatment. In some cases of unsuspected intraocular parasites, antiparasitic treatment may result in blindness.
  • Schistosomiasis:

    • Praziquantel might not have any effect on migratory Schistosomulae
    • Praziquantel may not be useful in treating the acute phase, according to observational data.
    • Additionally, use in schistosomiasis patients may be linked to clinical side effects such as paradoxical reactions or serum sickness. An abrupt inflammatory immunological response known as a Jarisch-Herxheimer-like reaction is most likely brought on by the release of schistosomal antigens.
    • The acute period is when these reactions occur most frequently. They may result in potentially fatal conditions such as respiratory failure, encephalopathy, and papilledema.

Praziquantel: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy)

Aprepitant

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Bosentan

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

Chloroquine

Praziquantel serum concentration can drop.

Cimetidine

Praziquantel serum concentration can drop.

Clofazimine

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

CYP3A4 Inducers (Moderate)

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

CYP3A4 Inhibitors (Strong)

May increase the serum concentration of Praziquantel.

Deferasirox

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Duvelisib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Erdafitinib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Erdafitinib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fosaprepitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Fosnetupitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Grapefruit Juice

May increase the serum concentration of Praziquantel.

Ivosidenib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Larotrectinib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Netupitant

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Palbociclib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Sarilumab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Siltuximab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Simeprevir

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Tocilizumab

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Risk Factor D (Consider therapy modification)

Dabrafenib

May lower the serum level of CYP3A4 substrates (High risk with Inducers).

Management: When possible, look for substitutes for the CYP3A4 substrate. If concurrent therapy cannot be avoided, pay special attention to the substrate's clinical consequences (particularly therapeutic effects).

Lorlatinib

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences.

MiFEPRIStone

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus.

St John's Wort

May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).

Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling.

Stiripentol

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.

Risk Factor X (Avoid combination)

Conivaptan

May elevate CYP3A4 substrates' serum concentration (High risk with Inhibitors).

CYP3A4 Inducers (Strong)

Praziquantel serum concentration can drop. Treatment: Praziquantel should not be used in conjunction with potent CYP3A4 inducers. Rifampin should be stopped 4 weeks before starting praziquantel therapy. The day after the last dose of praziquantel, rifampin may be started again.

Fusidic Acid (Systemic)

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Idelalisib

May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).

Monitoring parameters:

  • Liver function tests

  • cardiac irregularities 

  • seizures

  • culture urine or feces for ova before instituting therapy

How to administer Praziquantel?

  • When eating, take the pills with water.
  • The bitter taste of the tablets should be quickly taken to prevent gagging or vomiting.
  • Do not chew the tablet; it may be cut in half or quarters.
  • Tablets can be broken up or dissolved, then combined with semi-solid food or liquid; however, this mixture should be consumed within an hour.
  • The scored tablets can be divided into four pieces, each containing 150 mg.

Mechanism of action of Praziquantel:

Praziquantel makes calcium more permeable to cells in schistosomes. This leads to strong muscle spasms and worm paralysis.

As a result, suckers are detached from blood vessel walls and knocked loose.

Absorption:

  • Oral: 80%

Distribution:

  • CSF concentrations range from 14% to 20% of plasma levels.

Protein binding:

  • ~80%

Metabolism:

  • Significant first-pass impact; liver metabolizes to hydroxylated and conjugated metabolites

Half-life elimination:

  • Parent drug: 0.8 to 1.5 hours;
  • Metabolites: 4.5 hours

Time to peak, serum:

  • 1 to 3 hours

Excretion:

  • Urine ~80% (>99% as metabolites)

International Brands of Praziquantel:

  • Biltricide
  • Belicide
  • Biltricid
  • Biltricide
  • Cesol
  • Cisticid
  • Cysticide
  • Distocide
  • Droncit Vet
  • Epiquantel
  • Fluxide
  • Kalcide
  • Opticide
  • Prasikon
  • Prazine
  • Praziquin
  • Prazite
  • Prazitral
  • Vermaqpharma Vet
  • Wormicide

Praziquantel Brand Names in Pakistan:

Not available.