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: 20 mg/kg/dose 3 times a day at 4- to 6-hour intervals for 1 day

Praziquantel Dose in the treatment of Clonorchiasis/ opisthorchiasis:

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

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

  • Oral:
    • 50 mg/kg/day in 3 divided daily doses (in combination with albendazole) for 10 to 14 days;
    • The dose may be repeated if persistent viable lesions on 6-month follow-up imaging.
  • Note:

    • Initiate adjunctive corticosteroid therapy prior to initiation of antiparasitic therapy.
    • Antiparasitic therapy should not be prescribed in patients with untreated hydrocephalus, calcified lesions, or cysticerci encephalitis;
    • consultation with an infectious disease specialist for specific treatment recommendations is necessary.

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

  • Oral: 5 to 10 mg/kg as a single stat dose (25 mg/kg for Hymenolepis nana).

Praziquantel Dose in Childrens

  • Note: Dosing interval and duration highly variable dependent on condition; for 3 times daily doses, intervals of 4 to 6 hours are suggested.

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: 25 mg/kg/dose 3 times a day at 4- to 6-hour intervals for 1 to 2 days.

Fasciolopsiasis (Fasciolopsis buski [intestinal fluke]):

  • Children and Adolescents:

    • Oral: 25 mg/kg/dose 3 times a day for 1 day.

Paragonimiasis (Paragonimus spp. or lung fluke]):

  • Children and Adolescents:

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

Praziquantel Dose in the treatment of Schistosomiasis (Bilharziasis):

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

  • Note: Repeat treatment may be needed in 2-4 weeks to increase the effectiveness

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:
      • 40 mg/kg as a single dose;
      • a single dose of 40 mg/kg has been successfully used for the treatment of urogenital S. haematobium in children 1 to 10 years of age and S. mansoni in the population that included infants (age range: 5 months to 7 years)
      • however, pharmacokinetic data shows a lower cure rate in infants and preschool children. one possible explanation is that higher doses may be required in younger patients due to pharmacokinetic/dynamic differences;
      • In preschool children, one dose of 60 mg/kg was successfully used in children 3 to 8 years of age in a hyperendemic area to treat S.mansoni.

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 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.
  • The non-emergent treatment for neurocysticercosis may be postponed until after the completion of pregnancy.

Praziquantel use during breastfeeding:

  • Breast milk contains Praziquantel.
  • One study found that breast milk concentrations of praziquantel 50mg/kg or three 20mg/kg doses was 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 for breastfeeding females.

Praziquantel Dose in Kidney disease:

  • No dosage adjustment necessary.

Praziquantel Dose in Liver disease:

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

  • May be more frequent and/or serious in patients with a heavy 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, i.e. praziquantel, or any component of its formulation
  • 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 of central nervous system:

    • Praziquantel could be used to treat central nervous system disorders such as paragonimiasis or schistosomiasis.
    • Consider whether there is a greater risk for patients who have had seizures in the past or other signs that could indicate central nervous system involvement, such as subcutaneous nodules suggesting cysticercosis.
  • Hepatic impairment

    • Take care when you have moderate or severe hepatic impairment.
    • A decreased liver drug metabolism could lead to higher plasma concentrations of nonmetabolized praziquantel.
  • Neurocysticercosis:

    • Use only when indicated: Antiparasitic therapy can worsen neurocysticercosis symptoms by inducing an inflammation response.
    • 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 be effective against migrating Schistosomulae
    • Data from observation indicate that praziquantel may not be effective in treating the acute phase.
    • In addition, use in patients with schistosomiasis may be associated with clinical deterioration such as paradoxical reactions or serum sickness Jarisch-Herxheimer-like reactions, which is a sudden inflammatory immune response likely caused by the release of schistosomal antigens.
    • These reactions are most common during acute phase. They can lead to life-threatening events like 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 increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Bosentan May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Chloroquine May decrease the serum concentration of Praziquantel.
Cimetidine May increase the serum concentration of Praziquantel.
Clofazimine May increase the serum concentration of CYP3A4 Substrates (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 decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (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 increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Inducers (Strong) May decrease the serum concentration of Praziquantel. Management: Use of praziquantel with strong CYP3A4 inducers is contraindicated. Discontinue rifampin 4 weeks prior to initiation of praziquantel therapy. Rifampin may be resumed the day following praziquantel completion.
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;
  • monitor patients with cardiac irregularities during treatment;
  • monitor for seizures;
  • culture urine or feces for ova before instituting therapy

How to administer Praziquantel?

  • Administer tablets with water during meals.
  • Tablets should be swallowed promptly to avoid the bitter taste that may cause gagging or vomiting.
  • Tablets may be halved or quartered; do not chew.
  • Tablets may be crushed or disintegrated and mixed with semi-solid food or liquid, but should be used within 1 hour of mixing.
  • Tablets are scored and may be split into four segments of 150 mg.

Mechanism of action of Praziquantel:

  • This increases the cell permeability of calcium in schistosomes.
  • It causes strong contractions of worm muscle and paralysis of worms.
  • The result is detachment and dislodgment of suckers from blood vessel walls.

Absorption:

  • Oral: 80%

Distribution:

  • CSF concentration is 14% to 20% of plasma concentration

Protein binding:

  • ~80%

Metabolism:

  • Extensive first-pass effect; metabolized by the liver 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:

No Brands Available in Pakistan.

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