ANTICESTODALS

DRUGS

• Praziquantel [(vm: Droncit; hm: Biltricide]
• Epsiprantel [vm: Cestex; hm: none]
• Bunamidine [vm: Scoloban]; hm: none
• Febantel [vm: Vercom Paste; hm: none]
• Niclosamide [vm: Yomesan; hm: Niclocide]
• Mebendazole [vm, Telmin; hm: Vermox]
• Albendazole [vm: * ; hm: Zentel (Invest)]
• Paromomycin [hm: Humatin]

PRAZIQUANTEL

Examples

• vm: DRONCIT PO and Injectable dogs, cats, birds and other small animals.
• hm: BILTRICIDE Tablets only

Spectrum

• ADULT AND LARVAL CESTODES - animals & humans
  • Dogs: Dipylidium caninum, Taenia pisiformis, and Echinococcus granulosis
  • Cats: Dipylidium caninum and taenia taeiaeformis
• TREMATODES
  • Flukes - lung, liver, intestinal
  • Schistosomiasis

Mechanism of Action

• Root Mechanism
  • Rapidly taken up by parasite
  • Increases membrane permeability to mono and divalent cations, especially Ca⁺⁺
  • However, it acts differently than Ca++ and K+ ionophores
  • Praziquantel produces to prompt actions depending on the concentration.
• Low Concentrations
  • Increased muscular activity followed by contraction and SPASTIC PARALYSIS which causes the parasite to lose its attachment to the intestinal mucosa.
• Slightly Higher Concentrations (Still in therapeutic range)
  • Vacuolization and vesiculation of the tegument of susceptible organisms
  • If sufficiently pronounced, this ACTIVATES HOST DEFENSE MECHANISMS ultimately leading to the destruction of the parasites.
  • This mechanism correlates well with the effects in Schistosoma mansoni.

Contraindications

None described for animals by Theodorides 1985

Adverse effects

• Dogs: PO doses anorexia, vomiting, lethargy or diarrhea in less than 5%.
• Cats: PO doses salivation and diarrhea in less than 2%.
• Humans: Reversible Dizziness, headache, malaise, abdominal pain and nausea relatively common and higher doses.

Precautions / comments

• Single dose ususally adequate for tapeworms
• Humans: Drug appears in milk (ca. 25% of maternal serum) so women should not nurse for 72 hours. Express and discard milk.
• No embryotoxicity, teratogenesis, mutagenesis or carcinogenesis in rat studies at up to 40 x normal dose
• Caused 3-fold increase in abortions in rats at dose rate recommended for humans. [AMADE 90,4:23]
• No effect on reproductive performance in rats
• Not intended for use in puppies or kittens less than 4 weeks old.

Advantages

Disadvantages

Epsiprantel

• vm: CESTEX po once
• hm: none

Spectrum

• Dogs and cats: Dipylidium and taenia

Contraindications

• None on the label
• Probably not use in pups/kittens less than 7 weeks old

Adverse effects

• None expected
• 36-times recommended dose caused only vomiting in some kittens, nothing in dogs

Precautions / Comments

• Safety for pregnant animals unknown.
• Drug extremely poorly absorbed after po administration (<0.1% elimin urine, Most in stool with no metabolites detected yet.
• Worms digested, some completely, so not visible in stool.

  Advantages

  • Oral -- One time dose
  • No fasting

  Niclosamide

  Examples

  vm: YOMESAN -- largely abandoned in US vm.

  hm: NICLOCIDE

  Spectrum

  CESTODES in dogs and cats

  Contraindications

  intestinal atony

  acute diarrhea

  Adverse effects

  Chalky feces

  Precautions / Comments

  Overnight fast recommended

  Dead tapeworms eliminated in stool within 6 to 48 hr.

  Advantages

  Can use safely in young puppies/kittens and in pregnant animals

  Relatively safe and efficacious

  Disadvantages

  Not always satisfactory against Dipylidium

  Bunamidine

  Note: Largely abandoned in veterinary medicine

  Examples

  vm: SCOLOBAN

  Spectrum

  Common CESTODES, including Echinococcus

  Contraindications

  Hepatic or Cardiac disease

  Severely debilitated animals

  Male breeding dogs -- not within 28 days of breeding

  Highly excitable animals

  Concurrent use of BUTAMISOLE [STYQUIN]

  Adverse effects -- Not uncommon

  Emesis and Diarrhea

  Depression (up to 36 hours)

  Irritation of mucous membranes of conjunctiva

  Transient mild effect on spermatogenesis (?)

  Mild transient changes in ECG at excessive doses

  Sudden death

  Precautions / Comments

  Fasting 3 hr before and after treatment

  Safe during pregnancy

  Do not break tablets near eyes or crush in feed or liquid -- extreme irritation to mucous membranes

  Fright or flight response and associated release of catecholamines may sensitize heart to bunamidine causing sudden death of animal upon injection.

  For maximum efficacy vs Echinococcus give twice at 48-hr interval.

  Advantages

  Effective

  Disadvantages

  Adverse effects can be severe

  Possibility of drug interaction

  Must observe precautions or may have severe problem

  References

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  Gordon L. Coppoc, DVM, PhD
  Professor of Veterinary Pharmacology
  Head, Department of Basic Medical Sciences
  School of Veterinary Medicine
  Purdue University
  West Lafayette, IN 47907-1246
  Tel: 317-494-8633Fax: 317-494-0781
  Email: coppoc@vet.purdue.edu
  
  Last modified 10:52 PM on 4/25/96 GLC