Bithionol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [2]

Overview

Bithionol is an anthelmintic used to treat "Anoplocephala perfoliata" (tapeworms) in horses^[1] and Fasciola hepatica (liver flukes).

Brand Names

Bithionol is investigational in the U.S. The drug can be obtained from the Centers for Disease Control (CDC) Drug Service, CDC, Atlanta, Georgia 30333 (404-639-3670; evenings, weekends, or holidays: 404-639-2888).

Prescribing Information

Dosage

Adult Normal Dosage

Oral route

1) The recommended oral dose of bithionol for the treatment of Fascioliasis, and as alternative therapy in Paragonimiasis, is 30 to 50 milligrams/kilogram on alternate days for 10 to 15 doses.

2) Bithionol is usually given in 2 or 3 divided doses, and after meals to minimize gastrointestinal symptoms.

Pediatric Normal Dosage

Oral route

1) The recommended pediatric oral dose of bithionol for the treatment of Fascioliasis, and as alternative therapy in Paragonimiasis, is 30 to 50 milligrams/kilogram on alternate days for 10 to 15 doses.

2) Bithionol is usually given in 2 or 3 divided doses, and after meals to minimize gastrointestinal symptoms.

Pharmacokinetics

Onset

a) Fascioliasis, 2 to 9 days.

b) Resolution of fever has been reported 2 days after initiation of BITHIONOL therapy in fascioliasis, with eradication of ova in stools after 9 days.

c) Paragonimiasis, 3 to 5 days. (Significant improvement of hemoptysis in paragonimiasis has been reported after the third dose of oral BITHIONOL. Eradication of Paragonimus westermani ova has occurred after the fifth dose.)

Metabolism

Metabolism Sites and Kinetics: Not extensively studied in humans. Animal studies suggest that BITHIONOL is metabolized in the liver, with metabolites being excreted in bile and urine.

Contraindications

Previous hypersensitivity to BITHIONOL

Precautions

Renal insufficiency (potential accumulation)

Cardiovascular disease

Peptic ulcer disease

Asthma or other allergic-type disorders

Adverse Reactions

Cardiovascular Effects

Extrasystoles, first-degree heart block, and hypertension have been reported rarely after bithionol administration.

Blood pressure irregularities, and errors in cardiac conduction are reported in association with the therapeutic use of bithionol.

Hypotension

Dermatologic Effects

Endocrine/Metabolic Effects

Hypoalbuminemia
Increased body temperature

Gastrointestinal Effects

Abdominal pain
Diarrhea
Loss of appetite
Nausea
Vomiting

Hematologic Effects

Leukopenia

Hepatic Effects

Hepatitis
Increased liver enzymes

Immunologic Effects

Neurologic Effects

Respiratory Effects

Other

Angioedema

Therapeutic Uses

Infection by Fasciola (non-FDA approval)
Infection by Paragonimus (non-FDA approval)

Mechanism of Action

Bithionol is a chlorinated phenol derivative which has antimicrobial and anthelmintic activity by uncoupling oxidative phosphorylation in the parasite, leading to blockade of adenosine triphosphate synthesis and energy production.

References

↑ [1], Sanada Y, Senba H, Mochizuki R, et al. Evaluation of marked rise in fecal egg output after bithionol administration to horse and its application as a diagnostic marker for equine Anoplocephala perfoliata infection. J. Vet. Med. Sci. May 2009;71(5):617-620.

[1] [1], Sanada Y, Senba H, Mochizuki R, et al. Evaluation of marked rise in fecal egg output after bithionol administration to horse and its application as a diagnostic marker for equine Anoplocephala perfoliata infection. J. Vet. Med. Sci. May 2009;71(5):617-620.

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