FLUKANEX SUSPENSION

Indications

• Ascariasis
• Hookworm infection
• Strongyloidiasis
• Immunomodulation in colorectal cancer
• Autoimmune diseases

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing recommendations.

Adults: Refer to the BNF for specific adult dosing recommendations.

Mechanism of action

Levamisole acts by binding to nicotinic acetylcholine receptors on the muscle cells of helminths, leading to paralysis and expulsion of the parasites. It is also thought to enhance T-cell function and boost the immune system, particularly in the context of cancer therapy.

Pharmacodynamics

Levamisole exhibits its anthelmintic effects through neuromuscular paralysis of the parasites, which prevents them from attaching to the intestinal wall and allows for their elimination. Its immunomodulatory effects are attributed to its ability to enhance T-cell proliferation and stimulate interferon production, thus improving the host's immune response.

Pharmacokinetics

Levamisole is well absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It undergoes extensive hepatic metabolism, primarily through cytochrome P450 enzymes, and has a half-life of approximately 3 to 5 hours. The metabolites are primarily excreted via the urine. Food intake does not significantly affect its absorption.

Contra-indications

• Hypersensitivity to levamisole or any of its components
• Severe immunosuppression
• History of agranulocytosis

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Rash
• Agranulocytosis
• Hepatotoxicity
• CNS effects such as dizziness and headache

Interactions

• Increased risk of agranulocytosis when used with other myelosuppressive agents
• Possible interaction with warfarin, increasing anticoagulant effect
• Caution with concurrent use of drugs that affect the liver

Precautions

• Use with caution in patients with liver impairment
• Monitor blood counts during therapy due to risk of agranulocytosis
• Consider potential drug interactions before initiating therapy

Pregnancy

Levamisole is classified as category C. Use is not recommended unless the potential benefit outweighs the potential risk to the fetus.

Breast-feeding

It is not known whether levamisole is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.

Formulations

• Tablets
• Oral suspension

Indications

• Fasciolosis
• Liver fluke infections
• Parasitic infections in livestock

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Rafoxanide functions by inhibiting the succinate dehydrogenase enzyme in the parasite's mitochondria, which disrupts the energy production process. This ultimately leads to a depletion of ATP in the parasite, resulting in its death. The drug has a high affinity for the parasite's mitochondrial membranes, making it effective against trematodes and some nematodes.

Pharmacodynamics

Rafoxanide exhibits a rapid onset of action against susceptible parasites. The drug’s effectiveness is influenced by its lipophilicity, which aids in its absorption and distribution within the host. It demonstrates a high level of activity against adult and juvenile stages of flukes, providing a therapeutic benefit in the management of trematodiasis.

Pharmacokinetics

Rafoxanide is well absorbed after administration and achieves peak plasma concentrations relatively quickly. The drug is extensively metabolized in the liver, with metabolites being primarily excreted via the bile. Its elimination half-life allows for dosing at intervals that effectively manage parasitic infections. The pharmacokinetics may vary based on the animal species and health status.

Pregnancy

There is limited data on the use of rafoxanide in pregnancy. Caution is advised.

Breast-feeding

It is not known if rafoxanide is excreted in human milk. Caution is advised.

Storage

Store in a cool, dry place away from direct sunlight.