WHO Acute Hazard classification: Not listed

Mechanism of Action of Nitroxinil

• Nitroxinil is an uncoupler of the oxidative phosphorylation in the cell mitochondria, which disturbs the production of ATP, the cellular "fuel". This impairs the parasites motility and probably other processes as well.

Toxicity and Tolerance of Nitroxinil

• LD50 acute, rats, p.o. 170-450 mg/kg (various salts)
• In cattle, s.c. doses ≥55 mg/kg caused fatalities in adult cattle and calves. (Usual therapeutic dose is 7 to 13 mg/kg)
• In cattle and sheep s.c. doses ≥40 mg/kg caused toxic symptoms.
• The therapeutic index for cattle and sheep is ~4.
• As a general rule, at therapeutic doses nitroxinil is well tolerated by cattle and sheep.

Toxic Symptoms caused by Dicyclanil Nitroxinil

• Intoxication symptoms are similar to those of other uncouplers of oxidative phosphorylation.
• They include tachycardia (excessive heart rate), rapid breathing, hyperventilation, fever, increased excitability.

Nitroxinil Side Effects, Adverse Drug Reactions (ADRs) and Warnings

• Swelling and other skin reactions can develop at the injection site.
• Nitroxinil residues in milk can negatively affect cheese production.
• Contaminated hair is stained yellow.

Antidote and Treatment of Dicyclanil Intoxication

• There is no antidote for nitroxinil poisoning.
  
• Treatment consists in supportive and symptomatic measures.

Pharmacokinetics of Nitroxinil

• Injected nitroxinil binds very strongly and almost completely (>97%) to plasma proteins. Concentrations in blood are substantially higher than in the tissues.
• Unchanged nitroxinil is excreted through the liver and this is why high concentrations are found in the bile ducts, the preferential sites of adult liver flukes. It is also metabolized in the liver parenchyma to a metabolite that has flukicidal activity too, which explains its efficacy against late immature flukes that migrate through the liver tissues.
• Metabolism of nitroxinil is rather slow and occurs mainly in the liver. Excretion through feces and urine is quite slow as well, and takes about 30 days to be completed. Excretion half-life in sheep is about 8 days.
• After oral administration, microorganisms in the rumen break it down to ineffective compounds. This is why injectables are preferred over drenches.

Environmental Toxicity of Nitroxinil

• Nitroxinil is highly toxic to fish and aquatic invertebrates.
• Not being used in crop protection or in domestic or public hygiene little is know about its environmental fate.
• It can be assumed that correctly used in livestock nitroxinil is unlikely to be detrimental for the environment, including coprophagous insects.

Additional Information

Click here for a list and overview of all safety summaries of antiparasitic active ingredients in this site.

• Nitroxinil is not used in dogs or cats.
• Nitroxinil is not used in human medicines.
• Nitroxinil is not used in crop pesticides.
• Nitroxinil is not used in biocides for public or domestic hygiene.
• Click here for General safety of antiparasitics for domestic animals.
• Click here for General safety of antiparasitics for humans.
• Click here for General safety of antiparasitics for the environment.
• Click here for technical and commercial information on nitroxinil.