Nitrodox 34% injection

Indications

• Prevention of postoperative nausea and vomiting
• Treatment of nausea and vomiting
• Premedication for surgical procedures

Dosage

Children: Refer to the BNF for Children for age-appropriate dosing guidelines.

Adults: Refer to the BNF for specific dosing recommendations based on the clinical context and patient condition.

Mechanism of action

Droperidol primarily acts as an antagonist at dopamine D2 receptors in the central nervous system. This blockade of dopamine receptors leads to a decrease in nausea and vomiting, as dopamine is a key neurotransmitter involved in these processes. Furthermore, droperidol may also have some affinity for other receptor types, including adrenergic and serotonin receptors, contributing to its sedative and antiemetic effects.

Pharmacodynamics

The pharmacodynamic profile of droperidol includes its ability to reduce the incidence of nausea and vomiting through central action. It can also produce sedation and anxiolytic effects, making it useful in preoperative settings. The onset of action is typically rapid, with effects observed shortly after administration. Droperidol has a dose-dependent relationship, where higher doses may lead to increased sedation and potential extrapyramidal side effects due to its dopamine antagonism.

Pharmacokinetics

Droperidol is well-absorbed after parenteral administration, with peak plasma concentrations occurring within 30 minutes to 1 hour. It is metabolized in the liver, primarily via cytochrome P450 enzymes, and has a relatively short half-life, generally ranging from 1 to 3 hours. Droperidol is excreted mainly in urine as metabolites, with less than 1% of the dose excreted unchanged. The drug's pharmacokinetic profile can be influenced by factors such as age, liver function, and concurrent medications.

Interactions

• droperidol + dopaminereceptor agonists: Severe (decreases effects)
• droperidol + levodopa: Unknown (decreases effects)

Indications

• Fascioliasis
• Liver fluke infections
• Other helminth infections in livestock

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Nitroxynil disrupts the energy metabolism of helminths by interfering with mitochondrial function, leading to depletion of ATP levels. This results in paralysis and death of the parasites, making it effective against certain types of flukes and other parasitic infections.

Pharmacodynamics

The pharmacodynamics of nitroxynil involves its action as a potent inhibitor of oxidative phosphorylation in the mitochondria of parasites. The drug is selectively toxic to helminths, making it safe for use in animals when administered in appropriate doses. Its effects typically manifest through rapid paralysis and destruction of the parasites.

Pharmacokinetics

Nitroxynil is absorbed following administration and is metabolized primarily in the liver. It has a moderate half-life, allowing for effective dosing intervals. The drug's elimination occurs mainly through urine and feces, with metabolites also being excreted. Bioavailability may vary based on the route of administration.

Adverse effects

• Skin irritation
• Nausea
• Vomiting
• Anorexia
• Diarrhea

Precautions

• Use with caution in patients with a history of hypersensitivity to nitroxynil or similar compounds.
• Monitor liver function during treatment, especially in patients with pre-existing liver conditions.

Pregnancy

Nitroxynil should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There is limited data on its safety in pregnant women.

Breast-feeding

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

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Injectable solution