BRAVECTO® Plus Solution

Indications

• Flea infestation
• Tick infestation
• Prevention of flea and tick infestations

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing information regarding fluralaner.

Adults: Refer to the BNF for specific adult dosing guidelines, as fluralaner dosing may vary based on the weight of the animal and the formulation used.

Mechanism of action

Fluralaner acts as a potent inhibitor of the insect GABA-gated chloride channels and the glutamate-gated chloride channels. By blocking these channels, fluralaner disrupts the normal function of the nervous system in parasites, leading to paralysis and death of the flea and tick species.

Pharmacodynamics

Fluralaner exhibits a high level of selectivity for the target channels found in arthropods, resulting in reduced toxicity to mammals. Its efficacy against fleas and ticks is attributed to its ability to cause rapid paralysis and mortality in these parasites upon exposure.

Pharmacokinetics

Fluralaner is absorbed rapidly after oral administration, reaching peak plasma concentrations within 1-2 days. It has a high volume of distribution and is extensively metabolized in the liver. The elimination half-life ranges from several days to weeks, depending on the species treated. Fluralaner is excreted primarily in feces, with minimal renal excretion.

Adverse effects

• Vomiting
• Diarrhea
• Anorexia
• Lethargy
• Hypersensitivity reactions

Precautions

• Use with caution in animals with a history of seizures
• Not recommended for use in breeding, pregnant, or lactating animals

Pregnancy

Safety during pregnancy has not been established.

Breast-feeding

Safety during lactation has not been established.

Storage

Store at room temperature, protect from moisture and light.

Formulations

• Oral solution
• Topical solution

Indications

• Onchocerciasis
• River blindness

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Moxidectin selectively binds to the parasite's GABA-A and glutamate-gated chloride ion channels, essential for the functioning of invertebrate nerve and muscle cells. This binding increases the permeability of the cell membranes, allowing an influx of chloride ions, which results in flaccid paralysis of the parasite without directly killing it.

Pharmacodynamics

Moxidectin has shown remarkable efficacy against _Onchocerca volvulus_, demonstrating a superior ability to reduce microfilarial loads in infected individuals compared to ivermectin. The administration of moxidectin leads to a significant decrease in microfilariae levels to undetectable amounts, making it suitable for mass drug administration, while maintaining safety.

Pharmacokinetics

Moxidectin is well absorbed after oral administration with a long half-life, allowing for less frequent dosing compared to other treatments. Its pharmacokinetic profile supports its use in mass treatment strategies for onchocerciasis, although specific parameters such as absorption rate, distribution volume, and elimination route require detailed clinical studies for comprehensive understanding.

Pregnancy

There are no adequate data from the use of moxidectin in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is unknown whether moxidectin is excreted in human breast milk. Caution should be exercised when moxidectin is administered to a nursing woman.

Storage

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

Mechanism of action

Moxidectin selectively binds to the parasite's GABA-A and glutamate-gated chloride ion channels which are vital for the function of invertebrate nerve and muscle cells. It presents activity against the parasite but it does not kill him. Once moxidectin is bound, there is an increased permeability leading to an influx of chloride ions and flaccid paralysis of the parasite.

Pharmacodynamics

Moxidectin has been reported to be highly effective against _Onchocerca volvulus_ when compared to ivermectin. When moxidectin was administered in infected individuals, the microfilarial load in the skin was lower even when compared to the current therapy, ivermectin. The levels of microfilarial got reduced to an undetectable level while being safe to be used in mass drug administration.