Efficient, safe, and long-lasting insecticides and acaricides are crucial in the fields of pet health management and agricultural pest control. With the popularization of pet keeping, the threat of external parasites such as fleas and ticks to pet health is becoming increasingly prominent. They not only cause pet skin itching and allergies, but may also spread diseases. Meanwhile, agricultural pests have a serious impact on crop yield and quality. Traditional insecticides have gradually exposed problems such as increased resistance, high toxicity to non target organisms, and short duration of action during long-term use. In this context, Fluralaner has emerged as a novel broad-spectrum insecticide of the isoxazoline class, providing new solutions for the control of pet ectoparasites and agricultural pests.
Fluralaner belongs to the class of isoxazoline insecticides, which is a novel chemical structure category. Isoxazoline compounds have unique molecular structures, which enable them to exhibit excellent performance in the field of insecticides. Compared with traditional insecticides such as organophosphorus, carbamate, and pyrethroids, isoxazolines have significant differences in their mechanism of action, selectivity, and activity against target pests, providing a new approach for pest control. It was jointly developed by scientists from Nissan Chemical Industries in Japan and DuPont in the United States. During the research and development process, scientists conducted extensive experiments and screening, and discovered potential insecticidal structures of isoxazoline from numerous compounds. After further structural optimization and activity testing, the chemical structure of Fluralaner was finally determined and an international patent was obtained in 2005. Afterwards, after years of research and clinical trials, in 2014, the US Food and Drug Administration (FDA) approved the veterinary drug Bravecto, which mainly consists of Fluralaner ® Listed for the treatment and prevention of flea and tick infections in dogs and cats. This approval marks Fluralaner's official entry into the pet healthcare market, providing more effective protection for pet health.
The absorption of Fluralaner in pets varies depending on the method of administration. Taking dogs as an example, after oral administration, the peak absorption time (Tmax) of drugs in fasted and fed dogs is basically the same, but drug absorption is better under feeding conditions. The area under the curve (AUC) of Fluralaner and full diet orally administered to dogs for 91 days was 2.1 times that of fasted dogs, and the statistical difference was significant (P<0.05). This indicates that Fluralaner should be taken orally with food, as food can promote its absorption in pets. After oral administration, the average plasma concentration (Cmax) reaches its peak within one day, allowing the drug to quickly take effect and kill parasites on the pet's surface.
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After absorption, Fluralaner is distributed throughout the body of pets, with varying concentrations in different tissues. Among them, the concentration is highest in adipose tissue, followed by liver, kidney, and muscle. This distribution characteristic is related to the physicochemical properties of Fluralaner, which has a certain degree of lipid solubility and is prone to accumulation in adipose tissue. The higher concentrations in the liver and kidneys are related to the metabolism and excretion of drugs. The liver is the main organ for drug metabolism, while the kidneys are an important pathway for drug excretion. The distribution in muscle tissue enables drugs to work throughout the pet's body, effectively killing parasites in various parts.
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The metabolism and excretion process of Fluralaner in pets is relatively slow. In dogs, it is almost not metabolized and is mainly excreted in its original form through feces, with a small amount excreted through the kidneys. The half-life of plasma elimination is about 12-15 days, with an average retention time of 15-20 days. This longer half-life and retention time enable Fluralaner to maintain an effective blood concentration in pets for a longer period of time after administration, and to have long-lasting insecticidal activity after a single dose. For example, after oral administration of Fluralaner to dogs, its effectiveness in controlling fleas and ticks can last for 12 weeks, greatly reducing the frequency of administration and facilitating the use of the medication by pet owners.
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