Pikaridin
Pikaridin Uses, Dosage, Side Effects, Food Interaction and all others data.
Pikaridin, also known as Picaridin or hydroxy-ethyl isobutyl piperidine carboxylate, is a cyclic amine and a member of the piperidine chemical family. Piperidines are structural components of piperine, which is a plant extract from the genus _Piper _, or pepper. Pikaridin has been commonly used as a topically-applied insect repellent in various countries but was officially licensed for use in the United States in 2001 and Canada in 2012 . Pikaridin was synthesized by Bayer in the 1980s based on molecular modeling . It is considered to be the first choice of repellent by the Public Health Agency of Canada’s Canadian Advisory Committee on Tropical Medicine and Travel for travelers six months to 12 years of age . Pikaridin is reported to be less irritating than Diethyltoluamide, another common insect repellant, and products containing up to 20% of icaridin are considered safe for long-term use in adults .
Pikaridin is a cyclic amine and piperidine compound that is expected to stimulate the sensory hairs on the antennae of insects .
| Trade Name | Pikaridin |
| Generic | Icaridin |
| Icaridin Other Names | Icaridin, Icaridina, Icaridinum, Picaridin, Pikaridin, Propidine |
| Type | |
| Formula | C12H23NO3 |
| Weight | Average: 229.3159 Monoisotopic: 229.167793607 |
| Protein binding | There is no available information on the protein binding of icaridin. |
| Groups | Experimental |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Pikaridin is indicated for use to repel insects, such as mosquitoes, biting flies, ticks, chiggers, and fleas, via topical use or over clothing .
Pikaridin is also used to associated treatment for these conditions: Insect Bites
How Pikaridin works
The exact mechanism and target molecules of icaridin repelling insects are not fully understood; it is presumed that piperine interacts with the olfactory system consisting of odorant receptors (ORs) that need a common co-receptor (ORCO), and of ionotropic receptors (IR) , leading to the insect's inability to recognize its host's cues . It is also suggested that icaridin may bind to odorant binding protein 1 (AgamOBP1) at different binding sites . A study demonstrated that icaridin inhibited the odorant-induced responses of AaOR2 and AaOR8 expressed in Xenopus oocytes, leading to altered olfactory inputs by olfactory sensory neurons (OSN) .
Toxicity
Oral LD50 values in fasted and non-fasted male rats were 2236 mg/kg and 4743 mg/kg, respectively . Acute dermal LD50 values in rats were greater than 2000 mg/kg and 5000 mg/kg . The LC50 over a 4-hour exposure period exceeded 4364 mg/m^3 in male rats, and the NOEL was determined to be 2153 mg/m^3 . While icaridin is considered to be practically non-toxic upon dermal and inhalation exposure , there have been cases of allergic contact dermatitis associated with pruritis and erythema upon dermal application .
In an animal study following application of icaridin to the skin of rats at doses of 50, 100, or 200 mg/kg/day each weekday for two years, there were no signs of potential carcinogenicity . The United States Environmental Protection Agency claims that icaridin is not likely to be carcinogenic to humans . In a two-generation reproductive study on rats, administering 50, 100, or 200 mg/kg icaridin to the rats' skin weekly beginning 10 weeks before mating and continuing through to weaning of the pups. Findings from the study concluded that chronic icaridin exposure to the skin at doses as high as 200 mg/kg did not result in reproductive toxicity .
Food Interaction
No interactions found.Volume of Distribution
In a rat study, dermal application of icaridin at doses of either 20 mg/kg or 200 mg/kg resulted in plasma concentrations ranging from 0.5 μg/ml for males and 0.8-1.6 μg/ml for females in the 20 mg/kg test group, and 4.48 μg/ml in male rats and 1.70 μg/ml and female rats in the 200 mg/kg test group . Pikaridin applied to the arms of human volunteers was not found in blood plasma .
Elimination Route
In a dermal metabolism rat study, dermal application of 20 mg/kg of radio-labeled icaridin resulted in 61-66% of the dose absorbed through the skin . Following topical application of 20 mg/kg on rats, the peak plasma concentrations were measured to be 0.5 μg/mL in male rats and 0.8-1.6 μg/mL in female rats . In a study of human volunteers, less than 6% of the applied doses were absorbed after topical application of 14.7 or 15.0 mg of technical grade icaridin and covering the application site with a protective wrap for eight hours .
Half Life
The first elimination half-lives of icaridin were determined in a study of five male and female rats treated with a single dose of 20 mg/kg icaridin dermally. The half-lives were 35.7 hours for male and 23.9 hours in female rats . In another study of rats treated daily for 2 weeks with 20 mg/kg of unlabeled icaridin, followed by exposure to a single dose of 20 mg/kg of the radiolabeled icaridin for 7 days, the 1st elimination half-lives were 10.9 and 9.1 hours for the males and females, respectively . The 2nd half-lives were 144 and 105 hours, respectively .
Clearance
There is no available information on the clearance of icaridin.
Elimination Route
Following topical administration on rats at doses of 20 mg/kg, urinary excretion was reported to be the primary route of elimination where 73-88% of the parent compound was recovered in the urine . At doses of 200 mg/kg, 33-40% of the administered dose was excreted in the urine or feces . No data were available on the composition of parent compound and metabolites in the urine of either animals or humans .
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