The History of Icaridin

Written by: Dr. Hamza A. Khan, MBBS
Abstract
Icaridin is an insect-repellent that prevents bites from mosquitos, fleas, ticks, biting flies, and other such insects. It is one of the most effective products developed to date without the same side effects as others. As a result, it is widely used in sprays, lotions, and wipes for application on the skin. However, Icaridin was not the first insect-repellent to be developed. So, before we get into the history of Icaridin, we should know the history of insect repellents in general.
History Of Insect-Repellents
Insects have made human lives miserable as far back as we can remember. Mosquitos, for example, are considered humanity’s greatest foe, killing nearly half of all the humans who ever walked on this planet. Estimates are that more than 108 billion people have lived on earth in the last 200,000 years, and 52 billion of which were killed by mosquito-borne diseases (1). Even today, malaria (a mosquito-borne disease) alone kills more than half a million people every year (2).
Thus, humans had no choice but to find ways to protect themselves from such creatures. As soon as we industrialized, we found various ways to get rid of them. The aim of most of these preventive strategies was to prevent insects from flourishing in the first place. But there was a problem! What if you suddenly find yourself in an insect-ridden area? What if there was no time to implement preventive strategies? This is primarily the case with military personnel who often find themselves in such places. What can you do, then, against these deadly creatures?
This was the problem that led the US military to find chemicals to protect soldiers following its experience of jungle warfare in World War 2. Thus, the first insect repellent DEET, a derivative of coconut oil, was found. Samuel Gertler of the US Department of Agriculture first developed DEET in 1944. Later in 1946, the US military began to use it for the protection of soldiers, and the inventor received the patent to use it in commercial products in the form of sprays, lotions, and creams (3)(4). However, DEET was not registered for use by the general public until 1957, when it was approved by the Environmental Protection Agency (EPA) (5).
The chemical name of DEET is N, N-diethyl-meta-toluamide. It is available in concentrations between 4 to 100 percent in over 230 products registered with the EPA (6). It is effective against most insects and protects for an average of 8 to 10 hours against various insects (7). However, the duration of its protection and efficacy depends upon its concentration. According to the Center for Disease Control, a solution of 50 percent DEET gives the best results, and higher concentrations do not provide any added protection (8). Over the decades, it has become immensely popular, and nearly 30 percent of the US population uses DEET in one product or the other (9).
Some more insect-repellent products have recently made their way onto the market. One such example is IR3535 which was introduced in 1999 (10). It offers good protection for a long while but is not as effective as DEET or Icaridin.
History Of Icaridin
DEET became an instant hit as it provided the necessary protection in unusual circumstances. But there were many issues with it. First of all, it has a greasy feeling on the skin, which most people do not like. Plus, it has an unpleasant smell, can cause eye irritation, causes skin irritation or rash when used over a long period, and dissolves plastics and degrades rubber. In addition, though very rarely, DEET exposure has been linked to neurotoxicity (11). Thus, DEET use was a constant nuisance for many people as there were no alternatives.
These problems with the DEET made scientists look for equally effective alternatives without the same side effects. Ultimately, scientists at a German company named Bayer AG took the challenge and developed one more insect-repellent known as Icaridin in the 1980s (12). It was developed under the laboratory code name KBR 3023. However, it began to gain popularity in the late 90s and early 2000s. Bayer AG first sold Icaridin under the trade name Bayrepel. It has been commercialized in the European and Australian markets since 1998 (13). Other trade names include Saltidin, Autan, etc.
The name Picaridin was proposed to WHO as the International Non-proprietary Name (INN) -- the official generic name given to a pharmaceutical drug or active ingredient. However, WHO approved Icaridin as the official INN. The chemical name of Icaridin is hydroxyethyl isobutyl piperidine carboxylate. Also known as Picaridin, Icaridin is a synthetic chemical in the naturally occurring piperidine family. Thus, it only mimics the properties of piperidine. Piperidine is found in plants whose extracts are used to make black pepper -- the common spice on your dinner table. It is the reason why various kinds of peppers remain a popular home remedy to repel insects to this day.
(13). Most of the products today have a concentration of 20 percent. This is the optimal concentration because the efficacy or duration of icaridin protection does not increase beyond it. The average duration of Icaridin protection is more prolonged than DEET-- between 10 to 12 hours against various insects (14)(15). Icaridin-based products like TotalSTOP also offer more potent protection than DEET-based products (16).
Since Icaridin offered a better solution to the problem of insects, it has begun to gain wide recognition. More and more research is being done to see whether its claims are valid or just a hoax. And so far, most of the research has been promising. It does not cause the same side effects as DEET. It is also safe for children and pregnant women. As a result, public health institutions and world organizations like WHO have begun to recommend Icaridin as the insect-repellent of the first choice (17)(18). Thus, Icaridin continues to increase its market share in the insect-repellent market.
History Of Icaridin In The US And Canada
Icaridin reached the United States in 2001 when the EPA first approved it for use by the general public (19). However, it was not until 2005 that the first commercial product containing Icaridin became available (20). In this first product, the Icaridin concentration manufacturers used was 7 percent (21). But over time, as Icairidin's popularity grew and more commercial products were introduced, the concentration increased. These days, most products have a concentration of 20 percent. However, Health Canada approved Icairidin in 2012 (22).
DEET remained the most dominant insect repellent in the US market. As a result, it was studied extensively and became the gold standard for judging other repellents. However, the drawbacks DEET had made it unattractive and aesthetically unpleasant early on. But there were no alternatives, and many people had to buy something to protect themselves against the menace of insects. But that is all changing now. Icaridin has become widely popular, not only in North America but also in the rest of the world. Icaridin is being sold under many trade names, and as more and more people get familiar with the product, its consumer base is increasing substantially.
Icaridin is also known as Picaridin in the US as it is the name it was first registered with the EPA. Many Icaridin-based products use Picaridin as the official name of the ingredient on their labels.
Final Words
North America is a very diverse content. There are ice caps and glaciers, various mountain ranges, jungles, deserts and canyons, and many more landscapes. While these places are a beauty to behold, they are full of many kinds of living organisms, some friendly and some extremely hostile. Among such creatures are the ticks, flies, mosquitos, and other arthropods that, although they seem very harmless, are very dangerous. It’s not the insects themselves that are dangerous for humans, but rather the microbes they carry in their guts and spread to humans. Thus, it becomes crucial you prevent bites from these insects. And the primary defense you have got is in the form of insect repellents.
Diseases spread by ticks are widespread in the US and Canada. For example, Lyme disease spread by ticks is extremely common in North America, affecting 300,000 people each year in the US alone (23). Other diseases spread by ticks, flies, mosquitos, and other insects in North America include West Nile virus disease, Rocky Mountain spotted fever, plague, tularemia, and dengue fever. These diseases are also equally dangerous, but their incidence is low. So if you live in an insect-ridden place or occasionally go to one for vacations or any other purpose, make sure you got an insect-repellent. Products like TotalSTOP have you covered in this matter.

TotalSTOP is a DEET-free insect repellent utilizing Icaridin as an active ingredient. Icaridin is recommended by the World Health Organization (WHO), the CDC, and is EPA-Registered. It provides long-lasting, 12-hour protection from all kinds of ticks and mosquitos and 10-hour protection from black flies.
Icaridin is approved for use in 40+ countries, and TotalSTOP is perfect for the whole family including individuals with skin sensitivities, children that are 6+ months, pregnant, and nursing mothers!
TotalSTOP is available in spray & wipes. It is non-toxic, odourless & water-resistant with a non-greasy formula that lasts all day.
References And Citations:
- Reese, H. (2019, August 13). Mosquitoes might be humanity’s greatest foe. Should we get rid of them? Vox. https://www.vox.com/the-highlight/2019/8/13/20754834/mosquitoes-blood-type-zika-dengue
- Malaria. (n.d.). Who. Int. Retrieved May 7, 2022, from https://www.who.int/news-room/fact-sheets/detail/malaria
- Publication : USDA ARS. (n.d.). Usda.Gov. Retrieved May 7, 2022, from https://www.ars.usda.gov/research/publications/publication/?seqNo115=353864
- Smithsonian Lemelson Center. (2014, May 20). Buzz... Swat: Mosquito repellents. Lemelson Center for the Study of Invention and Innovation. https://invention.si.edu/buzz-swat-mosquito-repellents
- Epa, U. S., & OCSPP. (2013). DEET. https://www.epa.gov/insect-repellents/deet
- PubChem. (n.d.). Diethyltoluamide. Nih.Gov. Retrieved May 7, 2022, from https://pubchem.ncbi.nlm.nih.gov/compound/Diethyltoluamide
- Tawatsin, A., Thavara, U., Chansang, U., Chavalittumrong, P., Boonruad, T., Wongsinkongman, P., Bansidhi, J., & Mulla, M. S. (2006). Field evaluation of deet, Repel Care, and three plant-based essential oil repellents against mosquitoes, black flies (Diptera: Simuliidae), and land leeches (Arhynchobdellida: Haemadipsidae) in Thailand. Journal of the American Mosquito Control Association, 22(2), 306–313. https://doi.org/10.2987/8756-971X(2006)22[306:FEODRC]2.0.CO;2
- Fact Sheet for the general public. (n.d.). Cdc.Gov. Retrieved May 7, 2022, from https://www.cdc.gov/malaria/toolkit/deet.pdf
- DEET. (n.d.). Orst.Edu. Retrieved May 7, 2022, from http://npic.orst.edu/factsheets/DEETgen.html
- Carroll, S. P. (2008). Prolonged efficacy of IR3535 repellents against mosquitoes and Blacklegged ticks in North America. Journal of Medical Entomology, 45(4), 706–714. https://doi.org/10.1093/jmedent/45.4.706
- (N.d.). Consumerreports.Org. Retrieved May 7, 2022, from https://www.consumerreports.org/insect-repellent/how-safe-is-deet-insect-repellent-safety-a4952100929/
- PubChem. (n.d.). Icaridin. Nih.Gov. Retrieved May 7, 2022, from https://pubchem.ncbi.nlm.nih.gov/compound/Icaridin
- Sangha, G. K. (ghona). (2010). Toxicology and safety evaluation of the new insect repellent picaridin (saltidin). In Hayes’ Handbook of Pesticide Toxicology (pp. 2219–2230). Elsevier.
- Costantini, C., Badolo, A., & Ilboudo-Sanogo, E. (2004). Field evaluation of the efficacy and persistence of insect repellents DEET, IR3535, and KBR 3023 against Anopheles gambiae complex and other Afrotropical vector mosquitoes. Transactions of the Royal Society of Tropical Medicine and Hygiene, 98(11), 644–652. https://doi.org/10.1016/j.trstmh.2003.12.015
- Büchel, K., Bendin, J., Gharbi, A., Rahlenbeck, S., & Dautel, H. (2015). Repellent efficacy of DEET, Icaridin, and EBAAP against Ixodes ricinus and Ixodes scapularis nymphs (Acari, Ixodidae). Ticks and Tick-Borne Diseases, 6(4), 494–498. https://doi.org/10.1016/j.ttbdis.2015.03.019
- Badolo, A., Ilboudo-Sanogo, E., Ouédraogo, A. P., & Costantini, C. (2004). Evaluation of the sensitivity of Aedes aegypti and Anopheles gambiae complex mosquitoes to two insect repellents: DEET and KBR 3023. Tropical Medicine & International Health: TM & IH, 9(3), 330–334. https://doi.org/10.1111/j.1365-3156.2004.01206.x
- Myth breaker on dengue fever. (n.d.). Gov.Hk. Retrieved May 7, 2022, from https://www.chp.gov.hk/files/pdf/mythbreakerseries_df_03_eng.pdf
- (N.d.). Ewg.Org. Retrieved May 7, 2022, from https://static.ewg.org/reports/2013/bug_repellents/2013_EWGs_Guide_to_Bug_Repellents.pdf
- United States prevention, pesticides environmental protection and toxic substances May 2005 agency (7505C). (n.d.). Epa.Gov. Retrieved May 7, 2022, from https://www3.epa.gov/pesticides/chem_search/reg_actions/registration/fs_PC-070705_01-May-05.pdf
- Frances, S. (2006). Picaridin. In Insect Repellents (pp. 337–340). CRC Press.
- Sangha, G. K. (ghona). (2010). Toxicology and safety evaluation of the new insect repellent picaridin (saltidin). In Hayes’ Handbook of Pesticide Toxicology (pp. 2219–2230). Elsevier.
- (N.d.). Publications.Gc.Ca. Retrieved May 7, 2022, from https://publications.gc.ca/collections/collection_2011/sc-hc/H113-9-2011-10-eng.pdf
- NCEZID: Vector-borne Diseases (spread by bites from mosquitoes, ticks, or fleas). (2019, December 18). Cdc.Gov. https://www.cdc.gov/ncezid/what-we-do/our-topics/vector-borne-diseases.html