Insect repellents: An overview

doi:10.1016/S0190-9622(97)70289-5

Journal of the American Academy of Dermatology

Volume 36, Issue 2, February 1997, Pages 243-249

https://doi.org/10.1016/S0190-9622(97)70289-5 Get rights and content

Abstract

The optimal management of arthropod bites is prevention, and many over-the-counter insect repellents are available. Since first marketed in 1956, deet has remained the most effective repellent against mosquitoes, biting fleas, gnats, and chiggers. Permethrin is applied to clothing rather than to skin, and it is a better repellent against ticks than deet. The risk of serious side effects with the use of deet is slight; nevertheless, the lowest effective concentration should be used. The current, popular repellent agents (for adults and children) and their active ingredients are discussed. In addition, the Environmental Protection Agency guidelines for the safe use of insect repellents are supplied. (J Am Acad Dermatol 1997;36:243-9.)

Section snippets

BACKGROUND

Historically, repellents have included types of smoke, plants hung in dwellings or rubbed on the skin, oils, tars, and even camel urine. ⁷ Before World War II, there were only four main repellents: (1) oil of citronella, discovered in 1901; (2) dialkyl phthalates, discovered in 1929; (3) indalone, introduced in 1937; and (4) Rutgers 612, which became available in 1939. ⁷

DEET

Most early and recent research on insect repellents has been done by the U.S. Armed Forces in conjunction with the Department of Agriculture because military personnel in World War II, the Korean War, the Vietnam conflict, and Operation Desert Storm faced exposure to multiple arthropods that caused local and systemic reactions and were vectors for many diseases. Clinical trials began in 1942, with compounds selected at random from various commercial, governmental, or college laboratory shelves;

PERMETHRIN

Permethrin is both an insecticide and a repellent. It is active against a wide range of pests including lice, ticks, fleas, mites, mosquitoes, and black flies. It kills ticks on contact. ¹³ Percutaneous absorption of permethrin in humans is minimal, ¹³ and mammalian toxicity appears to be low. ¹⁵ A 5% cream (Elimite) is used against scabies mites, and a 1% cream rinse (Nix) is used against nits (the eggs of head lice). No serious adverse events were encountered in 18,950 patients treated with

CONCLUSION

The most effective repellent for preventing the bites of mosquitoes, black flies, midges, biting fleas, and chiggers is deet. Permethrin remains the best repellent against ticks. Insect repellents may have toxic effects, but when used according to the Environmental Protection Agency guidelines ³⁶ (Table II) , they can provide a safe means of minimizing the risk of bites and vector-borne diseases.

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Cited by (257)

Challenges encountered by natural repellents: Since obtaining until the final product
2023, Pesticide Biochemistry and Physiology
Vector-borne diseases, particularly the arboviruses dengue, Zika, chikungunya, and yellow fever caused by the Aedes aegypti mosquito, have been driving the use of repellents worldwide. The most representative synthetic repellent, DEET stands out as the market's oldest and most efficient repellent. It is considered a reference standard but presents considerable toxicity, not recommended for children up to 6 months old and pregnant women. For this reason, alternatives have been sought, and natural repellents derived mainly from essential oils have been studied, highlighting the essential oils of lemon (Corymbia citriodora), citronella (Cympobogon sp.), Andiroba (Carapa guianensis). However, the development and commercialization of products containing natural repellents are significantly lower when compared to DEET and other synthetic repellents. In order to understand the reasons, aspects related to safety, mechanism of action, efficacy as well development and complexity of the products were evaluated. It is concluded that, as for safety, there is lacking information in the literature regarding the effects on non-target organisms and robust toxicity data. The mechanism of action is based on theories, with less information on the exact mode of action, molecular targets, and interaction with the olfactory and taste receptors of insects. Despite being a current trend to search for actives from natural sources highly present in essential oils, however they reduced action time because due to rapid evaporation after application to the skin, thus requiring repellent vehicles. The development and complexity related to these products bring challenging aspects, beginning on the plant cultivation and extraction processes to produce essential oils with a more homogeneous chemical composition towards the formulation stabilization processes due to fast evaporation and short action time, with the use of pharmaceutical technology such as encapsulation techniques.
Nanoemulsion as a promising carrier of plant-derived repellents for mosquito-borne malaria control: Nanotechnology aspects
2023, Natural Products in Vector-Borne Disease Management
Malaria is transmitted by mosquito anopheles and the disease remains a main cause of illness and death in the world, particularly in endemic regions, i.e., sub-Saharan Africa. Furthermore, the growing trend of pyrethroid resistance constitutes a serious threat to malaria control programs. The need for development of new ecological methods for mosquito control and the continuous increase of resistance of mosquitos to insecticides like pyrethroids have encouraged study into repellents. Nanoemulsions-based repellents have demonstrated a great controlled release potential for Malaria control. The nanoemulsions are promising systems to be used in different fields because they have attractive properties of small size and high surface area. This chapter discusses the content about nanoemulsions as carriers for plant-based repellents for malaria control, focusing first on introduction, and the preparation and stability of nanoemulsion. Additionally, the methods of characterization of nanoemulsions and their application as product based on essential oils against mosquito-borne malaria were reported and discussed. Finally, we present conclusions and recommendations.
Insect repellents: An updated review for the clinician
2023, Journal of the American Academy of Dermatology
Malaria, Zika virus, West Nile virus, Dengue fever, and Lyme disease are common causes of morbidity and mortality around the world. While arthropod bites may cause local inflammation and discomfort, a greater concern is the potential to develop deadly systemic infection. The use of insect repellents (IRs) to prevent systemic infections constitutes a fundamental public health effort. Cost effectiveness, availability, and high efficacy against arthropod vectors are key characteristics of an ideal IR. Currently, numerous IRs are available on the market, with N,N-diethyl-3-methylbenzamide (DEET) being the most widely used. DEET has an excellent safety profile and remarkable protection against mosquitoes and various other arthropods. Other Environmental Protection Agency–registered IR ingredients (eg, permethrin, picaridin, IR3535, oil of lemon eucalyptus, oil of citronella, catnip oil, and 2-undecanone) are alternative IRs of great interest because some of these ingredients have efficacies comparable to that of DEET. These alternative IRs possess low toxicity and favorable customer experiences in use (eg, cosmetically pleasant, naturally occurring). This review summarizes the currently available Environmental Protection Agency–registered IRs, including their origins, mechanisms of action, side effect profiles, and available formulations. This review will enable the clinician to select the best IR option to meet a patient’s needs and provide the greatest protection from arthropod bites and their sequelae.
Theoretical investigation on degradation of DEET by •OH in aqueous solution: Mechanism, kinetics, process optimization and toxicity evaluation
2022, Journal of Cleaner Production
N, N-diethyl-3-methylbenzamide (DEET), as a widely used insect repellent, is frequently detected in the environment. UV/H₂O₂ is a valid technology to remove trace contaminants by generating hydroxyl groups. The density functional theory (DFT) calculation method was used to investigate the degradation mechanism and kinetics of DEET in water environment. •OH can attack DEET in two main modes, H-abstraction and •OH-addition, showing different reactivity. H-abstraction reaction is easier to occur compared with •OH-addition reaction. Especially the hydrogen on branch chain of DEET is more readily to be attacked by •OH. In the aqueous phase, the total rate constant is 2.04 × 10⁹ M⁻¹ s⁻¹ at 298 K. Calculated results showed that R5, R6, R8, R9 and R12 paths preferentially occur. Under alkaline conditions, it can significantly inhibit the DEET degradation. The influence of natural organic matter (NOM) in water and oxidant dosage, DEET concentration was also considered. The response surface methodology (RSM) was used to optimize the process parameters. The maximum degradation efficiency of 95.64% can be achieved under optimal conditions. Since most of the products are homologues of the parent compound, their acute and chronic toxicity are not significantly reduced. The products are non-mutagenic and non-bioconcentrated, but they are developmentally toxic.
Novel acylpiperidine analogues as potential aphid repellent agents: Rational design, synthesis and repellent activity
2022, Journal of Molecular Structure
Odorant-binding protein (OBP) is a promising potential target and can be used as a template for developing insect control agents due to its ability to bind to and transport semiochemicals to olfactory receptors, thus triggering behavioural responses among insects. In this study, 27 novel acylpiperidine analogues were designed and synthesised by introducing the hydrophobic long chain of the aphid alarm pheromone (E)-β-farnesene (EβF) into the polar acylpiperidine group of the commercial insect repellent icaridine based on the binding cavity characteristics of an OBP of the pea aphid Acyrthosiphon pisum, ApisOBP3. Compound 14c displayed good repellent activity against the pea aphids with a repellence rate of 61.5% at a concentration of 6 μg/μL. The equilibrium dissociation constant (K_i) of compound 14c against ApisOBP3 was 20.92 μM in competitive fluorescence binding assays; this value is similar to the K_i of the commercial insect repellent icaridine (20.56 μM). Molecular dynamics simulation revealed that the EβF long chain of compound 14c showed considerable hydrophobic interactions with the binding domain of ApisOBP3. Moreover, the acylpiperidine moiety of compound 14c formed one hydrogen bond and multiple carbon–hydrogen bonds with the Phe2 and Asn109 residues, respectively. The binding free energy analysis indicated that the contribution of the van der Waals force to the binding affinity was approximately twice as great as that of the electrostatic force. These studies provide significant guidance for the rational designing and efficient identification of novel insect repellent agents.
Recent advances in degradation of N,N-diethyl-3-toluamide (DEET)—an emerging environmental contaminant: a review
2024, Environmental Monitoring and Assessment

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^☆: Reprint requests: Adelaide A. Hebert, MD, Department of Dermatology, The University of Texas Medical School, 6431 Fannin, MSB 1.186, Houston, TX 77030.

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Insect repellents: An overview☆,☆☆

Abstract

Section snippets

BACKGROUND

DEET

PERMETHRIN

CONCLUSION

The attraction of mosquitoes to hosts

JAMA

Insects: topical insect repellents

Clin Pharmacol Ther

Relationships between insect repellency and chemical and physical parameters: a review

J Med Entomol

Use of insect repellents for maximum efficacy

Arch Dermatol

A study of insect repellents: II. Effect of temperature on protection time

J Econ Entomol

Mosquito attraction and repulsion

Nature

The Pesticide Book

San Francisco: WH Freeman

Insect repellents and attractants

J Agr Food Chem

Development of a systemic insect repellent

JAMA

Mosquito repellents: Being a report of the work of the mosquito repellent inquiry, Cambridge 1943-1945

J Hyg

Some corrections to the record on insect repellents and attractants

J Am Mosq Control Assoc

Prevention of Lyme disease: review

Am J Hosp Pharm

Field studies of tick repellents

Am J Trop Med Hyg

Synthesis of insect-repellent amino analogs of 2-ethyl-1,3-hexanediol (Rutgers 612)

J Med Chem

Observations on tick repellents

J Econ Entomol

Analysis of N,N -diethyl-m-toluamide (DEET) in human postmortem specimens

J Forensic Sci