Insect Repellents Handbook, Second Edition

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Several broadspectrum insect repellents are known antagonists of insect olfactory receptors, including deet,30 picaradin,25 and IR The -ant form of this word is etymologically correct not arrestent , being derived from the Latin arrestare. Creatures with exoskeleton consisting of chitin and jointed legs. Numerous other groups of animals affect humans directly through bites or envenomation e. Repellents may be useful against all these biters. Associated terms: to attract vb ; attractance n , the quality of attracting; attraction n , the act of attracting or the state of being attracted; and attractive adj.

Oviposition attractant serves for gravid females to locate suitable oviposition sites, e. According to this directive, member states had to transpose the rules before May 14, into national law. The Biocidal Product Directive aims to harmonize the European market for biocidal products and their active substances. At the same time, it aims to provide a high level of protection for humans, animals, and the environment. Biological variables that may influence repellency, such as physiological condition of the insect e. For ethical reasons, especially where vector-borne disease risks must be considered, it is customary to intercept the attacking insects before they actually bite possibly increasing catch efficiency ; the results are therefore reported in terms of the landing rate rather than the biting rate.

Other criteria for repellent testing under field conditions are the period of time to first bite TFB , or first confirmed bite, or duration of a reduction in biting, the choice of criterion depending inter alia on the local biting rate pressure. CAS numbers: unique numerical identifiers for chemical compounds, polymers, mixtures, and biological sequences.

Society, assigns these identifiers to every chemical described in the literature. Substances also receive unique CA index names, constructed using rigid nomenclature rules. In an effort to facilitate searching for related compounds, the most important functional groups of a substance are named first, followed by their modifications cf. Department of Health and Human Services. Insect ORs structurally and genetically unrelated to vertebrate receptors consist of two distinct molecules54 serving as receptor for the odorant and as an ion channel that is gated by the binding of the odorant.

Methods are proposed by manufacturers companies and tested internationally by the interlaboratory program for evaluation of test methods. Chapter VI of the U. Code, plus amendments currently administered by the FDA , defines cosmetics as articles intended to be applied to the human body for cleansing, beautifying, and. Products such as skin creams, lotions, perfumes, lipsticks, fingernail polishes, eye and facial makeup preparations, shampoos, permanent waves, hair colors, toothpastes, deodorants, and any material intended for use as a component of a cosmetic product are included in this definition.

Soap products consisting primarily of an alkali salt of a fatty acid and making no label claim other than cleansing the human body are not considered cosmetics under U. Likewise, insect repellents are not cosmetic products, although it would be possible to include repellent active ingredients in particular cosmetics as done with some sun screen anti-UV preparations combined with deet that enhances absorption, raising systemic toxicity 56 marketed for giving skin protection against both sunburn and biting insects.

The term cosmetic properties of a repellent product is often used to describe the properties of the formulation that do not affect performance but alter the subjective perception of the product e.

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DDT: dichlorodiphenyltrichloroethane insecticide. It is the dominant repellent used worldwide since the s. Globally, it is the leading active ingredient of insectrepellent products, being effective against all groups of biting arthropods and even leeches. Deet is registered for use by consumers, plus a few veterinary uses, but not for food treatment.

Market surveys in the United States show that about a third of the population uses deet-based products, currently available to the public in a variety of liquids, lotions, sprays, and impregnated materials e. Army in , deet was introduced for use by the general public in Further details on deet are given in Chapters 14, 18, and Associated terms include deter vb , to discourage or prevent, and deterrence n , the act of deterring. These terms fit the way that permethrin-impregnated materials e. Diptera: the insect order Diptera recognized by Aristotle in the fourth century bc includes approximately families of two-winged flies, true flies.

In repellent testing methodology, it is important that repellents are tested in noncompetitive assays to prevent diversion of mosquitoes onto controls that would result in overestimation of the efficacy of a repellent. EAG: electroantennogram. Paul, Minnesota. EIR: entomological inoculation rate. An important component is the surfactant emulsifier e. EPG: electropalpogram eradicate to completely remove or destroy a species or disease so that it cannot return cf.

Among the ones most effective78 as repellents are white cedar oil CAS number , peppermint oil CAS number , red thyme oil CAS number , bourbon geranium oil CAS number , linalool, and dehydrolinalool. When exposed to excitorepellent insecticides,46 mosquitoes tend to move toward light, resulting in their escape from treated houses. Department of Health and Human Services, having regulatory responsibility for cosmetics and medicines, and so on, but not for insect repellents. FDA status.

Good Field Practice and Good Laboratory Practice GFP and GLP : internationally recognized standards of conduct and procedure administered by the Organisation for Economic Co-operation and Development OECD to ensure the generation of high-quality and reliable test data related to the safety of industrial chemical substances and preparations in the framework of harmonizing testing procedures for Mutual Acceptance of Data www.

Appropriately limited to natural products, such as essential oils from plants Chapters 5, 9, and For repellents and other pesticides, the WHO classification87 based on rat LD50 by weight, following oral or dermal exposure, assuming solids are fourfold more hazardous than liquids, recognizes the following categories: class Ia, extremely hazardous; class Ib, highly hazardous; class II, moderately hazardous e.

Dogan and Rossignol90 describe an olfactometer for discriminating between attraction, inhibition, and repellency in mosquitoes. This mode of action has been demonstrated to function by inhibiting odorant-evoked currents30,89 mediated by odorant receptors ORs. Almost a million species of insects have been scientifically recognized.

The word insect derives from the Latin insectum for having been cut, referring to the articulated body. Adult insects typically have three pairs of legs hexapod. Main groups of insects comprise about 30 orders, with the order Diptera two-winged flies including several families with hematophagous biting habits, such as Ceratopogonidae biting midges or no-see-ums , Culicidae mosquitoes , Glossinidae tsetse , Simuliidae blackflies , Stomoxyinae stable flies , and Tabanidae deerflies, horseflies. Repellents may be useful against these biting flies and other blood-feeding bugs order Hemiptera such as bedbugs Cimicidae and kissing bugs Triatominae.

Variants of any chemical compound with the same molecular formula may have different structural formulas pl. Depending on the overall structure of isomeric adj. Stereochemistry is the study of these physical structures and interpretation of their different properties.

Insect Repellents-Principles_ Method_ and | Incense | Mosquito

The simplest isomerism is for a compound to exist in two equivalent forms, known as cis and trans isomers, forming mirror images of each other. This optical isomerism is commonly called enantiomerism. The so-called racemic mixture contains cis:trans; but properties of cis and trans are seldom the same, so the synthesis may be designed to favor more cis or more trans for reasons of cost versus benefit. When synthesized economically for commercial purposes, the so-called technical-grade permethrin is usually supplied with cis to trans ratios in the range from so-called medical permethrin, being safer for humans to more toxic.

Insecticide resistance may be isomer specific, depending on the relative cis:trans selection pressure and mechanism of resistance. Chiral compounds consist of matching isomers that are not mirror images of each other, like our right and left hands, so they are called dextro and laevo isomers from Latin terms for right and left or Recto and Sinistro isomers R and S. These descriptors are applied to each of several chiral centers of heterocyclic molecules. Isomerism of pesticides is generally correlated with differential potency of alternative isomers.

Knockdown resistance, Kdr. Hence, the rates of knockdown and mortality are scored separately, usually 1 hour and 24 hours after treatment in bioassays. Knockdown has another meaning in molecular biology, for gene incapacitation by siRNA. The effect may be to increase the speed of locomotion, to cause the insects to carry out avoiding reactions, or to decrease the rate of turning. Chapters 2 and MED: minimum effective dose; ref. Repellent products from plants botanicals are reviewed in Chapters 5, 12, 13, 14, 20, and 21; those from nonwoody plants are herbal that is: from herbs.

Azadirachtin, essential oils, and pyrethrins are important as both natural insecticides and repellents. Insects use ligand-gated ion channels for olfactory signal transduction and Orco functions as an obligate coreceptor with ligand-selective ORs to form a heteromeric, complex. Relatively little is known about their functional domains or the mechanisms by which odors activate the OR-Orco complex and how ions permeate it.

However, it is known that Orco is critical for OR olfactory signaling, as conventional ORs are nonfunctional when expressed without Orco. Orco functionality is required for OR-mediated chemoreception across all insects and enhances odorant responsiveness without altering ligand specificity when coexpressed with ORs. Targeting Orco provides new scope for broad-spectrum insect specific confusants. Rather than binding specific ligands, ORs may display an affinity for a range of odor molecules and, conversely, a single odorant molecule may bind to a number of olfactory receptors with varying affinities, with some such as pheromone receptors showing high affinities specificities.

Insect ORs are atypical seven-transmembrane domain proteins also known as G protein coupled receptors that form ligand-gated ion channels by assembling a ligandselective subunit with the olfactory receptor coreceptor Orco. Or: acronym for odorant receptor gene. Orco: acronym for olfactory receptor coreceptor. Organic: strictly, chemical compounds derived from plants or animals, plus other carbon-based materials. Essential oils from plants Chapter 9 include many useful organic repellents. In the terminology of modern farming and horticulture, so-called organic vegetables and other agricultural produce are defined as those grown and marketed without the application of synthetic pesticides and other potential pollutants.

Natural piperidine CAS number is the noxious ingredient of the poison hemlock Conium maculatum in the carrot family Apiaceae. Among more than such compounds identified in Piper, the relatively simple amides provide much of the hot, pungent, and spice taste as well as the biological activity in many species. The most active piperamide discovered to date is pipercide, which is approximately fold more active than piperine. Scott et al. Figure 1. This combination of useful traits suggests that Piper extracts may be good candidate pesticides with a rich range of insecticidal and repellent properties.

Whereas natural PMD-based repellents have long been popular in China and elsewhere, and registered in Europe for over a decade, synthetic PMD is used as the active ingredient for some of the repellents marketed as lemon eucalyptus in the United States. As described in Chapters 12 and 14, PMD exerts repellency of the highest order against a wide range of hematophagous arthropods. Formulations registered in the United States include liquids that are sprayed on skin or clothing, or lotions that are rubbed on skin. The proboscis of adult mosquitoes and other biting flies Diptera consists of labium upper sheath , labrum lower sheath , paired mandibular stylets, paired maxillary stylets, and hypopharynx with salivary duct bundled into a strong rostrum for biting, with a lumen canal for the fluid being ingested.

Tanacetum cinerariifolium Trevir ; also found in pyrethrum daisies: Chrysanthemum roseum Web. Chrysanthemum coccineum Willd Asteraceae. The crude pyrethrin extract contains three esters of chrysanthemic acid chrysanthemates: pyrethrin I, cinerin I, and jasmolin I plus three esters of pyrethrin acid pyrethrates: pyrethrin II, cinerin II, and jasmolin II , combined ratio , generally known as pyrethrins. Being lipophilic but having low aqueous solubility, pyrethrins are readily absorbed via arthropod cuticle but not via the skin of vertebrates.

Pyrethrins are very potent insecticidal knockdown agents, causing excitorepellency at sublethal doses, due to the disruption of sodium channel gating in myelinated nerves. Discovery and development of synthetic pyrethroids, during the. After early progress with allethrins transient space sprays and vaporizers , the first truly stable pyrethroids were fenvalerate and permethrin; their relative safety and potency greatly surpassed those of other classes of insecticides. Wide variations in potency occur between cis and trans isomers, and among enantiomers of pyrethroids, allowing much diversity in pyrethroid products, providing manufacturers and users with choices between knockdown versus insecticidal potency and degrees of residual stability.

With the commercialization of hundreds of pyrethroids, this class of compounds has come to dominate the insecticide industry during recent decades. Permethrin remains one of the favorites for its versatility as an insecticide with repellent and deterrent properties Chapters 6, 7, 17, and The editors of this book advocate that the term repellent should be restricted to the designation of products intended to reduce the rate of biting from hematophagous arthropods French: insectifuges corporels.

In this way, the technical literature will tend to use more precise terms that describe the effects of chemicals on specific behaviors. The introduction of the term phagomone is, in part, an attempt to facilitate this transition by providing the technical literature with an alternative to the term repellent used generally.

Selection for resistance against repellents might be expected, due to their ubiquitous usage and environmental persistence, of deet. Because no effort has been made to monitor the sensitivity of wild populations of the many arthropod species that repellents are used against, the possibilities of behavioral or physiological resistance to repellents remain unexplored.

However, studies with laboratory strains of mosquitoes and Drosophila demonstrate genetic selection of for insensitivity to deet, as well as reduced repellency following previous exposure, indicating the potential for resistance to deet and other repellents. Previous reports of tolerance, and resistance to deet involved comparisons between different species, not studies of inheritance or conditioning, although some intriguing contrasts were detected between strains of Anopheles albimanus in their responses to deet and its resolved isomer SS Rutgers the original proprietary name for ethyl hexanediol CAS number when used as a repellent product; withdrawn in for toxicological reasons.

Rutgers a repellent mixture consisting of six parts dimethyl phthalate, two parts Rutgers , and two parts indalone, optimized for military4,12 use during World War II as M For mosquitoes and other biting Diptera, those involved in olfaction include sensilla basiconica, sensilla coeloconica, and sensilla trichodea. Area repellent Chapter 12 is an easier term with the same meaning. The most commonly employed space repellents are certain volatile pyrethroids: allethrins, metofluthrin, transfluthrin, and some essential oils e. In biosystematics and nomenclature, groups of closely related species are classified as genera pl.

Formal names for each genus sing. Examples of different mosquito species names in the same genus are Anopheles funestus Giles and Anopheles gambiae Giles Related genera are classified into families e. Several hundred species of insects are likely to bite humans, justifying the use of repellents for personal protection.

The term feeding stimulant is synonymous with phagostimulant. Since the s, most commercial repellents are synthetic compounds. Synthetic pyrethroids are important insecticides and irritant repellents, usually including a chrysanthemic moiety homologous to natural pyrethrins. Movement toward the source being positive taxis; movement away from the source being negative taxis cf.

In many countries, regulatory systems set pesticide tolerances as maximum permissible levels of residues in foodstuffs, and so on established by the EPA in the United States and by the ECB in the EU. Tolerance has special meaning for quality control purposes, whereby the permissible range of variation is defined in product specifications with respect to the active ingredient, e.

Using this mathematical concept, Rutledge, assessed repellent tolerances of mosquito populations to compare ranges of responses and resistance potential. Dose-dependent criteria allow any material to be toxic, serving as a toxicant or toxin for sensitive tissues or organisms, although this term is normally applied to hazardous pathogens, pesticides,87 and other chemicals. For chemical safety purposes, in setting tolerances as mentioned earlier , toxicologists determine the no observed adverse effect level for laboratory animals.

For instance, acute tests the so-called six-pack comprise oral, dermal and inhalation lethal dosages LDs ; neurotoxicity; eye irritation; dermal irritation; and sensitization www. The so-called reference dose RfD is the average daily oral exposure that is estimated to be unlikely to cause harmful effects during a lifetime. RfDs are generally used by the EPA for health effects that are thought to have a low threshold dose limit for producing effects. The International Programme on Chemical Safety emphasizes the acceptable daily intake for each chemical, aggregated from all sources.

Whereas the mode of action of insect repellents is not well understood Chapter 11 , the toxicology of repellent compounds is not difficult to assess by standard methods. Collectively, they are responsible for pesticide regulatory management in the United States. Vector-borne pathogens cause disease, e. Hence the needs for vector control and personal protective measures including the use of repellents. Repellents do not affect vector competence, although there is mounting evidence that infective vectors may be less sensitive to repellents in some circumstances Chapter This formula expresses the capacity of the vector population to transmit the infection, based on the potential number of secondary inoculations originating per day from an infective person.

Values in the formula differ between vector species for intrinsic and environmental reasons. Where multiple vector species coexist, C is the sum of the vectorial capacities of all those vector species. Eesa and L. Wermuth et al. Gordh and D. Dethier and B. Browne, The designation of chemicals in terms of the responses they elicit from insects, J.

Gouck, T. McGovern, and M.

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Beroza, Chemicals tested as space repellents against yellow-fever mosquitoes. Esters, J. Schreck, Spatial action of mosquito repellents, J. Granett, Studies of mosquito repellents, I.

Insect Repellents Handbook

Test procedure and methods of evaluating test data, J. Granett, Studies of mosquito repellents, II. Relative performance of certain chemicals and commercially available mixtures as mosquito repellents, J. Christophers, Insect repellents, Brit. Christophers, Mosquito repellents, Rev. King, Repellents and insecticides for use against insects of medical importance, J. Government Printing Office, Agriculture Handbook No. Schreck, K. Posey, and D. Bernier and M.


Paluch and J. George et al. Jones et al. Natl Acad. USA, , , Xia et al. Bohbot and J. Syed and W. USA, 10, , Amoore, Specific anosmia: A clue to the olfactory code, Nature, , , Dogan et al. Bernier, Laboratory research and development of attractants, inhibitors, and repellents, Tech. Florida Mosq.

Control Assoc. Ditzen et al. Baldwin, Plant volatiles, Curr. Wright, D. Chambers, and I. Keiser, Insect attractants, anti-attractants, and repellents, Can. Quisenberry, and S. Linscombe, Investigation of antixenosis and antibiosis as mechanisms of resistance in rice to the rice weevil Coleoptera: Curculionidae , J.

Eickhoff et al. Kogan and E. Bernier et al. Urban Pests, 6, , Cilek et al. Control Soc. Mordue et al. Pelletier et al. Turner et al. Muirhead-Thomson, The significance of irritability, behaviouristic avoidance and allied phenomena in malaria eradication, Bull. Ritthison et al. Vector Ecol. Kennedy, Behaviorally discriminating assays of attractants and repellents, Chapter 13, in Chemical Control of Insect Behavior: Theory and Application, ed. Shorey and J. Robertson and H. Schreck et al. Federal Register, 75 , , Nasci, E.

Zielinski-Gutierrez, R. Wirtz, and W. Atlanta, GA: U. Centers for Disease Control and Prevention, Fort Collins, CO: U. Kaupp, Olfactory signalling in vertebrates and insects: Differences and commonalities, Nat. Pellegrino et al. Ross et al. Roy, S. Ghosh, and R. Chopra, Comparative efficacy of different culicifuges under laboratory conditions, Parasitology, 34, , Roy and S.

Ghosh, Further work on the comparative efficacy of different culicifuges under laboratory conditions, Parasitology, 34, , Berenbaum, The chemistry of defense: Theory and practice, Proc. Chauhan et al. Curtis, J. Myamba, and T. Wilkes, Comparison of different insecticides and fabrics for antimosquito bednets and curtains, Med. Miller et al. Ogoma, S. Moore, and M. Maia, A systematic review of mosquito coils and passive emanators: Defining recommendations for spatial repellency testing methodologies, Parasit.

Vectors, 5, , Moore et al. Results of a field study in Bolivia, Trop. Health, 12, 1, World Health Organization. Geneva, Switzerland: World Health Organization, Achee et al. Vectors, 28, , Environmental Protection Agency, Lengeler and R. Snow, From efficacy to effectiveness: Insecticide-treated bednets in Africa, Bull.

Logan et al. Heymann, Control, elimination, eradication and re-emergence of infectious diseases: Getting the message right, Bull. Trongtokit et al. Paluch, S. Bessett, and R. Bradbury, Development of essential oil-based arthropod repellent products, Chapter 10, pp. Barnard, Repellency of essential oils to mosquitoes Diptera: Culicidae , J. Kline et al. Pampana, A Textbook of Malaria Eradication, 2nd ed.

Roberts et al. Weldon, Nuisance arthropods, nonhost odors, and vertebrate chemical aposematism, Naturwissenschaften, 97, , Bohbot et al. Dogan and P. Rossignol, An olfactometer for discriminating between attraction, inhibition, and repellency in mosquitoes Diptera: Culicidae , J. Grieco et al. Fraenkel and D. Brady and N. Griffiths, Upwind flight responses of tsetse flies Glossina spp.

Diptera: Glossinidae to acetone, octenol and phenols in nature: A video study, Bull. Xue et al. Gilbert and S. Firestein, Dollars and scents: Commercial opportunities in olfaction and taste, Nat. Wright, Metarchons: Insect control through recognition signals, Bull. Solomon et al. Hudson, Odor and odorant: A terminological clarification, Chem. Senses, 25, , Murphy et al. Butler, Use of olfactometers for determining attractants and repellents, Chapter 9, pp.

Debboun, S. Frances, and D. Takken and B. Vosshall and B. Hansson, A unified nomenclature system for the insect olfactory coreceptor, Chem. Senses, 36, , Sato et al. Neuhaus et al. Weldon and J. Carroll, Vertebrate chemical defense: Secreted and topically acquired deterrents of arthropods, Chapter 3, pp. Larsson et al. Krieger et al.

Neural Behav. Stensmyr et al. Semmelhack and J. Wang, Select Drosophila glomeruli mediate innate olfactory attraction and aversion, Nature, , , Bruce and J. Grieco, A novel high throughput screening system to evaluate the behavioral response of adult mosquitoes to chemicals, J. Lee, Mosquito larvicidal activity of pipernonaline, a piperidine alkaloid derived from long pepper, Piper longum. Insect Biochem.

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Repellents and New “Spaces of Concern” in Global Health

Regnault-Roger, B. Miyakado et al. Miyakado, I. Nakayama, and H. Yoshioka, Insecticidal joint action of pipercide and co-occurring compounds isolated from Piper nigrum L. Dev and O. Forest Entomol. Carroll and J. Loye, A registered botanical mosquito repellent with deet-like efficacy, J. Curtis, Control of Disease Vectors in the Community, pp.

Pridgeon et al. Chapman, Mouthparts, pp. Resh and R. Coro and S. Suarez, Review and history of electronic mosquito repellers, Wing Beats, 11 2 , 6, Technical Report Series, No. Hemingway and H. Ranson, Insecticide resistance in insect vectors of human disease, Annu. Kolpin, Pharmaceuticals, hormones, and other organic wastewater contaminants in U. Sandstrom et al. Stanczyk et al.

Stancyzyk et al. Becker, The genetics of chemotaxis in Drosophila melanogaster: Selection for repellent insensitivity, Mol. Nordlund, R. Jones, and W. Lewis eds. Allan, Chemical ecology of tick-host interactions, Chapter 15, pp. Clements, Adult integumental sensilla: Their structure, physiology and connections with the brain, Chapter 25, pp. Revay et al. Thorsteinson, The experimental study of the chemotactic basis of host specificity in phytophagous insects, Can. Nakagawa et al. Benton et al. PLOS Biol. Leal, Maxillary palps are broad spectrum odorant detectors in Culex quinquefasciatus, Chem.

Senses, 32, , Reisen, Estimation of vectorial capacity: Relationship to disease transmission by malaria and arbovirus vectors, Bull. Kline and R. Axtell, Sensilla of the antennae and maxillary palps of Culicoides hollensis and C. Smith et al. Lee, S. Kim and C. Klun et al. Joseph C. More confounding is the fact that deet and other insect repellents do not prevent long-range attraction but rather perturb mosquito behavior at relatively close ranges.

The book includes thought-provoking discussions on how repellents work, their neuromolecular basis of action, and whether green chemistry can provide effective repellents. It also supplies an in-depth understanding of the development of repellents including testing methods, review of active ingredients, and the use of chemical mixtures as repellents.

It provides science-backed chapters on repellent use including best practices for use of personal protection products, criteria for repellent use, and insect repellents for other potential use. Forgot password? Remember Me? Forgot Password? It happens, just reset it in a minute. Sorry, incorrect details.

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