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PubMed2005

[Malaria: what about exposure prophylaxis?].

Malaria would not exist without mosquito bites. The growing resistance to antimalarial drugs has led to an increasing role of personal protection measures. However, insect repellents are not evaluated as medicinal products, and many products available on the market contain active substances that have been poorly evaluated or present in insufficient doses. The efficacy of the most active insect repellents, DEET and icaridin/KBR 3023, like that of medicinal products, is limited by the subject's compliance, bearing in mind that the Anopheles bite is painless and that humans are primarily bothered by the nuisance factor of the mosquito.

Animals↗
PubMed2001

Relative efficacy of DEPA and neem oil for repellent activity against Phlebotomus papatasi, the vector of leishmaniasis.

The insect repellent N, N-diethylphenyl acetamide (DEPA) was compared with neem oil, a commercial preparation, for protection against 3 day old un-fed female of the sandfly, Phlebotomus papatasi, (Diptera: Psychodidae) under laboratory conditions on mouse. The percentage protection against sandfly bite provided by neem oil was significantly higher than DEPA when applied at 1% and 2% concentrations (p = 0.000, t = 21.474; df = 6 and p = 0.001, t = 5.960; df = 6 respectively). However, neem oil did not show any significant difference with DEPA at 5% (p = 0.1682, t = 0.15667; df = 6). This clearly indicates that at higher concentration (5%) both neem oil and DEPA exhibited similar repellent action against P. papatasi.

Acetamides↗
PubMed1997

Evolution of repellent tolerances in representative arthropods.

Eight commercial insect repellents were tested against Ornithodoros parkeri (Acari: Argasidae), Dermacentor variabilis (Acari: Ixodidae), Aedes aegypti (Diptera: Culicidae), and Xenopsylla cheopis (Siphonaptera: Pulicidae). Patterns of tolerance to the test materials were distinctive for each test species. Levels of tolerance were coded as character state 0 (sensitive), 1 (intermediate), or 2 (tolerant) and mapped on a cladogram reflecting the accepted classification of the test species. Character state 0 was regarded as primitive, as indicated by the ontology of repellent tolerances in ticks. Aedes aegypti was least evolved and X. cheopis was most evolved in tolerance to repellents. Multiple parallelism of the arachnid and X. cheopis lines occurred in the evolution of the observed tolerances.

Aedes↗
PubMed1994

Relative potency of DEPA as a repellent against the sandfly Phlebotomus papatasi.

The insect repellent N,N-diethylphenylacetamide (DEPA) was compared with two commercial repellents, N,N-diethyl-m-toluamide (DEET) and dimethyl phthalate (DMP), for protection against 3-day-old unfed females of the sandfly Phlebotomus papatasi (Scopoli) under laboratory conditions, using host rabbits. Both DEPA and DEET were found to be more effective than DMP, but there was no significant difference between the efficacy of DEPA and DEET.

Acetamides↗
PubMed1964

CATNIP: ITS RAISON D' ETRE.

Catnip (nepetalactone) is closely related chemically to certain cyclopentanoid monoterpenes recently isolated from insects, and it shares with some of these terpenes an ability to repel insects. It is suggested that the adaptive function of catnip is to protect the plants that produce it against phytophagous insects.

Animals↗
PubMed1996

Evaluation of a eucalyptus-based repellent against Anopheles spp. in Tanzania.

A eucalyptus-based insect repellent (PMD) with the principal active ingredient p-menthane-3,8-diol was evaluated in the field in comparison with deet. In human landing catches in Tanzania, 3 formulations of PMD were tested against Anopheles gambiae and An. funestus. Repellents, applied to the legs and feet at doses chosen as used in practice, gave complete protection from biting for between 6 and 7.75 h, depending upon the formulation type, with no significant difference between PMD and deet in terms of efficacy and duration of protection.

Animals↗
PubMed2006

DEET-loaded solid lipid particles for skin delivery: in vitro release and skin permeation characteristics in different vehicles.

DEET (N,N-diethyl m-toluamide) is a lipophilic compound which has a common use as an insect repellent and causes not only skin irritation but also systemic side effects at high concentrations in long-term skin application. In this study, DEET is incorporated into solid lipid particles, a colloidal drug delivery system, in order to reduce the percutaneous permeation and avoid toxic effects and also maintain drug effectiveness on the skin surface for a long duration of insect repellence. Solid lipid particles were prepared based on emulsion systems at different concentrations and after the characterization studies, the formulation with 20% lipid phase and 1:1 drug:lipid ratio was carried to in vitro release and skin permeation studies. Solid lipid particles with DEET were compared to free DEET using cream and hydrophilic gel vehicles. Results showed that incorporation of DEET into solid lipid particles reduced the release rate and skin permeation of DEET. Imaging studies using scanning electron microscopy showed that there were still solid lipid particles on skin surface after 2 h indicating that DEET could be present for a longer time on the application site.

DEET↗
PubMed1990

Lyme disease in outdoor workers: risk factors, preventive measures, and tick removal methods.

A statewide cross-sectional study of risk factors for seropositivity for antibody to Borrelia burgdorferi in outdoor workers in New Jersey was performed in September and October 1988. The crude odds ratio associated with exposure to ticks on the primary state job was 2.2 (95% confidence interval (CI) 0.7-9.0). After adjustment for multiple confounding variables with logistic regression, the adjusted occupational tick exposure odds ratio was 5.1 (95% CI 1.1-23.6). Additional analyses revealed that any use of insect repellent or antibiotics may have decreased the risk of Lyme disease in these workers (adjusted odds ratios for not using insect repellent or antibiotics were 2.0 (95% CI 1.0-4.0) and 2.3 (95% CI 0.8-6.7), respectively). These data suggest that Lyme disease is a hazard of outdoor work and that increased recognition of this fact will be necessary to prevent Lyme disease in these workers.

Adult↗
PubMed2001

Nootkatone is a repellent for Formosan subterranean termite (Coptotermes formosanus).

We examined the behavior of Formosan subterranean termites toward one of the components of vetiver grass oil, the roots of which manufacture insect repellents. We found nootkatone, a sesquiterpene ketone, isolated from vetiver oil is a strong repellent and toxicant to Formosan subterranean termites. The lowest effective concentration tested was 10 micrograms/g substrate. This is the first report of nootkatone being a repellent to insects.

Animals↗
PubMedDate not supplied

Bite the hand that sprays you.

A 56-year-old man presented with a cutaneous lesion on his right hand (Figure 1). Approximately 6 weeks previously, he had traveled to Costa Rica for missionary work. During his travel he used a diethyltoluamide-containing insect repellant, but spent one night in the jungle without a mosquito net. Four weeks after his return, he noted a 3 x 2.5-cm ulcer with raised edges and surrounding erythema on the dorsum of his right hand. The patient recalled applying insect repellant with his right hand to other exposed areas of his body but was remiss in applying it to the right hand itself. On examination, the patient was noted to have an ulcerated nodule near his right earlobe (Figure 2) and a second 2 x 1-cm ulcer on the volar aspect of his right wrist (Figure 3). There were no mucocutaneous lesions noted. During the next several weeks, numerous nodules developed in a sporotrichoid pattern on the extensor surface of his right arm (Figure 4). Skin biopsy was performed at the time of initial evaluation and revealed cutaneous leishmaniasis due to Leishmania panamensis. After discussing the different treatment options, miltefosine was administered orally for 28 days. The patient experienced an excellent response to therapy.

Administration, Oral↗
PubMed1994

Laboratory and field trials of four repellents with Culex pipiens (Diptera: Culicidae).

During Operation "Desert Shield," 16 volunteers field-tested four insect repellents (deet, the lactone CIC-4, and the piperidine compounds AI3-37220 and AI3-35765) against biting mosquitoes at King Fahd Airport, Eastern Province, Saudi Arabia. CIC-4 and AI3-37220 (25% wt/vol) provided effective (> 90%) protection against bites for 4 h. Deet and AI3-35765 protected for only 2 h. The compounds subsequently were evaluated for repellency against laboratory-reared Culex pipiens L. CIC-4 was more effective than deet, AI3-37220, or AI3-35765 at the ED50 but not at the ED95 level in initial sensitivity tests using human volunteers. At the ED95 level, deet provided significantly better protection than either piperidine compound. In laboratory duration tests, AI3-37220 provided 8 h of effective (> 90%) protection against Cx. pipiens bites, deet and AI3-35765 7 h of protection, and CIC-4 2 h of protection.

Animals↗
PubMedDate not supplied

[Prevention and control of malaria in pregnant women in an urban setting (Yaoundé, Cameroun)].

The aim of this study was to evaluate the methods of preventing malaria (chemoprophylaxis, vector control) and of fever management (presumptive treatment of malaria) used for pregnant women in Yaounde, Cameroon and to identify the most important factors for assessing these practices. The 221 women studied were selected by cluster sampling. All had made extensive use of health services during pregnancy and 77% were using chemoprophylaxis. The number of febrile episodes in pregnant women who claimed to have used chemoprophylaxis was not significantly different to that in the women who did not use it. However, the mean birth weight of the babies of women who had used chemoprophylaxis was significantly higher. The women did not systematically use vector control measures; 21% used insect repellents (electric plaques, coil burners) and 20% used aerosol insecticides. Only 10% of the women slept under simple, untreated mosquito nets and none used mosquito nets impregnated with insecticide. Fifty per cent of the women had at least one episode of fever during pregnancy and 77% were treated for presumed malaria. However, the treatment was not standardized and was unsuitable in a third of cases. Possible changes in the chemoprophylaxis strategy are discussed.

Adult↗
PubMedDate not supplied

Pharmacokinetic assessment of the dermal absorption of N,N-diethyl-m-toluamide (DEET) in cattle.

Model-independent pharmacokinetic methods based on statistical moments were applied to investigate the plasma disposition characteristics of N,N-diethyl-m-toluamide (DEET insect repellent) after single-dose treatment of experimental cattle by rapid intravenous injection (2.5-2.7 mg/kg) and by dermal application (10 mg/kg) to the back. DEET was determined in jugular blood samples by capillary GC with a nitrogen-selective detector and an internal standard of N,N-dipropyl-m-toluamide. Using weighted least squares linear regression analysis, the assay was validated over the concentration range of 19-1910 ng/ml of plasma. Comparison of areas under the plasma concentration-time curves after intravenous and dermal treatments of four Hereford heifers indicated that 72.9 +/- 8.3% (mean +/- SD) of the dermally applied dose was absorbed into the systemic circulation. The time-to-peak plasma concentrations following dermal treatments was 37.5 +/- 8.7 min. Apparent elimination rate constants were not significantly different between the two routes of administration. Linear pharmacokinetics was demonstrated with four additional cattle by comparing systemic clearance after intravenous infusion to steady-state plasma levels of approximately 0.5 and 2.5 micrograms/ml. The rapid and extensive dermal absorption of DEET observed in this study will probably contribute to a short duration of insect repellent action if ethanol-based sprays are used to protect cattle under field conditions.

Administration, Cutaneous↗
PubMed2002

In vitro human metabolism and interactions of repellent N,N-diethyl-m-toluamide.

Oxidative metabolism of the insect repellent N,N-diethyl-m-toluamide (DEET) by pooled human liver microsomes (HLM), rat liver microsomes (RLM), and mouse liver microsomes (MLM) was investigated. DEET is metabolized by cytochromes P450 (P450s) leading to the production of a ring methyl oxidation product, N,N-diethyl-m-hydroxymethylbenzamide (BALC), and an N-deethylated product, N-ethyl-m-toluamide (ET). Both the affinities and intrinsic clearance of HLM for ring hydroxylation are greater than those for N-deethylation. Pooled HLM show significantly lower affinities (K(m)) than RLM for metabolism of DEET to either of the primary metabolites (BALC and ET). Among 15 cDNA-expressed P450 enzymes examined, CYP1A2, 2B6, 2D6*1 (Val(374)), and 2E1 metabolized DEET to the BALC metabolite, whereas CYP3A4, 3A5, 2A6, and 2C19 produced the ET metabolite. CYP2B6 is the principal cytochrome P450 involved in the metabolism of DEET to its major BALC metabolite, whereas CYP2C19 had the greatest activity for the formation of the ET metabolite. Use of phenotyped HLMs demonstrated that individuals with high levels of CYP2B6, 3A4, 2C19, and 2A6 have the greatest potential to metabolize DEET. Mice treated with DEET demonstrated induced levels of the CYP2B family, increased hydroxylation, and a 2.4-fold increase in the metabolism of chlorpyrifos to chlorpyrifos-oxon, a potent anticholinesterase. Preincubation of human CYP2B6 with chlorpyrifos completely inhibited the metabolism of DEET. Preincubation of human or rodent microsomes with chlorpyrifos, permethrin, and pyridostigmine bromide alone or in combination can lead to either stimulation or inhibition of DEET metabolism.

Animals↗
PubMed2001

Sampling and analysis of airborne particulate matter and aerosols using in-needle trap and SPME fiber devices.

A needle trap device (NTD) and commercial poly(dimethylsiloxane) (PDMS) 7-microm film thickness solid-phase microextraction (SPME) fibers were used for the sampling and analysis of aerosols and airborne particulate matter (PM) from an inhaler-administered drug, spray insect repellant, and tailpipe diesel exhaust. The NTD consisted of a 0.53-mm o.d. stainless steel needle having 5 mm of quartz wool packing section near the needle tip. Samples were collected by drawing air across the NTD with a Luertip syringe or via direct exposure of the SPME fiber. The mass loading of PM was varied by adjusting the volume of air pulled through the NTD or by varying the sampling time for the SPME fiber. The air volumes ranged from 0.1 to 50 mL, and sampling times varied from 10 s to 16 min. Particulates were either trapped on the needle packing or sorbed onto the SPME fiber. The devices were introduced to a chromatograph/mass spectrometer (GC/MS) injector for 5 min desorption. In the case of the NTD, 10 microL of clean air was delivered by a gas-tight syringe to aid the introduction of desorbed analytes. The compounds sorbed onto particles extracted by the SPME fiber or trapped in the needle device were desorbed in the injector and no carry-over was observed. Both devices performed well in extracting airborne polycyclic aromatic hydrocarbons (PAHs) in diesel exhaust, triamcinolone acetonide in a dose of asthma drug and DEET in a dose of insect repellant spray. Results suggest that the NTDs and PDMS 7-microm fibers can be used for airborne particulate sampling and analysis, providing a simple, fast, reusable, and cost-effective screening tool. The advantage of the SPME fiber is the open-bed geometry allowing spectroscopic investigations of particulates; for example, with Raman microspectroscopy.

Journal Article↗
PubMed2005

Effects of forced egg-retention in Aedes albopictus on adult survival and reproduction following application of DEET as an oviposition deterrent.

The insect repellent DEET (0.1% concentration), used as a mosquito oviposition deterrent in the laboratory, influenced the retention and maintenance of mature eggs by caged gravid female Aedes albopictus Skuse. This egg-retention mechanism could benefit survival because the gravid females were ultimately able to lay maintained eggs upon availability of water, but the length of forced egg-retention time reduced the number of eggs laid per female. Gravid females with retained eggs also laid a higher percentage of eggs that failed to tan, and this percentage increased with time duration of egg-retention. Percent egg hatch was not significantly affected by DEET when used as an oviposition deterrent; however, percent hatch was affected by time duration of egg-retention in both treated (exposed to DEET) and untreated (control) gravid females. The rate of egg hatch was considerably reduced after three weeks of retention; this reduction declined to zero for treated and control females at six and four weeks post-treatment, respectively. The fecundity and fertility of gravid female Ae. albopictus were affected by the time duration of forced egg-retention.

Aedes↗
PubMed1992

Reproductive and developmental toxicity of N,N-diethyl-m-toluamide in rats.

N,N-Diethyl-m-toluamide (mDET, DEET) is widely used as a topical insect repellent. It is the active ingredient in many consumer formulations, which usually contain 10-25% mDET in an alcohol base. More concentrated consumer products are also available, including some that are pure technical grade mDET. Persons living or employed in mosquito-infested areas may have very high seasonal exposures to mDET. Because contradictory reports had been published on the reproductive and developmental toxicity of mDET, a series of studies was conducted in male and female Sprague-Dawley rats. All treatments were administered by daily subcutaneous injections of undiluted mDET. A dose finding study was done using 12 time-mated females per group treated on Gestational Days (GD) 6-15 with 0.50, 0.62, 0.78, 0.92, or 1.2 ml mDET/kg/day. No females survived 10 days of mDET dosing with 1.2 ml/kg/day. Deaths occurred in all other groups except the low dose (0.50 ml/kg/day). Pregnant females treated on GD 6-15 with 0 or 0.30 ml/kg/day were used for the teratology study. Half of each group was euthanized on GD 20: the second half was singly housed in nesting boxes and allowed to deliver litters. Live pups were counted and weighed soon after birth on Postnatal Day (PD) 0 and again on PD 3, 9, and 14. Proven fertile males were treated 5 days/week for 9 weeks with 0, 0.30, 0.73, 1.15, or 1.80 ml mDET/kg/day for a male dose-finding study. Each group consisted of 20 males. No males survived the 1.80 ml/kg/day. Deaths occurred in all remaining dose groups except the 0.30 ml/kg/day and control group. Immediately following the final treatment of the male dose study, 11 males were randomly selected from the 0.30 and 0.73 ml/kg/day groups. They were cohabited for 7 days with 4 females per male during post-treatment Weeks 1 and 2. Half of the females were euthanized 12-14 days after the last day of cohabitation for a dominant lethal study; the remaining females were singly housed in nesting boxes and allowed to deliver litters. Live pups were counted and weighted on PD 0 and 3. There was no evidence of reproductive or developmental toxicity in any of these assays, but there were signs of neurotoxicity in treated adult male and female rats, which may relate to reports of neurotoxicity in humans heavily exposed to mDET-containing insect repellents.

Abnormalities, Drug-Induced↗
PubMed1996

Evaluation of a eucalyptus-based repellent against Culicoides impunctatus (Diptera:Ceratopogonidae) in Scotland.

A eucalyptus-based insect repellent (PMD) was evaluated against Culicoides impunctatus in Scotland in comparison with deet. In human landing catches, both repellents still afforded 98% protection from biting 8 h after application of 0.5 ml to the forearm. A second trial looking at protection between 8 and 10 h after repellent application showed 99.5% protection for PMD and 97% for deet as compared with controls.

Animals↗