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1.
Vet Parasitol ; 331: 110291, 2024 Oct.
Article in English | MEDLINE | ID: mdl-39190938

ABSTRACT

The acaricidal potential of various essential oils (EOs) has been evaluated based on their benefits in tick control. This study aimed to investigate the tick-killing activity of Pogostemon cablin "patchouli," Cymbopogon martinii "palmarosa," and Cymbopogon flexuosus "lemongrass" EOs on Rhipicephalus linnaei. Engorged females were collected from domiciled and non-domiciled dogs from Jataí city, Goiás state, to obtain larvae and nymphs in a controlled environment. Two commercial EOs brands were used in this study in different EOs concentrations (2.5, 5, 10, and 20 mg/mL), and was tested by immersion of larvae and nymphs. In the in vitro evaluation of EOs toxicity against R. linnaei larvae, 100 % mortality was achieved with 10 mg/mL of P. cablin oil, whereas mortality rates greater than 98 % were observed with 20 mg/mL of C. martinii and C. flexuosus. In nymphs, high sensitivity was observed, with 100 % mortality achieved using 5 mg/mL of P. cablin and 20 mg/mL of C. martinii and C. flexuosus. The EO of P. cablin "patchouli" demonstrated in vitro toxicity at a lower concentration than the other oils in the two development stages of R. linnaei, and was considered the most efficient and with verified acaricidal activity. Oils of C. martinii "palmarosa" and C. flexuosus "lemongrass" achieved mortality greater than 95 % in larvae and nymphs only at the highest concentration. Therefore, the acaricidal effects of the tested EOs are promising, especially of patchouli oil, which promoted high mortality at a low concentration (LC90 of 2.21 mg/mL).


Subject(s)
Acaricides , Larva , Nymph , Oils, Volatile , Rhipicephalus , Animals , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Rhipicephalus/drug effects , Acaricides/pharmacology , Larva/drug effects , Nymph/drug effects , Cymbopogon/chemistry , Female , Lamiaceae/chemistry , Plant Oils/pharmacology , Plant Oils/chemistry , Tick Infestations/veterinary , Tick Infestations/parasitology , Tick Infestations/drug therapy , Tick Infestations/prevention & control , Tick Control/methods , Dogs , Dog Diseases/parasitology , Dog Diseases/drug therapy
2.
Microorganisms ; 12(1)2024 Jan 18.
Article in English | MEDLINE | ID: mdl-38258028

ABSTRACT

In dogs, tick infestation can cause damage ranging from a simple skin irritation to severe diseases and/or paralysis leading to animal death. For example, Ixodes ricinus and I. scapularis are among the tick species incriminated the most in the transmission of Borrelia burgdorferi, the agent of human and canine Lyme borreliosis (LB). In this study, we aimed to compare the efficacy of two products designed for dogs-an oral systemic ectoparasiticide and a topical repellent ectoparasiticide-against the acquisition of B. burgdorferi by adult I. scapularis and I. ricinus using an ex vivo model. Thirty-two beagle dogs were included in a parallel-group-designed, randomized, single-center, negative-controlled efficacy study. The dogs were allocated to three groups based on gender and body weight: a fluralaner (F, Bravecto®) treatment group (n = 8), administered a single oral treatment on day 0 at the recommended dose; a dinotefuran-permethrin-pyriproxyfen (DPP, Vectra® 3D) treatment group (n = 8), topically treated on day 56 at the recommended dose; and an untreated control group (n = 16). Blood and hair were collected from each dog on days 58, 63, 70, 77, and 84. Hair was added to the silicone-based membrane separating two glass chambers forming the feeding unit (FU). Chamber 1 was filled with blood spiked with B. burgdorferi sensu stricto, strain B31 (105 cells/mL). Chamber 2, glued below chamber 1, was seeded with 20 adult I. scapularis or I. ricinus. The FUs (n = 240) were incubated at 37 °C with a humidity >90%. Tick survival, attachment, and feces presence were observed from 1 h up to 72 h after tick seeding. The uptake of B. burgdorferi was determined in ticks using nested polymerase chain reaction (nPCR). The acaricidal efficacy of DPP-treated hair was 100% within 1 h of tick release on every study day for both I. ricinus and I. scapularis. The speed of kill associated with DPP was sufficiently fast to prevent tick attachment and engorgement, and, consequently, to prevent the acquisition of B. burgdorferi. In the F-treated group, the acaricidal efficacy observed at 12 h, throughout the study, was <20% and <28% for I. scapularis and I. ricinus, respectively. Furthermore, tick feces were observed in the FUs, and several female ticks (I. scapularis (n = 55) and I. ricinus (n = 94)) tested positive for B. burgdorferi. The results provide proof of concept for the use of an ex vivo model based on an artificial feeding system to compare two ectoparasiticides against the acquisition of B. burgdorferi by I. ricinus and I. scapularis. In addition, our results demonstrate the superiority of DPP compared to F in the speed of acaricidal activity against ticks, as well as in preventing the acquisition of B. burgdorferi.

3.
Parasit Vectors ; 16(1): 440, 2023 Nov 27.
Article in English | MEDLINE | ID: mdl-38012748

ABSTRACT

BACKGROUND: Compliant ectoparasiticide product use is a comprehensive way to control ticks and reduce the risk of tick-borne pathogen transmission to dogs. Because the systemically acting isoxazoline ectoparasiticides require tick attachment for drug delivery, fast speed of kill is essential to minimize tick-borne pathogen transmission risk. METHODS: Dogs of satisfactory tick-carrying capacity were randomly allocated to treatment groups and administered, per label instructions, Bravecto® Chews (minimum 25 mg/kg fluralaner), Simparica TRIO® (minimum 1.2 mg/kg sarolaner, 24 µg/kg moxidectin, 5 mg/kg pyrantel), or no treatment. Dogs were infested with approximately 50 unfed adult (35 female, 15 male) Ixodes scapularis on Day -2, 21 and 28. Live tick counts were performed at 4, 8, 12 and 24 h post-treatment (Day 0) and post-infestation on Day 21 and 28. Tick control efficacy was determined by comparing live tick means for each product-treated group to the untreated control group and each other at all time points using a linear mixed model. The percent of dogs free of live ticks was analyzed using the Fisher's exact test for treatment group comparison. RESULTS: The untreated control group maintained adequate tick infestations throughout the study. Using geometric means, an existing I. scapularis infestation was controlled by 99.7% and 93.0% 12 h post-treatment and by 100% and 99.5% 24 h post-treatment, for Bravecto® and Simparica TRIO®-treated dogs, respectively. Ixodes scapularis infestations were controlled more quickly for Bravecto®- compared to Simparica TRIO®-treated dogs on Day 21 at 8 h (efficacy 74.0% vs. 0.0%, p = 0.003) and 12 h (efficacy 99.2% vs. 39.4%, p < 0.001) post-infestation and Day 28 at 8 h (efficacy 92.2% vs. 0.0%, p < 0.001) and 12 h (efficacy 99.6% vs. 27.7%, p < 0.001) post-infestation. On Day 28 post-treatment, the efficacy of Bravecto® and Simparica TRIO® to control a new I. scapularis infestation was 100% and 96.6%, respectively, by 24 h post-infestation. Of product-treated dogs, 100% of Bravecto®-treated dogs were free of live ticks by 24 h post-treatment or post-infestation. No treatment-related adverse reactions occurred during the study. CONCLUSIONS: Ixodes scapularis infestations are controlled more quickly 21 and 28 days post-treatment for dogs administered a single dose of Bravecto® compared to dogs administered a single dose of Simparica TRIO®.


Subject(s)
Acaricides , Dog Diseases , Ixodes , Tick Infestations , Animals , Dogs , Female , Male , Pyrantel/therapeutic use , Administration, Oral , Treatment Outcome , Dog Diseases/drug therapy , Dog Diseases/prevention & control , Time Factors , Tick Infestations/drug therapy , Tick Infestations/prevention & control , Tick Infestations/veterinary , Acaricides/therapeutic use
4.
Pest Manag Sci ; 79(10): 4078-4082, 2023 Oct.
Article in English | MEDLINE | ID: mdl-37288963

ABSTRACT

BACKGROUND: Fluralaner is the first isoxazoline ectoparasiticide developed to protect companion animals from fleas and ticks. Fluralaner primarily inhibits arthropod γ-aminobutyric acid receptors (GABARs), which are ligand-gated ion channels comprising five subunits arranged around the channel pore. We previously reported that the action site of fluralaner resides at the M1-M3 transmembrane interface between adjacent GABAR subunits. To investigate whether fluralaner interacts with the second transmembrane segment (M2) located deep in the interface, we generated four housefly RDL GABAR mutants with non-conservative amino acid substitutions in the M2 region. RESULTS: Electrophysiological analysis of GABARs expressed in Xenopus oocytes indicated that S313A and S314A mutants exhibited fluralaner sensitivities similar to that of the wild type. M312S mutant exhibited approximately seven-fold lower sensitivity than that of the wild type. Notably, the N316L mutant was almost insensitive to fluralaner. CONCLUSION: The findings of this study indicate that the conserved external amino acid residues of insect GABAR channels play a critical role in the antagonistic effect of fluralaner. © 2023 Society of Chemical Industry.


Subject(s)
Insecticides , Receptors, GABA , Animals , Receptors, GABA/genetics , Receptors, GABA/metabolism , Amino Acids , Insecticides/chemistry , Insecta/metabolism
5.
Adv Parasitol ; 120: 1-85, 2023.
Article in English | MEDLINE | ID: mdl-36948727

ABSTRACT

Vector-borne pathogens (VBPs) of canines are a diverse range of infectious agents, including viruses, bacteria, protozoa and multicellular parasites, that are pernicious and potentially lethal to their hosts. Dogs across the globe are afflicted by canine VBPs, but the range of different ectoparasites and the VBPs that they transmit predominate in tropical regions. Countries within the Asia-Pacific have had limited prior research dedicated to exploring the epidemiology of canine VBPs, whilst the few studies that have been conducted show VBP prevalence to be high, with significant impacts on dog health. Moreover, such impacts are not restricted to dogs, as some canine VBPs are zoonotic. We reviewed the status of canine VBPs in the Asia-Pacific, with particular focus on nations in the tropics, whilst also investigating the history of VBP diagnosis and examining recent progress in the field, including advanced molecular methods, such as next-generation sequencing (NGS). These tools are rapidly changing the way parasites are detected and discovered, demonstrating a sensitivity equal to, or exceeding that of, conventional molecular diagnostics. We also provide a background to the armoury of chemopreventive products available for protecting dogs from VBP. Here, field-based research within high VBP pressure environments has underscored the importance of ectoparasiticide mode of action on their overall efficacy. The future of canine VBP diagnosis and prevention at a global level is also explored, highlighting how evolving portable sequencing technologies may permit diagnosis at point-of-care, whilst further research into chemopreventives will be essential if VBP transmission is to be effectively controlled.


Subject(s)
Dog Diseases , Parasites , Animals , Dogs , Parasites/genetics , Bacteria , Asia/epidemiology , Chemoprevention , Dog Diseases/diagnosis , Dog Diseases/epidemiology , Dog Diseases/prevention & control
6.
Article in English | MEDLINE | ID: mdl-35865719

ABSTRACT

The tropical brown dog tick, Rhipicephalus linnaei, commonly infests canines in the tropics and is an important vector for disease-causing and sometimes lethal pathogens including Babesia spp., Ehrlichia canis, Hepatozoon canis and Anaplasma platys. In tropical climates ticks and their pathogens exert an extremely high infection pressure on unprotected dogs. To protect canines in such regions, effective acaricidal products possessing a speed of kill that blocks pathogen transmission is paramount. We conducted a 12-month community trial to compare the chemoprophylactic efficacy of two topical commercial acaricidal formulations: an imidacloprid 10% and flumethrin 4.5%, 8-month acting collar (Seresto®) against a monthly spot-on containing 12% w/v fipronil (Detick, Thailand). In a separate analysis, we used baseline data collected at the start of the trial to quantify tick-borne pathogen (TBP) infection status in dogs with a prior history of being administered a systemically-acting (isoxazoline) versus a topically-acting ectoparasiticide. We found that both topical products in the community trial demonstrated high efficacy at protecting dogs from ticks and TBP, with Seresto® demonstrating a moderate increase in protection at 3 (95% confidence interval (CI): 1-5) TBP-positive dogs per 100 dog-years at risk compared to 11 (95% CI: 4-26) TBP-positive dogs per 100 dog-years at risk for those on fipronil. Additionally, at baseline dogs treated with commercial systemic isoxazoline acaricides prior to the trial's commencement were 2.7 (95% CI: 0.5-15.0) times more likely to be TBP-positive compared to dogs that had been topically treated, highlighting such isoxazoline products as being less efficacious than topical products at preventing canine TBP acquisition in a tropical setting.

7.
Pestic Biochem Physiol ; 181: 105008, 2022 Feb.
Article in English | MEDLINE | ID: mdl-35082031

ABSTRACT

γ-Aminobutyric acid (GABA) receptors (GABARs) are ligand-gated Cl- channels, which cause an influx of Cl- that inhibits excitation in postsynaptic cells upon activation. GABARs are important targets for drugs and pest control chemicals. We previously reported that the isoxazoline ectoparasiticide fluralaner inhibits GABA-induced currents in housefly (Musca domestica) GABARs by binding to the putative binding site in the transmembrane subunit interface. In the present study, we investigated whether fluralaner inhibits the GABA response in the GABAR activated state, the resting state, or both, using two-electrode voltage clamp electrophysiology protocols. We found that inhibition progresses over time to steady-state levels by repeated short applications of GABA during fluralaner perfusion. The GABA response was not impaired by fluralaner treatment in the GABAR resting state. However, once inhibited, the GABA response was not restored by repeated applications of GABA. These findings suggest that fluralaner might reach the binding site of the activated conformation of GABARs in a stepwise fashion and tightly bind to it.


Subject(s)
Houseflies , Insecticides , Animals , Isoxazoles/pharmacology , Receptors, GABA/metabolism , Receptors, GABA-A
8.
Vet Parasitol ; 302: 109613, 2022 Feb.
Article in English | MEDLINE | ID: mdl-35094879

ABSTRACT

This second edition guideline was prepared to assist in the planning, conduct and interpretation of studies to assess the efficacy of parasiticides against ectoparasites of ruminants. It provides updated information on the selection of animals, dosage determination, dosage confirmation and field studies, record keeping and result interpretation. This guideline is intended to assist investigators on how to conduct specific studies, to provide specific information for registration authorities involved in the decision-making process, to assist in the approval and registration of new ectoparasiticides, and to facilitate the worldwide adoption of standard procedures.


Subject(s)
Antiparasitic Agents , Insecticides , Animals , Antiparasitic Agents/therapeutic use , Parasitology , Ruminants
9.
Parasit Vectors ; 15(1): 32, 2022 Jan 21.
Article in English | MEDLINE | ID: mdl-35062996

ABSTRACT

BACKGROUND: This study evaluated the timing of dog owner ectoparasiticide purchases to estimate administration compliance and assess the consequent impact of dose purchase gaps on the proportion of time that dogs were protected over a 12-month period. METHODS: Ectoparasiticide purchase transactions over a 12-month period were evaluated for 626 US veterinary hospitals to determine dose purchase timing and identify consequent gaps between dose administration in dogs. Orally administered prescription ectoparasitic medications with active ingredients from the isoxazoline family (afoxolaner, fluralaner, lotilaner, or sarolaner) were included in the analysis. A period was calculated for each of the four isoxazoline-containing medications that represented the duration of protection provided by two doses of ectoparasiticide plus the average gap between these two doses. The maximum percentage of time possible for ectoparasiticide protection for this aggregate period was then calculated for each active ingredient. RESULTS: Ectoparasiticide transaction records of owners were analyzed for 506,637 dogs. These showed that 43% of dog owners purchased just one dose over the 12-month period considered. If a dog owner purchased more than one dose, then the timing of their transactions could create a time gap between the completion of ectoparasite protection from the first dose and onset of protection from the subsequent purchase and administration of the second dose. Such gaps were observed in purchases made by 31-65% of dog owners, depending on the selected active ingredient and number of doses. The average gap duration between dose purchases was calculated for all possible dose combinations over 12 months of ectoparasite protection. Time gaps between the first and second doses are as follows: for sarolaner, 20.3 weeks; for afoxolaner, 12.9 weeks; for fluralaner ,12.8 weeks; and for lotilaner, 8.9 weeks. The proportion of time when protection was provided during the aggregate period between administration of the first and second doses was as follows: for fluralaner, 65%; for lotilaner, 49%; for afoxolaner, 40%; and for sarolaner, 30%. CONCLUSIONS: Dog owner ectoparasiticide purchase transactions showed that there were time gaps between doses leading to reduced ectoparasite protection. The longer re-administration interval for fluralaner, a consequence of its extended duration of activity, resulted in dog owners gaining the greatest proportion of ectoparasite protection time with this medication compared with shorter-acting monthly re-treatment medications.


Subject(s)
Dog Diseases , Ectoparasitic Infestations , Insecticides , Medication Adherence , Administration, Oral , Animals , Dog Diseases/parasitology , Dog Diseases/prevention & control , Dogs , Ectoparasitic Infestations/prevention & control , Ectoparasitic Infestations/veterinary , Hospitals, Animal , Insecticides/therapeutic use , Treatment Outcome , United States
10.
J Vet Pharmacol Ther ; 45(1): 1-15, 2022 Jan.
Article in English | MEDLINE | ID: mdl-33733534

ABSTRACT

The isoxazolines are a novel class of ectoparasiticides with potent inhibitory activity on glutamate- and gamma-aminobutyric acid-gated chloride channel located in nervous system of invertebrates. In recent years, studies have been performed to evaluate the efficacy and safety of isoxazolines against various types of ectoparasites, including fleas, ticks, and mites. As more single and combined isoxazoline products have been approved by the United States Food and Drug Administration and European Medicines Agency, a more comprehensive understanding of isoxazolines becomes essential for veterinary clinical practitioners. This article provides a complete review of isoxazolines with respect to pharmacodynamics, pharmacokinetics, ectoparasiticidal efficacy, and safety, which will provide veterinarians information to allow them to make the best choice of ectoparasiticide for their clients' specific needs.


Subject(s)
Flea Infestations , Insecticides , Siphonaptera , Ticks , Animals , Chloride Channels , Flea Infestations/veterinary , Isoxazoles/therapeutic use
11.
Molecules ; 26(16)2021 Aug 06.
Article in English | MEDLINE | ID: mdl-34443355

ABSTRACT

Amitraz, a member of the formamidine pesticide family, commonly used for ectoparasite control, is applied as a dip or low-pressure hand spray to cattle and swine, and the neck collar on dogs. Data on amitraz were generated mainly on laboratory animals, hens, dogs, and baboons. The data on the toxicity and disposition of amitraz in animals and its residues in the milk are inadequate. Therefore, the present study was intended to analyze the disposition kinetics of amitraz and its pattern of elimination in the milk of lactating does after a single dermal application at a concentration of 0.25%. Blood at predetermined time intervals and milk twice daily were collected for eight days post application. The drug concentration was assayed by high-performance liquid chromatography (HPLC). Amitraz was detected in whole blood as early as 0.5 h, which attained a peak concentration at 12 ± 5 h, followed by a steady decline; however, detection persisted until 168 h. Amitraz was present in the blood at its 50% Cmax even after 48 h, and was still detectable after 7 days. The disposition after a single dermal application was best described non-compartmentally. The mean terminal half-life (t1/2), mean residence time (MRT), and area under the curve (AUC0-t) were 111 ± 31 h, 168 ± 39 h, and 539 ± 211 µg/mL/h, respectively. The apparent volume of distribution (Vdarea) was 92 ± 36 mL/g with an observed clearance (Cl) of 0.57 ± 0.33 mL/kg/h. Thus, the drug was well absorbed, widely distributed and slowly eliminated from the animal body. Amitraz achieved milk concentration approximating 0.2 per cent of the total dose after a single exposure and the steady-state elimination of amitraz in milk above the recommended maximum residue limit (MRL) of 0.01 mg/kg can act as a source of public health concern when applied on lactating animals.


Subject(s)
Deer , Lactation , Pesticide Residues/metabolism , Toluidines/metabolism , Animals , Cholic Acids , Female , Half-Life , Kinetics
12.
Ir Vet J ; 74(1): 20, 2021 Jul 05.
Article in English | MEDLINE | ID: mdl-34225804

ABSTRACT

BACKGROUND: Pediculosis in cattle causes significant itching, irritation and stress to the animal, often resulting in skin damage and poor coat condition. The control of bovine pediculosis in Ireland is based predominantly on commercial insecticides belonging to one of two chemical classes, the synthetic pyrethroids and the macrocyclic lactones. In recent years, pyrethroid tolerance has been reported in a number of species of livestock lice in the United Kingdom and Australia. RESULTS: In this pilot survey, lice were detected in 16 (94%) out of 17 herds visited. Two species of lice, Bovicola bovis and Linognathus vituli were identified. In vitro contact bioassays showed evidence of deltamethrin tolerance in Bovicola bovis collected from 4 farms. This was confirmed by repeatedly assessing louse infestations on treated animals on one farm. CONCLUSIONS: To our knowledge this is the first record of insecticide tolerant populations of lice in Irish cattle. The results also provide new data on the species of lice infesting beef cattle in Ireland and the prevalence and control of louse infestations in Irish beef cattle herds.

13.
Parasit Vectors ; 14(1): 264, 2021 May 20.
Article in English | MEDLINE | ID: mdl-34016157

ABSTRACT

BACKGROUND: The study objective was to examine cat owner ectoparasiticide purchases in the United States and estimate the impact of purchase gaps on timely ectoparasite protection administration. These purchase gaps lead to periods of time when cats are unprotected from ectoparasites. METHODS: Ectoparasiticide purchase transactions for individual cats from 671 U.S. veterinary clinics from January 1, 2017 through June 30, 2019 were evaluated to determine time "gaps" between doses of ectoparasiticides purchased in a defined 12-month period. Ectoparasiticides examined were topically applied products that contained fluralaner, fipronil/(S)-methoprene/pyriproxyfen, imidacloprid/pyriproxyfen or selamectin as active ingredients. The duration of protection following administration of one dose was 8-12 weeks for the fluralaner-containing product and one month for the other products. RESULTS: Ectoparasiticide purchase records were obtained from 114,853 cat owners and analysis found that most owners bought ≤ 6 months of protection during the year, with 61-75% (depending on the product) purchasing just 1-3 months of protection. The size of the average purchase gap was determined for all dose combinations out to 12 months of protection (5-7 doses for fluralaner and 12 doses for the other three products dosed monthly. The largest gaps occurred between the first and second doses and the second and third doses. Average purchase gaps for the four different products between doses 1 and 2 ranged from 11.2 to 13.9 weeks and between doses 2 and 3 ranged from 7.7 to 12.2 weeks. The fraction of purchases separated by gaps and the average length of the gap tended to decrease with increasing number of doses purchased. Owners purchasing the 8 to 12-week duration product containing fluralaner provided ectoparasite protection ("doses plus gap period") for a larger proportion of each 2-dose period compared with owners purchasing products administered monthly. CONCLUSIONS: When cat owners purchase flea and tick medication, gaps between subsequent purchases reduces the proportion of time ectoparasite protection can be provided. The duration of the gap between doses has an impact on the effectiveness of flea/tick medication because it inserts a period without flea and tick protection between doses of flea and tick medication. The gaps between purchases were shorter and the period of ectoparasite protection was larger for owners purchasing a 12-week product than for owners purchasing a monthly product.


Subject(s)
Cat Diseases/drug therapy , Flea Infestations/drug therapy , Flea Infestations/veterinary , Insecticides/administration & dosage , Isoxazoles/administration & dosage , Tick Infestations/veterinary , Animals , Cat Diseases/economics , Cat Diseases/parasitology , Cats , Ctenocephalides/drug effects , Ctenocephalides/growth & development , Flea Infestations/economics , Flea Infestations/parasitology , Hospitals, Veterans/economics , Humans , Insecticides/economics , Isoxazoles/economics , Tick Infestations/drug therapy , Tick Infestations/economics , Tick Infestations/parasitology , Ticks/drug effects , Ticks/growth & development , United States
14.
Parasit Vectors ; 13(1): 541, 2020 Oct 31.
Article in English | MEDLINE | ID: mdl-33129346

ABSTRACT

BACKGROUND: Safe and effective flea and tick treatment options for cats are important in companion animal practice because of feline ectoparasite infestation prevalence and the potential for parasitic disease transmission. Retrospective cat owner purchasing transactions at United States of America (USA) veterinary clinics were obtained for three topical feline flea and tick ectoparasiticides. One medication, fluralaner, had a 12-week redosing interval, while two other medications (fipronil/s-methoprene/pyriproxyfen; imidacloprid/pyriproxyfen) were approved for monthly redosing. The annual number of doses purchased by cat owners was determined for each of the three medications and then compared between medications. The objective was to evaluate whether 12-week retreatment intervals resulted in a different duration of coverage compared to monthly treatments for ectoparasiticide products. METHODS: Study results were obtained by analyzing the transactional records from a commercial database derived from veterinary practice management software. The study database consisted of cat owner purchasing records from January 2017 through June 2019 from 671 veterinary practices representing 41,630 cats. RESULTS: Cat owners purchased an average of 1.5 doses of fluralaner per year which, based on a 12-week redosing interval, provides 4.2 months of treatment coverage. Cat owners who used monthly flea and tick medications respectively purchased 3.6 months (fipronil/s-methoprene/pyriproxyfen combination) and 2.8 months (imidacloprid/pyriproxyfen) annually of each of the two medications. Average yearly cat owner purchases of fluralaner provide a significantly longer duration of coverage than for cat owners purchasing fipronil/s-methoprene/pyriproxyfen (17% more) or imidacloprid/pyriproxyfen (50% more). CONCLUSIONS: Cat owners who obtained a flea and tick treatment with a 12-week redosing interval (fluralaner) protected their cats for up to 17% or 50% longer duration each year, respectively, compared to the duration of protection obtained by cat owners who used a medication re-dosed monthly. Cat owners should increase their duration of flea and tick coverage to come closer to achieving veterinary recommendations.


Subject(s)
Ectoparasitic Infestations/veterinary , Hospitals, Animal , Insecticides/economics , Ownership , Pets , Animals , Cat Diseases/drug therapy , Cats , Ectoparasitic Infestations/drug therapy , Ectoparasitic Infestations/epidemiology , Guideline Adherence , Insecticides/pharmacology , Isoxazoles/therapeutic use , Retrospective Studies , Siphonaptera/drug effects , Ticks/drug effects , United States/epidemiology
15.
Pestic Biochem Physiol ; 163: 123-129, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31973848

ABSTRACT

The isoxazoline ectoparasiticide fluralaner exerts antiparasitic effects by inhibiting the function of γ-aminobutyric acid (GABA) receptors (GABARs). The present study was conducted to identify the amino acid residues that contribute to the high sensitivity of insect GABARs to fluralaner. We generated housefly (Musca domestica) GABARs with amino acid substitutions in the first through third α-helical transmembrane segments (TM1-TM3) of the RDL subunit using site-directed mutagenesis and examined the effects of the substitutions on the sensitivity of GABARs expressed in Xenopus oocytes to fluralaner using two-electrode voltage clamp electrophysiology. The Q271L substitution in TM1 caused a significant reduction in the sensitivity to fluralaner. Although the I274A and I274F substitutions in TM1 did not affect fluralaner sensitivity, the I274C substitution significantly enhanced the sensitivity to fluralaner. In contrast, the L278C substitution in TM1 reduced fluralaner sensitivity. Substitutions of Gly333 in TM3 led to substantial reductions in the sensitivity to fluralaner. These findings indicate that Gln271, Ile274, Leu278, and Gly333, which are situated in the outer half of the transmembrane subunit interface, are closely related to the antagonism of GABARs by fluralaner.


Subject(s)
Houseflies , Receptors, GABA , Amino Acid Substitution , Animals , Isoxazoles , Oocytes , Receptors, GABA-A
16.
AAPS PharmSciTech ; 21(1): 9, 2019 Dec 03.
Article in English | MEDLINE | ID: mdl-31797083

ABSTRACT

Increased human-pet interactions have led to concerns related to the prevention and treatment of ectoparasite infestations. Fipronil (FIP) is a widely used ectoparasiticide in veterinary medicine available for topical administration; however, its use may cause damage to the owners and the environment. The aim of the study was to develop immediate-release tablets of FIP, as well as to determine its pharmacokinetic properties after oral administration in beagle dogs. The prepared FIP tablets were evaluated for pre-compression (angle of repose, speed flow, and Carr's index) and post-compression (weight variation, friability, thickness, hardness, disintegration time, and dissolution rate) parameters. Orally administered FIP at a dose of 2 mg/kg was rapidly absorbed with Cmáx of 3.13 ± 1.39 µg/mL at 1.83 ± 0.40 h post treatment (P.T.) and metabolized with 1.27 ± 1.04 µg/mL at 2.33 ± 0.82 h P.T. for fipronil sulfone (SULF) (the primary metabolite). The elimination of FIP and SULF occurred slowly and had maintained quantifiable plasma levels in the blood for up to 28 days P.T. The goal of the study is aligned with the concept of One Health, which aims to collaboratively achieve the best health for people, animals, and the environment. Therefore, the use of FIP tablets for the control of ectoparasites in dogs may be a safer alternative for owners and the environment.


Subject(s)
Antiparasitic Agents/chemistry , Antiparasitic Agents/pharmacokinetics , Pyrazoles/chemistry , Pyrazoles/pharmacokinetics , Administration, Oral , Animals , Antiparasitic Agents/administration & dosage , Dogs , Hardness , Pyrazoles/administration & dosage , Tablets , Water Pollution/prevention & control
17.
Parasit Vectors ; 11(1): 581, 2018 Nov 06.
Article in English | MEDLINE | ID: mdl-30400923

ABSTRACT

BACKGROUND: Veterinary clinic transaction records from the USA were examined to determine dog owner purchase patterns for three prescription ectoparasiticides. In-clinic purchases of formulations of fluralaner (with 12-week duration per dose) were compared with dog owner purchases of afoxolaner and spinosad (both with 4 week duration per dose) in a population of 231,565 dogs over a 12 month period. Prior studies in human and animal medicine have suggested that patients more closely adhere to prescriber dosing recommendations when they receive a longer-duration medication. RESULTS: Veterinary clinic transaction records were examined for the period June 2014 through March 2017 using records from approximately 650 veterinary clinics. Ectoparasiticide purchase patterns were compared for two products (afoxalaner and spinosad) with monthly dosing and one product (fluralaner) with an extended (12 week) dosing interval. The average dog owner who obtained fluralaner purchased significantly more months of flea/tick protection (5.7 months) over the 12-month study period than the average dog owner that selected either afoxolaner (4.6 months) or spinosad (3.3 months). The proportion of dog owners who obtained only one dose of ectoparasiticide per 12-month period was 42% for fluralaner, 30% for afoxolaner and 37% for spinosad. The proportion of dog owners who obtained 2 doses or less per 12-month period was 67% for fluralaner, 52% for afoxoalaner and 67% for spinosad. Owners that obtained fluralaner were significantly more likely to obtain 7.0-12.0 months of flea and tick protection and significantly less likely to purchase 1.0-6.9 months compared with dog owners who purchased afoxolaner or spinosad. CONCLUSIONS: Dog owners who obtained a flea and tick medication with a longer duration of action acquired significantly more months of protection in a year than dog owners who obtained shorter duration (1 month) products. Dog owners were better able to adhere to veterinary recommendations on ectoparasites control with a longer-acting flea/tick medication.


Subject(s)
Flea Infestations/veterinary , Medication Adherence , Ownership/statistics & numerical data , Records , Veterinary Drugs/therapeutic use , Veterinary Medicine , Animals , Dog Diseases/drug therapy , Dog Diseases/epidemiology , Dogs , Drug Combinations , Flea Infestations/drug therapy , Hospitals, Animal , Humans , Insecticides/administration & dosage , Insecticides/therapeutic use , Isoxazoles/administration & dosage , Isoxazoles/therapeutic use , Macrolides/administration & dosage , Macrolides/therapeutic use , Naphthalenes/administration & dosage , Naphthalenes/therapeutic use , Prescription Drugs/administration & dosage , Prescription Drugs/therapeutic use , Siphonaptera/drug effects , Ticks/drug effects , United States
18.
Parasit Vectors ; 11(1): 458, 2018 Aug 07.
Article in English | MEDLINE | ID: mdl-30086779

ABSTRACT

BACKGROUND: Doses of flea and tick medication acquired by dog owners over a 12 month period were determined from veterinary hospital transaction records in Spain. The number of months of flea and tick protection potentially obtained by dog owners prescribed fluralaner, a flea and tick medication with a 12 week re-dosing interval, was compared with months of flea and tick protection obtained by dog owners prescribed monthly oral or spot-on products. Prior studies in human and veterinary medicine have suggested that longer-acting medications benefit patients by providing improved adherence to provider recommendations. RESULTS: Dog owners took home, on average, significantly more months of protection when they obtained the 12 week duration product fluralaner (4.3 months) than they did when they obtained other flea and tick products providing 1 month of protection [3.24 months (oral), 2.9 months (spot-on)]. Many dog owners (46-64%) obtained only one dose of flea and tick product each year, regardless of the duration of protection offered by the product. Significantly more dog owners obtained 7-12 months of protection when they were prescribed fluralaner (15.7%) by their veterinarians compared with dog owners prescribed monthly flea and tick products [6.8% (oral), 8.3% (spot-on)]. CONCLUSION: Veterinary prescription of fluralaner delivers more months of potential flea and tick protection as shown by dog owner acquisition of flea and tick medication. The use of a longer-acting medication requires the administration of fewer doses and may translate into better adherence to veterinary ectoparasite control recommendations.


Subject(s)
Dog Diseases/prevention & control , Flea Infestations/veterinary , Insecticides/pharmacology , Tick Infestations/veterinary , Administration, Oral , Administration, Topical , Animals , Delayed-Action Preparations , Dogs , Drug Administration Schedule , Flea Infestations/epidemiology , Flea Infestations/prevention & control , Humans , Insecticides/administration & dosage , Isoxazoles/administration & dosage , Isoxazoles/pharmacology , Ownership , Retrospective Studies , Seasons , Spain/epidemiology , Tick Infestations/epidemiology , Tick Infestations/prevention & control
19.
Med Vet Entomol ; 31(4): 351-357, 2017 12.
Article in English | MEDLINE | ID: mdl-28714540

ABSTRACT

An ectoparasiticide combining three active ingredients [dinotefuran, permethrin and pyriproxyfen (DPP)] was used in mice in an experiment designed to evaluate its anti-feeding and insecticidal efficacy against Stegomyia albopicta (= Aedes albopictus) (Diptera: Culicidae) mosquitoes. Twenty-two adult mice were randomly allocated into two groups consisting of an untreated control group and a DPP-treated group. Mice were exposed individually for 1 h to a mean ± standard deviation of 27 ± 2 starved female mosquitoes on days 1, 7, 14, 21 and 28 post-treatment. At the end of the exposure (1 h), mosquitoes were assessed for immediate survival and engorgement status. Additionally, live mosquitoes in both groups were incubated separately and observed for mortality at 24 h after the end of the exposure. The anti-feeding efficacy of DPP after the 1-h exposure period was 99.2, 100, 98.0, 89.3 and 87.4% at 1, 7, 14, 21 and 28 days, respectively. Levels of insecticidal efficacy evaluated at 1 h and 24 h after exposure on days 1, 7, 14, 21 and 28 were 36.7, 28.9, 30.8, 23.1 and 11.9%, and 68.4, 45.0, 43.3, 37.9 and 19.9%, respectively. Based on the mouse model, the present study demonstrates that the DPP combination has significant anti-feeding and insecticidal efficacy against S. albopicta for at least 4 weeks.


Subject(s)
Aedes/drug effects , Guanidines/pharmacology , Insect Repellents/pharmacology , Insecticides/pharmacology , Neonicotinoids/pharmacology , Nitro Compounds/pharmacology , Permethrin/pharmacology , Pyridines/pharmacology , Administration, Cutaneous , Animals , Feeding Behavior/drug effects , Female , Mice , Random Allocation , Rats
20.
Med Vet Entomol ; 31(2): 132-139, 2017 06.
Article in English | MEDLINE | ID: mdl-27862092

ABSTRACT

This study, based on the rat model, was designed to explore the anti-feeding and insecticidal efficacy of a topical ectoparasiticide, dinotefuran-permethrin-pyriproxyfen (DPP), against Triatoma infestans (Hemiptera: Reduviidae), a vector of Trypanosoma cruzi (Trypanosomatida: Trypanosomatidae), for which dogs are domestic reservoir hosts. Twenty rats were divided into two equal groups: untreated and treated. Each rat was exposed under sedation to 16 T. infestans of mixed life stages for 1 h on days 1, 7, 14, 21 and 28 post-treatment. The anti-feeding and insecticidal effects of DPP were estimated after 1 h of exposure. Insecticidal efficacy was also assessed after incubation of the insects for 24 h post-exposure. Anti-feeding efficacy was 96.7, 84.7, 80.5, 81.5 and 42.6% on days 1, 7, 14, 21 and 28, respectively. Insecticidal efficacy evaluated at 1 and 24 h after exposure on days 1, 7, 14, 21 and 28 was 100, 91.2, 82.5, 80.0 and 29.1, and 100, 100, 100, 96.0 and 49.9%, respectively. This study demonstrates that a single administration of DPP spot-on treatment at a dose equivalent to the minimal recommended dose in rats has a powerful effect against T. infestans starting from day 1 that lasts for at least 3 weeks.


Subject(s)
Ectoparasitic Infestations/veterinary , Guanidines , Insect Control , Insecticides , Nitro Compounds , Permethrin , Pyridines , Triatoma , Animals , Disease Models, Animal , Ectoparasitic Infestations/prevention & control , Female , Male , Neonicotinoids , Nymph/growth & development , Rats , Triatoma/growth & development
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