Pharmacology of ivermectin

Bennett, J.L.; Williams, J. F.; Dave, Vivek

doi:10.1016/0169-4758(88)90163-9

Cited by 59 publications

(54 citation statements)

References 14 publications

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“…There is much interest in the potential of ivermectin (IVM) as a microfilaricide for the treatment of onchocerciasis (Bennett, Williams & Dave, 1988), and mass trials against onchocerciasis are being implemented in 12 African and Central American countries. IVM has proven to be a very effective antiparasitic drug and many of the common gastrointestinal nematodes are highly susceptible to IVM at concentrations much lower than those at which other anthelmintics are effective.…”

Section: Introductionmentioning

confidence: 99%

In vitro studies on the relative sensitivity to ivermectin of Necator americanus and Ancylostoma ceylanicum

Richards

Behnke

Duce

1995

International Journal for Parasitology

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Section: Introductionmentioning

confidence: 99%

In vitro studies on the relative sensitivity to ivermectin of Necator americanus and Ancylostoma ceylanicum

Richards

Behnke

Duce

1995

International Journal for Parasitology

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“…In vitro, IVM effects on mf appear only at concentrations far above levels achieved during therapy for filariases (9). In the model nematode Caenorhabditis elegans and intestinal parasitic nematodes, IVM affects pharyngeal pumping and motor activity at concentrations 0.1 to 10 nM (10)(11)(12).…”

mentioning

confidence: 99%

Ivermectin disrupts the function of the excretory-secretory apparatus in microfilariae of Brugia malayi

Moreno

Nabhan

Solomon

et al. 2010

Proc. Natl. Acad. Sci. U.S.A.

147

141

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Ivermectin (IVM) is a broad-spectrum anthelmintic used in filariasis control programs. By binding to nematode glutamate-gated chloride channels (GluCls), IVM disrupts neurotransmission processes regulated by GluCl activity. IVM treatment of filarial infections is characterized by an initial dramatic drop in the levels of circulating microfilariae, followed by long-term suppression of their production, but the drug has little direct effect on microfilariae in culture at pharmacologically relevant concentrations. We localized Brugia malayi GluCl expression solely in a muscle structure that surrounds the microfilarial excretory-secretory (ES) vesicle, which suggests that protein release from the ES vesicle is regulated by GluCl activity. Consistent with this hypothesis, exposure to IVM in vitro decreased the amount of protein released from microfilariae. To better understand the scope of IVM effects on protein release by the parasite, three different expression patterns were identified from immunolocalization assays on a representative group of five microfilarial ES products. Patterns of expression suggest that the ES apparatus is the main source of regulated ES product release from microfilariae, as it is the only compartment that appears to be under neuromuscular control. Our results show that IVM treatment of microfilariae results in a marked reduction of protein release from the ES apparatus. Under in vivo conditions, the rapid microfilarial clearance induced by IVM treatment is proposed to result from suppression of the ability of the parasite to secrete proteins that enable evasion of the host immune system. filarial nematode | macrocyclic lactone | glutamate-gated chloride channels

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“…Su gran tamaño molecular y el alto grado de unión a las proteínas del plasma limita su paso hacia el SNC a través de la BHE (Fisher y Mrozik 1992, Paul y Bajean 1993. Esta limitada distribución hacia el SNC parece ser el factor más importante en la diferenciación de la toxicidad selectiva hacia los invertebrados y de su amplio margen de seguridad para el huésped mamífero vertebrado (Campbell y Benz 1984, Bennet 1986). Sin embargo, algunos factores como el insuficiente desarrollo de la BHE en los recién nacidos o la acción de procesos febriles pueden determinar que se incremente el paso de moléculas de IVM hacia el SNC y logre concentraciones que sean capaces de actuar sobre las neuronas gabaergicas y ejercer alguna acción farmacológica.…”

Section: Residuos De Ivermectina En Predios Lecherosunclassified

Metodología analítica y detección de residuos de ivermectina en muestras de leche de rebaños de la provincia de Ñuble, Chile

et al. 2006

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SUMMARYA study was undertaken in order to validate a precise and reliable analytical method for ivermectin detection and quantification in milk and to determine the presence of ivermectin's residues in milk samples taken from dairy farms in the province of Ñuble. Analytical methodology was adequately validated using drug free milk samples fortified with increasing concentrations of ivermectin (0.5 to 25 ng/mL), which were subjected to solid phase extraction and analyzed by high performance liquid chromatography. Milk samples were taken from the storage tanks of medium and high productive level dairy farms in the province of Ñuble. Samples were collected in the four different season of the year: Summer (january), Fall (april), Winter (august) and Spring (November). The limit of quantification of the analytical method was established to be 0.043 ng/mL. The absence of interferences and the adequate symmetry of the chromatograms suggest a good specificity of the method, with a recovery ranging from 73.5 to 79.5% for the minimal and maximal drug concentration, respectively. The analytical method presented satisfactory results of specificity, precision and accuracy that allow its use for the detection of residues of ivermectin in milk. Of 96 milk samples obtained from the storage tanks of dairy farms in the province of Ñuble, 8.3% presented ivermectin concentrations which were greater than the limit of quantification of the analytical method. These results demonstrate that it is possible to find ivermectin residues in milk and they justify further studies in order to detect the presence of these drugs in milk, as their presence is a negative attribute in terms of quality. INTRODUCCIONPara la mayoría de las explotaciones ganaderas el parasitismo gastrointestinal representa una amenaza permanente al estado sanitario del rebaño, debido a la contaminación continua de las praderas por huevos y larvas de nemátodos. A pesar de que en los animales de lechería la inmunidad les confiere una mayor resistencia, la intensificación de la producción puede aumentar la susceptibilidad al parasitismo. Estudios han demostrado que la inmunidad parasitaria puede disminuir durante los períodos de estrés aumentando la vulnerabilidad del ganado a la acción patógena de los parásitos. Estas interferencias con las defensas del hospedador pueden producir pérdidas de productividad como consecuencia de los efectos causados por la enfermedad subclínica (Hawkins 1993). Por lo tanto, el mejoramiento de la calidad productiva muchas veces obliga a la introducción de medidas en el manejo sanitario de la explotación que involucran el uso de antihelmínticos para el control del parasitismo. Además, se ha demostrado que el tratamiento antihelmíntico ejerce un efecto positivo sobre el aumento de la producción láctea en los animales tratados (Ploeger y col 1989) En las últimas décadas el uso de ivermectina (IVM) se ha convertido en una de las alternativas de tratamiento de mayor eficacia y uso frecuente por parte de los ganaderos, debido a que se trata de ...

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Pharmacology of ivermectin

Cited by 59 publications

References 14 publications

In vitro studies on the relative sensitivity to ivermectin of Necator americanus and Ancylostoma ceylanicum

In vitro studies on the relative sensitivity to ivermectin of Necator americanus and Ancylostoma ceylanicum

Ivermectin disrupts the function of the excretory-secretory apparatus in microfilariae of Brugia malayi

Metodología analítica y detección de residuos de ivermectina en muestras de leche de rebaños de la provincia de Ñuble, Chile

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