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At least 811 records · Page 45Linked to original sources
PubMed2004

Validated capillary electrophoretic method for the analysis of ivermectin in plasma after intragastric administration in pigs and horses.

A capillary electrophoretic (CE) method has been developed for the determination of ivermectin (CAS 70288-86-7), a new generation drug with antiparasitic activity, in pig and horse plasma. The method was statistically validated for its linearity, accuracy, precision and selectivity. The linear range was from 1 to 30 ng mL(-1) with correlation coefficients greater than 0.999. The limit of detection was 0.3 ng mL(-1), while the quantitative limit was 1 ng mL(-1), using a 0.5 mL sample size. The validated procedure was used to determination of pharmacokinetic parameters of ivermectin after ingestion of 0.1 mg for pigs and 0.2 mg dose per kg body weight for horses, respectively. Studies were performed on a group of eight pigs and six horses. There were no significant differences between pigs and horses in any of the estimated pharmacokinetic parameters.

Animals↗
PubMed1995

Decreased biotolerability for ivermectin and cyclosporin A in mice exposed to potent P-glycoprotein inhibitors.

SDZ PSC 833 or SDZ 280-446 are strong blockers of the function of class I mdr gene-encoded P-glycoprotein molecules, which were developed for the reversal of multi-drug-resistance of tumor cells. When treated with such drugs, normal mice may display hypersensitivity to cyclosporin A and ivermectin. The recorded signs of acute toxicity are compatible with alterations of the murine central nervous system functions and with earlier data suggesting that P-glycoprotein expressed at the murine blood-brain barrier might be involved in the exclusion of cyclosporin A or ivermectin from brain tissue.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed1985

Pharmacokinetics of ivermectin administered intravenously to cattle.

Ivermectin, a macrocyclic lactone disaccharide antiparasitic agent, was administered intravenously to six young calves (one bull, five steers) as a bolus dose of 200 micrograms/kg. The disposition kinetics of ivermectin in cattle can be described by a three-compartment open model with elimination from the central compartment. Compartmental analysis yielded mean parameters as follows: terminal elimination rate constant (beta) = 0.258 d-1, biological half-life (t 1/2 beta) = 2.7 d; apparent volume of distribution of the central compartment (Vd1) = 0.45 L/kg; apparent volume of distribution at steady state (Vdss) = 2.4 L/kg. The area under the plasma concentration-time curve (AUC) was 254 ng X d/mL. Noncompartmental parameters, obtained by utilizing statistical moment theory, mean residence time (MRT), clearance (CL), and Vdss were calculated to be 2.8 d, 0.79 L/kg X d, and 2.2 L/kg, respectively.

Animals↗
PubMed2000

Eotaxin and RANTES expression by the dermal endothelium is associated with eosinophil infiltration after ivermectin treatment of onchocerciasis.

The roles of eotaxin, RANTES, and MCP-3 expression in eosinophil recruitment to the site of parasite killing that occurs following ivermectin treatment of onchocerciasis were assessed in the skin of 13 Onchocerca volvulus-infected subjects and two noninfected controls before and after ivermectin treatment. Adverse reactions in infected subjects were associated with the appearance of eosinophils in the dermis as part of a perivascular inflammatory infiltrate. Although no expression of RANTES and eotaxin was seen in dermal vascular endothelial cells in biopsies taken before treatment (nor at any time in the skin of uninfected controls), endothelial expression of both eotaxin and RANTES was noted by 24 h following treatment. While RANTES expression was transient, eotaxin expression increased in parallel with increasing eosinophil recruitment up to 60 h posttreatment. These observations indicate that endothelial expression of eotaxin and RANTES may have an important role in eosinophil recruitment into the skin during helminth-killing reactions.

Adult↗
PubMed1997

Ivermectin-induced killing of microfilariae in vitro by neutrophils mediated by NO.

Rat neutrophil granulocytes isolated after intraperitoneal casein injection of the donors exhibit high cytotoxic efficacy in vitro against microfilariae of Litomosoides carinii in the presence of ivermectin. Optimum effects of 80-90% killing of microfilariae were obtained with 100 ng ivermectin per milliliter and a microfilariae: cell ratio of 1:100. Spleen cells killed approximately 30% of the microfilariae under these conditions. Cytotoxic effects were independent of any adherence of the cell to the larvae. In contrast to the effects of spleen cells, cytotoxicity of neutrophils completely abrogated when cells and targets were separated by a membrane impermeable for the cells, suggesting a very short-living mediator in the latter case. Correspondingly, cytotoxic effects of neutrophils were completely inhibited by the addition of the arginine analogues NG-monomethyl-L-arginine and L-canavanine, indicating the involvement of reactive nitrogen intermediates. The nitric oxide scavenger hemoglobin also protected the microfilariae. Several compounds which are known to interfere with reactive oxygen intermediates were ineffective. An excess of ferrous ions in the medium in the presence of a reducing agent significantly reduced the cytotoxic efficacy of neutrophils.

Animals↗
PubMed1999

Echinococcus granulosus: in vitro effects of ivermectin and praziquantel on hsp60 and hsp70 levels.

Martinez, J., Perez-Serrano, J., Bernadina, W. E., Rodriguez-Caabeiro, F. 1999 Echinococcus granulosus: In vitro effects of ivermectin and praziquantel on hsp60 and hsp70 levels. Experimental Parasitology93, 171-180. Organisms or cells exposed to injurious stresses such as heat shock or chemicals respond by increased (or altered) expression of heat-shock proteins (HSPs). Conversely, an earlier exposure to stress can prepare cells to cope with a subsequent more severe stress. In the present study, protoscolices of Echinococcus granulosus were subjected to several anthelmintic treatments, involving storage of the protoscolices for 18, 30, and 50 h with 0.1 mg/ml of ivermectin (IV), praziquantel (PZ), and a combination of each with albendazole (ALB). The organisms were analyzed for the effects of drug treatment on cell integrity and on levels of hsp60 and hsp70 production. Drug efficacy was evaluated by microscopy and by protein content measurement. Hsp60 and hsp70 were detected by Western blotting and incubation with anti-hsp60 and anti-hsp70 antibody, respectively, and quantitation of these proteins was obtained using image analysis. Incubation with IV alone produced the most damage to the protoscolices as indicated by viability loss, decreased protein content, and altered hsp60 and hsp70 levels; incubation with IV + ALB produced less damage as manifested by fewer changes in the aforementioned damage parameters but PZ and PZ + ALB, in this context, were poor anthelmintics. Exposure of protoscolices to thermal stress prior to anthelmintic treatment, in most cases, increased drug efficacy. It is concluded that in the E. granulosus model system drug efficacy is associated with decreased levels of hsp70 expression and increased levels of hsp60 expression.

Albendazole↗
PubMed1993

Ticks (Acari: Ixodidae) infesting the Arabian camel (Camelus dromedarius) in the Sinai, Egypt with a note on the acaricidal efficacy of ivermectin.

In this study, tick burdens on camels (Camelus dromedarius) were determined in the vicinity of the St. Catherine monastery, Sinai, Egypt. In total 2,545 ticks (1,491 adults and 1,054 nymphs) were collected and identified. Mean tick burdens were relatively heavy and the range in number of ticks per camel was very broad (6-173). Hyalomma dromedarii was the predominant tick species and accounted for 95.6% of the adult ticks. Other ticks found were H. marginatum subspp. and H. anatolicum excavatum. All nymphs collected were Hyalomma spp. In addition, the effect of ivermectin (Ivomec MSD AGVET) on tick burdens, when given subcutaneously at 0.2 mg/kg-1, was evaluated in nine camels in the date-palm plantation of Kibbutz Yahel in the Arava valley, Israel. Initial tick burdens on these camels (half-body tick counts) ranged from 20-105 ticks per camel. Seven camels from the same herd with half-body tick counts ranging from 40-107 ticks per camel were not treated and served as a control group. Ivermectin was not effective against Hyalomma tick infestation in camels under these conditions.

Animals↗
PubMed1991

Ivermectin is not an agonist at a GABA receptor in tick salivary glands.

The avermectins, broad-spectrum anti-parasitic agents which are effective against ticks, act principally by stimulating gamma-aminobutyric acid (GABA) receptors directly or indirectly. GABA is known to potentiate dopamine-induced fluid secretion in the salivary glands of female ixodid ticks. We thus tested whether 10 microM ivermectin would have an effect similar to GABA in the isolated salivary gland preparation of Dermacentor andersoni. Ivermectin was not an agonist at this GABA receptor.

Animals↗
PubMed1996

Comparative efficacies of closantel, ivermectin, oxfendazole, thiophanate and levamisole against thiabendazole resistant Haemonchus contortus in sheep.

Forty-nine sheep artificially exposed to a thiabendazole (TBZ) resistant isolate of Haemonchus contortus were assigned to 7 groups of 7 animals each and used to conduct a controlled anthelmintic trial. One group of sheep served as untreated infected controls and 6 groups were treated as follows: closantel, 5.0 mg kg-1; ivermectin, 0.2 mg kg-1; oxfendazole, 5.0 mg kg-1; thiophanate, 50 mg kg-1, levamisole, 7.5 mgkg-1 and thiabendazole, 66 mg kg-1. Eggs per gram of faeces were determined on days 21, 24 and day 34 (10 days post-treatment) after infection and all animals were necropsied for residual worm counts. The calculated efficacies of the treatments against H. contortus as indicated by worm reduction were closantel (100%), ivermectin (99.3%), oxfendazole (35.2%), thiophanate (56.7%), levamisole (98.6%) and thiabendazole (24.3%). The data therefore indicate that the TBZ-resistant isolate of H. contortus used was highly resistant to the 2 benzimidazole (BZ) anthelmintics, oxfendazole and thiophanate. This is the first report in Kenya of a field strain of H. contortus resistant to thiophanate.

Animals↗
PubMed1987

Control of cattle mange in southern Africa using ivermectin.

Seven trials including 768 cattle were conducted in South Africa and Namibia to evaluate the efficacy of the systemic parasiticide ivermectin when administered subcutaneously at a dose rate of 200 micrograms/kg against sarcoptic (Sarcoptes scabiei var. bovis), chorioptic (Chorioptes bovis) and psoroptic (Psoroptes ovis var. bovis) mange mites. The efficacy of a single treatment against Psoroptes and Sarcoptes was greater than against Chorioptes. There was marked clinical cure in all treated cases with loss of crusts and hair regrowth. The number of cases of psoroptic mange in two large herds, of which 42.4% of 724 animals were clinically affected prior to mass treatment, was reduced by 99.3% following a single subcutaneous treatment with ivermectin; a single animal from which mites were recovered may not have been treated. The apparent prevalence and prospects for control and eradication of cattle mange in South Africa and Namibia are discussed.

Administration, Oral↗
PubMed2003

Efficacy of an in-feed preparation of ivermectin against helminths in the European wild boar.

The wild boar is one of Europe's most popular game species and its densities are increasing. Management tools such as farm breeding, supplementary feeding, and translocations are more frequently employed and anthelmintics are increasingly used in game farms and translocations. Here, we report the results of a controlled slaughter study on the efficacy of an in-feed preparation of ivermectin in European wild boars naturally infected with various helminths. The efficacy of ivermectin against adult stages of Metastrongylus sp., Ascaris suum, Ascarops strongylina, Physocephalus sexalatus, and Simondsia paradoxa was 100%. Its efficacy against Oesophagostomum dentatum was 85.1%. There was no sufficient effect on Globocephalus urosubulatus, Trichuris suis, and Capillaria garfiai. The egg reduction in the treated group ( n=12) was 100% 6 days after the treatment. The importance of parasite surveillance and the application of anthelmintic treatments to wild boars in game farms or during translocations are discussed. We conclude that any attempt at helminth treatment in wild boars should consider the addition of a second compound with a more consistent effect on trichurids and other helminths.

Administration, Oral↗
PubMed2006

Effects of parasitic helminths and ivermectin treatment on clinical parameters in the European wild boar (Sus scrofa).

Limited information exists on serum biochemistry and haematology of the European wild boar, and few correlations have been found between parasitic burden and clinical parameters in this species. Naturally infected wild boars were experimentally treated to study the effect of nematode parasites and ivermectin treatment on phytohaemagglutinin (PHA) skin reaction and haematological and serum biochemical parameters. White blood cells decreased in untreated wild boars, whereas triglyceride, lactate and creatinine concentrations increased in ivermectin-treated wild boars, and total protein and aspartate aminotransferase activity increased in both groups. Band neutrophils variation was positively correlated with the number of total adult parasites. Band neutrophils, creatinine and total protein variations were negatively correlated with both total egg counts and Metastrongylus eggs per gram variations. Alkaline phosphatase activity showed a negative correlation with Ascaris sp. eggs. The PHA skin reaction was positively correlated with the number of total adult parasites in untreated wild boars and with Metastrongylus sp. eggs of all wild boars at time 0. Two models including leukocytic and serum biochemical parameters were also highly correlated with the variation of Metastrongylus sp. eggs. Clinical parameters were thus in our study affected by helminth parasitism in the European wild boar, particularly those related to nutrients uptake, physical condition and immune response. Therefore, they could be useful in studies on subclinical effects of parasites, and parasitic burden must be considered when assessing the physical condition of European wild boars through haematological and serum biochemical parameters.

Alkaline Phosphatase↗
PubMed1996

Community-based ivermectin distributors: onchocerciasis control at the village level in Plateau State, Nigeria.

The use of community residents as agents for distributing mass ivermectin therapy for onchocerciasis provides a component of community participation absent from mobile team delivery methods. Community-based distribution, however, presupposes preexisting human resources in the endemic villages capable of fulfilling the essential functions of an ivermectin distribution process: mobilizing and educating the population, dispensing the drug, maintaining records, and monitoring and treating adverse reactions. Even when such human resources exist, the community workers must continue to receive tangible support from both external (government and donor agencies) and internal (community) sources. Donor and government agencies must accept that their data collection demands will be limited by the literacy standards of the communities being served. Community leaders must agree to set and use their own local standards of payment (including food stuffs or exchange in kind) to compensate the distributors for their time and efforts. The use of locally available human and remunerative resources is a prerequisite for true community ownership of a program.

Antinematodal Agents↗
PubMedDate not supplied

Effect of ivermectin on the ear mange mite, Psoroptes cuniculi, of rabbits.

Rabbits, naturally infected with ear mange mite, Psoroptes cuniculi, were injected subcutaneously with a single dose of ivermectin at 200 micrograms or 400 micrograms/kg of body weight. The effect of the drug was evaluated clinically and parasitologically over 4 weeks. The animals in both groups became negative for mites 6 days after treatment and remained so until the end of trial. The ear lesions disappeared in both groups. However, the regression of lesions was faster in rabbits administered 400 micrograms/kg of ivermectin.

Animals↗
PubMed1989

In vitro effects of levamisole and ivermectin against Echinococcus granulosus protoscoleces.

The in vitro effects of levamisole and ivermectin against Echinococcus granulosus protoscoleces were studied by means of light and electron microscopy. Both drugs had a protoscolicidal activity that increased proportionally with increasing concentrations of the drugs. Ivermectin showed the more rapid effects and caused contraction and paralysis of protoscoleces. A paralyzing effect was also observed with levamisole, followed by irreversible tissue vacuolation leading to death.

Animals↗
PubMed1986

Anticonvulsant effects of ivermectin in genetically-epileptic chickens.

In genetically-photosensitive epileptic chickens, the anti-parasitic agent ivermectin, at 1.0 and 5.0 mg/kg, decreased or prevented seizures induced by intermittent photic stimulation without any side-effects on the central nervous system. The latency and duration of this anti-convulsant effect was dose-dependent. When combined with diazepam, ivermectin prolonged the anti-convulsant action of diazepam.

Animals↗
PubMed1995

Influence of route of administration on the plasma concentrations of ivermectin in reindeer.

The concentration of ivermectin in the plasma of reindeer was measured after it was administered either topically as a pour-on preparation at 500 micrograms kg-1 bodyweight at different seasons to animals of different ages, or after subcutaneous and oral doses of 200 micrograms kg-1 bodyweight. The plasma concentrations of ivermectin were highest and least variable after it was administered subcutaneously.

Administration, Oral↗
PubMedDate not supplied

Mass chemoprophylaxis of lymphatic filariasis with a single dose of ivermectin in a Polynesian community with a high Wuchereria bancrofti infection rate.

In April 1991 supervised mass prophylaxis of lymphatic filariasis with a single dose of ivermectin, 100 micrograms/kg, was carried out in a Polynesian village with a high infection rate of Wuchereria bancrofti in humans and active transmission by the vector mosquito, Aedes polynesiensis. Of 876 inhabitants aged 3 years or more (pregnant women excluded), 864 (98.6%) were treated. Simultaneously, venous blood samples were collected from 577 (97.5%) of the 595 inhabitants aged 15 years or more, of whom 122 (21.4%) were found to be microfilaria (mf) carriers (86 males and 36 females). The geometric mean microfilariae (GMM) count was 358.7 mf/ml for the whole group, 387 mf/ml for males (range 1-8160 mf/ml) and 280 mf/ml for females (range 1-7769 mf/ml). Following treatment, 33 (3.8%) of the 864 persons treated experienced some adverse reactions (21 with grade 1 and 12 with grade 2). Of the 33 with reactions, 29 were among the 122 (23.8%) mf carriers and 4 among the 831 (0.5%) non-microfilaraemic persons. Six months later, 123 (21.1%) of 584 inhabitants sampled were microfilaraemic: the GMM count for the whole group was 106 mf/ml (1-8177), with 29 mf/ml (1-3740) in 35 female and 177 mf/ml (1-8177) in 88 male carriers. Of these 123, 15 (whose GMM count was 4.5 mf/ml; range 1-204) were amicrofilaraemic 6 months before, and 19 had a microfilaraemia level higher than that 6 months earlier, before treatment. 117 of the 122 carriers identified in April were resampled: comparison of their GMM counts before and 6 months after mass treatment indicated that treatment with a single dose of 100 micrograms/kg ivermectin resulted in a reduction of microfilaraemia by 69%.

Adolescent↗