Chemistry, pharmacology and safety of the macrocyclic lactones: ivermectin, abamectin and eprinomectin.

Shoop, Wesley L.; Soll, M. D.

doi:10.1079/9780851996172.0001

Cited by 34 publications

(30 citation statements)

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“…Despite of this, some differences have been observed in the efficacy of these compounds. Ivermectin is considered to be better than abamectin against arthropods, while the anthelmintic efficacy of abamectin has been shown to be greater than that of ivermectin (Shoop & Soll, 2002). Although the existence of side resistance between macrocyclic lactones has been reported by several authors (Conder et al.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of a new long acting endectocide formulation containing 2.25% ivermectin and 1.25% abamectin in cattle

Borges

Cho

Santos

et al. 2007

Vet Pharm & Therapeutics

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of a new long acting endectocide formulation containing 2.25% ivermectin and 1.25% abamectin in cattle. J. vet. Pharmacol. Therap. 30, 62-67.The objective of this study was to determine the kinetic parameters of a new formulation that contained 2.25% ivermectin combined with 1.25% abamectin in bovine plasma. The results for 2.25% ivermectin: C max (37.11 ng/ mL ± 7.42), T max (16 days ± 5.29), T 1/2 (44.62 days ± 53.89), AUC (928.2 ngAEday/mL ± 153.83) and MRT (36.73 days ± 33.64), and for 1.25% abamectin: C max (28.70 ng/mL ± 9.54), T max (14 days ± 4.04), T 1/2 (15.40 days ± 11.43), AUC (618.05 ngAEday/mL ± 80.27) and MRT (20.79 days ± 8.43) suggest that this combination of 2.25% ivermectin + 1.25% abamectin possesses properties that give this pharmaceutical formula a longer activity time than two of the commercial products tested (1% ivermectin and 1% abamectin), and showed similarity to 3.15% ivermectin.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of a new long acting endectocide formulation containing 2.25% ivermectin and 1.25% abamectin in cattle

Borges

Cho

Santos

et al. 2007

Vet Pharm & Therapeutics

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“…2 mg/kg single oral dose in primates). [115][116] At lower doses, toxicity is observed in animals that lack a functional P-glycoprotein, which allows the drug to accumulate in the nervous system. 117 The role of Pglycoprotein in Loa loa-infected subjects with serious adverse reactions after ivermectin treatment has been investigated.…”

Section: Parasitesmentioning

confidence: 99%

“…117 The role of Pglycoprotein in Loa loa-infected subjects with serious adverse reactions after ivermectin treatment has been investigated. [116][117][118][119][120][121][122] There is also evidence of developmental neurotoxicity (decreased body weight gain, delayed development, intermittent head and whole-body tremors, hind limb extension and then splay) in the F1 offspring of pregnant Sprague Dawley rats treated under controlled conditions with enamectin benzoate, another avermectin pesticide. 123 Whereas the F0 females showed no abnormal physical signs or deficits in reproductive performance when treated by oral gavage with 0.1-3.6 mg/kg once daily from gestation day 6 to lactation day 20, some pups delivered from the high-dose group developed intermittent head tremors beginning on post-natal day 6 (PND-6).…”

Section: Parasitesmentioning

confidence: 99%

Nodding syndrome in Mundri county, South Sudan: Environmental, nutritional and infectious factors

Spencer¹,

Vandemaele

Richer³

et al. 2013

Afr H. Sci.

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Background: Nodding Syndrome is a seizure disorder of children in Mundri County, Western Equatoria, South Sudan. The disorder is reported to be spreading in South Sudan and northern Uganda. Results: Nodding Syndrome was associated with Onchocerca volvulus and Mansonella perstans infections, with food use of a variety of sorghum (serena) introduced as part of an emergency relief program, and was inversely associated with a history of measles infection. There was no evidence to suggest exposure to a manmade neurotoxic pollutant or chemical agent, other than chemically dressed seed intended for planting but used for food. Food use of cyanogenic plants was documented, and exposure to fungal contaminants could not be excluded. Conclusion: Nodding Syndrome in South Sudan has an unknown etiology. Further research is recommended on the association of Nodding Syndrome with onchocerciasis/mansonelliasis and neurotoxins in plant materials used for food.

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“…The noticeable loss in concentration observed for ABM in DMF (apparent pH~9) was similar to aqueous alkaline hydrolysis, where AVMs are known to degrade fast with the formation of the 2-epi isomer and D2,3-ABM isomer as major impurities (10). Degradation of ABM in EL and DGBE (pH 3.0 and 4.2 after stress at 70°C) was expected to follow the known acidic hydrolysis behavior, which leads to the formation of monosaccharide and aglycone in trace amounts (9). In contrast, irrespective of the marked loss of ABM concentration, there were no corresponding major impurity peaks in the chromatograms of these two preparations.…”

Section: Effect Of Heat On the Degradation Profile Of Abm In Differenmentioning

confidence: 80%

“…Their exposure to mild acidic conditions leads to glycolysis, resulting in monosaccharide and aglycone derivatives (9). In contrast, alkaline hydrolysis results in epimerization to stereoisomer and regioisomer (2-epi-and D2,3-AVM) (10)(11)(12).…”

mentioning

confidence: 99%

Evaluation of degradation kinetics for abamectin in formulations using a stability indicating method

Awasthi¹,

Razzak²,

Al‐Kassas³

et al. 2013

Acta Pharmaceutica

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The aim of this study was to evaluate stability characteristics and kinetics behavior of abamectin (ABM) as a 1 % (m/V) topical veterinary solution. During the study, samples stressed at 55 and 70 °C were regularly analyzed for several parameters over 8 weeks on a chromatographic (HPLC) system, using a Prodigy C18, 250 x 4.6 mm, 5-μm, column eluting with 15 : 34 : 51 (V/V/V) water/methanol/ acetonitrile as mobile phase. The HPLC method was validated for precision, accuracy, linearity and specificity, and was found to be stability indicating. The results showed that degradation of ABM followed first-order kinetics and data on loss in kobs (s-1) and half life (t1/2, days) demonstrated ABM showing the maximum stability in glycerol formal. The degradation behavior of ABM varies from solvent to solvent. The effect of added alkali on pH change and loss of ABM was studied and found to be unique for all solvents and very distinct from typical hydrolysis degradation. The present study may serve as a platform to design and develop topical non-aqueous solutions of ABM for veterinary use given no such comprehensive efforts have been published to date on the stability profile of ABM in non-aqueous solvents.

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Chemistry, pharmacology and safety of the macrocyclic lactones: ivermectin, abamectin and eprinomectin.

Cited by 34 publications

References 0 publications

Pharmacokinetics of a new long acting endectocide formulation containing 2.25% ivermectin and 1.25% abamectin in cattle

Pharmacokinetics of a new long acting endectocide formulation containing 2.25% ivermectin and 1.25% abamectin in cattle

Nodding syndrome in Mundri county, South Sudan: Environmental, nutritional and infectious factors

Evaluation of degradation kinetics for abamectin in formulations using a stability indicating method

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