Animal Metabolism

ADME (absorption, distribution, metabolism and elimination) studies in rats indicate spinosad and spinetoram are rapidly absorbed, extensively distributed among tissues and extensively metabolized. Highest spinetoram concentrations were found in the gastrointestinal tract, fat, carcass and liver.130 For spinosad, key tissues were perirenal fat, liver, kidneys and thyroid.103,127 Fecal excretion was the major route of elimination, while urine was a minor route. Rat metabolism studies for spinosad showed no major differences between the bioavailability, routes or rates of excretion, or metabolism of spinosyn A or spinosyn D. Low (<2%) dermal absorption has been documented for spinosad.103

For both spinosad and spinetoram, the primary metabolic pathway in rats was glutathione conjugation, either the parent molecules, or the products of N-demethylation or O-dealkylation; cysteine conjugation was noted as well.103,130

For spinetoram, deglycosylation of each parent factor, as well as hydroxylation of parent XDE-175-J, was also noted, and the aglycone of XDE-175-L was subject to sulfate and glucuronide conjugation.130 Livestock metabolism studies conducted with 14C-labeled materials confirmed that overall dealkylation is a primary component of the metabolic pathway for both spinosad and spin-etoram in animals. O-dealkylation in the 2',3',4'-tri-O-methyl rhamnose and demethylation in the forosamine were observed for both molecules in the goat and hen. In addition, hydroxylation of the macrolide ring was noted for spinosad in goats and in hens, more extensive metabolism and eventual loss of the forosamine sugar was noted. For spinetoram and spinosad, unchanged parent compound was the primary residue component in milk, eggs and animal tissues, which is a consideration for potential human consumption. Generalized animal metabolism pathways are shown in Figures 5.5 and 5.6, with metabolites that could arise from rats, hens and/or goats. Pathways include both major (> 10%) and minor compounds as well as both tentative and confirmed structures.

Macroiide Hydroxyiation of [5.1] and [5.24] (Animal)

Oxidation to N-formyl-spinosyn A [5.32] (Plant)

N-deaikyiation to spinosyn B [5.24] (Plant, Animal)

Forosamine ioss to C17 PsAgly of spinosyn A [5.34] (Animal)

O-deaikyiation of[5.34] (Animal)

Nonextractable residues

(Animal)

Spinosyn A [5.1] Active Ingredient

Nonextractable residues

(Animal)

O-deaikyiation to spinosyn K [5.27], spinosyn J [5.3] (Animal)

O-dealkylation to spinosyn M [5.26],

W-desmethyl-spinosyn K [5.28], and/or related analogs (Animal)

O-dealkylation to

W-desmethyl -spinosyn P [5.30] and/or related analogs (Animal)

Photoproducts with 2 or 4 added oxygen atoms (Plant)

Polar residues and plant incorporated residues (Plant)

O-deaikyiation to spinosyn H [5.25] (Plant, Animal)

O-deaikyiation to spinosyn H [5.25] (Plant, Animal)

Glutathione and cysteine conjugates (Animal)

Figure 5.5 General plant and animal metabolism pathways for spinosyn A, the major component of spinosad. (Plant = representative crops [apple, lettuce, and turnip]; Animal = rat or hen, there was minimal metabolism in goat). See Figures 5.2 and 5.7 for structures.

Lantern Cut Out Template
Figure 5.6 General plant and animal metabolism pathways for XDE-175-J, the major component of spinetoram. (Plant = representative crops [apple, lettuce, and turnip]; Animal = rat or hen, there was minimal metabolism in goat). See Figures 5.2 and 5.7 for structures.
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