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Research ArticleArticle

Metabolism of3H/14C-Labeled 4"-Deoxy-4"-epimethylaminoavermectin B1aBenzoate in Chickens

Identification of Novel Fatty Acid Conjugates of 4"-Deoxy-4"-epimethylaminoavermectin B1a

Christopher L. Wrzesinski, Mohammad Mushtaq, Terry Faidley, Nelson Johnson, Byron Arison and Louis S. Crouch
Drug Metabolism and Disposition August 1998, 26 (8) 786-794;
Christopher L. Wrzesinski
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Mohammad Mushtaq
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Terry Faidley
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Nelson Johnson
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Byron Arison
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Identification of Novel Fatty Acid Conjugates of 4"-Deoxy-4"-epimethylaminoavermectin B1a

Abstract

The metabolism of3H/14C-labeled 4"-deoxy-4"-epimethylaminoavermectin B1a(MAB1a) benzoate, the major homologue (≥90%) of the avermectin insecticide emamectin benzoate, was studied in laying chickens. Ten Leghorn hens (Gallus domesticus) were orally dosed once daily for 7 days (1 mg/kg of body weight/day). Eggs and excreta were collected daily, and eggs were subsequently separated into whites and yolks. Chickens were euthanized within 20 hr after the last dose, and liver, kidney, heart, muscle, fat, ovaries, gizzard, gastrointestinal tract and contents, and carcass were collected. Approximately 70 and 6% of the total administered dose were recovered in the excreta plus gastrointestinal tract and contents and in the tissues plus eggs, respectively. Two novel metabolites, i.e. the 24-hydroxymethyl derivative of the parent compound (24-hydroxymethyl-4"-deoxy-4"-epimethylaminoavermectin B1a) and the N-demethylated derivative of 24-hydroxymethyl-4"-deoxy-4"-epimethylaminoavermectin B1a(24-hydroxymethyl-4"-deoxy-4"-epiaminoavermectin B1a), were identified. In addition, eight fatty acid conjugates of each of these two metabolites, comprising 8–75% of total radioactive residues in tissues and eggs, were isolated and identified. Although this represents some of the most extensivein vivo fatty acid conjugation to a xenobiotic reported to date, potential human exposure to MAB1a residues from consumption of chicken would be extremely low, because the dosage level in this study was ∼1000-fold greater than the MAB1a residue levels seen in crops and because the majority of the applied dose was recovered in the excreta. Based on these findings, the avian biotransformation of MAB1a differs substantially from the mammalian biotransformation.

Footnotes

  • Send reprint requests to: Christopher L. Wrzesinski, Schering-Plough Research Institute, P.O. Box 32, Lafayette, NJ 07848.

  • ↵1 Current address: Drug Safety & Metabolism-Animal Health, Schering-Plough Research Institute, P.O. Box 32, Lafayette, NJ 07848.

  • Abbreviations used are::
    MAB1a
    4"-deoxy-4"-epimethylaminoavermectin B1a
    MAB1b
    4"-deoxy-4"-epimethylaminoavermectin B1b
    24-OH-AB1a
    24-hydroxymethyl-4"-deoxy-4"-epiaminoavermectin B1a
    24-OH-MAB1a
    24-hydroxymethyl-4"-deoxy-4"-epimethylaminoavermectin B1a
    AB1
    4"-deoxy-4"-epiaminoavermectin B1 (a mixture of B1a and B1b homologues)
    AB1a
    4"-deoxy-4"-epiaminoavermectin B1a
    GIT
    gastrointestinal tract and contents
    APCI
    atmospheric pressure chemical ionization
    LSC
    liquid scintillation counting
    SPE
    solid-phase extraction
    EtOAc
    ethyl acetate
    TRR
    total radioactive residue(s)
    • Received December 18, 1997.
    • Accepted April 23, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition
Vol. 26, Issue 8
1 Aug 1998
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Research ArticleArticle

Metabolism of3H/14C-Labeled 4"-Deoxy-4"-epimethylaminoavermectin B1aBenzoate in Chickens

Christopher L. Wrzesinski, Mohammad Mushtaq, Terry Faidley, Nelson Johnson, Byron Arison and Louis S. Crouch
Drug Metabolism and Disposition August 1, 1998, 26 (8) 786-794;

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Research ArticleArticle

Metabolism of3H/14C-Labeled 4"-Deoxy-4"-epimethylaminoavermectin B1aBenzoate in Chickens

Christopher L. Wrzesinski, Mohammad Mushtaq, Terry Faidley, Nelson Johnson, Byron Arison and Louis S. Crouch
Drug Metabolism and Disposition August 1, 1998, 26 (8) 786-794;
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