Metabolism of Thioamide Antithyroid Drugs

Sitar, Daniel S.

doi:10.3109/03602539008991448

Cited by 3 publications

(2 citation statements)

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“…While other thionamide drugs are traditionally administered in several daily doses to achieve sustained antithyroid effect, only a single dose of MTZ is necessary to achieve the same pharmacological effect (Roti et al, 1989). High bioavailability (Jansson et al, 1985) and extensive tissue distribution (Sitar, 1990) may ensure that a single dose of MTZ will result in successful inhibition of liver ABZ sulphpxidation. The route of administration did not influence MTZ-induced changes in the pharmacokinetics of NTB metabolites, which may indicate similar MTZ absorption and bioavailability from both oral and i.m.…”

Section: Discussionmentioning

confidence: 99%

Methimazole‐mediated modulation of netobimin biotransformation in sheep: a pharmacokinetic assessment

Lanusse

Gascon

Prichard

1992

Vet Pharm & Therapeutics

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The effects of modulation of liver microsomal sulphoxidation on the disposition kinetics of netobimin (NTB) metabolites were investigated in sheep. A zwitterion suspension of NTB was given orally at 7.5 mg/kg to sheep either alone (control treatment) or co-administered with methimazole (MTZ) orally (NTB + MTZ oral treatment) or intra-muscularly (NTB + MTZ i.m.) at 3 mg/kg. Blood samples were taken serially over a 72 h period and plasma was analysed by HPLC for NTB and its major metabolites, i.e. albendazole (ABZ), albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO2). Only trace amounts of NTB parent drug and ABZ were detected in the earliest samples after either treatment. There were significant modifications to the disposition kinetics of ABZSO in the presence of MTZ. ABZSO elimination half-life increased from 7.27 h (control treatment) to 14.57 h (NTB + MTZ oral) and to 11.39 h (NTB + MTZ i.m.). ABZSO AUCs were significantly higher (P less than 0.05) for the NTB + MTZ oral treatment (+55%) and for the NTB + MTZ i.m. treatment (+61%), compared with the NTB alone treatment. The mean residence times for ABZSO were 12.66 +/- 0.68 h (control treatment), 18.85 +/- 2.35 h (NTB + MTZ oral) and 17.02 +/- 0.90 h (NTB + MTZ i.m.). There were no major changes in the overall pharmacokinetics of ABZSO2 for the concomitant MTZ treatments. However, delayed appearance of this metabolite in the plasma resulted in longer ABZSO2 lag times and a delayed Tmax for treatments with MTZ.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionmentioning

confidence: 99%

Methimazole‐mediated modulation of netobimin biotransformation in sheep: a pharmacokinetic assessment

Lanusse

Gascon

Prichard

1992

Vet Pharm & Therapeutics

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“…3 Thioamides are found in many natural compounds 4 and play an important role in regulating metabolic pathways. 1 a ,5 They also serve as valuable synthetic building blocks in the synthesis of useful organic molecules. 6 The classical routes to synthesize thioamides involve thionation with phosphorus pentasulfide/Lawesson's reagent and the Willgerodt–Kindler reaction.…”

Section: Introductionmentioning

confidence: 99%

Dithiocarbamate-mediated thioamidation of arylglyoxylic acids by decarboxylative–decarbonylative C–C bond formation reactions

Patra

Saha

2023

Org. Chem. Front.

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Doubling Förster Resonance Energy Transfer Efficiency in Proteins with Extrinsic Thioamide Probes: Implications for Thiomodified Nucleobases

Jena

Tulsiyan

Kar

et al. 2021

Chemistry A European J

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Designing a potential protein–ligand pair is pivotal, not only to track the protein structure dynamics, but also to assist in an atomistic understanding of drug delivery. Herein, the potential of a small model thioamide probe being used to study albumin proteins is reported. By monitoring the Förster resonance energy transfer (FRET) dynamics with the help of fluorescence spectroscopic techniques, a twofold enhancement in the FRET efficiency of 2‐thiopyridone (2TPY), relative to that of its amide analogue, is observed. Molecular dynamics simulations depict the relative position of the free energy minimum to be quite stable in the case of 2TPY through noncovalent interactions with sulfur, which help to enhance the FRET efficiency. Finally, its application is shown by pairing thiouracils with protein. It is found that the site‐selective sulfur atom substitution approach and noncovalent interactions with sulfur can substantially enhance the FRET efficiency, which could be a potential avenue to explore in the design of FRET probes to study the structure and dynamics of biomolecules.

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Metabolism of Thioamide Antithyroid Drugs

Cited by 3 publications

References 83 publications

Methimazole‐mediated modulation of netobimin biotransformation in sheep: a pharmacokinetic assessment

Methimazole‐mediated modulation of netobimin biotransformation in sheep: a pharmacokinetic assessment

Dithiocarbamate-mediated thioamidation of arylglyoxylic acids by decarboxylative–decarbonylative C–C bond formation reactions

Doubling Förster Resonance Energy Transfer Efficiency in Proteins with Extrinsic Thioamide Probes: Implications for Thiomodified Nucleobases

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