Oxidation and acetylation of sulfamonomethoxine by the snail Cepaea hortensis.

Tb, Vree; Ml, Vree; Ew, Beneken Kolmer; Ya, Hekster; Shimoda, Minoru; Jf, Nouws; Yoshioka, Takayuki; Hoji, Kazuhiko

doi:10.1292/jvms1939.51.369

The Japanese Journal of Veterinary Science

1989

DOI: 10.1292/jvms1939.51.369

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Oxidation and acetylation of sulfamonomethoxine by the snail Cepaea hortensis.

Vree Tb¹,

Vree Ml²,

Beneken Kolmer Ew³

et al.

Abstract: Sulfamonomethoxine is not O-demethylated in the snail Cepaea hortensis, but acetylated (15.2%) and oxidised (0.78%) at the 2 position of the pyrimidine nucleus.

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Pharmacokinetics and acetylation of sulfa‐2‐monomethoxine in humans

Vree

Kolmer

Shimoda

et al. 1992

Biopharm & Drug Disp

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In humans sulfa-2-monomethoxine (S) is metabolized by N4-acetylation (39.9 +/- 8.0 per cent). After an oral dose, S is eliminated biphasically (t1/2, 5.2 +/- 1.6 h and 13.2 +/- 3.4 h) which is similar in both fast and slow acetylators. The metabolite N4-acetylsulfa-2-monomethoxine (N4) is eliminated monophasically (t1/2, 30.0 +/- 5.7 h). The intrinsic mean residence time (MRT) of N4 is 33.5 +/- 8.8 h. The mean total body clearance of S is 11.6 +/- 2.7 ml min-1, and the Vdss is 12.3 +/- 1.01. The renal clearance of S during the first day was twice as high as on the following days for two of the six volunteers (8 vs 4 ml min-1). The renal clearance of N4 during the first day, for four out of the six volunteers, was twice as high as on the following days (8 vs 4 ml min-1). The protein binding of S is 95 per cent and that of its conjugate N4 98 per cent. Approximately 80 per cent of the oral dose of S is excreted in the urine as parent drug (41.0 +/- 6.2 per cent) and as N4 acetyl conjugate (39.9 +/- 8.0 per cent).

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Pharmacokinetics and acetylation of sulfa‐2‐monomethoxine in humans

Vree

Kolmer

Shimoda

et al. 1992

Biopharm & Drug Disp

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Hepatic Biotransformation Profiles of Sulphamonomethoxine in Food-Producing Animals and Rats in Vitro

Furusawa

2000

Acta Veterinaria Hungarica

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Hydroxylation and acetylation of sulphamonomethoxine (SMM) and deacetylation of N4-acetyl SMM (N4-AcSMM) were estimated in liver post-mitochondrial supernatants (S-9) from laying hens, female cattle, swine and rats. The formation of hydroxylated SMM, 2,6-dihydroxy SMM (2,6-diOH-SMM), was found only with hen S-9s. N4-acetylation rate of SMM was the highest in pig S-9s, followed by rat, then hen or cow S-9s. All S-9s from the four species deacetylated N4-AcSMM. In hen S-9s, the rate of 2,6-dihydroxylation was higher during incubation at 41 °C than at 37 °C.

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Oxidation and acetylation of sulfamonomethoxine by the snail Cepaea hortensis.

Abstract: Sulfamonomethoxine is not O-demethylated in the snail Cepaea hortensis, but acetylated (15.2%) and oxidised (0.78%) at the 2 position of the pyrimidine nucleus.

Cited by 2 publications

References 0 publications

Pharmacokinetics and acetylation of sulfa‐2‐monomethoxine in humans

Pharmacokinetics and acetylation of sulfa‐2‐monomethoxine in humans

Hepatic Biotransformation Profiles of Sulphamonomethoxine in Food-Producing Animals and Rats in Vitro

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