Role of Deacetylation in the Nonlinear Pharmacokinetics of Sulfamonomethoxine in Pigs
スポンサーリンク
概要
- 論文の詳細を見る
The role of deacetylation in the pharmacokinetics of sulfamonomethoxine (SMM) in pigs was studied using 6 Goettingen minipigs and a pig from a commercial breed. The rapid decrease of plasma concentration of the parent compound followed by the rapid increase of plasma concentration of the deacetylated metabolite, SMM, was observed after an i.v. injection of N^4-acetylsulfamonomethoxine (AcSMM ; 10mg/kg). The concentration of the metabolite, SMM, was greater than that of AcSMM and after reaching peak, both compounds decreased in parallel on a semilogarithmic graph. On the other hand, the acetylated compound of SMM (AcSMM) appeared in the plasma and reached peak after an i.v. injection of SMM. After reaching the peak, both SMM and AcSMM decreased in parallel. The slopes of the terminal phases of SMM and AcSMM after both injections showed no significant difference. After the i.v. injection of a high dose of SMM (100mg/kg), a nonlinear pharmacokinetics profile with capacity limited elimination type of SMM was observed. The concentration of plasma AcSMM increased rapidly and the parallel decrease of SMM and AcSMM was observed in both nonlinear and linear phases, while the renal excretion of AcSMM was saturated in the nonlinear phase. The results suggest that the deacetylation in pigs is so strong that it largely affected the pharmacokinetics of SMM in both high and low doses. In spite of the saturation in renal excretion of the main metabolite, AcSMM, after the high dose, the profile of the parallel decrease remained unchanged, which may be due to the rapid conversion of the excess AcSMM to SMM. The converted SMM was added to the existing plasma SMM. As a result, the nonlinear pharmacokinetics of SMM may have occurred after a high dose of SMM in pigs.
- 公益社団法人日本薬学会の論文
著者
-
SHIMIZU Takao
Department of Biochemistry and Molecular Biology, Faculty of Medicine, The University of Tokyo
-
Kokue Eiichi
Labo. Of Veterinary Pharmacol. Fac. Of Agriculture Tokyo Univ. Of Agriculture And Technology
-
Kokue Eiichi
Department Of Veterinary Medicine Tokyo University Of Agriculture And Technology
-
Hayama T
Tokyo Univ. Agriculture And Technology Tokyo Jpn
-
Hayama Toyoaki
Laboratory Of Veterinary Pharmacology Faculty Of Agriculture Tokyo University Of Agriculture And Tec
-
Hayama Toyoaki
Department Of Veterinary Medicine Faculty Of Agriculture Tokyo University Of Agriculture And Technol
-
Shimoda Minoru
Laboratory Of Veterinary Pharmacology Faculty Of Agriculture Tokyo University Of Agriculture And Tec
-
Shimoda Minoru
Department Of Veterinary Medicine Faculty Of Agriculture Tokyo University Of Agriculture And Technol
-
SHIMIZU Tadayori
University of Shizuoka, School of Pharmaceutical Sciences
-
MURAOKA Ryouichi
Department of Veterinary Medicine, Faculty of Agriculture, Tokyo University of Agriculture and Techn
-
Shimizu Takao
Department Of Biochemistry And Molecular Biology Faculty Of Medicine The University Of Tokyo
-
Shimizu Takao
Department Of Veterinary Medicine Faculty Of Agriculture Tokyo University Of Agriculture And Technol
-
Muraoka Ryouichi
Department Of Veterinary Medicine Faculty Of Agriculture Tokyo University Of Agriculture And Technol
関連論文
- Inhibition of Cytosolic Phospholipase A_2 Suppresses Production of Cholesteryl Ester through the Reesterification of Free Cholesterol but not Formation of Foam Cells in Oxidized LDL-Stimulated Macrophages(Highlighted paper selected by Editor-in-chief,Bioc
- Effects of Several Pyrethroids on Hepatic Cytochrome P450 Activities in Rats
- Singlet Oxygen Production and Photobiological Effects of Pinacyanol Chloride on Yeast Saccharomyces cerevisiae
- Focused lipidomics by tandem mass spectrometry
- Specific Detection of Lysophosphatidic Acids in Serum Extracts by Tandem Mass Spectrometry
- Prognostic significance of second-look laparotomy for surgically confirmed early-stage epithelial ovarian cancer : a multicenter retrospective study
- Characteristic Upregulation of Dopamine D_1-Receptor in Rat Striatum after 6-Hydroxydopamine Treatment
- Platelet-Activating Factor Receptor
- Inhibitory Effects of Ketoconazole, Cimetidine and Erythromycin on Hepatic CYP3A Activities in Cats
- Arachidonic Acid Metabolites Inhibit the Stimulatory Effect of Angiotensin II in Renal Proximal Tubules
- Rapid and Sensitive PCR Detection of Vibrio trachuri Pathogenic to Japanese Horse Mackerel ( Trachurus japonicus )
- Vibrio trachuri Sp. Nov., a New Species Isolated from Diseased Japanese Horse Mackerel
- The Majority of Lymphocytes in the Bone Marrow, Thymus and Extrathymic T Cells in the Liver Are Generated In Situ from Their Own Preexisting Precursors
- CONTRIBUTION OF RENAL ACTIVE SECRETION IN RENAL EXCRETION OF N^4-ACETYLSULFAMONOMETHOXINE IN CONSCIOUS PIGS
- Cross-Antigenicity between Penams and Cephems by Intradermal Skin Test and Leucocyte Migration Test in Guinea Pigs
- Antitumor Activity, Mitogenicity, and Lethal Toxicity of Chemically Synthesized Monosaccharide Analogs of Lipid A
- Interactions of Human-and Rat-Organic Anion Transporters With Pravastatin and Cimetidine
- The alteration of CYP-dependent drug metabolism in experimental animals during acute phase response(WORKSHOP 4 : NEW TECHNOLOGY AND EVALUATIONS OF IN VIVO TOXICITY STUDIES)
- 22D-11-1 The Alteration of Drug Disposition in Rabbits during Acute Phase Response.
- Pharmacokinetics of Oral Sulfa Drugs and Gastric Emptying in the Pig
- Antibody-Producing Effects in Mice by Synthetic Immunoactive Lipopeptides with the Conjugated Amino Acid Sequence of gp120 in Human Immunodeficiency Virus
- Leukotriene Receptors : Classification, Gene Expression, and Signal Transduction
- Comparison of Dihydrofolate Reductase Activities for Folic Acid in Pigs and Rats Using In Vivo and In Vitro Evaluation Techniques
- Roles of nitric oxide as a vasodilator in neurovascular coupling of mouse somatosensory cortex
- Crystal Structure of Anti-Configuration of Indomethacin and Leukotriene B_4 12-Hydroxydehydrogenase/15-Oxo-Prostaglandin 13-Reductase Complex Reveals the Structural Basis of Broad Spectrum Indomethacin Efficacy
- SITE OF EMETIC ACTION OF ORAL COPPER SULFATE IN DOGS (II) IMPORTANCE OF LOWER DUODENUM
- Ameliorative Effect of Folic Acid on Pyrimethamine Teratogenesis in Pigs
- Digested Bacterial Cell Powder (DBCP) as a Source of Reduced-form Folates for Pigs : Use of a Trimethoprim-resistant Strain and the Bioavailability of Folates in DBCP
- Multiple gastrinoma successfully resected with the aid of intraoperative arterial secretin injection test
- Effects of Folic Acid and Pyrimethamine, a Dihydrofolate Reductase Inhibitor, on Intestinal Absorption of Folates in Rats
- POSSIBLE ACTIVE TUBULAR SECRETION OF SULFAMONOMETHOXINE AND ITS METABOLITES IN PIGS
- Global analysis of triacylglycerols including oxidized molecular species by reverse-phase high resolution LC/ESI-QTOF MS/MS
- S14 TOLERANCE OF AGROCHEMICALS IN FOOD
- Effects of Pyrimethamine and Folic Acid on Plasma Level of 5-Methyltetrahydrofolic Acid in Rats
- Effects of Folic Acid and Folinic Acid on Pyrimethamine Teratogenesis in Rats
- "P-7 Folic acid does not cure a toxicity of methotrexate.
- Separation and quantification of sn-1 and sn-2 fatty acid positional isomers in phosphatidylcholine by RPLC-ESIMS/MS
- Analysis of oxidized phosphatidylcholines as markers for oxidative stress, using multiple reaction monitoring with theoretically expanded data sets with reversed-phase liquid chromatography/tandem mass spectrometry
- Effective Extraction and Analysis for Lysophosphatidic Acids and Their Precursors in Human Plasma Using Electrospray Ionization Mass Spectrometry
- SITE OF EMETIC ACTION OF ORAL COPPER SULFATE IN DOGS (I) THRESHOLDS OF VARIOUS PORTIONS OF GASTROINTESTINAL TRACT TO LOCALLY APPLIED COPPER SULFATE
- Correlation of Active Folate Availability with Effects of Folic Acid on Pyrimethamine Teratogenesis in Rats
- Effect of Folic Acid on Pharmacokinetics of Pyrimethamine in Rats
- A-9 EFFECTS OF FOLIC ACID ON THE TERATOGENICITY OF PYRIMETHAMINE IN RATS
- Role of Deacetylation in the Nonlinear Pharmacokinetics of Sulfamonomethoxine in Pigs
- Changes in the Level of 7α-Hydroxy-3-oxo-4-cholestenoic Acid in Cerebrospinal Fluid after Subarachnoid Hemorrhage
- Regulatory Mechanism and Physiological Role of Cytosolic Phospholipase A_2(Diversity of Phospholipase A_2 Enzymes)
- ANTIULCEROGENIC PROPERTY OF SODIUM POLYACRYLATE ON EXPERIMENTAL ULCERATIONS IN RATS
- Effect of Echo-Guided High-Intensity Focused Ultrasound Ablation on Localized Experimental Tumors
- ニワトリの慢性膵臓瘻管の装着法(短報)〔英文〕
- SOME CHEMICAL AND PHARMACOLOGICAL PROPERTIES OF AN AMINE (MALTOXIN) ISOLATED FROM MALT ROOTLET
- Mechanisms of veratramine-induced 5-HT syndrome in mice.
- Dose-dependent pharmacokinetics of intravenous sulfamonomethoxine in pigs.
- Platelet-Activating Factor Receptor.