Tissue Distribution and Renal Excretion of Ormetoprim after Intravascular and Oral Administration in the Channel Catfish (Ictalurus punctatus)

Ormetoprim is used to potentiate sulfadimethoxine in treating certain bacterial diseases of aquatic species. The tissue disposition and renal excretion of ormetoprim and metabolites were examined after intravascular and oral administration (4 mg∙kg−1) in channel catfish (Ictalurus punctatus). Peak plasma level (0.66 μg∙mL−1) of 14C-ormetoprim occurred at 6 h after oral dosing. The oral bioavailability was estimated at 52%. Ormetoprim and metabolites were widely distributed in the tissues. The tissue concentrations were highest in the liver, trunk kidney, head kidney, and spleen. Clearance of the radiolabel from tissues was rapid. The muscle contained 49.3% of the intravascularly administered dose at 2 h; however, at 72 h, less than 1% of the dose remained in this tissue. 14C-Ormetoprim was more persistent in the skin than in the muscle. Ormetoprim was extensively metabolized in catfish. After intravascular administration, 21.1% of the dose of 14C-ormetoprim was eliminated in the urine in 48 h, predominantly as polar metabolites; less than 4% of the dose was eliminated as the parent compound. Biliary excretion was a minor route of elimination (5–6% of the dose). The data suggest branchial excretion of ormetoprim and/or metabolites.

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Clopidogrel

Fibrinolytic and Antithrombotic Therapy ◽

10.1093/oso/9780195155648.003.0013 ◽

2006 ◽

Author(s):

Richard C. Becker ◽

Frederick A. Spencer

Keyword(s):

Steady State ◽

Oral Dose ◽

Oral Administration ◽

Randomized Clinical Trials ◽

Peak Plasma ◽

Parent Compound ◽

Plasma Concentrations ◽

Significant Inhibition ◽

Inhibiting Effect ◽

Dependent Inhibition

Clopidogrel, a thienopyridine derivative, is a novel platelet antagonist that is several times more potent than ticlopidine but associated with fewer adverse effects. After repeated 75-mg oral doses of clopidogrel, plasma concentrations of the parent compound, which has no platelet-inhibiting effect, are very low. Clopidogrel is extensively metabolized in the liver. The main circulating metabolite is a carboxylic acid derivative with a plasma elimination half-life of 7.7 ± 2.3 hours. Approximately 50% of an oral dose is excreted in the urine and the remaining 50% in feces over the following 5 days. Dose-dependent inhibition of platelet aggregation is observed 2 hours after a single oral dose of clopidogrel, with a more significant inhibition achieved with loading doses (≥300 mg) by approximately 6 hours. Repeated doses of 75 mg of clopidogrel per day inhibit adenosine diphosphate (ADP)-mediated aggregation, with steady state being reached between day 3 and day 7. At steady state, the average inhibition to ADP is between 40% and 60%. Based on ex vivo studies, clopidogrel is approximately 100-fold more potent than ticlopidine. There are no cumulative antiplatelet effects with prolonged oral administration. The combined administration of clopidogrel (300 mg loading dose) and aspirin yields a readily discernible platelet-inhibiting effect within 90 to 120 minutes. Clopidogrel selectively inhibits the binding of ADP to its platelet receptor (P2Y12) and the subsequent G-protein–linked mobilization of intracellular calcium and activation of the glycoprotein (GP)IIb/IIIa complex (Gachet et al., 1992). The specific receptor has been cloned and is abundantly present on the platelet surface (Hollopter et al., 2001). Clopidogrel has no direct effect on cyclooxygenase, phosphodiesterase, or adenosine uptake. Clopidogrel is rapidly absorbed following oral administration with peak plasma levels of the predominant circulating metabolite occurring approximately 60 minutes later. Administration with meals does not significantly modify the bioavailability of clopidogrel. The available information suggests that clopidogrel offers safety advantages over ticlopidine, particularly with regard to bone marrow suppression and other hematologic abnormalities. Although thrombotic thrombocytopenic purpura (TTP) has been reported with clopidogrel (Bennett et al., 2000), its occurrence (11 cases per 3 million patients treated) is rare, and has not been reported in randomized clinical trials performed to date.

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Masculinization of Channel Catfish Ictalurus punctatus by Oral Administration of Trenbolone Acetate

Journal of the World Aquaculture Society ◽

10.1111/j.1749-7345.1995.tb00832.x ◽

1995 ◽

Vol 26 (4) ◽

pp. 378-383 ◽

Cited By ~ 19

Author(s):

John I. Galvez ◽

Patricia M. Mazik ◽

Ronald P. Phelps ◽

Donald R. Mulvaney

Keyword(s):

Oral Administration ◽

Ictalurus Punctatus ◽

Channel Catfish ◽

Trenbolone Acetate

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Yeast cell walls stimulate viability, respiratory burst, and phagocytosis in channel catfish (Ictalurus punctatus) head-kidney macrophages

Aquaculture International ◽

10.1007/s10499-019-00417-y ◽

2019 ◽

Vol 27 (6) ◽

pp. 1655-1665

Author(s):

Jianjun Zhou ◽

Zhen Gao ◽

Wenbiao Wang ◽

Feng Huang ◽

Junpeng Hu ◽

...

Keyword(s):

Yeast Cell ◽

Ictalurus Punctatus ◽

Channel Catfish ◽

Respiratory Burst ◽

Cell Walls ◽

Head Kidney

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Isolated perfused Brockmann body as a model for studying pancreatic endocrine secretion

AJP Endocrinology and Metabolism ◽

10.1152/ajpendo.1982.243.5.e352 ◽

1982 ◽

Vol 243 (5) ◽

pp. E352-E359 ◽

Cited By ~ 3

Author(s):

P. Ronner ◽

A. Scarpa

Keyword(s):

Pancreatic Islet ◽

Ictalurus Punctatus ◽

Channel Catfish ◽

Glucose Concentration ◽

In Vitro Perfusion ◽

Morphological Criteria ◽

Endocrine Secretion ◽

A Minor ◽

Biphasic Release

The release of insulin, glucagon, and somatostatin was investigated in a newly developed in vitro perfusion preparation of the splenic Brockmann body (principal pancreatic islet) of the channel catfish (Ictalurus punctatus). The preparation was viable for up to 7 h by functional and morphological criteria. Glucose evoked a biphasic release of insulin and somatostatin, but had no effect on the release of glucagon. Arginine at basal glucose concentration caused a marked release of insulin and glucagon, but only a minor release of somatostatin.

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Absorption, Tissue Distribution and Elimination of 4-[3H]-Epigallocatechin Gallate in Beagle Dogs

International Journal of Toxicology ◽

10.1080/10915810305101 ◽

2003 ◽

Vol 22 (3) ◽

pp. 187-193 ◽

Cited By ~ 27

Author(s):

Robert R. Swezey ◽

Daphne E. Aldridge ◽

Susanna E. Le Valley ◽

James A. Crowell ◽

Yukihiko Hara ◽

...

Keyword(s):

Oral Administration ◽

Tissue Distribution ◽

Plasma Levels ◽

Half Life ◽

Peak Plasma ◽

Parent Compound ◽

Epigallocatechin Gallate ◽

Total Radioactivity ◽

Repeat Dose ◽

Beagle Dogs

Polyphenols found in tea are potent antioxidants and have inhibitory activity against tumorigenicity. The purpose of the described study was to assess the absorption, tissue distribution, and elimination of epigallocatechin gallate (EGCG), the principal catechin found in green tea, in a nonrodent species. 4-[3H]-EGCG was administered to beagle dogs by intravenous (IV) and oral routes. Following IV administration of 25 mg/kg, radioactivity in the bloodstream resided predominantly in the plasma. Distribution occurred during the first hour, and the plasma levels of total radioactivity declined with a mean half-life of approximately 7 hours. The apparent volume of distribution (0.65 l/kg) indicated wide distribution, and the total body clearance (1.01 ml/min-kg) was low. A subsequent single oral dose (250 mg/kg) was rapidly absorbed, with peak plasma levels at about 1 hour after administration, followed by elimination with a mean half-life of 8.61 hours. The mean area under the curve (AUC) for total radioactivity was approximately 20% of the value following IV administration (corrected for dose administered). Excretion of radioactivity in the feces predominated over urinary excretion following both IV and oral administration of [3H]-EGCG. Tissue distribution was determined 1 hour after an IV dose (25 mg/kg) administered after 27 days of oral treatment with EGCG (250 mg/kg/day) to mimic chronic consumption of tea. Radioactivity was distributed to a variety of epithelial tissues; the highest concentrations were observed in the liver and gastrointestinal tract tissues. Repeat dose oral administration of EGCG resulted in significantly lower blood radioactivity compared to the concentration following a single dose. These results are generally in accord with previous studies in rodents and indicate that, after oral administration, EGCG (as parent compound and metabolites) is widely distributed to tissues where it can exert a chemopreventive effect.

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Absorption of Selected Antimicrobic Drugs from Water by Channel Catfish, Ictalurus punctatus

Canadian Journal of Fisheries and Aquatic Sciences ◽

10.1139/f81-135 ◽

1981 ◽

Vol 38 (8) ◽

pp. 993-996 ◽

Cited By ~ 9

Author(s):

Kenneth E. Nusbaum ◽

Emmett B. Shotts jr.

Keyword(s):

Ictalurus Punctatus ◽

Channel Catfish ◽

Spore Germination ◽

Germination Inhibition ◽

Bacterial Diseases ◽

Minimum Inhibitory Concentrations ◽

Carrier Free ◽

Bacillus Subtilus ◽

Antibiotic Degradation

Although anitmicrobial drugs are frequently added to water to treat bacterial diseases of fish, their absorption is largely unquantified. Channel catfish weighing 3–5 g each were exposed to varying concentrations (4 mg/L to 32 mg/L) of chloramphenicol, erythromycin, furpyrinol, and oxytetracycline, respectively. Antibiotic levels measured after 5 h utilizing Bacillus subtilus spore germination inhibition showed that furpyrinol and oxytetracycline were absorbed by the fish in proportion to the antimicrobial concentration in the water. Minimum inhibitory concentrations can be attained in the fish with practical concentrations of these drugs in the water. Erythromycin (carrier-free) was poorly absorbed and chloramphenicol was not absorbed. Significant antibiotic degradation in water occurred in all drugs except furpyrinol.Key words: fish, antimicrobic, chloramphenicol, erythromycin, furance, oxytetracycline

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Oral Administration of Carbon-14 Labeled Cyanocobalamin (14C-Cbl) Reveals Variable Degradation of Vitamin B12 in the Gastrointestinal Tract That Impacts Vitamin B12 Absorption and Status.

Blood ◽

10.1182/blood.v114.22.3018.3018 ◽

2009 ◽

Vol 114 (22) ◽

pp. 3018-3018

Author(s):

Ralph Green ◽

Joshua W Miller ◽

Kyung-Seon Lee ◽

Syrukh Sutter ◽

Lindsay H Allen ◽

...

Keyword(s):

Gastrointestinal Tract ◽

Plasma Level ◽

Oral Administration ◽

Urinary Excretion ◽

Vitamin B12 ◽

Research Funding ◽

Peak Plasma ◽

Science Research ◽

Fecal Excretion ◽

Peak Plasma Level

Abstract Abstract 3018 Poster Board II-994 Recent evidence from our laboratory and others suggests that a variable portion of ingested cobalamin (Cbl), either crystalline or from food, is degraded in the gastrointestinal tract. We have developed a biosynthetic method to incorporate 14C into the lower axial ligand of cobalamin that has made it possible to study the fate of this vitamin during its passage through the gastrointestinal tract and to assess the presence of Cbl or its breakdown products in biological samples. Following oral administration of an aqueous physiological tracer dose of 14C-Cbl (1.3 μg, 50 nCi), blood, urine, and feces are analyzed for 14C by accelerator mass spectrometry. In 9 subjects, the plasma response was consistent with the expected behavior of peroral Cbl: 14C-Cbl first appeared in the plasma 3h post-dose reaching a peak level within 6-8h. Confirmation that this dose appears bound to the physiological transport protein transcobalamin (TC) was obtained in a subset of subjects by an immunoaffinity method using anti-human TC antibody-coated magnetic beads which selectively bound 95-98% of plasma 14C. Urinary excretion of 14C was maximal in the first 24h, with 14C first appearing in urine as early as 1.5h after dosing. Fecal excretion occurred variably over several days. The amount of 14C found in the urine (10-50% of the dose) was 100-fold greater than in previous reports using 57Co-labeled cyanocobalamin (0.1-0.5%), and fecal excretion was lower than expected (10-20% vs 30-70%). Urinary excretion of 14C was inversely correlated with the peak plasma level of 14C attained (r2=0.610; p<0.001). The bulk of urinary 14C was not associated with intact Cbl and first appeared in the urine before peak 14C levels were attained in the plasma. The peak plasma level of 14C attained also showed a strong positive correlation with plasma holotranscobalamin concentration measured before administration of the 14C-Cbl (r2=0.571; p<0.001). No such correlation was found with total plasma Cbl. In additional experiments on normal volunteers using eggs endogenously labeled with 14C Cbl following intramuscular injection of hens with 14C Cbl, comparably high urinary excretion of 14C was also observed. We conclude that a variable fraction of ingested Cbl is degraded in the gastrointestinal tract of normal individuals. This may be an important determinant of the amount of Cbl absorbed from food or supplement sources. Additionally, our findings suggest that the concentration of holoTC in the plasma reflects absorptive capacity and may therefore be a good surrogate for Cbl absorptive status. Our findings also have implications regarding the bioavailability of Cbl and may inform pending considerations to fortify food supplies with Cbl in order to mitigate the incidence of Cbl deficiency, particularly among the elderly. Intestinal degradation, either microbial or through the action of digestive enzymes, may also be a source of Cbl analogues that have previously been detected in the plasma and tissues. Cbl analogues may interfere with the physiological function of cobalamin, resulting in some of the manifestations of cobalamin deficiency. Disclosures: Green: Vitalea Science: Research Funding. Miller:Vitalea Science: Research Funding. Lee:Vitalea Science: Research Funding. Sutter:Vitalea Science: Research Funding. Allen:Vitalea Science: Research Funding. Dueker:Vitalea Science: Employment.

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Pharmacokinetics and Tissue Distribution of Aegeline after Oral Administration in Mice

Planta Medica ◽

10.1055/a-0851-6879 ◽

2019 ◽

Vol 85 (06) ◽

pp. 491-495

Author(s):

Vamshi Manda ◽

Mona Haron ◽

Tahir Mir ◽

Bharathi Avula ◽

Mohammad Ashfaq ◽

...

Keyword(s):

Oral Administration ◽

Tissue Distribution ◽

Half Life ◽

Therapeutic Potential ◽

Peak Plasma ◽

Biologically Active ◽

Active Constituent ◽

Peak Plasma Level ◽

Tissue Samples ◽

Obesity And Diabetes

AbstractAegeline is claimed to be a biologically active constituent of Aegle marmelos. Preclinical studies have reported possible therapeutic potential for aegeline against obesity and diabetes. In recent years, aegeline has been added to several weight loss products. However, the consumption of aegeline-containing supplements such as OxyELITE Pro and VERSA-1 has been linked to multiple cases of acute and chronic liver failure. This study was carried out to evaluate the pharmacokinetics and tissue distribution of aegeline in ND4 mice. Two doses of aegeline, a human equivalent dose (1×) 30 mg/kg and a 10× dose (300 mg/kg), were orally administered to the mice, and blood and tissue samples were collected over 8 h. The quantitative analysis of plasma and tissue homogenates (liver, kidney, and brain) was done by UHPLC-QTOF to determine aegeline concentrations. The peak plasma level of aegeline was achieved at a Tmax of 0.5 h, indicating its rapid absorption from the gastrointestinal tract. Aegeline was not detected in the plasma at 8 h after oral administration, with a half-life of 1.4 ± 0.01 and 1.3 ± 0.07 h for the 30 and 300 mg/kg doses, respectively. The half-life of aegeline in the liver was 1.2 h and 1.7 h for 30 and 300 mg/kg doses, respectively, with a Tmax of 1.9 h, which indicates relatively fast elimination of aegeline from the liver.

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