Inhibition of biliary excretion pdf
excretion and plasma exposure of TNP and TNP-G. Inhibition of the efflux transporters may affect the pharmacokinetics of TNP and result in a drug-drug interaction between TNP and the concomitant transporter inhibitor or inducer in clinic.
pdf. Inhibition of biliary bicarbonate secretion in ethinyl estradiol-induced cholestasis is not associated with impaired activity of the Cl −/HCO 3 − exchanger in the rat
How to Cite. Parasrampuria, R. and Mehvar, R. (2010), Dose-dependent inhibition of transporter-mediated hepatic uptake and biliary excretion of methotrexate by cyclosporine A in an isolated perfused rat liver model.
The biliary concentrations found in these subjects seem to be inferior to those required for the inhibition of the common bacteria of biliary infections. In renal failure, however, the biliary excretion of CIBA 36 278 Ba increased considerably.
Bilirubin is one of several organic anions that selectively inhibit the biliary secretion of phospholipid and cholesterol without affecting bile salt secretion. To determine the site of this inhibition and gain insight into its mechanism, normal, Sprague-Dawley and homozygous Gunn rats were infumsed with unconjugated bilirubin and a water
Effect of OATP-binding on the prediction of biliary excretion Mohsen Sharifi 1,2 , and Taravat Ghafourian 1,3 1 Medway School of Pharmacy, Universities of Kent and Greenwich, Chatham, Kent, UK, 2 Division of Systems Biology, National Center for
Because tubular secretion is an active process there may be competitive inhibition of the secretion of one compound by another. A common example of this phenomena is the inhibition of penicillin excretion by competition with
BILIARY EXCRETION INHIBITION BY TCDD 397 solution at 2.3 JJLI/S. Immediately after completion of the injection, 40 drops of bile were collected in a single vial.
These results indicated the important roles of P-gp and MRP2 in hepatobiliary excretion and plasma exposure of TNP and TNP-G. Inhibition of the efflux transporters may affect the pharmacokinetics of TNP and result in a drug-drug interaction between TNP and the concomitant transporter inhibitor or …
The lack of effect of Sn-protoporphyrin on biliary bilirubin excretion in primary biliary cirrhosis may be related to a differently affected hepatic clearance system or to a different distribution of tissue bilirubin pools in this condition.
The effect of cefoperazone, a third-generation cephalosporin, on biliary lipid secretion in rats was examined. Rats were anesthetized with ether and the mid-lumbar vein and common bile duct cannulated. Bile acid secretion was maintained by intravenous taurocholic acid infusion (28 μmol/hr). A 1-hr
GASTROENTEROLOGY 1992;102:1170-1175 Intestinal Heme Oxygenase Inhibition and Increased Biliary Iron Excretion by Metalloporphyrins GEORGE S. DRUMMOND, DANIEL W. ROSENBERG, and ATTALLAH KAPPAS
Agents that induce or inhibit the microsomal drug-metabolizing en-zymes increase or decrease, respectively, the biliary excretion of metabolites after the injection of 3H-7. 12-dimethylbenzanthracene. After the injection of metyrapone. an inhibition of biliary excretion is seen, although inhibition of metabolism of the hydrocarbon cannot be demonstrated using 1O.000g liver supernatant
genipin [6, 7, 10], as well as the biliary excretion of PCG itself [11]. In the present study, in order to study the effect of PCG on hepatic excretory pathways, the effect of colchicine and
Inhibition of mast cell‐secreted histamine decreases
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Impaired organic anion excretion and cholestasis caused by
biliary excretion (particularly those with a narrow therapeutic index such as vincristine and doxorubicin) for animals harboring the ABCB1-1Δ mutation. 99m Tc-MIBI is a cationic lipophilic agent and its uptake into the cells is passive
Efficacy, tissue distribution and biliary excretion of methyl ()-(E)-3,5-dihydroxy-9,9-diphenyl-6, 8-nonadienoate (CP-83101), A hepatoselective inhibitor of HMG-CoA reductase activity in the rat Author
The biliary excretion rate-time profiles (A) and their associated terminal half-lives (B), cumulative amounts excreted in bile (C), and CL b (D) values for different treatment groups are …
the biliary excretion of topotecan and cimetidine is also mainly regulated by Bcrp, considering the gender difference in the hepatic expression level of Bcrp and the plasma con-
HIDETAKA TACHIZAWA, NAOYO SANO and HAJIME TAKIKAWA, Effects of colchicine on the maximum biliary excretion of cholephilic compounds in rats, Journal of Gastroenterology and Hepatology, 19, 9, (1016), (2004).
In perfused rat liver menadione elicits substantial oxidation in both the NADPH and GSH redox systems. Biliary excretion of GSSG is increased several-fold.
for the excretion of lipid-soluble compounds such as bilirubin, cholesterol and drugs. Bile is synthesized by hepatocytes, the principal liver cell type, and is excreted into the biliary system through a specialized portion of the hepatocyte membrane, the canaliculus. Within the biliary system, bile is modified prior to transport to the gallbladder and intestine. Heritable defects of the
1.Biliary excretion of compounds is dependant on several transporter proteins for the active uptake of compounds from the blood into the hepatocytes. Organic anion-transporting polypeptides (OATPs) are some of the most abundant transporter proteins in the sinusoidal membrane and have been shown to
Developmental Changesin the Biliary Excretion of Methylmercury and Glutathione Abstract. Thelonghalf-timeformethylmercuryin the neonatalratis explainedby theneonatalliver’s inability tosecrete the toxin into bile, whichin adults is the main route ofelimination. Theability to secrete mercuryinto bile developsbetween2 and 4weeksof ageandis correlatedwith the increasing ability ofthe
P-glycoprotein and biliary excretion of vincristine Also, using the perfused rat liver, which is a more physiological system, we previously suggested the con-
Pitavastatin, a novel potent 3-hydroxymethylglutaryl coenzyme A reductase inhibitor, is distributed selectively to the liver and excreted into bile in unchanged form in rats. We reported previously that the hepatic uptake is mainly mediated by organic anion transporting polypeptide (OATP) 1B1, whereas the biliary excretion mechanism remains to
Papaverine is a nonspecific smooth muscle relaxant and a phosphodiesterase inhibitor. Its effects on biliary excretion of lipids and horseradish peroxidase were investigated in a single-pass
Linagliptin is a selective, competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, recently approved in the USA, Japan and Europe for the treatment of type 2 diabetes. It has non-linear pharmacokinetics and, unlike other DPP-4 inhibitors, a largely non-renal excretion route. It was hypothesised that
In PTU-treated rats biliary excretion was increased to 36.0% of the dose (P < .001) due to a dramatic increase in the sulfates of T 3 and 3,3′- diiodothyronine. Dichloronitrophenol by itself had no effect on the biliary clearance of T 3 , but greatly inhibited PTU-induced excretion of sulfates.
Purpose. To ameliorate the late-onset of severe gastrointestinal toxicity provoked by irinotecan (CPT-11), which may be related to the biliary excretion of CPT-11 and/or its metabolites. Methods. Effects of probenecid, an inhibitor of MRP2/ABCC2, on the biliary excretion and mucosal intestinal
MULTIPLE MECHANISMS ARE INVOLVED IN THE BILIARY EXCRETION OF ACETAMINOPHEN SULFATE IN THE RAT: ROLE OF MRP2 AND BCRP1 Maciej J. Zamek-Gliszczynski, Keith A. Hoffmaster, Xianbin Tian, Rong Zhao, Joseph W. Polli,
The effects of diclofenac, a nonsteroidal anti-inflammatory drug, on biliary excretion of ceftriaxone were evaluated in rabbits. In a previous study, we demonstrated that diclofenac increased the extravascular diffusion and antibacterial efficacy of ceftriaxone without any effect on serum protein binding and urinary excretion of this antibiotic.
PDF; Abstract. Fluoroquinolones are effective antibiotics for the treatment of bile duct infections. It has been shown that the biliary excretion of grepafloxacin is partly accounted for by multidrug resistance-associated protein 2 (MRP2/ ABCC2), whereas
A method of screening a candidate compound for susceptibility to biliary excretion. The method includes the steps of providing a culture of hepatocytes, the culture having at least one bile canaliculus; exposing a candidate compound to the culture; and determining an amount of candidate compound in the at least one bile canaliculus, the amount
The hepatic metabolism and biliary and pancreatic excretion of the serine protease inhibitor camostat mesilate and its metabolites FOY-251 and GBA were studied in …
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Printed in U.S.A. HEPATIC UPTAKE METABOLISM AND BILIARY
Gut, 1982, 23, 98-101 Inhibition ofpostprandialpancreatic andbiliary secretion byloperamidein patients withshort bowel syndrome* MARGOT REMINGTON, C RICHARD FLEMING, AND J-R MALAGELADAt
biliary excretion of sunitinib was also examined in SD rats and EHBR. The biliary clearance of sunitinib was significantly lower in EHBR, but the biliary excretion rate of EHBR was not different from that of SD rats, and the contribution of biliary excretion to systemic elimination was small, suggesting that sunitinib is mainly eliminated by cytochrome P450 3A4 (CYP3A4)-mediated metabolism and
Abstract. Sn(tin4+)-protoporphyrin, a potent competitive inhibitor of haeme oxygenase, the rate limiting enzyme in the degradation of haeme to bile pigments, was given intravenously to six patients with primary biliary cirrhosis and to four patients with idiopathic haemochromatosis.
Table 1: Comparison of biliary excretion of CPT-11 and its metabolites after i.v. administrations of CPT-11 lactone and carboxylate forms (100 µ g/body) in rats.
Biliary Excretion of Lecithin and Cholesterol in the Dog HENRY0.WHEELERandKATrERiNEK. KING Fromthe Department of Medicine, University of California, San Diego,
Pharmacokinetics of temocapril, an ACE inhibitor with preferential biliary excretion, in patients with impaired liver function S. Furuta t, K. Kiyosawa 1, M. Higuchi 1, …
The effect of the antianginal agent perhexiline maleate (160 mg/kg i.g., daily for 4 days) on the biliary excretion of sulfobromophthalein (BSP) and BSP-glutathione and the hepatic activity of glutathione S-transferases was investigated in Wistar rats.
inhibition ofthecommonbacteriaofbiliary infections. Inrenalfailure, however, the biliary excretion ofCIBA36 278Baincreased considerably. In earlier studies on the derivatives ofceph-alosporins, only a small part of the injected dose was found in the bile. However, the con-centrations attained with some of these drugs were sufficient to raise an interest in their possible use for the therapy of
95 Biliary excretion has major significance in determining the pharmacokinetic profiles of drugs. 96 In several disease states, the excretion of drugs through bile is affected and toxicities may 97 arise (1, 2).Biliary HCO,- secretion in EE cholestasis There is a general agreement that in EE-cholestatic rats the bile salt-dependent and independent fractions
Induction and Inhibition of Drug Metabolism Inhibition of Biliary Excretion by Nagaraju B 2. Induction and Inhibition Metabolism based drug-drug and other interactions can have a significant influence on the use and safety of many drugs. Induction of drug metabolism can lead to unexpected drops in drug concentration or the build-up of metabolites.
and its M1 and M3 metabolites were also subject to biliary excretion. Approximately 97% of the Approximately 97% of the administered radioactivity was excreted in feces; 83% of that was found to be unchanged orlistat.
Reduced Gastrointestinal Toxicity following Inhibition of the Biliary Excretion of Irinotecan and its Metabolites by Probenecid in Rats Masato Horikawa1, Yukio Kato1,2 and
The cumulative biliary excretion of BSP as a function of time after IV administration of 5 mg/kg in control and FK 506-treated rats at two dose levels for 5 to 6 weeks.
2 Abstract Biliary excretion of compounds is dependant on several transporter proteins for the active uptake of compounds from the blood into the hepatocytes.
The multidrug resistance gene 2 is an adenosine triphosphate‐binding cassette transporter, which encodes a P‐type glycoprotein responsible for the excretion of biliary phospholipids. 1, 3 Multidrug resistance 2 knockout (Mdr2 −/−) mice, which mimic human PSC progression, 3 lack this gene, causing bile acids to accumulate in the intrahepatic biliary system and disrupt portal tract function.
Unlike in rats, where sulfate and glucuronide conjugates were excreted into bile predominantly by Mrp2, mouse Bcrp mediated the biliary excretion of sulfate metabolites and also played a major role in the biliary excretion of the glucuronide metabolites, with some minor contribution from mouse Mrp2.
1/05/1991 · Full text Full text is available as a scanned copy of the original print version. Get a printable copy (PDF file) of the complete article (884K), or click on a page image below to browse page by page.
Oral administration of Sn-protoporphyrin (25 μmol/kg body weight) resulted in inhibition of intestinal heme oxygenase, however, no effect was observed on the splenic, hepatic, or renal enzymes. Intestinal heme oxygenase inhibition and increased biliary iron excretion by metalloporphyrins – …
US6780580B2 Method of screening candidate compounds for
Read “Conjugated bilirubin decreases the biliary excretion of phospholipids, Journal of Gastroenterology and Hepatology” on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
AF Hofmann. Biliary secretion and excretion in health and disease 17 a a aaa aa a salts. Bile salts have multiple functions in the organism, and current concepts of bile acid (salt) function are sum-
Concomitant cyclosporine interacts with mycophenolic acid (MPA) through inhibition of the biliary excretion of its glucuronide (MPAG). The aim of this study was to evaluate the influence of calcineurin inhibitors on the plasma disposition and urinary excretion …
Hypothetical substrates undergoing transporter-mediated hepatic uptake, metabolism, and enterohepatic circulation with different rate-determining processes with a combination of inhibition constants (K) for hepatic uptake, metabolism, and biliary excretion processes were generated with a constant K for uptake and incorporated into a physiologically based pharmacokinetic model. Analyses of the
The results indicate that 1) the glucuronidative clearance of T 4 is not affected by PTU; 2) the T 3 G/rT 3 G ratio in bile is a sensitive indicator of type I deiodinase inhibition; 3) T 4 undergoes significant sulfation in rats in vivo, and 4) biliary excretion of T 4 S is …
BILIARY EXCRETION OF CPT-I1 AND METABOLITES MATERIALS AND METHODS Materials. CPT-l 1, SN-38 and SN38-Gluwere providedkindly by Daiichi Pharmaceutical Co. Ltd. (Tokyo, Japan) and Yakult Honsha Co. Ltd. (Tokyo,
Impaired organic anion excretion and cholestasis caused by 1,3-bis-(2-chloroethyl)-1-nitrosourea (carmustine or BCNU) This was indicated by the inhibition of maximal excretion of BSP, inhibition of the biliary excretion of the non-metabolized dye, indocyanine green and the lack of inhibition of the conjugation of BSP with glutathione. Canalicular effects were also suggested …
Biliary Excretion and Enterohepatic Recycling of Proscillaridin A after Oral Administration to Man K.-E. Andersson, B. Bergdahl and G. Wettrell Department of Clinical Pharmacology, University Hospital, Lund, and Department of Clinical Pharmacology, University Hospital, Link6ping, Sweden Summary. A single oral dose of proscillaridin A (1.0-1.5rag) was given to six patients with T-tube drainage
Conjugated bilirubin decreases the biliary excretion of
biliary excretion Publications PubFacts
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Pretreatment pf rats with ITZ increased plasma levels and biliary excretion of amlodipine and made no changes in its plasma levels. In conclusion, ITZ inreased in vitro permeability of amlod ipine and bile in vivo. Whereas, CsA showed no significant efects on the levels of amlodipine in rat plasma and bile in vivo. Whereas, CsA showed no significant effects on the levels of amlodipine in rat
This study was designed to establish a strategy to predict drug interactions involving biliary excretion. The interaction between methotrexate and probenecid was examined as an interaction model
Biliary excretion rate (ng/min) is a function of drug concentration in bile (ng/ml) and biliary flow rate (ml/min). Biliary clearance ( CL b ) was estimated by plotting the average biliary excretion rate versus the plasma drug concentration at the midpoint of collection interval.
Inhibition of GGT by acivicin (100 mumol/kg i.v.) failed to influence the biliary excretion of methylmercury but increased urinary excretion 34-fold. Even though the urinary thiol excretion was much higher than the biliary thiol excretion in the acivicin-treated rats, methylmercury was preferentially excreted into bile rather than urine, indicating the importance of the liver as an excretory
In this study the effects of microtubule inhibition on biliary excretion of micelle- and non-micelle-forming bile salts and associated lipid were examined in rats. Low-dose col- chicine pretreatment had no effect on the baseline excretion of biliary bile
The reciprocal effects of Notch inhibition and activation on biliary development, coupled with the presence of hybrid cells in jagged and jagged/notch morphant larvae, are supportive of a model in which the Notch signal promotes the development of biliary cells from a bipotential progenitor.
After the injection of metyrapone, an inhibition of biliary excretion is seen, although inhibition of metabolism of the hydrocarbon cannot be demonstrated using 10,000g liver supernatant fractions obtained from injected animals.
The predicted degrees of inhibition by most compounds were minimal whereas approximately 75% inhibition was predicted for probenecid. Thus, probenecid may be a candidate which can be used clinically to inhibit the biliary excretion of CPT-11 metabolites, whereas an interaction between most of the other compounds and MRP2 is more unlikely.
Summary The single dose pharmacokinetics of temocapril, a novel prodrug type angiotensin converting enzyme (ACE) inhibitor with preferential biliary excretion, were evaluated in 6 patients main tained on haemodialysis and in 1 patient on continuous ambulatory peritoneal dialysis (CAPD).
Inhibition of biliary excretion of methotrexate by
The Important Role of Bcrp (Abcg2) in the Biliary
Effects of Cyclosporine A and Itraconazole on Permeability
like a house on fire cate kennedy free pdf
Induction and Inhibition of Drug Metabolism Inhibition of
(PDF) Inhibition of biliary cholesterol and phospholipid
Biliary Excretion of New Cephalosporin Cephacetrile
Pharmacokinetics of temocapril an ACE inhibitor with
Frontiers Inhibition of P-Glycoprotein and Multidrug
https://www.youtube.com/embed/8c3gqI6R-Vw
Reduced Gastrointestinal Toxicity Following Inhibition of
Conjugated bilirubin decreases the biliary excretion of
P-glycoprotein and biliary excretion of vincristine
In PTU-treated rats biliary excretion was increased to 36.0% of the dose (P < .001) due to a dramatic increase in the sulfates of T 3 and 3,3′- diiodothyronine. Dichloronitrophenol by itself had no effect on the biliary clearance of T 3 , but greatly inhibited PTU-induced excretion of sulfates.
The biliary concentrations found in these subjects seem to be inferior to those required for the inhibition of the common bacteria of biliary infections. In renal failure, however, the biliary excretion of CIBA 36 278 Ba increased considerably.
Biliary Excretion and Enterohepatic Recycling of Proscillaridin A after Oral Administration to Man K.-E. Andersson, B. Bergdahl and G. Wettrell Department of Clinical Pharmacology, University Hospital, Lund, and Department of Clinical Pharmacology, University Hospital, Link6ping, Sweden Summary. A single oral dose of proscillaridin A (1.0-1.5rag) was given to six patients with T-tube drainage
After the injection of metyrapone, an inhibition of biliary excretion is seen, although inhibition of metabolism of the hydrocarbon cannot be demonstrated using 10,000g liver supernatant fractions obtained from injected animals.
Because tubular secretion is an active process there may be competitive inhibition of the secretion of one compound by another. A common example of this phenomena is the inhibition of penicillin excretion by competition with
pdf. Inhibition of biliary bicarbonate secretion in ethinyl estradiol-induced cholestasis is not associated with impaired activity of the Cl −/HCO 3 − exchanger in the rat
The predicted degrees of inhibition by most compounds were minimal whereas approximately 75% inhibition was predicted for probenecid. Thus, probenecid may be a candidate which can be used clinically to inhibit the biliary excretion of CPT-11 metabolites, whereas an interaction between most of the other compounds and MRP2 is more unlikely.
Studies with the haeme oxygenase inhibitor Sn
Conjugated bilirubin decreases the biliary excretion of
The results indicate that 1) the glucuronidative clearance of T 4 is not affected by PTU; 2) the T 3 G/rT 3 G ratio in bile is a sensitive indicator of type I deiodinase inhibition; 3) T 4 undergoes significant sulfation in rats in vivo, and 4) biliary excretion of T 4 S is …
The reciprocal effects of Notch inhibition and activation on biliary development, coupled with the presence of hybrid cells in jagged and jagged/notch morphant larvae, are supportive of a model in which the Notch signal promotes the development of biliary cells from a bipotential progenitor.
Reduced Gastrointestinal Toxicity following Inhibition of the Biliary Excretion of Irinotecan and its Metabolites by Probenecid in Rats Masato Horikawa1, Yukio Kato1,2 and
Pretreatment pf rats with ITZ increased plasma levels and biliary excretion of amlodipine and made no changes in its plasma levels. In conclusion, ITZ inreased in vitro permeability of amlod ipine and bile in vivo. Whereas, CsA showed no significant efects on the levels of amlodipine in rat plasma and bile in vivo. Whereas, CsA showed no significant effects on the levels of amlodipine in rat
the biliary excretion of topotecan and cimetidine is also mainly regulated by Bcrp, considering the gender difference in the hepatic expression level of Bcrp and the plasma con-
Bilirubin is one of several organic anions that selectively inhibit the biliary secretion of phospholipid and cholesterol without affecting bile salt secretion. To determine the site of this inhibition and gain insight into its mechanism, normal, Sprague-Dawley and homozygous Gunn rats were infumsed with unconjugated bilirubin and a water
Agents that induce or inhibit the microsomal drug-metabolizing en-zymes increase or decrease, respectively, the biliary excretion of metabolites after the injection of 3H-7. 12-dimethylbenzanthracene. After the injection of metyrapone. an inhibition of biliary excretion is seen, although inhibition of metabolism of the hydrocarbon cannot be demonstrated using 1O.000g liver supernatant
genipin [6, 7, 10], as well as the biliary excretion of PCG itself [11]. In the present study, in order to study the effect of PCG on hepatic excretory pathways, the effect of colchicine and
Gut, 1982, 23, 98-101 Inhibition ofpostprandialpancreatic andbiliary secretion byloperamidein patients withshort bowel syndrome* MARGOT REMINGTON, C RICHARD FLEMING, AND J-R MALAGELADAt
Biliary secretion and excretion in health and disease
Excretion in Rats D-Scholarship@Pitt
Inhibition of GGT by acivicin (100 mumol/kg i.v.) failed to influence the biliary excretion of methylmercury but increased urinary excretion 34-fold. Even though the urinary thiol excretion was much higher than the biliary thiol excretion in the acivicin-treated rats, methylmercury was preferentially excreted into bile rather than urine, indicating the importance of the liver as an excretory
In perfused rat liver menadione elicits substantial oxidation in both the NADPH and GSH redox systems. Biliary excretion of GSSG is increased several-fold.
In this study the effects of microtubule inhibition on biliary excretion of micelle- and non-micelle-forming bile salts and associated lipid were examined in rats. Low-dose col- chicine pretreatment had no effect on the baseline excretion of biliary bile
1/05/1991 · Full text Full text is available as a scanned copy of the original print version. Get a printable copy (PDF file) of the complete article (884K), or click on a page image below to browse page by page.
and its M1 and M3 metabolites were also subject to biliary excretion. Approximately 97% of the Approximately 97% of the administered radioactivity was excreted in feces; 83% of that was found to be unchanged orlistat.
How to Cite. Parasrampuria, R. and Mehvar, R. (2010), Dose-dependent inhibition of transporter-mediated hepatic uptake and biliary excretion of methotrexate by cyclosporine A in an isolated perfused rat liver model.
After the injection of metyrapone, an inhibition of biliary excretion is seen, although inhibition of metabolism of the hydrocarbon cannot be demonstrated using 10,000g liver supernatant fractions obtained from injected animals.
Efficacy, tissue distribution and biliary excretion of methyl ()-(E)-3,5-dihydroxy-9,9-diphenyl-6, 8-nonadienoate (CP-83101), A hepatoselective inhibitor of HMG-CoA reductase activity in the rat Author
Read “Conjugated bilirubin decreases the biliary excretion of phospholipids, Journal of Gastroenterology and Hepatology” on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
GASTROENTEROLOGY 1992;102:1170-1175 Intestinal Heme Oxygenase Inhibition and Increased Biliary Iron Excretion by Metalloporphyrins GEORGE S. DRUMMOND, DANIEL W. ROSENBERG, and ATTALLAH KAPPAS
AF Hofmann. Biliary secretion and excretion in health and disease 17 a a aaa aa a salts. Bile salts have multiple functions in the organism, and current concepts of bile acid (salt) function are sum-
PDF; Abstract. Fluoroquinolones are effective antibiotics for the treatment of bile duct infections. It has been shown that the biliary excretion of grepafloxacin is partly accounted for by multidrug resistance-associated protein 2 (MRP2/ ABCC2), whereas
Summary The single dose pharmacokinetics of temocapril, a novel prodrug type angiotensin converting enzyme (ACE) inhibitor with preferential biliary excretion, were evaluated in 6 patients main tained on haemodialysis and in 1 patient on continuous ambulatory peritoneal dialysis (CAPD).
Inhibition by colchicine of biliary secretion of
Impact of calcineurin inhibitors on urinary excretion of
The biliary excretion rate-time profiles (A) and their associated terminal half-lives (B), cumulative amounts excreted in bile (C), and CL b (D) values for different treatment groups are …
The predicted degrees of inhibition by most compounds were minimal whereas approximately 75% inhibition was predicted for probenecid. Thus, probenecid may be a candidate which can be used clinically to inhibit the biliary excretion of CPT-11 metabolites, whereas an interaction between most of the other compounds and MRP2 is more unlikely.
The cumulative biliary excretion of BSP as a function of time after IV administration of 5 mg/kg in control and FK 506-treated rats at two dose levels for 5 to 6 weeks.
PDF; Abstract. Fluoroquinolones are effective antibiotics for the treatment of bile duct infections. It has been shown that the biliary excretion of grepafloxacin is partly accounted for by multidrug resistance-associated protein 2 (MRP2/ ABCC2), whereas
biliary excretion of sunitinib was also examined in SD rats and EHBR. The biliary clearance of sunitinib was significantly lower in EHBR, but the biliary excretion rate of EHBR was not different from that of SD rats, and the contribution of biliary excretion to systemic elimination was small, suggesting that sunitinib is mainly eliminated by cytochrome P450 3A4 (CYP3A4)-mediated metabolism and
for the excretion of lipid-soluble compounds such as bilirubin, cholesterol and drugs. Bile is synthesized by hepatocytes, the principal liver cell type, and is excreted into the biliary system through a specialized portion of the hepatocyte membrane, the canaliculus. Within the biliary system, bile is modified prior to transport to the gallbladder and intestine. Heritable defects of the
Concomitant cyclosporine interacts with mycophenolic acid (MPA) through inhibition of the biliary excretion of its glucuronide (MPAG). The aim of this study was to evaluate the influence of calcineurin inhibitors on the plasma disposition and urinary excretion …
Read “Conjugated bilirubin decreases the biliary excretion of phospholipids, Journal of Gastroenterology and Hepatology” on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
Table 1: Comparison of biliary excretion of CPT-11 and its metabolites after i.v. administrations of CPT-11 lactone and carboxylate forms (100 µ g/body) in rats.
Gut, 1982, 23, 98-101 Inhibition ofpostprandialpancreatic andbiliary secretion byloperamidein patients withshort bowel syndrome* MARGOT REMINGTON, C RICHARD FLEMING, AND J-R MALAGELADAt
Efficacy, tissue distribution and biliary excretion of methyl ()-(E)-3,5-dihydroxy-9,9-diphenyl-6, 8-nonadienoate (CP-83101), A hepatoselective inhibitor of HMG-CoA reductase activity in the rat Author
AF Hofmann. Biliary secretion and excretion in health and disease 17 a a aaa aa a salts. Bile salts have multiple functions in the organism, and current concepts of bile acid (salt) function are sum-
GASTROENTEROLOGY 1992;102:1170-1175 Intestinal Heme Oxygenase Inhibition and Increased Biliary Iron Excretion by Metalloporphyrins GEORGE S. DRUMMOND, DANIEL W. ROSENBERG, and ATTALLAH KAPPAS
Pretreatment pf rats with ITZ increased plasma levels and biliary excretion of amlodipine and made no changes in its plasma levels. In conclusion, ITZ inreased in vitro permeability of amlod ipine and bile in vivo. Whereas, CsA showed no significant efects on the levels of amlodipine in rat plasma and bile in vivo. Whereas, CsA showed no significant effects on the levels of amlodipine in rat
Ability of S-adenosyl-l-methionine (SAMe) to antagonize
Inhibition of biliary bicarbonate secretion in ethinyl
the biliary excretion of topotecan and cimetidine is also mainly regulated by Bcrp, considering the gender difference in the hepatic expression level of Bcrp and the plasma con-
Pharmacokinetics of temocapril, an ACE inhibitor with preferential biliary excretion, in patients with impaired liver function S. Furuta t, K. Kiyosawa 1, M. Higuchi 1, …
genipin [6, 7, 10], as well as the biliary excretion of PCG itself [11]. In the present study, in order to study the effect of PCG on hepatic excretory pathways, the effect of colchicine and
In perfused rat liver menadione elicits substantial oxidation in both the NADPH and GSH redox systems. Biliary excretion of GSSG is increased several-fold.
Papaverine is a nonspecific smooth muscle relaxant and a phosphodiesterase inhibitor. Its effects on biliary excretion of lipids and horseradish peroxidase were investigated in a single-pass
Reduced Gastrointestinal Toxicity following Inhibition of the Biliary Excretion of Irinotecan and its Metabolites by Probenecid in Rats Masato Horikawa1, Yukio Kato1,2 and
Efficacy, tissue distribution and biliary excretion of methyl ()-(E)-3,5-dihydroxy-9,9-diphenyl-6, 8-nonadienoate (CP-83101), A hepatoselective inhibitor of HMG-CoA reductase activity in the rat Author
Bilirubin is one of several organic anions that selectively inhibit the biliary secretion of phospholipid and cholesterol without affecting bile salt secretion. To determine the site of this inhibition and gain insight into its mechanism, normal, Sprague-Dawley and homozygous Gunn rats were infumsed with unconjugated bilirubin and a water
HIDETAKA TACHIZAWA, NAOYO SANO and HAJIME TAKIKAWA, Effects of colchicine on the maximum biliary excretion of cholephilic compounds in rats, Journal of Gastroenterology and Hepatology, 19, 9, (1016), (2004).
(PDF) Inhibition of biliary cholesterol and phospholipid
Developmental Changes Biliary Excretion of Methylmercury
Unlike in rats, where sulfate and glucuronide conjugates were excreted into bile predominantly by Mrp2, mouse Bcrp mediated the biliary excretion of sulfate metabolites and also played a major role in the biliary excretion of the glucuronide metabolites, with some minor contribution from mouse Mrp2.
In perfused rat liver menadione elicits substantial oxidation in both the NADPH and GSH redox systems. Biliary excretion of GSSG is increased several-fold.
HIDETAKA TACHIZAWA, NAOYO SANO and HAJIME TAKIKAWA, Effects of colchicine on the maximum biliary excretion of cholephilic compounds in rats, Journal of Gastroenterology and Hepatology, 19, 9, (1016), (2004).
biliary excretion (particularly those with a narrow therapeutic index such as vincristine and doxorubicin) for animals harboring the ABCB1-1Δ mutation. 99m Tc-MIBI is a cationic lipophilic agent and its uptake into the cells is passive
Concomitant cyclosporine interacts with mycophenolic acid (MPA) through inhibition of the biliary excretion of its glucuronide (MPAG). The aim of this study was to evaluate the influence of calcineurin inhibitors on the plasma disposition and urinary excretion …
pdf. Inhibition of biliary bicarbonate secretion in ethinyl estradiol-induced cholestasis is not associated with impaired activity of the Cl −/HCO 3 − exchanger in the rat
the biliary excretion of topotecan and cimetidine is also mainly regulated by Bcrp, considering the gender difference in the hepatic expression level of Bcrp and the plasma con-
1.Biliary excretion of compounds is dependant on several transporter proteins for the active uptake of compounds from the blood into the hepatocytes. Organic anion-transporting polypeptides (OATPs) are some of the most abundant transporter proteins in the sinusoidal membrane and have been shown to
Efficacy, tissue distribution and biliary excretion of methyl ()-(E)-3,5-dihydroxy-9,9-diphenyl-6, 8-nonadienoate (CP-83101), A hepatoselective inhibitor of HMG-CoA reductase activity in the rat Author
The effects of diclofenac, a nonsteroidal anti-inflammatory drug, on biliary excretion of ceftriaxone were evaluated in rabbits. In a previous study, we demonstrated that diclofenac increased the extravascular diffusion and antibacterial efficacy of ceftriaxone without any effect on serum protein binding and urinary excretion of this antibiotic.
Bilirubin is one of several organic anions that selectively inhibit the biliary secretion of phospholipid and cholesterol without affecting bile salt secretion. To determine the site of this inhibition and gain insight into its mechanism, normal, Sprague-Dawley and homozygous Gunn rats were infumsed with unconjugated bilirubin and a water
P-glycoprotein and biliary excretion of vincristine Also, using the perfused rat liver, which is a more physiological system, we previously suggested the con-
Gut, 1982, 23, 98-101 Inhibition ofpostprandialpancreatic andbiliary secretion byloperamidein patients withshort bowel syndrome* MARGOT REMINGTON, C RICHARD FLEMING, AND J-R MALAGELADAt
The effect of the antianginal agent perhexiline maleate (160 mg/kg i.g., daily for 4 days) on the biliary excretion of sulfobromophthalein (BSP) and BSP-glutathione and the hepatic activity of glutathione S-transferases was investigated in Wistar rats.
BILIARY EXCRETION OF CPT-I1 AND METABOLITES MATERIALS AND METHODS Materials. CPT-l 1, SN-38 and SN38-Gluwere providedkindly by Daiichi Pharmaceutical Co. Ltd. (Tokyo, Japan) and Yakult Honsha Co. Ltd. (Tokyo,
Inhibition of GGT by acivicin (100 mumol/kg i.v.) failed to influence the biliary excretion of methylmercury but increased urinary excretion 34-fold. Even though the urinary thiol excretion was much higher than the biliary thiol excretion in the acivicin-treated rats, methylmercury was preferentially excreted into bile rather than urine, indicating the importance of the liver as an excretory
Inhibition of mast cell‐secreted histamine decreases
P-glycoprotein and biliary excretion of vincristine
Pharmacokinetics of temocapril an ACE inhibitor with