The Experts below are selected from a list of 108 Experts worldwide ranked by ideXlab platform
Mark R. Marshall - One of the best experts on this subject based on the ideXlab platform.
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feasibility study of Colestipol as an oral phosphate binder in hemodialysis patients
Nephrology, 2015Co-Authors: Christopher John Hood, Martin Wolley, Mark R. Marshall, Angela L Kam, Jamie C KendrikjonesAbstract:Background Currently available calcium- and aluminium-based phosphate binders are dose limited because of potential toxicity, and newer proprietary phosphate binders are expensive. We examined phosphate-binding effects of the bile acid sequestrant Colestipol, a non-proprietary drug that is in the same class as sevelamer. Methods The trial was an 8 week prospective feasibility study in stable hemodialysis patients using Colestipol as the only phosphate binder, preceded and followed by a washout phase of all other phosphate binders. The primary study endpoint was weekly measurements of serum phosphate. Secondary endpoints were serum calcium, lipids and coagulation status. Analyses used random effects mixed models. Results Thirty patients were screened for participation of which 26 met criteria for treatment. At a mean dose of 8.8g/24h of Colestipol by study end, serum phosphate dropped from 2.24 to 1.96mmol/L (P<0.001). Three patients required calcium supplementation. LDL cholesterol dropped from 1.75 to 1.2mmol/L (P<0.001). Three patients dropped out because of side effects or intolerance of the required dose. Conclusion The results support the feasibility of a larger trial to determine the efficacy of Colestipol as a phosphate binder and that other non-proprietary anion-exchange resins may also warrant investigation. Summary at a Glance Phosphate binders are the predominant treatment at present for hyperphosphataemia in dialysis, and more research is needed to evaluate newer agents with phosphate-lowering efficacy but with less adverse effects than currently prescribed binders. This study outlines a prospective trial to assess the effects of Colestipol, a bile acid sequestrant, on phosphate-binding capacity and biochemical parameters in haemodialysis patients.
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Feasibility study of Colestipol as an oral phosphate binder in hemodialysis patients
Nephrology, 2015Co-Authors: Christopher John Hood, Martin Wolley, Jamie C Kendrik-jones, Mark R. MarshallAbstract:Background Currently available calcium- and aluminium-based phosphate binders are dose limited because of potential toxicity, and newer proprietary phosphate binders are expensive. We examined phosphate-binding effects of the bile acid sequestrant Colestipol, a non-proprietary drug that is in the same class as sevelamer. Methods The trial was an 8 week prospective feasibility study in stable hemodialysis patients using Colestipol as the only phosphate binder, preceded and followed by a washout phase of all other phosphate binders. The primary study endpoint was weekly measurements of serum phosphate. Secondary endpoints were serum calcium, lipids and coagulation status. Analyses used random effects mixed models. Results Thirty patients were screened for participation of which 26 met criteria for treatment. At a mean dose of 8.8g/24h of Colestipol by study end, serum phosphate dropped from 2.24 to 1.96mmol/L (P
Dale A. Freeman - One of the best experts on this subject based on the ideXlab platform.
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Colestipol-induced hepatotoxicity.
Pharmacotherapy, 2001Co-Authors: Susan M Sirmans, Joni Beck, Hoan Linh Banh, Dale A. FreemanAbstract:A 65-year-old man with type IIa dyslipidemia who received flavored Colestipol granules 2 scoops/day for 3 months developed asymptomatic hepatotoxicity. Several of his liver enzymes were elevated 10 times the upper limit of normal. One week after discontinuing Colestipol, serum transaminases fell dramatically, with some returning to normal limits. Four weeks after Colestipol was discontinued, all liver function tests were normal. Rechallenge was not attempted. Other potential causes of hepatocellular injury were evaluated. Bile acid-binding resins commonly are administered to treat type IIa dyslipidemia. Despite extensive use of the resins, significant elevations of transaminase levels are rare. Because the exact mechanism of bile acid resin-induced hepatotoxicity is unknown, high-risk patients may require liver function test monitoring and education on hepatotoxic side effects.
S.-d. Clas - One of the best experts on this subject based on the ideXlab platform.
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Quaternized Colestipol, an Improved Bile Salt Adsorbent: In Vitro Studies
Journal of pharmaceutical sciences, 1991Co-Authors: S.-d. ClasAbstract:Abstract Colestipol · HCl (col-HCl) was quaternized with methyl iodide to form col-CH 3 l. The in vitro binding capacities of the quaternized and protonated resins in water and in Tris-HCl buffer (0.0015 and 0.0025 M, pH 7.0) at ~ 22 °C for sodium glycocholate (NaGC) was determined by reversed-phase HPLC. The binding capacities were found to depend on the adsorption medium. In water, the binding capacity of col-CH 3 l was 30% greater than that of its protonated form. In Tris-HCl buffer at pH 7.0, the binding capacities of the resins were similar. When the quaternized Colestipol was converted to its chloride form, the binding capacity for NaGC in Tris-HCl increased significantly and was 30% greater than that for its protonated analogue. In Cotazym 65B-water, a medium used to test the binding capacity of the resins in the presence of various agents (to try to simulate intestinal conditions), the binding capacity of the quaternized resin was again greater than that of its protonated form. Quaternization thus increases the in vitro binding capacity of Colestipol for the glycocholate anion.
Donald M Black - One of the best experts on this subject based on the ideXlab platform.
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J Cardiovasc Pharrnacol Therapeut I(2): I 17-122, I996 Atorvastatin, a New HMG-CoA Reductase Inhibitor as Monotherapy and Combined With Colestipol
2016Co-Authors: Therese M. Heinonen, Helmut Schrott, James M Mckenney, Allan D Sniderman, Frances E Broyles, Frances Kivel, Ii James, H. Zavoral, Donald M BlackAbstract:Background: Atorvastatin, a new HhlG-CoA reductase inhibitor in clinical development has demonstrated an acceptable safety profile and marked cholesterol and triglyceride reduction at doses ranging from 10-80 mgday. Since bile acid sequestering resins are often used in combination with HMGRIs to enhance cholesterol reduction, this trial was conducted to explore the use of atorvastatin alone and combined with Colestipol in patients with primary hyperlipidemia. Metlids and Results: One hundred six patients with low-density lipoprotein (LDL) choles-terol> 4.1 mM/L (160 mddL) and plasma triglycerides < 3.9 mh4L (350 mg/dL) were ran-domized to treatment consisting of 20 glday Colestipol, 10 mg/day atorvastatin, or 10 mg/day atorvastatin plus 20 dday Colestipol for 12 weeks. Percent change from baseline in lipid vxi-ables was measured. The atorvastatin group showed a significant reduction in LDL choles-terol of 35 % after 12 weeks. Combination therapy provided an additional 10 % reduction in LDL cholesterol over that observed for atorvastatin alone. Twenty-one percent of all patients in the atorvastatin monotherapy group experienced associated adverse events compared with 60 % in the combination therapy group. Ninety percent of atorvastatin monotherapy patient
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atorvastatin a new hmg coa reductase inhibitor as monotherapy and combined with Colestipol
Journal of Cardiovascular Pharmacology and Therapeutics, 1996Co-Authors: Therese Heinonen, Helmut Schrott, James M Mckenney, Allan D Sniderman, Frances E Broyles, James H Zavoral, Frances Kivel, Donald M BlackAbstract:BACKGROUND: Atorvastatin, a new HMG-CoA reductase inhibitor in clinical development has demonstrated an acceptable safety profile and marked cholesterol and triglyceride reduction at doses ranging from 10-80 mg/day. Since bile acid sequestering resins are often used in combination with HMGRIs to enhance cholesterol reduction, this trial was conducted to explore the use of atorvastatin alone and combined with Colestipol in patients with primary hyperlipidemia. METHODS AND RESULTS: One hundred six patients with low-density lipoprotein (LDL) cholesterol >4.1 mM/L (160 mg/dL) and plasma triglycerides <3.9 mM/L (350 mg/dL) were randomized to treatment consisting of 20 g/day Colestipol, 10 mg/day atorvastatin, or 10 mg/day atorvastatin plus 20 g/day Colestipol for 12 weeks. Percent change from baseline in lipid variables were measured. The atorvastatin group showed a significant reduction in LDL cholesterol of 35% after 12 weeks. Combination therapy provided an additional 10% reduction in LDL cholesterol over that observed for atorvastatin alone. Twenty-one percent of all patients in the atorvastatin monotherapy group experienced associated adverse events compared with 60% in the combination therapy group. Ninety percent of atorvastatin monotherapy patients were compliant at every visit compared with 75% receiving combination therapy. CONCLUSIONS: Although the combination of atorvastatin plus Colestipol was more effective in lowering LDL cholesterol than atorvastatin alone, atorvastatin 10 mg/day monotherapy provided a better safety profile and improved patient compliance, which may result in improved long-term cholesterol control.
M.w. Gouda - One of the best experts on this subject based on the ideXlab platform.
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The effects of cholestyramine and Colestipol on the absorption of diclofenac in man
International journal of clinical pharmacology and therapeutics, 1994Co-Authors: Sulaiman R. Al-balla, Y. M. El-sayed, M. A. Al-meshal, M.w. GoudaAbstract:The effect of oral administration of the non-absorbable anion-exchange resins cholestyramine and Colestipol hydrochloride on the absorption of diclofenac in man was studied. Adsorption studies in vitro were also performed. In a randomized crossover study consisting of three phases, single doses of water suspensions of Colestipol hydrochloride (10 g), or cholestyramine (8 g), or water only were given to six healthy male volunteers immediately following ingestion of diclofenac (100 mg). After dosing, serial blood samples were collected for a period of 8 hours. Plasma harvested from blood was analyzed for diclofenac by a sensitive and accurate high-performance liquid chromatographic method. The area under the plasma concentration-time curve was moderately (33%, p < 0.05) reduced by Colestipol, and greatly reduced (62%) by cholestyramine. The maximum plasma concentration was reduced (58%) by Colestipol and even more (75%) by cholestyramine treatment. The in-vitro adsorption studies showed that Colestipol has a weaker capacity for adsorption of diclofenac compared to cholestyramine. The in-vivo data suggest a reduction of diclofenac bioavailability when Colestipol or cholestyramine is administered concomitantly.
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The effect of Colestipol and cholestyramine on the systemic clearance of intravenous ibuprofen in rabbits
The Journal of pharmacy and pharmacology, 1994Co-Authors: Y. M. El-sayed, M. A. Al-meshal, A. A. Al-angary, K. M. Lutfi, M.w. GoudaAbstract:— The effect of oral administration of the non-absorbable anion-exchange resins cholestyramine and Colestipol on the systemic clearance and other pharmacokinetic parameters of intravenously administered ibuprofen (25 mg kg−1) was studied in rabbits. Single doses of Colestipol hydrochloride (0·4 g kg−1) or cholestyramine (0·17 g kg−1) were given 30 min before ibuprofen administration. In cholestyramine-treated rabbits a significant reduction in ibuprofen plasma concentration was observed compared with both control (water only) and Colestipol-treated rabbits. Cholestyramine treatment resulted in a significant decrease in the terminal elimination half-life and the mean residence time. Furthermore, a 31% increase in the systemic clearance and 23% decrease in the area under the plasma concentration-time curve were also observed in cholestyramine-treated rabbits. Colestipol treatment did not change these parameters. The volume of distribution parameters (Vdss and Vdarea) did not change following either treatment. The changes in the pharmacokinetic parameters are compatible with an acceleration of ibuprofen elimination induced by oral administration of cholestyramine and not by Colestipol. This effect is thought to be due to augmentation of net biliary excretion through enteric binding.
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Effects of oral administration of Colestipol and cholestyramine on the pharmacokinetics of ketoprofen administered intramuscularly in man
International Journal of Pharmaceutics, 1994Co-Authors: Y. M. El-sayed, Sulaiman R. Al-balla, M. A. Al-meshal, A. A. Al-angary, M.w. GoudaAbstract:The effect of oral administration of the anion exchange resins Colestipol hydrochloride (10 g) or cholestyramine (8 g) on the systemic clearance and other pharmacokinetic parameters of intramuscularly administered ketoprofen (50 mg) has been studied in six healthy male subjects. The study was performed according to a randomized three-way crossover design with a 1 week washout period between each treatment phase. After dosing, serial blood samples were collected for a period of 8 h. Plasma harvested from blood was analyzed for ketoprofen by a sensitive high-performance liquid Chromatographie assay. Cholestyramine administration resulted in a significant reduction in ketoprofen plasma concentrations. No significant differences between Colestipol-treated and control groups were observed in the calculated pharmacokinetic parameters (Cl, AUC, Kel, t12 and MRT). Cholestyramine treatment resulted in a significant increase in the Kel (55%, p < 0.01), and Cl (32%, p < 0.005) and a significant decrease in the AUC (24%, p < 0.001), t12 (33%, p < 0.01) and MRT (30%, p < 0.001). These results indicate an enhancement of ketoprofen elimination following cholestyramine administration and a lack of interaction between Colestipol and ketoprofen.
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The effect of Colestipol and cholestyramine on ibuprofen bioavailability in man.
Biopharmaceutics & drug disposition, 1994Co-Authors: M. A. Al-meshal, Sulaiman R. Al-balla, Y. M. El-sayed, M.w. GoudaAbstract:The purpose of this study was to determine whether a concomitant single oral dose of one of the anion exchange resins Colestipol hydrochloride (10 g) or cholestyramine (8 g) administered with ibuprofen (400 mg) would alter the bioavailability of this non-steroidal anti-inflammatory agent. The study was performed according to a randomized three-way crossover design in six healthy male volunteers. After dosing, serial blood samples were collected for a period of 10 h. Plasma harvested from blood was analysed for ibuprofen by a sensitive high-performance liquid chromatographic method. There were no significant differences between Colestipol treatment and control for peak plasma concentration (Cmax), time to peak concentration (Tmax), area under the plasma concentration-time curve (AUC), mean residence time (MRT), elimination rate constant (Kel), or elimination half-life (t1/2). Cholestyramine treatment resulted in a significant decrease in AUC (26%, p < 0.05) and Cmax (34.4%, p < 0.01) and a significant increase in Tmax (80%, p < 0.01) and MRT (20.2%, p < 0.05). Cholestyramine administration showed no significant effect on the Kel and t1/2 values. A significant correlation was obtained between the increase in MRT and the increase in Tmax. The confidence intervals (90%) of the mean values of the pharmacokinetic parameters (AUC0-infinity and Cmax) for the Colestipol: control ratio were well within the acceptable range of 100 +/- 20, whereas those for the cholestyramine: control ratio were outside it. Colestipol treatment was found to be bioequivalent to the control treatment by Schuirmann's two one-sided t tests, while cholestyramine treatment was found to be bioinequivalent.(ABSTRACT TRUNCATED AT 250 WORDS)