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PubMed1992

Effectiveness of low-dose colestipol therapy in patients with moderate hypercholesterolemia.

Recommended doses of bile-acid binding resins have an established hypocholesterolemic effect, but data on responses to low doses, especially in women and subjects with moderate hypercholesterolemia, are sparse. A double-blind, placebo-controlled, randomized trial of 3 low doses of colestipol hydrochloride was conducted in women and men with moderate hypercholesterolemia. Men and women with plasma low-density lipoprotein (LDL) cholesterol concentrations greater than 4 mmol/liter (155 mg/dl) and triglyceride concentrations less than 2.82 mmol/liter (250 mg/dl) were recruited for the study. Eligible patients (54 women and 98 men) were placed on the American Heart Association step I diet 6 weeks before randomization. Participants were subsequently assigned to 1 of 4 drug treatment groups (placebo, and 5, 10 and 15 g/day of colestipol in 2 divided doses) for an additional 12 weeks. Of the 152 patients randomized, 141 completed all aspects of the study. For the treatment groups--placebo, and 5, 10 and 15 g of colestipol--LDL cholesterol reductions (mmol/liter) were observed respectively (n = 141): 0.10 +/- 0.49 (2.7%), 0.65 +/- 0.41 (16.3%), 0.98 +/- 0.36 (22.8%) and 1.17 +/- 0.47 (27.2%) (p less than 0.001). Similar changes were observed in total cholesterol and apolipoprotein B concentrations. The apolipoprotein B/LDL cholesterol ratio increased significantly with increasing colestipol dosage. Modest but insignificant changes in plasma triglyceride levels occurred, and high-density lipoprotein cholesterol levels remained unchanged. A dose of 5 g/day of colestipol achieved 51% of the LDL cholesterol reduction noted with 15 g/day. Low-dose colestipol therapy is effective in the treatment of patients with moderate hypercholesterolemia.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1983

Colestipol hydrochloride prophylaxis of diarrhea during pelvic radiotherapy.

Thirty-three patients were randomized prior to pelvic radiotherapy to receive the bile acid-sequestering resin colestipol hydrochloride, 5 grams qid, during the entire time of their therapy or diphenoxylate hydrochloride and atropine sulfate 2.5-20 mg per day (control) if they experienced diarrhea. The colestipol patients also took diphenoxylate if they had diarrhea. The patients in the colestipol group often experienced nausea, vomiting, and abdominal cramps and 8 were forced to discontinue the drug. There was no difference in the weekly stool frequency between the colestipol and the control patients but the colestipol patients who took at least 50% of the prescribed dose required fewer diphenoxylate tablets than the controls. The data suggest that colestipol hydrochloride is not of value in preventing radiation-induced diarrhea because of the side effects associated with the drug, but the theory on which the use of bile acid-sequestering agents is based may be correct.

Adult↗
PubMed1981

Colestipol plus nicotinic acid in treatment of heterozygous familial hypercholesterolaemia.

Thriteen patients with heterozygous familial hypercholesterolaemia (FH) were sequentially treated with: a low-cholesterol, fat-restricted diet; diet and colestipol; and diet and colestipol and nicotinic acid. Concentrations of plasma cholesterol decreased from 415 +/- 69 mg/dl on diet alone to 327 +/- 54 mg/dl on colestipol and fell to 246 +/- 49 mg/dl on the combined drug regimen. Plasma concentrations of LDL cholesterol declined 24% on colestipol; the subsequent addition of nicotinic acid resulted in a further 31% fall so that values on the combined drug regimen were 47% below those seen on diet alone. HDL cholesterol levels were similar on both the diet (40 mg/dl) and colestipol (43 mg/dl) treatment periods but increased to 53 mg/dl on the combined drug regimen. Treatment resulted in significant decreases in the LDL:HDL ratio which fell from 8.4 on diet to 3.3 on the colestipol plus nicotinic acid regimen. In most patients with heterozygous FH, combined use of a bile acid sequestrant and nicotinic acid affords the opportunity to maintain a normal lipid profile. Prolonged use of this regimen may reduce the incidence of premature coronary atherosclerosis which naturally occurs in these patients.

Adult↗
PubMed1990

The effect of colestipol dose on postprandial serum bile acid concentration: assessment by an enzymic bioluminescence procedure.

A dose-response study was performed with three doses of colestipol, using postprandial serum bile acid levels to assess bile acid sequestering activity in 40 volunteers with asymptomatic hyperlipidaemia. Subjects who entered the study had total serum cholesterol concentrations greater than 220 mg/dl and triglyceride concentrations less than 200 mg/dl. They were randomly assigned to one of four parallel treatment groups: (a) placebo b.d., (b) colestipol (as Colestid hydrochloride granules) 2.5 g b.d., (c) colestipol 5 g b.d., and (d) colestipol 7.5 g b.d. Subjects were maintained on a constant repeating solid diet throughout the 6-day study period, and colestipol was ingested 30 min before breakfast and dinner. No drug was administered on Days 1-3; baseline (pre-treatment) serum bile acid concentration profiles were determined on Day 3. The above treatments were given on Days 4-6, and total serum bile acid concentrations were determined at 30- or 60-min intervals for 10 h on Days 4 and 6. Serum bile acids were measured using a bioluminescence procedure which enzymically measures total 3 alpha hydroxy bile acids. Serum bile acid concentrations were significantly decreased from the pretreatment period by 5.0 and 7.5 g/day as compared to 2.5 g/day or placebo. Differences from the pre-treatment period in the area under the serum bile acid time curve revealed the same trends in the data as analysis of percentage difference (Day 6 vs pre-treatment period) in serum bile acid concentrations. These results indicate that postprandial serum bile acid concentrations are influenced by colestipol in a dose-related manner, with doses of 5 and 7.5 g b.d. having a significantly greater effect than 2.5 g b.d. The dose of 7.5 g b.d. had an identical effect on serum bile acid patterns as a dose of 5.0 g t.d.s., which was previously reported. Our findings also show that changes in serum bile acid concentrations may be used to follow the immediate effects of bile acid sequestration in hypercholes terolaemic subjects, and that the bioluminescence enzyme technique is sufficiently sensitive to detect such changes.

Bile Acids and Salts↗
PubMed1981

Effects of colestipol hydrochloride on cholesterol and bile acids absorption in the rat intestinal tract.

It was clearly shown that colestipol hydrochloride inhibits lymphatic absorption of not only endogenous but also exogenous cholesterol and triglyceride in thoracic duct cannulated rats. Inhibition of cholesterol absorption by colestipol hydrochloride was effectively blocked by administration of cholic acid. It was also suggested that colestipol hydrochloride inactivates bile acids which are essential for cholesterol absorption in the intestinal tract. Administration of colestipol hydrochloride to fasted rats decreased bile flow and biliary secretion of cholesterol and bile acids and increased fecal excretion of bile acids bound to colestipol hydrochloride. These results show that colestipol hydrochloride binds bile acids in the intestinal tract and interferes with bile acids reabsorption.

Administration, Oral↗
PubMed1980

Colestipol: a review of its pharmacological properties and therapeutic efficacy in patients with hypercholesterolaemia.

Colestipol is an anion exchange resin with bile acid sequestering properties resembling those of cholestyramine, another lipid-lowering binding resin. In daily doses of 15 to 30g colestipol reduces total plasma cholesterol concentrations (primarily low density lipoprotein cholesterol) by about 15 to 30%, but plasma triglyceride concentrations may be unchanged or in some patients increased. Thus, like cholestyramine, colestipol is of benefit in patients with primary hypercholesterolaemia without associated hypertriglyceridaemia (type IIa hyperlipoproteinaemia). Colestipol is odourless and tasteless, and is said by some to be more readily tolerated by patients than cholestyramine, leading to improved compliance, but such data has not been documented in most studies. Side effects of colestipol treatment are primarily gastrointestinal in nature since the drug is essentially unabsorbed. As with cholestyramine, colestipol may bind with other concomitantly administered drugs reducing their absorption or enterohepatic recirculation; dosage intervals of other concurrent medications should be adjusted to minimise the potential for such an interaction.

Colestipol↗
PubMed1976

Pediatric familial type II hyperlipoproteinemia: therapy with diet and colestipol resin.

Effects of a low-cholesterol, polyunsaturate-rich diet and a synthetic organic bile sequestrant polymer (U26,597A, colestipol) were studied in 21 children, heterozygous for familial hypercholesterolemia. Total cholesterol, beta-lipoprotein cholesterol, and triglyceride were measured twice on habitual diet, monthly for six months on a low-cholesterol diet, and monthly for six months on low-cholesterol diet plus 10 gm of colestipol per day. Total cholesterol (mean +/- 1 SD) was 295 +/- 37 on habitual diet, 278 +/- 29 on low-cholesterol diet, and fell significantly to 242 +/- 29 mg/100 ml on diet plus colestipol. Low-density lipoprotein (LDL) cholesterol was 234 +/- 37 on habitual diet, 220 +/- 28 on low-cholesterol diet, and fell significantly to 179 +/- 26 mg/100 ml on diet plus drug. Plasma triglyceride levels on habitual diet were 79 +/- 31, remained unchanged on low-cholesterol diet, 86 +/- 22, and were unaffected by low-cholesterol diet plus drug, 85 +/- 17 mg/100 ml. On diet alone, plasma LDL was not normalized (less than 170 mg/100 ml) in any of the 21 children, and cholesterol fell to within normal limits (less than 230 mg/100 ml) in only one child. The combination of diet plus colestipol resin normalized total and LDL cholesterol in 52% of the children. Cholesterol was lowered to a "moderately elevated" range of 230 to 250 mg/100 ml in an additional 14% of the children and LDL was lowered to a range of 170 to 190 mg/100 ml in an additional 29%. In 33% of the children, cholesterol remained greater than 250 mg/100 ml despite diet plus colestipol, while LDL was greater than 190 mg/100 ml in 19%. Colestipol is an effective and well-tolerated cholesterol lowering compound which, in conjunction with diet, may prove to be very useful in the treatment of children heterozygous for familial hypercholesterolemia.

Adolescent↗
PubMed1989

Colestipol-induced changes in LDL composition and metabolism. II. Studies in humans.

We investigated the effect of the bile acid sequestrant, colestipol hydrochloride, on the composition and metabolism of human low density lipoprotein (LDL). Colestipol treatment produced a disproportionate decrease in LDL cholesterol compared to LDL apoB, resulting in a significant decrease in the LDL cholesterol/apoB ratio. Electron microscopy revealed that LDL particles were smaller in size and analytical ultracentrifugation demonstrated that colestipol therapy selectively depleted larger, more buoyant LDL particles of Sf degrees 6-7. Thus, colestipol therapy produced LDL that were smaller in size, more dense, and characterized by a decreased cholesterol to protein ratio. To determine whether the altered LDL had different metabolic properties, autologous LDL was isolated from subjects before and during colestipol therapy and their fractional catabolic rates (FCR) were then simultaneously determined in the same patient while on therapy. Eight LDL turnover studies comparing the catabolism of LDL isolated during therapy (Rx-LDL) and LDL isolated off therapy (Con-LDL) were performed in six subjects. All subjects responded to colestipol treatment, with an average 29% fall in LDL cholesterol. In four of six subjects, and in six of eight studies, the FCR of Rx-LDL was substantially slower than that of Con-LDL. These studies demonstrate that a drug intervention may alter subpopulations of LDL particles in such a way that overall LDL composition is changed. This alteration may independently affect the intrinsic metabolic behavior of the LDL. We suggest that such drug- (or dietary-) induced changes in LDL composition need to be considered in kinetic studies designed to assess the overall impact of the perturbation being studied.

Adult↗
PubMed1994

The effects of cholestyramine and colestipol on the absorption of diclofenac in man.

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.

Absorption↗
PubMed1989

Impaired absorption of tetracycline by colestipol is not reversed by orange juice.

Nine volunteers received a 500 mg oral dose of tetracycline hydrochloride in three trials: A: With 180 ml water; B: With 30 gm colestipol in 180 ml water; C: With 30 gm colestipol in 180 ml orange juice. Tetracycline concentrations in multiple urine samples collected during 48 hours after each dose were determined by high pressure liquid chromatography. The three trials did not differ significantly in 48 hour cumulative urine volume (3086 vs 3207 vs 3194 ml for Trials A, B, and C). However, the three trials differed significantly in 48 hour excretion of tetracycline (F = 28.2; P less than .001). During Trial A, mean excretion was 237 mg; this was significantly (P less than .05) reduced to 109 mg in Trial B and 104 mg in Trial C. However, Trials B and C were not different. Thus, coadministration of tetracycline with colestipol significantly impairs tetracycline absorption by more than 50%. Mixing colestipol with orange juice does not alter colestipol-induced impairment of tetracycline absorption.

Adult↗
PubMed1993

In vitro studies to investigate the reasons for the low potency of cholestyramine and colestipol.

The association rates, dissociation rates, and equilibrium binding of bile acids with cholestyramine and colestipol were measured under physiological conditions with the most abundant bile acids found in humans. Cholestyramine and colestipol equilibrated with the bile acids (5 mM) within 1 h and they bound > 58% and > 17% of the bile acid, respectively, when at equilibrium with physiological concentrations of bile acid (4.3-10.1 mM). However, the conjugated trihydroxy bile acids taurocholic acid and glycocholic acid dissociated rapidly from both cholestyramine and colestipol when the sequestrants, preloaded with the bile acid, were washed with the Krebs-Henseleit buffer. The taurine-conjugated and dihydroxy bile acids dissociated more slowly from cholestyramine and colestipol than the glycine-conjugated and trihydroxy bile acids and, therefore, would be expected to avoid reabsorption to a greater extent by the terminal ileum and colon in vivo. We predict from these results that the reasons for the low potency of cholestyramine and colestipol are that they bind a relatively small proportion of the trihydroxy bile acids in the duodenum and jejunum and that all of the bile acids dissociate to varying extents from the sequestrants in the terminal ileum where the unbound bile acids are reabsorbed by the gut.

Bile↗
PubMed1980

The effects of colestipol when combined with clofibrate in the treatment of severe hyperlipidemia. Short-term and long-term studies.

Twenty-two patients suffering from hyperlipidemia and receiving therapy consisting of a lipid-lowering diet and clofibrate (1 g X 2) were in addition given colestipol hydrochloride (5 g X 3) (Colestid, Upjohn) in a randomized, cross-over study for 2 periods of 6 weeks. Both the cholesterol and the triglyceride concentrations in very low density lipoproteins remained unchanged during the colestipol treatment. The cholesterol concentration in low density lipoproteins decreased by 23% (P < 0.001) and increased in high density lipoproteins by 4% (P < 0.01). In a second part of the project, the effects on the lipoprotein lipids of 15 g of colestipol divided into 1, 2 or 3 daily doses were studied when added to ongoing therapy with clofibrate (1 g X 2) and lipid-lowering diet. When the colespitol was divided into 2 or 3 daily doses, the effects were manifested equally but were less pronounced when 1 dose per day was given. In a third study, 14 patients who were treated with a combination of lipid-lowering diet, clofibrate (1 g X 2) and colestipol hydrochloride (15 g daily) were followed over a 2-year period, during which time the serum cholesterol and triglyceride concentrations were maintained at a reduced level. The fasting blood glucose and serum insulin concentrations were increased during colestipol treatment. Such treatment should therefore not be given to patients with impaired glucose tolerance.

Alkaline Phosphatase↗
PubMed1981

Effects of colestipol, clofibrate, and placebo on plasma lipoproteins of patients with hypercholesterolemia.

To evaluate the effectiveness of colestipol and clofibrate in patients with hypercholesterolemia and normal concentrations of triglycerides, 27 patients were randomized into three groups, and colestipol, clofibrate, and avicel powder placebo were compared for effects on concentration of total plasma lipid and lipoprotein cholesterol and triglyceride in a single blind protocol over 8 mo. Mean pretreatment values for low density lipoprotein (LDL)-cholesterol and very low density lipoprotein (VLDL) triglyceride were 250 mg/dl and 68 mg/dl, respectively. Colestipol (30 g/day) lowered total- and LDL-cholesterol by 25% and 31%k, respectively, while VLDL-triglyceride rose. Overall clofibrate lowered total- and LDL-cholesterol by 13% and 12% while lowering VLDL-triglyceride 21% and VLDL cholesterol by 50%. For clofibrate, certain patients showed a more pronounced effect than others: in seven of nine patients clofibrate lowered both mean total- and LDL-cholesterol by 17% (range 8% to 31%) and 19% (range 10%--44%) respectively, whereas two patients did not respond to clofibrate. High density lipoproteins were not affected by either colestipol or clofibrate in these patients. Thus, while colestipol was more consistently effective, certain hypercholesterolemic patients responded equally well to clofibrate with substantial lowering of total-, LDL-, and VLDL-cholesterol.

Adult↗
PubMed1989

Low-dose colestipol plus fenofibrate: effects on plasma lipoproteins, lecithin:cholesterol acyltransferase, and postheparin lipases in familial hypercholesterolemia.

Effects on plasma lipoproteins, lecithin:cholesterol acyltransferase (LCAT), and postheparin lipase (LPL and HTGL) activities were studied in 18 patients with familial hypercholesterolemia during 8-week treatment periods with colestipol (15 g/d), fenofibrate (0.25 g/d), and colestipol plus fenofibrate. Lipoprotein lipids and apolipoproteins were determined by standard procedures, LCAT by a self-substrate method, and lipases by nonradioisotopic methods. Colestipol and fenofibrate, each given independently, caused similar percentage decreases in LDL cholesterol and apolipoprotein B: -18.4% and -8.6% v -17.4% and -10.6% Colestipol increased the VLDL cholesterol concentration, whereas fenofibrate reduced this parameter but increased HDL cholesterol and apolipoprotein A-I levels. The combination of both drugs led to a substantial fall in LDL cholesterol (-36.8%) and in apolipoprotein B (-28.3%) and maintained the other effects of fenofibrate on VLDL and HDL. Colestipol, given independently or with fenofibrate, produced an increase of the fractional esterification rate of the LCAT enzyme (+25.3% and +36.2%). Fenofibrate stimulated the postheparin LPL enzyme by +16.1% and +21.7%, respectively. This study indicates the complementarity in effectiveness when both drugs were administered together. The appropriate reduction in LDL was combined with the favorable effects on HDL in familial hypercholesterolemia.

Adolescent↗
PubMed1989

Effect of anions on adsorption of bile salts by colestipol hydrochloride.

The Langmuir affinity constant and adsorptive capacity for the adsorption of citrate anion or cholate anion by colestipol hydrochloride at pH 7.5, 37 degrees C, were similar. Prior exposure of colestipol hydrochloride to citrate anion caused the adsorption of cholate anion to decrease slightly in comparison to a control utilizing only cholate anion. The concentration of citrate anion was found to be directly related to the decrease in cholate anion adsorption. Simultaneous exposure of colestipol hydrochloride to citrate and cholate anions at pH 7.5, 37 degrees C, resulted in the same adsorption of cholate anion as sequential exposure to citrate anion followed by cholate anion. Sequential exposure of colestipol hydrochloride to simulated gastric fluid and simulated intestinal fluid containing cholate anion resulted in a small decrease in cholate adsorption which was attributed to competition with phosphate anion in simulated intestinal fluid. Pepsin in the simulated gastric fluid did not affect adsorption of cholate anion from simulated intestinal fluid. Preexposure to components of tomato juice and orange juice also slightly reduced the adsorption of cholate anion by colestipol hydrochloride.

Adsorption↗
PubMed1993

Effectiveness of low-dose lovastatin combined with low-dose colestipol in moderate to severe primary hypercholesterolaemia.

The effect of the combination of low-dose lovastatin and low-dose colestipol was studied among 57 subjects with moderate to severe primary hypercholesterolaemia (total cholesterol > or = 7.0 mmol l-1). Following an 8-week dietary phase, participants were randomized to treatment with 20 mg of lovastatin combined with 5 g or with 10 g of colestipol, or to matching placebo. Baseline total cholesterol was 7.7 +/- 0.9 mmol l-1 after dietary stabilization. Total cholesterol levels were reduced to 5.6 +/- 0.7 mmol l-1 and 5.8 +/- 0.7 mmol l-1 after 4 and 8 weeks of treatment in the lovastatin 5 g-1 colestipol group, and 74% of the subjects achieved the goal of low density lipoprotein (LDL) cholesterol levels of > or = 4.0 mmol l-1. Among the lovastatin 10 g-1 colestipol group, total cholesterol was reduced to 5.4 +/- 0.5 mmol l-1 and 5.5 +/- 0.9 mmol l-1 following 4 and 8 weeks, and 80% of subjects achieved the LDL cholesterol goal. No change was seen in the placebo group. Thus, low-dose combination therapy with lovastatin and colestipol, in conjunction with dietary treatment, is effective in moderate to severe primary hypercholesterolaemia, and is well tolerated.

Adult↗
PubMed1994

The effect of colestipol and cholestyramine on the systemic clearance of intravenous ibuprofen in rabbits.

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 Vd(area)) 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.

Administration, Oral↗
PubMed1996

Low dose colestipol in adolescents with familial hypercholesterolaemia.

The effects of orange flavoured colestipol granules, 10 g/day, in 37 boys and 29 girls aged 10-16 years with familial hypercholesterolaemia were examined first in an eight week double blind, placebo controlled protocol, then in open treatment for 44-52 weeks. All patients were on a low fat diet. Low density lipoprotein cholesterol levels were reduced by 19.5% by colestipol v 1.0% by placebo. Levels of serum folate, vitamin E, and carotenoids were reduced in the colestipol group, but not the vitamin E/cholesterol and carotenoid/cholesterol ratios or serum concentrations of vitamins A and D. After one year of colestipol, two thirds of the participants remained in the study, of whom half took > or = 80% of the prescribed dose. Those who took > or = 80% of the dose had a greater decrease in serum 25-hydroxyvitamin D levels than those who took < 80%. No adverse effects on weight gain or linear growth velocity were observed. Although low dose colestipol effectively reduces low density lipoprotein cholesterol levels, only a minority of adolescents adhered to the new formulation for one year. Folate and possibly vitamin D supplementation is recommended.

Adolescent↗