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PubMed1983

Alterations in human serum alkaline phosphatase and its isoenzymes by hypolipidemic agents: colestipol and clofibrate.

Total serum alkaline phosphatase (TSAP) determinations were done as part of the biochemical screening in comparative studies of lipid lowering agents in type lla hyperlipoproteinemic patients. TSAP determinations were made by using a modification of the Bessey-Lowry method and the Statland method. Increases in TSAP following colestipol treatment of 20% (P less than 0.05) and 32% (P less than 0.005) were seen by using the respective methods. Isoenzymatic determinations were done by employing the Statland method and all fractions were increased from baseline levels during colestipol therapy. Clofibrate was associated with 34% (P less than 0.005) and 28% (P less than 0.005) reductions in TSAP activity by using the respective methods; significant reductions in both "bone" and "other" isoenzymatic components occurred. Gamma-glutamyltransferase (gamma GT) results did not consistently reflect TSAP or "liver" isoenzyme results.

Adult↗
PubMed1983

Mevinolin and colestipol stimulate receptor-mediated clearance of low density lipoprotein from plasma in familial hypercholesterolemia heterozygotes.

In subject with heterozygous familial hypercholesterolemia (FH), a 50% deficiency of receptors for plasma low density lipoprotein (LDL) impairs the removal of LDL from plasma and produces hypercholesterolemia. In these patients mevinolin, an inhibitor of 3-hydroxy-3-methylglutaryl-CoA reductase, blocks cholesterol synthesis and lowers plasma LDL levels. To determine the mechanism for the LDL-lowering effect, we administered 131I-labeled LDL intravenously to six FH heterozygotes before and during treatment with mevinolin and calculated the apparent fractional catabolic rate (FCR) and synthetic rate for LDL. After mevinolin treatment, the mean plasma LDL-cholesterol level declined from 262 to 191 mg/dl (27% decrease), the mean FCR for 131I-labeled LDL increased from 0.30 to 0.41 pools per day (37% increase), and the mean calculated synthetic rate for LDL-protein did not change significantly. In one of FH heterozygote with an ileal bypass and in another who received colestipol, the addition of mevinolin caused, respectively, a 41% and 60% decrease in plasma LDL levels and a 60% and 100% increase in the FCR for plasma LDL. The contribution of receptor-dependent pathways to the FCR for plasma LDL was estimated in three FH heterozygotes by simultaneous measurements of the FCR for native 131I-labeled LDL and 125I-labeled glucosylated LDL, which does not bind to LDL receptors. Whereas the removal rate for native LDL increased after mevinolin treatment, the removal rate for glucosylated LDL did not change. The current data suggest that mevinolin alone or mevinolin plus bile acid depletion (i.e., ileal bypass or colestipol therapy) decreases plasma LDL levels primarily by raising the number of LDL receptors and, thus, enhancing the removal of LDL from plasma.

Anticholesteremic Agents↗
PubMed1989

Effect of the bile-acid sequestrant colestipol on postprandial serum bile-acid concentration: evaluation by bioluminescent enzymic analysis.

Chronic ingestion of bile-acid sequestrants has been shown to decrease the serum cholesterol concentration and coronary events in hypercholesterolaemic patients. To develop improved sequestrants, a rapid, convenient method for testing the bile-acid binding efficacy of sequestrants is needed. Serum bile-acid concentrations could be used to detect bile-acid binding by an administered sequestrant, since the serum bile-acid concentration is determined largely by the rate of intestinal absorption in healthy individuals. To test this, serum bile-acid concentrations were measured at frequent intervals over 24 h in five otherwise healthy hypercholesterolaemic subjects during the ingestion of three standard meals, with or without the addition of 5 g colestipol granules administered 30 min before each meal. Total serum bile-acid concentration was measured with a previously reported bioluminescent enzymic assay, that uses a 3 alpha-hydroxysteroid dehydrogenase, an oxido-reductase, and a bacterial luciferase co-immobilized on to Sepharose beads. Bile acids in 1 ml of serum were isolated by solid-phase extraction chromatography with reversed-phase C18 cartridges. Colestipol lowered the postprandial elevation of serum bile acids by one half, with a subsequent decrease in the cumulative area under the curve. The data suggest that measurement of serum bile-acid concentrations by bioluminescence is a rapid, simple way to document the efficacy of bile-acid sequestrants.

Adolescent↗
PubMed1993

Beneficial effects of colestipol-niacin therapy on the common carotid artery. Two- and four-year reduction of intima-media thickness measured by ultrasound.

BACKGROUND: Controlled clinical trials have reported treatment effects evaluated with serial imaging in coronary and femoral but not cervical arteries. The Cholesterol Lowering Atherosclerosis Study, a coronary, cervical, and femoral angiographic trial of colestipol plus niacin, included a pilot study of standardized carotid ultrasound imaging. METHODS AND RESULTS: Seventy-eight subjects had ultrasound studies at baseline, 2, and 4 years. Twenty-four drug and 22 placebo subjects had carotid ultrasound images at baseline, 2, and 4 years with matching cervical angiograms. Computer image processing was applied to ultrasound images of common carotid (far wall) and cervical angiograms. Computer operators were blind to treatment group. Carotid ultrasound measurements were tested for treatment effects and compared with measurements of atherosclerosis in coronary and cervical angiograms. Drug subjects showed significant progressive reduction in carotid thickness at 2 (P = .0001) and 4 years (P = .0001); placebo subjects significantly increased wall thickness at 2 and 4 years. Reduced levels of apolipoprotein B and increased levels of high density lipoprotein cholesterol and apolipoprotein C-III were significant predictors of carotid wall thinning. Ultrasound-measured carotid intima-media thickness was correlated at baseline with visually read coronary angiographic stenosis and at 2 years with a robust computer measurement of mild carotid atherosclerosis. CONCLUSIONS: Common carotid intima-media thickening can be reduced by colestipol-niacin treatment. Two-year image-processed carotid ultrasound trials can provide adequate power with 50 subjects per group to test for this treatment effect.

Adult↗
PubMed1978

Thyroid hormone and thyrotropin levels in patients placed on colestipol hydrochloride.

Bile acid sequestrant resins can bind T4 in vitro and in the gut. Therefore, the effect of colestipol HCl on thyroid function was studied prospectively in 17 subjects with type II hyperlipoproteinemia. Serum T4, T3, T3 resin uptake, and TSH levels were measured before and during therapy. No change in T4 levels and only small transient, but significant, decreases in T3 were noted in a minority of patients; TSH levels did not change. Small increases in T3 resin uptake were noted. We conclude that no major alterations in thyroid function occurred with colestipol therapy.

Colestipol↗
PubMed1981

Familial type II hyperlipoproteinemia with coronary heart disease: effect of diet-colestipol-nicotinic acid treatment.

Heterozygous familial type II hyperlipoproteinemia (F type II) is primarily manifested in hypercholesterolemia (due to low density lipoprotein-cholesterol [LDL-C] elevation) and premature coronary heart disease (CHD). We studied sequentially the effects of low cholesterol-low saturated fat-low simple carbohydrate diet; diet and colestipol, 30 g/day; and diet, colestipol, plus nicotinic acid (NA) 3 to 7 g/day on plasma cholesterol (Ch), LDL-C, triglyceride (TG), high density lipoprotein-cholesterol (HDL-C) and angiographically documented coronary arterial lesions of 32 F type II patients. Effective control of F type II resulted in arresting the progression of angiographically demonstrated coronary arterial lesions.

Adult↗
PubMed1987

Alterations in serum thyroid hormonal indices with colestipol-niacin therapy.

A serial blood-lipid-lowering study at the University of Southern California yielded unexpected findings on routine thyroid function monitoring. After 1 year of combined colestipol and niacin therapy, patients had reduced total serum thyroxine (T4) levels and increased triiodothyronine uptake ratios, an indicator of apparent decreases in thyroxine-binding globulin levels. Calculation of the free T4 index partially but not completely corrected for the apparent decrease in thyroxine-binding globulin, as determined by a relatively small decrease in the free T4 index compared with a large decrease in T4. Sequential sampling, using three separate methods, showed reduced thyroxine-binding globulin levels. The mechanism for these changes is unknown, but the fact that these patients were essentially euthyroid needs emphasis because the use of combined colestipol and niacin therapy is becoming more widespread.

Adult↗
PubMed1982

Colestipol and probucol: treatment of primary and familial hypercholesterolemia and amelioration of atherosclerosis.

Colestipol is a safe, effective, cholesterol-lowering, bile-acid sequestrant that lowers low-density-lipoprotein (LDL) and total plasma cholesterol levels without consistently affecting high-density-lipoprotein (HDL) cholesterol levels. Long-term colestipol therapy in conjunction with diet may reduce xanthoma size, arrest progression of coronary artery atherosclerosis, and may reduce mortality from coronary heart disease. Probucol, a bisphenol cholesterol-lowering drug, is an effective cholesterol-lowering agent that reduces levels of HDL cholesterol, HDL cholesterol, and apoprotein A-1, the major apolipoprotein of HDL. Because HDL cholesterol is independently and inversely associated with development of coronary heart disease, the ramifications of simultaneous lowering of LDL and HDL cholesterol levels by probucol treatment need further study. Long-term, placebo-controlled studies of repetitive coronary arteriography, coronary heart disease morbidity and mortality, or both are needed to ascertain the efficacy of long-term probucol use in relation to development of atherosclerosis.

Arteriosclerosis↗
PubMed1992

[Combined therapy of hyperlipoproteinemia. Colestipol and gemfibrozil in the treatment of heterozygous familial hypercholesterolemia].

Combined concurrent treatment with two or more hypolipidaemic agents is a modern trend in the pharmacotherapy of hyperlipoproteinaemias. Aggressive treatment of hyperlipoproteinaemias can lead not only to the arrest of progression but also to regression of the atherosclerotic process. The authors submit experience assembled with the treatment of 14 heterozygotes with familial hypercholesterolaemia by a combination of colestipol (Colestid Upjohn, Belgium) with gemfibrosil (Loped Parke-Davis, USA), 15 g and 1200 mg resp. per day. One month of administration of this combination of hypolipidaemic agents led to a drop of total cholesterol by 21% and of LDL-cholesterol by 30%. At the same time the authors recorded a marked and statistically significant increase of HDL-cholesterol by 23%. Favourable changes were observed also as regards apolipoprotein concentrations. The apolipoprotein A-1 level increased by 32%, while the level of the atherogenic apolipoprotein B declined by 30%. The triglyceride level declined also. It did not prove possible even by combined treatment to reduce the level of apolipoprotein(a). Combined treatment with colestipol and gemfibrosil was well tolerated by the patients and in none of the patients treatment had to be discontinued because of undesirable side-effects.

Adult↗
PubMed1976

The effects of colestipol on the metabolism of very-low-density lipoproteins in man.

Bile acid-binding resins, currently used for the treatment of Type II hyperlipoproteinemia, decrease LDL cholesterol by 25 to 35 per cent. Elevations of plasma triglycerides sometimes occur with resin therapy, suggesting that alterations in metabolism may not be confined solely to LDL. To characterize the effects of the resins on lipoproteins in greater detail, we carried out two studies using colestipol. In the acute study, seven Type IIA patients were studied on a metabolic ward before and for the first 7 to 10 days after initiation of therapy. Blood samples were drawn after 12 to 14 hour fasts every 1 to 3 days during hospitalization and at frequent intervals thereafter for the first 2 to 6 months of therapy. In the chronic study, 12 Type II patients were studied as outpatients at monthly intervals. Three fasting plasma samples were obtained before therapy and three additional samples were ovtained between 3 and 12 months after commencement of treatment. Lipoprotein quantification of individual plasma samples was performed by combined ultracentrifugal and MnCl2-heparin precipitation techniques. The size distribution of ultracentrifugally isolated VLDL was assessed by column chromatography in Sepharose 2B. In the acute study, LDL-Chol fell 24 to 28 hours after initiation of therapy in each subject. Concomitantly, VLDL-TG rose. By days 5 to 8, mean LDL-Chol of the group had fallen by 30 per cent and mean VLDL-TG had risen by 35 per cent. Although mean VLDL-Chol also rose (by about 14 per cent), since VLDL-TG rose more, VLDL became enriched with respect to TG. At peak triglyceridemia, LDL and HDL were also found to be relatively TG-enriched. Between 7 and 30 days after initiation of therapy, VLDL-TG levels returned to and below baseline as LDL-Chol continued to fall. LDL and HDL compositions also returned toward baseline. On gel filtration chromatography of VLDL, obtained during therapy, a peak, which was not present in baseline samples, appeared in the void volume of the column. The amounts of VLDL eluting in the usual positions were also increased. Thus, acute therapy was accompanied by (1) transient rises in levels of triglyceride-enriched VLDL of apparently larger size, (2) falls in LDL-Chol, and (3) changes in the composition of LDL and HDL. In the chronic study, mean total-Chol fell from 345 to 258 mg. per deciliter and mean LDL-Chol fell from 277 to 188 mg. per deciliter (p less than 0.001 for both comparisons). Total-TG and VLDL-TG were not significantly altered. The compositions of VLDL and HDL were unchanged from pretreatment values while LDL became relatively TG-enriched. These findings suggest that acutely colestipol produced alterations in the metabolism of all lipoproteins, but that with prolonged therapy, the levels of VLDL and HDL returned toward pretreatment levels.

Adult↗
PubMed1990

Anti-atherosclerotic activity of colestipol hydrochloride in SEA quail.

Young, male, SEA (Susceptible to Experimental Atherosclerosis) Japanese quail (Coturnix coturnix japonica) were fed an atherogenic diet consisting of yellow corn meal and soybean meal supplemented with 2% cholesterol and 1% cholic acid. A control group of ten animals was fed the atherogenic diet for eight weeks, and another group was fed the same diet containing 2% colestipol hydrochloride for the same length of time. At the end of the treatment period serum and arterial total cholesterols were measured and extent of macroscopic atherosclerotic lesions assessed. Colestipol hydrochloride treatment significantly reduced both serum and arterial total cholesterol levels by 50 and 59%, respectively. Grossly visible atherosclerosis was significantly reduced by 64%. These data further demonstrate that male SEA quail are an appropriate and relevant small animal model for examining the cardiovascular effects of bile acid sequestrants.

Animals↗
PubMedDate not supplied

Effects of combined therapy with lovastatin and colestipol in heterozygous familial hypercholesterolemia. Effects on kinetics of apolipoprotein B.

This investigation was carried out in 10 male patients with heterozygous familial hypercholesterolemia to determine the effects of combined drug therapy with lovastatin and colestipol on the kinetics of apolipoprotein B (apo B) in low density lipoproteins (LDL) and very low density lipoproteins (VLDL). Drug treatment produced reductions in plasma total cholesterol and LDL cholesterol averaging 41% and 48%, respectively. Levels of LDL apo B declined by only 34%, which resulted in a reduction in LDL cholesterol/apo B ratios. The major change in LDL apo B kinetics was a marked increase in fractional catabolic rate for LDL apo B, while production rates for LDL apo B were not changed. Combined drug therapy likewise produced a striking reduction in VLDL cholesterol. This change was associated with an increased clearance of a slowly catabolized fraction of VLDL apo B. Production rates for total VLDL apo B were unchanged. Overall, the combination of lovastatin and colestipol reduced plasma cholesterol and lipoprotein fractions to an acceptable range, and the primary mechanism appeared to be via an increase in the activity of LDL receptors and not by a reduction in production rates of lipoproteins.

Adult↗
PubMed1987

Beneficial effects of combined colestipol-niacin therapy on coronary atherosclerosis and coronary venous bypass grafts.

The Cholesterol-Lowering Atherosclerosis Study (CLAS) was a randomized, placebo-controlled, angiographic trial testing combined colestipol hydrochloride and niacin therapy in 162 nonsmoking men aged 40 to 59 years with previous coronary bypass surgery. During two years of treatment there was a 26% reduction in total plasma cholesterol, a 43% reduction in low-density lipoprotein cholesterol, plus a simultaneous 37% elevation of high-density lipoprotein cholesterol. This resulted in a significant reduction in the average number of lesions per subject that progressed (P less than .03) and the percentage of subjects with new atheroma formation (P less than .03) in native coronary arteries. Also, the percentage of subjects with new lesions (P less than .04) or any adverse change in bypass grafts (P less than .03) was significantly reduced. Deterioration in overall coronary status was significantly less in drug-treated subjects than placebo-treated subjects (P less than .001). Atherosclerosis regression, as indicated by perceptible improvement in overall coronary status, occurred in 16.2% of colestipol-niacin treated vs 2.4% placebo treated (P = .002).

Adult↗
PubMed1976

Effect of candicidin and colestipol on the testes and prostate glands of BIO 87.20 hamsters.

The oral treatment of groups of aged BIO 87.20 male hamsters, an inbred line of Syrian hamsters that develops spontaneous cystic prostatic hypertrophy, with either the heptaene macrolide, candicidin, or the bile acid-sequestering anion exchange resin, colestipol, resulted in a significant reduction of prostate size and weight. The effect was most prominent in the high dosage (75 mg per kg per day) candicidin group and moderate in the high dosage (400 mg per kg per day) colestipol group. It was observed microscopically that the extreme dilation of the prostatic acini of the untreated control prostate glands was partially prevented by the treatment, resulting in much less distended prostatic acini. Concomitantly, there was a notable decrease of the total cholesterol content of the entire prostate gland and the plasma of the high dosage candicidin group. The relationship of certain aspects of sterol metabolism and the possible prevention of cystic prostatic hypertrophy in this new experimental animal disease model is discussed. The effect of these drugs on the nutritional state of the animal and on the synthesis and metabolism of androgens from the testis are questions that remain to be answered.

Animals↗
PubMed1978

[A comparative study of colestipol and colestyramine in children and adolescents with familial hypercholesterolaemia (author's transl)].

Plasma lipids and lipoproteins were studied in 20 children and adolescents with familial hypercholesterolemia during the administration of two anion exchange resins. All the patients' cholesterol levels had been stabilized by treatment with a cholesterol-lowering diet for at least 12 months. Colestyramin (0.6 g per kg body weight) or Colestipol (0.5 g per kg body weight) were given for eight weeks each in a cross-over design. In 6 children, the study had to be terminated due to gastrointestinal problems. Cholesterol, triglycerides and phospholipids were determined serially in whole serum and in isolated lipoprotein fractions. Apolipoprotein-B was determined by radial immunodiffusion in whole serum and in the LDL-fraction. Total plasma cholesterol and LDL cholesterol were lowered by about 25% from initial values of 290 mg/100 ml and 230 mg/100 ml, respectively and Apo-B was lowered by 20%. Low HDL-cholesterol levels in the patients remained decreased during therapy. Triglyceride and phospholipid levels were not affected by treatment. Efficacy, tolerance and side-effects were similar with both Colestyramin and Colestipol.

Adolescent↗
PubMed1982

The effect of cholestyramine and colestipol on the absorption of hydrochlorothiazide.

The effect of cholestyramine and colestipol on the absorption of a single orally administered dose of 75 mg hydrochlorothiazide was determined. Both urinary excretion and plasma levels of hydrochlorothiazide were measured. Cholestyramine or colestipol administration decreased the total urinary excretion of hydrochlorothiazide by 85 and 43%, respectively. Similar effects were also noted on plasma hydrochlorothiazide levels.

Adolescent↗
PubMed1982

Probucol further lowers the serum cholesterol of colestipol-treated patients with hypercholesterolemia.

When probucol in therapeutic doses is added to the therapeutic regimen of patients previously treated with colestipol and diet, total and HDL cholesterol levels fell. LDL-C/apo B and apo AI/apo AII ratios also fell. One can conclude from these findings that probucol works by different mechanism than does colestipol, and that in addition to lowering levels of lipoproteins it also produces changes in the compositions of both LDL and HDL. The significance of these findings for the prevention or treatment of atherosclerosis is unknown.

Adult↗
PubMed1975

Colestipol hydrochloride, a new hypolipidemic drug: a two-year study.

Colestipol hydrochloride is an insoluble, nonabsorbable copolymer with bile-acid-binding capacity. It prevents reabsorption of cholates from the intestinal tract into the enterohepatic circulation causing a net loss of bile acids, and therefore of cholesterol. Sixty subjects with cholesterol levels over 250 mg/100 ml were studied for 104 weeks. Patients with normal phenotypes, types 2,3, and 4, were given 5 gm three times daily and experienced an average drop of 40 mg/100 ml (14%). While patients with types 2,3, and 4 hyperlipidemia responded effectively, cholesterol levels in type 2 patients dropped earliest and most consistently with an average decrease of 58 mg/100 ml (19%). A comparable group of patients with hyperlipidemia taking placebo showed on average no change in serum cholesterol. Serum triglyceride values were not altered significantly. The resin is not absorbed from the gastrointestinal tract and produces a slight increase in fecal volume. Results of chemistries, enzyme assays, prothrombin times, hematology, and urinalysis and body weights wer unaltered. There was no evidence of lithogenic bile production. Colestipol is a tasteless and ordorless copolymer with high acceptability. Side effects were limited to occasional bloating, gas, and constipation. The drug is a safe, effective, palatable hypolipedmic agent.

Adult↗