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PubMed1986

[Experimental study in the rabbit of the effect of cholestyramine in the treatment of infectious diarrhea caused by cholera].

Cholestyramine is a non-absorbable anion exchange resin. Cholestyramine treatment of new born's infectious diarrhea has been shown to be effective. Cholera toxin induces, in the adult rabbit ileal loop, histological, water electrolytes and enzymatic modifications similar to that observed in patients with acute infectious diarrhea. Using this experimental model, we try to exhibit the reduction of the pathologic secretory action of the toxin on intestinal loop, after contact with the resin. A prolonged contact of the cholera toxin with the resin does not abolish completely the activation of adenyl-cyclase induced by the toxin alone. However significant reduction of goblet cell degranulation, and of the secretory effect allowed to reduce the loss of water and electrolytes.

Animals↗
PubMed1985

Effect of time of administration of cholestyramine on plasma lipids and lipoproteins.

Cholestyramine was administered to 15 men with type II hyperlipoproteinemia in a dosage of 8 gm twice daily. For each subject, the p.m. dose was randomly assigned to one of four approximate time periods: mid-afternoon, 30 minutes before the evening meal, 60 minutes after the evening meal, and at bedtime. The time of the morning dose remained constant throughout the study. Each treatment period lasted eight weeks, and all participants completed all four treatment assignments. There was a significant reduction of both total plasma cholesterol (TPC) and LDL cholesterol (LDL-C) compared to baseline values (p less than 0.001) for all treatment regimens. TPC and LDL-C reduction was greatest when the p.m. dose was taken 30 minutes before the evening meal. This reduction was also significantly greater than when the p.m. dose was taken mid-afternoon (p less than 0.05). There was also a significant increase in triglycerides compared to baseline during all treatment periods (p less than 0.05). These findings indicate that the time of the p.m. dose of cholestyramine is important to obtain the maximum reduction of LDL-C. They also reveal that the most effective dosage schedule is administration immediately prior to the evening meal.

Adult↗
PubMed1972

Stimulatory effect of dietary lipid and cholestyramine on hepatic HMG CoA reductase.

The diurnal cycle of hepatic HMG CoA reductase activity was studied under conditions of controlled feeding where the percentage of dietary lipid, alone or in combination with 2% cholestyramine, was varied. Cholestyramine caused an increase in HMG CoA reductase activity that began soon after feeding started and peaked 6 hr later. In contrast, a diet containing 20% corn oil was a much weaker inducer of the enzyme but caused a prolonged elevation that began late in the fasting part of the cycle. These patterns suggest two different mechanisms of action.

Alcohol Oxidoreductases↗
PubMed1974

Restraint of cholesterol accumulation in tissue pools associated with drastic short-term lowering of serum cholesterol levels by clofibrate or cholestyramine in hypercholesterolemic swine.

In this study, young growing swine were made hypercholesterolemic (~300 mg/dl) by feeding milk and eggs for 7 wk. They were then divided into three groups (untreated, clofibrate-treated, and cholestyramine-treated), and the diet was continued for an additional 3-4 wk. A cholesterol balance study was carried out in the terminal week. When the swine were killed, the total carcass content of cholesterol was determined, as well as contents of individual tissues. Both drugs caused a 50% reduction in serum cholesterol levels. The total carcass cholesterol contents were significantly lower in both treatment groups than in the untreated group. The difference was due largely to lower concentrations in the plasma and in bulk tissues. [4-(14)C] Cholesterol was fed 7 days before the animals were killed, and specific activities of cholesterol in individual tissues were determined terminally. These gave a broad spectrum of values in tissues (excluding central nervous system) ranging rather evenly from 33% of plasma specific activity in the aorta to 100% in some tissues. The balance data suggest that cholestyramine reduces the enterohepatic bile acid pool and cholesterol absorption but increases fecal output of bile acids and total body cholesterol synthesis. The balance data, limited to the terminal week, give no indication of the mode of action of clofibrate. Even synthesis was not significantly lower than in the untreated swine.

Animals↗
PubMed1967

Hypercholesteremia. Treatment with cholestyramine, a bile acid sequestering resin.

The results of administration of cholestyramine to 19 patients for periods of two to 21 months are reported. All patients consistently taking the drug obtained a significant reduction in the serum cholesterol. The average reduction was 26 per cent and the range was from 16 to 52 per cent. Cholestyramine acts as a bile acid sequestering resin, causing an increased loss of bile salts (cholates) in the stool. The drug acts by increasing the normal excretory pathway for cholesterol.

Adult↗
PubMed1970

Use of 3H-labeled triether, a nonabsorbable oil-phase marker, to estimate fat absorption in rats with cholestyramine-induced steatorrhea.

A tritium-labeled glycerol triether was tested as a nonabsorbable oil-phase marker in studies of fat absorption in normal rats and in rats with steatorrhea induced by various doses of cholestyramine. Animals were fed a test meal containing (3)H-labeled triether and (14)C-labeled trilinolein. Fat absorption was estimated in the following three ways: (a) by isotope ratios (the change in (3)H/(14)C in the test meal and in feces); (b) by isotope recovery (the total fecal excretion of (14)C radioactivity); and (c) by chemical recovery (the total fecal fat excretion). Absorption calculated from isotope ratios agreed well with that calculated from isotope recovery over a range of fat absorption of 50-100%, thus validating the use of this lipid marker under these conditions of fat malabsorption. Absorption calculated from chemical recovery was consistently poorer than that calculated from isotope ratios or isotope recovery, thus suggesting that cholestyramine increased the excretion of nondietary (endogenous) fat. Triether may be of value for studying the absorption of compounds present predominantly in the oil phase during digestion and may have significant advantages over other proposed lipid markers.

Carbon Isotopes↗
PubMed1984

Double-blind placebo-controlled clinical trial of microporous cholestyramine in the treatment of intra- and extra-hepatic cholestasis: relationship between itching and serum bile acids.

In order to investigate the effectiveness of microporous cholestyramine in the pharmacological management of intra- and extrahepatic cholestasis, a double-blind placebo-controlled study was carried out in 10 patients. Microporous cholestyramine or placebo 3 g t.i.d. were given orally over a four-week period. The active drug resulted statistically superior to the placebo in reducing itching intensity (p less than 0.01) and serum bile acids (p less than 0.01). A positive linear relationship between itching and serum bile acids (p less than 0.01) was also demonstrated.

Adult↗
PubMed1984

Combined drug therapy--cholestyramine and compactin--for familial hypercholesterolemia.

Combined drug therapy with cholestyramine and compactin was found to be extremely effective against heterozygous cases of familial hypercholesterolemia. With a single drug regimen, compactin at a dosage of 15 mg/day produced a cholesterol reduction of 23% (70 mg/dl) in cases of combined hyperlipidemia, while twice the dosage (30 mg/day) was needed to produce a comparable effect with heterozygous familial hypercholesterolemia. When compaction was combined with cholestyramine (in a 4 g dose three times a day), the cholesterol-lowering effect of compactin was strongly improved with heterozygous familial hypercholesterolemia; half the dosage of compactin was enough to produce the additive effect compared with the effect produced by each single drug regimen.

Anticholesteremic Agents↗
PubMed1983

Effects of calcium, aluminium, magnesium and cholestyramine on hyperoxaluria in patients with jejunoileal bypass.

The urinary excretion of oxalate, calcium, magnesium and citrate as well as the inhibition of calcium oxalate crystal growth in diluted urine was studied in seven patients with hyperoxaluria following jejunoileal bypass. The study was performed on an outpatient basis before and during daily administration of 38 or 113 mmol calcium, 28 mmol of aluminum, 20 mmol of magnesium or 16 g of cholestyramine. Each substance was administered for seven days with a free interval of at least seven days. The mean urinary oxalate excretion was not reduced with any of these regimens. Administration of 38 mmol of calcium per day resulted in increased oxalate and magnesium excretion. Increased excretion of both calcium and citrate was observed during administration of 113 mmol of calcium per day. Calcium and magnesium excretion was increased with aluminium. An increased magnesium excretion was also observed during administration of magnesium, resulting in a decreased calcium/ magnesium ratio. Cholestyramine resulted in increased oxalate and decreased citrate excretion.

Adult↗
PubMed1981

Cholestyramine as an aid to management of prolonged diarrhoea in the hospital drip-room. Preliminary findings.

Two groups of children with diarrhoea of more than 7 days' duration were studied. While the length of stay in hospital of the two groups was similar, there was a significant improvement in the frequency and consistency of the stools of the children given cholestyramine. This improvement was also noted in children with positive stool cultures. Cholestyramine also plays an important role in reducing the number of children or intravenous therapy at any time.

Child↗
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↗
PubMed1978

Effects of cholestyramine and chenodeoxycholic acid on the metabolism of endogenous triglyceride in hyperlipoproteinemia.

Previous studies conducted under basal conditions have suggested a linkage between the formation of plasma triglyceride and the degradation of cholesterol to bile acids. To further examine this relationship, plasma endogenous triglyceride kinetics were determined using [(3)H]glycerol in 26 hyperlipidemic subjects before and during stimulated (cholestyramine treatment) and inhibited (chenodeoxycholic acid treatment) bile acid synthesis. All patients with hyperlipoproteinemia (HLP) type II (n = 9) treated with cholestyramine (12 g daily for 2-4 months) displayed increased apparent biosynthesis (12.8 +/- 1.5 vs. 9.7 +/- 1.2 micro mol kg(-1)hr(-1), mean +/- SEM, P < 0.005) and an elevated apparent fractional turnover rate (0.230 +/- 0.017 vs. 0.176 +/- 0.014 hr(-1), P < 0.001) as determined over a 10-hr period, in spite of essentially unchanged plasma triglyceride concentrations. No consistent effect of this therapy was encountered in the five patients studied with type IV HLP. Chenodeoxycholic acid feeding (1.9 mmol daily for 3-4 months) resulted in a reduced apparent synthesis of plasma triglycerides both in type IIa (n = 5, 7.9 +/- 0.5 vs. 13.1 +/- 1.2 micro mol kg(-1)hr(-1), P < 0.01) and type IV HLP (n = 7, 15.5 +/- 1.8 vs. 23.6 +/- 3.7 micro mol kg(-1)hr(-1), P < 0.02). Furthermore, a 20-25% reduction of the apparent fractional turnover rate was seen, and the plasma concentration of triglycerides was reduced by about 15%. It is concluded that the present experimental conditions that primarily influence cholesterol and bile acid biosynthesis also affect the metabolism of plasma triglycerides-and presumably that of very low density lipoprotein-in a regulatory manner. Hypothetically, this may be achieved via a hepatic pool of newly synthesized cholesterol.

Adult↗
PubMed1980

Effect of cholestyramine-induced bile acid depletion on the hepatobiliary transport of cholephilic organic anions in rats.

Four hours after oral administration of cholestyramine (1.0 g/kg) the biliary output of bile acids decreased to 21 per cent of the control value. The biliary excretion of indocyanine green (ICG; 15--60 mumol/kg i.v.), rose bengal (RB; 15--60 mumol/kg i.v.), bromsulphthalein (BSP; 15--60 mumol/kg i.v.), bromcresol green (BCG;15--60 mumol/kg i.v.) and eosine (EO; 30--120 mumol/kg i.v.) was considerably depressed by cholestyramine pretreatment. The extent and duration of the reduction in the biliary excretion of organic anions in response to bile acid depletion were found to increase with their doses. In contrast, the biliary excretion rates of bromsulphthalein-glutathione conjugate (BSP-GSH; 60--240 mumol/kg i.v.) and amaranth (AM; 60--240 mumol/kg i.v.) remained unchanged following bile acid depletion. The hepatic uptake of the cholephilic agents investigated was not affected by bile acid depletion. It is concluded that the biliary excretion rates of ICG, RB, BSP, BCG and EO are dependent on the excretion rates of endogenous bile acids. The hepatic transport rates of BSP-GSH and AM, however, seem to be relatively insensitive to the biliary output of endogenous bile salts.

Animals↗
PubMed1980

[Prolonged diarrhea in infancy: effect of deconjugated bile acids and cholestyramine action].

527 patients whose ages ranged from 3 months to 5 years, with acute diarrhea were studied. 517 showed satisfactory response to treatment. Diarrhea persisted in 10 patients (2 %) and bile acids were determined in intestinal juice before and after cholestyramine administration. 7 patients showed bile acids deconjugation, 6 of which cured clinically. 3 patients showed no deconjugation, and 1 of them improved after cholestyramine therapy. Side effects of drug were not observed.

Acute Disease↗
PubMed1995

[Cholestyramine for digoxin intoxication].

Cholestyramine, a bile acid sequestering resin, has been reported to bind digitalis in vitro. We gave 4 g every 6 hours to 3 patients with non-life threatening digoxin intoxication. In all 3 serum digoxin concentrations and digoxin half-life decreased: from 50 to 32 hours, from 50 to 10 hours and from 46 to 16 hours in the 3 cases, respectively. Cholestyramine is potentially useful and safe adjunct medication for non-life threatening digoxin intoxication.

Aged↗
PubMed1994

[Vasosan S--a cholestyramine in the treatment of hypercholesterolemia of various etiopathogenesis].

Cholestyramine was used for the first time in the treatment of hypercholesterolaemia by Tenneton in 1960 and it persist in the treatment to the present time. The authors had the opportunity to monitor under clinical conditions the hypolipidaemic action of cholestyramine - the preparation Vasosan (manufactured by AG Chemie, Germany) in the treatment of hypercholesterolaemia of different origin, and also when associated with hypertriacylglycerolaemia. The authors revealed that Vasosan S reduced significantly total cholesterol, LDL cholesterol and apoprotein B even after brief treatment (12 weeks) even when there is also hypertriacylglycerolaemia. The decrease of triacylglycerols is not significant, and the increase of HDL-cholesterol is not significant either. Vasosan does not affect the activity of AST, ALT, ALP and total bilirubin, it is well tolerated and causes few gastrointestinal side-effects which do not call for discontinuation of treatment.

Adult↗
PubMedDate not supplied

[Cholestyramine in a case of a prolonged diarrhea after a partial ileocolectomy].

The author reports the case of a 10 years old female child with history of retrocecal appendicular abscess complicated with terminal ileum and right colon necroses which called for partial ileocoletomy. Following this operation, the patient presented diarrhea which caused a loss in weight of 6 kgs. in two months. Antiacids and diphenoxylate were given with negative results. A low fat diet was then given and the patient recovered 1 kg. in weight, but the diarrhea persisted with high excretion of fats. Thereupon, cholestyramine and a normal diet were given followed, within the next 48 hours, by a remission of the diarrhea; the weight loss was recovered within the next 3 months. At present, the patient is still taking very small doses of cholestyramine with a normal diet.

Administration, Oral↗