Colestipol

Bile Acid Sequestrants. The bile acid binding resins, colestipol [26658424] and cholestyramine, ate also effective in controlling semm cholesterol levels (150). Cholestyramine, a polymer having mol wt > ICf, is an anion-exchange resin. It is not absorbed in the gastrointestinal tract, is not affected by digestive enzymes, and is taken orally after being suspended in water (151). 

Because colestipol and cholestyramine are not absorbed, but simply pass through the body by the GI tract, few severe side effects occur. Patients often complain of distaste and constipation, however. More severe side effects such as GI bleeding ate relatively uncommon (151). 

Endomethylene-A -tetrahydro benzaldehyde Cyclothiazide Epibromohydrin Carteolol Epichlorohydrin Acebutolol Atenolol Befunolol Betaxolol HCI Bufetrol Bunitrolol Bupranolol Carazolol Carnitine Celiprolol Colestipol Cromolyn sodium I ndenolol Mazindol Mepindolol Metoprolol tartrate Nadolol Nifuratel Oxprenolol Penbutolol Practolol Propafenone HCI Propranolol HCI Viloxazine HCI Xanthinol niacinate Epinephrine... 

Cliolestyramine (Questran) and colestipol (Colestid) are examples of bile acid sequestrants. Bile, which is manufactured and secreted by the liver and stored in the gallbladder, emulsifies fat and lipids as these products pass through the intestine Once emulsified, fats and lipids are readily absorbed in the intestine These drug bind to bile acids to form an insoluble substance that cannot be absorbed by the intestine, so it is secreted in the feces. With increased loss of bile acids, the liver uses cholesterol to manufacture more bile This is followed by a decrease in cholesterol levels. 

Colestipol granules The prescribed dose must be mixed in liquids, soup, cereals, carbonated beverages, or pulpy fruits. The granules will not dissolve. Therefore, when mixing widi a liquid, slowly stir die preparation until ready to drink. Take the entire drug, rinse die glass with a small amount of water, and drink. 

When administered with cholestyramine or colestipol there is a decreased absorption of the oral thyroid preparations. These drugs should not be administered within 4 of 6 hours of the thyroid hormones. When administered with the oral anticoagulants there is an increased risk of bleeding. It may be advantageous to decrease the dosage of the anticoagulant when a thyroid preparation is prescribed. There is a decreased effectiveness of the digitalis preparation if taken with a thyroid preparation. 

Colestipol 5 g packets 1 g tablets 5-30 g/day as a single dose or divided 2-16 g/day as a single dose or divided ... 

Cholestyramine, colestipol, and colesevelam are the bile acidbinding resins or sequestrants (BAS) currently available in the United States. Resins are highly charged molecules that bind to bile adds (which are produced from cholesterol) in the gut. The resin-bile acid complex is then excreted in the feces. The loss of bile causes a compensatory conversion of hepatic cholesterol to bile, reducing hepatocellular stores of cholesterol resulting in an up-regulation of LDL receptors to replenish hepatocellular stores which then result in a decrease in serum cholesterol. Resins have been shown to reduce CHD events in patients without CHD.26... 

Korhonen T, FIannukseia ML, Seppa-nen S, Kervinen K, Kesaniemi YA, Sa-volainen MJ. The effect of the apolipo-protein E phenotype on cholesteryl ester transfer protein activity, plasma lipids and apolipoprotein A I levels in hyperch-olesterolaemic patients on colestipol and lovastatin treatment. Eur J Clin Pharmacol 1999 54 903-910. 

Fed diets containing 10 mg PCP/kg for 14 days, then 21 days on PCP-free diets containing either no additives, 5% mineral oil, or 5% colestipol hydrochloride Eggs received single injected dose... 

Body burden at 14 days was 362 pg/bird or 1.1 pg/kg BW. After 21 days, body burdens were 255 pg/bird in no-additive diet and nondetectable levels of <0.7 pg/bird in mineral oil and colestipol additive diets (Polin etal. 1986)... 

Polin, D., B. Olson, S. Bursian, and E. Lehning. 1986. Enhanced withdrawal from chickens of hexachloroben-zene (HCB) and pentachlorophenol (PCP) by colestipol, mineral oil, and/or restricted feeding. Jour. Toxicol. Environ. Health 19 359-368. 

Cholestyramine, colestipol, orlistat, or mineral oil decrease vitamin D absorption Might induce hypercalcemia with thiazide diuretics in hypoparathyroid patients... 

Bile Acid Resins (Cholestyramine, Colestipol, Colesevelam)... 

Colestipol hydrochloride Bulk powder/5-g packets 10 g twice daily 30 g... 

The gritty texture and bulk may be minimized by mixing the powder with orange drink or juice. Colestipol may have better palatability than cholestyramine because it is odorless and tasteless. Tablet forms should help improve adherence with this form of therapy. 

Interactions Antacids ciclosporin colestipol druas metabolized bv cytochrome P450 3A4 fibrates oral-contraceptiyes warfarin niacin erythromycin diaoxin azole-antifunaals... 

Currently available BAS include cholestyramine, colestipol and colesevelam hydrochloride (colestimide). Cholestyramine comprises a long-chain polymer of styrene with divinylbenzene trimethylbenzylammonium groups, whereas colestipol is a long-chain polymer of l-chloro-2,3-epoxypropane with diethylenetriamine. Colesevelam HCl is poly(allylamine hydrochloride) cross-linked with epichlorohydrin and alkylated with 1-bromodecane and 6-bromo-hexyl-trimethylammonium bromide. Bile-acid binding is enhanced and stabilised in the latter compound by long hydrophobic sidechains, increased density of primary amines, and quaternary amine sidechains. For this reason, colesevelam HCl exhibits increased affinity, specificity and capacity to bind bile acids compared with the other BAS. Colesevelam HCl also binds dihydroxy and trihydroxy bile acids with equal affinity, contrasting with cholestyramine and colestipol that preferentially bind dihydroxy bile acids (CDCA and deoxycholic acid). The latter BAS can lead to an imbalance towards trihydroxy bile acids and a more hydrophilic bile-acid pool. 

Drugs (B). Colestyramine and colestipol are nonabsorbable anion-exchange resins. By virtue of binding bile acids, they promote consumption of cholesterol for the synthesis of bile acids the 2000 Thieme... 

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