Colestid

Colestid - General Information

Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.

Pharmacology of Colestid

Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. Only very small amounts of bile acids are found in normal serum. Colestid hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion.

Colestid for patients

COLESTID Tablets may be larger than pills you have taken before. If you have had swallowing problems or choking with food, liquids or other tablets or capsules in the past, you should discuss this with your doctor before taking COLESTID Tablets. It is important that you take COLESTlD Tablets correctly:

1. Always take one tablet at a time and swallow promptly.
2. Swallow each tablet whole. Do not cut, crush, or chew the tablets.
3. COLESTID Tablets must be taken with water or another liquid that you prefer. Swallowing the tablets will be easier if you drink plenty of liquid as you swallow each tablet.

Difficulty swallowing and temporary obstruction of the esophagus (the tube between your mouth and stomach) have been rarely reported in patients taking COLESTID Tablets. If a tablet does get stuck after you swallow it, you may notice pressure or discomfort. If this happens to you, you should contact your doctor. Do not take COLESTID Tablets again without your doctor's advice.
If you are taking other medications, you should take them at least one hour before or four hours after taking COLESTID Tablets.

Colestid Interactions

Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids. In vitro studies have indicated that colestipol hydrochloride binds a number of drugs. Therefore, COLESTlD Tablets may delay or reduce the absorption of concomitant oral medication. The interval between the administration of COLESTID Tablets and any other medication should be as long as possible. Patients should take other drugs at least one hour before or four hours after COLESTID Tablets to avoid impeding their absorption.

Repeated doses of colestipol hydrochloride given prior to a single dose of propranolol in human trials have been reported to decrease propranolol absorption. However, in a follow-up study in normal subjects, single-dose administration of colestipol hydrochloride and propranolol and twice-a-day administration for 5 days of both agents did not affect the extent of propranolol absorption, but had a small yet statistically significant effect on its rate of absorption; the time to reach maximum concentration was delayed approximately 30 minutes. Effects on the absorption of other beta-blockers have not been determined. Therefore, patients on propranolol should be observed when COLESTID Tablets are either added or deleted from a therapeutic regimen.

Studies in humans show that the absorption of chlorothiazide as reflected in urinary excretion is markedly decreased even when administered one hour before colestipol hydrochloride. The absorption of tetracycline, furosemide, penicillin G, hydrochlorothiazide, and gemfibrozil was significantly decreased when given simultaneously with colestipol hydrochloride; these drugs were not tested to determine the effect of administration one hour before colestipol hydrochloride.

No depressant effect on blood levels in humans was noted when colestipol hydrochloride was administered with any of the following drugs: aspirin, clindamycin, clofibrate, methyldopa, nicotinic acid (niacin), tolbutamide, phenytoin or warfarin. Particular caution should be observed with digitalis preparations since there are conflicting results for the effect of colestipol hydrochloride on the availability of digoxin and digitoxin. The potential for binding of these drugs if given concomitantly is present. Discontinuing colestipol hydrochloride could pose a hazard to health if a potentially toxic drug that is significantly bound to the resin has been titrated to a maintenance level while the patient was taking colestipol hydrochloride.

Bile acid binding resins may also interfere with the absorption of oral phosphate supplements and hydrocortisone.

Colestid Contraindications

COLESTID Tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components.

Additional information about Colestid

Colestid Indication: For use, as adjunctive therapy to diet, for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.
Mechanism Of Action: Colestid is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.
Drug Interactions: Anisindione The gastro-intestinal binding agent decreases the anticoagulant effect
Dicumarol The gastro-intestinal binding agent decreases the anticoagulant effect
Acenocoumarol The gastro-intestinal binding agent decreases the anticoagulant effect
Warfarin The gastro-intestinal binding agent decreases the anticoagulant effect
Digoxin The resin decreases the effect of digoxin
Fluvastatin Increased/decreased effect according to spacing
Hydrocortisone Cholestyramine decreases the effect of hydrocortisone
Levothyroxine The resin decreases the absorption of thyroid hormones
Liothyronine The resin decreases the absorption of thyroid hormones
Raloxifene The resin decreases the effect of raloxifene
Liotrix The resin decreases the absorption of the thyroid hormones
Thyroglobulin (Tg) The resin decreases the absorption of the thyroid hormones
Ursodeoxycholic acid The resin decreases the effect of ursodiol
Food Interactions: Take with food.
Generic Name: Colestipol
Synonyms: Colestipolum [INN-Latin]
Drug Category: Anion Exchange Resins; Antilipemic Agents
Drug Type: Small Molecule; Approved

Other Brand Names containing Colestipol: Cholestabyl; Colestid;
Absorption: Not absorbed from the gastrointestinal tract.
Toxicity (Overdose): Oral LD₅₀ in rats is > 1000 mg/kg. Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colestipol is not absorbed, the risk of systemic toxicity is low.
Protein Binding: Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Biotransformation: Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Half Life: Not Available
Dosage Forms of Colestid: Tablet Oral
Granule Oral
Chemical IUPAC Name: N'-(2-aminoethyl)-N-[2-(2-aminoethylamino)ethyl]ethane-1,2-diamine; 2-(chloromethyl)oxirane
Chemical Formula: C11H28ClN5O
Colestipol on Wikipedia: https://en.wikipedia.org/wiki/Colestipol
Organisms Affected: Humans and other mammals