The P-I-E-N-O Parkinsn's List Drug Database
colestipol / ColestidTM
CHOLESTEROL CONTROL:
Description: Colestipol hydrochloride is an oral antilipemic agent. It is a nonabsorbable bile acid sequestrant similar in action to cholestyramine. Colestipol and cholestyramine appear to be equal in their cholesterol-lowering effects. Since the development and release of HMG-CoA-reductase inhibitors, colestipol use has declined. Colestipol, however, is not absorbed and has a safer toxicity profile than do other antilipemics, thus making it a desirable agent in children and pregnant women. Colestipol was approved by the FDA in 1977.
Mechanism of Action: By releasing chloride, colestipol combines with bile acids in the intestine to form insoluble, nonabsorbable complexes that are excreted in the feces along with unchanged resin. Since cholesterol is the major precursor of bile acids, the removal of bile acids from the enterohepatic circulation increases the catabolism of cholesterol to form bile acids. The loss of bile acids stimulates a compensatory increase in the hepatic production of cholesterol. It is postulated that the increased hepatic production of cholesterol falls short of the amount lost, leading to a net decrease in circulating cholesterol. This effect, however, has not been clearly shown. It is likely that colestipol's cholesterol-lowering effect is related to increased catabolism of low-density lipoprotein (LDL). Clinically, colestipol lowers LDL and total cholesterol, but has little effect on HDL cholesterol. Triglycerides increase with colestipol therapy. Thus, colestipol is appropriate for type II hyperlipoproteinemia in patients without hypertriglyceridemia.
Colestipol can bind to substances other than bile acids, especially if they undergo enterohepatic recirculation as does digitoxin. While colestipol has been used clinically to accelerate the clearance of digitoxin in cases of toxicity, charcoal and Fab fragments are probably preferred agents for this use. Other agents that bind readily with colestipol include chenodiol, chlorothiazide, digoxin, fat-soluble vitamins, penicillin G, and tetracycline.
Pharmacokinetics: Since colestipol is not absorbed orally, serum concentrations and half-life parameters do not apply. Colestipol is not affected by digestive enzymes. It is eliminated in the stool. Reduction of the plasma cholesterol concentration usually is seen within 24-48 hours of starting therapy, and maximum effects are achieved within 1 month.
CONTRAINDICATIONS/PRECAUTIONS: Colestipol is contraindicated in patients with cholelithiasis or complete biliary obstruction. In these conditions, secretion of bile acids into the GI tract is impaired. Colestipol is also contraindicated in patients with primary biliary cirrhosis since it can further raise serum cholesterol.
Colestipol is relatively contraindicated in constipated patients because of the danger of fecal impaction. Colestipol is relatively contraindicated in patients with coronary artery disease or hemorrhoids because constipation can aggravate these conditions.
Because colestipol can bind with vitamin K, colestipol is relatively contraindicated in patients with any preexisting bleeding disorder or coagulopathy (see Interactions).
Because colestipol can bind with exogenous thyroid hormones if administered simultaneously (see Interactions), colestipol is relatively contraindicated in patients with hypothyroidism.
Colestipol is relatively contraindicated in patients with renal disease because colestipol releases chloride, which can increase the risk of developing hyperchloremic metabolic acidosis.
It is unknown whether or not cholestipol causes fetal harm if taken during pregnancy. Adequate studies have not been done. Cholestipol should only be used during pregnancy if the potential benefits justify the potential added risk to the fetus.
DRUG INTERACTIONS: Colestipol can bind with and possibly decrease the oral absorption of carbamazepine, thiazide diuretics, oral furosemide, oral penicillin G, propranolol, oral tetracyclines, orally administered vancomycin, and fat-soluble vitamins including vitamin A, vitamin D, and vitamin K or orally- administered phytonadione. Colestipol can bind with and delay or prevent absorption of thyroid hormones including dextrothyroxine. Colestipol also can bind with ursodiol. Staggering the doses of these agents by several hours should prevent binding with colestipol.
Colestipol may affect the hypoprothrombinemic actions of warfarin. Colestipol can bind with vitamin K in the diet, impairing vitamin K absorption, which, in turn, may increase warfarin's hypoprothrombinemic effect. Conversely, colestipol can bind with warfarin directly and impair warfarin bioavailability, although the effects of colestipol on warfarin absorption are less pronounced than the ability of cholestyramine to bind with warfarin. To avoid altering warfarin pharmacokinetics, doses of warfarin and colestipol should be staggered by at least 4-6 hours. Colestipol should be prescribed cautiously to any patient receiving warfarin, although colestipol may be an acceptable alternative to cholestyramine in a patient receiving warfarin who also requires therapy with a bile acid sequesterant.
Colestipol can bind with digitoxin and enhance digitoxin clearance. Because digitoxin undergoes enterohepatic recirculation, staggering the administration times of each agent may not prevent this drug interaction. Colestipol should be used cautiously in patients receiving digitoxin. Patients should be observed for loss of digitalis effect if colestipol is added or for digitalis toxicity if colestipol is discontinued in a patient stabilized on cardiac glycosides. Digoxin also may be similarly affected, albeit to a lesser degree since it undergoes less enterohepatic recirculation than digitoxin.
ADVERSE REACTIONS: The most common adverse reactions to colestipol therapy are GI- related. Constipation occurs in 10% of patients. It is usually mild and transient but can produce fecal impaction, requiring medical attention. Every effort should be made to avert possible constipation; the patient should be instructed to drink plenty of water and include additional fiber in the diet. Colestipol can worsen preexisting constipation or aggravate hemorrhoids. Bleeding hemorrhoids or blood in the stool occur infrequently and may result from severe constipation. Other adverse GI reactions include abdominal pain, eructation, flatulence, nausea/vomiting, diarrhea, or steatorrhea.
There have been rare reports of cholelithiasis, cholecystits, GI bleeding or peptic ulcer. A causal effect has not been established.
Because colestipol can bind with and impair the absorption of dietary vitamin K, hypoprothrombinemia can occur.
Other adverse reactions have been reported with colestipol. Cardiovascular effects are rare such as angina and tachycardia. There have been infrequent reports of a hypersensitivity rash, with urticaria and dermatitis. Reports include musculoskeletal aches and pains in the extremities, joint pain and arthritis, and backache. Neurologic effects include headache and occasional reports of dizziness or lightheadedness, and insomnia. Other infrequent effects include anorexia, shortness of breath, and swelling of the hands or feet.
PATIENT INFORMATION:
What do colestipol tablets do?
Colestipol (ColestidTM ) absorbs and combines with bile acids, which increases removal of cholesterol. It lowers blood fats and cholesterol for patients who are at risk of getting heart disease or a stroke. It is only for patients whose cholesterol level is not controlled by diet. It is not a cure. Generic colestipol tablets are not yet available.
What should my doctor, dentist, or pharmacist know before I take colestipol?
They need to know if you have any of these conditions:
How should I take this medicine?
Take colestid tablets by mouth. Follow the directions on the prescription label. Swallow the tablets whole with a drink of water; do not cut, crush or chew. Drink at least 4 fluid ounces of water with each dose of colestipol. Take your doses at regular intervals. Do not take your medicine more often than directed.
Special precautions for use in children:
This medicine is not for children.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.
What other medicines can interact with colestipol?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking colestipol?
Serious side effects with colestipol include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with colestipol include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take colestipol?
Colestipol will not cure your condition, but taken regularly it will help keep down your cholesterol level. Visit your doctor for regular checks on your progress. Do not stop taking colestipol, except on your doctor's advice.
Colestipol is only part of a total cholesterol-lowering program. Your doctor or dietician can suggest a low-cholesterol and low- fat diet that will reduce your risk of getting heart and blood vessel disease. Avoid alcohol and smoking, and keep a proper exercise schedule.
Drink plenty of water while you are taking colestipol, to reduce the chance of getting constipated. Increase the amount of fiber in your diet. Ask your doctor for advice if you are constipated.
Take colestipol at least 1 hour before, or 4 hours after any other medicines that you are taking, to avoid colestipol interfering with their absorption.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30C (59 and 86F). Protect from moisture. Throw away any unused medicine after the expiration date.
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