GENERIC NAME: colestipol

BRAND NAME: Colestid

DRUG CLASS AND MECHANISM: Colestipol is an oral cholesterol-lowering agent. It is not absorbed from the intestine and into the body. Colestipol attaches to bile acids that are made by the liver and secreted through the bile into the intestine. This binding in the intestine and subsequent elimination in the stool of bile acids reduces the bile acids that are absorbed from the intestine and forces the liver to make more bile acids to replace the lost bile acids. Since bile acids are made from cholesterol, the liver uses up cholesterol to form bile acids. This reduces the amount of cholesterol in the body. Colestipol works similarly to cholestyramine (Questran). Colestipol was approved by the FDA in 1977.

PRESCRIPTION: yes

GENERIC AVAILABLE: yes

PREPARATIONS: Granules in 5gm packets or in bulk (5gm per teaspoonful) in canisters; tablets: 1 gm.

STORAGE: Tablets and granules should be stored below at room temperature, 15-30°C (59-86°F).

PRESCRIBED FOR: Colestipol is used for the treatment of high cholesterol in conjunction with dietary control; for the treatment of diarrhea due to increased intestinal bile acids after some types of surgery; for the treatment of itching associated with partial obstruction to the flow of bile due to liver disease. (The itching is believed to be due to the accumulation of bile acids in the body.)

DOSING: Colestipol is most often prescribed in 2 to 4 divided doses but may also be prescribed once daily. The usual dose is 5 grams (1 packet per dose), but may be increased if necessary. In general, the dose is determined by the degree of cholesterol reduction and the patient's tolerance of the medication.

DRUG INTERACTIONS: Colestipol binds many different compounds in the gastrointestinal tract, thereby inhibiting the absorption of the other compounds. Colestipol can bind with and decrease the oral absorption of carbamazepine (Tegretol), diuretics such as hydrochlorothiazide (found in Dyazide, Maxzide) and furosemide (Lasix), propranolol (Inderal), tetracyclines, and fat-soluble vitamins (vitamins A, D, and K). Colestipol can bind with and inhibit the absorption of thyroid hormones. Colestipol also can bind with ursodiol. Separating the doses of colestipol and these other compounds by several hours should prevent binding with colestipol.

Colestipol binds to vitamin K, a vitamin which is required by the liver to make the factors that allow blood to clot. Colestipol, by reducing the action of vitamin K further, may exaggerate the effect of warfarin , reducing the body's ability to form blood clots. This interaction could lead to abnormal bleeding. On the other hand, colestipol can bind with warfarin directly and inhibit the absorption of warfarin. To avoid this interaction, doses of warfarin and colestipol should be staggered by at least 4-6 hours.

Colestipol is closely related to cholestyramine, another resin. Cholestyramine has been more extensively studied than colestipol. Therefore, there are several drug interactions which have been described with cholestyramine, for which data is lacking with colestipol. It would be prudent to assume that a similar interaction exists and to separate ingestion of colestipol from the other drugs by several hours. These interactions with cholestyramine include: acetaminophen (Tylenol), amiodarone (Cordarone), gemfibrozil (Lopid), pravastatin (Pravachol), piroxicam (Feldene), imipramine (Tofranil), glipizide (Glucotrol), and others.

PREGNANCY: It is not known whether or not colestipol causes harm to the fetus if taken during pregnancy although it is not absorbed and, therefore, does not cross the placenta to the fetus. However, colestipol is known to interfere with the absorption of fat-soluble vitamins (vitamins A, D, and K), which may lead to deficiencies even with supplementation. Colestipol, therefore, can be used in pregnancy if the physician feels that it is clearly indicated.

NURSING MOTHERS: It is not known if colestipol is secreted in breast milk although it is highly unlikely since its absorption is so poor. Therefore, the physician needs to decide whether to instruct the pregnant woman to discontinue nursing or the drug or to continue both nursing and drug, accepting the possible risk.

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