What is colestipol, and how does it work (mechanism of action)?
- Colestipol is an oral cholesterol-lowering drug
that is not absorbed from the intestine into the body. Rather, it works by
binding to bile acids in the intestine and promoting the elimination of bile
acids in the stool. Bile acids are formed in the
liver from cholesterol,
secreted into bile and with the bile enter the intestine. Most of the bile acids
are reabsorbed from the intestine back into the body to be cycled again through
the liver and bile. By promoting the elimination of bile acids, colestipol
forces the liver to convert more cholesterol into bile acids in order to replace
the lost bile acids. This reduces the levels of cholesterol within the body.
Colestipol works similarly to
- Colestipol was approved
by the FDA in 1977.
What brand names are available for colestipol?
Is colestipol available as a generic drug?
GENERIC AVAILABLE: Yes
Do I need a prescription for colestipol?
What are the uses for colestipol?
- Colestipol is used together with dietary modifications for
the treatment of high blood
- Other less common uses include
diarrhea due to increased intestinal bile acids after some types of
intestinal surgery and 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.
What are the side effects of colestipol?
The most common adverse effect is constipation. Other less frequent side effects are:
- Abdominal cramps
- Abdominal distension
Rarely, ulcers, reduced absorption of nutrients, fatty stools, and
stomach or intestinal bleeding may occur.
Other serious side effects of colestipol include:
- Fecal impaction
- Esophageal obstruction
- Gallbladder inflammation
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What is the dosage for colestipol?
- Colestipol is most often prescribed in 2 to 4 divided doses but may
also be prescribed once daily.
- The usual adult dose is 2-16 gm of tablets
administered once or twice daily or 5-30 grams of granules once daily or 4 times
- Tablets should not be cut, crushed or chewed.
- Granules should be mixed in
three ounces of fluid (water or fruit juice).
Which drugs or supplements interact with colestipol?
- Colestipol binds many different compounds in the gastrointestinal tract, thereby inhibiting their absorption into the body. For
example, colestipol can bind with and decrease the oral absorption of
carbamazepine (Tegretol), diuretics such as
hydrochlorothiazide (found in
Dyazide, Maxzide) and
propranolol (Inderal), tetracyclines,
vitamins (vitamins A, D, and K). Colestipol can bind with and
inhibit the absorption of thyroid hormones. Colestipol also can bind with
ursodiol (Actigall, Urso). Separating the doses of colestipol and these other compounds by
several hours should prevent binding with colestipol. Generally, other
should be administered one hour before colestipol or 4 hours after colestipol is
- 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, may exaggerate the effect of
(Coumadin), 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
separated by at least 4-6 hours.
- Colestipol is closely related to cholestyramine. 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
interactions exist for both drugs and to separate ingestion of colestipol from
the other drugs by several hours. These interactions with cholestyramine
What else should I know about colestipol?
What preparations of colestipol are available?
- Granules: 5 gm/ packet or bulk (5gm/teaspoonful) in canisters
- Tablets: 1 gm.
How should I keep colestipol stored?
Tablets and granules should be stored at room temperature, 20
C to 25 C (68 F to 77 F).