colesevelam, Welchol
GENERIC name: colesevelam
BRAND name: Welchol
DRUG CLASS AND MECHANISM: Colesevelam is an oral drug that
lowers cholesterol levels in the
blood. It also improves control of blood sugar in
type 2 diabetes.
Cholesterol made by the liver or from the food we eat can be converted into
bile acids by the liver. The bile acids are secreted by the liver into the bile
and enter the intestine with the bile. In the intestine the bile acids assist
with the digestion of fat. Some of the bile acids are excreted from the body
with the stool, but the majority of bile acids are absorbed from the intestine
into the blood, are removed by the liver from the blood, and are re-secreted
into the bile. Colesevelam binds bile acids in the intestine and causes more of
the bile acids to be excreted in the stool. This reduces the amount of bile
acids that returns to the liver and forces the liver to make more bile acids to
replace the bile acids lost in the stool. In order to make more bile acids, the
liver converts more cholesterol into bile acids, and this lowers the level of
cholesterol in the blood. Colesevelam is not absorbed into the body.
The mechanism whereby colesevelam improves blood sugar levels in people with
diabetes is
unknown.
GENERIC: No
PRESCRIPTION: Yes
PREPARATIONS: Tablet: 625 mg, white.
STORAGE: Colesevelam should be stored at room temperature, away from heat and light, and out of the reach of children.
PRESCRIBED FOR: Colesevelam
is used to treat high blood cholesterol levels, especially high levels of
LDL-cholesterol ("bad cholesterol"). It does not lower cholesterol as much as
the statin class of drugs, but when used in combination with a statin, it lowers cholesterol levels further than the statin alone. Colesevelam is used in combination with other drugs for treating type 2 diabetes such as metformin, sulfonylureas, or insulin to further lower blood sugar levels.
DOSING: Colesevelam usually is taken one or two times daily with a meal.
DRUG INTERACTIONS: Colesevelam reduces the absorption of cyclosporine,
glyburide (Micronase, DiaBeta,
Glynase, Prestab), levothyroxine sodium (Synthroid, Levoxyl, Levothroid,
Unithroid), and oral contraceptives containing ethinyl estradiol or norethindrone by binding to them in the stomach and preventing their absorption into the body. Colesevelam also may reduce the activity of
phenytoin (Dilantin) and
warfarin (Coumadin). Drugs that interact with colesevelam should be administered four hours before the administration of colesevelam and, when possible, drug levels should be monitored.
PREGNANCY: Although colesevelam has not been studied in
pregnant women, it has not been shown to cause birth defects or other problems in animal studies.
NURSING MOTHERS: It is not known whether colesevelam passes into breast milk, but very little colesevelam is absorbed from the intestine and is available for secretion in breast milk. Although most medicines pass into breast milk in small amounts, many of them may be used safely while
breastfeeding. Colesevelam may decrease the absorption of certain vitamins, which are important during breastfeeding. Mothers who are taking colesevelam and who wish to breast-feed should discuss this with their doctor.
SIDE EFFECTS: Colesevelam usually is well-tolerated. Side effects may include constipation, upset stomach, indigestion, headache, stomach pain, or diarrhea.
Reference: FDA Prescribing Information
Last Editorial Review: 1/5/2011
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