Colestid

Bile Acid Sequestrants and Ion-exchange Resins

 
NOTE: Patients receiving colesevelam therapy should also be placed on a standard cholesterol-lowering diet, and this diet should be continued throughout therapy. Serum lipoprotein concentrations should be determined periodically and dosage adjusted according to individual response and established treatment guidelines.

Administer as tablets or as a suspension. To minimize drug interactions, administer other drugs at least 1 hour before or at least 4 hours after colestipol.

Tablets: Instruct patients to take one tablet at a time and promptly swallow whole, using plenty of water or other appropriate liquid. Do not cut, crush, or chew tablets.

Granules for suspension: WARNING: Colestipol flavored granules contain aspartame which is metabolized to phenylalanine. Colestipol suspension should be avoided in patients with phenylketonuria or in patients who must restrict their intake of phenylalanine.
To avoid esophageal irritation or blockage, intestinal blockage or accidental inhalation, do not administer the dry granules. Mix with fluid before administration.
Mix the dose in 90 mL of water, milk, fruit juice, or another noncarbonated beverage and stir until completely mixed. Palatability and compliance may be increased if the entire next day's dose is mixed in the evening and then refrigerated. Complaints of consistency may be minimized by mixing in a heavy or pulpy fruit juice. If a carbonated beverage is used, foaming may be minimized by mixing slowly in a large glass.
Alternatively, the granules may be mixed with cereals, a highly fluid soup, or a pulpy fruit with a high moisture content (i.e., applesauce or crushed pineapple).
To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions.

peptic ulcer / Delayed / 0-1.0
GI bleeding / Delayed / 0-1.0

cholestasis / Delayed / 0-1.0
constipation / Delayed / 10.0
hemorrhoids / Delayed / Incidence not known
dysphagia / Delayed / Incidence not known
elevated hepatic enzymes / Delayed / Incidence not known
hypoprothrombinemia / Delayed / Incidence not known
chest pain (unspecified) / Early / Incidence not known
angina / Early / Incidence not known
sinus tachycardia / Rapid / Incidence not known
migraine / Early / Incidence not known
edema / Delayed / Incidence not known
dyspnea / Early / Incidence not known
folate deficiency / Delayed / Incidence not known

diarrhea / Early / Incidence not known
abdominal pain / Early / Incidence not known
anorexia / Delayed / Incidence not known
flatulence / Early / Incidence not known
eructation / Early / Incidence not known
vomiting / Early / Incidence not known
nausea / Early / Incidence not known
urticaria / Rapid / Incidence not known
rash / Early / Incidence not known
back pain / Delayed / Incidence not known
arthralgia / Delayed / Incidence not known
musculoskeletal pain / Early / Incidence not known
dizziness / Early / Incidence not known
insomnia / Early / Incidence not known
headache / Early / Incidence not known
weakness / Early / Incidence not known
fatigue / Early / Incidence not known

Colestid

Rx

Oral bile acid resin; similar to cholestyramine in its cholesterol-lowering effects.

5 g PO 1 to 2 times daily, initially. Monitor lipid concentrations as clinically appropriate and adjust dose as needed. May increase dose by 5 g/day every 1 to 2 months. Max: 30 g/day.

2 g PO 1 to 2 times daily, initially. Monitor lipid concentrations as clinically appropriate and adjust dose as needed. May increase dose by 2 to 4 g/day every 1 to 2 months. Max: 16 g/day.

Initially, 10 g PO as a single dose, followed by 5 g PO every 6—8 hours, has been used.

†Indicates off-label use

No dosage adjustment is needed; the drug is not systemically absorbed.

No dosage adjustment is needed; the drug is not systemically absorbed.
 
Intermittent hemodialysis
No dosage adjustment is needed; the drug is not systemically absorbed.

Alendronate; Cholecalciferol: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Aliskiren; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Alpha-glucosidase Inhibitors: (Moderate) It has been postulated that concomitant administration of acarbose or miglitol with colestipol may enhance the effects of acarbose. However, the clinical significance of such an interaction is unknown and co-use may also lead to an increased incidence of gastrointestinal side effects. Administer acarbose or miglitol at least 1 hour before or at least 4-6 hours after the administration of colestipol.
Amiloride; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Amlodipine; Atorvastatin: (Moderate) Coadministration of atorvastatin with colestipol resulted in approximately 25% lower plasma concentrations of atorvastatin. However, LDL-cholesterol reduction was greater when atorvastatin and colestipol were administered together than when either drug was given alone.
Amlodipine; Valsartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Atenolol; Chlorthalidone: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Atorvastatin: (Moderate) Coadministration of atorvastatin with colestipol resulted in approximately 25% lower plasma concentrations of atorvastatin. However, LDL-cholesterol reduction was greater when atorvastatin and colestipol were administered together than when either drug was given alone.
Atorvastatin; Ezetimibe: (Moderate) Coadministration of atorvastatin with colestipol resulted in approximately 25% lower plasma concentrations of atorvastatin. However, LDL-cholesterol reduction was greater when atorvastatin and colestipol were administered together than when either drug was given alone. (Moderate) The oral absorption of ezetimibe may be decreased by the concomitant administration of the bile acid sequestrants; the incremental LDL-cholesterol reduction expected to occur by adding ezetimibe to bile acid sequestrant therapy may be reduced by this interaction. To limit a potential interaction, ezetimibe should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. In a study of 40 hypercholesterolemic adult subjects, concomitant cholestyramine (4 grams PO twice daily) administration decreased the mean AUC values of total ezetimibe (ezetimibe plus ezetimibe-glucuronide) and ezetimibe by approximately 55% and 80%, respectively. A similar effect might be expected to occur with the concomitant administration of colestipol with ezetimibe; however, this potential interaction has not been studied.
Azilsartan; Chlorthalidone: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Bempedoic Acid; Ezetimibe: (Moderate) The oral absorption of ezetimibe may be decreased by the concomitant administration of the bile acid sequestrants; the incremental LDL-cholesterol reduction expected to occur by adding ezetimibe to bile acid sequestrant therapy may be reduced by this interaction. To limit a potential interaction, ezetimibe should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. In a study of 40 hypercholesterolemic adult subjects, concomitant cholestyramine (4 grams PO twice daily) administration decreased the mean AUC values of total ezetimibe (ezetimibe plus ezetimibe-glucuronide) and ezetimibe by approximately 55% and 80%, respectively. A similar effect might be expected to occur with the concomitant administration of colestipol with ezetimibe; however, this potential interaction has not been studied.
Benazepril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Bexarotene: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of orally administered vitamin A, such as bexarotene. Administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Bisoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Calcifediol: (Moderate) Separate administration of calcifediol by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins like calcifediol.
Calcitriol: (Moderate) Separate administration of calcitriol by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins like calcitriol.
Calcium; Vitamin D: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Candesartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Captopril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Carbamazepine: (Major) Concurrent administration of carbamazepine with colestipol results in a modest reduction in carbamazepine bioavailability. Although the reduction in carbamazepine bioavailability may not be clinically significant, staggering the times of administration of these agents should alleviate any drug interaction. In the same study, cholestyramine did not affect carbamazepine bioavailability.
Chenodiol: (Major) Bile acid sequestrants, such as colestipol, may interfere with the action of chenodiol by reducing its absorption. To minimize drug interactions, administer chenodiol at least 1 hour before or at least 4 hours after colestipol.
Chlorothiazide: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Chlorthalidone: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Chlorthalidone; Clonidine: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Cholic Acid: (Moderate) Do not administer cholic acid simultaneously with bile acid binding resins such as cholestyramine, colestipol, or colesevelam because a reduction in cholic acid absorption will occur. Administer cholic acid at least 1 hour before or 4 to 6 hours (or the maximal interval possible) after a bile acid binding resin.
Cranberry, Vaccinium macrocarpon Ait.: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Deferasirox: (Major) The concomitant administration of deferasirox and colestipol may result in decreased systemic exposure to deferasirox. Avoid the concomitant use if possible. If colestipol and deferasirox coadministration is necessary, consider increasing the initial dose of deferasirox to 30 mg/kg. Monitor serum ferritin levels and clinical responses for further dose modification.
Diclofenac: (Moderate) Limited data suggest that colestipol can substantially reduce the bioavailability of diclofenac. In a randomized cross-over study, six healthy subjects took a single oral dose of diclofenac with water, cholestyramine (8 g), or colestipol (10 g). Diclofenac AUC was reduced by 62% or 33%, respectively, during coadministration with cholestyramine or colestipol. Although the clinical implications of this pharmacokinetic interaction are uncertain, clinicians should be alert to loss of antiinflammatory or analgesic effect with diclofenac. Staggering the administration times may prevent this interaction.
Diclofenac; Misoprostol: (Moderate) Limited data suggest that colestipol can substantially reduce the bioavailability of diclofenac. In a randomized cross-over study, six healthy subjects took a single oral dose of diclofenac with water, cholestyramine (8 g), or colestipol (10 g). Diclofenac AUC was reduced by 62% or 33%, respectively, during coadministration with cholestyramine or colestipol. Although the clinical implications of this pharmacokinetic interaction are uncertain, clinicians should be alert to loss of antiinflammatory or analgesic effect with diclofenac. Staggering the administration times may prevent this interaction.
Digoxin: (Moderate) Although colestipol and cholestyramine have been reported to reduce the bioavailability of digitoxin, their effects on digoxin absorption are hypothesized to be less since digoxin undergoes less enterohepatic recycling than digitoxin. However, cholestyramine has been shown to significantly interfere with the absorption of digoxin. Colestipol is also expected to decrease the absorption of digoxin, and has been shown to produce a clinically significant decrease in the serum half-life of digoxin. The manufacturer of digoxin recommends measuring serum digoxin concentrations prior to initiation of colestipol or cholestyramine. Continue monitoring during concomitant treatment and increase the digoxin dose by 20-40% as necessary.
Doxercalciferol: (Moderate) Separate administration of doxercalciferol by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins like doxercalciferol.
Drospirenone; Ethinyl Estradiol; Levomefolate: (Major) L-methylfolate and colestipol should be used together cautiously. Colestipol administration may decrease L-methylfolate plasma concentrations. Patients taking both agents should take L-methylfolate 1 hour before or 4 to 6 hours after a dose of colestipol.
Enalapril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Eprosartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Ezetimibe: (Moderate) The oral absorption of ezetimibe may be decreased by the concomitant administration of the bile acid sequestrants; the incremental LDL-cholesterol reduction expected to occur by adding ezetimibe to bile acid sequestrant therapy may be reduced by this interaction. To limit a potential interaction, ezetimibe should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. In a study of 40 hypercholesterolemic adult subjects, concomitant cholestyramine (4 grams PO twice daily) administration decreased the mean AUC values of total ezetimibe (ezetimibe plus ezetimibe-glucuronide) and ezetimibe by approximately 55% and 80%, respectively. A similar effect might be expected to occur with the concomitant administration of colestipol with ezetimibe; however, this potential interaction has not been studied.
Ezetimibe; Simvastatin: (Moderate) The oral absorption of ezetimibe may be decreased by the concomitant administration of the bile acid sequestrants; the incremental LDL-cholesterol reduction expected to occur by adding ezetimibe to bile acid sequestrant therapy may be reduced by this interaction. To limit a potential interaction, ezetimibe should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. In a study of 40 hypercholesterolemic adult subjects, concomitant cholestyramine (4 grams PO twice daily) administration decreased the mean AUC values of total ezetimibe (ezetimibe plus ezetimibe-glucuronide) and ezetimibe by approximately 55% and 80%, respectively. A similar effect might be expected to occur with the concomitant administration of colestipol with ezetimibe; however, this potential interaction has not been studied.
Fat soluble vitamins: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Fenofibrate: (Major) Based on reported interactions with gemfibrozil, colestipol or cholestyramine can potentially reduce the oral bioavailability of fenofibrate if these agents are administered together. Although the presence of a drug interaction is uncertain, patients should take fenofibrate at least 1 hour before or 4 to 6 hours after a bile acid resin to avoid affecting the bioavailability of fenofibrate.
Fenofibric Acid: (Moderate) Based on reported interactions with gemfibrozil, colestipol can potentially reduce the oral bioavailability of fenofibric acid if these agents are administered together. Although the presence of a drug interaction is uncertain, patients should take fenofibric acid at least 1 hour before or 4 to 6 hours after colestipol to avoid affecting the bioavailability of fenofibric acid.
Fish Oil, Omega-3 Fatty Acids (Dietary Supplements): (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Fosinopril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Furosemide: (Moderate) In a study of 6 healthy volunteers, concurrent administration of cholestyramine with oral furosemide reduced the bioavailability of furosemide by 95% and reduced the diuretic response by 77%. Concomitant administration with colestipol reduced furosemide bioavailability by 80% and the diuretic response by 58%. The manufacturer of colestipol recommends administering other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol and that the interval between the administration of colestipol and other drugs should be as long as possible.
Gemfibrozil: (Moderate) Separate the administration of gemfibrozil and colestipol by at least 2 hours. Coadministration of bile acid resins such as colestipol results in a 30% reduction in gemfibrozil AUC; exposure to gemfibrozil was not significantly affected when the drugs were administed two hours apart.
Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Hydrochlorothiazide, HCTZ; Methyldopa: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Hydrochlorothiazide, HCTZ; Moexipril: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Hydrocortisone: (Moderate) The bile-acid sequestrant colestipol is well-known to cause drug interactions by binding and decreasing the oral administration of many drugs. Colestipol can bind with and possibly decrease the oral absorption of hydrocortisone. According to the manufacturer, administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Ibritumomab Tiuxetan: (Moderate) Colestipol may interfere with the oral absorption of phosphorus salts. According to the manufacturer, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol. The manufacturer also recommends that the interval between the administration of colestipol and other drugs should be as long as possible.
Irbesartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Isotretinoin: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of isotretinoin. Administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Levomefolate: (Major) L-methylfolate and colestipol should be used together cautiously. Colestipol administration may decrease L-methylfolate plasma concentrations. Patients taking both agents should take L-methylfolate 1 hour before or 4 to 6 hours after a dose of colestipol.
Lisinopril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Lomitapide: (Moderate) Separate administration of lomitapide and bile acid sequestrants by at least 4 hours. Although this interaction has not been studied, bile acid sequestrants can interfere with the absorption of oral medications.
Losartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Maralixibat: (Moderate) Take maralixibat at least 4 hours before or 4 hours after taking a bile acid sequestrant. Bile acid sequestrants may bind maralixibat in the gut, which may reduce its efficacy.
Methyclothiazide: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Metolazone: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Metoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Mycophenolate: (Major) Bile acid sequestrants, such as colestipol can interrupt enterohepatic recirculation and thus, reduce mycophenolic acid systemic exposure. The AUC of mycophenolic acid when given as mycophenolate mofetil is decreased by about 40% when take with cholestyramine. Concurrent use of a bile acid sequestrant, such as colestipol, or any drug that may interfere with enterohepatic recirculation of MPA is not recommended.
Niacin, Niacinamide: (Moderate) In vitro studies have shown that bile acid sequestrants bind niacin. Roughly 98% of niacin was bound to colestipol, and 10 to 30% of niacin was bound to cholestyramine. These results suggest that at least 4 to 6 hours should elapse between the ingestion of bile-acid-binding resins and the administration of niacin.
Niacin; Simvastatin: (Moderate) In vitro studies have shown that bile acid sequestrants bind niacin. Roughly 98% of niacin was bound to colestipol, and 10 to 30% of niacin was bound to cholestyramine. These results suggest that at least 4 to 6 hours should elapse between the ingestion of bile-acid-binding resins and the administration of niacin.
Obeticholic Acid: (Moderate) Bile acid binding resins such as colestipol absorb and reduce bile acid absorption and may reduce the absorption, systemic exposure, and efficacy of obeticholic acid. If used together, take obeticholic acid at least 4 hours before or 4 hours after taking the bile acid resin, or at as great an interval as possible.
Odevixibat: (Moderate) Take odevixibat at least 4 hours before or 4 hours after taking a bile acid sequestrant. Bile acid sequestrants may bind odevixibat in the gut, which may reduce its efficacy.
Olmesartan; Amlodipine; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Olmesartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Paricalcitol: (Moderate) Separate administration of paricalcitol by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins like paricalcitol.
Penicillin G Benzathine: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of penicillin G. To minimize drug interactions, administer penicillin at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Penicillin G Benzathine; Penicillin G Procaine: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of penicillin G. To minimize drug interactions, administer penicillin at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Penicillin G Procaine: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of penicillin G. To minimize drug interactions, administer penicillin at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Penicillin G: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of penicillin G. To minimize drug interactions, administer penicillin at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Phosphorated Carbohydrate Solution: (Moderate) Colestipol may interfere with the oral absorption of phosphorus salts. According to the manufacturer, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol. The manufacturer also recommends that the interval between the administration of colestipol and other drugs should be as long as possible.
Phosphorus: (Moderate) Colestipol may interfere with the oral absorption of phosphorus salts. According to the manufacturer, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol. The manufacturer also recommends that the interval between the administration of colestipol and other drugs should be as long as possible.
Phytonadione, Vitamin K1: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Potassium Phosphate: (Moderate) Colestipol may interfere with the oral absorption of phosphorus salts. According to the manufacturer, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol. The manufacturer also recommends that the interval between the administration of colestipol and other drugs should be as long as possible.
Potassium Phosphate; Sodium Phosphate: (Moderate) Colestipol may interfere with the oral absorption of phosphorus salts. According to the manufacturer, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of colestipol. The manufacturer also recommends that the interval between the administration of colestipol and other drugs should be as long as possible.
Pravastatin: (Major) Bile acid-sequestering agents, such as colestipol, have been shown to significantly reduce serum concentrations of pravastatin. Coadministration of the bile acid-sequestering agent cholestyramine decreases the AUC of pravastatin by about 40-50%. Administering pravastatin 1 hour before or 4 hours after a dose of cholestyramine is advised if both agents are used together.
Propranolol: (Moderate) Colestipol can bind with and possibly decrease the oral absorption of propranolol. To minimize drug interactions, administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Propranolol; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction. (Moderate) Colestipol can bind with and possibly decrease the oral absorption of propranolol. To minimize drug interactions, administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of colestipol.
Quinapril; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Rosuvastatin; Ezetimibe: (Moderate) The oral absorption of ezetimibe may be decreased by the concomitant administration of the bile acid sequestrants; the incremental LDL-cholesterol reduction expected to occur by adding ezetimibe to bile acid sequestrant therapy may be reduced by this interaction. To limit a potential interaction, ezetimibe should be administered at least 2 hours before or 4 hours after administration of a bile acid sequestrant. In a study of 40 hypercholesterolemic adult subjects, concomitant cholestyramine (4 grams PO twice daily) administration decreased the mean AUC values of total ezetimibe (ezetimibe plus ezetimibe-glucuronide) and ezetimibe by approximately 55% and 80%, respectively. A similar effect might be expected to occur with the concomitant administration of colestipol with ezetimibe; however, this potential interaction has not been studied.
Sodium Phenylbutyrate; Taurursodiol: (Major) Avoid coadministration of colestipol and taurursodiol, and consider other cholesterol lowering medications. Coadministration may decrease the absorption of taurursodiol.
Spironolactone; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Telmisartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Tetracyclines: (Major) Colestipol has been shown to reduce tetracycline absorption by roughly 50%. It is likely this is enough to cause a clinically significant effect. Although no data are available for other tetracyclines, it should be assumed that any tetracycline antibiotic may be affected similarly by colestipol. Staggering oral doses of each agent is recommended to minimize this pharmacokinetic interaction; administer tetracyclines at least 1 hour before or at least 4 to 6 hours after the administration of colestipol. Since doxycycline undergoes enterohepatic recirculation, it may be even more susceptible to this drug interaction than the other tetracyclines.
Thiazide diuretics: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Thyroid hormones: (Moderate) Administer oral levothyroxine or other oral thyroid hormones at least 4 hours before a dose of colestipol. Colestipol and other bile acid sequestrants have been shown to decrease the oral absorption of thyroid hormones. Monitor thyroid function periodically to ensure proper clinical management.
Tretinoin, ATRA: (Moderate) The bile-acid sequesterant colestipol is well-known to cause drug interactions by binding and decreasing the oral administration of many drugs, which may include interaction with oral tretinoin; to minimize drug interactions, administer other drugs at least 1 hour before or at least 4 to 6 hours after the administration of cholestyramine or colestipol.
Triamterene; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Ursodeoxycholic Acid, Ursodiol: (Moderate) Colestipol may interfere with the action of ursodeoxycholic acid, ursodiol by reducing its absorption. To minimize drug interactions, administer ursodiol at least 1 hour before or at least 4 hours after the bile acid sequestering agents.
Valsartan; Hydrochlorothiazide, HCTZ: (Moderate) Although to a lesser extent than cholestyramine, colestipol also has been shown to inhibit the GI absorption and therapeutic response of thiazide diuretics. Single doses of colestipol resins reduce the absorption of HCTZ by up to 43%. Administering thiazide diuretics at least 2 hours before colestipol has been suggested to minimize the interaction.
Vancomycin: (Major) The concurrent use of anion-exchange resins and oral vancomycin is contraindicated by clinical practice guidelines. Per FDA-approved labeling, administer other drugs at least 1 hour before or 4 hours after colestipol (or as great an interval as possible). Colestipol can bind other drugs, such as oral vancomycin, when given concurrently.
Vitamin A: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Vitamin D: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Vitamin E: (Moderate) Separate administration of fat-soluble vitamins by 1 hour before or 4 hours after a colestipol dose to limit effects on oral absorption. Because it sequesters bile acids, colestipol may interfere with normal fat absorption and thus may reduce absorption of fat-soluble vitamins.
Warfarin: (Major) 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 sequestrant.

Colestid/Colestipol/Colestipol Hydrochloride Oral Gran F/Recon: 5g
Colestid/Colestipol/Colestipol Hydrochloride Oral Tab: 1g

30 g/day PO colestipol granules or 16 g/day PO colestipol tablets.

30 g/day PO colestipol granules or 16 g/day PO colestipol tablets.

Safety and efficacy have not been established; 15 g/day PO has been used safely for hypercholesterolemia.

7—12 years: Safety and efficacy have not been established; 15 g/day PO has been used safely for hypercholesterolemia.
< 7 years: Safety and efficacy have not been established.

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.

Colestipol is administered orally. 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.

Colestipol is not absorbed systemically and is therefore not expected to cause fetal harm during pregnancy. There are no adequate and well-controlled studies in pregnant women. However, colestipol is known to interfere with the absorption of fat-soluble vitamins in pregnancy, which may lead to deficiencies even with supplementation. Maternal vitamin K deficiencies may lead to fetal deficiencies, resulting in coagulopathy and possible fetal hemorrhage and death. Published guidelines state that bile acid sequestrants, such as colestipol, may be administered to pregnant women and that vitamin K should be monitored during therapy. Monitor the patient's INR and supplement with vitamin K, if needed. In addition, other fat-soluble vitamins may need to be supplemented.

Colestipol is not systemically absorbed; for this reason, most experts consider nonabsorbable resins such as colestipol the drugs of choice for breast-feeding mothers who require pharmacotherapy for cholesterol management.[63892] It should be noted, however, that prolonged use of colesevelam may result in decreased absorption of fat-soluble vitamins (A, D, E, and K) in the mother and could potentially reduce vitamin concentrations in maternal milk.[48282] [28071] The possible need for vitamin supplementation should be discussed with the infant's pediatrician. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.