Colestid

Dosage Forms & Strengths

granules, bottle

• 5g

granules, packets

• 5g

tablet

• 1g

Hyperlipidemia

Tablets: 2 g PO qDay or q12hr; increases of 2 g should occur at 1- or 2-month intervals; titrate not to exceed 16 g/day

Granules: 5 g PO qDay; increases of 5 g should occur at 1- or 2-month intervals; titrate not to exceed 30 g/day

Overdose Management

Generally considered safe in acute overdose although not formally studied

Adverse drug reactions in overdose may include peripheral neuropathy, diarrhea, increase K+, myopathy , rhabdomyolysis, acute renal failure, elevated liver function tests, eye lens opacities)

Check renal function tests, urine myoglobin, CPK, LFT's

Administration

Mix dry form in water/fluids to avoid inhalation or esophageal distress

Mix granules in fluids or food; take before meals

Do not crush, chew, or cut tablets

Take 1 tablet at a time; swallow with water or other fluids

Other Information

Monitor: Serum cholesterol, triglycerides

Other Indications & Uses

Used in relief of pruritus associated with elevated levels of bile

Used to decrease plasma half-life of digoxin in toxicity

Hypercholesterolemia (adjunct to diet for Type IIa & IIb hyperlipidemia)

Safety & efficacy not established

Tablets: 2 g PO qDay or q12hr; increases of 2 g should occur at 1- or 2-month intervals; titrate not to exceed 16 g/day

Granules: 5 g PO qDay; increases of 5 g should occur at 1- or 2-month intervals; titrate not to exceed 30 g/day

Mechanism of Action

Forms a soluble complex after binding to bile acid, increasing fecal loss of bile acid-bound low-density lipoprotein cholesterol

Pharmacokinetics

Onset: initial effect: 24-48 hr; max effect: 1 wk

Bioavailability: Not absorbed

Metabolism: Not metabolized

Excretion: feces 100%

Colestid

Colestid is a prescription medication used in combination with dietary changes to treat high cholesterol. Colestid belongs to a group of drugs called bile acid sequestrants. These work by binding bile acids, substances that are bound to LDL cholesterol ("bad cholesterol"), and then removing them from the body. 

This medication comes tablets to be taken by mouth. It is usually taken 1 or 2 times per day, with meals.

Do not cut, crush, or chew the tablets. Swallow tablets whole with a full glass of liquid.

This medication also is available as granules for suspension. The granules are mixed with a liquid before taking.

Common side effects of Colestid include constipation, gas, and nausea.

Colestipol is a cholesterol-lowering drug.

Colestipol lowers "bad" cholesterol in the blood, which is also called LDL (low-density lipoprotein) cholesterol. Lowering your LDL cholesterol may reduce your risk of hardened arteries, which can lead to heart attacks, stroke, and circulation problems.

Lowering high cholesterol levels is an important part of preventing heart disease and arteriosclerosis (hardening of the arteries).

Colestipol may also be used for other purposes not listed in this medication guide.

Avoid taking other medicines at the same time you take colestipol. Taking colestipol can make it harder for your body to absorb certain drugs, making them less effective. Take your other medicines at least 1 hour before or 4 hours after you take colestipol.

Avoid constipation by drinking 8 to 12 full glasses (8 ounces each) every day while taking colestipol. Ask your doctor before using a laxative or stool softener.

• Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.166 167 Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver.166 167 This causes an increased demand for cholesterol in liver cells, resulting in a compensatory increase in hepatic uptake (and thus systemic clearance) of circulating LDL-cholesterol.166 167

• Reduces serum total and LDL-cholesterol concentrations.166 167 Serum triglyceride concentrations may increase or remain unchanged.166 167

• Antilipemic effects are additive when used with lovastatin or niacin.166 167

Colestipol is used to lower high cholesterol levels in the blood. This may help prevent medical problems caused by cholesterol clogging the blood vessels.

Colestipol works by attaching to certain substances in the intestine. Since colestipol is not absorbed into the body, these substances also pass out of the body without being absorbed.

Colestipol may also be used for other conditions as determined by your doctor.

Colestipol is available only with your doctor's prescription.

Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use.

Colestid Tablets are indicated as adjunctive therapy to diet for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet. Generally, Colestid Tablets have no clinically significant effect on serum triglycerides, but with their use, triglyceride levels may be raised in some patients.

Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Treatment should begin and continue with dietary therapy (see NCEP guidelines). A minimum of six months of intensive dietary therapy and counseling should be carried out prior to initiation of drug therapy. Shorter periods may be considered in patients with severe elevations of LDL-C or with definite CHD.

According to the NCEP guidelines, the goal of treatment is to lower LDL-C, and LDL-C is to be used to initiate and assess treatment response. Only if LDL-C levels are not available, should the Total-C be used to monitor therapy. The NCEP treatment guidelines are shown below.

Prior to initiating therapy with Colestid Tablets, secondary causes of hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism), should be excluded, and a lipid profile performed to assess total cholesterol, HDL-C, and triglycerides (TG). For individuals with TG less than 400 mg/dL (<4.5 mmol/L), LDL-C can be estimated using the following equation:

LDL-C = Total cholesterol − [(Triglycerides/5) + HDL-C]

For TG levels >400 mg/dL, this equation is less accurate and LDL-C concentrations should be determined by ultracentrifugation. In hypertriglyceridemic patients, LDL-C may be low or normal despite elevated Total-C. In such cases Colestid Tablets may not be indicated.

Because it sequesters bile acids, colestipol hydrochloride may interfere with normal fat absorption and, thus, may reduce absorption of folic acid and fat soluble vitamins such as A, D, and K.

Chronic use of colestipol hydrochloride may be associated with an increased bleeding tendency due to hypoprothrombinemia from vitamin K deficiency. This will usually respond promptly to parenteral vitamin K1 and recurrences can be prevented by oral administration of vitamin K1.

Serum cholesterol and triglyceride levels should be determined periodically based on NCEP guidelines to confirm a favorable initial and adequate long-term response.

Colestid Tablets may produce or severely worsen pre-existing constipation. The dosage should be increased gradually in patients to minimize the risk of developing fecal impaction. In patients with pre-existing constipation, the starting dose should be 2 grams once or twice a day. Increased fluid and fiber intake should be encouraged to alleviate constipation and a stool softener may occasionally be indicated. If the initial dose is well tolerated, the dose may be increased as needed by a further 2 to 4 grams/day (at monthly intervals) with periodic monitoring of serum lipoproteins. If constipation worsens or the desired therapeutic response is not achieved at 2 to 16 grams/day, combination therapy or alternate therapy should be considered. Particular effort should be made to avoid constipation in patients with symptomatic coronary artery disease. Constipation associated with Colestid Tablets may aggravate hemorrhoids.

While there have been no reports of hypothyroidism induced in individuals with normal thyroid function, the theoretical possibility exists, particularly in patients with limited thyroid reserve.

Since colestipol hydrochloride is a chloride form of an anion exchange resin, there is a possibility that prolonged use may lead to the development of hyperchloremia acidosis.

Carcinogenesis, Mutagenesis and Impairment of Fertility

In studies conducted in rats in which cholestyramine resin (a bile acid sequestering agent similar to colestipol hydrochloride) was used as a tool to investigate the role of various intestinal factors, such as fat, bile salts, and microbial flora, in the development of intestinal tumors induced by potent carcinogens, the incidence of such tumors was observed to be greater in cholestyramine resin treated rats than in control rats.

The relevance of this laboratory observation from studies in rats with cholestyramine resin to the clinical use of Colestid Tablets is not known. In the LRC-CPPT study referred to above, the total incidence of fatal and nonfatal neoplasms was similar in both treatment groups. When the many different categories of tumors are examined, various alimentary system cancers were somewhat more prevalent in the cholestyramine group. The small numbers and the multiple categories prevent conclusions from being drawn. Further follow-up of the LRC-CPPT participants by the sponsors of that study is planned for cause-specific mortality and cancer morbidity. When colestipol hydrochloride was administered in the diet to rats for 18 months, there was no evidence of any drug related intestinal tumor formation. In the Ames assay, colestipol hydrochloride was not mutagenic.

Use in Pregnancy

Since colestipol hydrochloride is essentially not absorbed systemically (less than 0.17% of the dose), it is not expected to cause fetal harm when administered during pregnancy in recommended dosages. There are no adequate and well-controlled studies in pregnant women, and the known interference with absorption of fat-soluble vitamins may be detrimental even in the presence of supplementation. The use of Colestid tablets in pregnancy or by women of childbearing potential requires that the potential benefits of drug therapy be weighed against possible hazards to the mother or child.

Nursing Mothers

Caution should be exercised when Colestid Tablets are administered to a nursing mother. The possible lack of proper vitamin absorption described in the "Pregnancy" section may have an effect on nursing infants.

Pediatric Use

Safety and effectiveness in the pediatric population have not been established.

Information for Patients

Colestid Tablets may be larger than pills you have taken before. If you have had swallowing problems or choking with food, liquids or other tablets or capsules in the past, you should discuss this with your doctor before taking Colestid Tablets.

It is important that you take Colestid Tablets correctly:

1. Always take one tablet at a time and swallow promptly.
2. Swallow each tablet whole. Do not cut, crush, or chew the tablets.
3. Colestid Tablets must be taken with water or another liquid that you prefer. Swallowing the tablets will be easier if you drink plenty of liquid as you swallow each tablet.

Difficulty swallowing and temporary obstruction of the esophagus (the tube between your mouth and stomach) have been rarely reported in patients taking Colestid Tablets. If a tablet does get stuck after you swallow it, you may notice pressure or discomfort. If this happens to you, you should contact your doctor. Do not take Colestid Tablets again without your doctor's advice.

If you are taking other medications, you should take them at least one hour before or four hours after taking Colestid Tablets.

DRUG INTERACTIONS

Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids. In vitro studies have indicated that colestipol hydrochloride binds a number of drugs. Therefore, Colestid Tablets may delay or reduce the absorption of concomitant oral medication. The interval between the administration of Colestid Tablets and any other medication should be as long as possible. Patients should take other drugs at least one hour before or four hours after Colestid Tablets to avoid impeding their absorption.

Repeated doses of colestipol hydrochloride given prior to a single dose of propranolol in human trials have been reported to decrease propranolol absorption. However, in a follow-up study in normal subjects, single-dose administration of colestipol hydrochloride and propranolol and twice-a-day administration for 5 days of both agents did not affect the extent of propranolol absorption, but had a small yet statistically significant effect on its rate of absorption; the time to reach maximum concentration was delayed approximately 30 minutes. Effects on the absorption of other beta-blockers have not been determined. Therefore, patients on propranolol should be observed when Colestid Tablets are either added or deleted from a therapeutic regimen.

Studies in humans show that the absorption of chlorothiazide as reflected in urinary excretion is markedly decreased even when administered one hour before colestipol hydrochloride. The absorption of tetracycline, furosemide, penicillin G, hydrochlorothiazide, and gemfibrozil was significantly decreased when given simultaneously with colestipol hydrochloride; these drugs were not tested to determine the effect of administration one hour before colestipol hydrochloride.

No depressant effect on blood levels in humans was noted when colestipol hydrochloride was administered with any of the following drugs: aspirin, clindamycin, clofibrate, methyldopa, nicotinic acid (niacin), tolbutamide, phenytoin or warfarin. Particular caution should be observed with digitalis preparations since there are conflicting results for the effect of colestipol hydrochloride on the availability of digoxin and digitoxin. The potential for binding of these drugs if given concomitantly is present. Discontinuing colestipol hydrochloride could pose a hazard to health if a potentially toxic drug that is significantly bound to the resin has been titrated to a maintenance level while the patient was taking colestipol hydrochloride.

Bile acid binding resins may also interfere with the absorption of oral phosphate supplements and hydrocortisone.

A study has shown that cholestyramine binds bile acids and reduces mycophenolic acid exposure. As colestipol also binds bile acids, colestipol may reduce mycophenolic acid exposure and potentially reduce efficacy of mycophenolate mofetil.

Pfizer

NDC 0009-0450-03

Colestid®

micronized colestipol
hydrochloride tablets

1 g

120 Tablets
Rx only

LactMed Record Number

514

Last Revision Date

20130907

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