Colestipol Hydrochloride

Pronunciation

Pronunciation: koe-LESS-tih-pole HIGH-droe-KLOR-ide
Class: Antihyperlipidemic agent, Bile acid sequestrant

Trade Names

Colestid
- Tablets 1 g
- Unflavored Granules 5 g
- Flavored Granules 5 g

Pharmacology

Binds with bile acids in the intestine to form an insoluble complex that is excreted in the feces, resulting in partial removal of bile acids from the enterohepatic circulation. The increased fecal loss of bile acids leads to an increased oxidation of cholesterol to bile acids, which results in a decrease in LDL cholesterol plasma levels and serum cholesterol levels.

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Pharmacokinetics

Absorption

Not absorbed.

Elimination

Less than 0.17% is excreted in the urine.

Indications and Usage

Adjunctive therapy to diet for the reduction of elevated serum total and LDL-cholesterol in patients with primary hypercholesterolemia who do not respond adequately to diet.

Unlabeled Uses

Treatment of digitalis toxicity; hyperoxaluria; diarrhea caused by bile acids; adjunctive treatment for hyperthyroidism; relief of pruritus associated with partial biliary obstruction (including primary biliary cirrhosis and various other forms of bile stasis); binds to the toxin produce by Clostridium difficile .

Contraindications

Standard considerations.

Dosage and Administration

Adults Tablets

PO 2 to 16 g/day given once or in divided doses. Start with 2 g once or twice daily and increase in amounts of 2 g once or twice daily at 1- or 2-mo intervals.

Granules

PO 5 to 30 g/day given once or in divided doses. Start with 5 g (1 level scoop or 1 single-use packet) once or twice daily and increase in amounts of 5 g daily over 1 to 2 mo intervals.

General Advice

  • Administer colistipol separate from other drugs. Give other drugs at least 1 h before or 4 h after colistipol.
  • To avoid accidental inhalation or esophageal distress, never administer granules in dry form. Always mix with water or other fluids before administering.
  • Mix contents of 1 single-dose packet or level scoopful in 3 oz or more of any liquid. Stir to uniform consistency and have patient drink suspension. Rinse glass with small amount of additional beverage to ensure that all the medication was taken. May also mix with highly fluid soups, in milk with hot or regular breakfast cereals, or pulpy fruits with high moisture content (eg, applesauce, crushed pineapple, peaches, pears).
  • Administer with meals unless dosing interval needs to be modified to avoid interference with absorption of other medications.
  • Administer tablets one at a time. Have patient swallow tablet whole with plenty of liquid. Caution patient not to cut, crush, or chew tablets.

Storage/Stability

Store at controlled room temperature (68° to 77°F).

Drug Interactions

Digitalis glycosides, fat soluble vitamins (ie, A, D, E, K), folic acid, furosemide, gemfibrozil, hydrocortisone, penicillin G, phosphate supplements, propanolol, tetracyclines, thiazide diuretics

Absorption of these drugs may be decreased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

EENT

Difficulty swallowing.

GI

Abdominal pain and cramping; bloody hemorrhoids and stools; constipation; diarrhea; esophageal obstruction; flatulence; heartburn; indigestion; intestinal bloating; nausea; vomiting.

Hematologic

Bleeding tendencies related to vitamin K deficiency.

Hepatic

Elevated LFTs.

Precautions

Monitor

Determine serum cholesterol levels at baseline, frequently during the first few mo of therapy, and periodically thereafter. Periodically measure serum triglyceride levels to detect significant changes.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Constipation

Colestipol may worsen pre-existing constipation. When using tablets, start with low dose (eg, 2 g daily or twice daily for 1 mo) and increase gradually (eg, 2 to 4 g/day at monthly intervals). When using granules, start with 1 packet or scoop daily for 5 to 7 days and increase to twice daily 4 to 6 wk apart. If tolerated, increase dose as needed by 1 dose/day (at monthly intervals). Increased fluid and fiber intake may be beneficial.

GI disorders

Use tablets with caution in patients who have swallowing problems or history of choking with food, liquids, or other tablets or capsules.

Hyperchloremic acidosis

Because colistipol is a chloride form of anion exchange resin, there is a possibility for producing hyperchloremic acidosis during prolonged use. Use with caution in younger and smaller patients, patients with renal insufficiency or volume depletion, or with concomitant spironolactone administration.

Phenylketonuria

Flavored granules for suspension (flavored Colestid ) contains phenylalanine. Do not administer to patient with phenylketonuria without first discussing with health care provider.

Secondary causes of hypercholesterolemia

Ensure that secondary causes of hyperlipidemia (eg, alcoholism, dysproteinemias, hypothyroidism, nephritic syndrome, obstructive liver disease, other drug therapy, poorly controlled diabetes) have been excluded before starting therapy.

Triglyceride levels

Consider dose reduction, drug discontinuation, or combined or alternate therapy if significant rise in triglyceride levels occurs.

Vitamin K deficiency

Chronic use may be associated with increased bleeding tendency caused by hypoprothrombinemia associated with vitamin K deficiency. This can be treated with parenteral vitamin K 1 and recurrence can be prevented by oral administration of vitamin K.

Overdosage

Symptoms

GI obstruction.

Patient Information

  • Advise patient to read patient information leaflet before using the first time and to reread and check for new information with each refill.
  • Advise patient to drink plenty of fluids and maintain a high fiber intake to minimize risk of constipation.
  • Advise patient to try to take each dose with a meal unless the dosing interval needs to be modified to avoid interference with absorption of other medications.
  • Advise patient using granules to mix contents of 1 level scoop or 1 single-dose packet in at least 3 oz of any beverage, stir to uniform consistency, and drink. Advise patient to rinse glass with small amount of additional beverage to make sure all the medication has been taken.
  • Advise patient that granules also can be mixed with highly fluid soups, milk in hot or regular cereal, or pulpy fruits with high moisture content (eg, applesauce, crushed pineapple, peaches, pears).
  • Advise patient using tablets to take only 1 tablet at a time and to swallow whole with plenty of fluids. Caution patient not to crush, chew, or cut tablet.
  • Instruct patient using tablets to stop using and notify health care provider if any tablets get stuck after swallowing or cause a choking sensation.
  • Inform patient that constipation, gas, nausea, and heartburn may occur but usually go away with continued therapy. Advise patient to notify health care provider if these effects become bothersome or if bleeding or unusual bruising occurs.
  • Instruct patient to take all other medications at least 1 h before or 4 h after taking colistipol.
  • Inform patient that drug helps control, but not does cure, lipid abnormality and to continue taking drug as prescribed when lipid levels are lowered.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
  • Emphasize to patient the importance of other modalities on cholesterol control: dietary changes (reduced saturated fat intake, increase soluble fiber intake); weight control; regular exercise; smoking cessation.

Copyright © 2009 Wolters Kluwer Health.

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