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Uses

Dyslipidemias

Adjunct to dietary therapy to decrease elevated serum total and LDL-cholesterol concentrations in the management of primary hypercholesterolemia in patients who do not respond adequately to diet.

Generally has no clinically relevant effect on serum triglyceride concentrations. However, because triglyceride concentrations may be increased in some patients, do not use alone in the management of hypertriglyceridemia.

As effective as cholestyramine in lowering serum cholesterol concentrations. Select bile acid sequestrant based on patient tolerance, including palatability and taste preference, and cost.

Dosage and Administration

General

• Patients should be placed on a standard lipid-lowering diet before initiation of colestipol therapy and should remain on this diet during treatment with the drug.
• To optimize antilipemic effects while minimizing the risk of adverse GI effects, adjust dosage carefully and titrate slowly.
• Instruct patients to take other drugs at least 1 hour before or 4 hours after taking colestipol tablets or suspension to minimize possible interference with absorption. (See Effects on GI Absorption of Drugs under Interactions.)

Monitoring during Antilipemic Therapy

• Monitor lipoprotein concentrations periodically to ensure that target LDL-cholesterol goals are achieved and maintained at <100 mg/dL (optional goal: <70 mg/dL) for patients with CHD or CHD risk equivalents; <130 mg/dL (optional goal: <100 mg/dL) for patients with ≥2 risk factors and 10-year risk of 10–20%; <130 mg/dL for patients with ≥2 risk factors and 10-year risk <10%; or <160 mg/dL for patients with 0–1 risk factor.

Administration

Oral Administration

Administer tablets one at a time; promptly swallow whole, using plenty of water or other appropriate liquid. The tablets must not be cut, crushed, or chewed.

To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.

To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions of the drug. After the mixture is ingested, rinse the glass with a small amount of additional fluid and ingest the remaining liquid to ensure that the entire dose has been taken.

Reconstitution

Add the prescribed amount of colestipol hydrochloride granules to at least 90 mL of a liquid (e.g., fruit juice, water, milk, soft drink) and stir until completely mixed (colestipol will not dissolve in the liquid). Palatability and compliance may be increased if the entire next-day’s dose is mixed in one of these liquids in the evening and then refrigerated. Use of a heavy or pulpy fruit juice may minimize complaints about consistency of suspensions of the drug. If a carbonated beverage is used, mix the powder slowly in a large glass to minimize excessive foaming; however, use of a carbonated beverage as a vehicle may be associated with adverse GI effects.

Alternatively, mix colestipol powder with milk in hot or regular breakfast cereals, a highly fluid soup, or pulpy fruit (e.g., crushed pineapple, pears, peaches, fruit cocktail).

Dosage

Available as colestipol hydrochloride; expressed in terms of the salt.

One dose (1 packet or 1 level teaspoon) of colestipol hydrochloride granules contains 5 g of colestipol hydrochloride. One dose (1 packet or 1 level scoop) of flavored colestipol hydrochloride granules contains 7.5 g of granules, which contains 5 g of colestipol hydrochloride.

Pediatric Patients

Dyslipidemias

Oral

Pediatric dosage has not been established; however, dosages of 10–20 g or 500 mg/kg daily in 2–4 divided doses have been used. Lower dosages (e.g., 125–250 mg/kg daily) have also been used in some children when serum cholesterol concentrations were only 15–20% above normal after dietary management alone.†

Adults

Dyslipidemias

Oral (Tablets)

Initially, 2 g once or twice daily. Increase dosage by 2 g once or twice daily at intervals of 1 or 2 months. Usual daily dosage range is 2–16 g taken once or in divided doses.

If the desired therapeutic effect is not achieved with the usual dosage of 2–16 g daily with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.

Oral (Granules for oral suspension)

Initially, 5 g (1 packet or 1 level scoop) once or twice daily. Titrate dose upward as necessary in 5-g increments at 1- or 2-month intervals. Usual daily dosage range is 5–30 g (1–6 packets or level scoops) taken once or in divided doses.

If the desired therapeutic effect is not achieved with the usual dosage of 1–6 doses per day with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.

Patients with preexisting constipation receiving granules for oral suspension: Initially, 5 g once daily for 5–7 days; then increase dosage to 5 g twice daily and monitor constipation and serum lipoprotein values, at least twice, 4–6 weeks apart. Thereafter, increase dosage as needed by 1 dose per day (at monthly intervals) with periodic monitoring of serum lipoprotein values; adjust dosage accordingly to achieve the desired effect while avoiding excessive dosage. If constipation worsens or the desired effect is not achieved with acceptable adverse effects with the usual dosage of 1–6 doses per day, consider combined therapy or alternative treatment.

30 g daily (as granules for oral suspension) has been used in combination with niacin in adults with heterozygous familial hypercholesterolemia.