Drug Detail:Cholestyramine (Cholestyramine [ koe-le-stye-ra-meen ])
Drug Class: Bile acid sequestrants
Usual Adult Dose for Hyperlipoproteinemia
Initial dose: 4 g (1 packet or level scoop) orally once or twice a day
Maintenance dose: 8 to 16 g (2 to 4 packets or level scoops orally in 2 divided doses
Maximum dose: 24 g (6 packets or level scoops) per day
Comments:
- Increases in dose should be gradual with periodic assessment of lipid/lipoprotein levels at intervals of not less than 4 weeks.
- Although the recommended dosing schedule is up to twice a day, this drug may be administered in 1 to 6 doses per day.
Uses:
- As adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet; may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern; this drug has also been shown to delay the progression and increase the rate of regression of coronary atherosclerosis
- For the relief of pruritus associated with partial biliary obstruction
Usual Adult Dose for Hyperlipoproteinemia Type IIa (Elevated LDL)
Initial dose: 4 g (1 packet or level scoop) orally once or twice a day
Maintenance dose: 8 to 16 g (2 to 4 packets or level scoops orally in 2 divided doses
Maximum dose: 24 g (6 packets or level scoops) per day
Comments:
- Increases in dose should be gradual with periodic assessment of lipid/lipoprotein levels at intervals of not less than 4 weeks.
- Although the recommended dosing schedule is up to twice a day, this drug may be administered in 1 to 6 doses per day.
Uses:
- As adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet; may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern; this drug has also been shown to delay the progression and increase the rate of regression of coronary atherosclerosis
- For the relief of pruritus associated with partial biliary obstruction
Usual Adult Dose for Pruritus of Partial Biliary Obstruction
Initial dose: 4 g (1 packet or level scoop) orally once or twice a day
Maintenance dose: 8 to 16 g (2 to 4 packets or level scoops orally in 2 divided doses
Maximum dose: 24 g (6 packets or level scoops) per day
Comments:
- Increases in dose should be gradual with periodic assessment of lipid/lipoprotein levels at intervals of not less than 4 weeks.
- Although the recommended dosing schedule is up to twice a day, this drug may be administered in 1 to 6 doses per day.
Uses:
- As adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet; may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern; this drug has also been shown to delay the progression and increase the rate of regression of coronary atherosclerosis
- For the relief of pruritus associated with partial biliary obstruction
Usual Pediatric Dose for Hyperlipoproteinemia
240 mg/kg/day orally in 2 to 3 divided doses not to exceed 8 g/day with dose titration based on response and tolerance
Comments:
- An optimal dosage schedule has not been established in pediatric patients.
- Dosage expressed in terms of anhydrous resin.
- The effects of long-term administration as well as this drug's effect in maintaining lowered cholesterol levels in pediatric patients are unknown.
Use: As adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet; may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern
Renal Dose Adjustments
Data not available
Liver Dose Adjustments
Data not available
Dose Adjustments
Patients with preexisting constipation: Initiate with 4 g (1 packet or 1 level scoop) orally once a day for 5 to 7 days; increasing to twice a day with monitoring of constipation and of serum lipoproteins, at least twice, 4 to 6 weeks apart. If the initial dose is well tolerated, the dose may be increased as needed by one dose/day (at monthly intervals) with periodic monitoring of serum lipoproteins.
Precautions
Consult WARNINGS section for additional precautions.
Dialysis
Data not available
Other Comments
Administration advice:
- Doses should be administered at mealtime but may be modified to avoid interference with absorption of other medications.
- Do not take dry powder; always mix with water or other fluids prior to ingestion.
- Concomitant medications should be taken at least 1 hour before or 4 to 6 hours after cholestyramine (or as great an interval as possible) to avoid impeding their absorption.
Reconstitution/preparation techniques:
- Mix contents of one single-dose packet or one level scoop with 2 to 6 ounces per dose of water or other noncarbonated beverage and stir to uniform consistency and drink.
- May also be mixed with highly fluid soups or pulpy fruits with high moisture content such as applesauce or crushed pineapple.
General:
- Prior to beginning therapy, secondary causes of hypercholesterolemia should be excluded.
- This drug should be used as a component of multiple risk factor intervention in patients at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia.
- Treatment should be used in conjunction with diet specific for the type of hyperlipoproteinemia.
- Excess body weight and caloric restriction for weight normalization should be addressed prior to drug therapy.
Monitoring:
- Metabolic: Serum cholesterol should be determined frequently during the first few months of therapy and periodically thereafter. Serum triglycerides should be measured periodically to detect whether significant changes have occurred.
Patient advice:
- Drink plenty of fluids and mix each dose with 2 to 6 ounces of fluid before drinking.
- Sipping or holding resin suspension in the mouth for prolonged periods may lead to changes in the surface of the teeth resulting in discoloration, erosion of enamel, or decay; good oral hygiene should be kept.