PHENYLKETONURICS: CHOLESTYRAMINE for ORAL SUSPENSION USP, LIGHT CONTAINS 14.0 mg PHENYLALANINE PER 5 GRAM DOSE.
There is currently no manufacturer warning information available for this drug.
1) Cholestyramine for Oral Suspension USP is indicated 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. Cholestyramine 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.
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 specific for the type of hyperlipoproteinemia determined prior to initiation of drug therapy. Excess body weight may be an important factor and caloric restriction for weight normalization should be addressed prior to drug therapy in the overweight.
Prior to initiating therapy with Cholestyramine, 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 (less than 4.5 mmol/L), LDL-C can be estimated using the following equation:
LDL-C = Total cholesterol – [(TG/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 Cholestyramine may not be indicated.
Serum cholesterol and triglyceride levels should be determined periodically based on NCEP guidelines to confirm initial and adequate long-term response. A favorable trend in cholesterol reduction should occur during the first month of Cholestyramine therapy. The therapy should be continued to sustain cholesterol reduction. If adequate cholesterol reduction is not attained, increasing the dosage of Cholestyramine or adding other lipid-lowering agents in combination with Cholestyramine should be considered.
Since the goal of treatment is to lower LDL-C, the NCEP 4 recommends that LDL-C levels be used to initiate and assess treatment response. If LDL-C levels are not available then Total-C alone may be used to monitor long-term therapy. A lipoprotein analysis (including LDL-C determination) should be carried out once a year. The NCEP treatment guidelines are summarized below.
| LDL-Cholesterol mg/dL (mmol/L) | |||
| Definite Atherosclerotic Disease* |
Two or More Other Risk Factors** |
Initiation Level | Goal |
| NO | NO | Greater Than or Equal to 190 (Greater Than or Equal To 4.9) |
Less Than 160 (Less Than 4.1) |
| NO | YES | Greater Than or Equal To 160 (Greater Than or Equal To 4.1) |
Less Than 130 (Less Than 3.4) |
| YES | YES or NO | Greater Than or Equal To 130 (Greater Than or Equal To 3.4) |
Less Than or Equal To 100 (Less Than or Equal To 2.6) |
* Coronary heart disease or peripheral vascular disease (including symptomatic carotid artery disease).
** Other risk factors for coronary heart disease (CHD) include: age (males greater than or equal to 45 years; females greater than or equal to 55 years or premature menopause without estrogen replacement therapy); family history of premature CHD; current cigarette smoking; hypertension; confirmed HDL-C less than 35 mg/dL (less than 0.91 mmol/L); and diabetes mellitus. Subtract one risk factor if HDL-C is greater than or equal to 60 mg/dL (greater than or equal to 1.6 mmol/L).
Cholestyramine monotherapy has been demonstrated to retard the rate of progression 2,3 and increase the rate of regression3 of coronary atherosclerosis.
2) Cholestyramine for oral suspension is indicated for the relief of pruritus associated with partial biliary obstruction. Cholestyramine for oral suspension has been shown to have a variable effect on serum cholesterol in these patients. Patients with primary biliary cirrhosis may exhibit an elevated cholesterol as part of their disease.
Cholestyramine for Oral Suspension USP, the chloride salt of a basic anion exchange resin, a cholesterol lowering agent, is intended for oral administration. Cholestyramine resin is quite hydrophilic, but insoluble in water. The cholestyramine resin in Cholestyramine is not absorbed from the digestive tract. Four grams of anhydrous cholestyramine resin is contained in 9 grams of Cholestyramine for Oral Suspension USP. Four grams of anhydrous cholestyramine resin is contained in 5 grams of Cholestyramine for Oral Suspension USP, Light. It is represented by the following structural formula:
Cholestyramine for Oral Suspension USP contains the following inactive ingredients: acacia, citric acid, D&C Yellow No. 10, FD&C Yellow No. 6, flavor (natural and artificial Orange), polysorbate 80, propylene glycol alginate and sucrose. Cholestyramine for Oral Suspension USP, Light contains the following inactive ingredients: aspartame, citric acid, colloidal silicon dioxide, D&C Yellow No. 10, FD&C Red No. 40, flavor (natural and artificial Orange), maltodextrin, propylene glycol alginate and xanthan gum.
