(Cholestyramine for Oral Suspension, USP)
Prevalite® (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 Prevalite® is not absorbed from the digestive tract. 5.5 grams of Prevalite® contain 4 grams of anhydrous cholestyramine resin.
Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces.
Prevalite® is indicated for the following:
1) Prevalite® 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. Prevalite® 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 resin, 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 (Total-C), high-density lipoprotein 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 - [(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 resin 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 resin therapy. The therapy should be continued to sustain cholesterol reduction. If adequate cholesterol reduction is not attained, increasing the dosage of cholestyramine resin or adding other lipid-lowering agents in combination with cholestyramine resin should be considered.
Since the goal of treatment is to lower LDL-C, the NCEP4 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.
Cholestyramine resin monotherapy has been demonstrated to retard the rate of progression2,3 and increase the rate of regression3 of coronary atherosclerosis.
2) Prevalite® is indicated for the relief of pruritus associated with partial biliary obstruction. Cholestyramine resin 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.
Media Articles Related to Prevalite (Cholestyramine)
FDA Approves New LDL-Lowering Agent Alirocumab (Praluent)
Source: theheart.org | Medscape Cardiology Headlines [2015.07.24]
This marks the first approval in the US for the novel PCSK-9 class of drugs for use in patients with hypercholesterolemia or high CV risk. It also comes just hours after a European regulatory body recommended the drug be approved.
EMA Backs Approval of Alirocumab (Praluent)
Source: theheart.org | Medscape Cardiology Headlines [2015.07.24]
The recommendation is for patients with primary hypercholesterolemia or mixed dyslipidemia who cannot reach LDL-C goals. However, "the effect on cardiovascular morbidity has not yet been determined."
Published Studies Related to Prevalite (Cholestyramine)
Efficacy of 10% sucralfate ointment in the reduction of acute postoperative pain
after open hemorrhoidectomy: a prospective, double-blind, randomized,
placebo-controlled trial. 
hemorrhoidectomy... CONCLUSIONS: Sucralfate ointment reduced the acute postoperative pain after
The effect of gemfibrozil, niacin and cholestyramine combination therapy on metabolic syndrome in the Armed Forces Regression Study. [2011.05]
INTRODUCTION: Metabolic syndrome is a powerful predictor of cardiovascular events independent of overt diabetes. Dietary restriction and weight loss modify metabolic syndrome components. This study addresses whether combination pharmacologic therapy focused on dyslipidemia provides additional benefit... CONCLUSIONS: The combination of gemfibrozil, niacin and cholestyramine has profound, beneficial effects on the components of metabolic syndrome. These benefits are additive to those seen with aggressive diet and lifestyle modification.
Colesevelam hydrochloride powder for oral suspension versus cholestyramine powder for oral suspension: comparison of acceptability and tolerability. [2011.03]
OBJECTIVE: To compare tolerability of colesevelam hydrochloride powder versus a cholesterol-lowering equivalent dose of generic cholestyramine powder, each mixed in water, by means of the validated Bile Acid Sequestrant Acceptability (BASA) Scale... CONCLUSION: Although study participants thought that the orange-colored generic cholestyramine powder had a better appearance, they also reported that colesevelam hydrochloride for oral suspension tasted better. A minority of study participants thought appearance was "very important"; a substantial majority thought taste was "very important" for potential long-term compliance.
The effect of gemfibrozil, niacin and cholestyramine combination therapy on
metabolic syndrome in the Armed Forces Regression Study. 
pharmacologic therapy focused on dyslipidemia provides additional benefit... CONCLUSIONS: The combination of gemfibrozil, niacin and cholestyramine has
Low doses of cholestyramine in the treatment of hyperthyroidism. [2008.12]
The enterohepatic circulation of thyroid hormones is increased in thyrotoxicosis... We conclude that low dose of cholestyramine is an effective and well-tolerated adjunctive agent in the treatment of hyperthyroid Graves' disease.
Clinical Trials Related to Prevalite (Cholestyramine)
PRELIMINARY EVALUATION OF PHARMACOLOGICAL LOWERING OF AGEs [Not yet recruiting]
There is evidence of the association between diabetic microangiopathy and elevated serum
concentrations of advanced glycation end-products (AGEs). AGEs levels are associated with
ingestion of specific foods (baked meats and milk powder); reducing their dietary intake
lowers AGEs concentrations, with beneficial metabolic effects; however threre is still no
evidence of whether this has an impact on microvascular complications of DM. We recently
applied for funding to compare in a RCT the effects of Cholestyramine versus placebo, on
visual electrophysiology. This drug is similar to Sevelamer in structure, both act as
chelators of bile salts, and reduce absorption of dietary AGE, lowering serum levels.
However it is essential to carry out preliminary tests to assess aspects that may imply
adjustments to the proposed protocol, such as: 1) tolerance to the drug 2) short term effect
of the drug versus placebo on serum levels of AGEs 3) effects of the drug versus placebo in
levels of fat soluble vitamins (D and K specifically) 4) intra and interindividual
variability of electrophysiological measurements of vision (ERGMF and optic nerve
conduction velocity) 5) drug versus placebo in electrophysiological measurements of vision
(neuroconduction ERGMF and optic nerve). Objective: The present project is planned as a
pilot study, which will clarify points 1 to 5. Methodology: patients (6 DM2, 25 - 50 y) will
be assessed through anthropometry, clinical laboratory tests (creatinine, chemistry profile,
lipid profile, microalbuminuria glycosylated hemoglobin, vitamin B12, 25OH vitamin D and
prothrombin), dietary recalls specifically designed to analyze the regular consumption of
AGEs, serum CML and neuro-ophthalmological study (fundus, ERGMF and optic nerve conduction).
Subsequently each patient will be assigned to treatment with placebo for 3 months and then
Cholestyramine 6 g / day for 12 weeks and at the end of each period will be reassessed using
the same methodology. If patients cannot tolerate the drug, they will be assigned to a
reduced AGE diet.
Expected results: Cholestyramine will have side effect similar to placebo (mainly
digestive). The active drug and not placebo will reduce serum levels of AGEs and
electrophysiological parameters of vision at 12 weeks. It is expected that a low AGEs diet
in patients who do not tolerate the drug will also reduce serum CML although to a lesser
degree and will also induce electrophysiologic changes.
Colesevelam Versus Placebo in Cholestatic Pruritus [Recruiting]
38 patients with pruritus due to chronic cholestatic liver disease will be evaluated in an
investigator initiated, multicenter, double-blind, placebo-controlled, 3-week study
assessing the effects of colesevelam on pruritus. Colesevelam is an oral, non-absorbable
bile-acid sequestrant much more potent than cholestyramine but free of adverse effects. It
is registered as a lipid lowering agent. The intensity of symptoms will be scored by means
of daily Visual Analogue Scales (VAS). Fatigue, quality of life and cutaneous scratch
lesions will also be evaluated using quantitative instruments.
PATIENT REVIEWS / RATINGS / COMMENTS
Based on a total of 1 ratings/reviews, Prevalite has an overall score of 6. The effectiveness score is 8 and the side effect score is 8. The scores are on ten point scale: 10 - best, 1 - worst.
Prevalite review by 40 year old female patient
|Overall rating:|| || |
|Effectiveness:|| || Considerably Effective|
|Side effects:|| || Mild Side Effects|
|Condition / reason:|| || diarreah |
|Dosage & duration:|| || 1/2 hour before each meal (dosage frequency: usually 3 x a day) for the period of perspcription was for 3 months |
|Other conditions:|| || irritable bowel syndrome|
|Other drugs taken:|| || thyroid medication |
|Benefits:|| || The benefits of this treatment was there was a decreased amount of bowel movements per day. Also severe cramping and urgency to empty the bowel was decreased by 50% and meals could be enjoyed, even when out in public places where a washroom might not be available. |
|Side effects:|| || Somtimes constipation would occur, and there would be a tight, bloating feeling in the lower abdomen. |
|Comments:|| || Treatment was to take this medication one half an hour before eating a meal. Powder was to be mixed in water or other fluid except carbonated beverages. Medication was to be taken for one month to see if there was an improvement in the symptoms of constant diareah after meals. |
Page last updated: 2015-07-24