Prevalite Powder – Antihypercholesterolemic, Antipruritec & Antidiarrheal

  1. Trade Name: Prevalite Powder
  2. Generic Name: Cholestyramine
  3. Composition: 4 gm/sachet Cholestyramine
  4. Pharmaceutical Form: Powder

Pharmacological Action

Cholestyramine, the active ingredient of Prevalite, is the chloride salt of a basic anion-exchange.resin.
In the small intestine, cholestyramine binds bile acids forming an insoluble complex which prevents intestinal reabsorption of bile acids and promotes their fecal excretion.

As a result, the rate of hepatic conversion of cholesterol to bile acids is increased causing depletion of the hepatocytes cholesterol contents with a subsequent increase in hepatic low-density lipoprotein (LDL) receptor activity.

These changes enhance the clearance of LDL from plasma and, in turn, reduce elevated plasma cholesterol levels.

Prevalite is also of therapeutic value for the relief of pruritus, due to partial biliary obstruction, and diarrhea caused by increased concentrations of bile acids in the colon.

Prevalite, in addition, is capable of binding oxalic acid and other negatively charged molecules within the lumen of the GIT, a property which broadens the therapeutic spectrum of Prevalite

Pharmacokinetics

Cholestyramine is not absorbed from the digestive tract.

Indications

Prevalite is used for:

  • Primary prevention of coronary heart disease in men between 35 and 59 years of age and with primary hypercholesterolaemia who have not responded to diet and other appropriate measures.
  • Reduction of plasma cholesterol in hypercholesterolaemia, particularly in those patients, who have been diagnosed as Fredrickson’s Type 2 (high plasma cholesterol with normal or slightly elevated triglycerides.
  • Relief of pruritus associated with partial billiary obstruction and primary biliary cirrhosis
  • Relief of diarrhea associated with ileal resection, Crohn’s disease, vagotomy and diabetic vagal neuropathy.
  • Management of radiation-induced diarrhea.

Dosages

Adults:

1- For primary prevention of coronary heart disease and to reduce cholesterol: After initial introduction over a three to four week period, 3 to 6 Prevalite sachets per day, administered either as a single daily dose or in divided doses up to four times daily, according to dosage requirements and patient acceptability.

Dosage may be modified according to response and can be increased to 9 sachets per day if necessary.

Occasional slight gastro-intestinal upsets, e.g. constipation, may occur on starting Prevalite. These usually pass with continued usage of Prevalite and are minimised by starting therapy gradually (see Table below)

Final dose required Week 1 Week 2 Week 3 Week 4
Sachets per day
3 1 2 3 3
4 1 2 3 4
6 1 2 3 5

2- To relieve pruritus: One or two sachets daily are usually sufficient.

3- To relieve diarrhea: As for reduction of cholesterol but it may be possible to reduce this dosage. In all patients presenting with diarrhoea induced by bile acid malabsorption, if a response is not seen within 3 days, then alternative therapy should be initiated.

Children:

Children 6-12 years: 80 mg/kg body weight. 3 times daily,

Infants and children under 6 years: the dosage has not been established.

Elderly:

No dosage adjustment is necessary.

Preparation and administration:

Prevalite should not be taken in dry form. The dose is prepared by adding the contents of one sachet to a glass of water (about 150 ml).

Allow to stand without stirring for 1-2 minutes, then stir and mix thoroughly to obtain a homogeneous suspension, Prevalite may also be taken with juices or other fluids.

Contraindications

In patients with complete biliary obstruction, since Prevalite cannot be effective where bile is not secreted into the intestine.

Side effects

Since Prevalite may interfere with the absorption of fat soluble vitamins, the diet may require supplementation with Vitamins A,D and K during prolonged high dose administration.

Chronic use of Prevalite may be associated with increased bleeding tendency due to hypoprothrombinaemia associated with Vitamin K deficiency. This will usually respond promptly to parenteral Vitamin K administration; recurrences can be prevented by oral administration of Vitamin K.

Hyperchloraemic acidosis has occasionally been reported following the prolonged use of anion exchange resins.

Gastro-intestinal side effects are those most frequently reported. The principal complaint is constipation which may be controlled with the usual remedies, and frequently disappears on continued usage of Prevalite.

Large doses of Prevalite can cause diarrhoea.

Drug Interactions

Prevalite may delay or reduce the absorption of certain drugs (such as digitalis, tetracycline, chlorothiazide, warfarin and thyroxine).

The response to concomitant medication should be closely monitored and appropriate adjustments made if necessary.

Prevalite may interfere with the pharmacokinetics of drugs that undergo enterohepatic recirculation. Patients should take other drugs at least one hour before or 4-6 hours after Prevalite to minimize possible interference with their absorption.

Reference files and articles related to Prevalite sachets

Ch0lestran powder PIL – Arabic / PDF file.

Ch0lestran powder PIL – English/Medical Professions – PDF.

Cholestyramine – Brand names of medicines available in the countries of the Middle East and North Africa

The following list contains a list of the trade names of medicines containing cholestyramine at a concentration of 4 grams (4000 milligrams) in each sachet. All the pharmaceutical products mentioned later are considered equivalent products, and any of them replaces the other in the event that it is not available:

  • Ch0lestran sachets – Pharco Pharmaceutical Company / Egypt.
  • Quantamash Bags – Mash Premier Company/ Egypt.
  • Qustran sachets – Bristol-Myers Squibb / Multinational Company

Cholestyramine

  • Trade name: Prevalite powder for oral suspension preparation.
  • Pharmaceutical form: sachets containing 4 grams of powder.
  • Scientific name: cholestyramine.
  • Common Uses: Increased cholesterol in the blood – Itching associated with jaundice
  • Legal description: dispensed by prescription
  • Therapeutic group: Blood lipid modulators.
  • Therapeutic subclass: bile acid sePrevalitets.
  • Therapeutic and Anatomical Classification Code: C10AC01.