Sequest

Cholestyramine.

Each sachet contains Cholestyramine 4 grams.

Cholestyramine resin absorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterophatic circulation by preventing their adsorption. The increased fecal loss of bile acids due to Cholestyramine resin administration leads to an increase oxidation of cholesterol to bile acids, a decrease in β-lipoprotein or low density lipoprotein plasma levels and decrease in serum cholesterol levels.

Adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia who do not respond adequately to diet.
Cholestyramine may be useful to lower elevated cholesterol that occurs in patients with combined hypercholesterolemia and hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormally of most concern.
For the relief of pruritus associated with partial biliary obstruction.
As an adjunct to rehydration therapy, for relieve of diarrhea due to bile acid malabsorption, associated with ileal resection, Chron's disease, vagotomy and diabetic vagal neuropathy.

Cholestyramine should not to be taken in its dry form. Always mix with water or other fluids before ingesting.
Place the content of one sachet in a glass and add least 60-180 mL of water or the beverage of your choice. Stir to a uniform consistency. Since Cholestyramine may bind other drugs given currently, patients should take other drugs at least one hour before or 4-6 hours after Cholestyramine to avoid impending their absorption.
Adult: To reduce cholesterol levels and incidence of heart attack: begin with one sachet (equivalent to 4 grams of anhydrous Cholestyramine resin) in 60-180 mL of fluid in the morning and in the evening. After 2-4 weeks, increase dose to 8 grams of Cholestyramine resin in 120-360 mL water in the morning and in the evening. If necessary, increase medication to the maximum 24 grams of Cholestyramine resin for cholesterol reduction. The suggested time of administration is mealtime, but this may be modified to avoid interference with absorption of other medications. Although the recommended dosing schedule is twice daily, Cholestyramine may be administered in 1-6 doses per day. If dose increases are necessary, they should be done gradually, and with periodic assessment of lipid/lipoprotein levels. Doses of more than 24 grams a day of Cholestyramine resin may interfere with normal fat absorption.
Concomitant therapy: The cholesterol-lowering effect of Cholestyramine on Total and LDL-Cholesterol is enhanced when it is combined with an HMG-CoA reductase inhibitor (e.g. Pravastatin, Simvastatin, Lovastatin). Enhanced lowering of LDL-cholesterol is also seen with combined Nicotinic Acid/Cholestyramine therapy.
To relieve pruritus due to partial biliary obstruction and primary biliary cirrhosis: 4-8 grams of Cholestyramine resin daily.
Children 6-12 years: To reduce cholesterol levels or to relieve pruritus: (see equation)


Click on icon to see table/diagram/image


Further adjustment may be required depend on the patient condition. Dosage for children below 6 years has not been established. To minimize potential gastrointestinal side effects, it is desirable to begin all therapy in children with one dose of Cholestyramine daily. The dosage is then increased gradually, every 5-7 days to desired level for effective control.
Note: In all patients presenting with a diarrhea induced by bile acid malabsorption, a response should be seen within days, if this is not the case, alternate therapy should be initiated. To relieve diarrhea induced by the bile-acid malabsorption: The initial dosage of Cholestyramine should be 4 grams Cholestyramine resin 3 times a day, with subsequent adjustment as needed.

Patient with a complete biliary obstruction where bile is not secreted into the intestine and in those individuals who have shown hypersensitivity to any of the components of SEQUEST.

Discontinue therapy if there is no significant reduction in cholesterol level.
Before constituting therapy with Cholestyramine, disease contributing to increased blood cholesterol such as hypothyroidism, diabetes mellitus, nephrotic syndrome, dysproteinemia and obstructive liver disease should be looked for and specifically treated. In addition, prior to instituting therapy with Cholestyramine, an attempt should be made to control serum cholesterol by appropriate dietary regimen, weight reduction and the treatment of any underlying disorder which might be the cause of the hypercholesterolemia. Serum cholesterol levels should be determined frequently during the first few months of therapy and periodically thereafter. A favourable trend in cholesterol reduction should occur during the first month of Cholestyramine therapy. The therapy should be continued to sustain cholesterol reduction.
Serum triglyceride levels should be measured periodically to detect whether significant changes have occurred.
Because it sequester bile acids, Cholestyramine resin may interfere with normal fat absorption when given in high doses (24 grams daily). When given in these high doses, Cholestyramine may prevent absorption of fat-soluble vitamins such as Vitamin A, D and K. therefore, when Cholestyramine is to be given in high doses for long time periods, daily supplement of Vitamin A, D and K should be considered.
[Chronic use of Choletyramine resin may be associated with increased bleeding tendency due to hypoprothrombinemia 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]. Reduction of serum or red cell folate has occurred and treatment with folic acid should be considered in these cases.
Since Cholestyramine resin may bind other drugs given concurrently, the interval between the administration of Cholestyramine resin and other medication should be as great as feasible.
There is a possibility that prolonged use of Cholestyramine resin in high doses may produce hyperchloremic acidosis, since it is the chloride form an anion exchange resin. This is especially true in younger and smaller patients where the relative dosage may be higher. Cholestyramine resin may aggravate pre-existing constipation or related condition such as haemorrhoids. In patients with constipation, the dosage of Cholestyramine resin should be decreased, since it may produce impaction. In patients presenting with symptomatic coronary artery disease, where straining of the stool is to be avoided, the dosage of Cholestyramine should be titrated to avert constipation.
Pregnancy and lactation: Since Cholestyramine resin is not absorbed systematically, it is not expected to cause fetal harm when administered during pregnancy in recommended dosage. Caution should be exercised when Cholestyramine resin is administered to nursing mother. The possible lack of proper vitamin adsorption described previously may have an effect on nursing infants.

Since Cholestyramine resin is not absorbed systematically, it is not expected to cause fetal harm when administered during pregnancy in recommended dosage. Caution should be exercised when Cholestyramine resin is administered to nursing mother. The possible lack of proper vitamin adsorption described previously may have an effect on nursing infants.

The most common side effect is constipation. Some patients require a temporary decrease in dosage or discontinuation of therapy.
Other side effect is abdominal discomfort, flatulence, nausea, vomiting, diarrhea, heartburn, anorexia, steatorrhea, rash and irritation on skin, tongue and perianal area.
Hematologic: prolonged prothrombin time ecchymosis or anemia.
Gastrointestinal: GI rectal bleeding, black stool/s, hemorrhoidal bleeding, ulcer attack, sour taste, pancreatitis, rectal pain or diverticulitis.
Hypersensitivity: urticaria, asthma, wheezing or shortness of breath.
Musculoskeletal: backache, muscle and joint pains or arthritis.
Neurologic: headache, anxiety, vertigo, dizziness, fatigue, tinnitus, syncope, drowsiness, femoral nerve pain.
Eye: uveitis.
Renal: hematuria, dysuria, diuresis.
Miscellaneous: weight loss, weight gain, increase libido, swollen glands, edema or dental bleeding.

Since Cholestyramine resin may bind other drug given concurrently, patients should take other drug at least 1 hour before or 4-6 hours after Cholestyramine resin to avoid impending their absorption.
Reduces absorption of phenylbutazone, warfarin, chlorothiazide, tetracycline, penicillin G, phenobarbital, thyroid preparations and digitalis.

Store at temperature 25°-30°C.
After reconstitution, store in maximum 24 hours at temperature 25°-30°C or 7 days in a refrigerator (2°-8°C).
It is recommended to drink it immediately after reconstitution.

Dyslipidaemic Agents / Antidiarrheals

C10AC01 - colestyramine ; Belongs to the class of bile acid sequestrants. Used in the treatment of hyperlipidemia.

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