High Cholesterol

COLESTID (Colestipol hydrochloride)

DESCRIPTION

The active ingredient in COLESTID Tablets is micronized colestipol hydrochloride, which is a lipid lowering agent for oral use.

Type of medication:

Part of group of medications called bile acid binders or resins

CLINICAL PHARMACOLOGY

Cholesterol is the major precursor of bile acids. During digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. Only very small amounts of bile acids are found in normal serum. Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. Colestipol is a resin.

INDICATIONS

COLESTID Tablets are indicated as adjunctive therapy to diet for the reduction of elevated serum total cholesterol and LDL cholesterol in patients with hypercholesterolemia who do not respond adequately to diet. COLESTID Tablets have no clinically significant effect on serum triglycerides. 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.

DOSAGE

For adults, COLESTlD Tablets are recommended in doses of 2 to 16 grams/day given once or in divided doses. The starting dose should be 2 grams once or twice daily. Dosage increases of 2 grams, once or twice daily should occur at 1- or 2-month intervals.

SIDE EFFECTS

Gastrointestinal The most common adverse reactions are confined to the gastrointestinal tract. To achieve minimal gastrointestinal disturbance with an optimal LDL cholesterol lowering effect, a gradual increase of dosage is recommended. Constipation is the major single complaint and at times is severe. Most instances of constipation are mild, transient, and controlled with standard treatment. Increased fluid intake and inclusion of additional dietary fiber should be the first step; a stool softener may be added if needed. Some patients require decreased dosage or discontinuation of therapy. Hemorrhoids may be aggravated. Other, less frequent gastrointestinal complaints consist of abdominal pain and cramping, intestinal gas (bloating and flatulence), indigestion, heartburn, diarrhea, loose stools, nausea and vomiting.

Cardiovascular: Chest pain, angina, and tachycardia have been reported.
Hypersensitivity: Rash has been reported. Urticaria and dermatitis have been rarely noted in patients receiving colestipol hydrochloride granules.
Musculoskeletal: Musculoskeletal pain, aches and pains in the extremities, joint pain and arthritis, and backache have been reported.
Neurologic: Headache, migraine headache, and sinus headache have been reported.
Other reported complaints include dizziness, light-headedness, and insomnia.

DRUG INTERACTIONS

Studies have indicated that colestipol hydrochloride binds a number of drugs. Therefore, COLESTlD Tablets may delay or reduce the absorption of concomitant oral medication. The interval between the administration of COLESTID Tablets and any other medication should be as long as possible. Patients should take other drugs at least one hour before or four hours after COLESTID Tablets to avoid impeding their absorption. Decrease of propranolol absorption has been reported. Chlorothiazide decreased. The absorption of tetracycline, furosemide, penicillin G, hydrochlorothiazide, and gemfibrozil was significantly decreased when given simultaneously with colestipol hydrochloride.

Use in Pregnancy

Since colestipol hydrochloride is not absorbed systemically, it is not expected to cause fetal harm when administered during pregnancy in recommended dosages.

Nursing Mothers

Caution should be exercised when COLESTID Tablets are administered to a nursing mother. The possible lack of proper vitamin absorption may have an effect on nursing infants.

CONTRAINDICATIONS

COLESTID Tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components.
 

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