Colestipol Hydrochloride 5000 MG Oral Granules [Colestid]
Generic Name: COLESTIPOL HYDROCHLORIDE
Brand Name: Colestid
- Substance Name(s):
- COLESTIPOL HYDROCHLORIDE
WARNINGS
TO AVOID ACCIDENTAL INHALATION OR ESOPHAGEAL DISTRESS, COLESTID GRANULES AND FLAVORED COLESTID GRANULES SHOULD NOT BE TAKEN IN ITS DRY FORM.
ALWAYS MIX COLESTID AND FLAVORED COLESTID WITH WATER OR OTHER FLUIDS BEFORE INGESTING.
PHENYLKETONURICS: FLAVORED COLESTID CONTAINS 18.2 MG PHENYLALANINE PER 7.5-GRAM DOSE.
DRUG INTERACTIONS
Drug Interactions Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids.
In vitro studies have indicated that colestipol hydrochloride binds a number of drugs.
Therefore, COLESTID and FLAVORED COLESTID resin may delay or reduce the absorption of concomitant oral medication.
The interval between the administration of COLESTID and FLAVORED COLESTID 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 and FLAVORED COLESTID to avoid impeding their absorption.
Repeated doses of colestipol hydrochloride given prior to a single dose of propranolol in human trials have been reported to decrease propranolol absorption.
However, in a follow-up study in normal subjects, single dose administration of colestipol hydrochloride and propranolol and twice-a-day administration for 5 days of both agents did not effect the extent of propranolol absorption, but had a small yet statistically significant effect on its rate of absorption; the time to reach maximum concentration was delayed 30 minutes.
Effects on the absorption of other beta-blockers have not been determined.
Therefore, patients on propranolol should be observed when COLESTID or FLAVORED COLESTID is either added or deleted from a therapeutic regimen.
Studies in humans show that the absorption of chlorothiazide as reflected in urinary excretion is markedly decreased even when administered one hour before colestipol hydrochloride.
The absorption of tetracycline, furosemide, penicillin G, hydrochlorothiazide, and gemfibrozil was significantly decreased when given simultaneously with colestipol hydrochloride; these drugs were not tested to determine the effect of administration one hour before colestipol hydrochloride.
No depressant effect on blood levels in humans was noted when colestipol hydrochloride was administered with any of the following drugs: aspirin, clindamycin, clofibrate, methyldopa, nicotinic acid (niacin), tolbutamide, phenytoin or warfarin.
Particular caution should be observed with digitalis preparations since there are conflicting results for the effect of colestipol hydrochloride on the availability of digoxin and digitoxin.
The potential for binding of these drugs if given concomitantly is present.
Discontinuing colestipol hydrochloride could pose a hazard to health if a potentially toxic drug that is significantly bound to the resin has been titrated to a maintenance level while the patient was taking colestipol hydrochloride.
Bile acid binding resins may also interfere with the absorption of oral phosphate supplements and hydrocortisone.
A study has shown that cholestyramine binds bile acids and reduces mycophenolic acid exposure.
As colestipol also binds bile acids, colestipol may reduce mycophenolic acid exposure and potentially reduce efficacy of mycophenolate mofetil.
OVERDOSAGE
Overdosage of COLESTID Granules or FLAVORED COLESTID Granules has not been reported.
Should overdosage occur, however, the chief potential harm would be obstruction of the gastrointestinal tract.
The location of such potential obstruction, the degree of obstruction and the presence or absence of normal gut motility would determine treatment.
DESCRIPTION
COLESTID Granules and FLAVORED COLESTID Granules contain colestipol hydrochloride, which is a lipid lowering agent for oral use.
Colestipol hydrochloride is an insoluble, high molecular weight basic anion-exchange copolymer of diethylenetriamine and 1-chloro-2, 3-epoxypropane, with approximately 1 out of 5 amine nitrogens protonated (chloride form).
It is a light yellow water-insoluble resin which is hygroscopic and swells when suspended in water or aqueous fluids.
COLESTID is tasteless and odorless.
Inactive ingredient: silicon dioxide.
One dose (1 packet or 1 level teaspoon) of COLESTID contains 5 grams of colestipol hydrochloride.
FLAVORED COLESTID is orange flavored and light orange in color.
One dose (1 packet or 1 level scoopful) of FLAVORED COLESTID is approximately 7.5 grams which contains 5 grams of colestipol hydrochloride.
This product also contains the following inactive ingredients: aspartame, beta carotene, citric acid, flavor (natural and artificial), glycerine, maltol, mannitol, and methylcellulose.
HOW SUPPLIED
COLESTID Granules are available as follows: Cartons of 30 foil packets — NDC 0009-0260-01 Cartons of 90 foil packets — NDC 0009-0260-04 Bottles of 300 grams with scoop — NDC 0009-0260-17 Bottles of 500 grams with scoop — NDC 0009-0260-02 Each packet or level scoop supplies 5 grams of COLESTID.
FLAVORED COLESTID Granules are available as follows: Cartons of 60 foil packets — NDC 0009-0370-03 Bottles of 450 grams (equivalent to approximately 60 doses) with scoop — NDC 0009-0370-05 Each packet or each level scoopful supplies approximately 7.5 grams of FLAVORED COLESTID containing 5 grams of colestipol hydrochloride.
Store at controlled room temperature 20° to 25° C (68° to 77° F) [see USP].
INDICATIONS AND USAGE
Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use.
COLESTID Granules and FLAVORED COLESTID Granules are indicated as adjunctive therapy to diet for the reduction of elevated serum total and low-density lipoprotein (LDL) cholesterol in patients with primary hypercholesterolemia (elevated low density lipoproteins [LDL] cholesterol) who do not respond adequately to diet.
Generally, COLESTID and FLAVORED COLESTID have no clinically significant effect on serum triglycerides, but with its use triglyceride levels may be raised in some patients.
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 (see NCEP guidelines).
A minimum of six months of intensive dietary therapy and counseling should be carried out prior to initiation of drug therapy.
Shorter periods may be considered in patients with severe elevations of LDL-C or with definite CHD.
According to the NCEP guidelines, the goal of treatment is to lower LDL-C, and LDL-C is to be used to initiate and assess treatment response.
Only if LDL-C levels are not available, should the Total-C be used to monitor therapy.
The NCEP treatment guidelines are shown below.
LDL-Cholesterol mg/dL (mmol/L) Definite Atherosclerotic DiseaseCoronary heart disease or peripheral vascular disease (including symptomatic carotid artery disease).
Two or More Other Risk FactorsOther risk factors for coronary heart disease (CHD) include: age (males: ≥45 years; females: ≥55 years or premature menopause without estrogen replacement therapy); family history of premature CHD; current cigarette smoking; hypertension; confirmed HDL-C <35 mg/dL (0.91 mmol/L); and diabetes mellitus.
Subtract one risk factor if HDL-C is ≥60 mg/dL (1.6 mmol/L).
Initiation Level Goal No No ≥190 (≥4.9) <160 (<4.1) No Yes ≥160 (≥4.1) <130 (<3.4) Yes Yes or No ≥130 (≥3.4) ≤100 (≤2.6)
PEDIATRIC USE
Pediatric Use Safety and effectiveness in the pediatric population have not been established.
PREGNANCY
Use in Pregnancy Since colestipol hydrochloride is essentially not absorbed systemically (less than 0.17% of the dose), it is not expected to cause fetal harm when administered during pregnancy in recommended dosages.
There are no adequate and well controlled studies in pregnant women, and the known interference with absorption of fat soluble vitamins may be detrimental even in the presence of supplementation.
The use of COLESTID or FLAVORED COLESTID in pregnancy or by women of childbearing potential requires that the potential benefits of drug therapy be weighed against possible hazards to the mother or child.
NUSRING MOTHERS
Nursing Mother Caution should be exercised when COLESTID or FLAVORED COLESTID is administered to a nursing mother.
The possible lack of proper vitamin absorption described in the “pregnancy” section may have an effect on nursing infants.
DOSAGE AND ADMINISTRATION
One dose (1 packet or 1 level teaspoon) of COLESTID Granules contains 5 grams of colestipol hydrochloride.
One dose (1 packet or 1 level scoopful) of FLAVORED COLESTID Granules is approximately 7.5 grams which contains 5 grams of colestipol hydrochloride.
The recommended daily adult dose is one to six packets or level scoopfuls given once or in divided doses.
Treatment should be started with one dose once or twice daily with an increment of one dose/day at one- or two-month intervals.
Appropriate use of lipid profiles as per NCEP guidelines including LDL-cholesterol and triglycerides is advised so that optimal, but not excessive doses are used to obtain the desired therapeutic effect on LDL-cholesterol level.
If the desired therapeutic effect is not obtained at one to six doses/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered.
To avoid accidental inhalation or esophageal distress, COLESTID and FLAVORED COLESTID should not be taken in its dry form.
COLESTID and FLAVORED COLESTID should always be mixed with water or other fluids before ingesting.
Patients should take other drugs at least one hour before or four hours after COLESTID or FLAVORED COLESTID to minimize possible interference with their absorption.
(See PRECAUTIONS, Drug Interactions.) Before COLESTID or FLAVORED COLESTID Administration Define the type of hyperlipoproteinemia, as described in NCEP guidelines.
Institute a trial of diet and weight reduction.
Establish baseline serum total and LDL-cholesterol and triglyceride levels.
During COLESTID or FLAVORED COLESTID Administration The patient should be carefully monitored clinically, including serum cholesterol and triglyceride levels.
Periodic determinations of serum cholesterol levels as outlined in the NCEP guidelines should be done to confirm a favorable initial and longer-term response.
Failure of total or LDL-cholesterol to fall within the desired range should lead one to first examine dietary and drug compliance.
If these are deemed acceptable, combined therapy or alternate treatment should be considered.
Significant rise in triglyceride level should be considered as indication for dose reduction, drug discontinuation, or combined or alternate therapy.
Mixing and Administration Guide COLESTID and FLAVORED COLESTID should always be mixed in a liquid such as water or the beverage of your choice.
It may also be taken in soups or with cereals or pulpy fruits.
COLESTID or FLAVORED COLESTID should never be taken in its dry form.
FLAVORED COLESTID is an orange-flavored product.
Although it may be mixed with a variety of liquids or foods, the selection should be based on patient preference.
With Beverages Add the prescribed amount of COLESTID or FLAVORED COLESTID to a glassful (three ounces or more) of water or the beverage of your choice.
A heavy or pulpy juice may minimize complaints relative to consistency.
Stir the mixture until the medication is completely mixed.
(COLESTID and FLAVORED COLESTID will not dissolve in the liquid.) COLESTID and FLAVORED COLESTID may also be mixed with carbonated beverages, slowly stirred in a large glass; however, this mixture may be associated with GI complaints.
Rinse the glass with a small amount of additional beverage to make sure all the medication is taken.
With cereals, soups, and fruits COLESTID and FLAVORED COLESTID may be taken mixed with milk in hot or regular breakfast cereals, or even mixed in soups that have a high fluid content.
It may also be added to fruits that are pulpy such as crushed pineapple, pears, peaches, or fruit cocktail.