General Description
White to buff-colored fine powder. Odorless or a slight amine odor. Insoluble in water. A synthetic strongly basic anion exchange resin in which quaternary ammonium groups are attached to a styrene/divinylbenzene copolymer chain.
Air & Water Reactions
Hygroscopic [Merck.] Insoluble in water.
Reactivity Profile
An amine. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.
Health Hazard
SYMPTOMS: Symptoms of exposure to CHOLESTYRAMINE RESIN may include nausea, abdominal discomfort indigestion and constipation. It also causes vitamin K deficiency, rash, mucous membrane irritation, osteoporosis and eosinophilia. Other symptoms include flatulence, vomiting, diarrhea, heartburn, anorexia, steatorrhea, vitamin A and D deficiencies and hyperchloremic acidosis in children.
Fire Hazard
Flash point data for CHOLESTYRAMINE RESIN are not available. CHOLESTYRAMINE RESIN is probably combustible.
Hazard
Low toxicity; tumorigen; questionable carcinogen; teratogen.
Chemical Properties
White or almost white, fine powder, hygroscopic.
Brand name
Cholybar (Parke-
Davis); Duolite AP143 Resin (Rohm and Haas); Questran
(Bristol Labs); Questran Light (Bristol Labs).
Pharmacology
Cholestyramine, an anion exchange resin,
is frequently effective, although, as mentioned earlier, its antipruritic effect
seems separate from its ability to normalize bile salt levels.
Clinical Use
Cholestyramine resin is the drug of choice for type IIa hyperlipoproteinemia.When used in conjunction with a controlleddiet, it reduces -lipoproteins. The drug is an insolublepolymer and, thus, probably one of the safest because itis not absorbed from the gastrointestinal tract to cause systemictoxic effects.
Synthesis
Cholestyramine (20.1.2) is a copolymer of divinylbenzene and styrene,
which undergoes chloromethylation and afterwards is reacted with triethylamine.
Drug interactions
Potentially hazardous interactions with other drugs
Anticoagulants: effect of coumarins and phenindione
may be enhanced or reduced.
Ciclosporin: may interact unpredictably with
ciclosporin. Take ciclosporin at least 1 hour before or
4-6 hours after to prevent problems with absorption.
Leflunomide: avoid concomitant use.
Raloxifene, thyroid hormones, bile acids, valproate,
cardiac glycosides and mycophenolate mofetil:
absorption reduced.
Metabolism
Not applicable as colestyramine resin is not absorbed
from the digestive tract.