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cholestyramine (Questran)

Tradename: Questran. Indications: 1) hypercholesterolemia* (increased LDL) 2) pruritus associated with elevated levels of bile acids 3) diarrhea associated with excess fecal bile acids 4) binding of toxic agents 5) pseudomembranous colitis 6) adjunctive treatment of digitalis toxicity 7) treatment of enteric hyperoxaluria [6] * Especially useful when inflammatory liver disorder coexists with hyperlipidemia, making use of niacin & HMG CoA reductase inhibitors (statins) problematic. Dosage: 1) start 4 g PO QD/BID 2) maintenance: 4 g PO 1-5 times/day Tabs: 1g Powder: 4 g/9 g of powder (378 g) 4 g/5 g of powder (378 g) with aspartame (Questran Light) Pharmacokinetics: 1) not abdorbed from the GI tract 2) peak effects within 21 days Adverse effects: 1) constipation (1-10%) 2) abdominal pain 3) abdominal distension 4) flatulence 5) nausea/vomiting 6) diarrhea 7) increased levels of triglycerides 8) rash 9) irritation of perianal area, skin or tongue 10) hyperchloremic acidosis 11) malabsorption of fat-soluble vitamins 12) increased urinary Ca+2 excretion* 13) may increase homocysteine levels 14) may increase serum transaminase levels [6] * but decreases hyperoxaluria [6] Drug interactions: - interferes with absorption of many medications Mechanism of action: 1) depletes bile acid pool 2) removes plasma LDL 3) upregulates hepatic LDL receptors 4) binds oxalate when excessive free fatty acids bind calcium [6]

Interactions

drug interactions drug adverse effects of anti-hyperlipidemic agents monitor with bile acid sequestrants

General

bile acid sequestrant

Properties

MISC-INFO: elimination route FECES pregnancy-category C safety in lactation ?

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 354
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 7(2):7, Feb. 2000
  5. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  6. Medical Knowledge Self Assessment Program (MKSAP) 17, 18. American College of Physicians, Philadelphia 2015, 2018
  7. Department of Veterans Affairs, VA National Formulary - non formulary drug request