Cholestasis Medication

Updated: Aug 09, 2017
  • Author: Hisham Nazer, MB, BCh, FRCP, , DTM&H; Chief Editor: Carmen Cuffari, MD  more...
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Medication

Choleretic agents

Class Summary

Ursodeoxycholic acid acts to increase bile formation and antagonizes the effect of hydrophobic bile acids on biological membranes.

Ursodeoxycholic acid (Actigall, Urso)

Shown to promote bile flow in cholestatic conditions associated with a patent extrahepatic biliary system. Decreases the cholesterol content of bile and therefore reduces bile stone and sludge formation.

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Barbiturates

Class Summary

These agents are used to induce hepatic enzyme metabolism in order to decrease serum bilirubin levels in some patients with cholestasis in order to improve function.

Phenobarbital (Luminal)

Mainly used as an anticonvulsant, which interferes with transmission of impulses from thalamus to cortex of brain, resulting in imbalance in central inhibitory and facilitatory mechanisms. Used in cholestasis to induce the CYP450 system in treatment of neonatal hyperbilirubinemia and lowering of bilirubin in chronic cholestasis.

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Vitamins

Class Summary

Fat-soluble vitamins A, D, E, and K must be administered as individual supplements to assure proper absorption.

Phytonadione (AquaMEPHYTON)

Vitamin K. Fat-soluble vitamin absorbed by the gut and stored in the liver. Necessary for the function of clotting factors in the coagulation cascade. Used to replace essential vitamins not obtained in sufficient quantities in the diet or to further supplement levels.

Vitamin E (Liqui E)

Vitamin E. Prevention and treatment of hemolytic anemia secondary to vitamin deficiency or need for dietary supplementation. Protects polyunsaturated fatty acids in membranes from attack by free radicals and protects RBC against hemolysis.

Vitamin A (Aquasol A)

Needed for bone development, growth, visual adaptation to darkness, testicular and ovarian function, and as a cofactor in many biochemical processes.

Ergocalciferol (Drisdol, Calciferol)

Vitamin D. Stimulates absorption of calcium and phosphate from small intestine and promotes release of calcium from bone into blood. PO solution comes as 8000 U/mL (200 mcg/mL, 40 U/mcg).

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Opioid antagonists

Class Summary

These agents are used to alleviate pruritus caused by cholestasis. They block opioid-mediated pathways of afferent nerves, which may be producing the itching sensation.

Naltrexone (ReVia)

Cyclopropyl derivative of oxymorphone that acts as a competitive antagonist at opioid receptors. Do not administer this medication until the patient is opioid-free for 7-10 d. Available as 50-mg tab.

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Bile salt resins

Class Summary

Bile acid–binding resins form a nonabsorbable complex with bile acids in the intestine, which inhibits enterohepatic reuptake of intestinal bile salts and thereby increases the fecal losses of bile salt–bound low-density lipoprotein cholesterol.

Cholestyramine (Questran, Prevalite)

May use as adjunct in primary hypercholesterolemia. Forms a nonabsorbable complex with bile acids in the intestine, which, in turn, inhibits enterohepatic reuptake of intestinal bile salts. Dose based on resin content.

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Antibiotics

Class Summary

Antitubercular agents induce liver enzymes and ameliorate pruritus secondary to cholestasis.

Rifampin (Rimactane, Rifadin)

Inhibits RNA synthesis in bacteria by binding to beta subunit of DNA-dependent RNA polymerase, which, in turn, blocks RNA transcription.

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Gastrointestinal Agents, Other

Obeticholic acid (Ocaliva)

It is a framesoid X receptor (FXR) agonist is recommended for the treatment of primary biliary cirrhosis. It has been licensed by the FDA. 

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