TRC: Bile acid resins

Bile acid resins

Bile acid resins or sequestrants (cholestyramine, cholesevelam) exchange chloride against bile acids in the intestine, thereby inhibiting the enterohepatic recirculation of bile acids. This promotes the upregulation of 7-α-hydroxylase (pink) and the conversion of more cholesterol in the hepatocyte into bile acids. This decreases the cholesterol content in the hepatocyte, which enhances LDL-receptor expression, which in turn increases the removal of LDL and VLDL remnant particles from the circulation. The liver also increases its synthesis of cholesterol, which sets a new equilibrium with lower LDL levels.

Bile acid resins are not absorbed from the GI tract and thus lack systemic toxicity. However, the GI side effects are numerous and dose limiting. These include constipation, bloating, abdominal pain, nausea, and flatulence.

Bile acid resins can decrease the absorption of other drugs administered concurrently, including fat-soluble vitamins, and so it is recommended that other drugs be taken an hour before or 4 hours after the bile acid resin.

Bile acid resins can cause all of the following EXCEPT

increased de novo synthesis of cholesterol in the liver

reduction of bile acid synthesis

establishment of a new LDL balance, which is 10% lower

downregulation of the LDL-receptor

Regarding the treatment of dyslipidemia: which is false?

Extra info: Bile acid sequestrants are less effective in lowering LDL and thus not the best option for refractory patients.

bile acid resins are a good option for patients who are intolerant of statins or whose condition is refractory to statins.

cholesterol absorption inhibitors lower trigl/chol levels by 20% regardless of concurrent therapy.

fibrates are recommended for patients with hypertriglyceridemia and atherogenic dyslipidemia

niacin is recommended for patients with isolated, low HDL levels and atherogenic dyslipidemia

Bile acid resins

Bile acid resins

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