Bile acid sequestrant for high cholesterol launched

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The Pharmaceutical Journal
Vol 279 No 7481 p641
8 December 2007

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Bile acid sequestrant for high cholesterol launched

Cholestagel impedes the reabsorption of bile acids in the intestine

Mechanism of action

Bile acid sequestrants bind bile acids in the intestine, impeding their reabsorption.

As the bile acid pool becomes depleted the liver enzyme cholesterol 7-a-hydroxylase is upregulated, increasing the conversion of cholesterol to bile acids.

Low-density lipoprotein receptor synthesis on hepatocyctes also increases, resulting in a reduction in circulating LDL-cholesterol. Colesevelam is not absorbed systemically.

Patients with high cholesterol may benefit from treatment with colesevelam hydrochloride, a new bile acid sequestrant therapy. The medicine is the first of its kind to be available in the UK in tablet form.

Marketed as Cholestagel by Genzyme, colesevelam is indicated as an adjunct to statin therapy and dietary measures for people with primary hypercholesterolaemia whose condition is not adequately controlled by the statin alone.

People who cannot take statins can use colesevelam as monotherapy for reduction of elevated total and low-density lipoprotein cholesterol.

The usual daily dose is six 625mg tablets. The dose can be taken as three tablets twice a day with meals or as a single six-tablet dose with a meal.

Because colesevelam can increase patients’ triglyceride levels, patients with triglyceride levels higher than 3.4mmol/L were excluded from clinical studies of the drug. The manufacturer therefore recommends caution when treating such patients.

Concomitant anticoagulation therapy should be monitored closely — bile acid sequestrants have been shown to interfere with both vitamin K absorption and the anticoagulant effect of warfarin.