Colesevelam, colestipol, and colestyramine are bile acid sequestrants used in the management of hyper-cholesterolaemia. They act by binding bile acids, preventing their reabsorption; this promotes hepatic conversion of cholesterol into bile acids; the resultant increased LDL-receptor activity of liver cells increases the clearance of LDL-cholesterol from the plasma. Bile
1. Simvastatin 10 mg tablets can be sold to the public to reduce risk of first coronary event in individuals at moderate risk of coronary heart disease (approx. 10-15% risk of major event in 10 years), max. daily dose 10 mg and pack size of 28 tablets; treatment should form part of a programme to reduce risk of coronary heart disease acid sequestrants effectively reduce LDL-cholesterol but can aggravate hypertriglyceridaemia.
Cautions Bile acid sequestrants interfere with the absorption of fat-soluble vitamins; supplements of vitamins A, D, K, and folic acid may be required when treatment is prolonged. Interactions: Appendix 1 (bile acid sequestrants)
Pregnancy and breast-feeding Bile acid sequestrants should be used with caution as although the drugs are not absorbed, they may cause fat-soluble vitamin deficiency on prolonged use.
Side-effects As bile acid sequestrants are not absorbed, gastro-intestinal side-effects predominate. Constipation is common, but diarrhoea has occurred, as have nausea, vomiting, and gastro-intestinal discomfort. Hypertriglyceridaemia may be aggravated. An increased bleeding tendency has been reported due to hypoprothrombinaemia associated with vitamin K deficiency.
Counselling Other drugs should be taken at least 1 hour before (4 hours before colesevelam), or 4-6 hours after bile acid sequestrants to reduce possible interference with absorption. Colesevelam can be taken at the same time as a statin or ezetimibe.
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