A Textbook of Clinical Pharmacology and Therapeutics

DRUGSUSED TOTREATDYSLIPIDAEMIA 181

Dietary fat

Bile acid

Fat

Muscle

Fat

Muscle

FFA FFA

Lipoprotein

lipase

Lipoprotein

lipase

Liver

Chylomicron Remnant VLDL IDL HDL

LDL Tissue

Intestine

Ezetimibe

Resins Fibrates

HMG CoA reductase

inhibitors statins

Figure 27.6:Sites of action of lipid-lowering drugs (see Figure 27.3for abbreviations).

Table 27.2:Drugs used in dyslipidaemia

Class/drug Biochemical Effect on Effect on Adverse effects Special situations

effect coronary longevity

artery disease

Statin/simvastin, LDLpp pp q(4S,WOSCOPS) Rare: myositisqliver Contraindicated in

pravastatin transaminase pregnancy, caution in

children

Resin/cholestyramine LDLpTGqp NP Constipation, flatulence, Contraindicated in biliary

nausea obstruction

Fibrate/gemfibrozil, TGppLDLpp NP Myocitis; gastro-intestinal Contraindicated in

bezafibrate HDLq symptoms alcoholics, renal/liver

impairment

Nicotinic acid TGppLDLpp NP Flushing (PGD 2 - Useful in familial

derivatives/high-dose HDLq mediated); diarrhoea; hypercholesterolaemia;

nicotinic acid, urticaria; epigastric pain; PG-related adverse

acipimox hyperuricaemia; effects ameliorated by

hyperglycaemia aspirin before the dose

Fish oil/eicosapentanoic TGp NP NP Belching with a fishy Used in patients with

acid-rich supplements after-taste pancreatitis caused by

raised TG. Contraindicated

in patients with familial

hypercholesterolaemia,

in whom it increases

cholesterol levels

Ezetimibe LDLp NP NP Mild GI effects, myalgia Adjunct to statin in

resistant dyslipidaemia

LDL, low-density lipoprotein; TG, triglycerides; HDL, high-density lipoprotein; NP, not proven.