Volume 1 Guidelines Lipid-Lowering Agents

LIPID-LOWERING AGENTS

For a description of indications, actions, side effects, potency of drugs and dosage see Credits.

Bile acid sequestrants (resins)

Bile acid sequestrants are effective in lowering LDL cholesterol, both in familial hypercholesterolaemia (at full dosage) and in other forms of diet-resistant hypercholesterolaemia (often in lower, easily tolerated dosage):

HDL cholesterol increases slightly

combination with a statin may be useful in severe hypercholesterolaemia

as triglyceride levels may increase, resins are not suitable in combined (mixed) hyperlipidaemia unless a triglyceride-lowering drug is also given

Dosage of bile acid sequestrants (resins)

Administered as powders mixed with fluid. Taken twice daily with meals or daily at low dosage:

cholestyramine 4 - 24 g/day

colestipol 5 - 30 g/day

HMG CoA reductase inhibitors (statins)

HMG CoA reductase inhibitors are highly effective in all conditions where LDL cholesterol elevation is the predominant disorder:

they are suitable first-line agents in familial hypercholesterolaemia

moderate effect in lowering triglyceride and in elevating HDL cholesterol

treatment is commenced at minimum dosage

serum lipids and alanine transferase are measured at 6 - 8 weeks and dosage is increased stepwise if necessary

patients with very high pretreatment cholesterol levels may need combined therapy with resins

statins should not be used in women of child-bearing age unless contraception is fully satisfactory

Dosage of HMG CoA reductase inhibitors (statins)*

HMG CoA reductase inhibitors are administered in tablet form:

lovastatin 10 - 80 mg/day once nightly with the evening meal, or in divided doses

pravastatin 5 - 40 mg nightly

simvastatin 5 - 40 mg nightly

* In some countries the dosage recommendations may vary: please consult product labeling.

Fibric acid derivatives (fibrates)

Fibric acid derivatives are particularly useful in patients with combined (mixed) hyperlipidaemia and hypertriglyceridaemia:

they reduce serum triglyceride effectively

they increase HDL cholesterol substantially

they can be used in mild to moderate hypercholesterolaemia, in which LDL cholesterol may be lowered

treatment is usually commenced with a recommended optimal dosage

serum alanine transferase is monitored

Dosage of fibric acid derivatives (fibrates)

Fibric acid derivatives are administered in tablet (capsule) form:

bezafibrate 20 mg x 3 daily
or sustained release form, 400 mg daily

ciprofibrate 100 - 200 mg daily

fenofibrate 100 mg x 3 daily
or micronised form, 200 mg x 1 daily

gemfibrozil 600 mg x 2 daily
or sustained release form, 900 mg x 1 daily

Nicotinic acid

Niocotinic acid effectively lowers booth serum cholesterol and triglyceride levels:

side effects tend to limit compliance

cutaneous flushing and abdominal symptoms are the most common problems

liver disease, gout and diabetes are relative contraindications

routine monitoring for signs of these diseases is necessary

Dosage of nicotinic acid

Nicotinic acid is available as tablets of 25 mg to 500 mg, also in sustained release form:

starting dose: 100 mg x 3 daily
titration of dose up to 2 - 6 g/day

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