CIPLADOC - Publications - Management of Hyperlipidaemia

Atorlip

A Practical Guide To Management of Hyperlipidaemia

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Drug treatment for hyperlipidaemia

Class	Examples	Dose	Effects on lipids
Statins (HMG-CoA reductase inhibitors)	Simvastatin	5-80 mg	LDL by 20-60%
	Lovastatin	10-80 mg	HDL by 5-15%
	Atorvastatin	10-80 mg	Triglycerides by 10-45%
Fibrates	Gemfibrozil	1200 g	LDL by 10-15%
			HDL by 10-15%
			Triglycerides by 20-50%
—	Nicotinic acid	0.5-3 g	LDL by 10-25%
			HDL by 15-35%
			Triglycerides by 20-50%
			Lp(a) by 5-30%
Resins (Bile acid sequestrants)	Cholestyramine	4-24 g	LDL by 15-30%
	Colestipol	5-30 g	HDL by 3-5%
			No effect or Triglycerides

Every 1% decrease in cholesterol decreases CHD risk by 2.5%

Class	Main side effects	Contraindications
Statins (e.g. simvastatin)	Intestinal irritation, liver enzyme elevation, skeletal muscle inflammation	Hypersensitivity, active liver disease or unexplained persistent elevations of liver enzymes, pregnancy and lactation
Fibrates (e.g. gemfibrozil)	Gastrointestinal disturbances, headache, itching, muscle damage, increased risk of developing gallstones,	Hypersensitivity, hepatic or severe renal dysfunction, pre-existing gall bladder disease liver enzyme elevations
Nicotinic acid	Flushing, pruritus, peptic ulcer, hyperglycaemia, hyperuricaemia, liver enzyme elevations, muscle damage	Hypersensitivity, significant or unexplained hepatic dysfunction, active peptic ulcer disease, arterial bleeding, active liver disease
Bile acid sequestrants (e.g. colestipol)	Gastrointestinal disturbances, liver enzyme elevation	Hypersensitivity

Statins: the new approach

Most potent cholesterol lowering drugs
Reduction in total cholesterol and LDL-cholesterol is more than twice the reduction seen with the other classes of drugs
Mechanism of action involves inhibition of the enzyme, hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, which is essential for cholesterol synthesis
Prevent LDL oxidation
Have demonstrated a reduction in total mortality; hence these should be the preferred drugs
Reduce cardiovascular morbidity and mortality in patients with established CHD as well as those at risk of developing CHD
Exhibit a good tolerability profile

Statins currently available

Benefits with statin therapy

Prevents as well as arrests the process of atherosclerosis
Stabilises the unstable atherosclerotic plaque
Improves endothelial function
Exhibits anti-thrombotic and anti-inflammatory effects
Reduces CHD events such as angina, myocardial infarction
Reduces the risk of cerebrovascular events such as stroke
Reduces the need for angioplasty/bypass surgery
Reduces risk of restenosis in patients who have undergone angioplasty or bypass surgery
Reduces the number of hospitalisations/duration of hospital stay

Drug combinations

Indicated in patients with persistently elevated LDL values (despite monotherapy) and particularly those with established coronary and vascular disease.
Combinations include a statin drug and addition of either nicotinic acid or fibrates.
Caution to be exercised since these combinations may be associated with increased incidence of liver damage and muscle damage.

"The statin drugs are to atherosclerosis what penicillin was to infectious diseases"

— William Cifford Roberts, Editor in Chief, American Journal of Cardiology 1996; 78: 377-8

Further Reading

Medicine Update. July 1996.
Drugs of Today 1997; 33: 307-314.
Second Report of the Expert Panel on Detection, Evaluation and Treatment of High Blood Cholesterol in Adults (Adult treatment panel II). Executive summary. National Institutes of Health Publication No. 93-3096, September 1993.
Drugs and Therapeutics Bulletin 1996; 34: 89-93.
Physicians Desk Reference. 1999.
American Journal of Medicine 1998; 104(6A): 28S-32S.

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