ANTILIPIDEMIC DRUGS

Presented by:JO-ANNE V. ROVIRA

Antilipidemia

It lowers the abnormal lipid levels. Lipids composed of cholesterol, triglycerides, and

phospholipids are transported in the body and are bound to protein in various amounts.

These lipoproteins are classified as chylomicrons, very low- density lipoproteins (VLDL), low- density lipoproteins (LDL), and high- density lipoproteins (HDL).

The HDL (friendly or “good” lipoproteins) have a higher percentage of protein and less lipids. Their function is to remove cholesterol from the bloodstream and deliver it to the liver.

The other three lipoproteins are composed mainly of cholesterol and triglycerides and contribute to atherosclerotic plaque in the blood vessels. They are “bad” lipoproteins.

When cholesterol, triglycerides, and LDL are elevated, the client is at risk for coronary artery disease (CAD).

NONPHARMACOLOGIC METHODS FOR CHOLESTEROL REDUCTION

Before antilipidemics are prescribed, nondrug therapy should be initiated for decreasing blood pressure. The saturated fats and cholesterol in the diet should be reduced. Total fat intake should be 300 mg or less. The client should read labels on containers and buy appropriate foods. Clients should choose lean meats, especially chicken and fish.

But in many cases, diet alone will not lower blood lipid levels. Because 75% to 85% of serum cholesterol is endogenously (internally) derived, dietary modification alone will typically lower total cholesterol levels by only 10% to 30%. This, and the fact that adherence to dietary restrictions is often short lived, explains why many clients do not respond to diet modification alone.

Exercise is an important aspect of the nonpharmacologic method to reduce cholesterol. For the hypertensive older adult, exercise can be walking and bicycling. If the client is obese, body-weight reduction decreases cholesterol levels and he risk of CAD. Smoking is another risk factor that should be eliminated. Smoking increases LDL cholesterol and decreases the HDL.

If nonpharmacologic methods are ineffective for reducing cholesterol and the lipoproteins LDL, and VLDL, and hyperlipidemia remains, antilipidemic drugs are prescribed. It must be emphasized to the client that dietary changes need to be made and an exercise program followed even after drug therapy has been initiated.

Types of Antilipidemic

Drugs

Drugs that lower lipid levels include: BILE- ACID SEQUESTRANTS FIBRATES (FIBRIC ACID) NICOTINIC ACID HEPATIC 3-HYDROXY-3 THYGLUTARYL

COENZYME A (HMG-CoA) REDUCTASE INHIBITORS (STATINS).

BILE ACID SEQUESTRANTS

Cholestyramine resin ( Questran)

Colestipol HCl (Colestid)

Colesevelem (Welchol)

Cholestyramine resin (Questran)

One of the first antilipidemics introduced in 1959.

It is a resin that binds with bile acids in the intestine and is effective against hyperlipidemia type II. The drug comes in a gritty powder, which is mixed thoroughly in water or juice.

Route and dosage: (adult) PO, – 4 g t.i.d. before meals, and at bedtime; mix powder in 120- 240 ml of fluid; maximum: 24 g/day.

Uses and considerations:- for type II hyperlipoproteinemia

(LDL). Decrease in LDL is apparent in 1 wk. Drug powder should be mixed well in fluid. It does not have any effecton VLDL and HDL but could increase triglyceride levels. GI upset and constipation can occur. Vitamin A, D, K deficiency may occur because of decreased GI absorption.• Pregnancy category: c • Protein binding: unknown• Half – life: unknown

Side effects and adverse reactions- constipation and Peptic ulcer. Early

signs of peptic ulcer are nausea, and abdominal discomfort, followed later by abdominal pain and distention.

Constipation can be decreased or alleviated by increasing intake of fluid and foods high in fiber.

To avoid GI discomfort, the drug must be taken with and followed by sufficient fluids.

For self- administration- instruct client to mix the powder well

in water or juice.

COLESEVELEM (Welchol) Usually same with questrans. Route and dosage: (adult) PO, -3 tablets (625 mg/

tab) b.i.d. or 6 tabs, daily. Uses and contraindications:

it has a cholesterol- lowering effect by binding with bile acid salts in the intestines to form an insoluble complex with fecal excretions, thus reducing circulating cholesterol including LDL. Triglycerides might be slightly increased.

Contraindicated with bowel obstruction. May be used in combination with other statin

drugs. Pregnancy category: B

Colestipol HCl (Colestid)

Is a resin antilipidemic similar to cholestyramine. Both are effective in lowering cholesterol.

Bile- acid sequestrants should not be used as the only drug therapy in clients with elevated triglycerides because they typically raise triglyceride levels.

Route and dosage: (adult) PO, 10 – 30 g/ day in divided doses before meals.

Used to reduce cholesterol and LDL levels. Contraindications are same with cholestyramine.

Pregnancy category: C

Nursing management

Advice client that constipation may occur with cholestyramine and colestipol. Increasing fluid intake and foodbulk should help to alleviate the problem.

Fibrates (fibric acid)

Clofibrate (Atromid – S)Gemfibrozil (Lopid)

Clofibrate,Probucol and Gemfibrozil

Both are fibric derivatives that are effective in reducing triglycerides and VLDL levels. They are used primarily to reduce hyperlipidemia type IV but can also be used for type II hyperlipidemia.

These drugs are highly protein boundand should not be taken with anticoagulants because they compete for protein sites.

The anticoagulant dose should be reduced during antilipidemic therapy.

Clofibrate, once a popular antilipidemic, is not suggested for long- term use because of its many side effects such as cardiac dysrhythmias, angina, thromboembolism, and gallstones.

Probucol, a biphenol, is poorly absorbed after oral dosage. It lowers the LDL and cholesterol levels in type II hyperlipidemia, but it is not as effective as other antilipidemic drugs. It is highly lipid soluble and is stored in body fat; thus it is slow to eliminate from the body. Diarrhea may result from use. Probucol is contraindicated for clients with cardiac dysrhythmias.

Nursing Interventions Advise client taking clofibrate and probucol

that decreased libido and impotence may occur and should be reported. Drug dosage can be change or another antilipidemic may be ordered.

Instruct clients with diabetes or those at risk for developing diabetes to monitor blood glucose levels if they take gemfibrozil. Dietary changes or insulin adjustment may be necessary.

Advise client with cardiac dysrhythmias to tell the health care provider before starting probucol. Cardiac dysrhythmias should be monitored and reported.

Nicotinic acid (Niacin) Also known as vitamin B2, reduces

VLDL and LDL. Nicotinic acid is effect on the lipid profile is highly desirable. Because it has numerous side effects and large doses are required, as few as 20% of clients can tolerate niacin initially. However, with proper client counseling, careful drug titration, and concomitant use of aspirin, this number can be increased to as high as 60% to 70% .

Route and dosage: (adult)PO: initially: 100 mg t.i.d.; maintenance: 1-3

g/d after meals in 3 divided doses, max: 6 g/d. Uses and considerations: for VLDL and LDL:

types II, III, IV, V hyperlipidemia. Doses are 100 times higher than for RDA (recommended daily allowance) to lower VLDL.

Pregnancy category: C PB: uk; half-life: 45 mins Side effects: GI disturbances, flushing of the

skin, abnormal liver function ( elevated serum liver enzymes), hyperglycemia, hyperuricemia.

However, aspirin and careful drug titration can reduce side effects to a manageable level in most clients.

Nursing Interventions: Instruct client to take the drug with

meals to decrease GI discomfort.

HMG-CoA Reductase Inhibitors

Atorvastatin Calcium (Lipitor) Fluvastatin Sodium ( Lescol) Lovastatin (Mevacor) Pravastatin Sodium( Pravachol) Rosuvastatin Calcium ( Crestor) Simvastatin ( Zocor)

Statins

The statin drugs, first introduced in 1987, inhibit the enzyme HMG CoA reductase in cholesterol biosynthesis; thus the statins are called HMG CoA Reductase Inhibitors. By inhibiting cholesterol synthesis in the liver, this group of antilipidemics decreases the LDL and slightly increases the HDL cholesterol. Reduction of LDL cholesterol may be seen in as early as 2 wks. The statin group has been useful in decreasing CAD and reducing mortality rates.

Atorvastatin Calcium( Lipitor)

Uses: to decrease cholesterol levels and to decrease serum lipids especially LDL, and triglycerides.

Mode of Action: inhibits HMG-CoA reductase. HMG-CoA Reductase is necessary for hepatic production of cholesterol.

Dosage: adult: PO: 10 mg/daily, may increase dose up to 80 mg/ dailychildren: safety is not established

Contraindications Active Liver disease and pregnancyCaution: history of liver disease, increase

alcohol ingestion, trauma, severe metabolic endocrine disorders, uncontrolled seizures.

Side effects include headache, rash/ pruritus, constipation/ diarrhea, sinusitis, pharyngitis (RARE).

Adverse reactions: rhabdomyolysis, myalgia, photosensitivity, cataracts.

PharmacokineticsAbsorption: rapidDistribution: protein binding: 98%Metabolism: half life: 14 h, metabolites:20-

30 hExcretion: primarily in the bile; some via

urine

PharmacodynamicsPO: Onset: 2 wks for decrease in cholesterol

peak: 1-2 hrs; 2-4 wks to be effectiveduration: 24 hrs

Fluvastatin Sodium (Lescol)

Uses and considerations: treatments of types IIA and IIB hyperlipidemia, total cholesterol, and elevated triglycerides. HDL is slightly increased. Monitor liver function (liver enzymes).

Pregnancy category: X; half life: 1.2 h; PB: 98%

Route and dosage: A: PO: initially: 20-40 mg at bedtime; maintenance: 20-80mg/d.

Lovastatin ( Mevacor) Was the first statin used to decrase

cholesterol. It is effective in lowering LDL (type II) with in several weeks.

GI disturbances, headaches, muscle cramps,and tiredness are early complaints.

Serum liver enzymes should be monitored, and an annual eye examination is needed because cataract formation may result from lovastatin therapy.

Simvastatin (zocor)

Route and dosage: ADULT:PO: initially: 5-10 mg/d in evening; maintenance: 20-80 mg/d in evening; max: 80 mg/d

Uses and considerationsmonitor liver enzymes.

Pregnancy category: X PB: 95% Half life: unknown

Nursing interventions Explain to client that the serum liver

enzyme levels are periodically monitored. Encourage client to report promptly any

unexplained muscle tenderness or weakness that may be caused by rhabdomyolysis.

Instruct client not to abruptly stop the statin drug because a seriuos rebound effect mightt occur and that could lead to an AMI and possible death. Before stopping a statin, client should talk to his or her health care provider.

Antihyperlipidemiaezetimibe (Zetia)

Route and dosage: adult:PO: 10 mg daily

Uses and considerations: it inhibits cholesterol absorption in the small intestine. Also, it reduces the total cholesterol, LDL, triglycerides, and increases HDL. Caution use should be with liver dysfunction and serum transaminase levels.

Pregnancy category: C

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