LOVASTATIN

LOVASTATIN
(loe-vah-stat'in)
Altoprev, Mevacor
Classifications: antilipemic; lipid-lowering agent; hmg-coa reductase inhibitor (statin);
Therapeutic: lipid-lowering agent
; statin
Pregnancy Category: X

Availability

10 mg, 20 mg, 40 mg tablets; 10 mg, 20 mg, 40 mg, 60 mg extended release tablets

Action

Reduces plasma cholesterol levels by interfering with body's ability to produce its own cholesterol. This cholesterol-lowering effect triggers induction of LDL receptors, which promote removal of LDL and VLDL remnants (precursors of LDL) from plasma. Also results in an increase in plasma HDL concentrations (HDL collects excess cholesterol from body cells and transports it to liver for excretion).

Therapeutic Effect

Reduces plasma cholesterol levels by interfering with body's ability to produce its own cholesterol, and it also lowers LDL and VLDL cholesterol.

Uses

Adjunct to diet for treatment of primary moderate hypercholesterolemia (types IIa and IIb) when diet and other nonpharmacologic measures have failed to reduce elevated total LDL cholesterol levels. Lovastatin is less effective in treatment of homozygous familial hypercholesterolemia than primary hypercholesterolemia, possibly because in these persons LDL receptors are not functional.

Contraindications

Active liver disease, unexplained elevations of serum transaminases; cholestasis, hepatic encephalopathy, hepatic disease, hepatitis, jaundice; rhabdomyolysis; surgery, trauma; hypotension, renal failure; pregnancy (category X), lactation, children <10 y.

Cautious Use

Patient who consumes substantial quantities of alcohol; history of liver disease; electrolyte imbalance, endocrine disease, females of childbearing age, infection, myopathy, renal disease, renal impairment, seizure disorder. Patient with risk factor predisposing to development of kidney failure secondary to rhabdomyolysis.

Route & Dosage

Hypercholesterolemia
Adult: PO 20–40 mg 1–2 times/d

Administration

Oral
  • Give with the evening meal if q.d. Give the first of 2 daily doses with breakfast.
  • Store tablets at 5°–30° C (41°–86° F) in light-resistant, tightly closed container.
  • Ensure that extended release tablets are not crushed or chewed. They must be swallowed whole.

Adverse Effects (≥1%)

Body as a Whole: Generally well tolerated. CNS: Dizziness, mild transient headache, insomnia, fatigue. Special Senses: Blurred vision. GI: Dyspepsia, dysgeusia, heartburn, nausea, constipation, diarrhea, flatus, abdominal pain, and cramps. Metabolic: Increases in serum transaminases, elevated creatine phosphokinase (CPK). Skin: Rash, pruritus.

Interactions

Drug: Clarithromycin, clofibrate, cyclosporine, danazol, erythromycin, fenofibrate, fluconazole, gemfibrozil, itraconazole, ketoconazole, miconazole, niacin, and protease inhibitors increase risk of myopathy and rhabdomyolysis; potentiate hypoprothrombinemia with warfarin. Food: Grapefruit juice (>1 qt/d) may increase risk of myopathy and rhabdomyolysis.

Pharmacokinetics

Absorption: 30% from GI tract; extensive first-pass metabolism. Onset: 2 wk. Peak: 4–6 wk. Distribution: Crosses blood–brain barrier and placenta; distributed into breast milk. Metabolism: In liver to active metabolites. Elimination: 83% in feces; 10% in urine. Half-Life: 1.1–1.7 h.

Nursing Implications

Assessment & Drug Effects

  • Lab tests: Perform liver function tests q4–6wk during first 15 mo of therapy. Monitor blood cholesterol levels and lipid profile periodically.
  • Drug-induced increases in serum transaminases, usually not associated with jaundice or other clinical S&S, return to normal when drug is discontinued. If these values rise and remain at 3 times upper level of normal, drug will be discontinued and liver biopsy considered.

Patient & Family Education

  • Do not interrupt, increase, decrease, or omit dosage without advice of physician.
  • Notify physician promptly of muscle tenderness or pain, especially if accompanied by fever or malaise. If CPK is elevated or if myositis is diagnosed, drug will be discontinued.
  • Avoid or at least reduce alcohol consumption.
  • Understand that lovastatin is not a substitute for, but an addition to, diet therapy.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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