Drugs: lovastatin

lovastatin
((mevinolin))
loe-va-STA-tin

Altoprev

Therapeutic class: Antilipemics

Pharmacologic class: HMG-CoA reductase inhibitors

Available Forms
Tablets: 10 mg; 20 mg; 40 mg
Tablets (extended-release) : 20 mg; 40 mg; 60 mg

Indications & Dosages

Adjust-a-dose (for all indications): Avoid use of lovastatin with fibrates or niacin at doses greater than 1
g daily. For patients also taking danazol, diltiazem, dronedarone, or verapamil, start lovastatin at 10 mg
(immediate-release) and don’t exceed 20 mg daily. For patients also taking amiodarone, lovastatin dosage
shouldn’t exceed 40 mg daily unless clinical benefit is likely to outweigh increased risk of myopathy or
rhabdomyolysis. For elderly patients or patients with CrCl of less than 30 mL/minute, carefully consider
dosage increase greater than 20 mg daily and implement cautiously if necessary. For patients requiring
smaller reductions in cholesterol levels, use immediate-release lovastatin.
To prevent and treat CAD; hyperlipidemia
Adults: Initially, 20 mg (immediate-release) PO once daily with evening meal. Recommended range is 10 to
80 mg as a single dose or in two divided doses; maximum daily recommended dose is 80 mg. Or, 20 to 60
mg extended-release tablets PO at bedtime.
Make dosage adjustments at intervals of 4 weeks or more.
Heterozygous familial hypercholesterolemia in adolescents
Adolescents ages 10 to 17: Give 10 to 40 mg (immediate-release) PO daily with evening meal. Patients
requiring reductions in LDL cholesterol level of 20% or more should start with 20 mg daily. Make dosage
adjustments at intervals of 4 weeks or more.
Primary prevention of CV disease
Adults ages 40 to 75 with type 1 or type 2 diabetes (moderate-intensity therapy): 40 mg (immediate-
release) PO once daily.
Adults ages 40 to 75 with an estimated 10-year atherosclerotic CV disease risk of 7.5% or more (moderate-
to high-intensity therapy): 40 mg (immediate-release) PO once daily.
Secondary prevention of CV disease (moderate-intensity therapy)
Adults older than age 75 or who aren’t candidates for high-intensity therapy: 40 mg (immediate-release)
PO once daily.

Administration
PO
Give immediate-release drug with evening meal, which improves absorption and cholesterol biosynthesis.
Give extended-release drug at bedtime.
Don’t crush, split, or allow patient to chew extended-release tablets.

Action
Inhibits HMG-CoA reductase, an early (and rate-limiting) step in cholesterol biosynthesis.

Route Onset Peak Duration

PO Unknown 2–4 hr Unknown
PO (extended-release) 3 days 12–14 hr Unknown
Half-life: 1.1 to 1.7 hours.

Adverse Reactions
CNS: headache, dizziness, insomnia, peripheral neuropathy.
EENT: blurred vision.
GI: abdominal pain or cramps, constipation, diarrhea, dyspepsia, flatulence, heartburn, nausea, vomiting.
GU: UTI.
Musculoskeletal: muscle cramps, myalgia, myositis, rhabdomyolysis.
Skin: alopecia, rash, pruritus.
Other: flulike syndrome, pain, infection.

Interactions
Drug-drug
Amiodarone: May decrease the metabolism of lovastatin. Avoid combining lovastatin at doses exceeding 40
mg daily with amiodarone unless clinical benefit is likely to outweigh increased risk of myopathy.
Azole antifungals: May cause myopathy and rhabdomyolysis. Avoid using together.
Colchicine: May increase risk of myopathy or rhabdomyolysis. If coadministration can’t be avoided, monitor
patient for unexplained muscle pain, tenderness, or weakness.
Cyclosporine, gemfibrozil: May cause severe myopathy and rhabdomyolysis. Avoid this combination.
Danazol, diltiazem, dronedarone, verapamil: May cause myopathy and rhabdomyolysis. Don’t exceed 20
mg lovastatin daily.
Dronedarone: May increase lovastatin serum concentration. Limit lovastatin to maximum of 20 mg/day (in
adults). Increase monitoring for signs and symptoms of lovastatin toxicity (such as myopathy and
rhabdomyolysis). Consider therapy modification.
Erythromycin, protease inhibitors (atazanavir, darunavir, fosamprenavir, indinavir, nefazodone, nelfinavir,
ritonavir, saquinavir, tipranavir), strong CYP3A inhibitors (clarithromycin, itraconazole, ketoconazole,
posaconazole, telithromycin, voriconazole): Increase risk of myopathy and rhabdomyolysis. Use together is
contraindicated.
Macrolides (azithromycin, clarithromycin, telithromycin), nefazodone: May decrease metabolism of HMG-
CoA reductase inhibitor, increasing toxicity. Monitor patient for adverse effects and report unexplained
muscle pain.
Mifepristone (CYP3A4 inhibitor): May increase lovastatin plasma level, increasing risk of toxicity. Use
together is contraindicated.
Niacin, other fibrates: May increase the risk for adverse and toxic effects of lovastatin. Avoid use of
lovastatin with fibrates or niacin at doses greater than 1 g daily.
Oral anticoagulants: May increase anticoagulant effect. Monitor patient closely.
Phenytoin: May decrease serum concentration of HMG-CoA reductase inhibitors. Consider therapy
modification.
Ranolazine: May increase risk of myopathy and rhabdomyolysis. Consider lovastatin dosage adjustment.
Drug-herb
Eucalyptus, kava: May increase risk of hepatotoxicity. Discourage use together.
Red yeast rice: May increase risk of adverse reactions because herb contains compounds similar to those in
drug. Discourage use together.
Drug-food
Grapefruit juice: May increase drug level, increasing risk of adverse effects. Discourage use together.
Drug-lifestyle
 Alcohol use: May increase risk of hepatotoxicity. Discourage use together.

Effects on Lab Test Results

May increase ALT, AST, and CK levels.
May cause thyroid function test abnormalities.

Contraindications & Cautions

Contraindicated in patients hypersensitive to drug and in those with active liver disease or unexplained
persistently increased transaminase level.
Use cautiously in patients who consume substantial quantities of alcohol or have a history of liver
disease.
Dialyzable drug: Unknown.

Pregnancy-Lactation-Reproduction
Drug may cause fetal harm and is contraindicated in women who are pregnant or may become
pregnant. Use in women of childbearing potential only when such patients are highly unlikely to
conceive. If patient becomes pregnant during therapy, discontinue drug and apprise her of potential
hazard to the fetus.
It isn’t known if drug appears in human milk. Use in breastfeeding women is contraindicated.

Nursing Considerations
Have patient follow a diet restricted in saturated fat and cholesterol during therapy.
Obtain LFT results at the start of therapy; then monitor results periodically.
Heterozygous familial hypercholesterolemia can be diagnosed in adolescent boys and in girls who are at
least 1 year postmenarche and are 10 to 17 years old; if after an adequate trial of diet therapy LDL
cholesterol level remains over 189 mg/dL or LDL cholesterol over 160 mg/dL and patient has a positive
family history of premature CV disease or two or more other CV disease risk factors.
Obtain CK level in patients with unexplained muscle pain.
Discontinue lovastatin immediately if markedly elevated CK levels occur or myopathy is diagnosed or
suspected. Predisposing factors for skeletal muscle effects include advanced age (65 and older), female
gender, uncontrolled hypothyroidism, and renal impairment.
Look alike-sound alike: Don’t confuse lovastatin with Lotensin.

Patient Teaching
Instruct patient to take immediate-release drug with the evening meal and extended-release drug at
bedtime.
Alert: Advise patient not to crush or chew extended-release tablets.
Teach patient about proper dietary management of cholesterol and triglycerides. When appropriate,
recommend weight control, exercise, and smoking cessation programs.
Instruct patient to store tablets at room temperature in a light-resistant container.
Advise patient of risk of myopathy and rhabdomyolysis and to promptly report unexplained muscle pain,
tenderness, or weakness, particularly when accompanied by malaise or fever.
Teach patient about substances that shouldn’t be taken with lovastatin and to inform other health care
providers about taking lovastatin, especially if a new medication is being prescribed.
Caution patient to avoid grapefruit juice while taking drug.
Alert: Tell female patient to stop drug and notify prescriber immediately if she is or may be pregnant or
if she’s breastfeeding.