What is lovastatin, and how does it work (mechanism of action)?
Lovastatin belongs to a class of
cholesterol-lowering drugs called HMG-CoA reductase inhibitors, or, more
commonly "statins." Other statins include simvastatin (Zocor), atorvastatin
(Lipitor), fluvastatin (Lescol), and rosuvastatin (Crestor). Statins reduce
cholesterol by inhibiting an enzyme in the liver (HMG-CoA reductase) that is
necessary for the production of cholesterol. In the blood, statins lower
total
cholesterol, low density lipoprotein (LDL) cholesterol ("bad" cholesterol) and
triglycerides. LDL cholesterol is believed to be an important cause of
atherosclerosis and coronary artery disease (cardiovascular disease). Lowering
LDL cholesterol levels slows and may even reverse coronary artery disease.
Statins also increase high density lipoprotein (HDL) cholesterol ("good"
cholesterol). Raising HDL cholesterol levels, like lowering LDL cholesterol, may
slow coronary artery disease. The FDA approved lovastatin in August 1987.
What brand names are available for lovastatin?
Mevacor, Altoprev
Is lovastatin available as a generic drug?
Yes
Do I need a prescription for lovastatin?
Yes
What are the side effects of lovastatin?
The most common side effects of lovastatin are:
Hypersensitivity reactions also have been reported.
The most serious
potential side effects are liver damage and muscle inflammation or breakdown. Lovastatin shares side effects, such as liver and muscle damage associated with
all statins. Serious liver damage caused by statins is rare. More often, statins
cause abnormalities of liver tests. Abnormal tests usually return to normal even
if a statin is continued, but if the abnormal test value is greater than three
times the upper limit of normal, the statin usually is stopped. Liver function
tests should be performed at the beginning of treatment and then as needed
thereafter. Inflammation of the muscles caused by statins can lead to a serious
breakdown of muscle cells called rhabdomyolysis. Rhabdomyolysis causes the
release of muscle protein (myoglobin) into the blood. Myoglobin can cause
kidney
failure and even death. When used alone, statins cause rhabdomyolysis in less
than 1% of patients. To prevent the development of rhabdomyolysis,
patients taking lovastatin should contact their healthcare provider immediately
if they develop unexplained muscle pain, weakness, or muscle tenderness.
Statins
have been associated with increases in
HbA1c and fasting serum glucose levels as
are seen in diabetes. There are also post-marketing reports of memory loss,
forgetfulness, amnesia, confusion, and memory impairment. Symptoms may start
one
day to years after starting treatment and resolve within a median of three weeks
after stopping the statin.
What is the dosage for lovastatin?
The dose range for lovastatin is 10-80 mg daily given
preferably in the evening when it may be most effective. The usual starting dose
is 20 mg once daily, and the maximum dose is 80 mg daily. Blood cholesterol
determinations are performed at regular intervals during treatment so that
adjustments in dosage can be made.
Which drugs or supplements interact with lovastatin?
Decreased elimination of lovastatin could increase
the levels of lovastatin in the body and increase the risk of muscle toxicity
from lovastatin. Examples of drugs that decrease elimination of lovastatin
include erythromycin (E-Mycin), ketoconazole (Nizoral), itraconazole (Sporanox),
clarithromycin (Biaxin), telithromycin (Ketek), cyclosporine (Sandimmune),
nefazodone (Serzone), boceprevir (Victrelis), telaprevir (incivek), voriconazole
(Vfend), and protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir).
They should not be combined with lovastatin.
Large quantities of grape fruit
juice (>1 quart daily) also will increase blood levels of lovastatin and should
be avoided.
Amiodarone (Cordarone), verapamil (Calan, Verelan, Isoptin),
diltiazem (Cardizem), danazol (Danocrine), niacin (Niacor, Niaspan, Slo-Niacin),
colchicine, ranolazine (Ranexa), gemfibrozil (Lopid), and fenofibrate (Tricor)
also may increase the risk of muscle toxicity when combined with lovastatin.
Cyclosporine or gemfibrozil should not be combined with lovastatin. Patients
taking amiodarone (Cordarone) should not exceed 40 mg daily of lovastatin.
Patients taking verapamil, diltiazem, or danazol should start with 10 mg and
should not exceed 20 mg of lovastatin daily. Patients taking niacin (greater
than or equal to 1 g/day), fenofibrate (Tricor) or cyclosporine (Gengraf, Neoral)
should not take more than 20 mg of lovastatin.
Lovastatin may increase the
effect of warfarin (Coumadin), a blood thinner. Patients taking lovastatin and
warfarin (Coumadin) should be monitored carefully for toxic effects of warfarin.
Is lovastatin safe to take if I’m pregnant or breastfeeding?
Pregnant women should not use lovastatin because the
developing fetus requires cholesterol for development, and lovastatin reduces
the production of cholesterol. Lovastatin should only be administered to women
of child bearing age if they are not likely to become pregnant.
Because of the risk of adverse effects to the
developing infant, lovastatin should not be administered to
nursing mothers.
What else should I know about lovastatin?
What preparations of lovastatin are available?
Tablets: 10, 20 and 40 mg. Extended release tablets: 10,
20, 40, and 60 mg.
How should I keep lovastatin stored?
Immediate release tablets should be stored between 5 C – 30 C
(41 F – 86 F). Extended release tablets should be stored at room temperature, 20 C – 25
C (68 F – 77 F).