Dosing & Uses
Dosage Forms & Strengths
Mevacor (immediate-release): 20 mg PO qDay with evening meal initially, or may divide daily dose BID; adjust dose at 4-week intervals if increase required; not to exceed 80 mg/day
Altoprev (extended-release): 10-60 mg PO qHS
Coadministration with danazol, diltiazem, or verapamil: Do not exceed 20 mg lovastatin daily
Coadministration with amiodarone: Do not exceed 40 mg lovastatin daily
Avoid large quantities of grapefruit juice (>1 qt/day)
- Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFTs, eye lens opacities
- Treatment is supportive
Renal impairment (severe; CrCl <30 mL/min): Doses >20 mg/day should be carefully considered and, if deemed necessary, implemented cautiously
Dosage Forms & Strengths
Heterozygous Familial Hypercholesterolemia
10-17 years: 20-40 mg PO qDay; not to exceed 40 mg/day
Initiate with 10 mg/day if patient requires smaller LDL-C reduction
Serious - Use Alternative
Significant - Monitor Closely
CPK elevation (11%)
Abdominal pain (2-3%)
Blurred vision (0.8-1%)
Muscle cramps (0.6-1%)
Hypersensitivity to lovastatin or other components
Active liver disease, or unexplained elevated transaminases
Concomitant administration with strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, cobicistat, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, and nefazodone)
Nonserious and reversible cognitive side effects may occur
Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake
Rhabdomyolysis, risk of myopathy: Risk increased by coadministration CYP3A4 inhibitors or other drugs that cause myopathy
Avoid coadministration with cyclosporine or gemfibrozil; caution with other fibrates or lipid-lowering doses of niacin (≥1 g/day) because of increased risk for myopathy
Heavy alcohol use, history of liver disease, renal failure
Discontinue if markedly elevated CPK levels occur or myopathy is diagnosed or suspected; also, temporarily withhold in any patient experiencing an acute or serious condition predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis; hypotension; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled epilepsy)
Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persists despite discontinuation of statin
Obtain baseline liver enzyme tests before initiating and then periodically thereafter
Brand Altocor renamed Altoprev due to confusion with Advicor
Pregnancy & Lactation
Pregnancy category: X
Lactation: Contraindicated; unsafe
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
HMG-CoA reductase inhibitor; inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
Bioavailability: 5% (Mevacor)
Onset: 3 d (Mevacor)
Duration: 4-6 wk (Mevacor)
Max effect: 4-6 wk (Mevacor)
Peak plasma time: 2-4 hr; 14 hr (ext-rel Altoprev)
Peak plasma concentration: 7.8 ng/mL; 5.5 ng/mL (ext-rel Altoprev)
AUC: 45 ng.hr/mL; 77 ng.hr/mL (ext-rel Altoprev)
Protein bound: 95% (Mevacor)
Extensive first pass in liver; activation to beta-hydroxyacid by nonenzymatic/nonspecific hydrolysis; major CYP3A4 substrate
Metabolite: Beta-hydroxyacid derivative (active) and others
Half-life: 1.1-1.7 hr (Mevacor)
Excretion (Mevacor): Feces (83%), urine (10% urine)
SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes
This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations
SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)
Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism
SLCO1B1 CC genotype is most common in Caucasians and Asians (15%)
Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and is 16.9-fold higher in CC homozygotes compared with TT homozygotes
Genetic testing laboratories
- Optivia Biotechnology, Inc (http://optiviabio.com)
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