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lovastatin/niacin (Discontinued)Brand and Other Names:Advicor

 
 
 

Dosing & Uses

AdultPediatric

Hypercholesterolemia & Mixed Dyslipidemia

December 31, 2015: Manufacturer voluntarily withdrew drug from the market and discontinued distribution

April 15, 2016: Based on several large cardiovascular outcome trials including AIM-HIGH, ACCORD, and HPS2-THRIVE, the FDA decided that "scientific evidence no longer supports the conclusion that a drug-induced reduction in triglyceride levels and/or increase in HDL-cholesterol levels in statin-treated patients results in a reduction in the risk of cardiovascular events"

Consistent with this conclusion, the FDA has determined that the benefits of niacin ER tablets for coadministration with statins no longer outweigh the risks, and the approval for this indication should be withdrawn

Not recommended

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Interactions

Interaction Checker

lovastatin/niacin and

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            Frequency Not Defined

            CPK elevation

            Muscle cramp

            Myalgia

            Myopathy

            Rhabdomyolysis

            Increased LFTs

            Hepatotoxicity

            Hyperglycemia

            Abdominal pain

            Constipation

            Diarrhea

            Flatulence

            GI upset

            Nausea/vomiting

            Dizziness

            Headache

            Weakness

            Facial flushing

            Pruritus

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            Warnings

            Contraindications

            Hypersensitivity to lovastatin or niacin

            Active liver disease, or unexplained elevated transminases, active PUD, arterial bleeding

            Concomitant administration of lovastatin with strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, cobicistat, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin and nefazodone)

            Pregnancy, lactation

            Cautions

            Avoid concomitant use with anticoagulants, or dilators, grapefruit juice (>1 quart/day)

            Heavy alcohol use, history of liver disease , renal failure, DM, gout, unstable angina

            Withhold or discontinue if myopathy develops, renal failure, or transaminase levels >3x ULN

            Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persist despite discontinuing statin

            Rhabdomyolysis risk and myopathy increased by coadministration of lovastatin with CYP3A4 inhibitors or other drugs (eg, fibrates, high-dose niacin, cyclosporine) that cause myopathy (see Contraindications)

            Avoid coadministration of lovastatin with cyclosporine or gemfibrozil; caution with other fibrates or lipid-lowering doses of niacin (≥1 g/day) because of increased risk for myopathy

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            Pregnancy & Lactation

            Pregnancy Category: X

            Lactation: Contraindicated

            Pregnancy Categories

            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.

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            Pharmacology

            Mechanism of Action

            Lovastatin: HMG-CoA reductase inhibitor, inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase

            Niacin: Component of 2 coenzymes necessary for tissue respiration, glycogenolysis, and lipid metabolism; inhibits synthesis of low density lipoproteins

            Pharmacokinetics

            Lovastatin

            • Onset: 3 days (reduction of LDL cholesterol); maximum response 4-6 weeks
            • Bioavailability: >30% with extended release formulation when taken in fasting state
            • Protein binding: >95%
            • Metabolism: Extensive hepatic metabolism; hydrolyzed to β-hydroxyacid (active metabolism)
            • Half-life: 1.1-1.7 hr
            • Peak plasma time: 2-4 hr (immediate release); 12-14 hr (extended release)
            • Excretion: Urine (10%); feces (80-85%)

            Niacin

            • Bioavailability: 60-76% (absorption rapid, extensive)
            • Half-life: 20-45 min
            • Peak plasma time: 30-60 min (immediate release); 4-5 hr (extended release formulation)
            • Excretion: Urine (60-88%)
            • Protein binding: 20%
            • Distribution: Hepatic, renal and adipose tissue distribution
            • Metabolism: First pass effect; conversted to nicotinamide adenine dinucleotide (NAD-active metabolite), [nicotinamide, nicotinuric acid] (inactive)

            Pharmacogenomics

            SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of simvastatin 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 more 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 16.9-fold higher in CC homozygotes compared with TT homozygotes

            Genetic testing laboratories

            • Optivia Biotechnology, Inc (http://optiviabio.com/index.html)
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            Administration

            Instructions

            Take with cold liquid

            Take with food (low fat snack); do not take on empty stomach

            Monitor LFT 6 weeks after initiation or dose escalation

            Pretreatment with nonenteric coated aspirin may reduce flushing

            If therapy interrupted >7 days reinstitution of therapy may begin by intitiating therapy at lowest dose and slow titration as needed

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