Trade Names:Advicor- Tablets 500/20 mg- Tablets 750/20 mg- Tablets 1,000/20 mg- Tablets 1,000/40 mg
Necessary for lipid metabolism, tissue respiration, and glycogenolysis; reduces total cholesterol, LDL cholesterol, and triglycerides (TG) while increasing HDL cholesterol.Lovastatin
Increases rate at which body removes cholesterol from blood and reduces production of cholesterol in body by inhibiting enzyme that catalyses early rate-limiting step in cholesterol synthesis; increases HDL; reduces LDL, VLDL, and TG.
C max of niacin averaged about 18 mcg/mL about 5 h after dosing; lovastatin C max averaged about 11 ng/mL about 2 h after dosing. The extent of niacin and lovastatin absorption was increased by administration with food.
Niacin is less than 20% bound to human serum proteins and distributes into milk. Niacin and its metabolites concentrate in the liver, kidney, and adipose tissue. Both lovastatin and its beta-hydroxyacid metabolite are highly bound (more than 95%) to human plasma proteins. Lovastatin is concentrated in the liver and crosses the blood-brain and placental barriers.
Niacin undergoes rapid and extensive first-pass metabolism forming nicotinuric acid and nicotinamide. Lovastatin undergoes extensive first-pass extraction and metabolism by CYP-450 3A4 in the liver. The major active metabolites are the beta-hydroxyacid of lovastatin (lovastatin acid), its 6'-hydroxy derivative.
Niacin is primarily excreted in urine mainly as metabolites. The plasma t ½ was about 4.5 hours for lovastatin and about 20 to 48 minutes for niacin.
Treatment of primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Frederickson Types IIa and IIb) in patients treated with lovastatin who require further TG-lowering or HDL-raising who may benefit from having niacin added to their regimen; patients treated with niacin who require further LDL-lowering who may benefit from having lovastatin added to their regimen.
Pregnancy, lactation, active liver disease, unexplained persistent elevations in serum transaminases, active peptic ulcer disease, arterial bleeding, hypersensitivity to any component of product.
PO Patients receiving a stable dose of Niaspan (niacin extended-release tablets) may be switched directly to a niacin-equivalent dose of Advicor . Patients receiving a stable dose of lovastatin may receive concomitant dosage titration with Niaspan and switch to Advicor once a stable dose of Niaspan has been reached. Advicor should be taken at bedtime.
Store tablets at controlled room temperature (68° to 77°F).
Niacin may potentiate effects resulting in postural hypotension.Aspirin
Metabolic Cl of niacin may be decreased.Bile acid sequestrants
Because of possible binding of niacin to these agents, allow 4 to 6 h (or as long an interval as possible) to elapse between the ingestion of bile acid-binding resins and administration of Advicor .Clarithromycin, cyclosporine, erythromycin, gemfibrozil, HIV protease inhibitors (eg, ritonavir), itraconazole, ketoconazole, nefazodone, niacin
May increase the risk of skeletal muscle disorders (eg, rhabdomyolysis).Coumarin anticoagulants (eg, warfarin)
Bleeding and increased PT may occur. Monitor anticoagulant parameters when starting, stopping, or changing the Advicor dose.Hot beverages or alcohol
May increase the adverse reactions of flushing and pruritus with niacin and should be avoided.
Niacin may produce false elevations in some fluorometric determinations of plasma or urinary catecholamines; niacin may give false-positive reactions with cupric sulfate solution ( Benedicts reagent) in urine glucose tests.
The incidence stated for the following adverse reactions were reported with Advicor (niacin/lovastatin) administration. Adverse reactions occurring with administration of either niacin or lovastatin listed in their respective monographs.
Headache (9%); asthenia (5%).
Flushing (71%); pruritus (7%); rash (5%).
Nausea (7%); diarrhea (6%); abdominal pain (4%); dyspepsia, vomiting (3%).
Back pain (5%); myalgia (3%).
Infection (20%); pain (8%); flu syndrome (6%).
Monitor blood sugar in diabetic patient when drug is started or dose is changed. Assess fasting blood glucose before starting therapy and periodically thereafter during therapy in patient with risk factors for diabetes mellitus (eg, obesity, family history of diabetes). Assess serum transaminases before starting therapy, every 6 to 12 wk for the first 6 mo of therapy, and periodically (eg, every 6 mo) thereafter as clinically indicated.
Category X .
Excreted in breast milk.Lovastatin
Safety and efficacy not established.
Use with caution in patients with unstable angina or in the acute phase of MI, or in patients predisposed to gout; use with caution in patients with a history of jaundice or hepatobiliary disease; administer with caution in patients with peptic ulcers and in patients who consume substantial quantities of alcohol and/or who have a history of liver disease.
Equivalent doses of Advicor may be substituted for equivalent doses of Niaspan but should not be substituted for other modified-release niacin preparations or immediate-release niacin preparations.
A dose related rise may be experienced in diabetic patients.
Severe hepatic toxicity, including fulminant hepatic necrosis, has occurred in patients substituting sustained-release niacin for immediate-release niacin in equivalent doses.
Have been reported when lovastatin is used in combination with lipid altering doses (at least 1 g/day) of niacin.
Because lovastatin may increase creatine phosphokinase and transaminase levels, this should be considered in differential diagnosis of chest pain.
Severe flushing, nausea, vomiting, diarrhea, dyspepsia, dizziness, syncope, hypotension, possible cardiac arrhythmias, clinical laboratory abnormalities.
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