Generic Name and Formulations:
Niacin 500mg, 750mg, 1g; ext-rel tabs.
Adjunct to diet in primary hyperlipidemia and mixed dyslipidemia to reduce elevated total-C, LDL-C, apo B, TG and to increase HDL-C; or combined with lovastatin or simvastatin when further reductions in TG or LDL-C or increases in HDL-C are needed, and monotherapy is inadequate. To reduce risk of recurrent nonfatal MI in patients with a history of MI and hyperlipidemia. Combined with a bile acid sequestrant to slow progression or promote regression of atherosclerosis in patients with coronary artery disease and hyperlipidemia. Combined with a bile acid sequestrant to reduce elevated total-C and LDL-C in primary hyperlipidemia when diet or diet + monotherapy has been inadequate. Adjunct in patients with severe hypertriglyceridemia who are at risk for pancreatitis, when determined dietary measures are inadequate. Limitations of use: no incremental benefit on cardiovascular morbidity/mortality over and above that demonstrated for niacin, simvastatin and lovastatin monotherapy, has been established. Niacin ext-rel at doses of 1500–2000mg/day, in combination with simvastatin, did not reduce incidence of cardiovascular events more than simvastatin in a randomized controlled trial of patients with cardiovascular disease and mean baseline LDL-C levels of 74mg/dL.
Swallow whole. Take at bedtime with low-fat snack. Avoid concomitant alcohol, hot beverages, or spicy foods; may pre-treat with aspirin (up to 325mg) ½ hour before dosing. >16yrs: initially 500mg once daily for 4 weeks, then 1g once daily for weeks 5–8. May increase by up to 500mg every 4 weeks to usual range of 1–2g daily; max 2g/day. Combined with lovastatin or simvastatin: max 2g niacin and 40mg lovastatin or simvastatin per day. Retitrate if restarting after an extended time. Women may respond at lower doses than men.
≤16yrs: not recommended.
Nicotinic acid deriv.
Active liver disease. Unexplained elevations of serum transaminases. Active peptic ulcer disease. Arterial bleeding.
Do not substitute for equivalent doses of immediate-release or sustained-release niacin (hepatotoxicity may occur). History of jaundice, hepatobiliary disease, peptic ulcer. Substantial alcohol consumption. Monitor serum transaminase levels (before treatment then every 6–12 weeks for 1 year then periodically); discontinue if transaminase levels ≥3xULN persist or if signs of liver disease occur. Renal dysfunction. Cardiovascular disease (eg, unstable angina, acute MI). Gout. Monitor blood glucose and for hypophosphatemia. Surgery. Diabetes or patients at risk for diabetes. Uncontrolled hypothyroidism. Elderly. Pregnancy (Cat.C), nursing mothers: not recommended (consider discontinuing drug).
Avoid other products with high amounts of niacin or nicotinamide, alcohol. Monitor for myopathy/rhabdomyolysis with HMG-CoA reductase inhibitors. May potentiate antihypertensives, other vasoactive drugs (eg, ganglionic or adrenergic blockers, nitrates, calcium channel blockers). Caution with anticoagulants (monitor PT and platelet counts). Antidiabetic agents may need adjustment. Separate dosing of bile acid sequestrants by at least 4–6 hours. May cause false (+) Benedict's test.
Flushing, diarrhea, nausea, vomiting, cough, pruritus, dizziness, tachycardia, palpitations, shortness of breath, sweating, chills, edema, pain, rhinitis, rash, glucose intolerance, peptic ulcer, abnormal liver function tests, jaundice.