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Uses

Prevention of Cardiovascular Events

Adjunct to dietary therapy in patients with a history of MI and hypercholesterolemia to reduce the risk of recurrent nonfatal MI.

Adjunct to bile acid sequestrant therapy in patients with CHD and hypercholesterolemia to slow progression or promote regression of atherosclerosis.

Dyslipidemias

Adjunct to dietary therapy to decrease elevated serum total cholesterol, LDL-cholesterol, apolipoprotein B (apo B), and triglyceride concentrations, and to increase HDL-cholesterol concentrations in the management of primary hypercholesterolemia and mixed dyslipidemia, including heterozygous familial hypercholesterolemia and other causes of hypercholesterolemia (e.g., polygenic hypercholesterolemia). Fixed combination of extended-release niacin and lovastatin (Advicor^®) should not be used as initial antilipemic therapy.

Adjunctive therapy in the management of severe hypertriglyceridemia in patients at risk of developing pancreatitis (typically those with serum triglyceride concentrations >2000 mg/dL and elevated concentrations of VLDL-cholesterol and fasting chylomicrons) who do not respond adequately to dietary management.

Also may be used in patients with triglyceride concentrations of 1000–2000 mg/dL who have a history of pancreatitis or of recurrent abdominal pain typical of pancreatitis.

Efficacy in patients with type IV hyperlipoproteinemia and triglyceride concentrations <1000 mg/dL who exhibit type V patterns subsequent to dietary or alcoholic indiscretion not adequately studied.

Not indicated for use in patients with type I hyperlipoproteinemia who have elevated triglyceride and chylomicron concentrations but normal VLDL-cholesterol concentrations.

Dietary Requirements

Adequate intake of niacin needed to prevent niacin deficiency and pellagra.

In the US, niacin is principally obtained from fish, meat, or poultry, and niacin-enriched or niacin-fortified food (e.g., enriched and whole grain breads and bread products). Conversion of dietary tryptophan to niacin also contributes to niacin intake.

Niacin Deficiency and Pellagra

Prevention of niacin deficiency.

Treatment of pellagra. Niacinamide preferred by some clinicians due to its lack of vasodilating effects.

Dosage and Administration

General

• Dietary supplements containing niacin are not FDA-labeled for prevention of cardiovascular events or management of dyslipidemias; use prescription-only preparations for these indications.
• Do not use different formulations (i.e., immediate-release, extended-release) interchangeably since pharmacokinetics (e.g., metabolism) may vary. (See Substitution of Different Niacin Preparations under Cautions.)
• Minimize flushing, pruritus, and GI distress by initiating therapy at low dosages, increasing dosage gradually, and avoiding administration on an empty stomach. May also administer a prostaglandin-synthesis inhibitor (e.g., aspirin 325 mg, ibuprofen 200 mg) 30 minutes prior to administration of niacin to reduce flushing.

Administration

Oral Administration

Immediate-release niacin (e.g., Niacor^®): Administer orally with meals.

Extended-release niacin (Niaspan^®) or extended-release niacin/lovastatin fixed combination (Advicor^®): Administer orally at bedtime following a low-fat snack. Take tablets whole; do not break, crush, or chew. Do not administer Advicor^® with grapefruit juice due to increased risk of myopathy associated with lovastatin component.

To minimize risk of flushing or pruritus, avoid administering concomitantly with alcohol or hot drinks.

Dosage

Commercially available as dietary supplements and as prescription-only preparations. Do not use these preparations interchangeably. (See Substitution of Different Niacin Preparations under Cautions.)

Pediatric Patients

Dietary Requirements

Recommended Daily Allowance (RDA) generally expressed in terms of niacin equivalents (NE). NE is calculated as follows: 1 mg of NE = 1 mg of niacin = 60 mg of tryptophan.

Oral

Niacin Deficiency

Pellagra

Oral

Niacin or niacinamide: 100–300 mg daily in divided doses.

Adults

Prevention of Cardiovascular Events

Oral

Extended-release niacin (Niaspan^®): Initially, 500 mg once daily at bedtime. If response is inadequate, increase dosage by no more than 500 mg at 4-week intervals until desired effect is observed or maximum daily dosage of 2 g is reached.

Usual maintenance dosage is 1–2 g once daily at bedtime.

In patients previously treated with immediate-release preparations or in those who have discontinued extended-release niacin (Niaspan^®) therapy for an extended period, titrate dosage as with initial therapy.

Dyslipidemias

Oral

Immediate-release preparations: Initially, 100–500 mg 3 times daily. Increase dosage gradually (e.g., 300 mg daily at 4- to 7-day intervals) until desired effect is achieved. Usual maintenance dosage is 1.5–3 g daily given in 2 or 3 divided doses.

Initial dosage of 250 mg daily following the evening meal recommended by manufacturer of Niacor^® (immediate-release preparation). Increase dosage of Niacor^® at 4- to 7-day intervals until desired effect is achieved or dosage of 1.5–2 g daily is reached. If adequate response is not achieved after 2 months, may then increase dosage at 2- to 4-week intervals to 3 g daily (1 g 3 times daily). Manufacturer of Niacor^® states that higher doses (up to 6 g daily) occasionally may be required in patients with marked lipid abnormalities. Usual maintenance dosage recommended by manufacturer of Niacor^® is 1–2 g daily given in 2 or 3 divided doses.

Extended-release niacin (Niaspan^®): Initially, 500 mg once daily at bedtime. If adequate response is not achieved after 4 weeks, increase dosage by no more than 500 mg at 4-week intervals until desired effect is observed. Usual maintenance dosage is 1–2 g once daily at bedtime. Titrate Niaspan^® dosage as with initial therapy in patients previously treated with immediate-release niacin preparations or in those in whom therapy with extended-release niacin (Niaspan^®) has been discontinued for a prolonged period.

Extended-release niacin (Niaspan^®) and lovastatin combination therapy: In patients already receiving a stable dosage of lovastatin, add Niaspan^® (using recommended titration schedule). In patients already receiving a stable dosage of Niaspan^®, add lovastatin (at initial dosage of 20 mg once daily). Adjust dosage at 4-week intervals.

Fixed combination of extended-release niacin and lovastatin (Advicor^®): Use only in patients already receiving a stable dosage of Niaspan^®; in patients currently receiving niacin preparations other than Niaspan^®, discontinue current niacin therapy and switch to Niaspan^®. Once a stable Niaspan^® dosage is reached, switch to Advicor^® at the same niacin-equivalent dosage as Niaspan^®. In patients currently receiving a stable dosage of lovastatin, add Niaspan^® (using the recommended titration schedule) until a stable dosage has been reached, then switch to Advicor^® at the same niacin-equivalent dosage as Niaspan^®. Increase Advicor^® dosage by no more than 500 mg (of the niacin component) at 4-week intervals. Usual maintenance dosage ranges from 500 mg of extended-release niacin and 20 mg of lovastatin to 2 g of extended-release niacin and 40 mg of lovastatin once daily. If Advicor^® therapy has been discontinued for >7 days, reinstitute at the lowest available dosage. Because of differences in bioavailability, do not substitute 1 tablet of Advicor^® 1 g/40 mg for 2 tablets of Advicor^® 500 mg/20 mg, or vice versa.

Dietary Requirements

RDA generally expressed in terms of NE. NE is calculated as follows: 1 mg of NE = 1 mg of niacin = 60 mg of tryptophan.

Oral

RDA for healthy men: 16 mg of NE daily.

RDA for healthy women: 14 mg of NE daily.

RDA for pregnant women: 18 mg of NE daily. Higher dosages required in women pregnant with >1 fetus.

RDA for lactating women: 17 mg of NE daily. Higher dosages required in mothers nursing >1 infant.

Higher dosages required in patients with Hartnup disease, liver cirrhosis, carcinoid syndrome, malabsorption syndrome, or in individuals receiving long-term isoniazid therapy or undergoing hemodialysis or peritoneal dialysis.

Niacin Deficiency

Pellagra

Oral

Niacin or niacinamide: 300–500 mg daily in divided doses.

Hartnup Disease

Oral

Niacin: 50–200 mg daily.

Prescribing Limits

Adults

Prevention of Cardiovascular Events

Oral

Extended-release niacin (Niaspan^®): Maximum 2 g daily.

Dyslipidemias

Oral

Immediate-release preparations: Maximum 4.5 g daily; manufacturer of Niacor^® states that maximum of 6 g daily generally should not be exceeded.

Extended-release niacin (Niaspan^®): Maximum 2 g daily. When used in combination with lovastatin, maximum 2 g of Niaspan^® and 40 mg of lovastatin daily.

Fixed combination of extended-release niacin and lovastatin (Advicor^®): Maximum 2 g of extended-release niacin and 40 mg of lovastatin daily.