Niacin (Niaspan)
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Niacin (Niaspan)

NIASPAN®
(niacin) Extended-Release Tablet, Film Coated, Extended Release for Oral Use.

DRUG DESCRIPTION

NIASPAN (niacin tablet, film-coated extended-release), contains niacin, which at therapeutic doses is an antihyperlipidemic agent. Niacin (nicotinic acid, or 3-pyridinecarboxylic acid) is a white, crystalline powder, very soluble in water, with the following structural formula:

NIASPAN®
  (niacin) Structural Formula Illustration

NIASPAN (niacin) is an unscored, medium-orange, film-coated tablet for oral administration and is available in three tablet strengths containing 500, 750, and 1000 mg niacin. NIASPAN (niacin) tablets also contain the inactive ingredients hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD&C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

What are the possible side effects of niacin ?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • feeling light-headed, fainting;
  • fast, pounding, or uneven heart beats;
  • feeling short of breath;
  • swelling;
  • jaundice (yellowing of your skin or eyes); or
  • muscle pain, tenderness, or weakness with fever or flu symptoms and dark colored urine.

If you are diabetic, tell your doctor about any changes in your...

Read All Potential Side Effects and See Pictures of Niaspan »

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hyperlipidemia. Niacin therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate.

  1. NIASPAN (niacin) is indicated to reduce elevated TC, LDL-C, Apo B and TG levels, and to increase HDL-C in patients with primary hyperlipidemia and mixed dyslipidemia.
  2. NIASPAN (niacin) in combination with simvastatin or lovastatin is indicated for the treatment of primary hyperlipidemia and mixed dyslipidemia when treatment with NIASPAN (niacin) , simvastatin, or lovastatin monotherapy is considered inadequate.
  3. In patients with a history of myocardial infarction and hyperlipidemia, niacin is indicated to reduce the risk of recurrent nonfatal myocardial infarction.
  4. In patients with a history of coronary artery disease (CAD) and hyperlipidemia, niacin, in combination with a bile acid binding resin, is indicated to slow progression or promote regression of atherosclerotic disease.
  5. NIASPAN (niacin) in combination with a bile acid binding resin is indicated to reduce elevated TC and LDL-C levels in adult patients with primary hyperlipidemia.
  6. Niacin is also indicated as adjunctive therapy for treatment of adult patients with severe hypertriglyceridemia who present a risk of pancreatitis and who do not respond adequately to a determined dietary effort to control them.

Limitations of Use

No incremental benefit of NIASPAN (niacin) coadministered with simvastatin or lovastatin on cardiovascular morbidity and mortality over and above that demonstrated for niacin, simvastatin, or lovastatin monotherapy has been established.

DOSAGE AND ADMINISTRATION

NIASPAN (niacin) should be taken at bedtime, after a low-fat snack, and doses should be individualized according to patient response. Therapy with NIASPAN (niacin) must be initiated at 500 mg at bedtime in order to reduce the incidence and severity of side effects which may occur during early therapy. The recommended dose escalation is shown in Table 1 below.

Table 1. Recommended Dosing

  Week(s) Daily dose NIASPAN Dosage
INITIAL TITRATION 1 to 4 500 mg 1 NIASPAN 500 mg tablet at bedtime
SCHEDULE 5 to 8 1000 mg 1 NIASPAN 1000 mg tablet or 2 NIASPAN 500 mg tablets at bedtime
  * 1500 mg 2 NIASPAN 750 mg tablets or 3 NIASPAN 500 mg tablets at bedtime
  * 2000 mg 2 NIASPAN 1000 mg tablets or 4 NIASPAN 500 mg tablets at bedtime
* After Week 8, titrate to patient response and tolerance. If response to 1000 mg daily is inadequate, increase dose to 1500 mg daily; may subsequently increase dose to 2000 mg daily. Daily dose should not be increased more than 500 mg in a 4-week period, and doses above 2000 mg daily are not recommended. Women may respond at lower doses than men.

Maintenance Dose

The daily dosage of NIASPAN (niacin) should not be increased by more than 500 mg in any 4—week period. The recommended maintenance dose is 1000 mg (two 500 mg tablets or one 1000 mg tablet) to 2000 mg (two 1000 mg tablets or four 500 mg tablets) once daily at bedtime. Doses greater than 2000 mg daily are not recommended. Women may respond at lower NIASPAN doses than men [see Clinical Studies].

Single-dose bioavailability studies have demonstrated that two of the 500 mg and one of the 1000 mg tablet strengths are interchangeable but three of the 500 mg and two of the 750 mg tablet strengths are not interchangeable.

If lipid response to NIASPAN (niacin) alone is insufficient or if higher doses of NIASPAN (niacin) are not well tolerated, some patients may benefit from combination therapy with a bile acid binding resin or statin [see DRUG INTERACTIONS, Concomitant Therapy below and Clinical Studies].

Flushing of the skin [see ADVERSE REACTIONS] may be reduced in frequency or severity by pretreatment with aspirin (up to the recommended dose of 325 mg taken 30 minutes prior to NIASPAN (niacin) dose). Tolerance to this flushing develops rapidly over the course of several weeks. Flushing, pruritus, and gastrointestinal distress are also greatly reduced by slowly increasing the dose of niacin and avoiding administration on an empty stomach. Concomitant alcoholic, hot drinks or spicy foods may increase the side effects of flushing and pruritus and should be avoided around the time of NIASPAN (niacin) ingestion.

Equivalent doses of NIASPAN (niacin) should not be substituted for sustained-release (modified-release, timed-release) niacin preparations or immediate-release (crystalline) niacin [see WARNINGS AND PRECAUTIONS]. Patients previously receiving other niacin products should be started with the recommended NIASPAN (niacin) titration schedule (see Table 1), and the dose should subsequently be individualized based on patient response.

If NIASPAN (niacin) therapy is discontinued for an extended period, reinstitution of therapy should include a titration phase (see Table 1).

NIASPAN (niacin) tablets should be taken whole and should not be broken, crushed or chewed before swallowing.

Concomitant Therapy

Concomitant Therapy with Lovastatin or Simvastatin

Patients already receiving a stable dose of lovastatin or simvastatin who require further TG-lowering or HDL-raising (e.g., to achieve NCEP non-HDL-C goals), may receive concomitant dosage titration with NIASPAN (niacin) per NIASPAN (niacin) recommended initial titration schedule [see DOSAGE AND ADMINISTRATION]. For patients already receiving a stable dose of NIASPAN (niacin) who require further LDL-lowering (e.g., to achieve NCEP LDL-C goals), the usual recommended starting dose of lovastatin and simvastatin is 20 mg once a day. Dose adjustments should be made at intervals of 4 weeks or more. Combination therapy with NIASPAN (niacin) and lovastatin or NIASPAN (niacin) and simvastatin should not exceed doses of 2000 mg NIASPAN (niacin) and 40 mg lovastatin or simvastatin daily.

Dosage in Patients with Renal or Hepatic Impairment

Use of NIASPAN (niacin) in patients with renal or hepatic impairment has not been studied. NIASPAN (niacin) is contraindicated in patients with significant or unexplained hepatic dysfunction. NIASPAN (niacin) should be used with caution in patients with renal impairment [see WARNINGS AND PRECAUTIONS].

HOW SUPPLIED

Dosage Forms and Strengths

500 mg unscored, medium-orange, film-coated, capsule-shaped tablets
750 mg unscored, medium-orange, film-coated, capsule-shaped tablets
1000 mg unscored, medium-orange, film-coated, capsule-shaped tablets

NIASPAN (niacin) tablets are supplied as unscored, medium-orange, film-coated, capsule-shaped (containing 500 or 750 mg of niacin) or oval shaped (containing 1000 mg of niacin) tablets, in an extended-release formulation. Tablets are printed with the Abbott 'A' logo and the tablet strength (500, 750 or 1000). Tablets are supplied in bottles of 90 as shown below.

500 mg tablets:bottles of 90 - NDC# 0074-3074-90
750 mg tablets:bottles of 90 - NDC# 0074-3079-90
1000 mg tablets:bottles of 90 - NDC# 0074-3080-90

Storage: Store at room temperature 20° to 25°C (68° to 77°F).

Manufactured for Abbott Laboratories, North Chicago, IL 60064, U.S.A. 500 mg tablets. Manufactured by Norwich Pharmaceuticals, Inc., Norwich, NY 13815 or 500 mg, 750 mg and 1000 mg tablets by Abbott Pharmaceuticals PR Ltd., Barceloneta, PR 00617. Revised: 11/2010

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

Clinical Studies Experience

In the placebo-controlled clinical trials database of 402 patients (age range 21-75 years, 33% women, 89% Caucasians, 7% Blacks, 3% Hispanics, 1% Asians) with a median treatment duration of 16 weeks, 16% of patients on NIASPAN (niacin) and 4% of patients on placebo discontinued due to adverse reactions. The most common adverse reactions in the group of patients treated with NIASPAN (niacin) that led to treatment discontinuation and occurred at a rate greater than placebo were flushing (6% vs. 0%), rash (2% vs. 0%), diarrhea (2% vs. 0%), nausea (1% vs. 0%), and vomiting (1% vs. 0%). The most commonly reported adverse reactions (incidence > 5% and greater than placebo) in the NIASPAN (niacin) controlled clinical trial database of 402 patients were flushing, diarrhea, nausea, vomiting, increased cough and pruritus.

In the placebo-controlled clinical trials, flushing episodes (i.e., warmth, redness, itching and/or tingling) were the most common treatment-emergent adverse reactions (reported by as many as 88% of patients) for NIASPAN (niacin) . Spontaneous reports suggest that flushing may also be accompanied by symptoms of dizziness, tachycardia, palpitations, shortness of breath, sweating, burning sensation/skin burning sensation, chills, and/or edema, which in rare cases may lead to syncope. In pivotal studies, 6% (14/245) of NIASPAN (niacin) patients discontinued due to flushing. In comparisons of immediate-release (IR) niacin and NIASPAN (niacin) , although the proportion of patients who flushed was similar, fewer flushing episodes were reported by patients who received NIASPAN (niacin) . Following 4 weeks of maintenance therapy at daily doses of 1500 mg, the incidence of flushing over the 4-week period averaged 8.6 events per patient for IR niacin versus 1.9 following NIASPAN (niacin) .

Other adverse reactions occurring in ≥ 5% of patients treated with NIASPAN (niacin) and at an incidence greater than placebo are shown in Table 2 below.

Table 2. Treatment-Emergent Adverse Reactions by Dose Level in ≥ 5% of Patients and at an Incidence Greater than Placebo; Regardless of Causality Assessment in Placebo-Controlled Clinical Trials

  Placebo-Controlled Studies NIASPAN Treatment
  Recommended Daily Maintenance Doses
  Placebo
(n=157)
%
500 mg
(n = 87)
%
1000 mg
(n=110)
%
1500 mg
(n=136)
%
2000 mg
(n = 95)
%
Gastrointestinal Disorders
  Diarrhea 13 7 10 10 14
  Nausea 7 5 6 4 11
  Vomiting 4 0 2 4 9
  Respiratory          
  Cough, Increased 6 3 2 < 2 8
Skin and Subcutaneous Tissue Disorders
  Pruritus 2 8 0 3 0
  Rash 0 5 5 5 0
Vascular Disorders
  Flushing& 19 68 69 63 55
Note: Percentages are calculated from the total number of patients in each column.
Adverse reactions are reported at the initial dose where they occur.
@ Pooled results from placebo-controlled studies; for NIASPAN (niacin) , n = 245 and median treatment duration =16 weeks. Number of NIASPAN (niacin) patients (n) are not additive across doses.
The 500 mg/day dose is outside the recommended daily maintenance dosing range [see DOSAGE AND ADMINISTRATION]. 10 patients discontinued before receiving 500 mg, therefore they were not included.
&In general, the incidence of adverse events was higher in women compared to men.

Postmarketing Experience

Because the below reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

The following additional adverse reactions have been identified during post-approval use of NIASPAN (niacin) :

Hypersensitivity reactions, including anaphylaxis, angioedema, urticaria, flushing, dyspnea, tongue edema, larynx edema, face edema, peripheral edema, laryngismus, and vesiculobullous rash; maculopapular rash; dry skin; tachycardia; palpitations; atrial fibrillation; other cardiac arrhythmias; syncope; hypotension; postural hypotension; blurred vision; macular edema; peptic ulcers; eructation; flatulence; hepatitis; jaundice; decreased glucose tolerance; gout; myalgia; myopathy; dizziness; insomnia; asthenia; nervousness; paresthesia; dyspnea; sweating; burning sensation/skin burning sensation; skin discoloration, and migraine.

Clinical Laboratory Abnormalities

Chemistry: Elevations in serum transaminases [see WARNINGS AND PRECAUTIONS], LDH, fasting glucose, uric acid, total bilirubin, amylase and creatine kinase, and reduction in phosphorus.

Hematology: Slight reductions in platelet counts and prolongation in prothrombin time [see WARNINGS AND PRECAUTIONS].

Read the Niaspan (niacin) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Statins

Caution should be used when prescribing niacin ( ≥ 1 gm/day) with statins as these drugs can increase risk of jnyopathy/rhabdomyolysis. Combination therapy with NIASPAN (niacin) and lovastatin or NIASPAN (niacin) and simvastatin should not exceed doses of 2000 mg NIASPAN (niacin) and 40 mg lovastatin or simvastatin daily, [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Bile Acid Sequestrants

An in vitro study results suggest that the bile acid-binding resins have high niacin binding capacity. Therefore, 4 to 6 hours, or as great an interval as possible, should elapse between the ingestion of bile acid-binding resins and the administration of NIASPAN [see CLINICAL PHARMACOLOGY].

Aspirin

Concomitant aspirin may decrease the metabolic clearance of nicotinic acid. The clinical relevance of this finding is unclear.

Antihypertensive Therapy

Niacin may potentiate the effects of ganglionic blocking agents and vasoactive drugs resulting in postural hypotension.

Other

Vitamins or other nutritional supplements containing large doses of niacin or related compounds such as nicotinamide may potentiate the adverse effects of NIASPAN.

Laboratory Test Interactions

Niacin may produce false elevations in some fluorometric determinations of plasma or urinary catecholamines. Niacin may also give false-positive reactions with cupric sulfate solution (Benedict's reagent) in urine glucose tests.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

NIASPAN (niacin) preparations should not be substituted for equivalent doses of immediate-release (crystalline) niacin. For patients switching from immediate-release niacin to NIASPAN (niacin) , therapy with NIASPAN (niacin) should be initiated with low doses (i.e., 500 mg at bedtime) and the NIASPAN (niacin) dose should then be titrated to the desired therapeutic response [see DOSAGE AND ADMINISTRATION].

Caution should also be used when NIASPAN (niacin) is used in patients with unstable angina or in the acute phase of an MI, particularly when such patients are also receiving vasoactive drugs such as nitrates, calcium channel blockers, or adrenergic blocking agents.

Niacin is rapidly metabolized by the liver, and excreted through the kidneys. NIASPAN (niacin) is contraindicated in patients with significant or unexplained hepatic impairment [see CONTRAINDICATIONS] and should be used with caution in patients with renal impairment. Patients with a past history of jaundice, hepatobiliary disease, or peptic ulcer should be observed closely during NIASPAN (niacin) therapy.

Skeletal Muscle

Cases of rhabdomyolysis have been associated with concomitant administration of lipid-altering doses ( > 1 g/day) of niacin and statins. Physicians contemplating combined therapy with statins and NIASPAN (niacin) should carefully weigh the potential benefits and risks and should carefully monitor patients for any signs and symptoms of muscle pain, tenderness, or weakness, particularly during the initial months of therapy and during any periods of upward dosage titration of either drug. Periodic serum creatine phosphokinase (CPK) and potassium determinations should be considered in such situations, but there is no assurance that such monitoring will prevent the occurrence of severe myopathy.

The risk for myopathy and rhabdomyolysis are increased when lovastatin or simvastatin are coadministered with NIASPAN (niacin) , particularly in elderly patients and patients with diabetes, renal failure, or uncontrolled hypothyroidism.

Liver Dysfunction

Cases of severe hepatic toxicity, including fulminant hepatic necrosis, have occurred in patients who have substituted sustained-release (modified-release, timed-release) niacin products for immediate-release (crystalline) niacin at equivalent doses.

NIASPAN (niacin) should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease. Active liver diseases or unexplained transaminase elevations are contraindications to the use of NIASPAN.

Niacin preparations have been associated with abnormal liver tests. In three placebo-controlled clinical trials involving titration to final daily NIASPAN (niacin) doses ranging from 500 to 3000 mg, 245 patients received NIASPAN (niacin) for a mean duration of 17 weeks. No patient with normal serum transaminase levels (AST, ALT) at baseline experienced elevations to more than 3 times the upper limit of normal (ULN) during treatment with NIASPAN (niacin) . In these studies, fewer than 1% (2/245) of NIASPAN (niacin) patients discontinued due to transaminase elevations greater than 2 times the ULN.

In three safety and efficacy studies with a combination tablet of NIASPAN (niacin) and lovastatin involving titration to final daily doses (expressed as mg of niacin/ mg of lovastatin) 500 mg/10 mg to 2500 mg/40 mg, ten of 1028 patients (1.0%) experienced reversible elevations in AST/ALT to more than 3 times the ULN. Three of ten elevations occurred at doses outside the recommended dosing limit of 2000 mg/40 mg; no patient receiving 1000 mg/20 mg had 3-fold elevations in AST/ALT.

Niacin extended-release and simvastatin can cause abnormal liver tests. In a simvastatin-controlled, 24 week study with a fixed dose combination of NIASPAN (niacin) and simvastatin in 641 patients, there were no persistent increases (more than 3x the ULN) in serum transaminases. In three placebo-controlled clinical studies of extended-release niacin there were no patients with normal serum transaminase levels at baseline who experienced elevations to more than 3x the ULN. Persistent increases (more than 3x the ULN) in serum transaminases have occurred in approximately 1% of patients who received simvastatin in clinical studies. When drug treatment was interrupted or discontinued in these patients, the transaminases levels usually fell slowly to pretreatment levels. The increases were not associated with jaundice or other clinical signs or symptoms. There was no evidence of hypersensitivity.

In the placebo-controlled clinical trials and the long-term extension study, elevations in transaminases did not appear to be related to treatment duration; elevations in AST levels did appear to be dose related. Transaminase elevations were reversible upon discontinuation of NIASPAN (niacin) .

Liver function tests should be performed on all patients during therapy with NIASPAN (niacin) . Serum transaminase levels, including AST and ALT (SGOT and SGPT), should be monitored before treatment begins, every 6 to 12 weeks for the first year, and periodically thereafter (e.g., at approximately 6-month intervals). Special attention should be paid to patients who develop elevated serum transaminase levels, and in these patients, measurements should be repeated promptly and then performed more frequently. If the transaminase levels show evidence of progression, particularly if they rise to 3 times ULN and are persistent, or if they are associated with symptoms of nausea, fever, and/or malaise, the drug should be discontinued.

Laboratory Abnormalities

Increase in Blood Glucose: Niacin treatment can increase fasting blood glucose. Frequent monitoring of blood glucose should be performed to ascertain that the drug is producing no adverse effects. Diabetic patients may experience a dose-related increase in glucose intolerance. Diabetic or potentially diabetic patients should be observed closely during treatment with NIASPAN (niacin) , particularly during the first few months of use or dose adjustment; adjustment of diet and/or hypoglycemic therapy may be necessary.

Reduction in platelet count: NIASPAN (niacin) has been associated with small but statistically significant dose-related reductions in platelet count (mean of -11% with 2000 mg). Caution should be observed when NIASPAN (niacin) is administered concomitantly with anticoagulants; platelet counts should be monitored closely in such patients.

Increase in Prothrombin Time (PT): NIASPAN (niacin) has been associated with small but statistically significant increases in prothrombin time (mean of approximately +4%); accordingly, patients undergoing surgery should be carefully evaluated. Caution should be observed when NIASPAN (niacin) is administered concomitantly with -anticoagulants; r»mthrpmbin time should be monitored closely in such patients.

Increase in Uric Acid: Elevated uric acid levels have occurred with niacin therapy, therefore use with caution in patients predisposed to gout.

Decrease in Phosphorus: In placebo-controlled trials, NIASPAN (niacin) has been associated with small but statistically significant, dose-related reductions in phosphorus levels (mean of -13% with 2000 mg). Although these reductions were transient, phosphorus levels should be monitored periodically in patients at risk for hypophosphatemia.

Patient Counseling Information

Patient Counseling

Patients should be advised to adhere to their National Cholesterol Education Program (NCEP) recommended diet, a regular exercise program, and periodic testing of a fasting lipid panel.

Patients should be advised to inform other healthcare professionals prescribing a new medication that they are taking NIASPAN (niacin) .

The patient should be informed of the following:

Dosing Time

NIASPAN (niacin) tablets should be taken at bedtime, after a low-fat snack. Administration on an empty stomach is not recommended.

Tablet Integrity

NIASPAN (niacin) tablets should not be broken, crushed or chewed, but should be swallowed whole.

Dosing Interruption

If dosing is interrupted for any length of time, their physician should be contacted prior to restarting therapy; re-titration is recommended.

Muscle Pain

Notify their physician of any unexplained muscle pain, tenderness, or weakness promptly. They should discuss all medication, both prescription and over the counter, with their physician.

Flushing

Flushing (warmth, redness, itching and/or tingling of the skin) is a common side effect of niacin therapy that may subside after several weeks of consistent NIASPAN (niacin) use. Flushing may vary in severity and is more likely to occur with initiation of therapy, or during dose increases. By dosing at bedtime, flushing will most likely occur during sleep. However, if awakened by flushing at night, the patient should get up slowly, especially if feeling dizzy, feeling faint, or taking blood pressure medications. Advise patients of the symptoms of flushing and how they differ from the symptoms of a myocardial infarction.

Use of Aspirin Medication

Taking aspirin (up to the recommended dose of 325 mg) approximately 30 minutes before dosing can minimize flushing.

Diet

Avoid ingestion of alcohol, hot beverages and spicy foods around the time of taking NIASPAN (niacin) to minimize flushing.

Supplements

Notify their physician if they are taking vitamins or other nutritional supplements containing niacin or nicotinamide.

Dizziness

Notify their physician if symptoms of dizziness occur.

Diabetics

If diabetic, to notify their physician of changes in blood glucose.

Pregnancy

Discuss future pregnancy plans with your patients, and discuss when to stop NIASPAN (niacin) if they are trying to conceive. Patients should be advised that if they become pregnant, they should stop taking NIASPAN (niacin) and call their healthcare professional.

Breastfeeding

Women who are breastfeeding should be advised to not use NIASPAN (niacin) . Patients, who have a lipid disorder and are breastfeeding, should be advised to discuss the options with their healthcare professional.

Nonclinical Toxicology

Carcinogenesis and Mutagenesis and Impairment of Fertility

Niacin administered to mice for a lifetime as a 1% solution in drinking water was not carcinogenic. The mice in this study received approximately 6 to 8 times a human dose of 3000 mg/day as determined on a mg/m2 basis. Niacin was negative for mutagenicity in the Ames test. No studies on impairment of fertility have been performed. No studies have been conducted with NIASPAN (niacin) regarding carcinogenesis, mutagenesis, or impairment of fertility.

Use In Specific Populations

Pregnancy

Pregnancy Category C

Animal reproduction studies have not been conducted with niacin or with NIASPAN. It is also not known whether niacin at doses typically used for lipid disorders can cause fetal harm when administered to pregnant women or whether it can affect reproductive capacity. If a woman receiving niacin for primary hyperlipidemia becomes pregnant, the drug should be discontinued. If a woman being treated with niacin for hypertriglyceridemia conceives, the benefits and risks of continued therapy should be assessed on an individual basis.

All statins are contraindicated in pregnant and nursing women. When NIASPAN (niacin) is administered with a statin in a woman of childbearing potential, refer to the pregnancy category and product labeling for the statin.

Nursing Mothers

Niacin is excreted into human milk but the actual infant dose or infant dose as a percent of the maternal dose is not known. Because of the potential for serious adverse reactions in nursing infants from lipid-altering doses of nicotinic acid, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. No studies have been conducted with NIASPAN (niacin) in nursing mothers.

Pediatric Use

Safety and effectiveness of niacin therapy in pediatric patients ( ≤ 16 years) have not been established.

Geriatric Use

Of 979 patients in clinical studies of NIASPAN (niacin) , 21% of the patients were age 65 and over. No overall differences in safety and effectiveness were observed between these patients and younger patients, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.

Renal Impairment

No studies have been performed in this population. NIASPAN (niacin) should be used with caution in patients with renal impairment [see WARNINGS AND PRECAUTIONS].

Hepatic Impairment

No studies have been performed in this population. NIASPAN (niacin) should be used with caution in patients with a past history of liver disease and/or who consume substantial quantities of alcohol. Active liver disease, unexplained transaminase elevations and significant or unexplained hepatic dysfunction are contraindications to the use of NIASPAN [see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS].

Gender

Data from the clinical trials suggest that women have a greater hypolipidemic response than men at equivalent doses of NIASPAN (niacin) .

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

Supportive measures should be undertaken in the event of an overdose.

CONTRAINDICATIONS

NIASPAN (niacin) is contraindicated in the following conditions:

  • Active liver disease or unexplained persistent elevations in hepatic transaminases [see WARNINGS AND PRECAUTIONS]
  • Patients with active peptic ulcer disease
  • Patients with arterial bleeding
  • Hypersensitivity to niacin or any component of this medication [see ADVERSE REACTIONS]

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Mechanism of Action

The mechanism by which niacin alters lipid profiles has not been well defined. It may involve several actions including partial inhibition of release office fatty acids from adipose tissue, and increased lipoprotein lipase activity, which may increase the rate of chylomicron triglyceride removal from plasma. Niacin decreases the rate of hepatic synthesis of VLDL and LDL, and does not appear to affect fecal excretion of fats, sterols, or bile acids.

Pharmacodynamics

Niacin functions in the body after conversion to nicotinamide adenine dinucleotide (NAD) in the NAD coenzyme system. Niacin (but not nicotinamide) in gram doses reduces total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), and triglycerides (TG), and increases high-density lipoprotein cholesterol (HDL-C). The magnitude of individual lipid and lipoprotein responses may be influenced by the severity and type of underlying lipid abnormality. The increase in HDL-C is associated with an increase in apolipoprotein A-I (Apo A-I) and a shift in the distribution of HDL subfractions. These shifts include an increase in the HDL2: HDL3 ratio, and an elevation in lipoprotein A-I (Lp A-I, an HDL-C particle containing only Apo A-I). Niacin treatment also decreases serum levels of apolipoprotein B-100 (Apo B), the major protein component of the very low-density lipoprotein (VLDL) and LDL fractions, and of Lp(a), a variant form of LDL independently associated with coronary risk. In addition, preliminary reports suggest that niacin causes favorable LDL particle size transformations, although the clinical relevance of this effect requires further investigation. The effect of niacin-induced changes in lipids/proteins on cardiovascular morbidity or mortality in individuals without preexisting coronary disease has not been established.

A variety of clinical studies have demonstrated that elevated levels of TC, LDL-C, and Apo B promote human atherosclerosis. Similarly, decreased levels of HDL-C are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the level of Total-C and LDL-C, and inversely with the level of HDL-C.

Like LDL, cholesterol-enriched triglyceride-rich lipoproteins, including VLDL, intermediate-density lipoprotein (IDL), and their remnants, can also promote atherosclerosis. Elevated plasma TG are frequently found in a triad with low HDL-C levels and small LDL particles, as well as in association with non-lipid metabolic risk factors for coronary heart disease (CHD). As such, total plasma TG has not consistently been shown to be an independent risk factor for CHD. Furthermore, the independent effect of raising HDL-C or lowering TG on the risk of coronary and cardiovascular morbidity and mortality has not been determined.

Pharmacokinctics

Absorption

Due to extensive and saturable first-pass metabolism, niacin concentrations in the general circulation are dose dependent and highly variable. Time to reach the maximum niacin plasma concentrations was about 5 hours following NIASPAN (niacin) . To reduce the risk of gastrointestinal (GI) upset, administration of NIASPAN (niacin) with a low-fat meal or snack is recommended.

Single-dose bioavailability studies have demonstrated that the 500 mg and 1000 mg tablet strengths are dosage form equivalent but the 500 mg and 750 mg tablet strengths are not dosage form equivalent.

Metabolism

The pharmacokinetic profile of niacin is complicated due to extensive first-pass metabolism that is dose-rate specific and, at the doses used to treat dyslipidemia, saturable. In humans, one pathway is through a simple conjugation step with glycine to form nicotinuric acid (NUA). NUA is then excreted in the urine, although there may be a small amount of reversible metabolism back to niacin. The other pathway results in the formation of nicotinamide adenine dinucleotide (NAD). It is unclear whether nicotinamide is formed as a precursor to, or following the synthesis of, NAD. Nicotinamide is further metabolized to at least N-methylnicotinamide (MNA) and nicotinamide-N-oxide (NNO). MNA is further metabolized to two other compounds, N-methyl-2-pyridone-5-carboxamide (2PY) and N-methyl-4-pyridone-5-carboxamide (4PY). The formation of 2PY appears to predominate over 4PY in humans. At the doses used to treat hyperlipidemia, these metabolic pathways are saturable, which explains the nonlinear relationship between niacin dose and plasma concentrations following multiple-dose NIASPAN (niacin) administration.

Nicotinamide does not have hypolipidemic activity; the activity of the other metabolites is unknown.

Elimination

Following single and multiple doses, approximately 60 to 76% of the niacin dose administered as NIASPAN was recovered in urine as niacin and metabolites; up to 12% was recovered as unchanged niacin after multiple dosing. The ratio of metabolites recovered in the urine was dependent on the dose administered.

No pharmacokinetic studies have been performed in this population ( ≤ 16 years) [see Use In Specific Populations].

Geriatric Use

No pharmacokinetic studies have been performed in this population ( > 65 years) [see Use In Specific Populations].

Renal Impairment

No pharmacokinetic studies have been performed in this population. NIASPAN (niacin) should be used with caution in patients with renal disease [see WARNINGS AND PRECAUTIONS].

Hepatic Impairment

No pharmacokinetic studies have been performed in this population. Active liver disease, unexplained transaminase elevations and significant or unexplained hepatic dysfunction are contraindications to the use of NIASPAN [see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS].

Gender

Steady-state plasma concentrations of niacin and metabolites after administration of NIASPAN (niacin) are generally higher in women than in men, with the magnitude of the difference varying with dose and metabolite. This gender differences observed in plasma levels of niacin and its metabolites may be due to gender-specific differences in metabolic rate or volume of distribution. Recovery of niacin and metabolites in urine, however, is generally similar for men and women, indicating that absorption is similar for both genders [see Gender].

Drug interactions

Fluvastatin

Niacin did not affect fluvastatin pharmacokinetics [see DRUG INTERACTIONS].

Lovastatin

When NIASPAN (niacin) 2000 mg and lovastatin 40 mg were co-administered, NIASPAN (niacin) increased lovastatin Cmax and AUC by 2% and 14%, respectively, and decreased lovastatin acid Cmax and AUC by 22% and 2%, respectively. Lovastatin reduced NIASPAN bioavailability by 2-3% [see DRUG INTERACTIONS].

Simvastatin

When NIASPAN (niacin) 2000 mg and simvastatin 40 mg were co-administered, NIASPAN (niacin) increased simvastatin Cmax and AUC by 1% and 9%, respectively, and simvastatin acid Cmax and AUC by 2% and 18%, respectively. Simvastatin reduced NIASPAN bioavailability by 2% [see DRUG INTERACTIONS].

Bile Acid Sequestrants

An in vitro study was carried out investigating the niacin-binding capacity of colestipol and cholestyramine. About 98% of available niacin was bound to colestipol, with 10 to 30% binding to cholestyramine [see DRUG INTERACTIONS].

Clinical Studies

Niacin Clinical Studies

The role of LDL-C in atherogenesis is supported by pathological observations, clinical studies, and many animal experiments. Observational epidemiological studies have clearly established that high TC or LDL-C and low HDL-C are risk factors for CHD. Additionally, elevated levels of Lp(a) have been shown to be independently associated with CHD risk.

Niacin's ability to reduce mortality and the risk of definite, nonfatal myocardial infarction (MI) has been assessed in long-term studies. The Coronary Drug Project, completed in 1975, was designed to assess the safety and efficacy of niacin and other lipid-altering drugs in men 30 to 64 years old with a history of MI. Over an observation period of 5 years, niacin treatment was associated with a statistically significant reduction in nonfatal, recurrent MI. The incidence of definite, nonfatal MI was 8.9% for the 1,119 patients randomized to nicotinic acid versus 12.2% for the 2,789 patients who received placebo (p < 0.004). Total mortality was similar in the two groups at 5 years (24.4% with nicotinic acid versus 25.4% with placebo; p=N.S.). At the time of a 15-year follow-up, there were 11% (69) fewer deaths in the niacin group compared to the placebo cohort (52.0% versus 58.2%; p=0.0004). However, mortality at 15 years was not an original endpoint of the Coronary Drug Project. In addition, patients had not received niacin for approximately 9 years, and confounding variables such as concomitant medication use and medical or surgical treatments were not controlled.

The Cholesterol-Lowering Atherosclerosis Study (CLAS) was a randomized, placebo-controlled, angiographic trial testing combined colestipol and niacin therapy in 162 non-smoking males with previous coronary bypass surgery. The primary, per-subject cardiac endpoint was global coronary artery change score. After 2 years, 61% of patients in the placebo cohort showed disease progression by global change score (n=82), compared with only 38.8% of drug-treated subjects (n=80), when both native arteries and grafts were considered (p < 0.005); disease regression also occurred more frequently in the drug-treated group (16.2% versus 2.4%; p=0.002). In a follow-up to this trial in a subgroup of 103 patients treated for 4 years, again, significantly fewer patients in the drug-treated group demonstrated progression than in the placebo cohort (48% versus 85%, respectively; p < 0.0001).

The Familial Atherosclerosis Treatment Study (FATS) in 146 men ages 62 and younger with Apo B levels ≥ 125 mg/dL, established coronary artery disease, and family histories of vascular disease, assessed change in severity of disease in the proximal coronary arteries by quantitative arteriography. Patients were given dietary counseling and randomized to treatment with either conventional therapy with double placebo (or placebo plus colestipol if the LDL-C was elevated); lovastatin plus colestipol; or niacin plus colestipol. In the conventional therapy group, 46% of patients had disease progression (and no regression) in at least one of nine proximal coronary segments; regression was the only change in 11%. In contrast, progression (as the only change) was seen in only 25% in the niacin plus colestipol group, while regression was observed in 39%. Though not an original endpoint of the trial, clinical events (death, MI, or revascularization for worsening angina) occurred in 10 of 52 patients who received conventional therapy, compared with 2 of 48 who received niacin plus colestipol.

The Harvard Atherosclerosis Reversibility Project (HARP) was a randomized placebo-controlled, 2.5-year study of the effect of a stepped-care antihyperlipidemic drug regimen on 91 patients (80 men and 11 women) with CHD and average baseline TC levels less than 250 mg/dL and ratios of TC to HDL-C greater than 4.0. Drug treatment consisted of an HMG-CoA reductase inhibitor administered alone as initial therapy followed by addition of varying dosages of either a slow-release nicotinic acid, cholestyramine, or gemfibrozil. Addition of nicotinic acid to the HMG-CoA reductase inhibitor resulted in further statistically significant mean reductions in TC, LDL-C, and TG, as well as a further increase in HDL-C in a majority of patients (40 of 44 patients). The ratios of TC to HDL-C and LDL-C to HDL-C were also significantly reduced by this combination drug regimen [see WARNINGS AND PRECAUTIONS].

NIASPAN (niacin) Clinical Studies

Placebo-Controlled Clinical Studies in Patients with Primary Hyperlipidemia and Mixed Dyslipidemia: In two randomized, double-blind, parallel, multi-center, placebo-controlled trials, NIASPAN (niacin) dosed at 1000,1500 or 2000 mg daily at bedtime with a low-fat snack for 16 weeks (including 4 weeks of dose escalation) favorably altered lipid profiles compared to placebo (Table 3). Women appeared to have a greater response than men at each NIASPAN (niacin) dose level (see Gender Effect, below).

Table 3. Lipid Response to NIASPAN (niacin) Therapy

Mean Percent Change from Baseline to Week 16*
Treatment n TC LDL-C HDL-C TC/HDL-C TG Lp(a) ApoB Apo A-I
NIASPAN1000 mg at bedtime 41 -3 -5 +18 -17 -21 -13 -6 +9
NIASPAN 2000 mg at bedtime 41 -10 -14 +22 -25 -28 -27 -16 +8
Placebo 40 0 -1 +4 -3 0 0 +1 +3
NIASPAN 1500 mg at bedtime 76 -8 -12 +20 -20 -13 -15 -12 +8
Placebo 73 +2 +1 +2 +1 +12 +2 +1 +2
n = number of patients at baseline;
* Mean percent change from baseline for all NIASPAN doses was significantly different (p < 0.05) from placebo for all lipid parameters shown except Apo A-I at 2000 mg.

In a double-blind, multi-center, forced dose-escalation study, monthly 500 mg increases in NIASPAN (niacin) dose resulted in incremental reductions of approximately 5% in LDL-C and Apo B levels in the daily dose range of 500 mg through 2000 mg (Table 4). Women again tended to have a greater response to NIASPAN (niacin) than men (see Gender Effect, below).

Table 4. Lipid Response in Dose-Escalation Study

  Mean Percent Change from Baseline*
Treatment n TC LDL-C HDL-C TC/HDL-C TG Lp(a) ApoB Apo A-I
Placebo 44 -2 -1 +5 -7 -6 -5 -2 +4
NIASPAN 87                
  500 mg at bedtime   -2 -3 +10 -10 -5 -3 -2 +5
  1 000 mg at bedtime   -5 -9 +15 -17 -11 -12 -7 +8
  1 500 mg at bedtime   -11 -14 +22 -26 -28 -20 -15 +10
  2000 mg at bedtime   -12 -17 +26 -29 -35 -24 -16 +12
n = number of patients enrolled;
Placebo data shown are after 24 weeks of placebo treatment.
* For all NIASPAN (niacin) doses except 500 mg, mean percent change from baseline was significantly different (p < 0.05) from placebo for all lipid parameters shown except Lp(a) and Apo A-I which were significantly different from placebo starting with 1500 mg and 2000 mg, respectively.

Pooled results for major lipids from these three placebo-controlled studies are shown below (Table 5).

Table 5. Selected Lipid Response to NIASPAN (niacin) in Placebo-Controlled Clinical Studies*

  Mean Baseline and Median Percent Change from Baseline (25th, 75th Percentiles)
NIASPAN Dose n LDL-C HDL-C TG
1 000 mg at bedtime 104      
Baseline (mg/dL) Percent Change   218
-7 (-15,0)
45
+14 (+7, +23)
172
-16 (-34, +3)
1 500 mg at bedtime 120      
Baseline (mg/dL) Percent Change   212
-13 (-21, -4)
46
+19 (+9, +31)
171
-25 (-45, -2)
2000 mg at bedtime 85      
Baseline (mg/dL) Percent Change   220
-16 (-26, -7)
44
+22 (+15, +34)
160
-38 (-52, -14)
* Represents pooled analyses of results; minimum duration on therapy at each dose was 4 weeks.

Gender Effect: Combined data from the three placebo-controlled NIASPAN (niacin) studies in patients with primary hyperlipidemia and mixed dyslipidemia suggest that, at each NIASPAN (niacin) dose level studied, changes in lipid concentrations are greater for women than for men (Table 6).

Table 6. Effect of Gender on NIASPAN (niacin) Dose Response

    Mean Percent Change from Baseline
NIASPAN n LDL-C HDL-C TG Apo B
Dose (M/F) M F M F M F M F
500 mg at bedtime 50/37 -2 -5 +11 +8 -3 -9 -1 -5
1000 mg at bedtime 76/52 -6* -11* +14 +20 -10 -20 -5* -10*
1500 mg at bedtime 104/59 -12 -16 +19 +24 -17 -28 -13 -15
2000 mg at bedtime 75/53 -15 -18 +23 +26 -30 -36 -16 -16
n = number of male/female patients enrolled.
* Percent change significantly different between genders (p < 0.05).

Other Patient Populations: In a double-blind, multi-center, 19-week study the lipid-altering effects of NIASPAN (niacin) (forced titration to 2000 mg at bedtime) were compared to baseline in patients whose primary lipid abnormality was a low level of HDL-C (HDL-C ≤ 40 mg/dL, TG ≤ 400 mg/dL, and LDL-C < 160, or ≤ 130 mg/dL in the presence of CHD). Results are shown below (Table 7).

Table 7. Lipid Response to NIASPAN (niacin) in Patients with Low HDL-C

  Mean Baseline and Mean Percent Change from Baseline*
  n TC LDL-C HDL-C TC/HDL-C TG Lp(a) ApoB Apo A-I LpA-I††
Baseline (mg/dL) 88 190 120 31 6 194 8 106 105 32
Week 19 (% Change) 71 -3 0 +26 -22 -30 -20 -9 +11 +20
n = number of patients
* Mean percent change from baseline was significantly different (p < 0.05) for all lipid parameters shown except LDL-C.
n = 72 at baseline and 69 at week 19.
††n = 30 at baseline and week 19.

At NIASPAN (niacin) 2000 mg/day, median changes from baseline (25th, 75th percentiles) for LDL-C, HDL-C, and TG were -3% (-14, +12%), +27% (+13, +38%), and -33% (-50, -19%), respectively.

NIASPAN (niacin) and Lovastatin Clinical Studies

Combination NIASPAN (niacin) and Lovastatin Study: In a multi-center, randomized, double-blind, parallel, 28-week study, a combination tablet of NIASPAN (niacin) and lovastatin was compared to each individual component in patients with Type Ha and lib hyperlipidemia. Using a forced dose-escalation study design, patients received each dose for at least 4 weeks. Patients randomized to treatment with the combination tablet of NIASPAN (niacin) and lovastatin initially received 500 mg/20 mg (expressed as mg of niacin/mg of lovastatin) once daily before bedtime. The dose was increased by 500 mg at 4-week intervals (based on the NIASPAN (niacin) component) to a maximum dose of 1000 mg/20 mg in one-half of the patients and 2000 mg/40 mg in the other half. The NIASPAN (niacin) monotherapy group underwent a similar titration from 500 mg to 2000 mg. The patients randomized to lovastatin monotherapy received 20 mg for 12 weeks titrated to 40 mg for up to 16 weeks. Up to a third of the patients randomized to the combination tablet of NIASPAN (niacin) and lovastatin or NIASPAN (niacin) monotherapy discontinued prior to Week 28. Results from this study showed that combination therapy decreased LDL-C, TG and Lp(a), and increased HDL-C in a dose-dependent fashion (Tables 8, 9,10, and 11). Results from this study for LDL-C mean percent change from baseline (the primary efficacy variable) showed that:

  1. LDL-lowering with the combination tablet of NIASPAN (niacin) and lovastatin was significantly greater than that achieved with lovastatin 40 mg only after 28 weeks of titration to a dose of 2000 mg/40 mg (p < 0.0001).
  2. The combination tablet of NIASPAN (niacin) and lovastatin at doses of 1000 mg/20 mg or higher achieved greater LDL-lowering than NIASPAN (niacin) (p < 0.0001).

The LDL-C results are summarized in Table 8.

Table 8. LDL-C mean percent change from baseline

Week Combination Tablet of NIASPAN and Lovastatin NIASPAN Lovastatin
  n* Dose (mg/mg) LDL n* Dose (mg) LDL n* Dose (mg) LDL
Baseline 57 - 190.9 mg/dL 61 - 189.7 mg/dL 61 - 185.6 mg/dL
12 47 1000/20 -30% 46 1000 -3% 56 20 -29%
16 45 1000/40 -36% 44 1000 -6% 56 40 -31%
20 42 1500/40 -37% 43 1500 -12% 54 40 -34%
28 42 2000/40 -42% 41 2000 -14% 53 40 -32%
* n = number of patients remaining in trial at each time point

Combination therapy achieved significantly greater HDL-raising compared to lovastatin and NIASPAN (niacin) monotherapy at all doses (Table 9).

Table 9. HDL-C mean percent change from baseline

Week Combination Tablet of NIASPAN and Lovastatin NIASPAN Lovastatin
  n* Dose (mg/mg) HDL n* Dose (mg) HDL n* Dose (mg) HDL
Baseline 57 - 45 mg/dL 61 - 47 mg/dL 61 - 43 mg/dL
12 47 1000/20 +20% 46 1000 +14% 56 20 +3%
16 45 1000/40 +20% 44 1000 +15% 56 40 +5%
20 42 1500/40 +27% 43 1500 +22% 54 40 +6%
28 42 2000/40 +30% 41 2000 +24% 53 40 +6%
* n = number of patients remaining in trial at each time point

In addition, combination therapy achieved significantly greater TG lowering at doses of 1000 mg/20mg or greater compared to lovastatin and NIASPAN (niacin) monotherapy (Table 10).

Table 10. TG median percent change from baseline

Week Combination Tablet of NIASPAN and Lovastatin NIASPAN Lovastatin
  n* Dose (mg/mg) TG n* Dose (mg) TG n* Dose (mg) TG
Baseline 57 - 174 mg/dL 61 - 186 mg/dL 61 - 171 mg/dL
12 47 1000/20 -32% 46 1000 -22% 56 20 -20%
16 45 1000/40 -39% 44 1000 -23% 56 40 -17%
20 42 1500/40 -44% 43 1500 -31% 54 40 -21%
28 42 2000/40 -44% 41 2000 -31% 53 40 -20%
* n = number of patients remaining in trial at each time poin

The Lp(a)-lowering effects of combination therapy and NIASPAN (niacin) monotherapy were similar, and both were superior to lovastatin (Table 11). The independent effect of lowering Lp(a) with NIASPAN (niacin) or combination therapy on the risk of coronary and cardiovascular morbidity and mortality has not been determined.

Table 11. Lp(a) median percent change from baseline

Week Combination Tablet of NIASPAN and Lovastatin NIASPAN Lovastatin
  n* Dose (mg/mg) Lp(a) n* Dose (mg) Lp(a) n* Dose (mg) Lp(a)
Baseline 57 - 34 mg/dL 61 - 41 mg/dL 60 - 42 mg/dL
12 47 1000/20 -9% 46 1000 -8% 55 20 +8%
16 45 1000/40 -9% 44 1000 -12% 55 40 +8%
20 42 1500/40 -17% 43 1500 -22% 53 40 +6%
28 42 2000/40 -22% 41 2000 -32% 52 40 0%
* n = number of patients remaining in trial at each time point

NIASPAN (niacin) and Simvastatin Clinical Studies

In a double-blind, randomized, multicenter, multi-national, active-controlled, 24-week study, the lipid effects of a combination tablet of NIASPAN (niacin) and simvastatin were compared to simvastatin 20 mg and 80 mg in 641 patients with type II hyperlipidemia or mixed dyslipidemia. Following a lipid qualification phase, patients were eligible to enter one of two treatment groups. In Group A, patients on simvastatin 20 mg monotherapy, with elevated non-HDL levels and LDL-C levels at goal per the NCEP guidelines, were randomized to one of three treatment arms: combination tablet of NIASPAN (niacin) and simvastatin 1000/20 mg, combination tablet of NIASPAN (niacin) and simvastatin 2000/20 mg, or simvastatin 20 mg. In Group B, patients on simvastatin 40 mg monotherapy, with elevated non-HDL levels per the NCEP guidelines regardless of attainment of LDL-C goals, were randomized to one of three treatment arms: combination tablet of NIASPAN (niacin) and simvastatin 1000/40 mg, combination tablet of NIASPAN (niacin) and simvastatin 2000/40 mg, or simvastatin 80 mg. Therapy was initiated at the 500 mg dose of combination tablet of NIASPAN (niacin) and simvastatin and increased by 500 mg every four weeks. Thus patients were titrated to the 1000 mg dose of combination tablet of NIASPAN (niacin) and simvastatin after four weeks and to the 2000 mg dose of combination tablet of NIASPAN (niacin) and simvastatin after 12 weeks. All patients randomized to simvastatin monotherapy received 50 mg immediate-release niacin daily in an attempt to keep the study from becoming unblinded due to flushing in the combination tablet of NIASPAN (niacin) and simvastatin groups. Patients were instructed to take one 325 mg aspirin or 200 mg ibuprofen 30 minutes prior to taking the double-blind medication to help minimize flushing effects.

In Group A, the primary efficacy analysis was a comparison of the mean percent change in non-HDL levels between the combination tablet of NIASPAN (niacin) and simvastatin 2000/20 mg and simvastatin 20 mg groups, and if statistically significant, then a comparison was conducted between the combination tablet of NIASPAN (niacin) and simvastatin 1000/20 mg and simvastatin 20 mg groups. In Group B, the primary efficacy analysis was a determination of whether the mean percent change in non-HDL in the combination tablet of NIASPAN (niacin) and simvastatin 2000/40 mg group was non-inferior to the mean percent change in the simvastatin 80 mg group, and if so, whether the mean percent change in non-HDL in the combination tablet of NIASPAN (niacin) and simvastatin 1000/40 mg group was non-inferior to the mean percent change in the simvastatin 80 mg group.

In Group A, the non-HDL-C lowering with combination tablet of NIASPAN (niacin) and simvastatin 2000/20 and combination tablet of NIASPAN (niacin) and simvastatin 1000/20 was statistically significantly greater than that achieved with simvastatin 20 mg after 24 weeks (p < 0.05; Table 12). The completion rate after 24 weeks was 72% for the combination tablet of NIASPAN (niacin) and simvastatin arms and 88% for the simvastatin 20 mg arm. In Group B, the non-HDL-C lowering with combination tablet of NIASPAN (niacin) and simvastatin 2000/40 and combination tablet of NIASPAN (niacin) and simvastatin 1000/40 was non-inferior to that achieved with simvastatin 80 mg after 24 weeks (Table 13). The completion rate after 24 weeks was 78% for the combination tablet of NIASPAN (niacin) and simvastatin arms and 80% for the simvastatin 80 mg arm.

The combination tablet of NIASPAN (niacin) and simvastatin was not superior to simvastatin in lowering LDL-C in either Group A or Group B. However, the combination tablet of NIASPAN (niacin) and simvastatin was superior to simvastatin in both groups in lowering TG and raising HDL (Tables 14 and 15).

Table 12. Non-HDL Treatment Response Following 24-Week Treatment Mean Percent Change from Simvastatin 20-mg Treated Baseline

Group A Combination Tablet of NIASPAN and Simvastatin 2000/20 Combination Tablet of NIASPAN and Simvastatin 1000/20 Simvastatin 20  
Week na Dose (mg/mg) Non-HDLb na Dose (mg/mg) Non-HDLb na Dose (mg/mg) Non-HDLb
Baseline 56   163.1 mg/dL 108   164.8 mg/dL 102   163.7 mg/dL
4 52 500/20 -12.9% 86 500/20 -12.8% 91 20 -8.3%
8 46 1000/20 -17.5% 91 1000/20 -15.5% 95 20 -8.3%
12 46 1500/20 -18.9% 90 1000/20 -14.8% 96 20 -6.4%
24 40 2000/20 -19.5% 78 1000/20 -13.6% 90 20 -5.0%
Dropouts by week 24: 28.6%     27.8%     11.8%    
a n=number of subjects with values in the analysis window at each timepoint
b The percent change from baseline is the model-based mean from a repeated measures mixed model with no imputation for missing data from study dropouts.
significant vs. simvastatin 20 mg at the primary endpoint (Week 24),p < 0.05

Table 13. Non-HDL Treatment Response Following 24-Week Treatment Mean Percent Change from Simvastatin 40-mg Treated Baseline

Group B Combination Tablet of NIASPAN and Simvastatin 2000/40 Combination Tablet of NIASPAN and Simvastatin 1000/40 Simvastatin 80
Week na Dose (mg/mg) Non-HDLb na Dose (mg/mg) Non-HDLb na Dose (mg/mg) Non-HDLb
Baseline 98   144.4 mg/dL 111   141.2 mg/dL 113   134.5 mg/dL
4 96 500/40 -6.0% 108 500/40 -5.9% 110 80 -11.3%
8 93 1000/40 -15.5% 100 1000/40 -16.2% 104 80 -13.7%
12 90 1500/40 -18.4% 97 1000/40 -12.6% 100 80 -9.5%
24 80 2000/40 -7.6%c 82 1000/40 -6.7%d 90 80 -6.0%
Dropouts by week 24: 18.4%     26.1%     20.4%    
a n=number of subjects with values in the analysis window at each timepoint
b The percent change from baseline is the model-based mean from a repeated measures mixed model with no imputation for missing data from study dropouts.
c non-inferior to simvastatin 80 arm; 95% confidence interval of mean difference in non-HDL for the combination tablet of NIASPAN (niacin) and simvastatin 2000/40 vs. simvastatin 80 is (-7.7%, 4.5%)
d non-inferior to simvastatin 80 arm; 95% confidence interval of mean difference in non-HDL for combination tablet of NIASPAN (niacin) and simvastatin 1000/40 vs. combination tablet of NIASPAN (niacin) and simvastatin 80 is (-6.6%, 5.3%)

Table 14. Mean Percent Change from Baseline to Week 24 in Lipoprotein Lipid Levels

  Treatment Group A
TREATMENT N LDL-C Total-C HDL-C TGa ApoB
Baseline (mg/dL)* 266 120 207 43 209 102
Simvastatin 20 mg 102 -6.7% -4.5% 7.8% -15.3% -5.6%
Combination Tablet of NIASPAN and Simvastatin 1000/20 108 -11.9% -8.8% 20.7% -26.5% -13.2%
Combination Tablet of NIASPAN and Simvastatin 1000/20 56 -14.3% -11.1% 29.0% -38.0% -18.5%
*either treatment naive or after receiving simvastatin 20 mg
a medians are reported for TG

Table 15. Mean Percent Change from Baseline to Week 24 in Lipoprotein Lipid Levels

  Treatment Group B
TREATMENT N LDL-C Total-C HDL-C TGa ApoB
Baseline (mg/dL)* 322 108 187 47 145 93
Simvastatin 80 mg 113 -11.4% -6.2% 0.1% 0.3% -7.5%
Combination Tablet of NIASPAN and Simvastatin 1000/40 111 -7.1% -3.1% 15.4% -22.8% -7.7%
Combination Tablet of NIASPAN and Simvastatin 1000/40 98 -5.1 -1.6% 24.4% -31.8% -10.5%
* after receiving simvastatin 40 mg
a medians are reported for TG

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

NIASPAN®
(ny-a-span)
(niacin extended-release) tablets

Read this information carefully before you start taking NIASPAN (niacin) and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment.

What is NIASPAN (niacin) ?

NIASPAN (niacin) is a prescription medicine used with diet and exercise to increase the good cholesterol (HDL) and lower the bad cholesterol (LDL) and fats (triglycerides) in your blood.

  • NIASPAN (niacin) can be used by itself or with other cholesterol-lowering medicines
  • NIASPAN (niacin) is also used to lower the risk of heart attack in people who have had a heart attack and have high cholesterol.
  • In people with coronary artery disease and high cholesterol, NIASPAN (niacin) , when used with a bile acid-binding resin (another cholesterol medicine) can slow down or lessen the build-up of plaque (fatty deposits) in your arteries

It is not known if NIASPAN (niacin) is safe and effective in children 16 years of age and under.

Who should not take NIASPAN (niacin) ?

Do not take NIASPAN (niacin) if you have:

  • liver problems
  • a stomach ulcer
  • bleeding problems
  • an allergy to niacin or any of the ingredients in NIASPAN (niacin) . See the end of this leaflet for a complete list of ingredients in NIASPAN (niacin) .

What should I tell my doctor before taking NIASPAN (niacin) ?

Tell your doctor about all of your medical conditions, including if you:

  • have diabetes. Tell your doctor if your blood sugar levels change after you take NIASPAN (niacin) .
  • have gout
  • have kidnev oroblems
  • are pregnant or plan to become pregnant. It is not known if NI ASP AN will harm your unborn baby. Talk to your doctor if you are pregnant or plan to become pregnant while taking NIASPAN (niacin) .
  • are breast-feeding or plan to breast-feed. NIASPAN (niacin) can pass into your breast milk. You and your doctor should decide if you will take NIASPAN (niacin) or breast-feed. You should not do both. Talk to your doctor about the best way to feed your baby if you take NIASPAN (niacin) .

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, herbal supplements or other nutritional supplements containing niacin or nicotinamide. NIASPAN (niacin) and other medicines may affect each other causing side effects. NIASPAN (niacin) may affect the way other medicines work, and other medicines may affect how NIASPAN (niacin) works.

Especially tell your doctor if you take:

  • other medicines to lower cholesterol or triglycerides
  • aspirin
  • blood pressure medicines
  • blood thinner medicines
  • large amounts of alcohol

Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine.

How should I take NIASPAN (niacin) ?

  • Take NIASPAN (niacin) exactly as your doctor tells you to take it.
  • Take NIASPAN (niacin) tablets whole. Do not break, crush or chew NIASPAN (niacin) tablets before swallowing.
  • Take NIASPAN (niacin) 1 time a day at bedtime after a low-fat snack. NIASPAN (niacin) should not be taken on an empty stomach.
  • All forms of niacin are not the same as NIASPAN. Do not switch between forms of niacin without first talking to your doctor as severe liver damage can occur.
  • Do not change your dose or stop taking NIASPAN (niacin) unless your doctor tells you to.
  • If you need to stop taking NIASPAN (niacin) , call your doctor before you start taking NIASPAN (niacin) again. Your doctor may need to lower your dose of NIASPAN (niacin) .
  • If you forget to take a dose of NIASPAN (niacin) , take it as soon as you remember.
  • If you take too much NIASPAN (niacin) , call your doctor right away.
  • Medicines used to lower your cholesterol called bile acid resins, such as colestipol and cholestyramine, should not be taken at the same time of day as NIASPAN (niacin) . You should take NIASPAN (niacin) and the bile acid resin medicine at least 4 to 6 hours apart.
  • Your doctor may do blood tests before you start taking NIASPAN (niacin) and during your treatment. You should see your doctor regularly to check your cholesterol and triglyceride levels and to check for side effects.

What are the possible side effects of NIASPAN (niacin) ?

NIASPAN (niacin) may cause serious side effects, including:

  • unexplained muscle pain, tenderness or weakness
  • severe liver problems. Signs of liver problems include:
    • increased tiredness
    • dark colored urine (tea-colored)
    • loss of appetite
    • light colored stools
    • nausea
    • right upper stomach (abdomen) pain
    • yellowing of your skin or whites of your eye
    • itchy skin
  • high blood sugar level (glucose)

Call your doctor right away if you have any of the side effects listed above. The most common side effects of NIASPAN (niacin) include:

  • flushing
  • rash
  • diarrhea
  • nausea
  • vomiting
  • increased cough

Flushing is the most common side effect of NIASPAN (niacin) . Flushing happens when tiny blood vessels near the surface of the skin (especially on the face, neck, chest and/or back) open wider. Symptoms of flushing may include any or all of the following:

  • warmth,
  • redness,
  • itching,
  • tingling of the skin

Flushing does not always happen. If it does, it is usually within 2 to 4 hours after taking a dose of NIASPAN (niacin) . Flushing may last for a few hours. Flushing is more likely to happen when you first start taking NIASPAN (niacin) or when your dose of NIASPAN (niacin) is increased. Flushing may get better after several weeks.

If you wake up at night because of flushing, get up slowly, especially if you:

  • feel dizzy or faint
  • take blood pressure medicines

To lower your chance of flushing:

  • Ask your doctor if you can take aspirin to help lower the flushing side effect from NIASPAN (niacin) . You can take aspirin (up to the recommended dose of 325 mg) about 30 minutes before you take NIASPAN (niacin) to help lower the flushing side effect.
  • Do not drink hot beverages (including coffee), alcohol, or eat spicy foods around the time you take NIASPAN (niacin) .
  • Take NIASPAN (niacin) with a low-fat snack to lessen upset stomach.

People with high cholesterol and heart disease are at risk for a heart attack. Symptoms of a heart attack may be different from a flushing reaction from NIASPAN (niacin) . The following may be symptoms of a heart attack due to heart disease and not a flushing reaction:

  • chest pain
  • pain in other areas of your upper body such as one or both arms, back, neck, jaw or stomach
  • shortness of breath
  • sweating
  • nausea
  • lightheadedness

The chest pain you have with a heart attack may feel like uncomfortable pressure, squeezing, fullness or pain that lasts more than a few minutes, or that goes away and comes back. Heart attacks may be sudden and intense, but often start slowly, with mild pain or discomfort.

Call your doctor right away if you have any symptoms of a heart attack.

Tell your doctor if you have any side effect that bothers you or does not go away.

These are not all the possible side effects of NIASPAN (niacin) . For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store NIASPAN (niacin) ?

  • Store NIASPAN (niacin) at 68°F to 77°F (20°C to 25°C).

Keep NIASPAN (niacin) and all medicines out of the reach of children.

General information about NIASPAN (niacin)

Medicines are sometimes prescribed for purposes other than those listed in a patient information leaflet. Do not use NIASPAN (niacin) for a condition for which it was not prescribed. Do not give NIASPAN (niacin) to other people, even if they have the same symptoms that you have. It may harm them.

This leaflet summarizes the most important information about NIASPAN (niacin) . If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about NIASPAN (niacin) that is written for health professionals.

For more information, go to www.NIASPAN (niacin) .com or call Abbott Medical Information at 1-800-633-9110.

What are the ingredients in NIASPAN?

Active ingredient: niacin

Inactive Ingredients: hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD& C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

For more information, go to www.NIASPAN (niacin) .com or call Abbott Medical Information at 1-800-633-9110.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

>

PATIENT INFORMATION

NIASPAN®
(ny-a-span)
(niacin extended-release) tablets

Read this information carefully before you start taking NIASPAN (niacin) and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your medical condition or your treatment.

What is NIASPAN (niacin) ?

NIASPAN (niacin) is a prescription medicine used with diet and exercise to increase the good cholesterol (HDL) and lower the bad cholesterol (LDL) and fats (triglycerides) in your blood.

  • NIASPAN (niacin) can be used by itself or with other cholesterol-lowering medicines
  • NIASPAN (niacin) is also used to lower the risk of heart attack in people who have had a heart attack and have high cholesterol.
  • In people with coronary artery disease and high cholesterol, NIASPAN (niacin) , when used with a bile acid-binding resin (another cholesterol medicine) can slow down or lessen the build-up of plaque (fatty deposits) in your arteries

It is not known if NIASPAN (niacin) is safe and effective in children 16 years of age and under.

Who should not take NIASPAN (niacin) ?

Do not take NIASPAN (niacin) if you have:

  • liver problems
  • a stomach ulcer
  • bleeding problems
  • an allergy to niacin or any of the ingredients in NIASPAN (niacin) . See the end of this leaflet for a complete list of ingredients in NIASPAN (niacin) .

What should I tell my doctor before taking NIASPAN (niacin) ?

Tell your doctor about all of your medical conditions, including if you:

  • have diabetes. Tell your doctor if your blood sugar levels change after you take NIASPAN (niacin) .
  • have gout
  • have kidnev oroblems
  • are pregnant or plan to become pregnant. It is not known if NI ASP AN will harm your unborn baby. Talk to your doctor if you are pregnant or plan to become pregnant while taking NIASPAN (niacin) .
  • are breast-feeding or plan to breast-feed. NIASPAN (niacin) can pass into your breast milk. You and your doctor should decide if you will take NIASPAN (niacin) or breast-feed. You should not do both. Talk to your doctor about the best way to feed your baby if you take NIASPAN (niacin) .

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, herbal supplements or other nutritional supplements containing niacin or nicotinamide. NIASPAN (niacin) and other medicines may affect each other causing side effects. NIASPAN (niacin) may affect the way other medicines work, and other medicines may affect how NIASPAN (niacin) works.

Especially tell your doctor if you take:

  • other medicines to lower cholesterol or triglycerides
  • aspirin
  • blood pressure medicines
  • blood thinner medicines
  • large amounts of alcohol

Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine.

How should I take NIASPAN (niacin) ?

  • Take NIASPAN (niacin) exactly as your doctor tells you to take it.
  • Take NIASPAN (niacin) tablets whole. Do not break, crush or chew NIASPAN (niacin) tablets before swallowing.
  • Take NIASPAN (niacin) 1 time a day at bedtime after a low-fat snack. NIASPAN (niacin) should not be taken on an empty stomach.
  • All forms of niacin are not the same as NIASPAN. Do not switch between forms of niacin without first talking to your doctor as severe liver damage can occur.
  • Do not change your dose or stop taking NIASPAN (niacin) unless your doctor tells you to.
  • If you need to stop taking NIASPAN (niacin) , call your doctor before you start taking NIASPAN (niacin) again. Your doctor may need to lower your dose of NIASPAN (niacin) .
  • If you forget to take a dose of NIASPAN (niacin) , take it as soon as you remember.
  • If you take too much NIASPAN (niacin) , call your doctor right away.
  • Medicines used to lower your cholesterol called bile acid resins, such as colestipol and cholestyramine, should not be taken at the same time of day as NIASPAN (niacin) . You should take NIASPAN (niacin) and the bile acid resin medicine at least 4 to 6 hours apart.
  • Your doctor may do blood tests before you start taking NIASPAN (niacin) and during your treatment. You should see your doctor regularly to check your cholesterol and triglyceride levels and to check for side effects.

What are the possible side effects of NIASPAN (niacin) ?

NIASPAN (niacin) may cause serious side effects, including:

  • unexplained muscle pain, tenderness or weakness
  • severe liver problems. Signs of liver problems include:
    • increased tiredness
    • dark colored urine (tea-colored)
    • loss of appetite
    • light colored stools
    • nausea
    • right upper stomach (abdomen) pain
    • yellowing of your skin or whites of your eye
    • itchy skin
  • high blood sugar level (glucose)

Call your doctor right away if you have any of the side effects listed above. The most common side effects of NIASPAN (niacin) include:

  • flushing
  • rash
  • diarrhea
  • nausea
  • vomiting
  • increased cough

Flushing is the most common side effect of NIASPAN (niacin) . Flushing happens when tiny blood vessels near the surface of the skin (especially on the face, neck, chest and/or back) open wider. Symptoms of flushing may include any or all of the following:

  • warmth,
  • redness,
  • itching,
  • tingling of the skin

Flushing does not always happen. If it does, it is usually within 2 to 4 hours after taking a dose of NIASPAN (niacin) . Flushing may last for a few hours. Flushing is more likely to happen when you first start taking NIASPAN (niacin) or when your dose of NIASPAN (niacin) is increased. Flushing may get better after several weeks.

If you wake up at night because of flushing, get up slowly, especially if you:

  • feel dizzy or faint
  • take blood pressure medicines

To lower your chance of flushing:

  • Ask your doctor if you can take aspirin to help lower the flushing side effect from NIASPAN (niacin) . You can take aspirin (up to the recommended dose of 325 mg) about 30 minutes before you take NIASPAN (niacin) to help lower the flushing side effect.
  • Do not drink hot beverages (including coffee), alcohol, or eat spicy foods around the time you take NIASPAN (niacin) .
  • Take NIASPAN (niacin) with a low-fat snack to lessen upset stomach.

People with high cholesterol and heart disease are at risk for a heart attack. Symptoms of a heart attack may be different from a flushing reaction from NIASPAN (niacin) . The following may be symptoms of a heart attack due to heart disease and not a flushing reaction:

  • chest pain
  • pain in other areas of your upper body such as one or both arms, back, neck, jaw or stomach
  • shortness of breath
  • sweating
  • nausea
  • lightheadedness

The chest pain you have with a heart attack may feel like uncomfortable pressure, squeezing, fullness or pain that lasts more than a few minutes, or that goes away and comes back. Heart attacks may be sudden and intense, but often start slowly, with mild pain or discomfort.

Call your doctor right away if you have any symptoms of a heart attack.

Tell your doctor if you have any side effect that bothers you or does not go away.

These are not all the possible side effects of NIASPAN (niacin) . For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store NIASPAN (niacin) ?

  • Store NIASPAN (niacin) at 68°F to 77°F (20°C to 25°C).

Keep NIASPAN (niacin) and all medicines out of the reach of children.

General information about NIASPAN (niacin)

Medicines are sometimes prescribed for purposes other than those listed in a patient information leaflet. Do not use NIASPAN (niacin) for a condition for which it was not prescribed. Do not give NIASPAN (niacin) to other people, even if they have the same symptoms that you have. It may harm them.

This leaflet summarizes the most important information about NIASPAN (niacin) . If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about NIASPAN (niacin) that is written for health professionals.

For more information, go to www.NIASPAN (niacin) .com or call Abbott Medical Information at 1-800-633-9110.

What are the ingredients in NIASPAN?

Active ingredient: niacin

Inactive Ingredients: hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD& C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

For more information, go to www.NIASPAN (niacin) .com or call Abbott Medical Information at 1-800-633-9110.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

NIASPAN®
(niacin) Extended-Release Tablet, Film Coated, Extended Release for Oral Use.

DRUG DESCRIPTION

NIASPAN (niacin tablet, film-coated extended-release), contains niacin, which at therapeutic doses is an antihyperlipidemic agent. Niacin (nicotinic acid, or 3-pyridinecarboxylic acid) is a white, crystalline powder, very soluble in water, with the following structural formula:

NIASPAN®
  (niacin) Structural Formula Illustration

NIASPAN (niacin) is an unscored, medium-orange, film-coated tablet for oral administration and is available in three tablet strengths containing 500, 750, and 1000 mg niacin. NIASPAN (niacin) tablets also contain the inactive ingredients hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD&C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

NIASPAN®
(niacin) Extended-Release Tablet, Film Coated, Extended Release for Oral Use.

DRUG DESCRIPTION

NIASPAN (niacin tablet, film-coated extended-release), contains niacin, which at therapeutic doses is an antihyperlipidemic agent. Niacin (nicotinic acid, or 3-pyridinecarboxylic acid) is a white, crystalline powder, very soluble in water, with the following structural formula:

NIASPAN®
  (niacin) Structural Formula Illustration

NIASPAN (niacin) is an unscored, medium-orange, film-coated tablet for oral administration and is available in three tablet strengths containing 500, 750, and 1000 mg niacin. NIASPAN (niacin) tablets also contain the inactive ingredients hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD&C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

NIASPAN®
(niacin) Extended-Release Tablet, Film Coated, Extended Release for Oral Use.

DRUG DESCRIPTION

NIASPAN (niacin tablet, film-coated extended-release), contains niacin, which at therapeutic doses is an antihyperlipidemic agent. Niacin (nicotinic acid, or 3-pyridinecarboxylic acid) is a white, crystalline powder, very soluble in water, with the following structural formula:

NIASPAN®
  (niacin) Structural Formula Illustration

NIASPAN (niacin) is an unscored, medium-orange, film-coated tablet for oral administration and is available in three tablet strengths containing 500, 750, and 1000 mg niacin. NIASPAN (niacin) tablets also contain the inactive ingredients hypromellose, povidone, stearic acid, and polyethylene glycol, and the following coloring agents: FD&C yellow #6/sunset yellow FCF Aluminum Lake, synthetic red and yellow iron oxides, and titanium dioxide.

Last reviewed on RxList: 12/13/2010
This monograph has been modified to include the generic and brand name in many instances.

Niaspan Patient Information Including Side Effects

Brand Names: B-3-50, B3-500-Gr, Niacin SR, Niacor, Niaspan ER, Slo-Niacin

Generic Name: niacin (nicotinic acid) (Pronunciation: NYE a sin (NIK oh TIN ik AS id))

What is niacin (Niaspan)?

Niacin, also called nicotinic acid, is a B vitamin (vitamin B3). It occurs naturally in plants and animals, and is also added to many foods as a vitamin supplement. Niacin is also present in many multiple vitamins and nutritional supplements.

Niacin is used to treat and prevent a lack of natural niacin in the body, and to lower cholesterol and triglycerides (types of fat) in the blood. It is also used to lower the risk of heart attack in people with high cholesterol who have already had a heart attack. Niacin is sometimes used to treat coronary artery disease (also called atherosclerosis).

Niacin may also be used for purposes other than those listed in this medication guide.

Niacin SR 125 mg-URL

brown/clear

Niaspan 500 mg

oblong, white, imprinted with KOS, 500

Niaspan ER 1000 mg

oblong, white, imprinted with 1000, KOS

Niaspan ER 750 mg

oblong, white, imprinted with 750, KOS

What are the possible side effects of niacin ?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • feeling light-headed, fainting;
  • fast, pounding, or uneven heart beats;
  • feeling short of breath;
  • swelling;
  • jaundice (yellowing of your skin or eyes); or
  • muscle pain, tenderness, or weakness with fever or flu symptoms and dark colored urine.

If you are diabetic, tell your doctor about any changes in your blood sugar levels.

Less serious side effects of niacin include:

  • mild dizziness;
  • warmth, redness, or tingly feeling under your skin;
  • itching, dry skin;
  • sweating or chills;
  • nausea, diarrhea, belching, gas;
  • muscle pain, leg cramps; or
  • sleep problems (insomnia).

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

Read the Niaspan (niacin) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about niacin?

Do not take this medication if you are allergic to niacin, or if you have severe liver disease, a stomach ulcer, or active bleeding.

Niacin can cause certain side effects, such as flushing (warmth, itching, redness, or tingly feeling under your skin). These effects can be made worse if you drink alcohol or hot beverages shortly after you take niacin. These effects should disappear over time as you keep taking the medication.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Avoid taking colestipol (Colestid) or cholestyramine (Locholest, Prevalite, Questran) at the same time you take niacin. If you take either of these other medications, take them at least 4 to 6 hours before or after you take niacin.

Niacin is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications. Follow your diet, medication, and exercise routines very closely.

Side Effects Centers

Niaspan Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking niacin ?

Do not take this medication if you are allergic to niacin, or if you have severe liver disease, a stomach ulcer, or active bleeding.

Before taking niacin, tell your doctor if you are allergic to any drugs, or if you have:

  • liver or kidney disease;
  • heart disease or uncontrolled angina (chest pain);
  • a stomach ulcer;
  • diabetes;
  • gout; or
  • a muscle disorder such as myasthenia gravis.

If you have any of these conditions, you may not be able to use niacin, or you may need dosage adjustments or special tests during treatment.

FDA pregnancy category C. Niacin may be harmful to an unborn baby when the medication is taken at doses to treat high cholesterol or other conditions. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Niacin can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take niacin ?

Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.

Niacin is sometimes taken at bedtime with a low-fat snack. Follow your doctor's instructions.

Niacin can cause certain side effects, such as flushing (warmth, itching, redness, or tingly feeling under your skin). These effects can be made worse if you drink alcohol or hot beverages shortly after you take niacin. These effects should disappear over time as you keep taking the medication.

Take niacin with a full glass of cold or cool water. Taking the medication with a hot drink may increase your risk of side effects such as flushing.

Do not crush, chew, break, or open an extended-release tablet or capsule. Swallow the pill whole. It is specially made to release medicine slowly in the body. Breaking or opening the pill would cause too much of the drug to be released at one time.

Niacin extended-release tablets and capsules contain higher strengths of the medicine than the regular niacin tablets. Take only the dose that is correct for the type of niacin tablet or capsule you are using.

Niacin can cause you to have unusual results with certain medical tests (urine tests). Tell any doctor who treats you that you are using niacin.

If you stop taking niacin for any length of time, talk with your doctor before starting the medication again. You may need to restart the medication at a lower dose.

Niacin is only part of a complete program of treatment that may also include diet, exercise, weight control, and other medications. Follow your diet, medication, and exercise routines very closely.

To be sure this medication is not causing harmful effects, your blood will need to be tested on a regular basis. Your kidney or liver function may also need to be tested. Do not miss any scheduled appointments.

Store niacin at room temperature away from moisture and heat.

Side Effects Centers

Niaspan Patient Information including If I Miss a Dose

What happens if I miss a dose?

Take the missed dose as soon as you remember. Be sure to take the missed dose with food if you normally take your niacin dose with a meal or snack.

If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include nausea, dizziness, itching, vomiting, upset stomach, and flushing.

What should I avoid while taking niacin ?

Avoid drinking hot beverages shortly after taking niacin. Hot drinks can worsen niacin's flushing effect (warmth, itching, redness, or tingly feeling under your skin).

Avoid drinking alcohol while taking niacin. Alcohol may increase your risk of liver damage, and can also worsen the flushing effects of niacin.

Avoid taking colestipol (Colestid) or cholestyramine (Locholest, Prevalite, Questran) at the same time you take niacin. If you take either of these other medications, take them at least 4 to 6 hours before or after you take niacin.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

What other drugs will affect niacin ?

Tell your doctor about all other cholesterol-lowering drugs you are taking with niacin, especially atorvastatin (Lipitor), fluvastatin (Lescol), lovastatin (Mevacor), pravastatin (Pravachol), or simvastatin (Zocor).

Before taking niacin, tell your doctor if you are also using any of the following drugs:

  • a blood thinner such as warfarin (Coumadin);
  • multivitamins or mineral supplements that contain niacin;
  • blood pressure or heart medications such as amlodipine (Norvasc), diltiazem (Tiazac, Cartia, Cardizem), felodipine (Plendil), nicardipine (Cardene), nifedipine (Procardia, Adalat), nimodipine (Nimotop), nisoldipine (Sular), or verapamil (Calan, Covera, Isoptin, Verelan); or
  • heart medications such as doxazosin (Cardura), isosorbide (Dilatrate, Imdur, Isordil, Monoket, Sorbitrate), nitroglycerin (Nitro-Bid, Nitro-Dur, Nitrostat), prazosin (Minipress), or terazosin (Hytrin).

This list is not complete and there may be other drugs that can interact with niacin. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about niacin.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 8.03. Revision date: 12/15/2010.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

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Side Effects Centers

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