Trade Names:Niacin- Tablets 50 mg- Tablets 100 mg- Tablets 250 mg- Tablets 500 mg
Trade Names:Niacin- Capsules, controlled-release 125 mg- Capsules, controlled-release 250 mg- Capsules, controlled-release 400 mg- Capsules, controlled-release 500 mg
Trade Names:Niacin- Tablets, controlled-release 1,000 mg
Trade Names:Niacor- Tablets 500 mg
Trade Names:Niaspan- Tablets, extended-release 500 mg- Tablets, extended-release 750 mg- Tablets, extended-release 1,000 mg
Trade Names:Slo-Niacin- Tablets, controlled-release 250 mg- Tablets, controlled-release 500 mg- Tablets, controlled-release 750 mgNi-odan Extended Release Formula (Canada)
At pharmacologic doses, reduces total cholesterol, LDL cholesterol, apolipoprotein B (ApoB), and triglycerides, while increasing HDL cholesterol. Also causes peripheral vasodilation, especially cutaneous vessels.
Niacin is rapidly and extensively absorbed from GI tract (60% to 76% of dose). T max is 30 to 60 min, and C max is 15 to 30 mcg/mL.
Rapid and extensive first-pass metabolism of niacin in liver.
Niacin is eliminated in urine (approximately 60% to 88% as unchanged and metabolic). Plasma t ½ is 20 to 45 min.
Steady-state plasma concentrations and metabolites are generally higher in women.Liver disease
Extended-release tablets are contraindicated in patients with active liver disease.Renal function impairment
No data available; however, use with caution.
Dietary supplement for prevention and treatment of niacin deficiency; adjunct to diet for the reduction of elevated total, LDL, ApoB, and triglyceride levels, and to decrease HDL in patients with primary hypercholesterolemia and mixed dyslipidemia when the response to diet and other nonpharmacologic measures alone has been inadequate; to reduce the risk of recurrent nonfatal MI in patients with history of MI and hypercholesterolemia ( Niaspan only); Niaspan in combination with bile acid–binding resin to slow progression or promote regression of atherosclerotic disease in patients with history of coronary artery disease; Niaspan in combination with lovastatin for the treatment of primary cholesterolemia and mixed dyslipidemia in patients taking lovastatin who require further triglyceride lowering or HDL raising and who may benefit from having niacin added to their regimen or in patients receiving niacin who require further LDL lowering who may benefit from having lovastatin added to their regimen; Niaspan in combination with a bile acid–binding resin as an adjunct to diet for adult patients with primary hypercholesterolemia (type ΙΙa); adjunctive therapy for treatment of adult patients with very high serum triglyceride levels (types IV and V hyperlipidemia) who present a risk of pancreatitis.
Significant or unexplained liver disease; active peptic ulcer; arterial hemorrhaging; hypersensitivity to niacin or any component of the product.
PO RDA: 16 mg/day for adult men. 14 mg/day for adult women. 18 mg/day during pregnancy. 17 mg/day during lactation.Children
PO RDA: 2 mg/day for infants up to 6 months of age. 4 mg/day for infants 7 to 12 months of age. 6 mg/day for children 1 to 3 yr of age. 8 mg/day for children 4 to 8 yr of age. 12 mg/day for children 9 to 13 yr of age. 16 mg/day for adolescents 14 to 18 yr of age.HyperlipidemiaAdults Extended-release
PO 500 mg at bedtime for 1 to 4 wk, then 1,000 mg at bedtime during wk 5 to 8. If response is inadequate and patient tolerates dose, the dose may be increased by no more than 500 mg in a 4-wk period (max, 2,000 mg/day). If lipid response is insufficient, or if a higher dose is not well tolerated, some patients may benefit from combination therapy with a bile acid–binding resin or an HMG-CoA reductase inhibitor.Immediate-release ( Niacor )
PO Initiate therapy at 250 mg after evening meal. The frequency of dose and total daily dose can be increased every 4 to 7 days until a dose of 1.5 to 2 g/day (in divided doses) is reached. If hyperlipidemia is not adequately controlled after 2 mo, increase dosage at 2- to 4-wk intervals to 1 g 3 times daily (max, 6 g/day).
Store at 59° to 86°F. Store Niaspan between 68° and 77°F.
May increase flushing or pruritus and should be avoided near time of niacin administration.Antihypertensive therapy
Effects of ganglionic-blocking agents and vasoactive drugs may be potentiated, resulting in postural hypotension.Aspirin
Metabolic Cl of nicotinic acid may be decreased.Bile acid sequestrants (eg, cholestyramine, colestipol)
Because niacin may bind to bile acid sequestrants, separate the administration times by as much as possible, allowing at least 4 to 6 h between ingestion of bile acid–binding resins and niacin administration.HMG-CoA reductase inhibitors
Increased risk of myopathy and rhabdomyolysis.
May produce fluorescent substances, which may cause false elevation in some fluorometric measurements of urinary catecholamines. May produce false-positive reaction with cupric sulfate solution used for urinary glucose determination.
Atrial fibrillation or other cardiac arrhythmias; hypotension; orthostasis; palpitations; syncope; tachycardia.
Headache (11%); dizziness; insomnia; migraine; nervousness; paresthesia; syncope.
Pruritus (6%); rash (5%); acanthosis nigricans; dry skin; flushing; hyperpigmentation; maculopapular rash; sweating; urticaria.
Cystoid macular edema; rhinitis; toxic amblyopia.
Diarrhea (11%); nausea (10%); vomiting (8%); dyspepsia (6%); abdominal pain (5%); activation of peptic ulcer; eructation; flatulence; peptic ulceration.
Prolongation in PT, reductions in platelet count.
Abnormal LFTs; jaundice; liver damage.
Anaphylaxis; angioedema; laryngismus, larynx edema, tongue edema; vesiculobullous rash.
Elevations in amylase, fasting glucose, LDH, total bilirubin, and uric acid; reductions in phosphorus.
Decreased glucose tolerance; gout; hyperuricemia.
Leg cramps; myalgia; myasthenia.
Pain (5%); asthenia; chills; edema; face edema, peripheral edema.
Monitor creatine phosphokinase and potassium in patients taking niacin and HMG-CoA reductase inhibitors.
Assess uric acid level before starting therapy. If patient has gout or a history of gouty arthritis, periodically evaluate uric acid during long-term treatment. Monitor blood sugar in diabetic patients when drug is started or dose is changed.
Assess fasting blood glucose before starting therapy and periodically thereafter during therapy in patients with risk factors for diabetes mellitus (eg, obesity, family history of diabetes). Assess transaminase levels before starting therapy, every 6 to 12 wk for the first 12 months of therapy, and periodically (eg, every 6 months) thereafter, as clinically indicated.
Closely monitor PT and platelet counts in patients undergoing surgery and/or receiving oral anticoagulant therapy; periodically monitor phosphorus levels in patients at risk of hypophosphatemia.
Category A ( Category C if used in doses above RDA).
Excreted in breast milk.
Safety and efficacy not established for doses exceeding nutritional requirements. Extended-release preparations not recommended for children.
Use with caution in patients who consume substantial quantities of alcohol or who have a history of liver disease.
Use drug with caution when administering to patients with gallbladder disease, hepatobiliary disease, arterial bleeding, glaucoma, history of jaundice, diabetes mellitus, anticoagulant therapy, renal function impairment, gout, or peptic ulcer.
Use with caution in patients with unstable angina or who are in the acute phase of an MI.
Commonly appears with oral therapy. Aspirin 30 min before niacin or an NSAID (eg, ibuprofen) may decrease flushing.
People who have recurrent chest pain (angina) or who recently suffered a heart attack should take niacin only under the supervision of a health care provider.
Severe hepatic toxicity has been reported in patients substituting sustained-release niacin for immediate-release niacin at equivalent doses.
Do not substitute equivalent doses for sustained-release niacin preparations or immediate-release niacin. Severe hepatic toxicity, including fulminant hepatic necrosis, has occurred in patients who have substituted sustained-release niacin for immediate-release niacin at equivalent doses.
May occur when used in combination with HMG-CoA reductase inhibitors.
No information available.
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