Niacin
( B 3 ; Nicotinic Acid ) Pronouncation: (NYE-uh-sin)Class: Water-soluble vitamin
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 mg
Pharmacology
Feedback for Niacin (B3; Nicotinic Acid)
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At pharmacologic doses, it reduces total cholesterol, LDL cholesterol, and triglycerides, while increasing HDL cholesterol. Also causes peripheral vasodilation, especially cutaneous vessels.
Pharmacokinetics
Absorption
Niacin is rapidly and extensively absorbed from GI tract. T max is 30 to 60 min, and C max is 15 to 30 mcg/mL.
Metabolism
Rapid and extensive first-pass metabolism of niacin in liver.
Elimination
Niacin is eliminated in urine (approximately 88% as unchanged and nicotinuric acid). Plasma t ½ is 20 to 45 min.
Special Populations
GenderSteady-state plasma concentrations and metabolites are generally higher in women.
Liver diseaseExtended-release tablets are contraindicated in patients with active liver disease.
Indications and Usage
Dietary supplement for prevention and treatment of niacin deficiency; adjunct to diet for the reduction of elevated total and LDL levels 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; 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 in patients taking lovastatin who require further triglyceride-lowering or HDL-raising 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; 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.
Contraindications
Significant liver disease; active peptic ulcer; severe hypotension; arterial hemorrhaging.
Dosage and Administration
Dietary SupplementationAdults
PO RDA is 15 to 20 mg/day for adult men and 13 to 15 mg/day for adult women. Increase niacin to 17 to 20 mg/day during pregnancy and lactation.
ChildrenPO RDA is 5 to 13 mg/day.
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 releasePO 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).
General Advice
- Administer with food or milk to reduce flushing. Do not provide hot liquids with or immediately after administration.
- Administer extended-release tablets ( Niaspan ) at bedtime, after a low-fat snack.
- If ordered, administer non-enteric coated aspirin or NSAID (eg, ibuprofen) 30 min before niacin dose to help ameliorate distressing or persistent flushing.
- Advise patient to swallow modified-release (eg, timed-release, controlled-release, sustained-release, extended-release) capsule whole and not to crush, chew, or open the capsule.
- Advise patient to swallow modified-release (eg, timed-release, controlled-release, sustained-release, extended-release) tablet whole and not to crush, chew, or break the tablet. Scored tablets may be split on the score line but the half-tablet should be swallowed whole.
Storage/Stability
Store tablets and capsules at controlled room temperature (59° to 86°F). Store extended-release tablets ( Niaspan ) between 68° and 77°F.
Drug Interactions
Alcohol, hot beveragesMay increase flushing or pruritus and should be avoided near time of niacin administration.
Antihypertensive therapyEffects of ganglionic-blocking agents and vasoactive drugs may be potentiated, resulting in postural hypotension.
AspirinMetabolic 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 inhibitorsIncreased risk of myopathy and rhabdomyolysis.
Laboratory Test Interactions
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.
Adverse Reactions
Cardiovascular
Atrial fibrillation or other cardiac arrhythmias; hypotension; orthostasis; palpitations; syncope; tachycardia.
CNS
Headache (11%); asthenia; dizziness; insomnia; migraine; syncope.
Dermatologic
Pruritus (6%); rash (5%); burning or tingling sensation; dry skin; flushing; hyperpigmentation (acanthosis nigricans); maculopapular rash; sweating; urticaria.
EENT
Rhinitis (5%); blurred vision; toxic amblyopia; xerostomia.
GI
Diarrhea (11%); nausea (10%); vomiting (8%); dyspepsia (6%); abdominal pain (5%); activation of peptic ulcer; bloating; flatulence; heartburn; hunger.
Hepatic
Abnormal LFT results; jaundice; liver damage.
Metabolic
Decreased glucose tolerance; gout; hyperglycemia; hyperuricemia.
Musculoskeletal
Myalgia.
Miscellaneous
Pain (5%); asthenia; chills; cystoid macular edema; edema.
Precautions
MonitorAssess 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 patient when drug is started or dose is changed. Assess fasting blood glucose before starting therapy and periodically thereafter during therapy in patient with risk factors for diabetes mellitus (eg, obesity, family history of diabetes). Assess 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. |
Pregnancy
Category A ; ( Category C if used in doses above RDA.)
Lactation
Excreted in breast milk.
Children
Safety and efficacy not established for doses exceeding nutritional requirements. Extended-release preparations not recommended for children.
Hepatic Function
Use with caution in patients who consume substantial quantities of alcohol or who have a past history of liver disease.
Special Risk Patients
Use drug with caution when administering to patients with gallbladder disease, history of jaundice, diabetes mellitus on anticoagulant therapy, renal function impairment, gout, peptic ulcer, or allergy. Also, patients allergic to aspirin may be allergic to this product.
Flushing
Commonly appears with oral therapy. Aspirin 30 min before niacin or a non-steroidal antiinflammatory drug (ibuprofen) may decrease flushing.
Heart disease
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.
Product substitution
Do not substitute equivalent doses of Niaspan 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.
Patient Information
- Explain LDL-C and triglyceride treatment goals.
- Advise patient that dose of medication may change, based on results of cholesterol and triglyceride blood tests, in an effort to reach LDL-C and triglyceride treatment goals.
- Advise patient using extended-release tablets ( Niaspan ) to take prescribed dose once daily at bedtime after a low-fat snack.
- Advise patient using modified-release (eg, timed-release, sustained-release) capsules to swallow capsules whole and not to crush, chew, or open the capsule.
- Advise patient using modified-release (eg, timed-release, controlled-release, sustained-release, extended-release) tablets to swallow tablets whole and not to crush, chew, or break the tablet. Advise patient that scored tablets may be split on the score line but to swallow the half-tablet whole.
- Caution patient that taking this medication on an empty stomach increases the risk of flushing, itching, and stomach distress.
- Caution patient that drinking alcohol or hot drinks around the time of medication administration will increase the risk of flushing.
- Caution patient not to change the dose or stop taking unless advised by health care provider.
- Caution patient that if medication is not taken for an extended length of time (eg, more than 7 days) to contact health care provider before restarting the medication. Advise patient that re-titration of the dose of medication may be required.
- Emphasize to patient importance of other modalities on cholesterol control: dietary changes (reduced saturated fat intake, increase soluble fiber intake), weight control, regular exercise, and smoking cessation.
- Advise patient that drug helps control, but not does cure, cholesterol or triglyceride abnormality and to continue taking drug as prescribed when LDL-C and triglyceride treatment goals have been met.
- Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
- Advise patient that flushing, itching, tingling, headache, and a sensation of warmth, especially of the face and upper body, which may last for several hours after dosing, are common adverse reactions of therapy when starting, increasing the dose, or changing the brand of niacin. Advise patient that these symptoms, if they occur, usually go away after several weeks of consistent use. Advise patient to notify health care provider if these effects occur and do not improve or become intolerable. Advise patient that taking non-enteric coated aspirin or an NSAID (eg, ibuprofen) 30 min before niacin dose may ameliorate this problem and to discuss this potential therapy with health care provider before starting.
- Caution patient that if flushing awakens them during the night to rise slowly to reduce the risk of dizziness or fainting.
- Advise patient who is also taking a bile acid sequestrant (eg, cholestyramine) to take the niacin/lovastatin at least 2 h before or 4 h or more after the sequestrant.
- Instruct patient to immediately notify health care provider if they experience any unexplained muscle pain, tenderness and/or weakness, unquenchable thirst, frequent urination, frequent episodes of dizziness, persistent flu-like symptoms (eg, nausea, vomiting, loss of appetite, generally not well feeling), dark urine, or if they note any other unusual unexplained feelings (eg, sudden onset of joint pain).
- Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
- Advise women of childbearing potential to use effective contraception during treatment with niacin/lovastatin.
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Hyperlipoproteinemia, Hyperlipoproteinemia Type IV (Elevated VLDL), Hyperlipoproteinemia Type V (Elevated Chylomicrons + VLDL), Pellagra, Niacin (Vitamin B3) Deficiency
