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Niacin
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Test Interactions
Cardiovascular Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(NYE a sin)

U.S. Brand Names
Niaspan®; Nicobid®[OTC]; Nicolar®[OTC]; Nicotinex [OTC]; Slo-Niacin®[OTC]

Generic Available

Yes


Synonyms
Nicotinic Acid; Vitamin B3

Pharmacological Index

Antilipemic Agent (Miscellaneous); Vitamin, Water Soluble


Use

Adjunctive treatment of hyperlipidemias; peripheral vascular disease and circulatory disorders; treatment of pellagra; dietary supplement


Pregnancy Risk Factor

A (C if used in doses greater than RDA suggested doses)


Contraindications

Hypersensitivity to niacin or niacinamide; liver disease; active peptic ulcer; severe hypotension; arterial hemorrhage


Warnings/Precautions

Use caution in heavy ethanol users, unstable angina or CAD (risk of arrhythmias at high doses), diabetes (interfere with glucose control), renal disease, active gallbladder disease (can exacerbate), gout, or allergies. Avoid large pharmacological amounts in patients with a history of liver disease. Flushing is common and can be attenuated with a gradual increase in dose. Monitor liver function tests.


Adverse Reactions

1% to 10%:

Cardiovascular: Generalized flushing

Central nervous system: Headache

Gastrointestinal: Bloating, flatulence, nausea

Hepatic: Abnormalities of hepatic function tests, jaundice

Neuromuscular & skeletal: Paresthesia in extremities

Miscellaneous: Increased sebaceous gland activity, sensation of warmth

<1% (Limited to important or life-threatening symptoms): Tachycardia, syncope, vasovagal attacks, dizziness, rash, liver damage (dose-related incidence), blurred vision, wheezing


Overdosage/Toxicology

Symptoms of acute overdose include flushing, GI distress, pruritus; chronic excessive use has been associated with hepatitis

Antihistamines may relieve niacin-induced histamine release; otherwise treatment is symptomatic


Drug Interactions

Oral hypoglycemics: Effect may be decreased by niacin.

Sulfinpyrazone and probenecid; niacin may inhibit uricosuric effects.

Aspirin decreases adverse effect of flushing.

Lovastatin (and possibly other HMG CoA reductase inhibitors): Increased risk of toxicity (myopathy).

Adrenergic blocking agents additive vasodilating effect and postural hypotension.


Mechanism of Action

Component of two coenzymes which is necessary for tissue respiration, lipid metabolism, and glycogenolysis; inhibits the synthesis of very low density lipoproteins


Pharmacodynamics/Kinetics

Peak serum concentrations: Oral: Within 45 minutes

Metabolism: Depending upon the dose, niacin converts to niacinamide; following this conversion, niacinamide is 30% metabolized in the liver

Half-life: 45 minutes

Elimination: In urine; with larger doses, a greater percentage is excreted unchanged in urine


Usual Dosage

Administer I.M., I.V., or S.C. only if oral route is unavailable and use only for vitamin deficiencies (not for hyperlipidemia)

Pellagra: 50-100 mg/dose 3 times/day

Recommended daily allowances:

0-0.5 years: 5 mg/day

0.5-1 year: 6 mg/day

1-3 years: 9 mg/day

4-6 years: 12 mg/day

7-10 years: 13 mg/day

Children and Adolescents: Oral: Recommended daily allowances:

Male:

11-14 years: 17 mg/day

15-18 years: 20 mg/day

19-24 years: 19 mg/day

Female: 11-24 years: 15 mg/day

Adults: Oral:

Recommended daily allowances:

Male: 25-50 years: 19 mg/day; >51 years: 15 mg/day

Female: 25-50 years: 15 mg/day; >51 years: 13 mg/day

Hyperlipidemia: 1.5-6 g/day in 3 divided doses with or after meals using a dosage titration schedule

Pellagra: 50-100 mg 3-4 times/day, maximum: 500 mg/day

Niacin deficiency: 10-20 mg/day, maximum: 100 mg/day


Dietary Considerations

Should be administered after meals


Monitoring Parameters

Blood glucose, liver function tests (with large doses or prolonged therapy), serum cholesterol


Test Interactions

False elevations in some fluorometric determinations of urinary catecholamines; false-positive urine glucose (Benedict's reagent)


Cardiovascular Considerations

Niacin is a very effective agent in the treatment of hyperlipidemia. Niacin lowers LDL cholesterol and triglycerides and increases HDL cholesterol. An important problem with niacin is the flushing and the need for frequent daily dosing. Adverse effects of niacin (itching, tingling, headache) may be attenuated by increasing the dose slowly or by taking aspirin or an NSAID 30 minutes to 1 hour prior to niacin dosing. Sustained release niacin may decrease the incidence of flushing and circumvent the need for multiple daily dosing. Sustained release niacin may not increase HDL cholesterol or decrease triglycerides as well as immediate release niacin.


Mental Health: Effects on Mental Status

May rarely cause dizziness


Mental Health: Effects on Psychiatric Treatment

None reported


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

May experience transient cutaneous flushing and sensation of warmth, especially of face and upper body; itching or tingling, and headache may occur, these adverse effects may be decreased by increasing the dose slowly or by taking aspirin or a NSAID 30 minutes to 1 hour prior to taking niacin; may cause GI upset, take with food; if dizziness occurs, avoid sudden changes in posture; report any persistent nausea, vomiting, abdominal pain, dark urine, or pale stools to the physician; do not crush sustained release capsule


Nursing Implications

Monitor closely for signs of hepatotoxicity and myositis; avoid sudden changes in posture


Dosage Forms

Capsule, timed release: 125 mg, 250 mg, 300 mg, 400 mg, 500 mg

Elixir: 50 mg/5 mL (473 mL, 4000 mL)

Injection: 100 mg/mL (30 mL)

Tablet: 25 mg, 50 mg, 100 mg, 250 mg, 500 mg

Extended release: 500 mg, 750 mg, 1000 mg

Timed release: 150 mg, 250 mg, 500 mg, 750 mg


References

Brown WV, "Niacin for Lipid Disorders. Indications, Effectiveness, and Safety," Postgrad Med, 1995, 98(2):185-9, 192-3.

Colletti RB, Neufeld EJ, Roff NK, et al, "Niacin Treatment of Hypercholesterolemia in Children." Pediatrics, 1993, 92(1):78-82.

Dalton TA and Berry RS, "Hepatotoxicity Associated With Sustained-Release Niacin," Am J Med, 1992, 93(1):102-4.

Dunn RT, Ford MA, Rindone JP, et al, "Low-Dose Aspirin and Ibuprofen Reduce the Cutaneous Reactions Following Niacin Administration," Am J Therapeut, 1995, 2:478-80.

Lasagna L, "Over-the-Counter Niacin," JAMA, 1994, 271(9):709-10.

McKenney JM, Proctor JD, Harris S, et al, "A Comparison of the Efficacy and Toxic Effects of Sustained- vs Immediate-Release Niacin in Hypercholesterolemic Patients," JAMA, 1994, 271(9):672-7.

Schwab RA and Bachhuber BH, "Delirium and Lactic Acidosis Caused by Ethanol and Niacin Coingestion," Am J Emerg Med, 1991, 9(4):363-5.

"Summary of the Second Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel II)," JAMA, 1993, 269(23):3015-23.


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