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Pronunciation |
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(NYE
a sin) |

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

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Generic
Available |
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Yes |

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Synonyms |
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Nicotinic Acid; Vitamin B3 |

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Pharmacological Index |
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Antilipemic Agent (Miscellaneous); Vitamin, Water Soluble |

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

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Pregnancy Risk
Factor |
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A (C if used in doses greater than RDA suggested doses) |

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

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Warnings/Precautions |
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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. |

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Adverse
Reactions |
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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 |

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Overdosage/Toxicology |
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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 |

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Drug
Interactions |
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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. |

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

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Pharmacodynamics/Kinetics |
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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 |

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Usual Dosage |
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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 |

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Dietary
Considerations |
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Should be administered after meals |

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

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

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Cardiovascular
Considerations |
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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. |

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Mental Health: Effects
on Mental Status |
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May rarely cause dizziness |

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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |

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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |

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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |

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Patient
Information |
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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 |

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

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Dosage Forms |
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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 |

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References |
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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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