Niacin (Nicotinic Acid; Vitamin B3)

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Bulgaria: Niaspan; France: Niaspan; Germany: Niaspan; Greece: Niacin; Hungary: Acidum Nicotinicum; Ireland: Niaspan; Portugal: Niaspan; Romania: Niaspan; Sweden: Niaspan; UK: Niaspan.

North America

Canada: Niacin, Niaspan, Niodan; USA: Niacor, Niaspan.

Latin America

Argentina: Niaspan; Brazil: Acinic-Biolab Sanus, Metri; Mexico: Hipocol, Niaspan.

Asia

Japan: Nicortinic Acid, Nyclin.

Drug combinations

Niacin and Laropiprant

Niacin and Lovastatin

Niacin and Simvastatin

Other Niacin combinations: Ascorbic Acid (Vitamin C); Beta-Carotene; Biotin (Vitamin B~7~); Calcium Phosphate; Cholecalciferol (Vitamin D~3~); Chromium; Coenzyme Q~10~; Copper Sulfate; Cyanocobalamin (Vitamin B~12~); Cystine; Dexamethasone; Ergocalciferol (Vitamin D~2~); Ferrous Fumarate; Folic Acid (Vitamin B~9~); Ginkgo biloba; Ginseng; Inositol; Iron; L-Arginine; L-Carnitine; Magnesium Oxide; Manganese; Methionine; Molybdenum; Niacinamide; Pantothenic Acid (Vitamin B~5~); Phosphorus; Phytonadione (Vitamin K~1~); Pollen; Potassium; Pyridoxine (Vitamin B~6~); Retinol (Vitamin A); Riboflavin (Vitamin B~2~); Rutoside; Saccharomyces cerevisiae; Selenium; Sodium; Soy Protein; Taurine; Thiamine (Vitamin B~1~); Tocopherol (Vitamin E); Zinc; Zinc Oxide

Chemistry

Niacin: C~6~H~5~NO~2~. Mw: 123.11. (1) 3-Pyridinecarboxylic acid; (2) Nicotinic acid. CAS-59-67-6.

Pharmacologic Category

Antilipemic Agents, Miscellaneous. Vitamins; Vitamin B Complex. (ATC-Code: C04AC01; C10AD02).

Mechanism of action

Component of two coenzymes necessary for tissue respiration, lipid metabolism, and glycogenolysis. Inhibits synthesis of very low density lipoproteins (VLDL) and low density lipoproteins (LDL). May also increase rate of chylomicron triglyceride removal from plasma.

Therapeutic use

Adjunctive treatment of dyslipidemias (types II~a~ and II~b~ or primary hypercholesterolemia) to lower risk of recurrent myocardial infarction and/or slow progression of coronary artery disease. Treatment of hypertriglyceridemia in risk of pancreatitis. Treatment of peripheral vascular disease and circulatory disorders. Treatment of pellagra. Dietary supplement.

Pregnancy and lactiation implications

If a woman becomes pregnant while receiving niacin for primary hypercholesterolemia, niacin should be discontinued. If a woman becomes pregnant while receiving niacin for hypertriglyceridemia, benefits and risks of continuing niacin should be assessed. Enters breast milk.

Unlabeled use

Contraindications

Hypersensitivity to niacin, niacinamide, or any component of the formulation. Active hepatic disease or significant or unexplained hepatic dysfunction. Active peptic ulcer. Arterial hemorrhage.

Warnings and precautions

Flushing is common. Cases of severe hepatotoxicity, including fulminant hepatic necrosis, occurred when immediate release (crystalline) niacin products were substituted with sustained-release (modified release, timed-release) niacin products at equivalent doses. Use with caution in unstable angina or myocardial infarction. Use niacin with caution in diabetes mellitus (niacin may increase fasting blood glucose). Use with caution in active gallbladder disease (can be exacerbated). Use may be associated with hyperuricemia. Use with caution in gout, and in past history of hepatic impairment. Contraindicated with active liver disease or unexplained transaminase elevation. Use with caution in renal impairment, and in patients taking anticoagulants (may slightly increase prothrombin time). Rare cases of rhabdomyolysis occurred during concomitant use with HMG-CoA reductase inhibitors. Use with caution in heavy ethanol users. Formulations of niacin (regular release vs extended release) not interchangeable (bioavailability varies).

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