Niacin

What is Niacin?

• Niacin, also known as nicotinic acid and vitamin B3, is a water soluble, essential B vitamin which, when given in high doses, is effective in lowering low density lipoprotein (LDL) cholesterol and raising high density lipoprotein (HDL) cholesterol, which makes this agent of unique value in the therapy of dyslipidemia.

Niacin structure

Niacin

Niacin-3D-balls

Niacin-3D-spacefill

What are the uses of this medicine?

Niacin is used:

• To reduce elevated TC, LDL-C, Apo B and TG, and to increase HDL-C in patients with primary hyperlipidemia and mixed dyslipidemia.
• To reduce the risk of recurrent nonfatal myocardial infarction in patients with a history of myocardial infarction and hyperlipidemia.

In combination with a bile acid binding resin:

• Slows progression or promotes regression of atherosclerotic disease in patients with a history of coronary artery disease (CAD) and hyperlipidemia.
• As an adjunct to diet to reduce elevated TC and LDL-C in adult patients with primary hyperlipidemia.

• To reduce TG in adult patients with severe hypertriglyceridemia.

Limitations of use:

• Addition of niacin extended-release tablets USP did not reduce cardiovascular morbidity or mortality among patients treated with simvastatin in a large, randomized controlled trial.

How does this medicine work?

• The mechanism by which niacin alters lipid profiles has not been well defined.
• It may involve several actions including partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity, which may increase the rate of chylomicron triglyceride removal from plasma.
• Niacin decreases the rate of hepatic synthesis of VLDL and LDL, and does not appear to affect fecal excretion of fats, sterols, or bile acids.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Active liver disease or unexplained persistent elevations in hepatic transaminases
• Patients with active peptic ulcer disease
• Patients with arterial bleeding
• Hypersensitivity to niacin or any component of this medication

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• anticoagulants ('blood thinners') such as warfarin (Coumadin)
• aspirin
• insulin or oral medications for diabetes
• medications for high blood pressure
• nutritional supplements or other products containing niacin
• other medications for lowering cholesterol or triglycerides
• insulin or oral diabetes medication

• If you are taking a bile acid-binding resin such as colestipol (Colestid) or cholestyramine (Questran), take it at least 4 to 6 hours before or 4 to 6 hours after niacin.

Is this medicine FDA approved?

• Niacin was officially approved for use in the United States in 1957 and is still widely used, although its role in management of hyperlipidemia in patients taking statins and other cholesterol lowering agents remains uncertain and controversial.
• Regular niacin is available in multiple generic forms, under several brand names (including Niacor), in many concentrations as either tablets or capsules from 50 to 1,000 mg each.
• When used to treat hyperlipidemia, regular niacin is generally referred to as intermediate release [IR] niacin.
• IR-niacin must be taken several times daily and is associated with a high rate of cutaneous flushing.
• The recommended dosage for hyperlipidemia is 1 to 6 grams daily, starting at low doses (100 mg three times daily) and increasing at weekly intervals based upon tolerance and effect.
• Sustained release [SR] formulations of niacins have been developed which are available over-the-counter.
• SR niacin can be taken once daily and is less likely to cause flushing, but is not approved for use in hyperlipidemia and has been associated with a high rates of hepatotoxicity in some studies.
• Extended release (ER) capsules and tablets of niacin are available in concentrations ranging from 125 to 1,000 mg, which are approved for use in hyperlipidemia and have not been associated with a higher rate of hepatotoxicity compared to regular niacin.

How should this medicine be used?

Recommended dosage: Niacin extended-release tablets: Dose range:

• 500 mg to 2000 mg once daily.
• Therapy with niacin extended-release tablets must be initiated at 500 mg at bedtime in order to reduce the incidence and severity of side effects which may occur during early therapy and should not be increased by more than 500 mg in any 4 week period.

Maintenance dose:

• 1000 to 2000 mg once daily.
• Doses greater than 2000 mg daily are not recommended.

Niacin tablets:

• The usual adult dosage of nicotinic acid is 1 to 2 grams two or three times a day.
• Doses should be individualized according to the patient's response.
• Start with one-half tablet (250 mg) as a single daily dose following the evening meal.
• The frequency of dosing and total daily dose can be increased every four to seven days until the desired LDL cholesterol and/or triglyceride level is achieved or the first-level therapeutic dose of 1.5 to 2 grams/day is reached.
• If the patient's hyperlipidemia is not adequately controlled after 2 months at this level, the dosage can then be increased at two to four week intervals to 3 grams/day (1 gram three times per day).
• In patients with marked lipid abnormalities, a higher dose is occasionally required, but generally should not exceed 6 grams/day.

Administration:

• Niacin comes as a tablet and an extended-release (long-acting) tablet to take by mouth.
• The regular tablet usually is taken two to three times a day with meals, and the extended-release tablet is taken once a day, at bedtime, after a low-fat snack.
• Swallow the extended-release tablets whole; do not split, chew, or crush them.
• Your doctor will probably start you on a low dose of niacin and gradually increase your dose.
• Continue to take niacin even if you feel well.
• Do not stop taking niacin without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet and an extended-release (long-acting) tablet

This medicine is available in fallowing brand namesː

• Niacor
• Niaspan
• Nicolar
• Slo-Niacin

What side effects can this medication cause?

The most common side effects of this medicine include:

• flushing, diarrhea, nausea, vomiting, increased cough, and pruritus.

Less common side effects may include: Cardiac Disorders: tachycardia, palpitations, atrial fibrillation, other cardiac arrhythmias

Eye Disorders:

• blurred vision, macular edema

Gastrointestinal Disorders:

• peptic ulcers, eructation, flatulence

Hepatobiliary Disorders:

• hepatitis, jaundice

Immune system disorders:

• hypersensitivity reactions (including anaphylaxis, angioedema, urticaria, flushing, dyspnea, tongue edema, larynx edema, face edema, peripheral edema, laryngismus, and vesiculobullous rash)

Metabolism and nutrition Disorders:

• decreased glucose tolerance, gout

Musculoskeletal and connective tissue Disorders:

• myalgia, myopathy

Nervous system Disorders:

• dizziness, insomnia, asthenia, nervousness, paresthesia, migraine

Respiratory, thoracic and mediastinal Disorders:

• dyspnea

Skin and subcutaneous tissue Disorders:

• maculopapular rash, dry skin, sweating, burning sensation/skin burning sensation, skin discoloration, acanthosis nigricans

Vascular Disorders:

• syncope, hypotension, postural hypotension

Hematology:

• Slight reductions in platelet counts and prolongation in prothrombin time.

What special precautions should I follow?

• Severe hepatic toxicity has occurred in patients substituting sustained-release niacin for immediate-release niacin at equivalent doses.
• Myopathy has been reported in patients taking niacin extended-release tablets. The risk for myopathy and rhabdomyolysis are increased among elderly patients; patients with diabetes, renal failure, or uncontrolled hypothyroidism; and patients being treated with a statin.
• Cases of severe hepatic toxicity, including fulminant hepatic necrosis, have occurred in patients who have substituted sustained-release (modified-release, timed-release) niacin products for immediate-release (crystalline) niacin at equivalent doses.
• Niacin extended-release tablets should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease. Active liver diseases or unexplained transaminase elevations are contraindications to the use of niacin extended-release tablets.
• Use with caution in patients with unstable angina or in the acute phase of an MI.
• Niacin extended-release tablets can increase serum glucose levels. Glucose levels should be closely monitored in diabetic or potentially diabetic patients particularly during the first few months of use or dose adjustment.
• Flushing (warmth, redness, itching and/or tingling of the skin) is a common side effect of niacin therapy that may subside after several weeks of consistent niacin extended-release tablets use. Flushing may vary in severity and is more likely to occur with initiation of therapy, or during dose increases. By dosing at bedtime, flushing will most likely occur during sleep. However, if awakened by flushing at night, the patient should get up slowly, especially if feeling dizzy, feeling faint or taking blood pressure medications. Advise patients of the symptoms of flushing and how they differ from the symptoms of a myocardial infarction.
• Taking aspirin (up to the recommended dose of 325 mg) approximately 30 minutes before dosing can minimize flushing.
• Avoid ingestion of alcohol, hot beverages and spicy foods around the time of taking niacin extended-release tablets to minimize flushing.
• Advise patients not to breastfeed during treatment with niacin extended-release tablets.
• Niacin can cause mild-to-moderate serum aminotransferase elevations and high doses and certain formulations of niacin have been linked to clinically apparent, acute liver injury which can be severe as well as fatal.
• The recommended dietary allowance (RDA) of this vitamin is 14 to 16 mg daily in adults, and slightly more for pregnant women (18 mg) and less for children (2 to 12 mg). Niacin given at or around these doses is not associated with significant side effects or liver injury. Niacin is a component of most multivitamin and vitamin B preparations in concentrations close to the minimum daily requirement, which are not effective in lowering lipid levels. Niacin is also found in many herbal mixtures and energy drinks, but generally in low or modest doses.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Supportive measures should be undertaken in the event of an overdose.

Can this medicine be used in pregnancy?

• It is also not known whether nicotinic acid at doses typically used for lipid disorders can cause fetal harm when administered to pregnant women or whether it can affect reproductive capacity.
• If a woman receiving nicotinic acid for primary hypercholesterolemia (Types IIa or IIb) becomes pregnant, the drug should be discontinued.
• If a woman being treated with nicotinic acid for hypertriglyceridemia (Types IV or V) conceives, the benefits and risks of continued drug therapy should be assessed on an individual basis.

Can this medicine be used in children?

• Safety and effectiveness in children and adolescents have not been established.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• NIACIN

Inactive Ingredients:

• croscarmellose sodium
• hydrogenated soybean oil
• magnesium stearate
• microcrystalline cellulose

Who manufactures and distributes this medicine?

Niacin tablets: Manufactured for:

• Emerald Therapeutics, LLC
• Birmingham, AL

Niacin extended-release tablets: Manufactured for:

• Lupin Pharmaceuticals, Inc.
• Baltimore, Maryland
• United States

Manufactured by:

• Lupin Limited
• Goa, INDIA

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted to 15 to 30°C (59 to 86°F).

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Niacin
• FDA Niacin

Niacin Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Vitamins A Vitamin A B Biotin Vitamin B1 (see Thiamin) Vitamin B12 Vitamin B6 C Calcium Choline Chromium Copper Vitamin C D Vitamin D

E Energy Drinks Exercise and Athletic Performance Vitamin E F Fluoride Folate I Iodine Iron K Vitamin K

M Magnesium Multivitamin/mineral Supplements N Niacin P Pantothenic Acid Phosphorus Potassium Primary Mitochondrial Disorders R Riboflavin

S Selenium T Thiamin V Vitamin A Vitamin B1 (see Thiamin) Vitamin B12 Vitamin B6 Vitamin C Vitamin D Vitamin E Vitamin K Z Zinc