pharmacopeia
GET
/api/v1/drug/niacin
2D structure
pyridine-3-carboxylic acid
SMILES C1=CC(=CN=C1)C(=O)O
InChIKey PVNIIMVLHYAWGP-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

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.

Indications

Sourced from openFDA
  • Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hyperlipidemia. Niacin therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate.ICD-10: E78.5

Contraindications

Sourced from openFDA
  • Niacin extended-release tablets are contraindicated in the following conditions: Active liver disease or unexplained persistent elevations in hepatic transaminases [see Warnings and Precautions (5.3) ] Patients with active peptic ulcer disease Patients with arterial bleeding Hypersensitivity to niacin or any component of this medication [see Adverse Reactions (6.1) ] Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels. ( 4 , 5.3 ) Active peptic ulcer disease.contraindicated

Dosage & administration

Sourced from openFDA

Niacin extended-release tablets should be taken at bedtime with a low-fat snack. ( 2.1 ) Dose range: 500 mg to 2,000 mg once daily. ( 2.1 ) 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. ( 2.1 ) Maintenance dose: 1,000 mg to 2,000 mg once daily. ( 2.2 ) Doses greater than 2,000 mg daily are not recommended. ( 2.2 ) 2.1 Initial Dosing Niacin extended-release tablets should be taken at bedtime, after a low-fat snack, and doses should be individualized according to patient response. 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. The recommended dose escalation is shown in Table 1 below. Table 1. Recommended Dosing Week(s) Daily dose Niacin Extended-Release Tablets Dosage INITIAL TITRATION SCHEDULE 1 to 4 500 mg 1 Niacin extended-release 500 mg tablet at bedtime 5 to 8 1,000 mg 1 Niacin extended-release 1,000 mg tablet or 2 Niacin extended-release 500 mg tablets at bedtime * 1,500 mg 2 Niacin extended-release 750 mg tablets or 3 Niacin extended-release 500 mg tablets at bedtime * 2,000 mg 2 Niacin extended-release 1,000 mg tablets or 4 Niacin extended-release 500 mg tablets at bedtime * After Week 8, titrate to patient response and tolerance.

Warnings & precautions

Sourced from openFDA

Niacin extended-release tablet preparations should not be substituted for equivalent doses of immediate-release (crystalline) niacin. For patients switching from immediate-release niacin to niacin extended-release tablets, therapy with niacin extended-release tablets should be initiated with low doses (i.e., 500 mg at bedtime) and the niacin extended-release tablets dose should then be titrated to the desired therapeutic response [see Dosage and Administration (2.1) ] . Caution should also be used when niacin extended-release tablets are used in patients with unstable angina or in the acute phase of an MI, particularly when such patients are also receiving vasoactive drugs such as nitrates, calcium channel blockers, or adrenergic blocking agents. Niacin is rapidly metabolized by the liver, and excreted through the kidneys. Niacin extended-release tablets are contraindicated in patients with significant or unexplained hepatic impairment [see Contraindications (4) and Warnings and Precautions (5.3) ] and should be used with caution in patients with renal impairment. Patients with a past history of jaundice, hepatobiliary disease, or peptic ulcer should be observed closely during niacin extended-release tablets therapy. Severe hepatic toxicity has occurred in patients substituting sustained-release niacin for immediate-release niacin at equivalent doses. ( 5.3 ) Myopathy has been reported in patients taking niacin extended-release tablets.

Adverse reactions

Sourced from openFDA

The following adverse reactions are discussed in greater detail in other sections of the labeling: Mortality and Coronary Heart Disease Morbidity [see Warnings and Precautions (5.1) ] Skeletal Muscle (rhabdomyolysis) [see Warnings and Precautions (5.2) ] Liver Dysfunction [see Warnings and Precautions (5.3) ] Laboratory Abnormalities [see Warnings and Precautions (5.4) ] Most common adverse reactions (incidence >5% and greater than placebo) are flushing, diarrhea, nausea, vomiting, increased cough, and pruritus. ( 6.1 ) Flushing of the skin may be reduced in frequency or severity by pretreatment with aspirin (up to the recommended dose of 325 mg taken 30 minutes prior to niacin extended-release tablets dose). ( 2.2 ) To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. In the placebo-controlled clinical trials database of 402 patients (age range 21 to 75 years, 33% women, 89% Caucasians, 7% Blacks, 3% Hispanics, 1% Asians) with a median treatment duration of 16 weeks, 16% of patients on niacin extended-release tablets and 4% of patients on placebo discontinued due to adverse reactions.

Use in specific populations

Sourced from openFDA

Pregnancy: Discontinue in patients with hyperlipidemia; assess individual risks and benefits in patients with hypertriglyceridemia. ( 8.1 ) Lactation: Advise patients not to breastfeed during treatment. ( 8.2 ) Renal impairment: Niacin extended-release tablets should be used with caution in patients with renal impairment. ( 5 , 8.6 ) Hepatic impairment: Niacin extended-release tablets are contraindicated in active liver disease or significant or unexplained hepatic dysfunction or unexplained elevations of serum transaminases. ( 4 , 5 , 5.3 , 8.7 ) 8.1 Pregnancy Risk Summary Discontinue niacin extended-release tablets when pregnancy is recognized in patients receiving the drug for the treatment of hyperlipidemia. Assess the individual risks and benefits of continuing niacin extended-release tablets during pregnancy in patients receiving the drug for the treatment of hypertriglyceridemia. Advise patients to inform their healthcare provider of a known or suspected pregnancy. The potential for embryofetal toxicity with the doses of niacin in niacin extended-release tablets is unknown. The available data on niacin extended-release tablets use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Due to extensive and saturable first-pass metabolism, niacin concentrations in the general circulation are dose dependent and highly variable. Time to reach the maximum niacin plasma concentrations was about 5 hours following niacin extended-release tablets.

Overdosage

Sourced from openFDA

Supportive measures should be undertaken in the event of an overdose.

Approval history

Sourced from openFDA
  • May 3, 2000ANDAANDA040378Avondale Pharms
  • Mar 20, 2014ANDAANDA090892Chartwell Rx
  • Apr 23, 2014ANDAANDA200484Sun Pharm
  • Apr 23, 2014ANDAANDA201273Sun Pharm
  • Jul 24, 2015ANDAANDA203578Amneal Pharms
  • Dec 11, 2015ANDAANDA204178Amneal Pharms
  • Jun 16, 2017ANDAANDA203899Lannett Co Inc
  • Feb 1, 2018ANDAANDA209236Aurobindo Pharma Ltd

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
12,194 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue7996.6%
  2. 2Drug Ineffective7646.3%
  3. 3Nausea7165.9%
  4. 4Diarrhoea6845.6%
  5. 5Dizziness5894.8%
  6. 6Dyspnoea5584.6%
  7. 7Pain5344.4%
  8. 8Headache5174.2%
  9. 9Drug Hypersensitivity5004.1%
  10. 10Asthenia4643.8%
  11. 11Arthralgia4133.4%
  12. 12Fall4093.4%
  13. 13Pain In Extremity3993.3%
  14. 14Rash3803.1%
  15. 15Vomiting3733.1%

Literature

View JSON

Recent PubMed references pinned to Niacin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 1,420 ClinicalTrials.gov registrations naming Niacin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Niacin 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.
What is Niacin used for?
According to FDA labeling, Niacin carries indications including: Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hyperlipidemia. Niacin therapy is indicated as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Niacin?
Niacin is classified as Nicotinic acid and derivatives, Nicotinic Acid, Enzyme Interactions, Cellular Activity Alteration, Decreased Cholesterol Synthesis, Glucose Metabolism Alteration.
What are the brand names for Niacin?
Niacin is marketed under brand names including Concept OB, Endur-Acin, Endur-Amide, Endur-Thine, Folivane-F, Irospan Tablet, MVC-Fluoride, Niacor.
What are the contraindications for Niacin?
Niacin labeling lists contraindications including: Niacin extended-release tablets are contraindicated in the following conditions: Active liver disease or unexplained persistent elevations in hepatic transaminases [see Warnings and Precautions (5.3) ] Patients with active peptic ulcer disease Patients with arterial bleeding Hypersensitivity to niacin or any component of this medication [see Adverse Reactions (6.1) ] Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels. ( 4 , 5.3 ) Active peptic ulcer disease.. Always consult the full prescribing information and a clinician.
Note. Data for niacin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients