Nicotinic acid 500mg modified-release tablets
Requires a prescription from a doctor or prescriber
Niacin is a B vitamin used to treat vitamin deficiencies as well as hyperlipidemia, dyslipidemia, hypertriglyceridemia, and to reduce the risk of myocardial infarctions.[L7550,L7553,L7556,L7559,L7562,L7565]
Official documents, adverse reaction reporting, and safety monitoring
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Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Nicotinic acid
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Report a side effect
Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
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Suspected adverse reactions reported for Nicotinic acid
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3 branded products available
WHO defined daily dose (DDD)
2 gram
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via NHS dm+d BNF mapping files. Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Clinical guidelines and formulary information
British National Formulary
Nicotinic acid
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(4)
Cardiovascular disease: risk assessment and reduction, including lipid modification (NG238)
Ezetimibe for treating primary heterozygous-familial and non-familial hypercholesterolaemia (TA385)
Volanesorsen for treating familial chylomicronaemia syndrome (HST13)
Cilostazol, naftidrofuryl oxalate, pentoxifylline and inositol nicotinate for the treatment of intermittent claudication in people with peripheral arterial disease (TA223)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
Pharmacy stock checkers
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Supply & product information
Official product databases and supply status monitoring
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
82 found
Half-life
0.9h
Mechanism
Niacin performs a number of functions in the body and so has many mechanisms, no…
Food interactions
2 warnings
Human targets
5 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
0.06µg/mL
Half-life
0.9h
[A181556]
Protein binding
Volume of distribution
Metabolism
Elimination
69.5%
[A181556]
37.9%…
Clearance
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
[L7550][L7553][L7556][L7559]
Niacin oral tablets are indicated as a monotherapy or in combination with simvastatin or lovastatin to treat primary hyperlipidemia and mixed dyslipidemia.
[L7562][L7565]
It can also be used to reduce the risk of nonfatal myocardial infarctions in patients with a history of myocardial infarction and hyperlipidemia.
[L7562][L7565]
Niacin is also indicated with bile acid binding resins to treat atherosclerosis in patients with coronary artery disease and hyperlipidemia or to treat primary hyperlipidemia.
[L7562][L7565]
Finally niacin is indicated to treat severe hypertriglyceridemia.
[L7562][L7565]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 566 interactions
[A181499]
Patients experiencing an overdose should be treated with supportive measures which may include intravenous fluids.
[A181499][L7550]
The oral LD50 in the mouse is 3720mg/kg, in the rabbit is 4550mg/kg, in the rat is 7000mg/kg, and the dermal LD50 in the rat is >2000mg/kg.
[L7580]
Niacin inhibits hepatocyte diacylglycerol acyltransferase-2.[A19555] This action prevents the final step of triglyceride synthesis in hepatocytes, limiting available triglycerides for very low density lipoproteins (VLDL).[A19555] This activity also leads to intracellular degradation of apo B and decreased production of low density lipoproteins, the catabolic product of VLDL.[A19555]
Niacin also inhibits a high density lipoprotein (HDL) catabolism receptor, which increases the levels and half life of HDL.[A19555]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[A181511]
The Tmax is 3.0 hours for a 1000mg or 1500mg oral dose.
[A181511]
The AUC is 1.44µg\*h/mL for a 500mg oral dose, 6.66µg\*h/mL for a 1000mg oral dose, and 12.41µg\*h/mL for a 1500mg oral dose.
[A181511]
These values did not drastically differ in patients requiring dialysis.
[A181511]
[A181556]
[A181541]
[A181556]
37.9% of the recovered dose was N-methyl-2-pyridone-5-carboxamide, 16.0% was N-methylnicotinamide, 11.6% was nicotinuric acid, and 3.2% was niacin.
[A181556]
Proteins and enzymes this drug interacts with in the body
Receptor activation by nicotinic acid results in reduced cAMP levels which may affect activity of cAMP-dependent protein kinase A and phosphorylation of target proteins, leading to neutrophil apoptosis. The rank order of potency for the displacement of nicotinic acid binding is 5-methyl pyrazole-3-carboxylic acid = pyridine-3-acetic acid > acifran > 5-methyl nicotinic acid = acipimox >> nicotinuric acid = nicotinamide
PMID:21823666 PMID:23455543 PMID:8182091
Plays a central role in regulating cellular methylation potential, by consuming S-adenosyl-L-methionine and limiting its availability for other methyltransferases. Actively mediates genome-wide epigenetic and transcriptional changes through hypomethylation of repressive chromatin marks, such as H3K27me3 .
PMID:23455543 PMID:26571212 PMID:31043742
In a developmental context, contributes to low levels of the repressive histone marks that characterize pluripotent embryonic stem cell pre-implantation state .
PMID:26571212
Acts as a metabolic regulator primarily on white adipose tissue energy expenditure as well as hepatic gluconeogenesis and cholesterol biosynthesis. In white adipocytes, regulates polyamine flux by consuming S-adenosyl-L-methionine which provides for propylamine group in polyamine biosynthesis, whereas by consuming nicotinamide controls NAD(+) levels through the salvage pathway (By similarity).
Via its product N1-methylnicotinamide regulates protein acetylation in hepatocytes, by repressing the ubiquitination and increasing the stability of SIRT1 deacetylase (By similarity). Can also N-methylate other pyridines structurally related to nicotinamide and play a role in xenobiotic detoxification PMID:30044909
PMID:27184406
Probably plays a central role in cytosolic lipid accumulation. In liver, is primarily responsible for incorporating endogenously synthesized fatty acids into triglycerides (By similarity).
Also functions as an acyl-CoA retinol acyltransferase (ARAT) (By similarity). Also able to use 1-monoalkylglycerol (1-MAkG) as an acyl acceptor for the synthesis of monoalkyl-monoacylglycerol (MAMAG) PMID:28420705
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:10454528 PMID:10525100 PMID:10966938 PMID:17509700 PMID:20722056 PMID:33124720
Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium.
Relative uptake activity ratio of carnitine to TEA is 11.3 .
PMID:10454528 PMID:10525100 PMID:10966938
In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from B.subtilis which induces cytoprotective heat shock proteins contributing to intestinal homeostasis .
PMID:18005709
May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:10873595 PMID:11159893 PMID:11932330 PMID:12724351 PMID:14610227 PMID:16908597 PMID:18501590 PMID:20507927 PMID:22201122 PMID:23531488 PMID:25132355 PMID:26383540 PMID:27576593 PMID:28408210 PMID:29871943 PMID:34628357
Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S) .
PMID:11932330 PMID:12409283
Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver .
PMID:11159893
Mediates the intestinal uptake of sulfated steroids .
PMID:12724351 PMID:28408210
Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain .
PMID:16908597 PMID:25132355
Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons .
PMID:25132355
May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC .
PMID:35714613
Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition .
PMID:26383540
Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:14610227 PMID:19129463 PMID:22201122
The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound .
PMID:19129463 PMID:20507927 PMID:26277985
Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions .
PMID:19129463
Cytoplasmic glutamate may also act as counteranion in the placenta .
PMID:26277985
An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) PMID:20507927
PMID:12946269 PMID:32946811 PMID:33333023
Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, acetate and the ketone bodies acetoacetate and beta-hydroxybutyrate, and thus contributes to the maintenance of intracellular pH .
PMID:12946269 PMID:33333023
The transport direction is determined by the proton motive force and the concentration gradient of the substrate monocarboxylate. MCT1 is a major lactate exporter (By similarity). Plays a role in cellular responses to a high-fat diet by modulating the cellular levels of lactate and pyruvate that contribute to the regulation of central metabolic pathways and insulin secretion, with concomitant effects on plasma insulin levels and blood glucose homeostasis (By similarity).
Facilitates the protonated monocarboxylate form of succinate export, that its transient protonation upon muscle cell acidification in exercising muscle and ischemic heart .
PMID:32946811
Functions via alternate outward- and inward-open conformation states. Protonation and deprotonation of 309-Asp is essential for the conformational transition PMID:33333023
PMID:14966140 PMID:15090606 PMID:16729224 PMID:16805814 PMID:17178845 PMID:17245649 PMID:17526579 PMID:20211600 PMID:30604288
Catalyzes passive carrier mediated diffusion of iodide .
PMID:12107270
Mediates iodide transport from the thyrocyte into the colloid lumen through the apical membrane .
PMID:12107270
May be responsible for the absorption of D-lactate and monocarboxylate drugs from the intestinal tract .
PMID:17245649
Acts as a tumor suppressor, suppressing colony formation in colon cancer, prostate cancer and glioma cell lines .
PMID:12829793 PMID:15867356 PMID:18037591
May play a critical role in the entry of L-lactate and ketone bodies into neurons by a process driven by an electrochemical Na(+) gradient and hence contribute to the maintenance of the energy status and function of neurons .
PMID:16805814
Mediates sodium-coupled electrogenic transport of pyroglutamate (5-oxo-L-proline) .
PMID:20211600
Can mediate the transport of chloride, bromide, iodide and nitrate ions when the external concentration of sodium ions is reduced PMID:19864324
PMID:11101640 PMID:23935841 PMID:31719150
Plays a predominant role in L-lactate efflux from highly glycolytic cells (By similarity)
Proteins that carry this drug through the body
ATC C10AD02
ATC C10AD52
ATC C10BA01
ATC C04AC01
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Niacin
Matched from: Nicotinic acid
Additional database identifiers
Drugs Product Database (DPD)
5019
Drugs Product Database (DPD)
474
ChemSpider
913
BindingDB
23515
PDB
NIO
Guide to Pharmacology
1594
ZINC
ZINC000000001795
HUGO Gene Nomenclature Committee (HGNC)
HGNC:16824
GenAtlas
GPR109B
GeneCards
HCAR3
GenBank Gene Database
D10923
GenBank Protein Database
219867
Guide to Pharmacology
313
UniProt Accession
HCAR3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:24827
GenAtlas
GPR109A
GeneCards
HCAR2
GenBank Gene Database
AY148884
GenBank Protein Database
28975188
Guide to Pharmacology
312
UniProt Accession
HCAR2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9755
GenAtlas
QPRT
GeneCards
QPRT
GenBank Gene Database
D78177
GenBank Protein Database
1060907
UniProt Accession
NADC_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:7861
GenAtlas
NNMT
GeneCards
NNMT
GenBank Gene Database
U08021
GenBank Protein Database
494989
Guide to Pharmacology
3205
UniProt Accession
NNMT_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:16940
GeneCards
DGAT2
Guide to Pharmacology
3211
UniProt Accession
DGAT2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2625
GenAtlas
CYP2D6
GeneCards
CYP2D6
GenBank Gene Database
M20403
GenBank Protein Database
181350
Guide to Pharmacology
1329
UniProt Accession
CP2D6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2637
GenAtlas
CYP3A4
GeneCards
CYP3A4
GenBank Gene Database
M18907
Guide to Pharmacology
1337
UniProt Accession
CP3A4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2631
GeneCards
CYP2E1
GenBank Gene Database
J02625
GenBank Protein Database
181360
Guide to Pharmacology
1330
UniProt Accession
CP2E1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:11583
GenAtlas
SERPINA7
GeneCards
SERPINA7
GenBank Gene Database
M14091
GenBank Protein Database
338697
UniProt Accession
THBG_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10969
GenAtlas
SLC22A5
GeneCards
SLC22A5
GenBank Gene Database
AF057164
GenBank Protein Database
3273741
UniProt Accession
S22A5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10962
GenAtlas
SLCO2B1
GeneCards
SLCO2B1
GenBank Gene Database
AB026256
GenBank Protein Database
5006263
Guide to Pharmacology
1224
UniProt Accession
SO2B1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10922
GenAtlas
SLC16A1
GeneCards
SLC16A1
GenBank Gene Database
L31801
GenBank Protein Database
561722
Guide to Pharmacology
988
UniProt Accession
MOT1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:19119
GeneCards
SLC5A8
Guide to Pharmacology
922
UniProt Accession
SC5A8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10924
GenAtlas
SLC16A3
GeneCards
SLC16A3
GenBank Gene Database
U81800
GenBank Protein Database
2463634
Guide to Pharmacology
989
UniProt Accession
MOT4_HUMAN
International reference pricing
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
All patents expired, 5 expired
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: