Peringatan Keamanan

Overdose of niacin may present with severe prolonged hypotension.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

DB00627

small molecule approved investigational nutraceutical

Deskripsi

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

Struktur Molekul 2D

Berat 123.1094
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of niacin is 0.9h, nicotinuric acid is 1.3h, and nicotinamide is 4.3h.[A181556]
Volume Distribusi Data regarding the volume of distribution of niacin is not readily available.
Klirens (Clearance) Data regarding the clearance of niacin is not readily available.

Absorpsi

In patients with chronic kidney disease, the Cmax is 0.06µg/mL for a 500mg oral dose, 2.42µg/mL for a 1000mg oral dose, and 4.22µg/mL for a 1500mg oral dose.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

Metabolisme

The metabolism of niacin is poorly described in the literature, but the metabolites niacinamide, niacinamide N-oxide, nicotinuric acid, N1-methyl-2-pyridone-5-carboxamide, N1-methyl-4-pyridone-5-carboxamide, and trigonelline have been identified in human urine.A181541

Rute Eliminasi

69.5% of a dose of niacin is recovered in urine.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

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Alcohol increases the chance of flushing and pruritus.
  • 2. Take with food. Food reduces gastrointestinal upset and irritation.

Interaksi Obat

565 Data
Pravastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Pravastatin.
Cerivastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Cerivastatin.
Atorvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Atorvastatin.
Fluvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Fluvastatin.
Rosuvastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Rosuvastatin.
Mevastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Mevastatin.
Pitavastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Niacin is combined with Pitavastatin.
Colestipol Colestipol can cause a decrease in the absorption of Niacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Niacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Niacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Niacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Niacin.
Ethanol The risk or severity of adverse effects can be increased when Ethanol is combined with Niacin.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Niacin.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Niacin.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Niacin.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Niacin.
Troglitazone The therapeutic efficacy of Troglitazone can be decreased when used in combination with Niacin.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be decreased when used in combination with Niacin.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Niacin.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Niacin.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be decreased when used in combination with Niacin.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Niacin.
Quinine The therapeutic efficacy of Quinine can be decreased when used in combination with Niacin.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Niacin.
Nateglinide The therapeutic efficacy of Nateglinide can be decreased when used in combination with Niacin.
Pentamidine The therapeutic efficacy of Pentamidine can be decreased when used in combination with Niacin.
Mifepristone The therapeutic efficacy of Mifepristone can be decreased when used in combination with Niacin.
Repaglinide The therapeutic efficacy of Repaglinide can be decreased when used in combination with Niacin.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Niacin.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be decreased when used in combination with Niacin.
Pioglitazone The therapeutic efficacy of Pioglitazone can be decreased when used in combination with Niacin.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Niacin.
Sitagliptin The therapeutic efficacy of Sitagliptin can be decreased when used in combination with Niacin.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Niacin.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Niacin.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Niacin.
Insulin aspart The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Niacin.
Insulin detemir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Niacin.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be decreased when used in combination with Niacin.
Glymidine The therapeutic efficacy of Glymidine can be decreased when used in combination with Niacin.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be decreased when used in combination with Niacin.
Buformin The therapeutic efficacy of Buformin can be decreased when used in combination with Niacin.
Vildagliptin The therapeutic efficacy of Vildagliptin can be decreased when used in combination with Niacin.
Voglibose The therapeutic efficacy of Voglibose can be decreased when used in combination with Niacin.
NN344 The therapeutic efficacy of NN344 can be decreased when used in combination with Niacin.
AMG-222 The therapeutic efficacy of AMG-222 can be decreased when used in combination with Niacin.
Bisegliptin The therapeutic efficacy of Bisegliptin can be decreased when used in combination with Niacin.
Alogliptin The therapeutic efficacy of Alogliptin can be decreased when used in combination with Niacin.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be decreased when used in combination with Niacin.
Saxagliptin The therapeutic efficacy of Saxagliptin can be decreased when used in combination with Niacin.
Liraglutide The therapeutic efficacy of Liraglutide can be decreased when used in combination with Niacin.
Gosogliptin The therapeutic efficacy of Gosogliptin can be decreased when used in combination with Niacin.
Linagliptin The therapeutic efficacy of Linagliptin can be decreased when used in combination with Niacin.
Canagliflozin The therapeutic efficacy of Canagliflozin can be decreased when used in combination with Niacin.
Benfluorex The therapeutic efficacy of Benfluorex can be decreased when used in combination with Niacin.
Empagliflozin The therapeutic efficacy of Empagliflozin can be decreased when used in combination with Niacin.
Albiglutide The therapeutic efficacy of Albiglutide can be decreased when used in combination with Niacin.
Dulaglutide The therapeutic efficacy of Dulaglutide can be decreased when used in combination with Niacin.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Niacin.
Netoglitazone The therapeutic efficacy of Netoglitazone can be decreased when used in combination with Niacin.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be decreased when used in combination with Niacin.
Ciglitazone The therapeutic efficacy of Ciglitazone can be decreased when used in combination with Niacin.
Lixisenatide The therapeutic efficacy of Lixisenatide can be decreased when used in combination with Niacin.
Insulin beef The therapeutic efficacy of Insulin beef can be decreased when used in combination with Niacin.
Insulin degludec The therapeutic efficacy of Insulin degludec can be decreased when used in combination with Niacin.
Insulin peglispro The therapeutic efficacy of Insulin peglispro can be decreased when used in combination with Niacin.
Insulin tregopil The therapeutic efficacy of Insulin tregopil can be decreased when used in combination with Niacin.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be decreased when used in combination with Niacin.
Dutogliptin The therapeutic efficacy of Dutogliptin can be decreased when used in combination with Niacin.
Allicin The therapeutic efficacy of Allicin can be decreased when used in combination with Niacin.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be decreased when used in combination with Niacin.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be decreased when used in combination with Niacin.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Niacin.
Teneligliptin The therapeutic efficacy of Teneligliptin can be decreased when used in combination with Niacin.
Omarigliptin The therapeutic efficacy of Omarigliptin can be decreased when used in combination with Niacin.
Carmegliptin The therapeutic efficacy of Carmegliptin can be decreased when used in combination with Niacin.
Gemigliptin The therapeutic efficacy of Gemigliptin can be decreased when used in combination with Niacin.
Anagliptin The therapeutic efficacy of Anagliptin can be decreased when used in combination with Niacin.
Evogliptin The therapeutic efficacy of Evogliptin can be decreased when used in combination with Niacin.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be decreased when used in combination with Niacin.
Balaglitazone The therapeutic efficacy of Balaglitazone can be decreased when used in combination with Niacin.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be decreased when used in combination with Niacin.
Guar gum The therapeutic efficacy of Guar gum can be decreased when used in combination with Niacin.
Semaglutide The therapeutic efficacy of Semaglutide can be decreased when used in combination with Niacin.
Taspoglutide The therapeutic efficacy of Taspoglutide can be decreased when used in combination with Niacin.
Englitazone The therapeutic efficacy of Englitazone can be decreased when used in combination with Niacin.
Tirzepatide The therapeutic efficacy of Tirzepatide can be decreased when used in combination with Niacin.
Gastric inhibitory polypeptide The therapeutic efficacy of Gastric inhibitory polypeptide can be decreased when used in combination with Niacin.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Niacin.
Patent Blue The therapeutic efficacy of Niacin can be decreased when used in combination with Patent Blue.
Aripiprazole The metabolism of Aripiprazole can be decreased when combined with Niacin.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be decreased when combined with Niacin.
Leuprolide The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Leuprolide is combined with Niacin.
Somatotropin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Somatotropin is combined with Niacin.
Infliximab The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Infliximab is combined with Niacin.
Daptomycin The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Daptomycin is combined with Niacin.
Baclofen The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Baclofen is combined with Niacin.
Cladribine The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Cladribine is combined with Niacin.
Pamidronic acid The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Pamidronic acid is combined with Niacin.

Target Protein

Hydroxycarboxylic acid receptor 3 HCAR3
Diacylglycerol O-acyltransferase 2 DGAT2
Hydroxycarboxylic acid receptor 2 HCAR2
Nicotinate-nucleotide pyrophosphorylase [carboxylating] QPRT
Nicotinamide N-methyltransferase NNMT

Referensi & Sumber

Synthesis reference: Joseph E. Toomey, Jr., "Electrochemical synthesis of niacin and other N-heterocyclic compounds." U.S. Patent US5002641, issued 1914.
Artikel (PubMed)
  • PMID: 16496499
    Mularski RA, Grazer RE, Santoni L, Strother JS, Bizovi KE: Treatment advice on the internet leads to a life-threatening adverse reaction: hypotension associated with Niacin overdose. Clin Toxicol (Phila). 2006;44(1):81-4.
  • PMID: 20562093
    Reiche I, Westphal S, Martens-Lobenhoffer J, Troger U, Luley C, Bode-Boger SM: Pharmacokinetics and dose recommendations of Niaspan(R) in chronic kidney disease and dialysis patients. Nephrol Dial Transplant. 2011 Jan;26(1):276-82. doi: 10.1093/ndt/gfq344. Epub 2010 Jun 17.
  • PMID: 18375237
    Kamanna VS, Kashyap ML: Mechanism of action of niacin. Am J Cardiol. 2008 Apr 17;101(8A):20B-26B. doi: 10.1016/j.amjcard.2008.02.029.
  • PMID: 25386386
    Taguchi K, Fukusaki E, Bamba T: Determination of niacin and its metabolites using supercritical fluid chromatography coupled to tandem mass spectrometry. Mass Spectrom (Tokyo). 2014;3(1):A0029. doi: 10.5702/massspectrometry.A0029. Epub 2014 Aug 1.
  • PMID: 17725178
    Menon RM, Adams MH, Gonzalez MA, Tolbert DS, Leu JH, Cefali EA: Plasma and urine pharmacokinetics of niacin and its metabolites from an extended-release niacin formulation. Int J Clin Pharmacol Ther. 2007 Aug;45(8):448-54. doi: 10.5414/cpp45448.

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