Peringatan Keamanan

NOAEL is 4000mg. Inositol nicotinate can cause muscle pain, headache, redness of face, nausea, vomiting, edema and rash.

Inositol nicotinate

DB08949

small molecule approved withdrawn

Deskripsi

Inositol nicotinate, also known as Inositol hexaniacinate/hexanicotinate or "no-flush niacin", is a niacin ester and vasodilator. It is used in food supplements as a source of niacin (vitamin B3), where hydrolysis of 1 g (1.23 mmol) inositol hexanicotinate yields 0.91 g nicotinic acid and 0.22 g inositol. Niacin exists in different forms including nicotinic acid, nicotinamide and other derivatives such as inositol nicotinate. It is associated with reduced flushing compared to other vasodilators by being broken down into the metabolites and inositol at a slower rate. Nicotinic acid plays an essential role in many important metabolic processes and has been used as lipid-lowering agent. Inositol nicotinate is prescribed in Europe under the name Hexopal as a symptomatic treatment for severe intermittent claudication and Raynaud’s phenomenon.

Struktur Molekul 2D

Berat 810.732
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean elimination half life in healthy human adults is approximately one hour [A19550].
Volume Distribusi Mean Vd following intravenous administration of 50mg/kg of inositol nicotinate in rats is 1051±250 mL/kg [A19550].
Klirens (Clearance) Mean clearance rate following intravenous administration of 50mg/kg of inositol nicotinate in rats is 65.4±19 mL/min/kg [A19550].

Absorpsi

Gastrointestinal absorption of inositol hexanicotinate varies widely, with an average of 70% of an orally ingested dose absorbed from stomach and upper small intestines into the bloodstream as intact form. The maximum serum levels of nicotinic acid is reached approximately 6-10 hours after oral ingestion. At low concentrations, the absorption of nicotinic acid and nicotinamide is mediated by sodium ion-dependent facilitated diffusion. At higher concentrations, passive diffusion predominates with doses of 3 to 4 g of niacin being almost completely absorbed L810.

Metabolisme

Inositol nicotinate undergoes hydrolysis by plasma esterases, releasing free nicotinic acid and inositol in a sustained manner. The process takes more than 48hours, where the bloodstream enzymatic hydrolysis of inositol hexanicotinate was found to be slower in the first ester linkage of inositol hexanicotinate than in subsequent linkages L810. Sequential hydrolytic steps of inositol nicotinate forms one nicotinic acid molecule in each step, producing eventually six molecules of nicotinic acid and one inositol moiety A19550.

Rute Eliminasi

Unabsorbed inositol nicotinate is detected in feces.

Interaksi Obat

3 Data
Patent Blue The therapeutic efficacy of Inositol nicotinate can be decreased when used in combination with Patent Blue.
Isosorbide mononitrate Inositol nicotinate may increase the vasodilatory activities of Isosorbide mononitrate.
Iloprost Iloprost may increase the hypotensive activities of Inositol nicotinate.

Target Protein

Hydroxycarboxylic acid receptor 3 HCAR3
Hydroxycarboxylic acid receptor 2 HCAR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14986567
    Dib JG, Dedeyan S: Purported benefits of inositol niacinate. Am J Health Syst Pharm. 2004 Feb 1;61(3):307-8.
  • PMID: 23347001
    Milton SG, Robinson K, Ma J, Wei B, Poon IO, Liang D: Biotransformation and pharmacokinetics of inositol hexanicotinate in rats. Xenobiotica. 2013 Sep;43(9):817-22. doi: 10.3109/00498254.2012.762591. Epub 2013 Jan 24.
  • PMID: 15642562
    Canner PL, Furberg CD, Terrin ML, McGovern ME: Benefits of niacin by glycemic status in patients with healed myocardial infarction (from the Coronary Drug Project). Am J Cardiol. 2005 Jan 15;95(2):254-7.
  • PMID: 15183629
    Karpe F, Frayn KN: The nicotinic acid receptor--a new mechanism for an old drug. Lancet. 2004 Jun 5;363(9424):1892-4.
  • PMID: 546424
    Harthon L, Brattsand R: Enzymatic hydrolysis of pentaerythritoltetranicotinate and meso-inositolhexanicotinate in blood and tissues. Arzneimittelforschung. 1979;29(12):1859-62.
  • 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: 11122723
    Kamanna VS, Kashyap ML: Mechanism of action of niacin on lipoprotein metabolism. Curr Atheroscler Rep. 2000 Jan;2(1):36-46.
  • PMID: 12873710
    Ganji SH, Kamanna VS, Kashyap ML: Niacin and cholesterol: role in cardiovascular disease (review). J Nutr Biochem. 2003 Jun;14(6):298-305.
Menampilkan 8 dari 10 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    23. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 291). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 8 • International brands: 6
Produk
  • DermaNIC
    Tablet • - • Oral • US
  • Flush Free Niacin With Inositol
    Capsule • - • Oral • Canada • OTC • Approved
  • Inositol Nicotinate 250 mg
    Tablet • - • Oral • Canada • OTC • Approved
  • Inositol Nicotinate 250 mg
    Tablet • - • Oral • Canada • OTC • Approved
  • TL-Care DHA
    Capsule • - • Oral • US
  • Tricare Prenatal DHA One
    Capsule, gelatin coated • - • Oral • US
  • Tricare Prenatal DHA One Rx Multivitamin
    Capsule, gelatin coated • - • Oral • US
  • Tricare Prenatal DHA One With Folate
    - • - • Oral • US
International Brands
  • Hexaniton — Ni-The
  • Hexazin — Johnson
  • Hexin — New Chemical
  • Hexopal — Clonmel
  • Iexaniton — Ni-The
  • Nicoxatin — Fuso Pharmaceutical

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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