Niacinamide, an amide of vitamin B3 (niacin), is a hydrophilic endogenous substance. Its effects after epicutaneous application have long been described in the literature. Given a sufficient bioavailability, niacinamide has antipruritic, antimicrobial, vasoactive, photo-protective, sebostatic and lightening effects depending on its concentration. Within a complex metabolic system niacinamide controls the NFκB-mediated transcription of signalling molecules by inhibiting the nuclear poly (ADP-ribose) polymerase-1 (PARP-1). Niacinamide is a well-tolerated and safe substance often used in cosmetics. Clinical data for its therapeutic use in various dermatoses can increasingly be found in the literature. Although the existing data are not sufficient for a scientifically founded evaluation, it can be stated that the use of niacinamide in galenic preparations for epicutaneous application offers most interesting prospects.

1.
Burgess C: Topical vitamins. J Drugs Dermatol 2008;7(suppl 7):s2-s6.
2.
Larm NE, Geme G: Understanding the chemistry of the reaction between nicotinamide and trichloroacetic acid. Abstr Am Chem Soc 2009, p 237.
3.
Yang J, Klaidman LK, Adams JD: Medicinal chemistry of nicotinamide in the treatment of ischemia and reperfusion. Mini Rev Med Chem 2002;2:125-134.
4.
DiPalma JR, Thayer WS: Use of niacin as a drug. Annu Rev Nutr 1991;11:169-187.
5.
Bellen N: Application of polarography in analytical control of industrial processes on example of synthesis of nicotinic-acid and nicotinamide from 3-picoline by ICHP method. Przemysl Chemiczny 1973;52:226-229.
6.
Wiegand C, Holman WIM: Synthesis of derivatives of N-methyl-2-pyridone from nicotinic acid and nicotinamide. Nature 1948;162:659-660.
7.
Maiese K, Chong ZZ, Hou J, Shang YC: The vitamin nicotinamide: translating nutrition into clinical care. Molecules 2009;14:3446-3485.
8.
Hoffer A: Biochemistry of nicotinic acid and nicotinamide. Psychosomatics 1967;8:95-100.
9.
Stratford MR, Dennis MF: Pharmacokinetics and biochemistry studies on nicotinamide in the mouse. Cancer Chemother Pharmacol 1994;34:399-404.
10.
Matsui A, Yin Y, Yamanaka K, Iwasaki M, Ashihara H: Metabolic fate of nicotinamide in higher plants. Physiol Plant 2007;131:191-200.
11.
Telepneva VI, Meshter R: Concerning the content and method for determination of nicotinamide nucleotides in denervated and intact skeletal muscles (in Russian). Biokhimiia 1969;34:160-165.
12.
Tamagnone G, DeMaria R: New method for isolating nicotinamide-adenine dinucleotide (Nad) from baker's yeast. Int Z Vitaminforsch 1967;37:367-370.
13.
Rex A, Fink H: Pharmacokinetic aspects of reduced nicotinamide adenine dinucleotide (NADH) in rats. Front Biosci 2008;13:3735-3741.
14.
Chaykin S, Dagani M, Johnson L, Samli M: The fate of nicotinamide in the mouse. Urinary metabolites. J Biol Chem 1965;240:932-938.
15.
Sivapirabu G, Yiasemides E, Halliday GM, Park J, Damian DL: Topical nicotinamide modulates cellular energy metabolism and provides broad-spectrum protection against ultraviolet radiation-induced immunosuppression in humans. Br J Dermatol 2009;161:1357-1364.
16.
Rochette-Egly C, Ittel ME, Bilen J, Mandel P: Effect of nicotinamide on RNA and DNA synthesis and on poly(ADP-ribose) polymerase activity in normal and phytohemagglutinin stimulated human lymphocytes. FEBS Lett 1980;120:7-11.
17.
Althaus FR, Lawrence SD, Sattler GL, Pitot HC: The effect of nicotinamide on unscheduled DNA synthesis in cultured hepatocytes. Biochem Biophys Res Commun 1980;95:1063-1070.
18.
Berger NA, Sikorski GW: Nicotinamide stimulates repair of DNA damage in human lymphocytes. Biochem Biophys Res Commun 1980;95:67-72.
19.
Lee HI, Jang SY, Kang HT, Hwang ES: p53-, SIRT1-, and PARP-1-independent downregulation of p21WAF1 expression in nicotinamide-treated cells. Biochem Biophys Res Commun 2008;368:298-304.
20.
Lin SJ, Guarente L: Nicotinamide adenine dinucleotide, a metabolic regulator of transcription, longevity and disease. Curr Opin Cell Biol 2003;15:241-246.
21.
Ungerstedt JS, Blomback M, Soderstrom T: Nicotinamide is a potent inhibitor of proinflammatory cytokines. Clin Exp Immunol 2003;131:48-52.
22.
Otsuka A, Hanafusa T, Miyagawa J, Kono N, Tarui S: Nicotinamide and 3-aminobenzamide reduce interferon-gamma-induced class Ii MHC (HLA-DR and -DP) molecule expression on cultured human endothelial cells and fibroblasts. Immunopharmacol Immunotoxicol 1991;13:263-280.
23.
Fujimura M, Tominaga T, Yoshimoto T: Nicotinamide inhibits inducible nitric oxide synthase mRNA in primary rat glial cells. Neurosci Lett 1997;228:107-110.
24.
Andrade J, Ramirez R, Conde M, Sobrino F, Bedoya FJ: Nicotinamide inhibits inducible nitric oxide synthase enzyme activity in macrophages by allowing nitric oxide to inhibit its own formation. Life Sci 1997;61:1843-1850.
25.
Pietrzak L, Mogielnicki A, Buczko W: Nicotinamide and its metabolite N-methylnicotinamide increase skin vascular permeability in rats. Clin Exp Dermatol 2009;34:380-384.
26.
Collins TM, Caimi R, Lynch PR, Sheffield J, Mitra A, Stueber K, Smith YR: The effects of nicotinamide and hyperbaric oxygen on skin flap survival. Scand J Plast Reconstr Surg Hand Surg 1991;25:5-7.
27.
Collins TM, Denish A, Sheffield J, Mitra A, Stueber K, Smith YR: Nicotinamide enhances skin flap survival. Scand J Plast Reconstr Surg Hand Surg 1989;23:177-179.
28.
Fivenson DP: The mechanisms of action of nicotinamide and zinc in inflammatory skin disease. Cutis 2006;77:5-10.
29.
Khanna-Gupta A, Berliner N: Vitamin B3 boosts neutrophil counts. Nat Med 2009;15:139-141.
30.
Tanno O, Ota Y, Kitamura N, Katsube T, Inoue S: Nicotinamide increases biosynthesis of ceramides as well as other stratum corneum lipids to improve the epidermal permeability barrier. Br J Dermatol 2000;143:524-531.
31.
Bissett D: Topical niacinamide and barrier enhancement. Cutis 2002;70:8-12; discussion 21-23.
32.
Soma Y, Kashima M, Imaizumi A, Takahama H, Kawakami T, Mizoguchi M: Moisturizing effects of topical nicotinamide on atopic dry skin. Int J Dermatol 2005;44:197-202.
33.
Bekier E, Wyczolkowska J, Szyc H, Maslinski C: The inhibitory effect of nicotinamide on asthma-like symptoms and eosinophilia in guinea pigs, anaphylactic mast cell degranulation in mice, and histamine release from rat isolated peritoneal mast cells by compound 48-80. Int Arch Allergy Appl Immunol 1974;47:737-748.
34.
Middleton E Jr, Devi A: Effect of nicotinamide on in vitro histamine release and slow-reacting substance formation in anaphylactically sensitized lung and its relation to acid-soluble nucleotides. J Allergy 1963;34:331-336.
35.
Parrot JL, Wyczolkowska Y, Santais MC, Ruff F, Mordelet-Dambrine M, Maslinski C: The action of nicotinamide on the release of histamine. Agents Actions 1974;4:202.
36.
Wyczolkowska J, Maslinski C: Inhibition by nicotinamide of a homologous PCA reaction and antigen-induced histamine release from isolated rat peritoneal mast cells. Agents Actions 1974;4:202-203.
37.
Wyczolkowska J, Maslinski C: Inhibition by nicotinamide of antigen-induced histamine release from mouse peritoneal mast cells. Int Arch Allergy Appl Immunol 1976;50:729-736.
38.
Yamasaki H, Muraoka S, Sugiyama M, Endo K: Mechanism of histamine-release inhibition by nicotinamide in in vitro antigen-antibody reaction. Jpn J Pharmacol 1961;11:54-64.
39.
Bekier E, Maslinski C: Antihistaminic action of nicotinamide. Agents Actions 1974;4:196.
40.
Nakama M, Murakami Y, Tanaka H, Nakata S: Decrease in nicotinamide adenine dinucleotide dehydrogenase is related to skin pigmentation. J Cosmet Dermatol 2012;11:3-8.
41.
Greatens A, Hakozaki T, Koshoffer A, Epstein H, Schwemberger S, Babcock G, Bissett D, Takiwaki H, Arase S, Wickett RR, Boissy RE: Effective inhibition of melanosome transfer to keratinocytes by lectins and niacinamide is reversible. Exp Dermatol 2005;14:498-508.
42.
Hakozaki T, Takiwaki H, Miyamoto K, Sato Y, Arase S: Ultrasound enhanced skin-lightening effect of vitamin C and niacinamide. Skin Res Technol 2006;12:105-113.
43.
Patam M, Jin XP, Pan JY, Shen GZ, Jin TY: The intervention of nicotinamide on skin melanocyte's cell proliferation after UVA (365 nm) exposed (in Chinese). Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi 2005;23:12-15.
44.
Patam M, Jin XP, Zhang YB, Pan JY, Shen GZ: Intervention of nicotinamide on skin melanin genesis after UVA exposed (in Chinese). Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi 2007;25:465-469.
45.
Burnett CL, Bergfeld WF, Belsito DV, Hill RA, Klaassen CD, Liebler DC, Marks JG Jr, Shank RC, Slaga TJ, Snyder PW, Andersen FA: Final report of the safety assessment of kojic acid as used in cosmetics. Int J Toxicol 2010;29:244S-273S.
46.
Shah NS, Mathur PP, Martin SP: Nicotinamide adenine dinucleotidase activity in experimental tuberculosis. Biochim Biophys Acta 1966;117:263-265.
47.
Murray MF: Nicotinamide: an oral antimicrobial agent with activity against both Mycobacterium tuberculosis and human immunodeficiency virus. Clin Infect Dis 2003;36:453-460.
48.
Greenstein RJ, Su L, Brown ST: Growth of M. avium subspecies paratuberculosis in culture is enhanced by nicotinic acid, nicotinamide, and alpha and beta nicotinamide adenine dinucleotide. Dig Dis Sci 2011;56:368-375.
49.
Moell A, Skog O, Ahlin E, Korsgren O, Frisk G: Antiviral effect of nicotinamide on enterovirus-infected human islets in vitro: effect on virus replication and chemokine secretion. J Med Virol 2009;81:1082-1087.
50.
Savarino A, Martini C, Orofino GC, Cantamessa C, Castelli L, Pich PG, Sinicco A, Pugliese A: Apoptotic DNA fragmentation, and its in vitro prevention by nicotinamide, in lymphocytes from HIV-1-seropositive patients and in HIV-1-infected MT-4 cells. Cell Biochem Funct 1997;15:171-179.
51.
Boshoff HI, Xu X, Tahlan K, Dowd CS, Pethe K, Camacho LR, Park TH, Yun CS, Schnappinger D, Ehrt S, Williams KJ, Barry CE 3rd: Biosynthesis and recycling of nicotinamide cofactors in Mycobacterium tuberculosis. An essential role for NAD in nonreplicating bacilli. J Biol Chem 2008;283:19329-19341.
52.
Zhang HS, Sang WW, Wang YO, Liu W: Nicotinamide phosphoribosyltransferase/sirtuin 1 pathway is involved in human immunodeficiency virus type 1 Tat-mediated long terminal repeat transactivation. J Cell Biochem 2010;110:1464-1470.
53.
Ciebiada-Adamiec A, Malafiej E, Ciebiada I: Inhibitory effect of nicotinamide on enzymatic activity of selected fungal strains causing skin infection. Mycoses 2010;53:204-207.
54.
Gupta KP: Effects of nicotinamide on mouse skin tumor development and its mode of action. Biomed Environ Sci 1999;12:177-187.
55.
Kim N, Yang A, Kirsner RS: Topical nicotinamide prevents UV immunosuppression. J Invest Dermatol 2008;128:250.
56.
Ludwig A, Dietel M, Schafer G, Muller K, Hilz H: Nicotinamide and nicotinamide analogues as antitumor promoters in mouse skin. Cancer Res 1990;50:2470-2475.
57.
Damian DL: Photoprotective effects of nicotinamide. Photochem Photobiol Sci 2010;9:578-585.
58.
Cosmetic Ingredient Review Expert Panel: Final report of the safety assessment of niacinamide and niacin. Int J Toxicol 2005;24(suppl 5):1-31.
59.
Hammar H: Epidermal nicotinamide adenine dinucleotides in psoriasis and neurodermatitis (lichen simplex hypertrophicus). Arch Dermatol Forsch 1975;252:217-227.
60.
Beningo KE, Scott DW, Miller WH Jr, Rothstein E: Observations on the use of tetracycline and niacinamide as antipruritic agents in atopic dogs. Can Vet J 1999;40:268-270.
61.
Hammar H: Epidermal nicotinamide adenine dinucleotides in psoriasis during treatment with dithranol. Arch Dermatol Forsch 1975;252:229-236.
62.
Levine D, Even-Chen Z, Lipets I, Pritulo OA, Svyatenko TV, Andrashko Y, Lebwohl M, Gottlieb A: Pilot, multicenter, double-blind, randomized placebo-controlled bilateral comparative study of a combination of calcipotriene and nicotinamide for the treatment of psoriasis. J Am Acad Dermatol 2010;63:775-781.
63.
Kademian M, Bechtel M, Zirwas M: Case reports: new onset flushing due to unauthorized substitution of niacin for nicotinamide. J Drugs Dermatol 2007;6:1220-1221.
64.
Draelos ZD, Ertel K, Berge C: Niacinamide-containing facial moisturizer improves skin barrier and benefits subjects with rosacea. Cutis 2005;76:135-141.
65.
Shalita AR, Smith JG, Parish LC, Sofman MS, Chalker DK: Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris. Int J Dermatol 1995;34:434-437.
66.
Dos SK, Barbhuiya JN, Jana S, Dey SK: Comparative evaluation of clindamycin phosphate 1% and clindamycin phosphate 1% with nicotinamide gel 4% in the treatment of acne vulgaris. Indian J Dermatol Venereol Leprol 2003;69:8-9.
67.
Draelos ZD, Matsubara A, Smiles K: The effect of 2% niacinamide on facial sebum production. J Cosmet Laser Ther 2006;8:96-101.
68.
Chiu PC, Chan CC, Lin HM, Chiu HC: The clinical anti-aging effects of topical kinetin and niacinamide in Asians: a randomized, double-blind, placebo-controlled, split-face comparative trial. J Cosmet Dermatol 2007;6:243-249.
69.
Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, Greatens A, Hillebrand GG, Bissett DL, Boissy RE: The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br J Dermatol 2002;147:20-31.
70.
Kimball AB, Kaczvinsky JR, Li J, Robinson LR, Matts PJ, Berge CA, Miyamoto K, Bissett DL: Reduction in the appearance of facial hyperpigmentation after use of moisturizers with a combination of topical niacinamide and N-acetyl glucosamine: results of a randomized, double-blind, vehicle-controlled trial. Br J Dermatol 2010;162:435-441.
71.
Moloney F, Vestergaard M, Radojkovic B, Damian D: Randomized, double-blinded, placebo controlled study to assess the effect of topical 1% nicotinamide on actinic keratoses. Br J Dermatol 2010;162:1138-1139.
72.
Gensler HL: Prevention of photoimmunosuppression and photocarcinogenesis by topical nicotinamide. Nutr Cancer 1997;29:157-162.
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