DL-ALPHA LIPOIC ACID

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This monograph is intended to serve as a guide to industry for the preparation of Product Licence Applications (PLAs) and labels for natural health product market authorization. It is not intended to be a comprehensive review of the medicinal ingredient.

Notes

• Text in parentheses is additional optional information which can be included on the PLA and product label at the applicant's discretion.
• The solidus (/) indicates that the terms and/or statements are synonymous. Either term or statement may be selected by the applicant.

Date

June 3, 2019

Proper name(s), Common name(s), Source material(s)

Table 1. Proper name(s), Common name(s), Source material(s)

Proper name(s)	Common name(s)	Source ingredient(s)
		Common name(s)	Preparation
(+-)-1,2-Dithiolane-3-pentanoic acid DL-alpha-Lipoic acid	DL-alpha-Lipoic acid DL-Thioctic Acid	DL-alpha-Lipoic acid	Synthetic

References: Proper names: NIH 2016; Common names: NIH 2016; Source ingredient: NIH 2016.

Route of Administration

Oral

Dosage Form(s)

This monograph excludes foods or food-like dosage forms as indicated in the Compendium of Monographs Guidance Document.

Acceptable dosage forms for any age category listed in this monograph for the specified route of administration are listed in the Compendium of Monographs Guidance Document.

Use(s) or Purpose(s)

• Source of/Provides antioxidants (Borcea et al. 1999, Marangon et al.1999).
• Helps to promote healthy glucose metabolism (Morcos et al. 2001, Jacob et al. 1999, Konrad et al. 1999).

Dose(s)

Subpopulation(s)

Adults 18 years and older

Quantity(ies)

Antioxidant

Not to exceed 600 milligrams of DL-alpha-Lipoic acid, per day (Morcos et al. 2001, Borcea et al. 1999, Marangon et al.1999).

Glucose metabolism

600 milligrams of DL-alpha-Lipoic acid, per day (Jacob et al. 1999, Konrad et al. 1999).

Direction(s) for use

No statement required.

Duration(s) of Use

No statement required.

Risk Information

Caution(s) and warning(s)

All products

Consult a health care practitioner/health care provider/health care professional/doctor/physician prior to use if you are pregnant, breastfeeding or have diabetes (Jacob et al. 1999, Konrad et al. 1999, Packer et al. 1995).

Products providing 42 milligrams or more of DL-alpha lipoic acid, per day

Stop use and consult a health care practitioner/health care provider/health care professional/ doctor/physician if you experience sweating, paleness, chills, headache, dizziness and/or confusion (as these may be symptoms of serious low blood sugar) (Bae et al., 2013; Gullo et al., 2014; Bresciani et al., 2011; Chang et al., 2009).

Contraindication(s)

No statement required.

Known adverse reaction(s)

No statement required.

Non-medicinal ingredients

Must be chosen from the current Natural Health Products Ingredients Database (NHPID) and must meet the limitations outlined in the database.

Storage conditions

No statement required.

Specifications

• The finished product specifications must be established in accordance with the requirements described in the Natural and Non-prescription Health Products Directorate (NNHPD) Quality of Natural Health Products Guide.
• The medicinal ingredient must comply with the requirements outlined in the NHPID.

References Cited

• Bae SM, Bae MN, Kim EY, Kim IK, Seo MW, Shin JK, Cho SR, Jeong GH. Recurrent Insulin Autoimmune Syndrome Caused by ?-Lipoic Acid in Type 2 Diabetes. Endocrinol Metab (Seoul). 2013; 28(4):326-30.
• Borcea V, Nourooz-Zadeh J, Wolff SP, Klevesath M, Hofmann M, Urich H, Wahl P, Ziegler R, Tritschler H, Halliwell B, Nawroth PP. 1999. Alpha-Lipoic acid decreases oxidative stress even in diabetic patients with poor glycemic control and albuminuria. Free Radical Biology & Medicine 22(11/12):1495-1500.
• Bresciani E, Bussi A, Bazzigaluppi E, Balestrieri G. Insulin autoimmune syndrome induced by ?-lipoic acid in a Caucasian woman: case report. Diabetes Care. 2011 Sep;34(9):e146. doi: 10.2337/dc11-0600.
• Chang HJ, Choi HS, Park MY, Leem SM, Jang YS, Park KS, Lee JM. A case of insulin autoimmune syndrome related to alpha-lipoic acid. Korean J Med 2009; 76: 600-4.
• Gullo D, Evans JL, Sortino G, Ira D. Goldfine and Vigneri R. Insulin autoimmune syndrome (Hirata Disease) in European Caucasians taking a-lipoic acid. Clinical Endocrinology 2014; 81, 204-209.
• Jacob S, Ruus P, Hermann R, Tritschler HJ, Maerker E, Renn W, Augustin HJ, Dietze GJ, Rett
• K. 1999. Oral administration of RAC-alpha-lipoic acid modulates insulin sensitivity in patients with type-2 diabetes mellitus: a placebo-controlled pilot trial. Free Radical Biology & Medicine 27(3-4):309-314.
• Khanna S, Atalay M, Laaksonen DE, Gul M, Roy S, Sen CK. 1999. Alpha-lipoic acid supplementation: tissue glutathione homeostasis at rest and after exercise. Journal of Applied Physiology 86(4):1191-1196.
• Konrad T, Vicini P, Kusterer K, Höflich A, Assadkhani A, Böhles HJ, Sewell A, Tritschler HJ, Cobelli C, Usadel KH. 1999. Alpha-Lipoic acid treatment decreases serum lactate and pyruvate concentrations and improves glucose effectiveness in lean and obese patients with type 2 diabetes. Diabetes Care 22(2):280-287.
• Marangon K, Devaraj S, Tirosh O, Packer L, Jialal I. 1999. Comparison of the effect of alpha- lipoic acid and alpha-tocopherol supplementation on measures of oxidative stress. Free Radical Biology & Medicine 27(9/10):1114-1121.
• Morcos M, Borcea V, Isermann B, Gehrke S, Ehret T, Henkels M, Schiekofer S, Hofmann M, Amiral J, Tristschler H, Ziegler R, Wahl P, Nawroth PP. 2001. Effect of ¿alpha-lipoic acid on the progression of endothelial cell damage and albuminuria in patients with diabetes mellitus: an exploratory study. Diabetes Research and Clinical Practice 52(3):175-183.
• NIH 2016: National Institute of Health. [Internet]. [Accessed 2019 May 13]. Available from: http://chem.sis.nlm.nih.gov/chemidplus/rn/1077-28-7
• Packer L, Witt EH, Tritschler HJ. 1995. alpha-Lipoic acid as a biological antioxidant. Free Radical Biology & Medicine 19(2):227-250.
• Reljanovic M, Reichel G, Rett K, Lobisch M, Schuette K, Möller W, Tritschler HJ, Mehnert H. 1999. Treatment of diabetic polyneuropathy with the antioxidant thioctic acid (alpha-lipoic acid): a two year multicenter randomized double-blind placebo-controlled trial (ALADIN II). Alpha Lipoic Acid in Diabetic Neuropathy. Free Radical Research 31(3):171-179.
• Ruhnau KJ, Meissner HP, Finn JR, Reljanovic M, Lobisch M, Schütte K, Nehrdich D, Tritschler HJ, Mehnert H, Ziegler D. 1999. Effects of 3-week oral treatment with the antioxidant thioctic acid (alpha-lipoic acid) in symptomatic diabetic polyneuropathy. Diabetic Medicine 16(12):1040-1043.
• Sola S, Mir MQ, Cheema FA, Khan-Merchant N, Menon RG, Parthasarathy S, Khan BV. 2005. Irbesartan and lipoic acid improves endothelial function and reduce markers of inflammation in
• the metabolic syndrome: results of the Irbesartan and Lipoic Acid in Endothelial Dysfunction (ISLAND) study. Circulation 111(3):343-348.

References Reviewed

• Burekovic A, Terzic M, Alajbegovic S, Vukojevic Z, Hadzic N. 2008. The role of alpha-lipoic acid in diabetic polyneuropathy treatment. Bosnian Journal of Basic Medical Science 8(4):341- 345.
• Kamenova P. 2006. Improvement of insulin sensitivity in patients with type 2 diabetes mellitus after oral administration of alpha-lipoic acid. Hormones (Athens) 5(4):251-258.
• McIntyre RS, Soczynska JK, Lewis GF, MacQueen GM, Konarski JZ, Kennedy SH. 2006. Managing psychiatric disorders with antidiabetic agents: translational research and treatment opportunities. Expert Opinion on Pharmacotherapy 7(10):1305-1321.
• Mignini F, Streccioni V, Tomassoni D, Traini E, Amenta F. 2007. Comparative crossover, randomized, open-label bioequivalence study on the bioequivalence of two formulations of thioctic acid in healthy volunteers. Clinical and Experimental Hypertension 29(8):575-586.
• Sharman JE, Gunaruwan P, Knez WL, Schmitt M, Marsh SA, Wilson GR, Cockcroft JR, Coombes JS. 2004. Alpha-lipoic acid does not acutely affect resistance and conduit artery function or oxidative stress in healthy men. British Journal of Clinical Pharmacology 58(3):243- 248.
• Vincent HK, Bourguignon CM, Vincent KR, Taylor AG. 2007. Effects of alpha-lipoic acid supplementation in peripheral arterial disease: a pilot study. Journal of Alternative and Complementary Medicine 13(5):577-584.
• Zembron-Lacny A, Szyszka K, Szygula Z. 2007. Effect of cysteine derivatives administration in healthy men exposed to intense resistance exercise by evaluation of pro-antioxidant ratio. Journal of Physiological Science 57(6):343-348.
• Ziegler D, Ametov A, Barinov A, Dyck PJ, Gurieva I, Low PA, Munzel U, Yakhno N, Raz I, Novosadova M, Maus J, Samigullin R. 2006. Oral treatment with alpha-lipoic acid improves symptomatic diabetic polyneuropathy: the SYDNEY 2 trial. Diabetes Care 29(11):2365-2370.