DL-ALPHA-LIPOIC ACID/R-ALPHA-LIPOIC ACID

Date

June 27, 2025

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

References: Proper names: NIH 2023; Common names: NIH 2023; Source information: NIH 2023.

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 oral use are indicated in the dosage form drop-down list of the web-based Product Licence Application form for Compendial applications.

Use(s) or Purpose(s)

• Source of (an) antioxidant(s)/Provides (an) antioxidant(s) (Borcea et al. 1999, Marangon et al.1999).
• Source of (an) antioxidant(s)/Provides (an) antioxidant(s) that help(s) fight/protect (cell) against/reduce (the oxidative effect of/the oxidative damage caused by/cell damage caused by) free radicals (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).

Note: If DL-alpha-Lipoic or R-alpha-Lipoic acid is combined with other medicinal ingredients with antioxidant properties at Class II and III, there is an option to use the claim in plural. The singular should be used when the product only contains one chemical substance as the medicinal ingredient associated with this claim.

Dose(s)

Subpopulation(s)

Adults 18 years and older

Quantity(ies)

DL-alpha-Lipoic acid

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).

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

R-alpha-Lipoic acid

Antioxidant

Not to exceed 300 milligrams of R-alpha-Lipoic acid*, per day.

Glucose metabolism

300 milligrams of R-alpha-Lipoic-acid*, per day.

*Note: The quantity of R-alpha-lipoic acid is calculated from the quantity of DL-alpha-lipoic acid (i.e. 50%).

Direction(s) for use

No statement required.

Combination rule

No permitted combinations between the two medicinal ingredients listed in this monograph.

Duration(s) of use

No statement required.

Risk information

Caution(s) and warning(s)

All products

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

Products providing 42 milligrams or more DL-alpha-lipoic acid or 21 milligrams or more R-alpha-lipoic acid, per day

Stop use and ask 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

Must be established in accordance with the requirements described in the Natural Health Products Regulations.

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.

EXAMPLE OF PRODUCT FACTS:

Consult the Guidance Document, Labelling of Natural Health Products for more details.

References cited

• Bae SM, Bae MN, Kim EY, Kim IK, Seo MW, Shin JK, Cho SR, Jeong GH. Recurrent Insulin Autoimmune Syndrome Caused by α-Lipoic Acid in Type 2 Diabetes. Endocrinol Metab (Seoul). 2013;28(4):326-330.
• Borcea V, Nourooz-Zadeh J, Wolff SP, Klevesath M, Hofmann M, Urich H, Wahl P, Ziegler R, Tritschler H, Halliwell B, Nawroth PP. Alpha-Lipoic acid decreases oxidative stress even in diabetic patients with poor glycemic control and albuminuria. Free Radical Biology & Medicine 1999;22(11/12):1495-1500.
• Bresciani E, Bussi A, Bazzigaluppi E, Balestrieri G. Insulin autoimmune syndrome induced by α-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;76:600-604.
• 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. 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 1999;27(3-4):309-314.
• Khanna S, Atalay M, Laaksonen DE, Gul M, Roy S, Sen CK. Alpha-lipoic acid supplementation: tissue glutathione homeostasis at rest and after exercise. Journal of Applied Physiology 1999;86(4):1191-1196.
• Konrad T, Vicini P, Kusterer K, Höflich A, Assadkhani A, Böhles HJ, Sewell A, Tritschler HJ, Cobelli C, Usadel KH. 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 1999;22(2):280-287.
• Marangon K, Devaraj S, Tirosh O, Packer L, Jialal I. Comparison of the effect of alpha- lipoic acid and alpha-tocopherol supplementation on measures of oxidative stress. Free Radical Biology & Medicine 1999;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. 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 2001;52(3):175-183.
• NIH 2023: National Institutes of Health. PubChem. Bethesda (MD): National Library of Medicine, US Department of Health & Human Services. [Accessed 2023 October 23]. Available from: https://pubchem.ncbi.nlm.nih.gov/
• Packer L, Witt EH, Tritschler HJ. Alpha-Lipoic acid as a biological antioxidant. Free Radical Biology & Medicine 1995;19(2):227-250.
• Reljanovic M, Reichel G, Rett K, Lobisch M, Schuette K, Möller W, Tritschler HJ, Mehnert H. 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 1999;31(3):171-179.
• Ruhnau KJ, Meissner HP, Finn JR, Reljanovic M, Lobisch M, Schütte K, Nehrdich D, Tritschler HJ, Mehnert H, Ziegler D. Effects of 3-week oral treatment with the antioxidant thioctic acid (alpha-lipoic acid) in symptomatic diabetic polyneuropathy. Diabetic Medicine 1999;16(12):1040-1043.
• Sola S, Mir MQ, Cheema FA, Khan-Merchant N, Menon RG, Parthasarathy S, Khan BV. 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 2005;111(3):343-348.

References reviewed

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

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