Lipoic Acid(Cinderella Injection)
Lipoic acid(LA) is synonymous with thioctic acid and is approved as an insurance-covered treatment for diabetic peripheral neuropathy. In the pharmaceutical formulation, R type and S type coexist but only the R type is used in the body. Unlike other antioxidants, lipoic acid takes an oxidized form. After intravascular administration, oxidized lipoic acid immediately infiltrates into the intracellular fluid and bonds with hydrogen to form dihydrolipoic acid(DHLA). Unlike other antioxidants, both the oxidized form of LA and DHLA have antioxidant actions(Figure 4).
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Figure 4. Chemical structure of lipoic acid and DHLA.
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Oral lipoic acid is better absorbed on an empty stomach. Oral administration has about 30-40% absorption and the serum half-life is about 10-20 minutes. Lipoic acid is a very potent antioxidant that works both on hydrophilic and hydrophobic tissues.
Lipoic acid is a type of PDC(Pyruvate Dehydrogenase Complex). PDC consists of vitamins B1, B2, B3, B5 and lipoic acid. PDC is involved in energy metabolism and neural regeneration and improves insulin sensitivity. It is also involved in endothelial functions in diabetes and recovery of peripheral neuropathy.
Lipoic acid also has antioxidant actions on singlet oxygen and hydroxyl group, oxygen free radicals with strong mutagenicity. It tends to promote synthesis of glutathione and recovers(reduces) other antioxidants to repeat their beneficial actions(Figure 5).
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Figure 5. Recycle pathways of antioxidants by DHLA.
Lipoic acid is available in the 25mg 1A and in general, 1A-3A are diluted in 100ml saline solution or dextrose fluid to be administered in the fastest speed. One should be cautious in patients with vitamin B1 deficiency as IV lipoic acid can cause nausea and vomiting. I recommend combining lipoic acid with vitamin B1(nicknamed Garlic Injection).
-To be continued-
