What is Alpha Lipoic Acid?

Alpha lipoic acid is a coenzyme found in mitochondria, similar to vitamins, which eliminates free radicals that cause accelerated aging and disease. Lipoic acid enters cells after it is absorbed through the intestinal tract in the body and has both lipid-soluble and water-soluble properties.

As a coenzyme, lipoic acid plays a role in two key oxidative decarboxylation reactions, namely, pyruvate dehydrogenase complex and -ketoglutarate dehydrogenase complex, which catalyze the production and transfer of acyl groups. Lipoic acid can accept the acyl group of pyruvate and pyruvate to form a thioester bond, and then transfer the acetyl group to the sulfur atom of the CoA molecule. The dihydrolipoamide forming the prosthetic group can be oxidized by dihydrolipoamide dehydrogenase (needs NAD ⁺ ) to regenerate oxidized lipoamide. -lipoic acid contains a disulfide five-membered ring structure, has a high electron density, has a significant electrophilicity and the ability to react with free radicals, so it has antioxidant properties, has high health care functions and medical value (such as anti- Fatty liver and lowering plasma cholesterol). In addition, the thiol group of lipoic acid can easily undergo redox reaction, so it can protect the thiolase from the poison of heavy metal ions. Lipoic acid is widely distributed in nature, especially in liver and yeast cells. Lipoic acid is often present in food with vitamin B1. The human body can synthesize. Humans have not been found to have a deficiency of lipoic acid.

Chinese name: lipoic acid

Chinese alias: DL-Alpha-lipoic acid; DL--lipoic acid;

English name: lipoic acid

English alias: Lipoic acid; 1,2-Dithiolane-3-pentanoic acid; R-Alpha-Lipoic Acid;

CAS number: 62-46-4

Molecular formula: C ₈ H ₁₄ O ₂ S ₂

Molecular weight: 206.32600

Exact mass: 206.04400

PSA: 87.90000

LogP: 2.78510

At first, lipoic acid was used as a medicine for diabetes, so the Japanese Ministry of Health, Labour and Welfare classified it as a medicine, but in fact it has many functions in addition to curing diabetes, so in June 2004 Reclassification from medicine to food. Then let's introduce its function:

Stabilization of blood glucose level

Since it was originally treated as

Lipoic acid is a disulfide compound and is an essential factor for energy metabolism in human cells. The organism can synthesize it on its own, but the biochemical synthesis pathway has not been clearly studied.

Impact on diabetes

Lipoic acid is helpful in the treatment of various chronic diseases such as cardiovascular disease, diabetes, liver and kidney disease, and can reduce the incidence of fundus lesions and glaucoma in patients with diabetes.

Mechanism of Lipoic Acid:

The biochemical reactions involved in lipoic acid are mainly in the mitochondria, the energy center of the cell. Lipoic acid is also an essential factor in the glucose metabolism cycle of the human body. Although the human body can synthesize lipoic acid required for basic physiological reactions, the additional supplemental lipoic acid can significantly increase the sensitivity of cells with diabetes to insulin, increase the generation of ATP in the cell energy cycle, and improve the myocardial disease complicated by diabetes Have a positive meaning

In addition, lipoic acid is a non-hydrophilic antioxidant. However, lipoic acid can exert antioxidant effects in both water-soluble and water-insoluble environments. It is useful for diabetes and neuropathy caused by alcohol or chemically toxic substances. Therapeutic effect, but also helps to make a long-term transition to stimulated

Lipoic acid may increase the sensitivity of cells in patients with non-insulin-dependent (type 2) diabetes to insulin, so it may be necessary to reduce the dose of hypoglycemic drugs. Diabetics already taking hypoglycemic drugs, Within one to two weeks, it is best to monitor your blood sugar regularly to avoid low blood sugar.

Drug Name

Common name: Lipoic Acid Injection

English name: Thioctic Acid Injection

Phonetic script (Hanyu Pinyin): Liuxinsuan Zhusheye

[Ingredients]

Chemical name: (±) -5- [3- (1,2-dithiacyclopentane)]-pentanoic acid.

Chemical Structure:

Molecular formula: C ₈ H ₁₄ O ₂ S ₂

Molecular weight: 206.33

Ingredients: The main ingredient of this product is lipoic acid.

This product contains auxiliary materials: benzyl alcohol and ethylenediamine.

[Character]

The product is a light yellow clear liquid.

[Indications]

Paresthesia due to diabetic peripheral neuropathy.

specification

12ml: 0.3g.

Dosage

This product can be used for intravenous injection. Intravenous injection should be slow and the maximum rate is 50mg lipoic acid per minute (equivalent to 2ml of this injection). This product can also be added to saline intravenously, such as 250-500mg lipoic acid (equivalent to 10-20ml of this injection) added to 100-250ml physiological saline, the intravenous drip time is about 30 minutes.

Unless there is special medical order, patients with severe paresthesia caused by diabetic peripheral neuropathy can be administered by intravenous infusion, 300-600mg per day (equivalent to 12-24ml of this injection), a course of 2-4 weeks.

Adverse reactions

Intravenous infusion may cause bloating and dyspnea, but it can relieve itself. After using this product in a very few patients, convulsions, diplopia, purple epilepsy, and bleeding tendency due to abnormal platelet function occur.

There are very few cases of allergy to benzyl alcohol in this product.

[Taboo]

People who are allergic to this product.

Precautions

The prepared infusion is wrapped in aluminum platinum paper and protected from light, which can be stable for 6 hours. This product cannot be used in combination with glucose solution, Ringer's solution, and all solutions that may react with sulfur or disulfide bonds. In the treatment of diabetic peripheral neuropathy, control of diabetes itself is also necessary. Since the active ingredients are sensitive to light, the ampoules should be removed from the box before use.

[Medication for pregnant and lactating women]

Pregnant and lactating women should not use this product.

[Child medication]

This injection contains benzyl alcohol, so it cannot be used in newborns, especially premature infants.

[Medicine for the elderly]

There is no clinical need to adjust the dosage.

medicine interactions

This product may inhibit the efficacy of cisplatin.

[Drug overdose]

No related information.

[Pharmacology and Toxicology]

This product is widely used in the treatment of neuropathy in diabetes. In vitro tests have shown that this product can reduce the lipid oxidation of nerve tissues. This product may prevent the glycosylation of proteins; and it can inhibit aldose reductase, thus preventing the conversion of glucose or galactose to sorbitol, so lipoic acid Can prevent diabetes, control blood sugar and prevent neuropathy caused by hyperglycemia.

Lipoic acid is a powerful antioxidant in both water-soluble and oil-soluble matrices. Either lipoic acid or dihydrolipoic acid in its reduced form can exert an antioxidant effect. They can directly or indirectly promote the regeneration of vitamin C and vitamin E in the body. Studies have shown that lipoic acid can increase intracellular levels of glutathione and coenzyme Q10.

Lipoic acid can chelate certain metal ions (such as copper, manganese, zinc) to form stable chelate bodies. In animal models, it has been shown to protect arsenic poisoning and reduce liver toxicity after chromium poisoning. In vitro tests have also found that mercury ions can be chelated from kidney sections.

The product is safe in the range of clinical application doses. LD50 is 400-500 mg / kg when dogs are taken orally. For rats that are severely deficient in vitamin B1, 20 mg / kg can be fatal in animal experiments. There is not enough test data to ensure safe use for pregnant women. Clinical side effects are rare. Among the recorded side effects, skin sensitization is the main phenomenon, and medication should be stopped at this time.

Pharmacokinetics

Lipoic acid can be synthesized by the human body. Lipoic acid is easily reduced to dihydrolipoic acid in many body tissues after injection (injected or orally). Lipoic acid or dihydrolipoic acid can exert its pharmacological effects both inside and outside the cell.

Storage

Keep away from light and in a cool place (not more than 20 ).

package

Available in brown ampoules, 2 per box.

[Validity Period]

18 months

[Executive standards]

YBH01692005

Approval Number

National Medicine Standard H20053402 ^[3]