[Background and Overview][1][2]
Monoammonium glycyrrhizinate and diammonium glycyrrhizinate solvent are derivatives of the active ingredients of licorice and have the effect of protecting liver cells from damage. Monoammonium glycyrrhizinate is a β-body licorice derivative, and its anti-inflammatory, anti-allergic, protective membrane structure and immunomodulatory effects are well known. Diammonium glycyrrhizinate is the 18α body of glycyrrhizic acid. Monoammonium glycyrrhizinate, which is more lipophilic than the β body, easily binds to receptor proteins and target cell receptors of steroid hormones in the body. Animal experiments have shown that the drug can reduce the damage to the liver caused by carbon tetrachloride, and by blocking non-specific anti-inflammatory effects such as the liver inflammatory process caused by various cytokines released after liver damage, it can protect the membrane structure and reduce ALT.
Diammonium glycyrrhizinate is the third-generation extract of the active ingredient of traditional Chinese medicine licorice. It has strong anti-inflammatory effects, protects liver cell membranes and improves liver function. Pharmacological experiments have shown that oral administration of diammonium glycyrrhizinate to mice can reduce the increase in serum alanine aminotransferase and aspartate aminotransferase caused by carbon tetrachloride, thioacetamide and D-aminogalactic acid, and can also significantly reduce the increase in D-aminogalactic acid. Damage to the morphology of the liver and improve chronic damage to the morphology of the liver by immune factors. Diammonium glycyrrhizinate injection (Ganlixin) can significantly inhibit the metabolites of arachidonic acid (AA), leukotrienoic acids (LTs) and prostaglandin E2 (PGE 2) in liver tissue in a dose-dependent manner and has no effect on ALT. Direct inactivation. Studies have found that Ganlixin can inhibit the release of AA from cell membrane phospholipids or inhibit the activity of phospholipase A2 (PLA2), thereby reducing the metabolites of AA through cyclooxygenase and lipoxygenase, LTs and PGE2. In addition, diammonium glycyrrhizinate not only easily binds to target cells of steroid hormones, but also has a strong inhibitory effect on the activity of Δ4-5β-reductase, which can increase the level of intrahepatic lipocortin, which in turn can be affected by PLA2. Inhibition, producing dual physiological activities. Therefore, ganlixin may exert anti-hepatic damage effects by controlling inflammation.
[Indications][3]
Diammonium glycyrrhizinate has strong anti-inflammatory effects, improves liver cell damage caused by immune factors, and enhances the detoxification function of the liver. It also has the effects of anti-allergy, inhibiting calcium ion influx, immune regulation and inducing the production of gamma-interferon. It is mainly used for various types of chronic hepatitis and toxic liver damage accompanied by elevated ALT.
[Specifications][4]
Capsule: 50 mg; injection: 500 mg/10 ml.
【Usage and Dosage】[4]
Capsules: 50mg each; injection: 50mg/10ml each. Oral administration, 150 mg each time, 3 times a day; intravenously, add 30 ml of diammonium glycyrrhizinate into 250 ml of 10% glucose solution, dilute it and infuse slowly, once a day.
[Pharmacological effects and mechanism of action] [4]
Diammonium glycyrrhizinate is the third-generation extract of the active ingredient of licorice. It is a replacement product of Diantanin. It has strong anti-inflammatory, liver cell protection and liver function improvement effects; it can reduce the risk of tetrachloride in experimental animals. It can also significantly reduce the liver morphological damage caused by D-galactosamine and improve the chronic liver morphological changes caused by immune damage factors.
[Pharmacokinetics][4]
Diammonium glycyrrhizinate is not completely absorbed after oral administration, and its bioavailability is not affected by food; its plasma concentration reaches its peak 8 hours after oral administration; its active metabolite appears in the blood after 4 hours and reaches its peak at 12 hours. The blood concentration drops rapidly 1 hour after intravenous injection and reaches a low level after 24 hours. The binding capacity of diammonium glycyrrhizinate and its metabolites to protein is 92.5% and 98.4% respectively. It is mainly distributed in the liver, kidneys and lungs in the body. It is mainly excreted from bile into feces, part of it is excreted from respiratory tract as CO2, and only a small amount is excreted in urine.
[Adverse reactions][4]
1. A few patients may have elevated blood pressure, dizziness, headache, nausea, upper abdominal discomfort, abdominal distension, rash and fever, etc., but this does not affect treatment.
2. Blood pressure and serum potassium and sodium concentrations should be measured regularly during treatment. If high blood pressure, sodium retention, hypokalemia, etc. occur, administration should be suspended or the dose should be appropriately reduced.
3. It is contraindicated in patients with severe hypokalemia, hypernatremia, hypertension, heart failure, and renal failure. Pregnant women should not use it either. The dosage and adverse reactions for neonates, infants and young children have not been determined and are not used for the time being.
[Drugs for pregnant and lactating women][5]
Pregnant women should not use this product.
【Children’s Medication】[5]
The dosage and adverse reactions of neonates, infants and young children have not been determined and are not used for the time being.
[Drug Interaction][6]
When combined with diuretics (such as diuretic acid, furosemide, ethiazide, trichlorothiazide, etc.), its diuretic effect can enhance the potassium excretion effect of diammonium glycyrrhizinate, resulting in a decrease in serum potassium. Attention should be paid to the measurement of serum potassium levels.
[Main reference materials]
[1] Zhao Rong; Lu Ling. Progress in pharmacological research and clinical application of diammonium glycyrrhizinate. Asia Pacific Traditional Medicine, 2008, 4.3: 31-36.
[2] Deng Zhiping; Deng Zhiming; Deng Zhiqing; Qin Huaiguo CN201210209114.8 Diammonium glycyrrhizinate chloride
20120625
[3] Safe application and compatibility of injections
[4] Commonly used clinical drugs
[5] Rational use of drugs for digestive system diseases
[6] Safe application and compatibility of 452 injections
