Background and overview[1][2]
Calcium dibutyryl cyclic adenosine monophosphate is a new type of nucleotide derivative. It plays an important role in the body as a G protein-coupled receptor drug. G protein is a type of protein that exists in the cell membrane. The inner regulatory protein is a trimer composed of three different subunits a, β, and γ. It regulates GTPase activity, activates phospholipase C (PLC), regulates Ca2+, K+ plasma channels, and regulates guanosine Acid cyclase also has an activating effect and mediates a variety of effects. Recently, it has been found that G protein also mediates the activation of phospholipase A2 (PLA2) to produce arachidonic acid (AA). Therefore, as a G protein-coupled receptor, Calcium dibutyryl cyclic adenosine monophosphate naturally plays an important role in the body and is used clinically to treat coronary heart disease. Protein dysfunction can manifest as increased or decreased function, which can lead to certain cardiovascular diseases such as angina pectoris, myocardial infarction, myocarditis, cardiogenic shock, immunogenetic diseases such as lupus erythematosus, psoriasis, infectious diseases and tumors. Such as: hepatitis, acute leukemia, etc. Calcium dibutyryl cyclic adenosine monophosphate can treat various diseases caused by G protein dysfunction.
Calcium adenosine diphosphate can catalyze the most basic biochemical metabolism in the human body – oxidative phosphorylation reaction and tricarboxylic acid cycle, activate most proteins and enzymes, activate various reactions in the human body, and produce a large amount of ATP at the same time , improve cell and energy metabolism, thereby achieving its effects of promoting nerve regeneration, transforming abnormal cells, dilating blood vessels, relaxing smooth muscles, and improving myocardial ischemia.
Calcium dibutyryl cyclic adenosine monophosphate is a protease activator that can activate protein kinase A and protein kinase C at the same time (cAMP only activates protein kinase A). Protein kinase is an allosteric enzyme composed of two catalytic subunits and It consists of 2 regulatory subunits, and the catalytic subunit has the function of catalyzing protein (or enzyme) phosphorylation. Therefore, calcium dibutyryl cyclic adenosine monophosphate can catalyze the most basic biochemical metabolic oxidative phosphorylation reaction and tricarboxylic acid cycle in the human body, activate most proteins and enzymes, and activate various reactions in the human body. At the same time, a large amount of ATP is produced to improve cell or energy metabolism. In this way, it can promote nerve regeneration, transform abnormal cells, expand blood vessels, relax smooth muscles, and improve myocardial hypoxia and ischemia.
Character
This product is a light yellow powder; it has a special odor and is easily soluble in water and ethanol, but insoluble in ether.
Pharmacological effects【3】
This product is a chemically synthesized derivative of cyclic adenosine monophosphate. It has the same pharmacological effects as cyclic adenosine monophosphate, but the latter does not pass through the cell membrane, and cAMP entering the cell is quickly hydrolyzed by phosphodiesterase. The cerium compound of cAMP, calcium dibutyryl cyclic adenosine monophosphate, is more permeable to cells than cAMP and can resist the degradation of phosphodiesterase in the body, so its action time and speed are longer and faster than cAMP.
Indications
This product can be used to treat angina pectoris, acute myocardial infarction, myocarditis, cardiogenic shock and psoriasis, and can assist in the treatment of leukemia.
Use
This crystal is a sanitary product of cyclic adenosine monophosphate and a protein kinase activator. Cyclic adenosine dibutyryl monophosphate is more permeable to cells than cAMP and can resist the destructive effect of phosphodiesterase in the body, so its action time and speed are longer and faster than cAMP. Mainly used for angina pectoris, acute myocardial infarction, myocarditis, cardiogenic shock, and also used for psoriasis.
Usage and dosage【4】
Coronary heart disease: intramuscular injection, 20 mg twice a day; intravenous infusion, 40 mg each time dissolved in 5% glucose injection 500 mi, once a day, 15 days as a course of treatment. Rheumatic heart disease: Dissolve 20 mg of this crystal in 10 ml of normal saline injection. Select acupoints at Zusanli on both sides. First, acupuncture the acupoints. If there is a feeling of soreness and bloating, inject 1 ml of each, that is, a total of 4 mg, once a day, 15 times. Each time is 1 course of treatment. Psoriasis: intravenous infusion, 60-80rr of this product is dissolved in 500ml of 5% glucose injection, once a day, 2-3 weeks as a course of treatment. Leukemia: It can be used to induce remission of acute leukemia. It is especially suitable for some patients with low peripheral white blood cell count and who are temporarily not suitable for chemotherapy with other drugs. It can be used with chemotherapy; intramuscular injection, 2 times a day, 20 mg each time; in severe cases, intravenous infusion, 40 mg of this crystal is dissolved in 500 ml of 5% glucose injection, and one month is a course of treatment.
Adverse reactions
Dizziness, drowsiness, nausea, vomiting, joint pain, etc. may occasionally occur.
Notes
During the treatment process, taking the phosphodiesterase inhibitor Hanwha PVC paste resin aminophylline 0.1g orally three times a day can increase the efficacy of this drug.
Dosage form specifications
Injection: 20rug.
Preparation
Add 200 L anhydrous ethanol to the above 1, stir until completely dissolved (a); weigh 28.26 g anhydrous calcium chloride, dissolve in 75 mL 50% ethanol (b). Slowly add solution b to In a, continue stirring at room temperature for 10 min, and then distill under reduced pressure until dryness. The crude product is 120.2 g. The above solid was dissolved in 250 mL of absolute ethanol, cooled in an ice-water bath, 1 800 mL of absolute ether was added dropwise, and continued stirring for 3 h, white crystals precipitated. Filter and wash the filter cake with anhydrous ether (50 mL×2), P: 0. Dry in vacuum overnight to obtain 2111.8 g, purity 98.8% (HPLC normalization method, as shown in Figure 2), content 97.5% (paper chromatography) system, the total yield was 72.1%. Confirmation of molecular weight by LC-MS determination.
References
[1]Huang Zhenhui;Zhang Zhigang;[F]Chinese patent: CN1554358.2004-12-15
[2] Zhang Renyou. Clinical observation on the application of calcium dibutyryl cyclic adenosine monophosphate [J]. Shanxi Medical Journal, 2004(09):754.
[3] Shen Yunsun, Sun Rentong, Chen Tonghui, Shanghai Practical Handbook of Drugs, Wenhui Publishing House, July 1992, first edition, page 1055
[4] Zhang Chuanhai Ding Yuanjing Chu Xiuying Editor-in-chief Gong Weiliang Wang Antioxidant 1010 Chunxiang Wang Haixia Sun Yunfeng Zhang Zipu Li Xiuzhen Li Chengyan Yang Ping Chen Xiyun Zhao Yushan Xu Aihong Huang Chuanying Xue Youyan Ju Yongcai Deputy editor-in-chief Ju Fuxia, Practical Circulatory System Drug Handbook, Jilin People’s Publishing House, 2006 April 1st edition, page 114
