Mercaptopurine Tablets
Function and Efficacy
It is a cell cycle specific drug that inhibits the purine synthesis pathway. Its chemical structure is similar to that of hypoxanthine, so it can competitively inhibit the conversion process of hypoxanthine. After entering the body, this product must be converted into 6-mercaptopurine ribonucleotide by phosphoribosyltransferase in the cell before it becomes active. It has two main action links: (1) It inhibits amidotransferase through negative feedback, thereby preventing the conversion of 1-pyrophosphate-5-phosphoribosyl (PRPP) to 1-amino-5-phosphoribosyl (PRA), interfering with the initial stage of purine nucleotide synthesis. (2) Inhibits the mutual conversion between complex purines, that is, it can inhibit the conversion of inosine nucleotides to adenine nucleotides and inosine nucleotides to xanthine nucleotides and guanine nucleotides. At the same time, this product also inhibits the synthesis of coenzyme I (NAD) and reduces deoxyadenosine triphosphate (dATP) and deoxyguanosine triphosphate (dGTP) necessary for the biosynthesis of DNA, so that tumor cells cannot proliferate. This product is more sensitive to cells in the S proliferation cycle. In addition to inhibiting the synthesis of cell DNA, it also has a mild inhibitory effect on the synthesis of cell RNA. The use of mercaptopurine to treat leukemia often produces drug resistance, which may be due to the appearance of mutant leukemia cell lines in the body, which have lost the ability to convert mercaptopurine into mercaptopurine ribonucleotides.
Ingredients
The main ingredient of this product is: mercaptopurine.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| 6-MercaptopurineIngredients |
It is a cell cycle specific drug that inhibits the purine synthesis pathway. Its chemical structure is similar to that of hypoxanthine, so it can competitively inhibit the conversion process of hypoxanthine. After entering the body, this product must be converted into 6-mercaptopurine ribonucleotide by phosphoribosyltransferase in the cell before it becomes active. It has two main action links: (1) It inhibits amidotransferase through negative feedback, thereby preventing the conversion of 1-pyrophosphate-5-phosphoribosyl (PRPP) to 1-amino-5-phosphoribosyl (PRA), interfering with the initial stage of purine nucleotide synthesis. (2) Inhibits the mutual conversion between complex purines, that is, it can inhibit the conversion of inosine nucleotides to adenine nucleotides and inosine nucleotides to xanthine nucleotides and guanine nucleotides. At the same time, this product also inhibits the synthesis of coenzyme I (NAD) and reduces deoxyadenosine triphosphate (dATP) and deoxyguanosine triphosphate (dGTP) necessary for the biosynthesis of DNA, so that tumor cells cannot proliferate. This product is more sensitive to cells in the S proliferation cycle. In addition to inhibiting the synthesis of cell DNA, it also has a mild inhibitory effect on the synthesis of cell RNA. The use of mercaptopurine to treat leukemia often produces drug resistance, which may be due to the appearance of mutant leukemia cell lines in the body, which have lost the ability to convert mercaptopurine into mercaptopurine ribonucleotides. More |
50-44-2 | 10 |
Appearance
This product is light yellow tablet.
Indication
It is suitable for choriocarcinoma, malignant hydatidiform mole, acute lymphocytic leukemia, acute non-lymphocytic leukemia, and the blast crisis of chronic myeloid leukemia.
Usage and Dosage
1. Choriocarcinoma: Common dosage for adults: 6 mg to 6.5 mg/kg per day, taken orally in two divided doses. A course of treatment is 10 days, with an interval of 3 to 4 weeks. 2. Leukemia: (1) Initially, 2.5 mg/kg or 80 to 100 mg/m2 per day, taken once a day or in divided doses. Generally, significant effects can be seen 2 to 4 weeks after medication. If there is no clinical improvement and a decrease in white blood cell count after 4 weeks of medication, consider increasing the dosage to 5 mg/kg per day under careful observation; (2) Maintenance: 1.5 mg to 2.5 mg/kg or 50 mg to 100 mg/m2 per day, taken orally once a day or in divided doses.
Adverse Reactions
1. The most common is bone marrow suppression: there may be a decrease in white blood cells and platelets; 2. Liver damage: it can cause cholestasis and jaundice; 3. Digestive system: nausea, vomiting, loss of appetite, stomatitis, diarrhea, but it rarely occurs and can be seen in patients who take too much medicine. 4. Hyperuricemia: it is more common in the early stage of leukemia treatment, and severe cases may cause uric acid nephropathy; 5. Interstitial pneumonia and pulmonary fibrosis are rare.
Precautions
Patients with known hypersensitivity to this product are contraindicated.
Drug Interactions
1. When taken simultaneously with allopurine, the latter inhibits the metabolism of mercaptopurine, significantly increasing the efficacy and toxicity of mercaptopurine; 2. When this product is taken simultaneously with drugs that are toxic to hepatocellular cells, there is a risk of increased toxicity to hepatocellular cells; 3. When this product is used in combination with other anti-tumor drugs or radiotherapy that suppress the bone marrow, the effect of mercaptopurine will be enhanced, so it is necessary to consider adjusting the dosage and course of treatment of this product.
Storage
Keep in a light-proof and airtight container.
Packaging Specification
50mg
Manufacturer
Shanghai Sine Pharmaceutical Laboratories Co., Ltd.
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Founded in:
1993-10-23 -
Address:
No. 905, Xinjinqiao Road, China (Shanghai) Pilot Free Trade Zone -
Tax NO.:
91310000133742534B -
Registered Funds:
1,191,611,312 yuan -
Website:
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Email: