PuriNethol medicine 50mg
Pharmacological Group: Anticancer drugs and effects on the immune system
Brand Name: Mercaptoprine
Pharmacodynamics : Mercaptopurine is an anti-cancer drug and purine metabolite.
Pharmacokinetics:
- Absorption: Mercaptopurine is unevenly and incompletely absorbed from the gastrointestinal tract, but usually about 50% of the absorbed dose. The absolute bioavailability of oral mercaptopurin appears to be lower and very variable.
- Distribution: Mercaptopurin and its metabolites are distributed throughout the body’s water content. The volume of distribution of mercaptopurin often exceeds the amount of total water in the body. Although the drug crosses the blood-brain barrier, the concentration in the cerebrospinal fluid is not sufficient to treat meningococcal disease.
- Metabolism: Mercaptopurin is rapidly and rapidly oxidized in the liver to 6-thiouric acid by the enzyme xanthin oxydase. The sulfhydryl group of mercaptopurin can be methylated and then oxidized.
- Elimination : Mercaptoprin is excreted in the urine as unchanged drug and metabolites.
PuriNethol drug effects:
- Mercaptopurin is one of the purine analogs that prevents nucleic acid biosynthesis. Mercaptopurin competes with hypoxanthin and guanin for the enzyme hypoxanthin-guanin phosphoribosyltransferase (HGPRTase) and the drug itself is metabolized in the cell into a ribonucleotid, which functions as a purine antagonist. Eventually RNA and DNA synthesis is inhibited.
- Mercaptopurin is also a strong immunosuppressant, a strong inhibitor of the initial immune response, selective inhibition of humoral immunity, and also has a small inhibitory effect on cellular immune responses. revealed cross-resistance with drugs similar to mercaptopurin, thioguanin and 8-azaguanin.
- The most common in vitro drug resistance mechanism is the decline or complete lack of HGPRTase enzyme in cancer cells. In addition, resistance may be due to a decrease in enzyme affinity for its substrates.
Point :
Acute leukocytes, chronic myeloid leukemia, sarcom Also used to suppress immunity (to treat some autoimmune diseases).
Acute leukocytes, chronic myeloid leukemia, sarcom Also used to suppress immunity (to treat some autoimmune diseases).Contraindications:
- Severe neutropenia, thrombocytopenia accompanied by bleeding syndrome, liver damage. Breastfeeding.
Caution when using:
- – Only use the medication with the guidance and instructions of a physician.
- – Drugs that cause severe myelosuppression, must regularly check blood (especially leukopenia and thrombocytopenia, if sharply reduced to stop smoking). If carefully monitored and used at the right time, myelosuppression may be reversed with other full support.
- – Hepatotoxic drugs must be checked regularly for liver function weekly, if the jaundice is marked, discontinue the drug.
- – Monitor blood uric acid and urine levels to prevent risk of kidney disease.
- – The drug can cause mutations and chromosomal damage. The drug has the potential to cause cancer.
- – Not recommended for pregnant (weigh / benefit) and lactating people.
- – The drug causes anorexia, nausea, vomiting, mouth ulcers, fever, skin rash (rare).
Drug interactions :
- Allopurinol inhibits the oxidation of mercaptopurin by xanthinoxydase, thereby increasing the toxicity of mercaptopurin, especially causing marrow depression.
- Caution and strict monitoring of liver function in patients taking mercaptopurin concurrently with other hepatotoxic drugs.
- With other drugs: mercaptopurine has been shown to both increase and decrease the anticoagulant activity of warfarin.
Side effects
- The main and most serious toxic effect of mercaptopurin is myelosuppression and hepatotoxicity.
- Common: cholestasis in the liver, central lobular necrosis (manifested as hyperbilirubinemia, increased alkaline phosphatase, and GOT), jaundice, hyperpigmentation, hyperuricemia, nausea, vomiting, Diarrhea, stomatitis, anorexia, gastric and mucositis, leukopenia, thrombocytopenia, anemia (in high doses), kidney toxicity.
- Uncommon: Drug-induced fever, dry skin, desquamation rash, glossitis, tarry stools, eosinophilia.
Amount :
- Adults: 2-2.5mg / kg / 24 hours orally, in 2 divided doses. Use 3-4 weeks.
Overdose :
Overdose may occur immediately such as: anorexia, nausea, vomiting and diarrhea or slow as marrow failure, liver dysfunction and gastroenteritis.
- There is no antidote mercaptopurin.
- Hemodialysis does not remove mercaptopurin from the body.
- Treatment of overdose: Immediately stop the drug, can cause immediate vomiting, symptomatic treatment, if necessary, blood transfusions may be given.
Preservation:
- Poison Table A.
- Store mercaptopur tablets in a tightly closed vial, at a temperature of 15 – 25 degrees C in a dry place.
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Reference sources of mercaptopurine:
- The reputable source is compiled by index-china Purinethol 50mg Mercaptopurin accessed September 19, 2019.
- Source of Purinethol Medicines at Drugs.com accessed September 19, 2019.
- Source of Mercaptopurin Medicines at webmd.com accessed September 19, 2019.
- Source PuriNethol drug at rxlist.com accessed September 19, 2019.
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