Has antineoplastic and immunosuppressive effect. Is competitive antagonist of purine bases. It competes with hypoxanthine and guanine for hypoxanthine-guanine-phosphoribosyltransferase. Transformed into merkaptopurinfosforibozil that influenced tiopurinmetiltransferazy turns into metilmerkaptopurin. Both deca durabolin side effects inhibit 5-glutamine fosforibozilpirofosfatamidotransferazu – the first enzyme in the synthesis of purine ribonucleotides; as a result of impaired mitotic cycle (S-phase), especially in rapidly proliferating cells of the bone marrow and tumors, inhibited the growth of malignancies and is manifested cytotoxic effect. PharmacokineticsAbsorption after oral administration is variable, is about 50% on average. Communication with plasma proteins – about 20%. Poorly penetrates the blood-brain barrier and is found in the cerebrospinal fluid in small amounts. The half – phase: I phase – 47 minutes in adults and 21 minutes in children, II, and III phase – 2.5 and 10 hours, is quite rapid destruction associated with its inclusion in the pathway common to all purines. The pharmacological effect is largely due to metabolites, which excretion occurs via the kidneys by tubular secretion and glomerular filtration. The urinary metabolites obnaruzhivayutsyauzhe 2 hours after administration, 46% of the drug is excreted in the first day. Metabolites continue to be determined in the urine for several weeks after cessation of treatment;metabolites are pharmacologically active and have a greater half-life than the mercaptopurine. In the urine after oral administration are determined by: the unmodified drug, tiomochevaya acid (formed by direct oxidation with xanthine oxidase) and several methylated thiopurine. toxicity zoom joint appointment with allopurinol is associated with blockade xanthine oxidase and the latter, respectively, with the accumulation of the pharmacologically active substances.
Acute lymphoblastic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia and myeloblastic (remission induction and maintenance therapy).
: Hypersensitivity. Pregnancy and lactation.
Be wary – inhibition of bone marrow hematopoiesis, acute viral (including chicken pox, herpes zoster), fungal and bacterial diseases, renal and / or hepatic insufficiency, hyperuricemia, gout or urate nefrourolitiaz, age up to 2 years.
Dosing and Administration
Inside. For adults and children, the initial dose – 2-2.5 mg / kg or 80-100 mg / m² per day for 4 weeks; further adjusted depending on the effect and status of bone marrow hematopoiesis, the nature and dosage of other cytotoxic drugs, prescribed in combination with mercaptopurine. With good tolerability for 4 weeks and the effect of insufficient severity, the dose may be increased up to 5 mg / kg per day, but no more. Maintenance dose: 1.5-2.5 mg / kg or 75 mg / m per day. Children:. 2.5 mg / kg or 75 mg / m² per day
. The daily dose is appointed once or in several stages
At the first sign of severe leukopenia reception termination is recommended for 2-3 days. If during this time is not aggravated by leukopenia, resume treatment.
Patients with hepatic and / or renal insufficiency, the dose should be reduced.
In a joint application with allopurinol dose of mercaptopurine is reduced by 25-35%.
Side effect On the part of hematopoiesis: anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia From the digestive system: loss of appetite, nausea, vomiting, diarrhea, gepatonekroz, intrahepatic cholestasis (liver toxicity is toxic and allergic genesis and occurs more often in excess of the recommended dose 2.5 mg / kg / day), ulceration of the oral mucosa, rarely – ulceration of the intestinal mucosa, pancreatitis. Allergic reactions: skin rash, pruritus, rarely – drug fever. Other: decreased immunity, accession secondary infections, skin pigmentation, alopecia ., hyperuricemia, nephropathy, transient oligospermia deca durabolin side effects potential opportunities – mutagenicity, carcinogenicity.
Overdose Symptoms : immediate – nausea, vomiting, anorexia, diarrhea; deferred – myelosuppression, liver dysfunction, gastroenteritis. Treatment: symptomatic (no effective antagonist, hemodialysis practically ineffective). In the first 60 minutes after an overdose can cause vomiting and conduct gastric lavage.
Interaction with other medicinal products and other forms of interaction
When combined with drugs that block tubular secretion (especially with uricosuric drugs protivopodagricakih – probenecid, sulfinpyrazone, colchicine) increases the risk of developing nephropathy. Vincristine and methotrexate increase (each) Activity and Toxicity.
Allopurinol azatiaprin and reduce the intensity of metabolism mercaptopurine by xanthine oxidase blockade.
Enhances the effects of indirect anticoagulants, thereby increasing the risk of bleeding.
Drugs that suppress bone marrow hematopoiesis (including ko- trimoksozol), cytotoxic agents and radiation therapy increase the severity of leukopenia and thrombocytopenia.
while the use of corticosteroids, azathioprine, chlorambucil, corticotropin, cyclophosphamide and cyclosporine increases the risk of infections and secondary tumors (increased immunosuppressive action.)
simultaneous treatment with doxorubicin significantly increases the risk development of hepatotoxicity.
There cross-resistance of cells to mercaptopurine and thioguanine derivatives.
In combination with live virus vaccines can cause an intensification of the process of replication of the vaccine virus. Perhaps the increased side effects of vaccines and reducing the production of antibodies in response to the introduction, both live and inactivated vaccines.
. Mercaptopurine should only be used under the supervision of physicians experienced in the use of cytotoxic drugs
Treatment should be under the close supervision of the expanded blood count, as well as the “liver” tests (every week – at the start of treatment, every month – during maintenance therapy) and content . of uric acid in the blood serum
in applying mercaptopurine may experience delayed myelotoxic effect.
to prevent hyperuricaemia recommend drinking plenty of fluids, if necessary -. allopurinol and alkalinization of the urine
by reducing the number of leukocytes and platelets below an acceptable level, the propensity to bleeding, deca durabolin side effects or the appearance of jaundice mercaptopurine should be abolished.
during treatment of any sexual partners it is recommended to use reliable methods of contraception.
The drug can increase the risk of secondary malignancy and nephropathy (due to an increase in the formation of uric acid). Caution is advised when handling the tablets (for example, the separation of them in half) in order to avoid contamination of hands or by inhalation of the drug.
During the treatment, and for at least 3 months should abandon immunization and avoid contact with people who have received oral polio vaccine . Running low dose t3 clen cycle trying to lose bodyfat isn’t a real hot idea imo.