Pharmacological properties masteron enanthate is a bifunctional alkylating agent belonging to chloroethylamino group. The process consists in the alkylation covalent svyazshanii formed of two bis-2-chloroethyl group carbon intermediates with guanine in position 7 and the DNA cross-linking of two DNA strands, resulting in the disruption of cell replication. Active against quiescent and actively dividing tumor cells. Pharmacokinetics Absorption of the drug when administered incomplete and variable: the time of detection of drug in plasma ranges from 0 to 336 minutes (due to the variable absorbability in the digestive tract, the rapid hydrolysis and the presence of the effect of “first pass” through the liver ) and concentration peak value – from 70 to 630 ng / ml. The bioavailability ranges from 25% to 89%, averaging 61%. Upon receiving masteron enanthate oral dose of 0.2-0.25 mg / kg body weight of the maximum plasma concentration (87-350 ng / ml) was observed after 0.5-2,0 hours Connection to plasma proteins -. 60-90%, about 30 % binds irreversibly. The volume of distribution – 0.5 l / kg. It is metabolized to inactive metabolites in body fluids and tissues. The average half-life -. 1.12 hr ± 0.15 When receiving Alkeran tablets directly after a meal time to reach maximum concentration increases, and the area under the curve ( “Plasma concentration – time”) is reduced by 39-45%. Excreted by the kidneys – 50% (10-15% unchanged), with faeces – 20-50%. Not removed by hemodialysis.
- multiple myeloma
- Advanced ovarian cancer
- polycythemia vera
- Hypersensitivity to masteron enanthate and other components of the tablets.
- Pregnancy and lactation
Precautions: condition after radiotherapy, preceded cytostatic therapy, anemia, leukopenia (white blood cell count below 2000 cells / mm), thrombocytopenia (less than 50,000 / microliter), chickenpox, herpes zoster and other infections, end-stage disease;. heavy comorbidities: parenchymal hepatitis, arthritis, gout, urate nephropathy, nephritis and diseases of the cardiovascular system in the stage of decompensation.
Dosing and Administration
Inside. When receiving the tablets should not be divided into parts.
The absorption of oral masteron enanthate after variable. If necessary, the dose can be gradually increased until myelosuppression characteristics so as to provide therapeutic concentration of the drug. Multiple myeloma Generally, the dose is 0.15 mg / kg body weight per day (taken in divided doses) for 4 days at intervals of 6 weeks. For more information on using other regimens is recommended to refer to the literature. In some regimens further include prednisolone, which increases the effectiveness of the treatment compared with monotherapy Alkeran, combination therapy is usually performed intermittent courses. Long-term therapy over one year does not improve results. ovarian cancer progressing Generally, the dose is 0.2 mg / kg of body weight per day for 5 days. Courses are repeated every 4-8 weeks or whenever the recovery of bone marrow function. Polycythemia for remission induction drug typically administered at a dose of 6-10 mg / day. for 5-7 days, then dose reduced to 2.4 mg / day. to achieve a therapeutic effect. For maintenance therapy, the drug is prescribed in a dose of 2-6 mg once a week. Use in children Alkeran in the usual range of doses used in children only rarely, so the specific dosing recommendations are not available. Use in elderly patients Alkeran is frequently used in elderly persons age in the general range of doses, with caution due to a possible reduction in kidney, liver, heart, and simultaneously the therapy of opportunistic diseases. Special information for use in patients in this age group do not have the drug. Use in patients with renal insufficiency clearance Alkeran in renal failure can be reduced. Existing data on the pharmacokinetics does not support the absolute need to reduce the dose Alkeran in patients with renal impairment, but it is advisable in the early stages of treatment to determine its tolerability in the therapy reduced doses. Patients in this case should be kept under close supervision. The starting dose is adjusted to the clearance of creatinine; subsequent doses determined in accordance with the response from the peripheral blood.
Side effect On the part of hematopoiesis: leukopenia, thrombocytopenia, rarely – anemia. On the part of the liver and the digestive system: nausea, vomiting (30%), diarrhea, stomatitis, gastric ulcer and duodenal ulcer (the risk of these side effects is greatly enhanced during combined tsytostaticheskoy therapy), rarely – liver dysfunction, clinically manifested hepatitis or jaundice. Allergic reactions: hives, swelling, skin rash, anaphylactic shock. The respiratory system: rarely – interstitial pneumonitis and pulmonary fibrosis. Other: hyperuricemia, seldom – alopecia very rarely – hemolytic anemia. Perhaps the development of amenorrhea and azoospermia. Patients with the original signs of renal failure in patients receiving masteron enanthate in the early stages of treatment a marked transient increase urea levels in blood serum. Against the background of leukopenia / neutropenia may develop secondary infections. Melfapan (like other antitumor alkylating agents) during prolonged use can cause the development of acute leukemia.
The most likely early manifestations of acute overdose Alkeran ingestion are disorders of the gastrointestinal tract, including nausea, vomiting and diarrhea. The main toxic effect of masteron enanthate is to suppress the bone marrow with the development of leukopenia, thrombocytopenia and anemia. Treatment – symptomatic. There is no specific antidote. Careful monitoring of peripheral blood counts for at least 4 weeks after the overdose until there are signs of normalization.
Interaction with other medicines and other forms of interaction
Co-administration with nalidixic acid in children can lead to death due to the development of hemorrhagic enterocolitis.
Chlorpromazine, chloramphenicol and sodium metamizole mielodepressivnogo increase the severity of the action.
Cisplatin induced renal failure and reduces the clearance of masteron enanthate. Cyclosporin and high doses of masteron enanthate are a potentially dangerous combination because of the possible development of renal dysfunction (itself nephrotoxic drug does not possess).
In simultaneous reception with live virus vaccines is possible intensification of the process of replication of vaccine virus, increasing its side / adverse effects and / or reduction of antibody in the patient in response to the vaccine.
Alkeran should be used only under the supervision of a physician who is experienced in the use of anticancer drugs.
Since Alkeran is a potent myelosuppressive agent, it is necessary to carry out regular monitoring of blood cell composition in order to prevent possible development of excessive myelosuppression and the risk of irreversible bone marrow aplasia. The number of blood cells may continue to fall after discontinuation of the drug, so at the first sign too sharp decline in the number of white blood cells or platelets, treatment should be temporarily discontinued.
Alkeran should be used with caution in patients who recently have undergone radiation therapy or chemotherapy, for the opportunity to gain toxic effect on bone marrow.
in appointing the patients with multiple myeloma and related chronic renal failure may be a temporary increase in urea in the plasma.
For the prevention of hyperuricemia is recommended to drink plenty of liquids, alkalizing urine drugs, allopurinol.
Need refusal of immunization (if it is not approved by the physician in the range of 3 months to 1 year after drug administration).; other members of the patient’s family, residing with him, should abandon immunization oral polio vaccine (to avoid contact with people who received the polio vaccine or wearing a protective mask that covers the nose and mouth).
If you use Alkeran should implement the recommendations on the use of cytotoxic drugs.
Women and men during treatment with Alkeran and for at least 3 months. after it should use reliable methods of contraception.