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Composition:


active ingredient: oxaliplatin;


1 vial contains 50 mg or 100 mg or 150 mg of oxaliplatin; 1 ml of reconstituted solution contains 5 mg of oxaliplatin;


excipient: lactose monohydrate.


Dosage form. Lyophilized powder for the preparation of a solution for infusions.


Basic physical and chemical properties: White freeze-dried powder.


Pharmacotherapeutic group.


Platinum derivatives. ATX code L01X A03.


Pharmacological properties.


Pharmacodynamics.


Oxaliplatin is an antineoplastic drug belonging to a new class of platinum-based compounds that contain a platinum atom complex with 1,2-diaminocyclohexane (DATSH) and an oxalate group.


Oxaliplatin is a separate enantiomer, CIS-[oxalate(trans-l-1,2-DATG) platinum].


Oxaliplatin exhibits a wide range of cytotoxicity in vitro and antitumor activity in vivo in various models of tumor systems, including models of human colorectal cancer. Oxaliplatin also demonstrates in vitro and in vivo activity in various cisplatin-resistant tumor models. A synergistic cytotoxic effect is observed in combination with 5-fluorouracil both in vitro and in vivo.


Studies of the mechanism of action of oxaliplatin, although they do not fully clarify the latter, demonstrate that water derivatives formed as a result of oxaliplatin biotransformation,


they interact with DNA to form both Inter-and intra-chain cross-links, which leads to a violation of DNA synthesis and causes cytotoxic and antitumor effects.


In patients with metastatic colorectal cancer, the efficacy of oxaliplatin (85 mg/m2 every 2 weeks) in combination with 5-fluorouracil/folic acid has been reported


(5-FU / FC) in three clinical trials.


Pharmacokinetics.


The pharmacokinetics of individual active compounds have not been studied. Pharmacokinetics of ultrafiltrable platinum, represented by a mixture of all free, active and inactive platinum varieties after a two-hour infusion of oxaliplatin at a dose of 130 mg/m2 every 3 weeks (from 1 to 5 cycles), and oxaliplatin at a dose of 85 mg/m2 every 2 weeks (from 1 to 3 cycles).


Biotransformation


In vitro biotransformation is thought to be the result of nonenzymatic decomposition, and there is no evidence of cytochrome P450-mediated metabolism of the diaminocyclohexane (DATSH) ring.


Oxaliplatin undergoes extensive biotransformation in the body of patients, the drug in unchanged form was not found in the plasma ultrafiltrate after the end of the two-hour infusion. Several cytotoxic biotransformation products, in particular monochlor -, Dichlor -, and diaqua-DATG platinum compounds, have been identified in the systemic circulation along with a number of inactive conjugates at later time points.


Elimination


Platinum is mainly excreted in the urine; clearance is observed mainly during


48 hours after administration. By day 5, approximately 54% of the total dose is excreted in the urine and


A significant decrease in clearance from 17.6 ± 2.18 L/h to 9.95 ± 1.91 L/H was observed in renal failure, along with a statistically significant decrease in the volume of distribution from 330 ± 40.9 to 241 ± 36.1 L. the effect of severe renal damage on platinum clearance was not studied.


Clinical characteristics.


Indications.


In combination with 5-fluorouracil (5-FU) and folinic acid (FC), oxaliplatin is indicated for:


 adjuvant therapy of Stage III (Duke stage C) colon cancer after complete removal of the primary tumor;


§ treatment of metastatic colorectal cancer.


Contraindications.


Oxaliplatin is contraindicated in patients:


* with a known history of hypersensitivity to the active substance or to any of the excipients;


* breast-feeding;


* with myelosuppression before the start of the first course of treatment, which is indicated by the initial neutrophil level x 109 / L and / or platelet count x 109 / L;


* with the presence of peripheral sensory neuropathy with functional impairment before the first course of treatment;


* with severe renal insufficiency (creatinine clearance


Special security measures.


Instructions for use and destruction.


As with other potentially toxic substances, caution should be exercised when using and preparing oxaliplatin solutions.


According to the rules of the medical institution, the preparation of injectable solutions of cytotoxic agents is carried out by experienced specialists who have knowledge of the drug used in conditions that guarantee Environmental Protection and especially the protection of personnel who administer the drug. You need a separate area for preparing the drug. It is forbidden to smoke, eat or drink in the preparation area of the drug.


Personnel should be provided with appropriate protective materials, namely: long dressing gowns with sleeves, protective masks, caps, safety glasses, sterile disposable gloves, a protective coating of the work area, containers and waste collection bags.


Excrement and vomit should be treated with caution.


Pregnant women should be warned about the dangers of using cytotoxic agents and working with them.


Damaged packaging should be handled with care and treated as contaminated waste. Contaminated waste should be incinerated in suitable labeled rigid containers.


If oxaliplatin powder, concentrate solution, or diluted infusion solution gets on the skin, it should be rinsed immediately and thoroughly with water. If oxaliplatin powder, concentrate solution, or infusion solution gets on the mucous membranes, they should be immediately and thoroughly rinsed with water.

Recycling.


Drug residues and all items used for the dissolution, dilution and administration of oxaliplatin must be destroyed in accordance with standard hospital procedures for the disposal of cytotoxic substances in accordance with the current legislation on the disposal of hazardous waste.

Dosage and administration.


Reconstituted solution-concentrate in the original bottle


For microbiological and chemical reasons, the reconstituted concentrate solution should be diluted immediately.


Solution for infusion after dilution


After dilution of the reduced concentrate solution with 5% glucose solution, chemical and physical stability was demonstrated for 24 hours at a temperature of 2-8 °C.


From a microbiological point of view, the product should be used immediately. If the solution was not used immediately, the user is responsible for the duration and storage conditions, which should not exceed 24 hours at a temperature of 2-8 °C.


The drug is intended for the treatment of adults only.


The recommended dose of oxaliplatin for adjuvant therapy is 85 mg/m2 intravenously with repeated doses every 2 weeks for 12 cycles (6 months).


The recommended dose of oxaliplatin for the treatment of metastatic colorectal cancer is 85 mg/m2 intravenously with repeated doses every 2 weeks.


Doses should be adjusted for tolerability (see "application features").


Oxaliplatin should always be administered earlier than fluoropyrimidines, such as 5-fluorouracil.


Oxaliplatin should be administered as an intravenous infusion lasting 2-6 hours in 250-500 ML


5% glucose solution to provide concentrations from 0.2 mg/mL to 0.7 mg/mL; 0.7 mg/mL is the highest concentration in clinical practice for an oxaliplatin dose of 85 mg/m2.


Oxaliplatin should be used mainly according to the scheme based on continuous infusion


5-fluorouracil. If a 5-fluorouracil regimen is used, combine bolus administration and continuous infusion of 5-fluorouracil every 2 weeks.


Special patient groups


Patients with impaired renal function.


Studies of oxaliplatin involving patients with severe renal impairment have not been conducted. Treatment of patients with moderate kidney damage can be started at the usual recommended dose (see "special instructions for use"). There is no need for dose adjustment for patients with mild renal impairment.


Patients with liver damage.


In the Phase I study, which included patients with varying levels of liver damage, the frequency and severity of hepatobiliary disorders may have been associated with progressive disease and abnormal liver test results at the start of the study. In the course of clinical studies, no special dose adjustment was performed for patients with impaired liver function.


Elderly patients.


There was no increase in the incidence of severe toxicity with oxaliplatin as monotherapy or in combination with 5-fluorouracil in patients over 65 years of age. Therefore, there is no need for special dose adjustment for elderly patients.


Method of application


Oxaliplatin should be administered as an intravenous infusion. Administration of oxaliplatin does not require prior hydration. Oxaliplatin should be administered through the central venous line or peripheral vein diluted in 250-500 ml of 5% glucose solution to ensure a concentration of at least 0.2 mg/mL; the infusion duration should be 2-6 hours. Oxaliplatin infusion should always be administered before 5-fluorouracil infusion.


In case of extravasation, the drug should be stopped immediately.


Special safety measures for use


* It is not allowed to use equipment containing aluminum for injection;


· It is not allowed to administer the drug undiluted;


* dilute only 5 % glucose solution for infusions (50 mg / mL);


* It is not allowed to dilute oxaliplatin with sodium chloride solution or solutions containing chlorine;


* Extravasal administration should be avoided;


* It is not allowed to mix with other medicines in the same infusion bottle or be administered simultaneously in the same infusion line;


* It is not allowed to mix oxaliplatin with alkaline drugs or solutions, in particular 5-fluorouracil, folinic acid preparations containing trometamol as an auxiliary substance, and salts of trometamol and other active substances. Alkaline drugs or solutions negatively affect the stability of oxaliplatin.


Instructions for use with folinic acid (calcium folinate or disodium folinate).


Oxaliplatin at a dose of 85 mg/m2, diluted in 250-500 ml of 5% glucose solution (50 mg/mL), is administered by intravenous infusion simultaneously with an intravenous infusion of folinic acid diluted in 5% glucose solution; the duration of the infusion is 2-6 hours and is carried out through the Y-line established immediately before the infusion.


These two medications are not allowed to be mixed in the same infusion bottle. Folic acid should not contain trometamol as an auxiliary substance, and it should only be diluted with an isotonic 5% glucose solution, and never use alkaline solutions or solutions containing chlorine, including sodium chloride, for dilution.


Instructions for use with 5-fluorouracil.


Oxaliplatin should always be administered before Administration of fluoropyrimidines, such as


5-fluorouracil.


After oxaliplatin administration, the system should be washed and then 5-fluorouracil should be administered.


For more information about the combination of drugs with oxaliplatin, see the brief description of the drug from the respective manufacturers. 


Any ready-made solution in the presence of mechanical inclusions is not allowed to be introduced, such a solution must be destroyed in accordance with the current legislation on the disposal of hazardous waste (see "disposal").


Preparation of a powder concentrate solution


* To prepare the concentrate solution, use water for injection or a 5% glucose solution (50 mg/mL).


* Add 10 ml of solvent to a 50 mg vial to obtain an oxaliplatin concentration of 5 mg/mL.


* Add 20 ml of solvent to a 100 mg vial to obtain an oxaliplatin concentration of 5 mg /mL.


* Add 30 ml of solvent to a 150 mg vial to obtain an oxaliplatin concentration of 5 mg /mL.


Dilution before infusion


Take the required amount of concentrate solution from the bottle (s) and then dilute


250-500 ml of 5% glucose solution to ensure oxaliplatin concentrations from 0.2 mg/mL to 0.7 mg/mL – the range of concentrations for which the physico-chemical stability of oxaliplatin has been demonstrated.


Administration by intravenous infusion


After diluting the concentrate solution in 5% glucose solution, chemical and physical stability was demonstrated for 24 hours at a temperature of 2-8 °C. From a microbiological point of view, the infusion solution should be used immediately. If the solution was not used immediately, the user is responsible for the duration and storage conditions, which should not exceed 24 hours at a temperature of 2-8 °C.


Before Administration, the solution must be examined. Only a clear solution without mechanical inclusions is suitable for use. For one-time use only. Any unused medicinal product must be destroyed (see the "disposal"section below).


Never use a sodium chloride solution to prepare a reconstituted concentrate or diluted solution.


The compatibility of oxaliplatin infusion solution with a typical sample of a PVC infusion system was tested.


Infusion


Administration of oxaliplatin does not require prior hydration. Oxaliplatin should be administered through the central venous line or peripheral vein diluted in 250-500 ml of 5% glucose solution to ensure a concentration of at least 0.2 mg/mL; the infusion duration should be 2-6 hours. Oxaliplatin infusion should always be performed before the infusion


5-fluorouracil.


Children. The drug is intended for use only in adult patients.


Overdose.


The antidote for oxaliplatin is unknown. In case of overdose, there may be an increase in the severity of side effects. It is necessary to carry out hematological monitoring simultaneously with symptomatic treatment of other manifestations of intoxication.

Tags: Oxaliplatin