Choloxan powder for infusion solution 2g vial, 1pc

Composition

1 bottle contains:

Active partnerships:

ifosfamide 2 g.

In a bottle of 2 g of powder.

In a cardboard box 1 bottle.

Pharmacological action

Pharmacodynamics

Ifosfamide is an alkylating cytostatic agent from the nitrogenous mustard gas group, a derivative of oxazaphosphorins. The antitumor activity of ifosfamide is caused by alkylation of nucleophilic centers, disruption of DNA synthesis, and blocking of mitotic division of tumor cells. DNA damage most often occurs in the G1 and G2 phases of the cell cycle.

Pharmacokinetics

After intravenous use, the Active ingredient, which is a prodrug (inactive transport form), is metabolized to the pharmacologically active metabolite 4-hydroxyphosphamide. It is activated by enzymes (phosphoamidase) of the liver and tumor tissue. In patients with impaired liver function, activation is slowed or even reduced.

After a single intravenous injection of 5 g/m2, the plasma concentration decreases bioexponentially, with T1 / 2 of the final phase-15 hours and elimination of 61% of the dose unchanged; at lower doses (1.6-2.4 g/m2), elimination proceeds monoexponentially, with T1/2 about 7 hours, while the proportion of unchanged drug in the urine decreases 4-5 times (12-18% of the dose).

Indications

• Germinogenic tumors; ovarian
• cancer;testicular malignancies;
• lung cancer
• ;breast cancer;
• pancreatic
• cancer;endometrial
• cancer;cervical cancer;
• malignant lymphomas;
• soft tissue sarcomas;
• osteogenic sarcomas;
• Wilms ‘ tumor;
• Ewing’s sarcoma.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Contraindications

• Severe bone marrow suppression;
• severe renal impairment;
• urinary tract obstruction;
• cystitis;
• pregnancy;
• lactation;
• hypersensitivity to ifosfamide.

With caution: hypoproteinemia, hypoalbuminemia, electrolyte imbalance, advanced age, immune suppression, diabetes mellitus, chronic liver failure, brain metastases, cerebral symptoms, chickenpox (including recently transferred or after contact with patients), herpes zoster, acute infectious diseases.

Side effects

From the hematopoietic system: leukopenia, thrombocytopenia, anemia. The lowest level of the number of white blood cells and platelets is noted in 7-14 days, the restoration of the blood picture usually occurs 21 days after the end of the course.

From the digestive system: nausea and vomiting; rarely-stomatitis, impaired liver function, usually manifested in the form of increased activity of liver enzymes and / or serum bilirubin levels.

From the urinary system: hemorrhagic cystitis, dysuria, frequent urination and other symptoms of bladder inflammation (blood in the urine, painful urination), impaired renal function (increased serum creatinine and urea concentrations, decreased creatinine clearance. glucosuria). Proteinuria and metabolic acidosis may also occur.

From the central nervous system: disorientation, confusion, hallucinations, increased fatigue, agitation, encephalopathy; less often-dizziness; rarely-convulsive seizures, coma, peripheral polyneuropathy.

From the reproductive system: violation of the function of the sex glands (azoospermia, amenorrhea).

From the skin and skin appendages: reversible alopecia, photosensitization.

Local reactions: redness, swelling, or pain at the injection site.

Other: cardiotoxic effects, immunosuppression, infectious complications, slowing the rate of wound healing, pulmonary symptoms (cough or shortness of breath), fever, allergic reactions.

Interaction

When used concomitantly with drugs that cause myelotoxic, neurotoxic and nephrotoxic effects, it is possible to increase the side effect.

When combined with inducers of microsomal liver enzymes, an increase in the formation of alkylating metabolites is possible.

When used concomitantly, it enhances the hypoglycemic effect of antidiabetic drugs.

Allopurinol increases myelosuppression.

Mesna reduces nephrotoxicity.

Ifosfamide may increase the skin’s response to radiation.

Concomitant use of warfarin may lead to reduced blood clotting and an increased risk of bleeding.

How to take, course of use and dosage

Ifosfamide is included in many chemotherapeutic treatment regimens, and therefore, when choosing the regimen and doses in each individual case, you should be guided by the data of the specialized literature.

The drug is administered intravenously for 30 minutes or as a 24-hour infusion. Use a solution with a concentration of no higher than 4%.

• 1.2-2.4 g/l/day for 3-5 consecutive days or every other day until a total dose rate of 10-12 g/m 2 courses repeated every 3 weeks;
• 3-5 g/m2 1 time in 2 weeks;
• 5-8 g/m2 as a 24-hour infusion of 1 every 3-4 weeks or 3.2 g/m2/day of 5-day continuous infusion every 3-4 weeks.

To reduce the likelihood of hemorrhagic cystitis, mesna is used simultaneously with ifosfamide in a total dose of 60% of the ifosfamide dose.

Preparation of the solution for intravenous use

Powder in vials is dissolved in water for injection to obtain a concentration of 40 mg/1 ml.

For intravenous use for 30 minutes, the resulting solution is diluted in 500 ml of 0.9% sodium chloride solution, Ringer’s solution or 5% dextrose solution.

To administer the drug as a 24-hour infusion, the resulting solution of the drug is diluted in 3 liters of 0.9% sodium chloride solution or 5% dextrose solution. Ifosfamide and mesna can be mixed in the same infusion solution.

Overdose

Symptoms: faster development and greater severity of the main side effects.

Treatment: symptomatic, with mandatory use of Mesna.

Special instructions

Before starting treatment, it is necessary to sanitize foci of chronic infection and correct possible electrolyte disturbances.

During treatment with the drug, it is necessary to regularly monitor the picture of peripheral blood (especially, paying attention to the number of neutrophils and platelets), laboratory parameters of liver and kidney function, and regularly conduct a urine test for the presence of red blood cells, the appearance of which may precede the development of hemorrhagic cystitis.

Women and men should use reliable methods of contraception during treatment and for 3 months after the end of ifosfamide therapy.

With impaired renal function and urinary outflow, it is possible to increase the frequency of toxic effects of the drug on the central nervous system, and therefore it may be necessary to reduce the dose of ifosfamide.

To ensure the elimination of uric acid, patients should consume a sufficient amount of fluids.

Ifosfamide therapy should be discontinued at the first sign of bladder inflammation or the appearance of blood in the urine.

When treated with ifosfamide, natural defense mechanisms may be suppressed, and antibody production in the patient’s body may decrease in response to the introduction of vaccines.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

During therapy with Holoxan, nausea and vomiting may occur, as well as encephalopathy, which may affect the ability to drive a car or work with other mechanisms. Therefore, you should refrain from driving a car or other vehicles. You should also avoid working with electric tools and mechanisms.

Form of production

Powder for preparation of solution for intravenous use

Storage conditions

Store at a temperature not exceeding 25°C out of the reach of children. Store the prepared solution at a temperature not exceeding 8°C.

Shelf

life is 5 years. The prepared solution should be used within 24 hours.

Active ingredient

Ifosfamide

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

For adults as directed by your doctor

Indications

Cancer