Endoxan

Endoxan demonstrates antitumor therapeutic activity.

The cyclophosphamide component is a cytostatic agent of an alkylating type of exposure. Inside the tumor cells, the substance undergoes biotransformation with the formation of active metabolic elements that destroy the binding processes of RNA and DNA by forming transverse ligaments between the strands of these structures. At the same time, metabolites block the processes of mitotic division and slow down protein binding.

[1], [2]

Indications Endoksana

It is used to eliminate such disorders:

• lymphogranulomatosis;
• lymphosarcoma;
• multiple myeloma;
• lymphoblastic leukemia type in the active phase;
• osteosarcoma;
• non-Hodgkin's lymphomas;
• neuroblastoma ;
• breast carcinoma;
• lymphocytic leukemia, having a chronic nature;
• ovarian carcinoma;
• retinoblastoma.

In combination with other anticancer drugs used in the treatment of carcinoma of the uterine cervix, lung and urinary tract, and in addition sarcoma that affects the prostate or soft tissues, as well as reticulosarcoma.

As an immunosuppressant, it is prescribed in the case of arthritis of a psoriatic or rheumatoid variety, progressive collagenosis, nephrotic syndrome, and also to prevent possible rejection of a transplanted organ.

Release form

The release of the drug element is implemented in tablets - 50 pieces inside the box. It is also produced in the form of a lyophilisate for the preparation of the liquid used for IV injection.

[3]

Pharmacokinetics

The absorption of cyclophosphamide from the gastrointestinal tract is full.

Exchange processes take place inside the liver; at the same time formed with the active metabolic components of an alkylating nature. Partially, these elements are converted to metabolites that do not have activity, and the residue is transformed into metabolic components that have a cytotoxic effect. After IV injection, Cmax metabolites are recorded after 2-3 hours.

The excretion of metabolic elements is realized through the kidneys; 5-25% of the dose as unchanged substance is excreted in the urine. In adults, the term half-life equals 7 hours, and in a child, 4 hours.

[4], [5], [6], [7], [8]

Dosing and administration

The dosage scheme is selected individually, given the clinical picture. Tablets must be taken orally, half an hour before meals or after 2 hours after. Often, 1-4 tablets of drugs (0.05-0.2 g) are applied per day. The course lasts 14-21 days.

For performance in / in pricks it is necessary to dissolve the medicinal substance. Every day you need to enter at 0.05-0.1 g / m ². When conducting injections 3 times a week, the dosage is 0.1-0.2 g / m ²; when performing procedures 1 time per 2 weeks - 0.6-0.75 g / m ². If injections are administered 1-fold per month, a dose of 1.5-2 g / m ² is required. The total dosage for the entire treatment course is 6-14 years.

To control the severity of myelosuppression (platelet counts with leukocytes), a regular blood test is performed. It is also necessary to control the presence of red blood cells inside the urine (this is a sign of hemorrhagic cystitis, in the event of which it is necessary to cancel the therapy). Termination of treatment is also carried out with the appearance of secondary infections - complications of severe myelosuppression.

During therapy, you can not drink alcohol.

[12], [13]

Use Endoksana during pregnancy

It is forbidden to use Endoxan during pregnancy.

Cyclophosphamide is excreted in breast milk, which is why breastfeeding should be abandoned for the duration of therapy. The development of platelet and neutropenia, as well as diarrhea, and a decrease in hemoglobin indices were observed in infants who were breastfed by mothers during treatment.

Contraindications

The main contraindications:

• suppression of bone marrow activity;
• cystitis;
• cachexia, which is pronounced;
• urinary retention;
• active phase infections;
• pathology in the terminal stage;
• severe intolerance associated with medication.

Caution in use is required in the case of gout, nephroluritiasis, adrenalectomy, bone marrow suppression, and severe kidney, liver, or heart disease.

[9], [10]

Side effects Endoksana

Among the adverse events:

• platelet, leuko- or neutropenia;
• vomiting, abdominal pain, obstipation or diarrhea, nausea, loss of appetite, and in addition stomatitis, jaundice and colitis;
• alopecia;
• epidermal itching, rashes and urticaria;
• skin pigmentation;
• cystitis or urethritis of hemorrhagic nature, nephropathy, hyperuricemia, and disorder in the work of the kidneys;
• myocarditis of hemorrhagic species (occasionally);
• pulmonary fibrosis (prolonged therapy with large portions);
• amenorrhea and disorder of spermatogenesis and oogenesis (can sometimes be incurable).

[11]

Overdose

In case of poisoning, there is a potentiation of adverse signs, including cardiotoxicity or myelosuppression.

The antidote is missing. Symptomatic treatment procedures are performed.

Interactions with other drugs

Using anti-gouty drugs together of a uricosuric nature increases the likelihood of nephropathy, because cyclophosphamide increases the volume of uric acid formed.

The combination with allopurinol potentiates the toxic effect on the bone marrow.

Substances that induce the oxidation of microsomes potentiate the metabolic processes of cyclophosphamide, as a result of which the volumes of metabolic components formed increase and the effect exerted by the drug is potentiated.

Cyclophosphamide enhances the anticoagulant properties of drugs, as well as potentiates the cardiotoxic activity of anti-infective anti-tumor nature, daunorubicin and doxorubicin.

Combination with immunosuppressants (among them azathioprine, GCS, mercatopurin with cyclosporine, and chlorambucil) increases the likelihood of developing infections, as well as secondary tumors.

When using Endoxan together with substances that cause myelosuppression, as well as with radiation therapy, bone marrow suppression is enhanced.

The introduction of cyclophosphamide with lovastatin in people with a transplanted heart has a high risk of developing ARF or skeletal muscle necrosis.

[14], [15], [16]

Storage conditions

Endoxan must be maintained at temperatures in the range of 25 ° C.

[17], [18],

Shelf life

Endoxan can be used for a 36-month period from the date of sale of the drug.

[19], [20]

Application for children

The experience of using drugs in pediatrics is extremely limited.

[21], [22], [23], [24]

Analogs

Analogs of drugs are Cyclophosphamide, Ledoxin, Cytoxane with Cyclophosphamide, and Endoxan-Asta.

[25], [26], [27], [28], [29], [30], [31], [32], [33], [34], [35]

Reviews

Endoxan receives many reviews that mention the development of adverse symptoms as a result of its use. Almost all patients speak of flushing to the skin on the face after IV injection. They complain of hyperhidrosis with headaches. In addition, suppression of hematopoietic processes and complete or partial baldness are noted among the frequent negative manifestations in user comments (hair begins to grow after the end of therapy).

[36], [37], [38], [39], [40]