Endoxan

Endoxan demonstrates antitumor therapeutic activity.

The cyclophosphamide component is a cytostatic agent of the alkylating type of action. Inside tumor cells, the substance undergoes biotransformation with the formation of metabolic elements with activity, which destroy the processes of binding RNA and DNA by forming cross-links between the threads of these structures. At the same time, the metabolites block the processes of mitotic division and slow down protein binding.

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Indications Endoxan

It is used to eliminate the following disorders:

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

In combination with other antitumor drugs, it is used in the treatment of carcinoma of the cervix, lungs and bladder, as well as sarcoma affecting the prostate or soft tissues, as well as reticulosarcoma.

As an immunosuppressant, it is prescribed in cases of psoriatic or rheumatoid arthritis, progressive collagenoses, nephrotic syndrome, and in addition to this, to prevent possible rejection of a transplanted organ.

Release form

The medicinal element is released in tablets - 50 pieces per box. It is also produced in the form of a lyophilisate for the preparation of liquid used for intravenous injections.

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Pharmacokinetics

Absorption of cyclophosphamide from the gastrointestinal tract is complete.

Metabolic processes occur inside the liver; in this case, active metabolic components of an alkylating nature are formed. Part of these elements are converted into metabolites that do not have activity, and the remainder is transformed into metabolic components that have a cytotoxic effect. After an intravenous injection, the Cmax values of metabolites are recorded after 2-3 hours.

Excretion of metabolic elements is realized through the kidneys; 5-25% of the portion as unchanged substance is excreted with urine. In adults, the half-life is 7 hours, and in children - 4 hours.

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Dosing and administration

The dosage regimen is selected individually, taking into account the clinical picture. The tablets must be taken orally, half an hour before meals or 2 hours after. Often 1-4 tablets of the drug (0.05-0.2 g) are used per day. The course lasts 14-21 days.

To perform intravenous injections, it is necessary to dissolve the medicinal substance in advance. Every day it is necessary to administer 0.05-0.1 g/m2 ^. When administering injections 3 times a week, the dosage is 0.1-0.2 g/m2 ^; when performing procedures once every 2 weeks - 0.6-0.75 g/m2 ^. If injections are administered once a month, a dose of 1.5-2 g/m2 is required ^. The total dosage for the entire course of treatment is 6-14 g.

Regular blood tests are performed to monitor the severity of myelosuppression (platelet and leukocyte levels). It is also necessary to monitor the presence of erythrocytes in the urine (this is a sign of hemorrhagic cystitis, in the event of which therapy should be discontinued). Treatment is also discontinued if secondary infections occur - a complication of severe myelosuppression.

You should not consume alcoholic beverages during therapy.

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Use Endoxan during pregnancy

It is prohibited to use Endoxan during pregnancy.

Cyclophosphamide is excreted in breast milk, which is why breastfeeding should be discontinued during therapy. In infants whose mothers breastfed during treatment, thrombocyto- and neutropenia, as well as diarrhea, and decreased hemoglobin levels were observed.

Contraindications

Main contraindications:

• suppression of bone marrow activity;
• cystitis;
• cachexia of a pronounced nature;
• urinary retention;
• infections in the active phase;
• pathologies in the terminal stage;
• severe intolerance associated with a drug.

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

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Side effects Endoxan

Side effects include:

• thrombocyto-, leuko- or neutropenia;
• vomiting, abdominal pain, constipation 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 a hemorrhagic nature, nephropathy, hyperuricemia and renal dysfunction;
• hemorrhagic myocarditis (rarely);
• fibrosis affecting the lungs (long-term therapy using large doses);
• amenorrhea and disorders of spermatogenesis and oogenesis (sometimes may be incurable).

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Overdose

In case of poisoning, a potentiation of side effects is observed, including cardiotoxicity or myelosuppression.

There is no antidote. Symptomatic treatment is performed.

Interactions with other drugs

The use of uricosuric antigout drugs together increases the likelihood of developing nephropathy, because cyclophosphamide increases the volume of uric acid formed.

Combination with allopurinol potentiates the toxic effect on bone marrow.

Substances that induce microsomal oxidation potentiate the metabolic processes of cyclophosphamide, resulting in an increase in the volume of metabolic components formed and a potentiation of the effect of the drug.

Cyclophosphamide enhances the anticoagulant properties of medications and also potentiates the cardiotoxic activity of antitumor antibiotics, daunorubicin and doxorubicin.

Combination with immunosuppressants (including azathioprine, GCS, mercatopurine with cyclosporine, and chlorambucil) increases the likelihood of developing infections, as well as secondary neoplasms.

When Endoxan is used together with substances that provoke myelosuppression, as well as with radiation therapy, bone marrow suppression is increased.

Administration of cyclophosphamide with lovastatin to heart transplant recipients carries a high risk of developing acute renal failure or skeletal muscle necrosis.

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Storage conditions

Endoxan must be stored at temperatures within 25°C.

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Shelf life

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

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Application for children

Experience with the use of drugs in pediatrics is extremely limited.

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Analogues

Analogues of the drug are Cyclophosphamide, Lidoksin, Cytoxan with Cyclophosphamide, and Endoxan-Asta.

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Reviews

Endoxan receives many reviews mentioning the development of side effects as a result of its use. Almost all patients report blood rushes to the skin on the face after intravenous injections. They also complain of hyperhidrosis with headaches. In addition, among the frequent negative manifestations in the comments of users, suppression of hematopoietic processes and complete or partial baldness are noted (hair begins to grow back after the end of therapy).

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