Health, Preparations
"Endoksan": instructions for use, reviews, similar products, manufacturer
The drug "Endoksan" belongs to the group of antitumour agents. Depending on the form of release, it can be taken orally or parenterally. What kind of drug to prescribe and in what dosage, only the attending physician decides, relying on the actual circumstances of the patient's condition.
Composition and properties of the preparation
The main active substance of the drug "Endoxane" instructions for use calls cyclophosphamide. In one tablet it contains 50 mg. The drug belongs to the group of antitumor drugs and is a biconvex tablets with a white shell and a core of the same hue.
What is the pharmacology of the drug?
The main active substance of the drug, namely cyclophosphamide, has an alkylating and cytostatic effect. By its nature, it is close to mustard gas, being its nitrogen analogue.
The mechanism of action of cyclophosphamide is based on the formation of cross-links between DNA and RNA molecules and suppression of the synthesis of protein bodies.
Pharmacokinetics of the drug
The main active substance of the drug "Endoksan" has almost full degree of absorption from the gastrointestinal tract. Its concentration in the blood after oral and intravenous administration is the same. The metabolism of cyclophosphamide occurs mainly in the liver, where the oxidative microsomal mechanism produces active alkylating metabolites. Some of them are converted into inactive forms, another group moves to cells where, under the action of enzymes, phosphatases are transformed into substances with cytotoxic properties.
The degree of binding of the initial form of the drug to blood proteins is insignificant and is 12-14%. However, the same indicator in metabolites is already 60%.
The excretion of cyclophosphamide is produced by the kidneys mostly in the form of metabolites. About 5-25% of the drug is excreted in its original form with urine and bile.
The T1 / 2 parameter for the drug is 7 hours for adult patients and 4 hours for children.
In what dose to take the medicine?
The drug "Endoxan" in the tablet form is taken orally before meals for half an hour or after a meal, after 2 hours.
Due to the fact that this pharmaceutical product is included in a large number of chemotherapeutic schemes, the choice of the way of its administration and dosage is considered by the doctor individually.
"Endoxan" - tablets - the instruction recommends taking in a dosage of 1-3 mg / kg of body weight per day, which can range from 50 to 200 mg of cyclophosphamide for 24 hours. Duration of treatment is 2-3 weeks.
If the drug is taken together with other drugs that have anti-tumor properties, then the dosage of all elements of therapy is subject to correction.
Can an overdose occur?
The presence of a specific antidote for the drug "Endoxan" instruction for use does not confirm. In case of excess of the required dose, it is recommended to use maintenance therapy in the form of appropriate treatment of infectious diseases, removal of cardiotoxicity and elimination of signs of myelosuppression.
How is the drug combined with other drugs?
If the patient takes drugs that provoke microsomal oxidation in the liver, then when co-administered with the Endoxan preparation, the instruction indicates an increase in the synthesis of metabolites with alkylating activity, a decrease in the half-life of cyclophosphamide, and an increase in its effectiveness.
This drug suppresses cholinesterase activity and the metabolic pathway of cocaine, increasing its toxicity, and increases the effectiveness of suxamethonium.
If "Endoxan" is used in conjunction with "Allopurinol", then there is an increased negative impact on the bone marrow.
In the case of simultaneous treatment with cyclophosphamide, colchicine, probenecid, sulfinpyrazone, the doctor usually adjusts the dose of drugs against gout. This is associated with an increasing risk of developing nephropathy with the joint use of "Endoxan" with uricosuric medicines.
Cyclophosphamide reduces the synthesis of factors in the liver, responsible for clotting and the formation of platelets, so with simultaneous treatment with anticoagulants, the activity of the latter decreases.
For patients taking ENDOXAN, the instructions for use recommend the exclusion of grapefruit juice from the diet, as it contains components that disrupt the activation and effectiveness of the main active ingredient of the medication.
When co-administration of cyclophosphamide with Doxorubicin or Daunorubicin, the cardiotoxic effect of these drugs increases.
Combination with other immunosuppressants, such as "Azathioprine", "Cyclosporine", "Chlorambucil", "GCS", "Mercapturin" leads to an increase in the occurrence of infections and tumors of the secondary type.
In the case of the combined use of Endoxan and Lovastine in patients with heart transplantation, there may be a risk of necrosis of skeletal muscles and renal failure in acute form.
If treatment with cyclophosphamide is combined with myelosuppressants or radiotherapy, then it is possible to increase the inhibition of bone marrow functioning.
Simultaneous reception of "Endoxan" with elevated doses of cytarabine during preparatory manipulations for bone marrow transplantation increases the incidence of cardiomyopathy with a fatal outcome.
How does this drug affect reproductive function?
The drug "Endoxane", patients' reviews confirm this, can provoke sterility in patients of both sexes, which can be irreversible.
In most cases, women have amenorrhea, but the regularity of menstruation usually recovers several months after the end of treatment with cyclophosphamide. If the therapy was performed in girls of prepubertal age, there were no deviations in the development of secondary sexual manifestations. Menstruation was normal, the ability to conceive was not lost.
When treating men with Endoxan, the instruction indicates that azoospermia or oligospermia were recorded in a number of cases. This is due to increased production of gonadotropins at the rate of testosterone release. The level of libido and potency in men does not decrease. If treatment with cyclophosphamide was performed in boys of prepubertal age, then secondary sexual manifestations occurred in them normally. However, cases of azoospermia, oligospermia and an increase in gonadotropins were noted. Also, atrophy of testicles may occur. It should be noted that azoospermia is reversible, although restoration of this function may occur several years after the end of treatment.
What side effects does the drug have?
Admission of the drug "Endoxane", the instruction for use confirms this, can cause some violations of the hematopoiesis system:
- Leukopenia, neutropenia - quite often.
- Less common are anemia and thrombocytopenia.
After 1-2 weeks from the start of treatment, the patient has a maximum decrease in leukocytes and platelets in the blood. These indicators are restored to normal after 7-10 days after the end of therapy.
In the treatment of cyclophosphamide, there may be adverse reactions from the gastrointestinal tract:
- Nausea and vomiting.
- Anorexia.
- Stomatitis.
- Pain in the abdominal area.
- Violations of the stool.
- Jaundice.
- Hemorrhagic colitis.
Rarely, liver dysfunction is associated with an increase in enzyme activity and an increase in the level of bilirubin. In a fairly large group of patients who have aplastic anemia and receive high doses of "Endoxan" or combining it with busulfan, endophlebitis of the liver of the liver is noted. This phenomenon can develop 1-3 weeks after the bone marrow transplantation and is manifested in a sharp increase in body weight, ascites, hepatomegaly and hyperbilirubinemia, hepatic encephalopathy.
When taking the drug, unwanted reactions from the skin can occur:
- Reversible alopecia.
- Rash.
- Pigmentation of skin and nails.
A disturbance of the urinary system during treatment with Endoxan may also be provoked. Instruction, reviews of doctors and patients indicate the following conditions:
- Cystitis in combination with fibrosis of the bladder (or without it).
- Hemorrhagic urethritis.
- Necrotic phenomena of the renal tubules up to a lethal outcome.
In the urine, the patient can have an epithelium of the bladder. If the form of hemorrhagic cystitis is severe, the drug is stopped. The best prevention of this condition is the medication "Mesna". If doses of "Endoxan" are increased, kidney dysfunction in the form of nephropathy and hyperureukemia may develop.
If a patient has a severe degree of immunosuppression, severe cyclophosphamide can be treated with severe infections.
The following side effects can also develop:
- Cardiotoxicity (when taking high doses), severe degrees of heart failure.
- Pulmonary fibrosis of interstitial nature.
- Violation of normal oogenesis and spermatogenesis, reversible and irreversible sterility.
- Development of secondary malignancies: bladder cancer, myeloproliferation and lymphoproliferation.
- Allergy in the form of rash, itching, hives, sometimes in the form of anaphylactic reaction.
- Poor wound healing.
- Redness of the face, increased sweating, headache.
The presence of serious side effects from taking the drug always raises the question of the possible benefits against the possible risks for a single patient.
At what diseases are prescribed this drug?
Endoxan tablets can be given to a patient if they have the following diseases:
- Lymphogranulomatosis.
- Multiple myeloma.
- Mammary cancer.
- Lymphoblastic lymphatic leukemia in acute or chronic form.
- Lymphomas of non-Hodgkin's type.
- Retinoblastoma.
- Neuroblastoma.
- Mycosis fungoid nature.
Indicates the acceptability of the instruction in the complex anti-carcinogenic therapy applied to the Endoxan preparation. The manufacturer recommends that it be included in the treatment of cervical and bladder cancer, oncology of the lung and prostate gland, sarcoma and reticulosarcoma, Ewing and Wilms disease.
The drug based on cyclophosphamide can be used as an immunosuppressant for autoimmune diseases of progressive type: psoriatic and rheumatoid arthritis, hemolytic anemia, collagenosis, nephrotic syndrome, and to avoid rejection of the graft.
When is the drug contraindicated?
The drug Endoxan has a lot of contraindications, among which:
- Pregnancy and lactation.
- Cystitis.
- Infections in active form.
- Disturbance of bone marrow functioning of pronounced form.
- Presence of hypersensitivity to the main and additional substances of the drug.
- Delayed urination.
With special care, doctors prescribe this drug for heart disease, kidney and liver of severe degree, gout, adrenalectomy, the presence of infiltration processes in the bone marrow, nephrourolythiasis.
Special instructions for treatment
During the reception of the drug "Endoksan", blood (concentration of platelets and neutrophils) and urine (the presence of erythrocytes) of the patient are subject to mandatory control.
In some cases, it is recommended that Endoxan be discontinued. Instructions for use of the tablet recommend doing this under the following conditions:
- Manifestation of cystitis.
- Lowering the concentration of leukocytes and platelets to critical values.
- The emergence of infections (dose adjustment is possible).
If "Endoxan" is used in large doses, the patient is prescribed a medication "Mesna" for the prevention of cystitis of the hemorrhagic type.
When treating this drug should refrain from drinking alcohol and use reliable methods of contraception.
If the patient is assigned "Endoxane" within 10 days after the operation with a general anesthesia, then an anesthesiologist is informed about it.
After adrenalectomy, dose adjustment of "Endoxan" and other GCS preparations is carried out.
Drug analogues
If there are serious contraindications and risks, then offers to refuse to take the medicine "Endoxan" instruction. Analogues can be prescribed by the doctor as a suitable alternative. Among them:
- "Ledoksin."
- "Cyclophosphane".
- "Cytoxan".
- "Cyclophosphamide - Teva."
- Cyclophosphane-Lance.
- Endoxan - ASTA.
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