Oncological diseases are one of the most common causes of death. The pharmaceutical industry is constantly looking for drugs that can help people with oncology maintain health and life. One such remedy is Leukeran. Instructions for use, composition, indications and analogues to this medicine will be considered in our article. We also provide information about the reviews that doctors and patients leave about this drug.
Pharmacological affiliation
This is the earliest group of drugs that can fight cancerous tumors. Instructions for its use clearly indicate its pharmacological affiliation with the Leukeran preparation. It belongs to the group of alkylating agents. It is based on beta-chloroethylamine derivatives. The group of these drugs begins its history from the 40s of the XX century, when during the Second World War the study of the effects of the toxic substances of mustard gas and nitrogen mustard was carried out. Having passed the path in several decades, alkylating preparations became less toxic and more effective, which allowed their widespread use in the treatment of many deadly diseases.
In what form is the medicine released?
All the important information is provided by the instruction for the Leukeran preparation. The composition and application are spelled out in great detail. The drug, used in some forms of cancer, is available in the form of tablets, which are coated with an enteric brown coating. The tablets are round, convex on both sides. Each has an indented inscription. On the one hand it is the letter L, and on the other - a combination of GX EG3. The license for the production of Leukeran is owned by the German pharmaceutical corporation GlaxoSmithKline Trading (Glaxo Wellcome Operations).
How does it work
Instructions for use with "Leukeran" (tb 2mg) indicate that the drug has one active component - chlorambucil. This substance is an aromatic derivative of nitrogen-containing mustard. Its type is alkylating, bifunctional. The substance has a cyclone-specific effect. Its chemical formula is as follows:
4- [bis (2-chloroethyl) amino] benzenebutanoic acid.
As auxiliary forming components, the composition of the tablets includes:
- Stearic acid.
- Silicon colloidal anhydrous.
- Lactose anhydrous.
- Microcrystalline cellulose.
- Opadry brown (coloring component)
25 Leukeran tablets are packed in a plastic jar with a screw cap. The bottle is placed in a cardboard box, where the instructions for use are included.
How the active component works
The instruction for the use of Leukeran tablets indicates that the substance chlorambucil acts as the active ingredient in it. Once in the body and penetrating into the blood and tissues, it passes through a ligament with nucleoproteins of the nuclei of cells. This process serves as a signal for the formation of highly active ethyleneimonium radicals, and by alkylation causes DNA strands to replicate. Also, this substance causes apoptosis of cancer cells.
Chlorambucil, which is part of Leukeran, inhibits the tissues of the tumors and bone marrow, moreover, lymphoid tissues, rather than granular granulocytes, are more susceptible to its negative effects. When conducting tests on animals and in the process of human therapy, scientists have revealed that the drug negatively affects the gonads, which causes azoospermia and amenorrhea. It was found that the drug is able to cause chromosomal and chromatid disorders, as well as the development of myelodysplastic disorders, having a carcinogenic effect on the body. The instructions for use with Leukeran tablets indicate that prolonged use of the drug can cause the appearance of secondary malignant tumors. This is one of the most serious adverse reactions.
The pathway of the substance in the patient’s body
In the description to "Leukeran" it is indicated that the drug is taken only orally. The active substance of the tablets is rapidly absorbed from the gastrointestinal tract into the systemic circulation, is almost completely absorbed (up to 99%). Communication in the blood occurs mainly with albumin. Chlorambucil, performing its work, metabolizes to phenylacetic mustard gas. This substance also has an antitumor effect, and in the blood it is one and a half times longer than the original component.
The maximum concentration of the active compound in the blood is detected after 15 minutes and remains for 2 hours. The half-life for chlorambucil is 1.5 hours, and for its active metabolite, 2.5 hours. Chlorambucil is converted to mono- and dihydroxyl derivatives. In a small amount, they are excreted in the urine.
To obtain a clinical effect, the drug "Leikeran" must be taken within a month. In many cases, long-term therapy (at least 2 years) normalizes the total number of leukocytes, stabilizes up to 20% of the number of lymphocytes in the bone marrow. Also, lymph nodes are restored during this period and splenomegaly is inhibited. Long-term use of the drug is recommended only by a specialist. At the same time, constant monitoring of the patient’s health is necessary.
In what cases is the use of the drug indicated
According to the instructions for the use of Leukeran tablets, the drug is prescribed for such diseases:
- Hodgkin's disease.
- Lymphoid leukemia.
- Diffuse non-Hodgkin's lymphoma.
- Waldenstrom macroglobulinemia.
Any of these diseases should be correctly diagnosed. The drug has the right to appoint only a specialist who has experience working with him.
When a medicine cannot be used in therapy
All relevant information is reported on the antitumor drug "Leykeran" instructions for use. It also lists contraindications and restrictions on the use of these pills. Basically, there is only one ban - for people who have recently undergone chemotherapy or radiation. Since the drug penetrates the placental barrier, it should not be taken by pregnant women and young mothers who are breast-feeding a baby. It is also forbidden to prescribe "Leukeran" to those who have hypersensitivity to any component that is part of the chemical composition of the drug.
With extreme caution (weighing all the risks and benefits), the administration of chlorambucil is prescribed to patients who have such problems:
- Inhibition (hypoplasia) of the bone marrow, expressed by leukopenia, thrombocytopenia.
- Suffering from epilepsy.
- People with kidney failure.
- Having severe abnormalities in the liver.
- With caution and under the close supervision of medical personnel, the drug should be taken by patients suffering from herpes zoster, as well as those who have recently had chickenpox.
- Suffering with urate nephroulithiasis.
- People with acute, bacterial, viral, or fungal infections.
- For those who have recently suffered a head injury or are prone to epileptic seizures.
Until the ability of chlorambucil to penetrate the blood-brain barrier has been identified. Taking this medicine without a doctor’s prescription is strictly prohibited.
Possible effects of therapy
It is required to observe very precisely the doses prescribed in the instructions for use with Leukeran. They are defined for each disease in which this remedy is prescribed. We should not forget about the possible side effects of treatment with tablets containing chlorambucil. The negative effects of this medication may occur as follows:
- Azoospermia.
- Amenorrhea.
- Gastrointestinal disorders.
- Jaundice.
- Acute leukemia that appears after a course of drug therapy.
- Fever.
- Myelosuppression
- Impaired liver function.
- Peripheral neuropathy.
- Toxic epidermal necrolysis.
- Pneumonia.
- Seizures, which children with nephrotoxic syndrome are especially prone to.
- Stevens-Johnson Syndrome.
- Skin rash.
- Aseptic cystitis.
- Pulmonary fibrosis.
Once again, we note that when conducting treatment with this drug, the patient must strictly observe the recommended dosage. If, for whatever reason, the drug was taken more than necessary, the following health problems occur: ataxia, increased irritability, pancytopenia reversible, epileptic seizures. There is no specialized antidote for chlorambucil, therefore, help with an overdose comes down to symptomatic therapy after the drug is removed by washing the stomach. During this period, blood tests should be carried out regularly and the body's functionality should be maintained with the help of medical manipulations and drugs.
How to take medicine
In the instructions for use of the drug "Leykeran" dosage is indicated in detail and clearly. Everyone can figure out how to take the remedy. However, only a doctor can take into account all the features of the patient’s body condition, the course of the disease, in order to recommend a specific regimen of tablets.
In Hodgkins disease, this drug is used in monotherapy in the amount of 1 tablet per 10 kilograms of the patient’s body weight per day. This algorithm applies to the treatment of both adults and children.
Non-Hodgkin lymphomas require initial therapy within 1-2 months at the rate of 0.1-0.2 mg per kilogram of patient’s body weight in one day. Further, the treatment will be supportive, in which the doctor can prescribe a daily lower dosage of the drug or use intermittent therapy.
If the patient is diagnosed with chronic lymphocytic leukemia, then until the number of leukocytes decreases within 10 · 10 9 / l, the patient is prescribed a daily dose of the drug at the rate of 0.15 mg per 1 kilogram of weight. Then you need a break in therapy with Leukeran tablets for 4 weeks. Then the treatment continues with the calculation of the dosage per day in the amount of 0.1 mg / kg.
In the treatment of other malignant diseases, as reported in the instructions to the "Leykeran", complex therapy is most often used. So, with Waldenstrom's macroglobulinemia, an initial dosage of 6-12 mg a day before the development of leukopenia will be prescribed. Then you should switch to maintenance therapy, which consists of calculating 2-8 mg of the drug in one day for an indefinite period of time. All important information about Leukeran tablets should be considered by a specialist when prescribing cancer therapy.
Therapy of chronic lymphocytic leukemia, accompanied by bone marrow failure, involves a preliminary course of taking Prednisolone, which helps suppress the immune system.
As can be seen from the above information, it is necessary to study the instructions for the "Leikeran". Indications for use in each case should be indicated only by the attending physician. A tablet of the drug is recommended to be taken completely, swallowing and drinking water. It is strictly forbidden to divide it into parts or chew. While the active substance is in the shell, it has no effect on the tissue, for example, when the patient holds the tablet in his hand.
During the course of therapy should not drink alcohol, as this can provoke gastrointestinal bleeding.
Complex treatment
Malignant diseases require the use of special drugs that can inhibit the development and growth of cancer cells. Often, such treatment should be comprehensive. The specialist must take into account the interaction of drugs prescribed to the patient. For Leukeran tablets, the instruction stipulates the conditions of complex therapy.
Myelotoxicity of the drug will increase with the simultaneous use of drugs that inhibit hematopoiesis. The concentration of uric acid will increase if chlorambucil is taken together with medicines for gout.
The combination of Leukeran and tricyclic antidepressants, haloperidol, maprotiline, monoamine oxidase inhibitors, phenothiazines, thioxanthenamides is often the cause of convulsive seizures. The administration of inactivated (killed) vaccines becomes ineffective, and living ones can cause an increase in the side effects of one and the other medicine.
Any combination of drugs for oncological diseases should be carefully thought out by the attending physician in order to obtain a qualitative result and avoid deterioration of the patient's well-being.
What can be replaced
We continue to consider the instructions for use with Leukeran. Analogues of this drug should have the same therapeutic effect. If the same substance works in the drug, then it is called a synonym. For Leukeran tablets, this is the Chlorobutyl medication, also available in tablet form.
Medicines - analogues of "Leukeran" composition may have a slightly different, but will have a similar effect. Such drugs include Alkeran based on melphalan, Endoxan, and Cyclophosphamide, in which cyclophosphamide, Ribomustin, the active substance in which is bendamustine, work. The group of alkylating drugs includes other drugs that have a cytotoxic effect and are used in the treatment of cancer. Which drug should be used in each case, only the attending physician decides, taking into account the individual characteristics of the patient's body and the course of the disease.
What doctors and patients say about the drug
Oncological diseases are an acute problem of mankind. Drugs that suppress malignant tumors should take into account many of the nuances of therapy. Both Leukeran tablets and analogues of this medicine have mixed reviews.
Experts believe this drug is very effective for the treatment of certain types of oncology. Despite the frequent occurrence of side effects due to the cytotoxic effect of the active component, oncologists call these tablets a very effective way of inhibiting the growth of malignant cells.
Many patients note the effectiveness of the drug. In their reviews, they report on the received positive effect, which is most important for them.
Among the shortcomings, people indicate that these pills are very difficult to buy in ordinary pharmacies, and their cost is very high. For one package (25 tablets) you need to pay about 3000 rubles. In some responses, there are reports that in online pharmacies, especially on foreign sites, you can buy fake medicine that does not have the desired effect. Both specialists and many patients warn that there is no need to respond to ads on the sale of Leykeran tablets from the hands, since in most cases such drugs turn out to be fakes.
Conclusion
The antineoplastic drug "Leykeran" has established itself as a very effective medication that has been successfully used in the treatment of certain types of cancer. The component chlorambucil working in it belongs to the pharmaceutical group of alkylating agents developed on the basis of bis- (beta-chloroethyl) amine. This medication should be taken only as directed by the attending physician after a thorough examination and correct diagnosis. In no case should you take this medicine on your own initiative or on the recommendation of friends.