Methotrexate: instruction manual, reviews, analogs

According to information in the manual, "Methotrexate” – drug to combat tumors. The name of the tool due to the active ingredient methotrexate. On average one pack costs 200 rubles and more. "Methotrexate" produces the Austrian pharmaceutical company “Ebewe Pharma”. On pharmacy shelves, the tool presents cardboard boxes containing pills "Methotrexate" and instructions. In one of the packs – a Bank of plastic in it – fifty pills. Each instance contains 2.5 mg of active compound. In addition, "Methotrexate" is made in the form of a substance for injective administration.

Pharmacological characteristics

"Methotrexate" belongs to the class of anticancer drugs having the effect of cytotoxic drugs. The vehicle belongs to the class of antimetabolites that can inhibit digidrofolatreduktaza participating in chemical reactions of dihydrofolic acid. Therefore, in the body is controlled by the number of generated tetrahydrofolic acid, which is able to transport the enzymes of the carbon involved in the processes of generation of purine nucleotides, products of their interactions with other substances.

The Manufacturer in the instructions for "Methotrexate" indicates that shortly after entering active compounds in the organism is inhibited mitosis at the cellular level. A certain influence on the DNA (production, repair). The greatest effect "Methotrexate" shows a relatively robust proliferative tissues. Studies have shown that it is:

• The epithelium of the mucous membranes of the mouth;
• Intestinal environment;
• Tissue of the bladder;
• Atypical malignant cells;
• Embryonic structure
• Elements of the bone marrow.

The user "Methotrexate" it is mentioned that the drug belongs to the category of not only antitumor, but also immunosuppressive funds. Keep this in mind when assigning its patients within the therapeutic course, particularly long.

Kinetics of materials

Instructions for use "Methotrexate" States that the body's ability to absorb the active connection is determined by the dosage of the medication. If simultaneous use of 30 mg, then the absorbability is good enough, and bioavailability reaches 60%.

If "Methotrexate" is used to treat children who have leukemia, absorption is estimated at 23-95%.

In the instructions for use "Methotrexate" the manufacturer pays attention to: the greatest concentration of active compounds in the circulatory system achievable no earlier than 40 minutes after receiving the tablets in food but not later than four hours from the time of admission. If you take the pill during a meal, the rate of absorption is reduced, reduced maximum concentrations in the circulatory system.

The Ability to enter into connection with the structures of blood protein (albumin) is estimated at 50%. Soon after absorption the substance is distributed to organs and tissues. The highest rates of accumulation characteristic:

• Liver;
• Kidneys;
• The spleen.

At the same time the transformation in polyglutamate.

In the instructions for use "Methotrexate" indicates the possibility of a cumulative effect in these organs, and the substance can accumulate for weeks and months.

If you use the medication in the dosage recommended by the manufacturer, methotrexate practically seeps through the brain barrier. Tests showed that the substance penetrates into mother's milk.

Features of biological reactions

In the instructions for use "Methotrexate" the manufacturer warns that oral use of the drug part of the process of metabolism occurs through the intestinal tract, but the bulk of reactions have on the liver. Localization (liver) does not depend on the form of the introduction of methotrexate in the body of the patient.

The Main metabolite of the active connection – poly-glutamic form. This substance has pharmacological activity, inhibits digidrofolatreduktaza, warns of reaction for the formation of thymidine.

If the medicine is appointed in a dosage up to 30 mg/m², the duration of the half-life is estimated at 2-4 hours for the initial phase, but the end requires some big time periods – up to ten hours, if the dose is small, with only five hours more if "Methotrexate" assigned to a high dosage.

The Duration of half-life, as specified in the instructions for use "Methotrexate" (injections, tablets), may increase significantly if the patient suffers from insufficiency of kidney function. The main route of excretion – tubular, glomerular filtration. Substance leaves the body with urine. Approximately one tenth of the total volume excreted by the bile, in the intestinal tract is the process of reabsorbtsii. If there is evidence of renal dysfunction, ascites, transudate in pronounced form, elimination is slow. Reuse "Methotrexate" provokes a cumulative effect. Accumulation occurs inthe form of metabolites – polyglutamates.

When to use?

In the instructions for "Methotrexate" (injections, pills) indicated that the drug can improve the condition of patients diagnosed with:

• Leukaemia;
• Psoriasis in severe form;
• Mycosis fungoides (advanced stages);
• Rheumatoid arthritis (with the ineffectiveness of alternative treatment methods);
• Non-Hodgkin's lymphoma;
• Trophoblastic medical education.

Not!

Instructions for use of tablets "Methotrexate" refers to inability to use the staff, if they had severe, severe violations of liver function, kidneys. Should not be used if the diagnosis contains the mention:

• Hypoplastic bone marrow;
• Diseases of the blood;
• Leukopenia, thrombocytopenia;
• Anemia;
• Infection in the acute stage.

A guide to pills "Methotrexate" do not use the medication if the patient suffers from increased susceptibility, sensitivity to any compound used in the manufacture of drugs. A similar condition applies to the form of release for injective administration.

"Methotrexate" permitted strictly for patients above the age of three. The drug should not be used during pregnancy and lactation. Do not use the tool if the identified immune deficiency syndrome.

Special case

The need For especially careful monitoring of patients suffering from ulcer of the stomach or intestines, instructed "Methotrexate". Ampoules containing the active compound, pills based on it is allowed to eat with ulcerative colitis, but only in case, if you have the opportunity to provide the appropriate level of care. The manufacturer indicates the need for careful attention, if the patient is installed:

• Infection with bacteria, viruses, pathological fungi;
• Ascites;
• Lack of water in the body;
• The presence in the pleural cavity effusion;
• Gout, nephrolithiasis, referred to in the history of the disease.

You Can use "Methotrexate" according to the instructions in rheumatoid arthritis, tumor processes, if the patient previously had been in therapy for chemotherapy and radiation, but the history also require extremely careful monitoring of the patient's condition.

Tablets: rules of admission

As noted by those taking the drug in their reviews for "Methotrexate" of the instruction manual gives a clear explanation of the rules for use of the drug, therefore, to follow the installed program is easy. The tablets are intended for oral administration, and duration of treatment and dosage is chosen by the doctor, assessing the individual characteristics of the client. This takes into account whether the patient chemotherapy, a diagnosis was the reason for the appointment of "Methotrexate" (instructions for use in rheumatoid arthritis is slightly different from the rules of treatment of a tumor), what are the individual peculiarities of reaction to the medication.

If the basis for the appointment of the tablets became trophoblastic disease, then the recommended per day use from 15 mg up to twice the amount. Take the whole amount at one time. The duration of the course – five days. If necessary, repeat the program, maintaining between sets week break or a little more. The manufacturer indicates the ability to repeat the course with this diagnosis 3-5 times. Features of treatment will depend on the severity of the toxic effect.

Another method of dealing with trophoblastic tumors – intake of 50 mg daily for five consecutive days, then make a month or a longer break. The course in food use 300-400 mg of active compound.

Diagnosis and rules

According to the reviews and the instructions for use, "Methotrexate" effective if the identified non-Hodgkin's lymphoma. The drug is used as part of an integrated program. Per square meter of body surface administered 15 to 20 mg of active compound. The medicine is taken for once a week – twice. Alternative – 7.5 mg/m² per day for five consecutive days.

Feedback and instruction for "Methotrexate" contain a reminder of the effectiveness of a drug in some forms of leukemia, but the drug is used only as one of the points of the complex treatment because monotherapy did not show significant effect. For acute lymphoblastic leukemia are shown to make a 3.3 mg/m². The drug is combined with medicines containing prednisone. After achieving remission, it is possible to use the considered the drug of 15 mg/m² twice a week. Alternatively, 2.5 mg/kg every two weeks.

Other diseases

Most Often users are interested in, as you can see from the questions and responses, the instructions for "Methotrexate" in rheumatoid arthritis, but this disease – not the only class of non-oncological for which the effective consider pills and injections. In particular, the widespread practice of using the drug against psoriasis. Dosage for a week – from 10 to 25 mg. the doctor Gradually increases the volume, trackingthe reaction of the patient. Decrease start when you will be able to achieve the expressed clinical effect. The main task – to identify what is the minimum amount of medication allows you to get the desired result.

With mushroom mycosis the drug is administered twice per week at 25 mg, then adjusts the volume based on the reaction of the body. Evaluate the quality of the functioning of the circulatory system, side effects, response to pathology. There are two options: reducing the used amounts of the drug or its complete cancellation.

The Greatest interest to many causes instructions for use "Methotrexate" in rheumatoid arthritis. Means begin using a dose of 7.5 mg. This volume is consumed once a week or thrice, maintaining between them a twelve-hour time intervals. To get a pronounced, persistent clinical effect, it is possible to increase the quantities up to 20 mg. Instructions for use "Methotrexate" arthritis recommended minimum effective dosage, the choice of which is carried out, first reaching effect, and then started to decrease used patient dose. The task of the doctor – to be able to select such volumes, when "Methotrexate" effective, and its toxic effects for the patient.

If the arthritis in the chronic form developed the child, the teenager, the dosage is calculated as follows: 10-30 mg/m² or 0.3-1 mg/kg Obtained for such calculation the amount of the drug should be consumed once a week. The product is used at a time.

Side effects

Like many other similar drugs, analogs, "Methotrexate" (feedback, instruction manual confirm this) could trigger a large variety of adverse reactions due to increased toxicity of the components. The manufacturer indicates the following possible negative consequences of usage:

• Thrombohemorrhagic, natro-, pancito-, leucopenia;
• Anemia;
• Agranulocytosis;
• Eosinophilia;
• Effusion in the pericardial region;
• Lower blood pressure;
• Blood clots;
• Vomiting, nausea;
• Weight loss
• Erosions, ulcers, bleeding in the gastrointestinal tract;
• Pancreatitis;
• Activation of enzymes of the liver;
• Hepatitis;
• Encephalopathy;
• Craving to sleep;
• Sick and dizzy;
• Paresis;
• Blurred vision;
• Pulmonary fibrosis;
• COPD;
• Signs of interstitial pneumonia;
• Skin reaction;
• Necrotic processes;
• Nephropathy;
• The presence in urine of protein structures, nitrogen and inclusions of blood;
• Sexual dysfunction, fertility;
• Dysmenorrhea;
• Myalgia;
• Allergies;
• Diabetes;
• Lymphoma;
• Infection with cytomegalovirus;
• Vasculitis;
• Tinea versicolor;
• Herpes.

About possible negative reactions before starting the course be sure to alert the doctor. The doctor evaluates the patient's condition and analyzes which negative answers are most likely, just gives instructions, explains how to proceed if a condition against the use of "Methotrexate" deteriorating.

Too many!

Clinical observations have shown that there are no specific symptoms if you use too much volume "Methotrexate" does not arise. To reveal the fact of overabundance, it is necessary to take blood samples for laboratory analysis and identification of parameters the concentration of active compounds in the liquid.

The Most effective measure of stabilizing the patient and preventing the severe consequences of overdose – the use of a specific antidote. Currently, the substances used folinate calcium. It is desirable to use it as soon as possible after admission to the body of excess "Methotrexate". The best effect of the procedure will show if the antidote is taken during the first hours after the main drug. The dosage of calcium folinate – equal used in food volumes "Methotrexate" or more.

After establishing the fact of accepting too much of the drug for the patient's condition is necessary to establish control. From time to time take samples of blood serum to determine the concentration of methotrexate, based on these data, make a decision on the re-application of the antidote. To speed up the withdrawal of the drug from the body, you should drink more, to take measures to boost alkalinity of the urine. To reduce the likelihood of nephropathy induced precipitate the active compounds before introduction to further investigate the urine for the level of alkalinity, to do repeated analyses with six-hour intervals in the application of the antidote. Calcium folinate is used until be achieved in the blood plasma methotrexate concentration up to 0.05 mol/L. the alkalinity must exceed seven units.

Special conditions

Cytological toxicity "Methotrexate" forcing to use the tool very carefully. The drug is prescribed only by experienced, qualified doctors. Actions of medicine is quite specific, so professional enters the patient in the course of possible adverse reactions, including severe. Note that "Methotrexate" could provoke a fatal, irreversible negative effects. To minimize risks, you need to strictly follow the instructions anddeveloped a therapeutic program.

To use "Methotrexate" was as safe as possible, it is important to take a course under the supervision of a physician. Medical supervision will allow time to understand that toxic heavy, and to take steps to improve the condition of the patient. Before you can assign "Methotrexate" the doctor sends the patient for blood tests, to set amounts of platelets, liver enzymes activity, bilirubin, albumin. Additionally prescribe x-ray of the chest, studying the health of the kidneys, and in some cases doing tests to verify the presence of tuberculosis, hepatitis. Is strictly forbidden to use "Methotrexate" discretion – it will cause serious consequences (including death).

Reception: nuances

If the patient is assigned a "Methotrexate", will have to undergo regular tests for quality control of the peripheral circulatory system, blood-forming organs. Doctors monitor the concentration of platelets, leukocytes, on the basis of the received test data to make a decision about the necessity of cancellation of the program, if a drug is poorly tolerated patients.

The First month of use of medication requires blood tests a day, and then lengthen the intervals to three, sometimes five days. Prolonged course of systematic monitoring of blood carried out with ten-day intervals, and in the period of remission – two weeks.

First use "Methotrexate" of the patient should undergo a doctor's examination. The doctor will check the condition of the pharynx, the mucous membranes of the oral cavity. From time to time make tests to determine the activity of liver enzymes, the clearance creatininemia and content of nitrogen in urine and in the blood – uric acid. The patient shows a fluoroscopy of the chest. Three times (before the start of the course, during its passage and upon completion) check operation of the blood-forming organs.

"Methotrexate": effects on liver

In some cases, the drug shows a pronounced toxic effect on the liver, and such is possible as in the acute form and in the chronicle. There is a risk of cirrhosis, fibrosis. In the chronic form, liver toxicity is sometimes observed with a cumulative dose of half a gram or a long (two years and longer) treatment program. In this situation there is a risk of death.

Because the drug is toxic, the manufacturer recommends that in the period of its use to avoid other means can poison the liver. The exception – a situation when the need to use such drugs is obvious, but without them is not possible.

The Level of toxicity depends on the contributing factors that worsen the General condition of the patient. In particular, "Methotrexate" has a stronger impact on the liver when excess weight, diabetes, as well as the elderly and persons suffering from addiction to alcohol.

To adequately assess liver function, it is necessary not only to take samples for analyses in biochemistry, but also to do a biopsy of the organ. As a rule, this analysis first administered before the start of the course, repeat study after 2-4 months.

If selected hepatic fibrosis moderate if symptoms allows to suspect cirrhosis, "Methotrexate" cancel. If the fibrosis has developed a mild degree, six months later, after revealing this fact, need to undergo a repeat biopsy of the organ. If the histological changes is quite weak, "Methotrexate" continue to use, but do it very carefully so as to notice the deterioration of the patient.

Immunity and certain diagnoses

If "Methotrexate" was the cause of diarrhea, stomatitis, complicated by ulcers, the treatment stopped, because the symptoms point to an increased risk of hemorrhagic enteritis. In addition, the high probability of perforation of the intestinal wall.

During the course of treatment is wise to avoid ultraviolet radiation, direct sunlight, because there is a likelihood of sensitivity to light.

"Methotrexate" affects the immune system of the patient. Physicians should take this into account by assigning tests to identify features of the functioning of the immune system. Under the influence of active components of the drug may be an atypical response to the vaccine. After the abolition of the "Methotrexate" from three months to a year is necessary to avoid immunization if the case is not recommended by the doctor directly. All the people living with the patient, at this period must refuse vaccinations against polio. To avoid accidental contact with the people who received this vaccine, you need to wear a protective mask.

Lifestyle and treatment

During the reception, "Methotrexate” patients of reproductive age should use reliable methods of preventing conception. Upon completion of the program, and men must use contraceptives for at least three months, and women – one ovulatory cycle.

To the toxicity of the components of "Methotrexate" was less pronounced during the course, you should use calcium folinate.

"Methotrexate" affects the Central nervous system, causing lethargy, fatigue, and sometimes causes dizziness. This imposes restrictions on the ability of the transport management work with the exact mechanisms.

"Methotrexate": counterparts

Instructions for use of the drug indicates that active compound called "methotrexate" it is because of him the medication was given such a name. On the same connection based drugs:

• ‘Motortec”.
• “Saksat”.
• ‘Metrics”.

As can be seen from the user, analogues "Methotrexate" are drugs ‘Metoject”, “Texan”. If you can not acquire prescribed by a doctor option, the replacement choice should be agreed with the attending physician, otherwise the results of treatment are unpredictable. You need to remember about the toxicity of the active substance, which is based on all these medicines. To use it by choice is unacceptable – the consequences can be very severe.