Methotrexate in psoriasis: treatment and dosage regimen

Methotrexate in psoriasis is one of the components of the main treatment of the disease.

Psoriasis is characterized by limited or widespread damage to the skin, the development of inflammation, itching. In the pathological process can involve both skin integuments, and joints, and even internal organs.

Psoriasis is considered a chronic disease that occurs with periodic exacerbations and stages of relief (remission).

[1], [2], [3]

Indications of the methotrexate in psoriasis

Methotrexate is used to treat severe forms of psoriasis. The purpose of the drug is:

• acceleration of tissue regeneration;
• stop the development of inflammatory reaction;
• relief of movements in psoriasis of joints.

Despite the fact that Methotrexate is a medicine from the group of cytostatics, its action is not limited to the properties of the antitumor drug. Methotrexate inhibits the active progression of psoriasis, relieves pain syndrome. The earlier the treatment is started, the more effective the effect of the drug will be.

In addition to the severe forms of psoriasis, Methotrexate is used to treat rheumatoid arthritis, with severe mycotic lesions, with trophoblastic neoplasms, and with acute form of lymphoblastic leukemia.

[4], [5]

Release form

Methotrexate is an antitumor agent that is produced in the form of tablets for ingestion, or as a solution for injection (intramuscular or intravenous injection).

The active ingredient of the drug is methotrexate - an antineoplastic agent, an antimetabolite, a structural analogue of folic acid.

[6], [7], [8], [9]

Pharmacodynamics

Methotrexate is a drug that belongs to the group of antimetabolites and exhibits cytostatic and immunosuppressive effects. The structure of this substance is close to the structural structure of folic acid, however, Methotrexate is considered its antagonist. Other properties Methotrexate:

• inhibition of the conversion of dihydrofolic acid to tetrahydrofolic acid;
• oppression of DNA production and the process of cell division, production of RNA and protein.

The most sensitive to the action of the drug are tumor tissues, bone marrow, epithelium and fetal cell structures.

[10], [11], [12], [13]

Pharmacokinetics

After ingestion of Methotrexate in the body, the limiting amount of the drug is detected after about 45 minutes. The active component freely spreads in tissues and body fluids. In kidneys, remnants of the drug are found for several weeks, in the liver - for several months.

When a standard amount of the drug Methotrexate is administered, its penetration through the blood-brain barrier is not observed.

The metabolic processes take place mainly in the liver, with the formation of the active substance - polyglutamate.

The half-life period depends on the dose of methotrexate taken, and can be from 3 to 10 hours with a small amount of the drug, or from 8 to 15 hours with a significant amount of the drug.

Most of the drug (at least 90%) is excreted from the body by the kidneys, and only a small amount is removed from the bile, throughout the day.

[14], [15], [16], [17]

Dosing and administration

Methotrexate in psoriasis is taken in an amount of 10-25 mg per week, with a gradual increase in dosage. The initial dose is usually 5 to 10 mg once a week.

The drug can be taken orally, either as intramuscular or intravenous injections, depending on the patient's condition.

The maximum amount of the drug is 30 mg per week.

The scheme for taking methotrexate in psoriasis

The regimen for taking methotrexate in psoriasis should comply with the following rules:

• taking the next dose should be done on the same day of the week, at the same time;
• the drug is administered with a gradual increase in dosage;
• at the time when the clinical effect of Methotrexate becomes noticeable, proceed to a gradual lowering of the dosage, stopping at an optimally low amount of the drug.

Currently, these regimens of methotrexate are most commonly used:

1. The course of admission is 4-6 weeks, three times a week in the amount of 2.5 mg.
2. With the increase and regression of acute symptoms 1 time per week from 10 to 30 mg. The course of admission is 4-6 weeks.

Methotrexate in psoriasis is better taken before meals, or 1-1,5 hours after it.

[23], [24], [25], [26], [27]

Use of the methotrexate in psoriasis during pregnancy

It has been proved that Methotrexate has a significant teratogenic effect and can provoke death or intrauterine defects of the fetus.

In situations where the patient becomes pregnant during the treatment with Methotrexate medicament, it is necessary to raise the issue of artificial abortion, since the risk of fetal damage is considered very likely. Usually, before proceeding to treatment with the drug, women of childbearing age are recommended to take oral contraceptives in order to avoid a possible pregnancy.

During lactation, taking Methotrexate is also contraindicated, since the drug has the property of getting into the composition of breast milk.

Contraindications

Methotrexate is not prescribed for psoriasis:

• during pregnancy and breastfeeding;
• with serious pathologies of the liver and (or) kidneys;
• with serious violations of hematopoiesis or with a significant drop in hemoglobin;
• with exacerbation of infectious pathologies;
• with HIV infection;
• with a tendency to allergy to methotrexate;
• in childhood (up to 3 years).

Methotrexate in psoriasis is used only under the constant supervision of a doctor in such situations:

• with the accumulation of fluid in the abdominal or pleural cavity;
• with ulcer of stomach and duodenum;
• with ulceration of the intestine;
• with pronounced dehydration;
• with gout;
• after carrying out irradiation or treatment with chemotherapy;
• during viral, microbial or fungal infections.

[18], [19], [20], [21]

Side effects of the methotrexate in psoriasis

Admission Methotrexate in psoriasis can be accompanied by a large number of adverse events. The most common symptoms are:

• anemia, changes in blood picture;
• emaciation, attacks of nausea and vomiting, inflammatory changes in mucous membranes, erosion and ulcers in the digestive system;
• inflammation of liver tissue, pancreatitis;
• pain in the head, sleep disturbance, impaired sensitivity in the limbs, convulsions;
• instability of the emotional state;
• conjunctivitis, temporary deterioration of vision;
• lowering of blood pressure, thrombosis, inflammation of the pericardium;
• pulmonary fibrosis, pulmonary obstruction, interstitial pneumonia;
• impaired kidney function, inflammation of the bladder, impaired sperm quality, impaired libido, difficulty in conceiving, miscarriage;
• redness of the skin, acne, burning;
• pain in the joints, muscle pain, osteoporosis;
• allergy, sepsis, hyperhidrosis;
• development of lymphoma.

[22],

Overdose

Excess of substance Methotrexate in the blood is characterized by the following symptoms:

• sharp and growing thinning;
• dizziness, fog before the eyes;
• depressive state;
• coma;
• increasing leukopenia.

To eliminate signs of overdose, calcium folinate is prescribed, which is a substance that neutralizes the toxic effect of Methotrexate.

Calcium folinate is used as an intravenous infusion, in an amount of 75 mg for 12 hours. After this, they switch to intramuscular injection of the substance, in an amount of 12 mg four times with a time interval of six hours.

With the development of negative side effects from treatment with the drug Methotrexate, intramuscular calcium folinate is administered in an amount of 6 to 12 mg four times with a six-hour time interval.

[28], [29], [30], [31]

Interactions with other drugs

When using Methotrexate in psoriasis, there may be a weakening of the natural immune response.

The combination of methotrexate and the introduction of live vaccines can lead to pronounced antigenic reactions.

Acceleration of excretion Methotrexate can cause drugs such as salicylates, sulfonamides, tetracycline antibiotics, chloramphenicol, cyclophosphamide, hypnotics.

Methotrexate is excreted mainly through the kidneys, so interactions with medications that are similarly produced can occur. Result of such interaction can become changes in the level of Methotrexate in the blood.

In combination with the drug Probenecid, the dosage of Methotrexate is reduced.

Methotrexate is incompatible with hepatotoxic and nephrotoxic medicines, as well as with alcohol.

Combinations of medicines Methotrexate and non-steroidal anti-inflammatory drugs can lead to an increase in toxic side effects.

[32], [33], [34], [35], [36], [37]

Storage conditions

Methotrexate is kept at a moderate room temperature, not exceeding + 25 ° C, away from children's access.

[38], [39], [40], [41]

Shelf life

Shelf life of the drug - up to 2 years.

[42], [43]

Acceptance of Methotrexate in psoriasis

Methotrexate is a potent enough drug, the reception of which has its positive and negative sides.

On the one hand, Methotrexate in psoriasis really helps. This drug is often prescribed in the most neglected and complex cases of the disease, when it is not possible to achieve relief from the use of other medications.

On the other hand, Methotrexate has a large list of side effects. And they are by no means harmless: it can be a defeat of the respiratory, cardiovascular, nervous system, as well as some other organs.

Take Methotrexate in psoriasis, or not - this decision should be made by the patient, after consultation with a doctor in advance. If there are no contraindications, then it is possible to conduct a trial course of treatment with the drug, adhering to the optimally effective but minimal dosage. If you have unwanted symptoms, you must tell them about it - maybe it will change the dosage or replace the drug with another one that is more suitable for your body.

[44], [45], [46], [47], [48], [49],