Methotrexate belongs to the group of antimetabolites with cytostatic activity. It inhibits the conversion of dihydrofolic acid into tetrahydrofolic acid. Thymidylic acid and purine synthesis are disrupted, which, in turn, suppresses DNA synthesis and cell division. The maximum absorption of the medicine is observed after 30 to 60 minutes. The drug is metabolized by enzymes of the intestinal microflora, hepatocytes, and other cells.
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The pills are a component of the group of antimetabolites with cytostatic activity. They reduce the change of dihydrofolic acid in tetrahydrofolic acid.
There are changes in Timpilo acid and purine, which in turn changes the connection of DNA and division of cells, the connection of RNA and protein. The peculiarity of the drug is in the s-phase of the cell cycle. The most sensitive to the drug are tissues with high proliferative potential (tumor tissue, bone marrow, epithelial cells, and fetal cells).
After 30 to 60 minutes, administration to the muscle has the highest concentration. The drug is well dispersed in body tissues, as well as in ascitic and pleural fluids. The kidney tissue is determined in several weeks and the tissues of the liver, for three months. When the pills are used in medium amounts, they do not penetrate the blood-brain barrier. It is metabolized by enzymes of the intestinal microflora, hepatocytes and other cells with the formation of active metabolite – pollutant (inhibitor of dihydrofolate reductase and timdelaghetto).
The terminal half-life time is dose-dependent and lasts from three to ten hours and eight to fifteen hours when using small and large doses of the drug. 90% of the received dose comes out with urine in its present form by glomerular filtration and active tubular secretion and only ten percent – within 24 hours with bile (followed by reabsorption in the intestine).
The components mostly come out with urine and its characteristics do not change. When the activity of kidney function is impaired, the elimination of methotrexate decreases speed, while its concentration in the blood plasma increases. The components could be released into breast milk.
The pills cannot be combined with strong oxidants and acids. If they are mixed with chlorpromazine hydrochloride, droperidol, metoclopramide hydrochloride, heparin solution, prednisolone sodium phosphate and hydrochloride promethazine it would be possible to obtain its turbidity or precipitate formation.
The amount is calculated according to the weight of the person or the surface area of the skin. The tablets are effective in case of a large number of cancers as a monotherapy, and in combination with other chemotherapy drugs.
The pills have a negative impact on the blood system: it inhibits bone marrow function (as a result it leads to infection, sepsis, bleeding), thrombocytopenia, leukopenia, anemia, and hematoma. In the digestive system, there are such problems as gingivitis, stomatitis, pharyngitis, nausea may appear, and the patient often goes to the toilet experiencing stomach disorders. Sometimes people taking this drug feel a violation of liver function. There a liver dystrophy, erosive and ulcerative disorders of the mucous membrane of the stomach and intestines, and a liver failure may happen.
As for disorders in the nervous system, a person has a headache, dizziness, vision impairment, hemiparesis, seizures. After intrathecal administration, the pressure of cerebrospinal fluid increases. In the genitourinary system: a person starts to suffer from cystitis, azotemia, hematuria, women have the menstrual disorder, infertility, vaginal, spontaneous abortion, teratogenic effect, decreased libido, impotence, ovogenesis, spermatogenesis. Pills can lead to negative consequences of the skin such as rash, skin can itch, acne, furunculosis develops. Sometimes there is a Stevens-Johnson syndrome.