Phenteramine

Methotrexate

Methotrexate


Methotrexate

Pharmacokinetics

The antitumoral, cytostatic agent of group of antimetabolites.
Brakes synthesis, a reparation of DNA and a cellular mitosis. Along with the antitumoral possesses immunodepressive action.
The absorption at peroral reception depends on a dose: at reception of 30 mg / sq. m is soaked up well, average bioavailability - 60 %. The absorption decreases at reception in the doses exceeding 80 mg / sq. m (believe, owing to saturation).
It is deduced mainly by kidneys in not changed kind by a glomerular filtration and canalicular secretion (at i.v. introduction of 80-90 % it is deduced during 24), with bile about 10 % are deduced. Deducing of a preparation at patients with disturbance of function of the kidneys, the expressed ascites or a transudate is considerably slowed down. At repeated introduction collects in tissues in the form of polyglutamates.

Indications

A mammary gland cancer, an epidermoid cancer of a head and a neck, a lung cancer, a cancer of a neck of a uterus, an ovary cancer, a bladder cancer, a colorectal cancer, an esophagus cancer, a carcinoma of the stomach, a pancreas cancer, a testicle cancer, a lymphogranulomatosis, a fungoides mycosis, not metastatic osteosarcoma, a sarcoma of soft tissues, a cancer of cerebral covers.
Serious forms of a psoriasis, psoriasis arthritis, pseudorheumatism, dermatomyositis, HARD CURRENCY, ankylosing spondylarthritis.

Contraindications

Hypersensitivity, an immunodeficiency, pregnancy, the lactemia period.
At treatment of a psoriasis and rheumatic diseases (in addition): serious oppression of a medullar hemopoiesis, serious hepatic/renal insufficiency.

Dosage

Doses and treatment terms establish individually depending on the scheme of chemotherapy, indications, the scheme of treatment, "answer" of the patient and shipping, pay off proceeding from the area of a surface of a body or body mass.

Side effect

From hemopoiesis organs: a leukopenia and a thrombocytopenia, a pancytopenia, an anaemia (including aplastic), a neutropenia, an agranulocytosis, an eosinophilia, a lymphadenopathy.
From the alimentary system: an anorexia, a nausea, vomiting, a stomatitis, an ulitis, a pharyngitis, an enteritis, erozivno-ulcer lesions and a bleeding from GASTROINTESTINAL TRACT (including a melena, a hematemesis), a hepatotoxic (an acute hepatitis, a fibrosis and a cirrhosis, hepatic insufficiency, a hypoalbuminemia, rising of activity of "hepatic" transaminases), a pancreatitis.
From nervous system: a headache, drowsiness, a dysarthtia, an aphasia, a hemiparesis, a paresis, cramps; emotional lability; unusual cranial sensitivity, an encephalopathy (including a leukoencephalopathy).
From genitourinary system: a cystitis, a nephropathy, disturbance of function of kidneys (an azotemia, a hematuria, a hyperuricemia), ovogenesis and spermatogenesis disturbances, a dysmenorrhea, an oligospermatism, sterility, an abortion, anomalies of a fetation.
From integuments: an erythematic eruption, a skin itch, an urticaria, photosensitivity, xanthopathy disturbance, an alopecia, an ecchymoma, a telangiectasia, eels, a furunculosis, a toxic epidermal necrolysis, an ulceration and a skin necrosis, an exfoliative dermatitis.
From a sight organ: a conjunctivitis, sight disturbance (including transient blindness).
From respiratory system: seldom - a pneumosclerosis, respiratory insufficiency, an alveolitis, an intersticial pneumonitis (including fatal).
From party SSS: a pericarditis, a pericardiac exudate, BP depression, a thromboembolism (including an arterial clottage, a clottage of cerebral vessels, a deep vein thrombosis, a retina vein thrombosis, a thrombophlebitis, a pulmonary embolism).
From genitourinary system: a serious nephropathy or renal insufficiency, an azotemia, a cystitis, a hematuria, a proteinuria, disturbance spermato - and an ovogenesis, a transitional oligospermatism, an impotency, a dysmenorrhea, vaginal allocation, a gynecomastia, sterility, destruction of a foetus, defects of a fetation.
From a locomotorium: an arthralgia, an osteoporosis, an osteonecrosis, fractures.

Overdosage

Symptoms: no, it is diagnosed on concentration of Methotrexatum in plasma.

Special indicatings

Methotrexatum is a cytotoxic preparation, therefore in circulation it is necessary to be careful with it.
It is necessary to observe carefully measures on contraception when one of partners accepted Methotrexatum.
For timely revealing of symptoms of an intoxication it is necessary to supervise a condition of peripheric blood, activity of "hepatic" transaminases, function of kidneys (an urea nitrogen, KK and-or Serum creatinine), concentration of urinary acid in blood serum, periodically to spend a roentgenoscopy of organs of a thorax.
It is necessary to carry out researches of an oral cavity of the patient on presence of ulcerations before each application.
At development of a diarrhoeia and a stomacace it is necessary to interrupt therapy by Methotrexatum owing to high risk of development of a hemorrhagic enteritis and perforation of a wall of an intestine which can lead to death of the patient.
Methotrexatum can potentially lead to development of symptoms of an acute or chronic hepatotoxic (including to a fibrosis and a cirrhosis). The chronic hepatotoxic usually develops after long application of Methotrexatum (usually within 2 or more years) or achievements of the general cumulative dose not less than 1.5 g and can lead to a failure. The hepatotoxic effect can be caused also the burdened accompanying anamnesis (an alcoholism, adiposity, a diabetes) and senile age.

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