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Trexall

Generic Name: Methotrexate Sodium
Drug Category: Antimetabolite
Litigation Alert Level: Medium
This drug has been approved for use by males and females over the age of 2 years old for a maximum duration of 4 years.

Approved Uses

Indicated for:

Neoplastic Diseases:

• The treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole.

• Methotrexate is used in maintenance therapy in combination with other chemotherapeutic agents.

• Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas.

Psoriasis:

• The symptomatic control of severe, recalcitrant, disabling psoriasis that is not adequately responsive to other forms of therapy, but only when the diagnosis has been established, as by biopsy and/or after dermatologic consultation. It is important to ensure that a psoriasis “flare” is not due to an undiagnosed concomitant disease affecting immune responses.

Rheumatoid Arthritis Including Polyarticular-Course Juvenile Rheumatoid Arthritis:

• The management of selected adults with severe, active, rheumatoid arthritis (ARC criteria), or children with active polyarticular-course juvenile rheumatoid arthritis, who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of first-line therapy including full dose non-steroidal anti-inflammatory agents (NSAIDs).

Safety and effectiveness in pediatric patients have been established, only in cancer chemotherapy and in polyarticular-course juvenile rheumatoid arthritis.

Patients with psoriasis or rheumatoid arthritis with alcoholism, alcoholic liver disease or other chronic liver disease should not receive methotrexate.

Patients with psoriasis or rheumatoid arthritis who have overt or laboratory evidence of immunodeficiency syndromes should not receive methotrexate.

Patients with psoriasis or rheumatoid arthritis who have preexisting blood dyscrasias, such as bone marrow hypoplasia, leukopenia, thrombocytopenia or significant anemia, should not receive methotrexate. 

Because of the possibility of serious toxic reactions (which can be fatal): methotrexate should be used only in life threatening neoplastic diseases, or in patients with psoriasis or rheumatoid arthritis with severe, recalcitrant, disabling disease which is not adequately responsive to other forms of therapy.

Deaths have been reported with the use of methotrexate in the treatment of malignancy, psoriasis, and rheumatoid arthritis.

Patients should be closely monitored for bone marrow, liver, lung and kidney toxicities.

Methotrexate causes hepatotoxicity, fibrosis and cirrhosis, but generally only after prolonged use. Acutely, liver enzyme elevations are frequently seen. These are usually transient and asymptomatic, and also do not appear predictive of subsequent hepatic disease. Liver biopsy after sustained use often shows histologic changes, and fibrosis and cirrhosis have been reported; these latter lesions may not be preceded by symptoms or abnormal liver function tests in the psoriasis population. For this reason, periodic liver biopsies are usually recommended for psoriatic patients who are under long-term treatment.

Persistent abnormalities in liver function tests may precede appearance of fibrosis or cirrhosis in the rheumatoid arthritis population.Methotrexate-induced lung disease is a potentially dangerous lesion, which may occur acutely at any time during therapy and which has been reported at doses as low as 7.5 mg/week. It is not always fully reversible. Pulmonary symptoms (especially a dry, nonproductive cough) may require interruption of treatment and careful investigation.

Diarrhea and ulcerative stomatitis require interruption of therapy; otherwise, hemorrhagic enteritis and death from intestinal perforation may occur.

Malignant lymphomas, which may regress following withdrawal of methotrexate, may occur in patients receiving low-dose methotrexate and, thus, may not require cytotoxic treatment. Discontinue methotrexate first and, if the lymphoma does not regress, appropriate treatment should be instituted.

Like other cytotoxic drugs, methotrexate may induce “tumor lysis syndrome” in patients with rapidly growing tumors. Appropriate supportive and pharmacologic measures may prevent or alleviate this complication.

Severe, occasionally fatal, skin reactions have been reported following single or multiple doses of methotrexate. Reactions have occurred within days of oral, intramuscular, intravenous, or intrathecal methotrexate administration. Recovery has been reported with discontinuation of therapy.

Potentially fatal opportunistic infections, especially Pneumocystis carinii pneumonia, may occur with methotrexate therapy.

Methotrexate given concomitantly with radiotherapy may increase the risk of soft tissue necrosis and osteonecrosis.

Unexpectedly severe (sometimes fatal) bone marrow suppression, aplastic anemia, and gastrointestinal toxicity have been reported with concomitant administration of methotrexate (usually in high dosage) along with some non-steroidal anti-inflammatory drugs (NSAIDs).

Combined use of methotrexate, USP with gold, penicillamine, hydroxychloroquine, sulfasalazine, or cytotoxic agents, has not been studied and may increase the incidence of adverse effects. Rest and physiotherapy as indicated should be continued.

Oral antibiotics such as tetracycline, chloramphenicol, and nonabsorbable broad spectrum antibiotics, may decrease intestinal absorption of methotrexate or interfere with the enterohepatic circulation by inhibiting bowel flora and suppressing metabolism of the drug by bacteria.

Penicillins may reduce the renal clearance of methotrexate; increased serum concentrations of methotrexate with concomitant hematologic and gastrointestinal toxicity have been observed with methotrexate. Use of methotrexate with penicillins should be carefully monitored.

Patients receiving concomitant therapy with methotrexate and other potential hepatotoxins (e.g., azathioprine, retinoids, sulfasalazine) should be closely monitored for possible increased risk of hepatotoxicity.

Methotrexate may decrease the clearance of theophylline; theophylline levels should be monitored when used concurrently with methotrexate.

Certain side effects such as mouth sores may be reduced by folate supplementation with methotrexate.

Trimethoprim and sulfamethoxazole has been reported rarely to increase bone marrow suppression in patients receiving methotrexate, probably by an additive antifolate effect.

Methotrexate has been reported to cause fetal death and/or congenital anomalies. Therefore, it is not recommended for women of childbearing potential unless there is clear medical evidence that the benefits can be expected to outweigh the considered risks. Pregnant women with psoriasis or rheumatoid arthritis should not receive methotrexate.

Women of childbearing potential should not be started on methotrexate until pregnancy is excluded and should be fully counseled on the serious risk to the fetus should they become pregnant while undergoing treatment. Pregnancy should be avoided if either partner is receiving methotrexate; during and for a minimum of three months after therapy for male patients, and during and for at least one ovulatory cycle after therapy for female patients.

Because of the potential for serious adverse reactions from methotrexate in breast fed infants, it is contraindicated in nursing mothers.

GoToSource

Off-label Uses

• Use for psoriasis in patients under the age of 18. GoToSource 

• Chronic inflammatory rheumatic diseases. GoToSource 

• Dermatomyositis and systemic (polymyositis) sarcoid vasculitis. GoToSource 

• For early abortion. GoToSource 

• Alopecia areata. GoToSource 

• Ulcerative colitis. GoToSource 

• Implant-related temporomandibular joint pain. GoToSource 

• Ankylosing spondylitis. GoToSource 

• Sarcoidosis. GoToSource 

• Steroid-resistant relapsing IgG4-related pachymeningitis. GoToSource 

• Posterior uveitis. GoToSource

Adverse Events

Acute encephalomyelitis (inflammation of the brain and spinal cord). GoToSource 

Skin erosions. GoToSource

Birth defects. GoToSource 

Interstitial pneumonitis (progressive scarring of the lungs). GoToSource 

Subclinical ovarian dysfunction (loss of ovarian activity). GoToSource

B-cell lymphoproliferative disorders. GoToSource

Central nervous system toxicity including seizures. GoToSource 

Fatalities. GoToSource

Fibrosing cholestatic hepatitis. GoToSource 

Liver fibrosis (scarring of the liver). GoToSource

Myeloid sarcoma. GoToSource 

Pleuropericarditis and eosinophilic pleural effusion. GoToSource 

Hepatotoxicity (liver damage). GoToSource 

Nephrotoxicity (kidney damage). GoToSource 

Epstein-barr virus-associated lymphoproliferative disorder in the gingiva. GoToSource 

Increased risk of cancer. GoToSource 

Mouth ulcers. GoToSource 

Hemiparesis and facial palsy. GoToSource 

Myelopathy (spinal cord disorder). GoToSource 

Pulmonary tuberculosis, renal cell carcinoma and lateral uveitis (eye inflammation). GoToSource 

Cirrhosis (late-stage scarring of the liver). GoToSource 

Stomatitis (inflammation of the mucous membrane of the mouth). GoToSource

Pancytopenia (reduced number of red and white blood cells and platelets), anaemia (low number of red blood cells) and thrombocytopenia (low blood platelet count). GoToSource 

Bone loss. GoToSource

Litigation

Lawsuits filed for lymphomas, liver, lung and kidney damage. 

The material contained in GoToPills is for informational purposes only and not intended to replace the judgment, evaluation and treatment of physicians, pharmacists and other healthcare providers. GoToPills does not provide medical advice, diagnoses or treatment. Always seek the advice of your physician or other qualified health provider regarding a medical condition or treatment.

 

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Site Last Updated March 28, 2024