Methotrexate (Trexall)

Generic Name: Methotrexate

Trexall (methotrexate tablets USP) (formerly Amethopterin) is an antimetabolite used in the treatment of certain neoplastic diseases, severe psoriasis, and adult rheumatoid arthritis. Chemically methotrexate, USP is N-[4[[(2,4-diamino-6-pteridinyl) methyl] methyl-amino]benzoyl]-L-glutamic acid. The structural formula is:


Trexall™ (methotrexate) Structural Formula Illustration

Trexall (methotrexate tablets USP), for oral administration, is available in 5 mg, 7.5 mg, 10 mg and 15 mg strengths.

Each tablet contains methotrexate sodium in an amount equivalent to the labeled amount of methotrexate, USP, and contains the following inactive ingredients: anhydrous lactose, crospovidone, hydroxypropyl methylcellulose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, pregelatinized corn starch, sodium carbonate monohydrate, talc and titanium dioxide.

The 5 mg also contains: D&C yellow no. 10 aluminum lake, FD&C blue no. 1 aluminum lake and FD&C yellow no. 6 aluminum lake.

The 7.5 mg also contains: FD&C blue no.1 aluminum lake.

The 10 mg also contains: FD&C red no. 40 aluminum lake.

The 15 mg also contains: FD&C blue no. 2 aluminum lake and FD&C red no. 40 aluminum lake.

No health feed found.

Methotrexate is an antimetabolite of the antifolate type. It is thought to affect cancer and rheumatoid arthritis by two different pathways. For cancer, methotrexate competitively inhibits dihydrofolate reductase (DHFR), an enzyme that participates in the tetrahydrofolate synthesis. The affinity of methotrexate for DHFR is about 1000-fold that of folate. DHFR catalyses the conversion of dihydrofolate to the active tetrahydrofolate. Folic acid is needed for the de novo synthesis of the nucleoside thymidine, required for DNA synthesis. Also, folate is essential for purine and pyrimidine base biosynthesis, so synthesis will be inhibited. Methotrexate, therefore, inhibits the synthesis of DNA, RNA, thymidylates, and proteins.

For the treatment of rheumatoid arthritis, inhibition of DHFR is not thought to be the main mechanism, but rather multiple mechanisms appear to be involved, including the inhibition of enzymes involved in purine metabolism, leading to accumulation of adenosine; inhibition of T cell activation and suppression of intercellular adhesion molecule expression by T cells; selective down-regulation of B cells; increasing CD95 sensitivity of activated T cells; and inhibition of methyltransferase activity, leading to deactivation of enzyme activity relevant to immune system function. Another mechanism of MTX is the inhibition of the binding of interleukin 1-beta to its cell surface receptor.

Chemotherapy

Methotrexate was originally developed and continues to be used for chemotherapy, either alone or in combination with other agents. It is effective for the treatment of a number of cancers, including: breast, head and neck, leukemia, lymphoma, lung, osteosarcoma, bladder, and trophoblastic neoplasms.

Autoimmune disorders

It is used as a disease-modifying treatment for some autoimmune diseases, including rheumatoid arthritis, juvenile dermatomyositis, psoriasis, psoriatic arthritis, lupus, sarcoidosis, Crohn's disease, eczema and many forms of vasculitis. Although originally designed as a chemotherapy drug (using high doses), in low doses, methotrexate is a generally safe and well tolerated drug in the treatment of certain autoimmune diseases. Because of its effectiveness, low-dose methotrexate is now first-line therapy for the treatment of rheumatoid arthritis. Weekly doses are beneficial for 12 to 52 weeks duration therapy, although discontinuation rates are as high as 16% due to adverse effects. Although methotrexate for autoimmune diseases is taken in lower doses than it is for cancer, side effects such as hair loss, nausea, headaches, and skin pigmentation are still common. Use of low doses of methotrexate together with NSAIDS such as aspirin or analgesics such as paracetamol is relatively safe in people being treated for rheumatoid arthritis, if adequate monitoring is done.

Not everyone with rheumatoid arthritis responds favorably to treatment with methotrexate, but multiple studies and reviews showed that the majority of people receiving methotrexate for up to one year had less pain, functioned better, had fewer swollen and tender joints, and had less disease activity overall as reported by themselves and their doctors. X-rays also showed that the progress of the disease slowed or stopped in many people receiving methotrexate, with the progression being completely halted in about 30% of those receiving the drug. Those individuals with rheumatoid arthritis treated with methotrexate have been found to have a lower risk of cardiovascular events such as myocardial infarctions (heart attacks) and strokes.

Recently, use of methotrexate in combination with anti-TNF agents has been shown to be effective for the treatment of ulcerative colitis.

Methotrexate has also been used for multiple sclerosis.

It is not commonly used for lupus, and only tentative evidence exists to support the practice.

During pregnancy

Methotrexate is an abortifacient and is commonly used to terminate pregnancies during the early stages, generally in combination with misoprostol. It is also used to treat ectopic pregnancies, provided the fallopian tube has not ruptured. Methotrexate with dilatation and curettage is used to treat molar pregnancy.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

  • Black, tarry stools
  • blood in the urine or stools
  • bloody vomit
  • diarrhea
  • joint pain
  • reddening of the skin
  • sores in the mouth or lips
  • stomach pain
  • swelling of the feet or lower legs

Less common

  • Back pain
  • blurred vision
  • confusion
  • convulsions (seizures)
  • cough or hoarseness
  • dark urine
  • dizziness
  • drowsiness
  • fever or chills
  • headache
  • lower back or side pain
  • painful or difficult urination
  • pinpoint red spots on the skin
  • shortness of breath
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Hair loss, temporary
  • loss of appetite
  • nausea or vomiting

Less common

  • Acne
  • boils on skin
  • pale skin
  • skin rash or itching

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For cancer:
      • Adults—Dose is based on type of cancer and body size and must be determined by your doctor. A dose of 10 to 30 milligrams (mg) once per day may be given for several days and then repeated after a rest period. For some conditions, 5 to 50 mg once per week may be used. Your doctor may adjust your dose as needed.
      • Children—Dose is based on type of cancer and body size and must be determined by your doctor. The dose is generally given once per day for several days and then repeated after a rest period. The dose may also be given once per week. Your doctor may adjust your dose as needed.
    • For psoriasis:
      • Adults—At first, 10 to 25 milligrams (mg) once per week or 2.5 mg every 12 hours for 3 doses once each week. Your doctor may adjust your dose as needed. However, the dose is usually not more than 30 mg once per week.
      • Children—Use and dose must be determined by your doctor.
    • For rheumatoid arthritis or juvenile arthritis:
      • Adults—At first, 7.5 milligrams (mg) once per week or 2.5 mg every 12 hours for 3 doses once each week. Your doctor may adjust your dose as needed.
      • Children—Dose is based on body size and must be determined by your doctor. The starting dose is 10 milligrams (mg) per square meter (m(2)) of body size once per week. Your doctor may adjust your dose as needed.

Missed Dose

This medicine needs to be given on a fixed schedule. If you miss a dose or forget to use your medicine, call your doctor or pharmacist for instructions.

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Measles Virus Vaccine, Live
  • Mumps Virus Vaccine, Live
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Varicella Virus Vaccine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Aceclofenac
  • Acemetacin
  • Adenovirus Vaccine
  • Amoxicillin
  • Amtolmetin Guacil
  • Asparaginase
  • Aspirin
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Bentiromide
  • Bromfenac
  • Bufexamac
  • Capecitabine
  • Celecoxib
  • Chloral Hydrate
  • Cholera Vaccine, Live
  • Choline Salicylate
  • Clonixin
  • Dantrolene
  • Dasabuvir
  • Dexibuprofen
  • Dexketoprofen
  • Dexlansoprazole
  • Diclofenac
  • Dicloxacillin
  • Diflunisal
  • Dipyrone
  • Doxifluridine
  • Doxycycline
  • Droxicam
  • Esomeprazole
  • Etodolac
  • Etofenamate
  • Felbinac
  • Fenbufen
  • Fenoprofen
  • Fepradinol
  • Feprazone
  • Floctafenine
  • Floxacillin
  • Flufenamic Acid
  • Fluorouracil
  • Flurbiprofen
  • Foscarnet
  • Fosphenytoin
  • Hydrochlorothiazide
  • Ibuprofen
  • Ibuprofen Lysine
  • Indomethacin
  • Influenza Virus Vaccine, Live
  • Ketoprofen
  • Ketorolac
  • Leflunomide
  • Levetiracetam
  • Lornoxicam
  • Loxoprofen
  • Lumiracoxib
  • Meclofenamate
  • Mefenamic Acid
  • Meloxicam
  • Mezlocillin
  • Morniflumate
  • Nabumetone
  • Naproxen
  • Nepafenac
  • Niflumic Acid
  • Nimesulide
  • Nimesulide Beta Cyclodextrin
  • Omeprazole
  • Oxaprozin
  • Oxyphenbutazone
  • Pantoprazole
  • Parecoxib
  • Penicillin G
  • Penicillin V
  • Phenylbutazone
  • Phenytoin
  • Piketoprofen
  • Piperacillin
  • Piroxicam
  • Pirprofen
  • Poliovirus Vaccine, Live
  • Pristinamycin
  • Probenecid
  • Proglumetacin
  • Propionic Acid
  • Propyphenazone
  • Proquazone
  • Pyrimethamine
  • Rabeprazole
  • Salicylic Acid
  • Salsalate
  • Simeprevir
  • Smallpox Vaccine
  • Sodium Salicylate
  • Sulfamethizole
  • Sulfamethoxazole
  • Sulfapyridine
  • Sulfisoxazole
  • Sulindac
  • Tamoxifen
  • Tegafur
  • Tenoxicam
  • Teriflunomide
  • Tiaprofenic Acid
  • Ticarcillin
  • Tolfenamic Acid
  • Tolmetin
  • Triamterene
  • Trimethoprim
  • Typhoid Vaccine
  • Valdecoxib
  • Warfarin
  • Yellow Fever Vaccine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Amiodarone
  • Cyclosporine
  • Eltrombopag
  • Etoricoxib
  • Mercaptopurine
  • Procarbazine
  • Rofecoxib
  • Theophylline

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Cola

Take this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of methotrexate for the treatment of cancer and juvenile idiopathic arthritis in children. However, safety and efficacy have not been established in children with psoriasis.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of methotrexate in the elderly. However, elderly patients are more likely to have kidney problems, which may require caution and an adjustment in the dose.

Pregnancy

Studies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.

Breastfeeding

Studies in women breastfeeding have demonstrated harmful infant effects. An alternative to this medication should be prescribed or you should stop breastfeeding while using this medicine.

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