Methotrexate

Pronunciation
Generic Name: methotrexate (oral) (meth oh TREX ate)
Brand Names: Rheumatrex Dose Pack, Trexall

What is methotrexate?
Methotrexate interferes with the growth of certain cells of the body, especially cells that
reproduce quickly, such as cancer cells, bone marrow cells, and skin cells.

Methotrexate is used to treat certain types of cancer of the breast, skin, head and neck,
or lung. It is also used to treat severe psoriasis and rheumatoid arthritis.

Methotrexate is usually given after other medications have been tried without successful
treatment of symptoms.

Methotrexate may also be used for purposes not listed in this medication guide.

Important information
Methotrexate is usually taken once or twice per week and not every day. You must use
the correct dose for your condition. Some people have died after taking methotrexate
every day by accident.

Do not use methotrexate to treat psoriasis or rheumatoid arthritis if you have liver
disease (especially if caused by alcoholism), or a blood cell or bone marrow disorder.

Do not use methotrexate if you are pregnant or breast-feeding a baby.

Methotrexate can lower blood cells that help your body fight infections and help your

blood to clot. You may get an infection or bleed more easily. Call your doctor if you have

unusual bruising or bleeding, or signs of infection (fever, chills, body aches).

Methotrexate can cause serious or life-threatening side effects on your liver, lungs, or

kidneys. Tell your doctor if you have upper stomach pain, loss of appetite, dark urine,

clay-colored stools, jaundice (yellowing of the skin or eyes), dry cough, shortness of

breath, blood in your urine, or little or no urinating.

Before taking this medicine

You should not use this medicine if you are allergic to methotrexate. Do not use

methotrexate to treat psoriasis or rheumatoid arthritis if you have:

alcoholism, cirrhosis, or other liver disease;
a blood cell disorder such as anemia (lack of red blood cells) or leukopenia (lack
of white blood cells);
a bone marrow disorder; or
if you are breast-feeding a baby.
Methotrexate is sometimes used to treat cancer even when patients do have one of the

conditions listed above. Your doctor will decide if this treatment is right for you.
To make sure methotrexate is safe for you, tell your doctor if you have:
kidney disease;
a folate deficiency;
pneumonia or lung disease;
stomach ulcers;
any type of infection; or
if you are receiving radiation treatments.
FDA pregnancy category X. Methotrexate can cause birth defects in an unborn baby. Do

not use methotrexate to treat psoriasis or rheumatoid arthritis if you are pregnant. Tell

your doctor right away if you become pregnant during treatment.

See also: Pregnancy and breastfeeding warnings (in more detail)
You may need to have a negative pregnancy test before starting this treatment.
Use birth control to prevent pregnancy while you are using methotrexate, whether you

are a man or a woman. Methotrexate use by either parent may cause birth defects.
If you are a man, use a condom to keep from causing a pregnancy while you are using

methotrexate. Continue using condoms for at least 90 days after your treatment ends.
If you are a woman, use an effective form of birth control while you are taking

methotrexate, and for at least one cycle of ovulation after your treatment ends.
Do not give this medicine to a child without the advice of a doctor.
Older adults may be more likely to have side effects from this medication.
How should I take methotrexate?

Take methotrexate exactly as it was prescribed for you. Follow all directions on your

prescription label. Do not take this medicine in larger or smaller amounts or for longer

than recommended.
You must use the correct dose of methotrexate for your condition. Methotrexate is

sometimes taken once or twice per week and not every day. Follow the directions on

your prescription label. Some people have died after taking methotrexate every day by

accident. Ask your doctor or pharmacist if you have questions about your dosage or how

often to take this medicine.

Use methotrexate regularly to get the most benefit. Get your prescription refilled before

you run out of medicine completely.

Methotrexate can lower blood cells that help your body fight infections and help your

blood to clot. Your blood will need to be tested often, and you may need an occasional

liver biopsy. Your cancer treatments may be delayed based on the results of these tests.
Store at room temperature away from moisture and heat.
See also: Dosage Information (in more detail)

What happens if I miss a dose?

Call your doctor for instructions if you miss a dose of methotrexate.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An

overdose of methotrexate can be fatal.

What should I avoid?

Methotrexate can pass into body fluids (urine, feces, vomit). Caregivers should wear

rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or

laundry or changing diapers. Wash hands before and after removing gloves. Wash

soiled clothing and linens separately from other laundry.

Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds), especially if

you are being treated for psoriasis. Methotrexate can make your skin more sensitive to

sunlight and your psoriasis may worsen.

Avoid drinking alcohol while taking methotrexate.

Methotrexate side effects

Get emergency medical help if you have any signs of an allergic reaction to

methotrexate: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Stop using methotrexate and call your doctor at once if you have:
dry cough, shortness of breath;
diarrhea, vomiting, white patches or sores inside your mouth or on your lips;
blood in your urine or stools;
swelling, rapid weight gain, little or no urinating;
seizure (convulsions);
fever, chills, body aches, flu symptoms;
pale skin, easy bruising, unusual bleeding, weakness, feeling light-headed or
short of breath;
liver problems - nausea, upper stomach pain, itching, tired feeling, loss of
appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
severe skin reaction - fever, sore throat, swelling in your face or tongue, burning
in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially
in the face or upper body) and causes blistering and peeling.
Common methotrexate side effects may include:
vomiting, upset stomach;
headache, dizziness, tired feeling; or
blurred vision.
This is not a complete list of side effects and others may occur. Call your doctor for

medical advice about side effects. You may report side effects to FDA at 1-800-FDA-

1088.
See also: Side effects (in more detail)

Methotrexate dosing information

Usual Adult Dose of Methotrexate for Acute Lymphoblastic Leukemia:

Induction: 3.3 mg/m2/day orally or IM (in combination with prednisone 60 mg/m2).

Maintenance (during remission): 15 mg/m2 IM or orally twice a week.

Alternate remission dosing: 2.5 mg/kg IV every 14 days.

Usual Adult Dose of Methotrexate for Choriocarcinoma:
15 to 30 mg IM or orally daily for 5 days. Repeat courses 3 to 5 times with a rest period

of greater than or equal to 1 week between courses, until any manifesting toxic

symptoms subside.

Effectiveness of therapy is ordinarily evaluated by 24 hour quantitative analysis of

urinary chorionic gonadotropin (hCG), which generally will return to normal or less than

50 intl units/24 hours usually after the third or fourth course and usually followed by a

complete resolution of measurable lesions in 4 to 6 weeks. One to two courses of

methotrexate after normalization of hCG is usually recommended.

Usual Adult Dose of Methotrexate for Trophoblastic Disease:
15 to 30 mg IM or orally daily for 5 days. Repeat courses 3 to 5 times with a rest period

of greater than or equal to 1 week between courses, until any manifesting toxic

symptoms subside.
Effectiveness of therapy is ordinarily evaluated by 24 hour quantitative analysis of

urinary chorionic gonadotropin (hCG), which generally will return to normal or less than

50 intl units/24 hours usually after the third or fourth course and usually followed by a

complete resolution of measurable lesions in 4 to 6 weeks. One to two courses of

methotrexate after normalization of hCG is usually recommended.

Usual Adult Dose of Methotrexate for Lymphoma:
For Burkitt's tumor in Stages I-II: 10 to 25 mg orally once a day for 4 to 8 days

Malignant lymphoma in Stage III: 0.625 to 2.5 mg/kg orally daily as a part of

combination chemotherapy.

Treatment in all stages usually consists of several courses of the drug interposed with 7

to 10 day rest periods.

Usual Adult Dose for Meningeal Leukemia:
12 mg/m2 intrathecally every 2 to 5 days until the cell count of the CSF returns to

normal. At this point, one additional dose is advisable. Administration at intervals of less

than 1 week may result in increased subacute toxicity.

Usual Adult Dose for Mycosis Fungoides:
2.5 to 10 mg PO daily or 50 mg IM once a week or 25 mg IM twice a week.
Usual Adult Dose for Osteosarcoma:
Initial Dose: 12 g/m2 intravenously as a 4 hour infusion (in combination with other

chemotherapeutic agents). If this dose is not adequate to achieve a peak serum

concentration of 1000 micromolar at the end of the infusion, the dose may be increased

to 15 g/m2.

Treatments may occur at 4, 5, 6, 7, 11, 12, 15, 16, 29, 30, 44, and 45 weeks after

surgery.
If the patient is vomiting or unable to tolerate oral medication, leucovorin should be

added to this regimen at the same dose and schedule as the methotrexate.
Usual Adult Dose for Psoriasis:
Single Dose: 10 to 25 mg/week orally, IM, or IV until adequate response is achieved.

Divided Dose: 2.5 mg orally, IM, or IV every 12 hours for 3 doses once a week.

Maximum weekly dose: 30 mg.

Usual Adult Dose for Rheumatoid Arthritis:
Single dose: 7.5 mg orally weekly.

Divided dose: 2.5 mg orally every 12 hours for 3 doses once a week.

Maximum weekly dose: 20 mg.

Usual Adult Dose for Neoplastic Diseases:
I.V.: Range is wide from 30-40 mg/m2/week to 100-12,000 mg/m2 with leucovorin

rescue
Usual Pediatric Dose for Acute Lymphocytic Leukemia:
100 mg/m2 over 1 hour followed by a 35 hour infusion delivering 900 mg/m2/day.
Usual Pediatric Dose for Dermatomyositis:
15 to 20 mg/m2 orally once weekly.
Usual Pediatric Dose for Meningeal Leukemia:
less than 4 months: 3 mg/dose intrathecally.

greater than or equal to 4 months less than 1 year: 6 mg/dose intrathecally.

greater than or equal to 1 year less than 2 years: 8 mg/dose intrathecally.

greater than or equal to 2 years less than 3 years: 10 mg/dose intrathecally.

greater than or equal to 3 years: 12 mg/dose intrathecally.

The dose may be administered every 2 to 5 days until CSF counts return to normal

followed by a dose administered once weekly for 2 weeks and monthly thereafter.

Administration at intervals of less than 1 week may result in increased subacute toxicity.
Usual Pediatric Dose for Neoplastic Diseases:
7.5 to 30 mg/m2 IM or orally every 2 weeks.

Alternate dosing: 10 to 18,000 mg/m2 IV bolus or continuous infusion over 6 to 42

hours.
Usual Pediatric Dose for Rheumatoid Arthritis:
5 to 15 mg/m2 IM or orally once weekly.
Usual Pediatric Dose for Solid Tumors:
less than 12 years: 12000 mg/m2 IV.

greater than or equal to 12 years: 8000 mg/m2 IV.

Maximum dose: 18 grams.

What other drugs will affect methotrexate?

Many drugs can interact with methotrexate. Not all possible interactions are listed here.

Tell your doctor about all your medications and any you start or stop using during

treatment with methotrexate, especially:

azathioprine;
leucovorin;
phenytoin;
probenecid;
theophylline;
an antibiotic or sulfa drugs;
isotretinoin, retinol, tretinoin;
NSAIDs (non-steroidal anti-inflammatory drugs) - ibuprofen (Advil, Motrin),
naproxen (Aleve), celecoxib, diclofenac, indomethacin, meloxicam, and others; or
salicylates - aspirin, Nuprin Backache Caplet, Kaopectate, KneeRelief, Pamprin
Cramp Formula, Pepto-Bismol, Tricosal, Trilisate, and others.
This list is not complete and many other drugs can interact with methotrexate. This

includes prescription and over-the-counter medicines, vitamins, and herbal products.

Give a list of all your medicines to any healthcare provider who treats you.

In Summary
Commonly reported side effects of methotrexate include: increased liver enzymes.

See below for a comprehensive list of adverse effects.

For the Consumer

Applies to methotrexate: oral tablet

Other dosage forms:

injectable, powder for solution, solution

In addition to its needed effects, some unwanted effects may be caused by

methotrexate. In the event that any of these side effects do occur, they may require

medical attention.

Major Side Effects

You should check with your doctor immediately if any of these side effects occur

when taking methotrexate:

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

Minor Side Effects

Some of the side effects that can occur with methotrexate may not need medical

attention. As your body adjusts to the medicine during treatment these side effects may

go away. Your health care professional may also be able to tell you about ways to

reduce or prevent some of these side effects. If any of the following side effects

continue, are bothersome or if you have any questions about them, check with your

health care professional:

More common:

Hair loss, temporary

 loss of appetite
nausea or vomiting
Less common:
Acne
boils on skin
pale skin
skin rash or itching