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methotrexate (injection)

Pronunciation

Generic Name: methotrexate (injection) (meth oh TREX ate)
Brand Name: Methotrexate Sodium, Preservative Free, Otrexup, Rasuvo

What is methotrexate injection?

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

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

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

What is the most important information I should know about methotrexate injection?

Methotrexate can be toxic to your organs, such as your stomach, liver, lungs, kidneys, nerves, skin, and bone marrow (immune system). Your blood and urine will need to be tested often, and you may need an occasional liver biopsy or chest X-ray.

Methotrexate can harm an unborn baby or cause birth defects. Do not use if you are pregnant.

Some medicines can cause unwanted or dangerous effects when used with methotrexate, especially a nonsteroidal anti-inflammatory drug (NSAID) for pain, arthritis, fever, or swelling. This includes aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve), celecoxib (Celebrex), diclofenac, indomethacin, meloxicam, and others.

Call your doctor right away if you have a serious side effect: signs of stomach bleeding--diarrhea, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds; lung problems--sudden chest pain or discomfort, wheezing, dry cough or hack; signs of infection--sudden weakness or ill feeling, fever, chills, sore throat, mouth sores, red or swollen gums, trouble swallowing; or severe skin reaction--red or purple skin rash that spreads and causes blistering and peeling.

What should I discuss with my healthcare provider before receiving methotrexate injection?

You should not use methotrexate if you are allergic to it. Methotrexate injection should not be used to treat psoriasis or rheumatoid arthritis if you have:

  • chronic liver disease;

  • alcoholism or cirrhosis of the liver;

  • a blood cell disorder such as low red or white blood cell counts, or low levels of platelets in your blood;

  • a weak immune system or bone marrow disorder; or

  • if you are pregnant or breast-feeding.

Methotrexate injection 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;

  • liver disease;

  • lung disease or pneumonia;

  • stomach ulcer, ulcerative colitis;

  • any type of infection; or

  • if you are receiving phototherapy or radiation treatments.

This medication can harm an unborn baby or cause birth defects. Do not use methotrexate if you are pregnant. You may need to have a negative pregnancy test before starting this treatment. Tell your doctor right away if you become pregnant during treatment.

This medication may affect fertility (your ability to have children), whether you are a man or a woman. However, both men and women should use birth control to prevent pregnancy while receiving this medicine. Methotrexate use by either parent may cause birth defects.

If you are a woman, use an effective form of birth control while you are using methotrexate injection, and for at least one cycle of ovulation after your treatment ends.

If you are a man, use a condom to keep from causing a pregnancy while you are using methotrexate injection. Continue using condoms for at least 90 days after your treatment ends.

Methotrexate can pass into breast milk and may harm a nursing baby. Do not breast-feed while you are using methotrexate.

How is methotrexate injection given?

Your doctor will perform blood tests to make sure you do not have conditions that would prevent you from safely using methotrexate.

Methotrexate is injected under your skin, into a muscle, or into a vein through an IV. Methotrexate may also be injected directly into a joint, or into the area around your spinal cord. A healthcare provider will give you this injection.

You may be shown how to use injections at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine. Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Otrexup or Rasuvo (methotrexate injected under the skin) is for use only 1 time each week. Do not use Otrexup or Rasuvo every day.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions. It is very important not to inject too much methotrexate when you are using this medication at home.

Do not use this medicine if it has changed colors or has lumps or particles in it. Call your pharmacist for new medication.

Use a disposable needle and syringe only once. Follow any state or local laws about throwing away used needles and syringes. Use a puncture-proof "sharps" disposal container (ask your pharmacist where to get one and how to throw it away). Keep this container out of the reach of children and pets.

Use a disposable needle only once, then throw away in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

Methotrexate can be toxic to your organs, such as your stomach, liver, lungs, kidneys, nerves, skin, and bone marrow (immune system). To check for harmful effects, your blood will need to be tested often. Your kidney or liver function may also need to be tested, and you may need an occasional liver biopsy or chest X-ray. Visit your doctor regularly.

Store at room temperature away from moisture, heat, and light. Do not freeze.

What happens if I miss a dose?

Call your doctor for instructions if you miss an appointment for your methotrexate injection, or if you forget to use the medicine at home.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of methotrexate injection can be fatal.

What should I avoid while receiving methotrexate injection?

Do not drink alcohol. Serious side effects can occur when alcohol is combined with methotrexate.

Do not receive a "live" vaccine while using methotrexate, or you could develop a serious infection. Live vaccines include measles, mumps, rubella (MMR), rotavirus, typhoid, yellow fever, varicella (chickenpox), zoster (shingles), and nasal flu (influenza) vaccine.

This medicine can pass into body fluids (urine, feces, vomit). For at least 48 hours after you receive a dose, avoid allowing your body fluids to come into contact with your hands or other surfaces. 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.

Methotrexate may impair your thinking or reactions. Avoid driving or operating machinery until you know how this medicine will affect you.

Avoid exposure to sunlight or artificial UV rays (sunlamps, tanning beds, or PUVA treatment), especially if you have psoriasis. Methotrexate injection can make your skin more sensitive to sunlight and your psoriasis may worsen.

Methotrexate injection side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • nerve problems--confusion, weakness, coordination problems, drowsiness, feeling irritable, back pain, headache, neck stiffness, seizure (convulsions), vision problems, loss of movement in any part of your body;

  • signs of stomach bleeding--diarrhea, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;

  • lung problems--sudden chest pain or tightness, wheezing, trouble breathing, dry cough or hack;

  • signs of infection--sudden weakness or ill feeling, fever, chills, sore throat, cough with mucus, vomiting, weight loss, night sweats, swollen glands, mouth sores, red or swollen gums, trouble swallowing;

  • kidney problems--swelling, rapid weight gain, little or no urinating; 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 side effects may include:

  • nausea, vomiting, stomach pain or discomfort, diarrhea;

  • blisters or ulcers in your mouth, red or swollen gums, trouble swallowing;

  • mild skin rash;

  • headache, dizziness;

  • runny or stuffy nose, sore throat, wheezing, trouble breathing;

  • abnormal liver function tests;

  • easy bruising or bleeding;

  • temporary hair loss;

  • occasional headache, blurred vision; or

  • burning sensation of psoriasis skin lesions.

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 for Acute Lymphoblastic Leukemia:

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

Comments:
-Remissions were usually achieved within a period of 4 to 6 weeks in 50% of patients.
-Acute lymphoblastic leukemia in pediatric patients and young adolescents is the most responsive to present day chemotherapy. In young adults and older patients, clinical remission is more difficult to obtain and early relapse is more common.

Maintenance (during remission): 15 mg/m2 IM or orally 2 times a week: Alternate remission dosing: 2.5 mg/kg IV every 14 days

Use: Acute lymphoblastic leukemia (ALL)

Usual Adult Dose for Choriocarcinoma:

CHORIOCARCINOMA AND SIMILAR TROPHOBLASTIC DISEASES:
Orally or IM: 15 to 30 mg daily for a 5 day course; courses are usually repeated for 3 to 5 times, with rest periods of one or more weeks between courses, until any manifesting toxic symptoms subside

Comments:
-The effectiveness of therapy is evaluated by 24 hour quantitative analysis of urinary chorionic gonadotropin (hCG), which should return to normal or less than 50 IU/24 hr usually after the third or fourth course and usually be followed by a complete resolution of measurable lesions in 4 to 6 weeks.
-One to two courses of therapy after normalization of hCG is usually recommended.
-Since hydatidiform mole may precede choriocarcinoma, prophylactic chemotherapy with this drug has been recommended.
-Chorioadenoma destruens is considered to be an invasive form of hydatidiform mole. This drug is administered in these disease states in doses similar to those recommended for choriocarcinoma.

Use: Gestational trophoblastic disease (GTD) including gestational choriocarcinoma, chorioadenoma destruens, and hydatidiform mole

Usual Adult Dose for Trophoblastic Disease:

CHORIOCARCINOMA AND SIMILAR TROPHOBLASTIC DISEASES:
Orally or IM: 15 to 30 mg daily for a 5 day course; courses are usually repeated for 3 to 5 times, with rest periods of one or more weeks between courses, until any manifesting toxic symptoms subside

Comments:
-The effectiveness of therapy is evaluated by 24 hour quantitative analysis of urinary chorionic gonadotropin (hCG), which should return to normal or less than 50 IU/24 hr usually after the third or fourth course and usually be followed by a complete resolution of measurable lesions in 4 to 6 weeks.
-One to two courses of therapy after normalization of hCG is usually recommended.
-Since hydatidiform mole may precede choriocarcinoma, prophylactic chemotherapy with this drug has been recommended.
-Chorioadenoma destruens is considered to be an invasive form of hydatidiform mole. This drug is administered in these disease states in doses similar to those recommended for choriocarcinoma.

Use: Gestational trophoblastic disease (GTD) including gestational choriocarcinoma, chorioadenoma destruens, and hydatidiform mole

Usual Adult Dose for Lymphoma:

For Burkitt's tumor in Stages I to 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.

Use: Lymphomas

Usual Adult Dose for Meningeal Leukemia:

12 mg/m2 (maximum 15 mg) intrathecally every 2 to 5 days until the cell count of the CSF returns to normal; at this point, one additional dose is advisable.

Comments:
-Administration at intervals of less than 1 week may result in increased subacute toxicity.
-The preserved formulations of this drug contain benzyl alcohol and must not be used for intrathecal or high dose therapy.

Use: Treatment and prophylaxis of meningeal leukemia

Usual Adult Dose for Mycosis Fungoides:

Early stage dosing: 5 to 50 mg once a week; alternatively, 15 to 37.5 mg 2 times a week may be used in patients who have responded poorly to weekly therapy

Comments:
-Therapy with this drug as a single agent appears to produce clinical responses in up to 50% of patients treated.
-Dose reduction or cessation is guided by patient response and hematologic monitoring.
Combination chemotherapy regimens that include IV MTX at higher doses with leucovorin rescue have been utilized in advanced stages of disease.

Use: Mycosis fungoides (cutaneous T cell lymphoma)

Usual Adult Dose for Osteosarcoma:

Initial Dose: 12 g/m2 IV 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 IV.

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

Comments:
-If the patient is vomiting or unable to tolerate oral medication, leucovorin given IV or IM should be added to this regimen at the same dose and schedule as the methotrexate.
-Consult product labeling or local protocol for dosage of concomitant medications in the chemotherapy regimen.

Use: Osteosarcoma

Usual Adult Dose for Psoriasis:

Single Dose: 7.5 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: 20 mg

Comments:
-Once optimal clinical response has been achieved, each dosage schedule should be reduced to the lowest possible amount of drug and to the longest possible rest period.
-The use of MTX may permit the return to conventional topical therapy, which should be encouraged.

Use: For 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.

Usual Adult Dose for Rheumatoid Arthritis:

Single dose: 7.5 mg orally once a week
Divided dose: 2.5 mg orally every 12 hours for 3 doses once a week
Maximum weekly dose: 20 mg
Duration of therapy: Unknown

Comments:
-Dosages may be adjusted gradually to achieve optimal response.
-Limited experience shows a significant increase in the incidence and severity of serious toxic reactions, especially bone marrow suppression, at doses greater than 20 mg per week in adults.
-Therapeutic response usually begins within 3 to 6 weeks and the patient may continue to improve for another 12 weeks or more.

Use: For the management of selected adults with severe, active rheumatoid arthritis (ACR criteria) who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of first-line therapy including full dose nonsteroidal anti-inflammatory agents (NSAIDs).

Usual Adult Dose for Breast Cancer -- Adjuvant:

40 mg/m2 IV once on days 1 and 8 of each cycle

Use: As adjuvant treatment to radical mastectomy in primary breast cancer with positive axillary lymph nodes

Usual Adult Dose for Neoplastic Diseases:

-Oral administration in tablet form is often preferred since absorption is rapid and effective serum levels are obtained.
-TEST DOSE (PARENTERAL): 5 to 10 mg IM or IV once given 1 week prior to initiation of therapy.
-Doses are usually based on the patient's body surface area (BSA): For conversion of mg/kg bodyweight to mg/m2 of body surface area or the reverse, a ratio of 1:30 is given as a guideline. The conversion factor varies between 1:20 and 1:40 depending on age and body build.
-Doses greater than 100 mg should be given parenterally and should be administered with leukovorin rescue.

Usual Pediatric Dose for Acute Lymphoblastic Leukemia:

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

Comments:
-Remissions were usually achieved within a period of 4 to 6 weeks in 50% of patients.
-Acute lymphoblastic leukemia in pediatric patients and young adolescents is the most responsive to present day chemotherapy. In young adults and older patients, clinical remission is more difficult to obtain and early relapse is more common.

Maintenance (during remission): 15 mg/m2 IM or orally 2 times a week: Alternate remission dosing: 2.5 mg/kg IV every 14 days

Use: Acute lymphoblastic leukemia (ALL)

Usual Pediatric Dose for Meningeal Leukemia:

Less than 1 year: 6 mg/dose intrathecally
1 year of age: 8 mg/dose intrathecally
2 years of age: 10 mg/dose intrathecally
3 years of age or older: 12 mg/dose intrathecally

Comments:
-The dose may be administered every 2 to 5 days until CSF counts return to normal followed by one additional dose.
-For prophylaxis against meningeal leukemia, the dosage is the same as for treatment except for the intervals of administration. The physician should consult the medical literature.

Usual Pediatric Dose for Rheumatoid Arthritis:

-Initial dose: 10 mg/m2 orally once a week; adjust doses gradually to achieve optimal response
Maximum dose: 20 mg/m2 once a week (limited experience exists with doses of 30 mg/m2 per week)

Comments:
-Experience suggests that children receiving 20 to 30 mg/m2/week (0.65 to 1.0 mg/kg/week) may have better absorption and fewer gastrointestinal side effects if the drug is administered either IM or subcutaneously.
-Therapeutic response usually begins within 3 to 6 weeks and the patient may continue to improve for another 12 weeks or more.

Use: Polyarticular-Course Juvenile Rheumatoid Arthritis

What other drugs will affect methotrexate injection?

Many drugs can interact with methotrexate. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your medications and any you start or stop using during treatment with methotrexate.

Where can I get more information?

  • Your doctor or pharmacist can provide more information about methotrexate injection.
  • Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
  • Disclaimer: Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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