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methotrexate (injection)

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.

Side Effects (complete list)

Methotrexate dosing information

Usual Adult Dose for Acute Lymphoblastic Leukemia:

Note: A variety of combination chemotherapy regimens have been used for both induction and maintenance therapy in acute lymphoblastic leukemia. The physician should be familiar with the new advances in anti-leukemic therapy.

-Induction: 3.3 mg/m2/day orally or parenterally (in combination with prednisone 60 mg/m2) daily for 4 to 6 weeks
-Maintenance dose during remission: 30 mg/m2 orally or IM 2 times a week
-Alternate maintenance dose during remission: 2.5 mg/kg IV every 14 days

Comments:
-When relapse occurs, reinduction of remission can usually be obtained by repeating the initial induction regimen.
-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.

Use: Acute lymphoblastic leukemia (ALL)

Usual Adult Dose for Choriocarcinoma:

15 to 30 mg orally or IM 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 an invasive form of hydatidiform mole. This drug is administered in these disease states in doses like those recommended for choriocarcinoma.

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

Usual Adult Dose for Trophoblastic Disease:

15 to 30 mg orally or IM 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 an invasive form of hydatidiform mole. This drug is administered in these disease states in doses like those recommended for choriocarcinoma.

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

Usual Adult Dose for Lymphoma:

-Burkitt's tumor Stages I to II: 10 to 25 mg orally once a day for 4 to 8 days
-Burkitt's tumor Stage III: Methotrexate is commonly given concomitantly with other antitumor agents
-Duration of therapy: All stages usually require several courses of therapy interposed with 7 to 10 day rest periods
-Lymphosarcoma Stage III: 0.625 to 2.5 mg/kg orally daily as a part of combination chemotherapy

Uses:
-Burkitt's tumor
-Lymphoma

Usual Adult Dose for Burkitt's Tumor:

-Burkitt's tumor Stages I to II: 10 to 25 mg orally once a day for 4 to 8 days
-Burkitt's tumor Stage III: Methotrexate is commonly given concomitantly with other antitumor agents
-Duration of therapy: All stages usually require several courses of therapy interposed with 7 to 10 day rest periods
-Lymphosarcoma Stage III: 0.625 to 2.5 mg/kg orally daily as a part of combination chemotherapy

Uses:
-Burkitt's tumor
-Lymphoma

Usual Adult Dose for Meningeal Leukemia:

12 mg (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 orally or parenterally 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.

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

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: 10 to 25 mg/week orally, IM, IV, or subcutaneously until adequate response is achieved
Divided Dose: 2.5 mg orally every 12 hours for 3 doses once a week
Maximum dose: 30 mg/week

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 or subcutaneously 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.
-Therapeutic response usually begins within 3 to 6 weeks and the patient may continue to improve for another 12 weeks or more.

Use: For severe active rheumatoid arthritis in patients 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 Pediatric Dose for Acute Lymphoblastic Leukemia:

Note: A variety of combination chemotherapy regimens have been used for both induction and maintenance therapy in acute lymphoblastic leukemia. The physician should be familiar with the new advances in anti-leukemic therapy.

-Induction: 3.3 mg/m2/day orally or parenterally (in combination with prednisone 60 mg/m2) daily for 4 to 6 weeks
-Alternate induction: 20 mg/m2 orally once a week as a component of a multi-agent combination
-Maintenance dose during remission: 30 mg/m2 orally or IM 2 times a week
-Alternate maintenance dose during remission: 2.5 mg/kg IV every 14 days

Comments:
-When relapse occurs, reinduction of remission can usually be obtained by repeating the initial induction regimen.
-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.

Use: Acute lymphoblastic leukemia (ALL)

Usual Pediatric Dose for Meningeal Leukemia:

-Less than 1 year old: 6 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
-One year old: 8 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
-Two years old: 10 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
-Three years and older: 12 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 Pediatric Dose for Juvenile Rheumatoid Arthritis:

Initial dose: 10 mg/m2 orally or subcutaneously once a week
Maximum dose: 20 mg/m2/week (although there is experience with doses up to 30 mg/m2/week in children, there are too few published data to assess how doses over 20 mg/m2/week might affect the risk of serious toxicity in children; experience suggests that children receiving 20 to 30 mg/m2/week [0.65 to 1 mg/kg/week] may have better absorption and fewer GI side effects if this drug is administered either IM or subcutaneously)

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.
-Therapeutic response usually begins within 3 to 6 weeks and the patient may continue to improve for another 12 weeks or more.

Use: For 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 nonsteroidal anti-inflammatory agents (NSAIDs)

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.

Copyright 1996-2012 Cerner Multum, Inc. Version: 3.08.

Last reviewed: July 29, 2016
Date modified: December 03, 2017

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