Methotrexate is a drug to treat cancer, such as breast cancer, choriocarcinoma, leukemia, bone cancer, lymphoma, or mycosis fungoides. In addition, this drug can also be used in the treatment of autoimmune diseases, such as psoriasis, rheumatoid arthritis, Crohn's disease, or lupus.
Methotrexate belongs to the class of anticancer which has an immunosuppressant effect. This drug works by inhibiting the action of enzymes that are important for the formation of cell DNA. That way, the process of cell replication and growth can be slowed or stopped.
Methotrexate trademarks: Emthexate PF, Ferxate, Metoject, Methotrexate, Rheu-Trex, Kemotrexate, Sanotrexat, Methorexate Ebewe
What is Methotrexate
| group | Prescription drugs |
| Category | Anticancer and immunosuppressant |
| Benefit | Treats various types of cancer and is used in the treatment of autoimmune diseases, such as psoriasis, Crohn's disease, or rheumatoid arthritis. |
| Used by | Adults and children |
| Methotrexate for pregnant and lactating women | Category X: Studies in experimental animals and humans have demonstrated fetal abnormalities or a risk to the fetus. Drugs in this category should not be used by women who are or may become pregnant. Methotrexate can be absorbed into breast milk. If you are breastfeeding, do not use this medicine without consulting your doctor first. |
| Drug form | Tablets and injections |
Precautions Before Using Methotrexate
Methotrexate should only be used as prescribed by a doctor. Below are some things you need to pay attention to before taking methotrexate:
- Tell your doctor about any allergies you have. Methotrexate should not be used by patients who are allergic to this drug.
- Tell your doctor if you have or have had liver disease, kidney disease, pulmonary fibrosis, alcoholism, stomach ulcers, weakened immune system, blood disorders, bone marrow disease, ulcerative colitis, folic acid deficiency, or an infectious disease, such as chickenpox.
- Tell your doctor if you are being treated for cancer with radiation therapy or radiotherapy. Methotrexate can increase the risk of radiation therapy side effects and causing damage to the skin, bones, or other parts of the body.
- Tell your doctor if you are pregnant, breastfeeding, or planning a pregnancy. Use effective birth control while on treatment with methotrexate.
- Tell your doctor that you are taking methotrexate if you are having surgery, including dental surgery.
- Talk to your doctor if you plan to get vaccinated while on treatment with methotrexate.
- Avoid close contact with people with infectious diseases that are easily transmitted, such as the flu, measles, or chickenpox, during treatment with methotrexate, as this can increase your risk of contracting it.
- Do not drive a vehicle or do activities that require alertness while you are taking methotrexate, as this medicine can cause dizziness.
- See your doctor right away if you have an allergic drug reaction, overdose, or serious side effects after taking methotrexate.
Dosage and Instructions for Use of Methotrexate
The dose of methotrexate varies, depending on the goals of treatment and the condition and age of the patient. The following are general doses of methotrexate based on the form of the drug and the intended use for adults:
Drug form: Tablet
- Purpose: Overcome choriocarcinomaThe dose is 15–30 mg per day, for 5 days. The dose is again given after a gap of at least 1 week. Dosage can be repeated 3-5 times.
- Purpose: Treating acute lymphoblastic leukemia
The maintenance dose is 15 mg/m2 body surface area (LPT) 1-2 times a week, in combination with other types of drugs.
- Purpose: Treating Burkitt's lymphomaBurkitt lymphoma)
The dose is 10–25 mg per day, for 4–8 days. Dosage is repeated after 7–10 days.
- Purpose: Skin type T-cell lymphoma mycosis fungoidesThe dose is 2.5–10 mg per day.
- Purpose: Overcoming psoriasis
The dose is 10–25 mg per week as a single dose. Dosage adjustments are made based on the body's response.
- Purpose: Overcome rheumatoid arthritisThe dose is 7.5 mg once a week. Dosage adjustments are made based on the body's response. The maximum dose is 20 mg per week.
- Purpose: Treating Crohn's disease
The dose is 12.5–22.5 m, 1 time per week. Treatment is carried out for up to 1 year.
Drug form: Inject
Injectable methotrexate will be given directly by a doctor or medical officer under the supervision of a doctor, in a hospital. The injection is done through a muscle (intramuscular/IM) or an injection into a vein (intravenous/IV), or the intrathecal space.
- Purpose: Treating acute lymphoblastic leukemia
If given by IM injection, maintenance dose is 15 mg/m2 LPT 1-2 times weekly. Meanwhile, if given by IV injection, the dose is a maintenance dose of 2.5 mg/kgBW every 14 days.
- Purpose: Overcome choriocarcinomaIf given by IM injection, the dose is 15–30 mg per day, for 5 days. The dose is given again after a gap of 1 week for 3-5 times. An alternative dose of 0.25–1 mg/kg is given, every 48 hours, in 4 doses. The maximum dose is 60 mg per day.
- Purpose: Treating Crohn's disease
The dose is 25 mg, once a week, for 16 weeks. Maintenance dose 15 mg per week. The drug is given by IM injection.
- Purpose: Overcome mycosis fungoidesThe dose is 50 mg once a week, divided in 1-2 doses. The drug is given by IM injection.
- Purpose: Overcoming breast cancer
The dose is 10–60 mg/m2 LPT, combined with cyclophosphamide and fluorouracil, given by IV injection.
- Purpose: Treat advanced lymphosarcoma
The dose is up to 30 mg/kgBW, given by IV injection, followed by administration of leucovorin.
- Purpose: Overcoming psoriasis
The dose is 10–25 mg per week given as a single dose, by IM or IV injection.
- Purpose: Overcome osteosarcomaThe recommended starting dose is 12 g/m2 LPT, given by infusion over 4 hours. The dose can be increased up to 15 g/m2 LPT.
- Purpose: Treating leukemia lining the brain and spine (meningeal leukemia) in adults
The dose is 12–15 mg/m2 LPT, once a week for 2–3 weeks. Follow-up doses are then given once every 1 month. Alternative dose, 0.2–0.5 mg/kg every 2–5 days. The drug is administered by intrathecal injection.
- Purpose: Treating leukemia lining the brain and spine (meningeal leukemia) in children
Children aged >3 years the dose is 12 mg. Children aged 2 years the dose is 10 mg. Children aged 1 year dose 8 mg. Children aged <1 year the dose is 6 mg. The drug is administered by intrathecal injection
How to Use Methotrexate Correctly
Methotrexate in injectable form will be given by a doctor or medical officer under the supervision of a doctor. Injections can be administered intramuscularly, intravenously, intrathecal, or put in an IV into a vein. Always follow the doctor's advice while undergoing treatment with this medicine.
Take methotrexate tablets according to the dosage recommended by your doctor. Avoid increasing or decreasing the dose without your doctor's knowledge.
Methotrexate in tablet form should be taken before meals. Wash your hands before and after handling the tablet. Swallow the tablet whole with the help of a glass of water. Avoid taking the drug with milk. If you have stomach pain, it is best to take methotrexate tablets after meals.
This medicine needs to be taken regularly to be effective. If you forget to take your medicine, contact your doctor immediately.
Before and after treatment with methotrexate, you may need regular chest X-rays, liver or kidney function tests, skin reactions, or complete blood tests. This is done so that the development of the condition and the effectiveness of the drug can always be monitored.
Methotrexate tablets should be stored in a closed container in a cool, dry place. Keep this medicine away from direct sunlight and keep this medicine out of reach of children.
Methotrexate Interactions with Other Drugs
The following are some of the effects of drug interactions that can occur when methotrexate is used with other drugs:
- Decreased effectiveness of methotrexate when used with folic acid
- Decreased levels of valproic acid in the blood
- Decreased blood levels of methotrexate when used with cholestyramine
- Increased blood levels of methotrexate when used with omeprazole
- Increased risk of side effects when used with fluorouracil
- Increased levels of mercaptopurine in the blood
- Increased risk of drug toxicity if used with nonsteroidal anti-inflammatory drugs (NSAIDs), aspirin, probenecid, penicillins, aminoglycosides, neomycin, paromomycin, sulfonamides, cotrimoxazole, trimethoprim, cisplatin, etretinate, or ciclosporin
Side Effects and Dangers of Methotrexate
There are several side effects that can occur due to the use of methotrexate, including:
- Headache or dizziness
- Drowsiness
- Gums feel sore and swollen
- Decreased appetite
- Nausea, vomiting, or stomach pain
- Red eye
- Hair loss
Call your doctor if the above side effects do not improve or get worse. See a doctor immediately if you have an allergic reaction to the drug or serious side effects such as:
- Chest pain, wheezing, shortness of breath, cough that doesn't get better
- Canker sores, difficulty swallowing, or swollen gums that don't get better
- Diarrhea, vomiting, bloody stools, or bloody urine
- Low blood cell counts which can be characterized by the appearance of symptoms of anemia, low platelet count (thrombocytopenia), or low white blood cell count (leukopenia)
- Impaired kidney function characterized by certain symptoms, such as infrequent urination, very little urine, or swelling in the legs
- Impaired liver function that can be characterized by certain symptoms, such as severe abdominal pain, jaundice, loss of appetite, or dark urine
- Disorders of nerve function that can be characterized by certain symptoms, such as confusion, stiffness in the neck, blurred vision, movement disorders, seizures, or restlessness
- The emergence of tumor lysis syndrome which can be characterized by symptoms such as fatigue, weakness, muscle cramps, nausea, vomiting, palpitations, bradycardia, or tingling