- What is methotrexate, and how does it work (mechanism of action)?
- What brand names are available for methotrexate?
- Is methotrexate available as a generic drug?
- Do I need a prescription for methotrexate?
- What are the side effects of methotrexate?
- What is the dosage for methotrexate?
- Is methotrexate safe to take if I'm pregnant or breastfeeding?
- What else should I know about methotrexate?
What is methotrexate, and how does it work (mechanism of action)?
Methotrexate is classified as an antimetabolite drug which means it is capable of blocking the metabolism of cells. (Metabolism consists of the production and destruction of important components of the cell as well as the production of energy for use by the cell.) As a result of this effect, it has been found helpful in treating certain diseases associated with abnormally rapid cell growth, such as cancer of the breast and psoriasis. Recently, methotrexate has been shown to be effective in inducing miscarriage, for example in patients with ectopic pregnancy. This effect of methotrexate is attributed to its action of killing rapidly growing cells such as those of the placenta. It also has been found very helpful in treating rheumatoid arthritis, although its mechanism of action in this illness is not known. It seems to work, in part, by altering immunity which may play a role in causing rheumatoid arthritis. The FDA approved methotrexate in December 1953.
What are the side effects of methotrexate?
Methotrexate can cause severe toxicity which usually is related to the dose taken. The most frequent reactions include:
- mouth sores,
- stomach upset;
- low white blood counts;
- severe toxicity of the liver, kidneys and bone marrow, which require regular monitoring with blood tests;
What is the dosage for methotrexate?
Methotrexate may be taken with or without food. For rheumatoid arthritis and psoriasis, the dose of methotrexate is given weekly, by injection or orally. The oral dose is 7.5 to 20 mg once weekly. For psoriasis, the starting oral dose is a single 7.5 mg dose weekly or 2.5 mg every 12 hours for three doses, once weekly. The final dose ranges between 10 and 25 mg weekly orally or by injection.
Is methotrexate safe to take if I'm pregnant or breastfeeding?
Methotrexate should not be used in pregnancy, as it can be toxic to the embryo and can cause fetal defects and spontaneous abortion (miscarriage). It should be discontinued prior to conception if used in either partner. Male patients should stop taking methotrexate at least 3 months prior to a planned conception in order to avoid the theoretical risk of methotrexate-induced abnormal sperm. Women should discontinue use for at least one ovulatory cycle before conception to reduce exposure of a developing ovarian follicle to methotrexate.
What else should I know about methotrexate?
What preparations of methotrexate are available?
Injectable: 25 mg/ml. Powder for injection: 1 g. Tablet: 2.5, 5, 7.5, 10 and 15 mg
How should I keep methotrexate stored?
Methotrexate should be stored at room temperature 15 C to 30 C (59 F to 86 F), avoiding light.
Methotrexate (Rheumatrex, Trexall) is a drug prescribed to treat cancer, psoriasis, inflammatory diseases of the skin, arthritis (rheumatoid arthritis in adults and children), psoriatic arthritis, polymyositis, lupus, and to induce miscarriage in women with ectopic pregnancies. Side effects drug interactions, dosage, and pregnancy safety information should be reviewed prior to taking this drug.
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Related Disease Conditions
Liver disease can be cause by a variety of things including infection (hepatitis), diseases, for example, gallstones, high cholesterol or triglycerides, blood flow obstruction to the liver, and toxins (medications and chemicals). Symptoms of liver disease depends upon the cause and may include nausea, vomiting, upper right abdominal pain, and jaundice. Treatment depends upon the cause of the liver disease.
Rheumatoid Arthritis (RA)
Rheumatoid arthritis (RA) is an autoimmune disease that causes chronic inflammation of the joints, the tissue around the joints, as well as other organs in the body. Early RA signs and symptoms include anemia, both sides of the body affected (symmetric), depression, fatigue, fever, joint deformity, joint pain, joint redness, joint stiffness, joint swelling, joint tenderness, joint warmth, limping, loss of joint function, loss of joint range of motion, and polyarthritis.
Lupus (Systemic Lupus Erythematosus or SLE)
Systemic lupus erythematosus is a condition characterized by chronic inflammation of body tissues caused by autoimmune disease. Lupus can cause disease of the skin, heart, lungs, kidneys, joints, and nervous system. When only the skin is involved, the condition is called discoid lupus. When internal organs are involved, the condition is called systemic lupus erythematosus (SLE).
Psoriasis is a long-term skin condition that may cause large plaques of red, raised skin, flakes of dry skin, and skin scales. There are several types of psoriasis, including psoriasis vulgaris, guttate psoriasis, inverse psoriasis, and pustular psoriasis. Symptoms vary depending on the type of psoriasis the patient has. Treatment of psoriasis may include creams, lotions, oral medications, injections and infusions of biologics, and light therapy. There is no cure for psoriasis.
Pulmonary fibrosis is scarring throughout the lungs. Pulmonary fibrosis can be caused by many conditions including chronic inflammatory processes, infections, environmental agents, exposure to ionizing radiation, chronic conditions, and certain medications. Symptoms include shortness of breath, coughing, and diminished exercise tolerance. Treatment options are dependent on the type of pulmonary fibrosis; lung transplant and/or medications are options.
Ulcerative colitis is a chronic inflammation of the colon. Symptoms and signs include abdominal pain, diarrhea, and rectal bleeding. Ulcerative colitis is closely related to Crohn's disease, and together they are referred to as inflammatory bowel disease. Treatment depends upon the type of ulcerative colitis diagnosed.
Ankylosing spondylitis is a type of arthritis that causes chronic inflammation of the spine. The tendency to develop ankylosing spondylitis is genetically inherited. Treatment incorporates medications, physical therapy, and exercise.
Scleritis is inflammation of the white part of the eye. It may be caused by a serious underlying condition, such as an autoimmune disease. Symptoms include redness, pain, tearing, sensitivity to light, and decreased visual acuity. Treatment may include eyedrops as well as treatment for any underlying disease process. Scleritis cannot be prevented.
Sarcoidosis, a disease resulting from chronic inflammation, causes small lumps (granulomas) to develop in a wide range of body tissues and can appear in almost any body organ. However, sarcoidosis most often starts in the lungs or lymph nodes.
Polymyositis and Dermatomyositis
Polymyositis is a disease of the muscle featuring inflammation of the muscle fibers. It results in weakness of the muscles which can be severe and when associated with skin rash, is referred to as dermatomyositis. Although the cause of this disease is unknown, diagnosis includes physical examination of muscle strength, blood tests for muscle enzymes, electrical tests of muscle and nerves, and conformation by a muscle biopsy. Treatment of polymyositis and dermatomyositis includes high doses of cortisone-related medications, immune suppression, and physical therapy.
Psoriatic arthritis is a disease that causes skin and joint inflammation. Symptoms and signs include painful, stiff, and swollen joints, tendinitis, and organ inflammation. Treatment involves anti-inflammatory medications and exercise.
Scleroderma is an autoimmune disease of the connective tissue. It is characterized by the formation of scar tissue (fibrosis) in the skin and organs of the body, leading to thickness and firmness of involved areas. Scleroderma is also referred to as systemic sclerosis, and the cause is unknown. Treatment of scleroderma is directed toward the individual features that are most troubling to the patient.
Crohn's Disease vs. Ulcerative Colitis
Crohn's disease and ulcerative colitis are diseases that cause inflammation of part of or the entire digestive tract (GI). Crohn's affects the entire GI tract (from the mouth to the anus), while ulcerative colitis or ulcerative colitis only affects the large and small intestine and ilium. Researchers do not know the exact cause of either disease. About 20% of people with Crohn's disease also have a family member with the disease. Researchers believe that certain factors may play a role in causing UC. Both Crohn's disease and ulcerative colitis are a type of inflammatory bowel disease or IBD. Crohn's disease and ulcerative colitis both have similar symptoms and signs, for example, nausea, loss of appetite, fatigue, weight loss, episodic and/or persistent diarrhea, fever, abdominal pain and cramping, rectal bleeding, bloody stools, joint pain and soreness, eye redness, or pain. Symptoms unique to Crohn’s disease include anemia and skin changes. Symptoms of unique to ulcerative colitis include certain rashes, and an urgency to defecate (have a bowel movement). Doctors diagnose both diseases with similar tests and procedures. While there is no cure for either disease, doctors and other health care professionals can help you treat disease flares, and manage your Crohn's or ulcerative colitis with medication, diet, nutritional supplements, and/or surgery.
Vasculitis (arteritis, angiitis) is a general term for a group of uncommon diseases which feature inflammation of the blood vessels. Each form of vasculitis has its own characteristic pattern of symptoms. The diagnosis of vasculitis is definitively established after a biopsy of involved tissue demonstrates the pattern of blood vessel inflammation. Treatment is directed toward decreasing the inflammation of the arteries and improving the function of affected organs.
Crohn's disease is a chronic inflammatory disease, primarily involving the small and large intestine, but which can affect other parts of the digestive system as well. Abdominal pain, diarrhea, vomiting, fever, and weight loss are common symptoms and signs.
IBS vs. IBD: Differences and Similarities
IBS (irritable bowel syndrome) and IBD (inflammatory bowel disease) are both problems with the digestive tract (gastrointestinal or GI tract), but they are not the same disease. Check out the center below for more medical references on IBS and IBD, including multimedia (slideshows, images, and quizzes), related disease conditions, treatment and diagnosis, medications, and prevention or wellness.
Polymyalgia rheumatica (PMR) is a disorder of the muscles and joints that causes pain and stiffness in the arms, neck, shoulders, and buttocks. Treatment for polymyalgia rheumatica aims to reduce inflammation with aspirin, ibuprofen, and low doses of cortisone medications.
Mixed Connective Tissue Disease (MCTD)
Connective tissue diseases are disorders featuring abnormalities involving the collagen and elastin. Connective tissue diseases that are strictly inheritable include Marfan syndrome and Ehlers-Danlos syndrome. The classic immune-related connective tissue diseases include systemic lupus erythematosus, rheumatoid arthritis, scleroderma, polymyositis, and dermatomyositis. Treatment is often directed at suppressing the inflammation present in the tissues by using anti-inflammatory and immunosuppressive medications.
Reactive arthritis is a chronic, systemic rheumatic disease characterized by three conditions, including conjunctivitis, joint inflammation, and genital, urinary, or gastrointestinal system inflammation. Inflammation leads to pain, swelling, warmth, redness, and stiffness of the affected joints. Non-joint areas may experience irritation and pain. Treatment for reactive arthritis depends on which area of the body is affected. Joint inflammation is treated with anti-inflammatory medications.
Uveitis is inflammation of the eye. Symptoms include blurred vision, eye pain, eye redness, photophobia, and floaters. Treatment may involve prescription eyedrops, antibiotics, and wearing dark glasses.
Primary Biliary Cirrhosis (PBC)
Primary Biliary Cirrhosis (PBS) is a liver disease in which bile building up in the organ damages bile ducts. Ultimately, this can cause liver failure. A number of drugs are available to treat this disease of unknown cause, but the only ultimate cure is a liver transplant.
Male Breast Cancer
Male breast cancer accounts for 1% of all breast cancers, and most cases are found in men between the ages of 60 and 70. A man's risk of developing breast cancer is one in 1,000. Signs and symptoms include a firm mass located below the nipple and skin changes around the nipple, including puckering, redness or scaling, retraction and ulceration of the nipple. Treatment depends upon staging and the health of the patient.
Optic neuritis is inflammation of the optic nerve, the structure that connects the eye to the brain. The precise cause of optic neuritis is unknown, but it is thought to be a type of autoimmune disorder. Optic neuritis most commonly develops due to an autoimmune disorder that may be triggered by a viral infection.
Relapsing polychondritis is an uncommon, chronic disorder of the cartilage that is characterized by recurrent episodes of inflammation of the cartilage of various tissues of the body. Tissues containing cartilage that can become inflamed include the ears, nose, joints, spine, and windpipe (trachea). Tissues that have a biochemical makeup similar to that of cartilage such as the eyes, heart, and blood vessels, can also be affected. Nonsteroidal anti-inflammatory medications (NSAIDs) is used as treatment for mild cases of the disease. Steroid-related medications also are usually required.
Still's disease is a disorder characterized by inflammation with high fever spikes, fatigue, salmon-colored rash, and/or arthritis. Though there have been several theories regarding the cause(s) of Still's disease, the cause is not yet known. Many symptoms of Still's disease are often treatable with anti-inflammatory drugs.
SAPHO syndrome is a chronic disorder that involves the skin, bone, and joints. SAPHO syndrome is an eponym for the combination of synovitis, acne, pustulosis, hyperostosis, and osteitis. SAPHO syndrome is related to arthritic conditions such as ankylosing spondylitis and reactive arthritis. Treatment is directed toward the individual symptoms that are present, and includes medications such as nonsteroidal anti-inflammatory drugs (NSAIDs), and cortisone medications.
Scalp Psoriasis (Psoriasis of the Scalp)
Scalp psoriasis causes red, raised, scaly patches that may extend from the scalp to the forehead and the back of the neck and ears. Symptoms and signs include itching, hair loss, flaking, silvery scales, and red plaques. Treatment includes topical medicated shampoos, creams, gels, oils, ointments, and soaps, medications, and light therapy.
Primary Sclerosing Cholangitis (PSC)
Primary sclerosing cholangitis or PSC is a disease of the liver. The cause of PSC is not known. Symptoms may include itching, fatigue, jaundice, fever, and confusion. The only treatment for Primary sclerosing cholangitis is a liver transplant.
What Is Eosinophilic Fasciitis (Shulman's Syndrome)?
Eosinophilic fasciitis is a skin disease that causes thickening and inflammation of the skin and fascia. Symptoms include redness, warmth, and hardening of the skin, as well as occasional tissue and joint pain. Treatment for eosinophilic fasciitis aims to eliminate inflammation through the use of aspirin, NSAIDs, and cortisone.
Bullous pemphigoid is a skin disease that causes blistering eruptions on the skin's surface and sometimes affects the inner lining of the mouth. Symptoms include severe itching and burning sensations. Treatment involves topical cortisone and sometimes high doses of cortisone. Severe cases may require immune-suppression drugs such as azathioprine.
Primary Biliary Cirrhosis (PBC) Treatment
Primary biliary cirrhosis (PBC) is thought to be an autoimmune disorder that involves the deterioration of the liver's small bile ducts. These ducts are crucial to transport bile to the small intestine, digesting fats and removing wastes. Symptoms of PBC are edema, itching, elevated cholesterol, malabsorption of fat, liver cancer, gallstones, urinary tract infections (UTIs), and hypothyroidism. Treatments include ursodeoxycholic acid (UDCA); colchicine (Colcrys); and immunosuppressive medications, such as corticosteroids; obeticholic acid (Ocaliva); and medications that treat PBC symptoms. For PBC that is associated with cirrhosis of the liver, liver transplantation may be indicated in extreme cases.
Granulomatosis With Polyangiitis
Granulomatosis with polyangiitis is a condition that usually affects young or middle-aged adults, is an inflammation of the arteries supplying blood to the sinuses, lungs, and kidneys. Symptoms of granulomatosis with polyangiitis include bloody sputum, fatigue, weight loss, joint pain, sinusitis, shortness of breath, and fever. Granulomatosis with polyangiitis may be fatal within months without treatment. Treatment aims to stop inflammation with high doses of prednisone and cyclophosphamide.
Juvenile Rheumatoid Arthritis (JRA)
Juvenile rheumatoid arthritis (JRA) annually affects one child in every thousand. There are six types of JRA. Treatment of juvenile arthritis depends upon the type the child has and should focus on treating the symptoms that manifest.
Osteoarthritis vs. Rheumatoid Arthritis
Osteoarthritis (OA) and rheumatoid arthritis (RA) are chronic joint disorders. RA is also an autoimmune disease. OA and RA symptoms and signs include joint pain, warmth, and tenderness. Over-the-counter pain relievers treat both diseases. There are several prescription medications that treat RA.
Takayasu disease (also referred to as Takayasu arteritis) is a chronic inflammation of the aorta and its branch arteries. Takayasu disease is most common in women of Asian descent and usually begins between 10-30 years of age. Symptoms include painful extremities, dizziness, headaches, chest and abdominal pain, and a low-grade fever. Treatment for Takayasu disease includes cortisone medication to suppress the inflammation.
Cleft Palate and Cleft Lip
Cleft palate and cleft lip are facial and oral defects that occur early in pregnancy. A cleft lip is a split of the two sides of the upper lip, and a cleft palate is a split in the roof of the mouth. Cleft lip the fourth most common birth defect in the U.S. Repair of a cleft palate or cleft lip may require multiple surgeries.
Felty's syndrome is a complication of long-term rheumatoid arthritis. Felty's syndrome is defined by the presence of three conditions: rheumatoid arthritis, an enlarged spleen, and an abnormally low white blood count. Treatment of Felty's syndrome is not always required; however, treatment for patients with infections is available.
Treatment & Diagnosis
- Ectopic Pregnancy
- Rheumatoid Arthritis (RA)
- Systemic Lupus Erythematosus (SLE)
- Ankylosing Spondylitis (Bechterew's Disease)
- Psoriatic Arthritis
- Ulcerative Colitis
- Reactive Arthritis
- Bladder Cancer
- Lung Cancer
- Inflammatory Bowel Disease
- Pulmonary Fibrosis
- Crohn's Disease
- Bullous Pemphigoid
- Doctor: Checklist to Take To Your Doctor's Appointment
- Juvenile Idiopathic Arthritis
- Granulomatosis With Polyangiitis (GPA)
- Still's Disease
- Mixed Connective Tissue Disease (MCTD)
- Rheumatoid Arthritis FAQs
- Psoriasis FAQs
- Ulcerative Colitis FAQs
- Ankylosing Spondylitis FAQs
- Rheumatoid Arthritis (RA): 17 Warning Signs of Serious Complications
- Drugs: Buying Prescription Drugs Online Safely
- Drugs: The Most Common Medication Errors
- Medication Disposal
- Dangers of Mixing Medications
- How To Reduce Your Medication Costs
- Pharmacy Visit, How To Get The Most Out of Your Visit
- Indications for Drugs: Approved vs. Non-approved
- Arava Approved For Rheumatoid Arthritis
- Patient Story: Rheumatoid Arthritis and Pregnancy
- Does Methotrexate Cause Liver Damage?
- Patient Story: Rheumatoid Arthritis Treatment
- Psoriasis PUVA Therapy Can Increase Melanoma Risk
- Herbs: Toxicities and Drug Interactions
- Generic Drugs, Are They as Good as Brand-Names?
Medications & Supplements
Prevention & Wellness
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.