Methotrexate

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Methotrexate

This is the medication I have been on at various times in my disease process. I have asked not to take it anymore because of the wide range of side effects I manifest while on this medication. Each person is different in what may or may not mainfest in them during treatment. I have heard from a great many patients that while taking this, if they also take folic acid, it keeps the side effects to a minimum.

There are many lupus patients who have had great results with this medication as well. It is best if you and your doctor determine the course for your particular pathway of lupus. Always discuss these things with your doctor and do not self medicate.

This is a powerful medication for most people, yet one of the most used as well. While it is so effective in treating many different things in the autoimmune spectrum, it is still to be considered powerful. Please read the following information if you would like the basic information on this medication.

I got this information from Wikipedia. Their information follows:

Uses

In cancer chemotherapy

Methotrexate was originally used as part of combination chemotherapy regimens to treat many kinds of cancers. It is still the mainstay for the treatment of many neoplastic disorders including acute lymphoblastic leukemia.

Medical termination of pregnancy

Methotrexate is commonly used (generally in combination with misoprostol) to terminate pregnancies during the early stages (i.e. as an abortifacient). It is also used to treat ectopic pregnancies.[7] In the case of early missed miscarriage (particularly a blighted ovum), in which fetal demise has occurred but the body has not expelled the fetus, methotrexate may be used to help the body begin the miscarriage process.

Other uses

It has come into use as a treatment for some autoimmune diseases, including myasthenia gravis, polymyositis, dermatomyositis, inclusion body myositis, ankylosing spondylitis, Crohn’s disease, psoriasis, pustular psoriasis, psoriatic arthritis, rheumatoid arthritis, Wegener’s granulomatosis, Adult-onset Still’s disease, and scleroderma (see disease-modifying antirheumatic drugs). A parallel use with TNFα blockers, such as adalimumab, infliximab, or etanercept, has been shown to markedly improve symptoms.[8]

It is also sometimes used to treat a rare condition called Behçet’s disease where it is taken weekly, along with folic acid daily. In the case of immune disorders, such as Behçet’s disease and rheumatoid disorders, it is believed that the clinical goal of the low dose methotrexate regimen is to inhibit AICAR transformylase, which leads to increased AICA ribose (AICAR transformylase’s substrate). The AICA ribose inhibits adenosine deaminase, resulting in a build-up of extracellular adenosine. Extracellular adenosine inhibits the expression of IL-2 receptors on circulating T-lymphocytes, causing a suppression of the immune system, and thus ameliorating the effects of the immune disorder.

Drug Interactions

There is a risk of a severe adverse reactions if penicillins or related antibiotics are used alongside methotrexate. There have been numerous case reports of possible decreased urinary excretion of methotrexate due to competition by some acidic drugs like beta-lactams (penicillins, cephalosporins, carbapenems, and monobactams) for secretion in the renal tubule, with toxicity resulting due to increased blood methotrexate concentration.

Administration

It can be taken orally or administered by injection (subcutaneous, intramuscular, intravenous or intrathecal). Although daily preparations are occasionally used, most patients take weekly doses, which decreases the risk of certain side-effects. People taking this medicine must get appropriate tests done regularly, especially older people, to make sure no potentially fatal damage is being done to blood cells and immune system.

Adverse effects Possible side effects can include anemia, neutropenia, increased risk of bruising, hair loss, nausea and vomiting, dermatitis and diarrhea. A small percentage of patients develop hepatitis, and there is an increased risk of pulmonary fibrosis where dry cough can be an important sign.

The higher doses of methotrexate often used in cancer chemotherapy can cause toxic effects to the rapidly-dividing cells of bone marrow and gastrointestinal mucosa. The resulting myelosuppression and mucositis are often prevented (termed Leucovorin “rescue”- as this is the folic acid based drug used).

Methotrexate is a highly teratogenic drug and categorized in Pregnancy Category X by the FDA. Women must not take the drug during pregnancy, if there is a risk of becoming pregnant, or if they are breastfeeding. Men who are trying to get their partner pregnant must also not take the drug. To engage in any of these activities (after discontinuing the drug), women must wait until the end of a full ovulation cycle and men must wait three months.

Reports of central nervous system reactions to methotrexate especially when given via the intrathecal route which include myelopathies and leucoencephalopathies. It has a variety of cutaneous side effects, in particular when administered in high doses.

Generally, the more “non-specific” action a pharmacological substance has, the more possible side effects can be expected. Methotrexate has like all “cell toxic” substances a broad array of possible adverse effects. Care should always be taken to read the manufacturer’s original instructions for the preparation in question.

Here is a more thorough list of potential side effects for Methotrexate:

Most frequent Ulcerative stomatitis, leukopenia, nausea, abdominal distress.

Other frequent Hair loss, malaise, undue fatigue, chills and fever, dizziness and lowered resistance to infection.

Other rarer reactions (related to or attributed to Methotrexate) nodulosis, vasculitis, arthralgia/myalgia, loss of libido/impotence, diabetes, osteoporosis, osteonecrosis, sudden death, reversible lymphomas, tumor lysis syndrome, soft tissue necrosis, anaphylactoid reactions.

By organ system:

Alimentary system Anorexia, nausea, vomiting, diarrhea; Gingivitis, pharyngitis, stomatitis, hematemesis, melena, gastrointestinal ulceration/bleeding, enteritis, pancreatitis.

Blood/lymphatic system Anemia, aplastic anemia, pancytopenia, leukopenia, neutropenia, thrombocytopenia, lymphadenopathy and lymphoproliferative disorders. Hypogammaglobulinemia.

Cardiovascular system Pericarditis, pericardial effusion, hypotension, thromboembolic events (cerebral thrombosis, deep vein thrombosis, retinal vein thrombosis, thrombophlebitis, and pulmonary embolus).

Central nervous system Headaches, drowsiness, blurred vision, transient blindness, speech impairment including dysarthria and aphasia, hemiparesis, paresis and convulsions. Occasional reports of transient subtle cognitive dysfunction, mood alteration (depression), unusual cranial sensations, leukoencephalopathy, encephalopathy.

Hepatobiliary system Hepatotoxicity, acute hepatitis, chronic fibrosis/cirrhosis, decrease in serum albumin, liver enzyme elevations.

Immune system (infections) Fatal opportunistic infections (Pneumocystis carinii pneumonia, pneumonia, sepsis, nocardiosis, histoplasmosis, cryptococcosis, Herpes zoster, Herpes simplex hepatitis and disseminated Herpes simplex).

Musculoskeletal system Stress fracture.

Ophthalmic Conjunctivitis, serious visual changes (without known cause).

Respiratory system Respiratory fibrosis, respiratory failure, interstitial pneumonitis, and chronic interstitial obstructive pulmonary disease. Dry cough possibly being a symptom of these aforementioned conditions..

Dermatologic Acne, rashes (Erythematous rashes), pruritus, urticaria, photosensitivity, pigmentary changes, alopecia, ecchymosis, telangiectasia, furunculosis, erythema multiforme, toxic epidermal necrolysis, papular eruption, Stevens-Johnson Syndrome, skin necrosis, skin ulceration and exfoliative dermatitis.

Urogenital system Severe nephropathy or renal failure, azotemia, cystitis, hematuria; defective oogenesis or spermatogenesis, transient oligospermia, menstrual dysfunction, vaginal discharge, and gynecomastia; infertility, abortion, crystalluria,fetal defects

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