Generic Name

Brand Name

Dosage

Side-effects

Comments

auranofin

Ridaura

3 mg bid or tid

Major side-effect with auranofin which is an oral form of gold is diarrhea, also additional GI side-effects including nausea or vomiting.  May also have mouth sores and irritation.  May develop a gold induced skin rash.  May cause changes in renal function with protein in the urine

Auranofin or oral gold is not being utilized with any great frequency now.  It did not prove to be all that effective in rheumatoid arthritis and had a significant incidence of diarrhea.  It also had the potential for similar side-effects as injectable gold with kidney toxicity and rash

aurothioglucose

Solganal

May be given IM 10 mg as a test dose and then 25 to 50 mg weekly

Mouth irritation, rash, kidney side-effects especially with protein in the urine, changes in the blood count with decreased red cells, white cells or platelets

azathioprine

Imuran

50 mg bid or tid with food

GI upset, liver function abnormalities

This is an immunosuppressive drug and therefore would have to be withdrawn or held if any significant infectious disease occurred

cyclophosphamide

Cytoxan

50 mg once a day up to tid with meals.  This medication may also be given intravenously usually on a monthly treatment schedule

Blood in the urine with bladder inflammation with the potential for the development of bladder cancer, GI upset, loss of fertility with the cessation of menses in females.  Suppression of the bone marrow with decreased hemoglobin, white count or platelets.  Anemia might induce fatigue and weakness.  The decrease in the white blood count could predispose an individual towards an increased incidence of infections, the decrease in platelets could cause significant bruising and bleeding

This is a very potent immunosuppressive drug.  Its use in rheumatoid arthritis is limited to the rare case of severe vasculitis not controlled with other measures.  This medication is useful in severe systemic lupus erythematosus particularly with significant lupus nephritis.  There is the potential of developing malignancies secondarily with long-term use of this medication.  In SLE it is mainly given initially on a monthly basis intravenously for severe disease and then the patient may be converted to an oral form of treatment.  The medication is obviously limited by its potential side-effects and needs to be monitored closely

cyclosporin

Neoral

Sandimmune

100 to 400 mg daily in divided dosages based on individual's body weight which is usually 2.5-5 mg/kg (1 kg equals 2.2 pounds)

Hair growth, kidney dysfunction, increase in the blood pressure, changes in the gums with actual enlargement of the gums or inflammation of the gums

Difficult medication to use because it has to be monitored closely regarding any changes in the serum creatinine.  It has been used, however, successfully to control rheumatoid arthritis either alone or even in combination with methotrexate, but the patient needs to be under extremely close supervision.  The dosage needs to be tapered back with any 25% increase in the creatinine level above the baseline value.  Patients needs to be monitored regarding any liver toxicity as well.  This drug has been used for many years in prevention of rejection of transplanted organs and has helped increase the number of successful transplants.

gold sodium thiomalate

Myochrysine

10 mg IM as a test dose, then increasing up to 25 mg to 50 mg weekly

Kidney function abnormalities with protein in the urine, changes in the blood count, rash.

Gold was the standard treatment for many years in rheumatoid arthritis.  This has been supplanted by the use of methotrexate.  The major concerns with using gold are the development of kidney disease and a drop in any of the important blood cells including the red blood cells, white blood cells and platelets.

hydroxychloroquine

Plaquenil

200 mg once daily or twice daily

GI upset, rash, visual changes involving the macula portion of the eye

This medication is effective in approximately 50% of rheumatoid arthritis patients particularly those with mild to moderate disease.  The side-effects in the eyes are rare in patients who are taking 400 mg per day or less of this medication, but rheumatologists recommend that patients be monitored by an ophthalmologist at baseline prior to starting this medication and then every six months to make sure that no early changes are occurring.  It is also an important medication in systemic lupus erythematosus particularly when the patient is having joint symptoms, skin involvement or pleurisy.

methotrexate

Rheumatrex

7.5 mg to 25 mg weekly given orally or may be given by intramuscular injection up to 50 mg weekly maximum

GI upset, rash, hair loss, liver function abnormalities, change in blood count, in rare cases pulmonary toxicity

Patients should not be taking alcohol while on methotrexate.  It is imperative that they be monitored initially every two weeks for the first two to three months and then monthly with CBC, creatinine and liver profile to make sure there are no changes in any of these important lab values.  Methotrexate now serves as the most often prescribed DMARD in rheumatoid arthritis.  If patients fail to be completely controlled with methotrexate, then it may be combined with Arava or Enbrel or Remicade.  It also may be used in conjunction with Plaquenil.

leflunomide

Arava

10 to 20 mg daily in a single dose (after 100 mg a day loading dose for three days)

Hair loss, skin rash, diarrhea, liver function changes

The diarrhea, hair loss and liver changes may dissipate or decrease with lowering of the Arava dosage from 20 to 10 mg daily.  Otherwise if these side-effects continue, then this medication may have to be stopped.  In patients with methotrexate toxicity who could not continue on that drug, then Arava is an excellent alternative.  It also may be used in conjunction with methotrexate in those patients who have not had a complete remission.  Patients need to be monitored regularly with a CBC, creatinine and liver profile similar to the monitoring that goes on with methotrexate.  In patients who wish to conceive a child after being on Arava, it is important to use a resin called cholestyramine over eleven days to try to remove a significant amount of this medication.  Levels of Arava may be obtained in a laboratory to determine if there are any significant amounts of medication remaining.  The cholestyramine may also be used in cases of any acute toxicity.  Female patients who are on Arava should use appropriate birth control measures as there is a significant potential for fetal abnormalities if patient gets pregnant while on Arava

penicillamine

Cuprimine Depen

125 to 250 mg up to tid

GI side-effects including diarrhea, decrease in taste, nausea or vomiting, rash, kidney side-effects including protein in the urine

This medicine is not used as much now as it was years ago mainly because of the development of newer and more potent medications.  Also penicillamine has significant side-effects including the development of kidney disease as well as potential changes in the blood count

sulfasalazine

Azulfidine

500 mg one or two tabs bid or tid

GI upset with diarrhea, rash, liver function abnormalities, changes in the blood count

Patients who are allergic to sulfa drugs should not use this medication as it is a sulfa derivative.  It has been used more in Europe to treat rheumatoid arthritis than in the United States, but is gaining acceptance in the U.S. as well.  It also has been used a great deal in treating ankylosing spondylitis particularly in Europe