Lupus Medications

Patients and Providers: Working Together

Educating Patients About Lupus Medications

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

Antimalarials

Corticosteroids

Immunosuppressives

Medications are an important aspect of the management of many patients with SLE. An array of drug therapies is now available, which has increased the potential for effective treatment and excellent patient outcomes. Once a person has been diagnosed with lupus, a treatment plan will be developed by the doctor based on the person’s age, health, symptoms, and lifestyle. It should be reevaluated regularly and revised as necessary to ensure it is as effective as possible. The goals for treating a patient with lupus include

• reducing tissue inflammation caused by the disease,
• suppressing immune system abnormalities that are responsible for tissue inflammation,
• preventing flares and treating them when they do occur, and
• minimizing complication

Patients and Providers: Working Together

Lupus patients should work with their doctors to develop their medication treatment plan. Patients should thoroughly understand the reason for taking a drug, its action, dose, administration times, and common side effects. Pharmacists also can be a good resource for patients in helping them understand their medication treatment plan. If a patient experiences a problem believed to be related to a medication, the patient should notify her or his doctor immediately. It can be dangerous to suddenly stop taking some medications, and patients should not stop or change treatments without first talking to their doctor.

The array of drugs and the complexity of treatment plans can be overwhelming and confusing. Newly diagnosed patients and patients whose treatment plans have changed should be closely followed and have immediate access to a nurse or doctor if they are having problems with the prescribed medications. Most SLE patients do well on lupus medications and experience few side effects. Those who do experience negative side effects should not become discouraged, because alternative drugs are often available.

Health professionals should review drug treament plans with the lupus patient at each office visit to determine her or his understanding of and compliance with the plan. Questions should be encouraged and additional teaching done to reinforce or provide additional information as needed. It is important to note that lupus patients often require drugs for the treatment of conditions commonly seen with the disease. Examples of these types of medications include diuretics, antihypertensives, anticonvulsants, and antibiotics.

This chapter describes some of the main drugs used to treat SLE. The information presented is intended as a brief review and reference. Drug references and other medical and nursing texts provide more complete and detailed information regarding the use of each drug and associated nursing care responsibilities.

Chapter 7, Patient Information contains a Patient Information Sheet on each category of lupus medication covered here. The sheets can be used to teach lupus patients about the medications they may need to take. Each sheet contains general information about the category of drug, specific instructions on how and when to take the specific medication prescribed, information about possible side effects, and precautions.

Brand names included in this book are provided as examples only; their inclusion does not mean that these products are endorsed by NIH or any other Government agency. Also, if a particular brand name is not mentioned, this does not mean or imply that the product is unsatisfactory.

The NSAIDs comprise a large and chemically diverse group of drugs that possess analgesic, anti-inflammatory, and antipyretic properties. Pain and inflammation are common problems in patients with SLE, and NSAIDs are usually the drugs of choice for patients with mild SLE with little or no organ involvement. Patients with serious organ involvement may require more potent anti-inflammatory and immunosuppressive drugs.

Types of NSAIDs
There are as many as 70 NSAIDs on the market, and new ones are constantly becoming available. Some can be purchased as over-the-counter preparations, whereas larger doses of those drugs or other preparations are available only by prescription. For example, prescriptions are required for diclofenac sodium (Voltaren), indomethacin (Indocin), diflunisal (Dolobid), and nabumetone (Relafen).

Mechanism of Action and Use
The therapeutic effects of NSAIDs stem from their ability to inhibit the release of prostaglandins and leukotrienes, which are responsible for producing inflammation and pain. NSAIDs are very useful in treating joint pain and swelling and muscle pain. They may also be used to treat pleuritic chest pain. An NSAID may be the only drug needed to treat a mild flare; more active disease may require additional medications.

Although all NSAIDs appear to work in the same way, not every one has the same effect on every person. In addition, patients may do well on one NSAID for a period of time, then, for some unknown reason, derive no benefit from it. Switching the patient to a different NSAID should produce the desired effects. Patients should use only one NSAID at any given time.

Side/Adverse Effects
Gastrointestinal: Dyspepsia, heartburn, epigastric distress, and nausea; less frequently, vomiting, anorexia, abdominal pain, GI bleeding, and mucosal lesions. Misoprostol (Cytotec), a synthetic prostaglandin that inhibits gastric acid secretion, may be given to prevent GI intolerance. It prevents gastric ulcers and their associated GI bleeding in patients receiving NSAIDs.

Genitourinary: Fluid retention, reduction in creatinine clearance, and acute tubular necrosis with renal failure.

Hepatic: Acute reversible hepatotoxicity.

Cardiovascular: Hypertension and moderate to severe noncardiogenic pulmonary edema.

Hematologic: Altered hemostasis through effects on platelet function.

Other: Skin eruption, sensitivity reactions, tinnitus, and hearing loss.

Pregnancy and Lactation
NSAIDs should be avoided during the first trimester and just before delivery; they may be used cautiously at other times during pregnancy. NSAIDs appear in breast milk and should be used cautiously by breastfeeding mothers.

Antimalarials

This group of drugs was first developed during World War II because quinine, the standard treatment for malaria, was in short supply. Investigators discovered antimalarials could also be used to treat the joint pain that occurs with rheumatoid arthritis. Subsequent use of antimalarials showed that they are effective in controlling lupus arthritis, skin rashes, mouth ulcers, fatigue, and fever. They have also been shown to be effective in the treatment of DLE. Antimalarials are not used to manage more serious, systemic forms of SLE that affect the organs. It may be weeks or months before the patient notices that these drugs are controlling disease symptoms.

Types of Antimalarials
The drugs most often prescribed are hydroxychloroquine sulfate (Plaquenil) and chloroquine (Aralen).

Mechanism of Action and Use
The anti-inflammatory action of these drugs is not well understood. In some patients who take antimalarials, the total daily dose of corticosteroids can be reduced. Antimalarials also affect platelets to reduce the risk of blood clots and lower plasma lipid levels.

Side/Adverse Effects
Central Nervous System: Headache, nervousness, irritability, dizziness, and muscle weakness.

Gastrointestinal: Nausea, vomiting, diarrhea, abdominal cramps, and loss of appetite.

Ophthalmologic: Visual disturbances and retinal changes manifested by blurring of vision and difficulty in focusing. A very serious potential side effect of antimalarial drugs is damage to the retina. Because of the relatively low doses used to treat SLE, the risk of retinal damage is small. However, patients should have a thorough eye examination before starting this treatment and every 6 months thereafter.

Dermatologic: Dryness, pruritus, alopecia, skin and mucosal pigmentation, skin eruptions, and exfoliative dermatitis.

Hematologic: Blood dyscrasia and hemolysis in patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency.

Pregnancy
Antimalarials are considered to have a small risk of harming a fetus and should be discontinued in lupus patients who are attempting to become pregnant.

Corticosteroids

Corticosteroids are hormones secreted by the cortex of the adrenal gland. SLE patients with symptoms that do not improve or who are not expected to respond to NSAIDs or antimalarials may be given a corticosteroid. Although corticosteroids have potentially serious side effects, they are highly effective in reducing inflammation, relieving muscle and joint pain and fatigue, and suppressing the immune system. They are also useful in controlling major organ involvement associated with SLE. These drugs are given in much higher doses than the body produces and act as potent therapeutic agents. The decision to use corticosteroids is highly individualized and is dependent upon the patient’s condition.

Once the symptoms of lupus have responded to treatment, the dose is usually tapered until the lowest possible dose that controls disease activity is achieved. Patients must be monitored carefully during this time for flares or recurrence of joint and muscle pain, fever, and fatigue that can result when the dosage is lowered. Some patients may require corticosteroids only during active stages of the disease; those with severe disease or more serious organ involvement may need long-term treatment.

Treatment with corticosteroids must not be stopped suddenly if they have been taken for more than 4 weeks. Administration of corticosteroids causes the body’s own production of adrenal hormones to slow down or stop, and adrenal insufficiency will result if the drug is stopped suddenly. Tapering the dose allows the body’s adrenal glands to recover and resume production of the natural hormones. The longer a patient has been on corticosteroids, the more difficult it is to lower the dose or discontinue use of the drug.

Types of Corticosteroids
Prednisone (Orason, Meticorten, Deltasone, Cortan, Sterapred), a synthetic corticosteriod, is most often used to treat lupus. Others include hydrocortisone (Cortef, Hydrocortone), methlyprednisolone (Medrol), and dexamethasone (Decadron). Corticosteroids are available as a topical cream or ointment for skin rashes, as tablets, and as an injectable for intramuscular or intravenous administration.

Mechanism of Action and Use
The frequently prescribed corticosteroids are highly effective in reducing inflammation and suppressing the immune response. These drugs may be used to control exacerbation of symptoms and are used to control severe forms of the disease. The drug is usually administered orally. During periods of serious illness, it may be administered intravenously; once the patient has been stabilized, oral administration should be resumed.

Side/Adverse Effects
Central Nervous System: Convulsions, headache, vertigo, mood swings, and psychosis.

Cardiovascular: Congestive heart failure (CHF) and hypertension.¹

Endocrine: Cushing’s syndrome, menstrual irregularities, and hyperglycemia.

Gastrointestinal: GI irritation, peptic ulcer, and weight gain.

Dermatologic: Thin skin, petechiae, ecchymoses, facial erythema, poor wound healing, hirsutism,¹ and urticaria.

Musculoskeletal: Muscle weakness, loss of muscle mass, and osteoporosis.¹

Ophthalmologic: Increased intraocular pressure, glaucoma, exophthalmos, and cataracts.¹

Other: Immunosuppression and increased susceptibility to infection.

¹Long-term effects.

Pregnancy and Lactation
Corticosteroids cross the placenta, but can be used cautiously during pregnancy. They also appear in breast milk; patients taking large doses should not breastfeed.

Immunosuppressives

Immunosuppressive agents are generally used to reduce rejection of transplanted organs. They are also used in serious, systemic cases of lupus in which major organs such as the kidneys are affected or in which there is severe muscle inflammation or intractable arthritis. Because of their steroid-sparing effect, immunosuppressives may also be used to reduce or sometimes eliminate the need for corticosteroids, thereby sparing the patient from undesirable side effects of corticosteroid therapy.

Immunosuppressives can have serious side effects. Patients need to understand, however, that side effects are dose dependent and are generally reversible by reducing the dose or stopping the medication.

Types of Immunosuppressives
A variety of immunosuppressive drugs is available to treat lupus. Although they have different mechanisms of action, each type functions to decrease or prevent an immune response. The immunosuppressives most frequently used with SLE patients are azathioprine (Imuran), cyclophosphamide (Cytoxan), methotrexate (Rheumatrex), and cyclosporine (Sundimmune, Neoral).

Mechanism of Action and Use
Drugs like azathioprine, methotrexate, and cyclosporine are referred to as antimetabolite agents. These drugs block metabolic steps within immune cells and then interfere with immune function. Cytotoxic drugs like cyclophosphamide work by targeting and damaging autoantibody-producing cells, thereby suppressing the hyperactive immune response and reducing disease activity.

Risks
There are many serious risks associated with the use of immunosuppressives. They include immunosuppression (resulting in increased susceptibility to infection), bone marrow suppression (resulting in decreased numbers of RBCs, WBCs, and platelets), and development of malignancies.

Side/Adverse Effects
Dermatologic: Alopecia (cyclophosphamide only).

Gastrointestinal: Nausea, vomiting, stomatitis, esophagitis, and hepatotoxicity.

Genitourinary: Hemorrhagic cystitis, hematuria, amenorrhea,¹ impotence,¹ and gonadal suppression (cyclophosphamide only).²

¹ Temporary or reversible once drug therapy is discontinued.
² Recovery of function after drug is discontinued is unpredictable.

Hematologic: Thrombocytopenia, leukopenia, pancytopenia, anemia, and myelo-suppression.

Respiratory: Pulmonary fibrosis.¹

Other: Increased risk of serious infections or malignancies.

Pregnancy and Lactation
Use of immunosuppressives presents definite risks to the fetus. Female patients should use contraceptive measures during treatment and for 12 weeks after ending azathioprine therapy. Azathioprine may pass into breast milk, and women using this drug should consult with their doctors before breastfeeding.

¹ With high doses.

       
1. Erythematosus  2. Advances  3. Tests  4. Care  5. Medications 
6. Psychosocial Aspects  7. Patient Info.  8. Resources

January 26, 1999