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Immunosupressants

BRAND NAMES

Azasan©, CellCept©, Copaxone©, Gengraf©, Imuran©, Meticorten©, Neoral©, Orthoclone OKT3©, Prograf©, Rapamune©, Sandimmune©, SangCya©, Simulect©, Zenapax©.

BACKGROUND

Immunosuppressants are drugs that are used to weaken the body's immune system. The immune system protects the body from infections and diseases.

Sometimes the immune system can cause harm to the body, and immunosuppressants are needed to prevent or minimize damage. For instance, immunosuppressants are commonly used to treat autoimmune disorders, such as lupus, rheumatoid arthritis, and multiple sclerosis (MS). Autoimmune disorders occur when the immune system launches an attack against body cells because they are mistaken for harmful invaders, such as bacteria. Left untreated, the immune system can potentially destroy body tissues and organs, which may lead to organ failure. Organ failure is fatal unless the patient receives an organ transplant.

Immunosuppressants are also used to prevent transplant rejection in patients who receive transplanted organs. Transplant rejection occurs when the recipient's immune system does not recognize the donated organ as part of its own body. The white blood cells attack the new organ because it is identified as a harmful foreign invader. Therefore, patients who receive an organ transplant take a combination of immunosuppressants for the rest of their lives to prevent the body from destroying the new organ.

Immunosuppressants are only available by prescription. Commonly prescribed immunosuppressants include cyclosporine (Neoral©, Sandimmune©, Gengraf©), azathioprine (Azasan©, Imuran©), basiliximab (Simulect©), aclizumab (Zenapax©), muromonab CD3 (Orthoclone OKT3©), tacrolimus (Prograf©), glatiramer acetate (Copaxone©), mycopehnolate (CellCept©), and sirolimus (Rapamune©). They are available in tablet, capsule, liquid, and injectable forms. The recommended dosage depends on the specific drug, condition it is being used for, as well as the age and overall health of the patient.

Patients who are taking immunosuppressants should visit their healthcare providers regularly to monitor treatment and check for unwanted side effects. Patients should also take medications exactly as prescribed.

SIDE EFFECTS AND COMPLICATIONS

General: Side effects of treatment depend on the specific dose and medication, as well as the overall health of the patient. Some of the most common side effects include high blood pressure, increased hair growth, loss of appetite, vomiting, and upset stomach. Some patients may develop serious side effects, including kidney problems or decreased levels of red or white blood cells. Patients should tell their healthcare providers if they experience any of these symptoms.

Cancer: Patients who take immunosuppressants long-term (such as organ transplant recipients) have an increased risk of developing certain cancers, especially skin cancer and cancer of the lymph nodes (lymphoma). To help avoid the risk of skin cancer, patients should wear a sunblock with a sun protection factor (SPF) of 15 or higher. The sunblock should offer protection against both ultraviolet A and ultraviolet B rays. Patients should look for products that are PABA-free. PABA is a chemical that is found in many sunblocks, and it has shown to cause irritation in sensitive patients. Tanning beds should be avoided. There is currently no known method of prevention for lymphoma.

Infections: Since immunosuppressants weaken the immune system, patients have an increased risk of developing infections. Patients should regularly wash their hands with soap and water. Avoiding close contact with individuals who have contagious illnesses may help reduce the risk of contracting infections. Patients should consult their healthcare providers if they develop symptoms of an infection, such as fever, sore throat, or enlarged lymph nodes.

Potassium levels: Some immunosuppressants, including cyclosporine (Neoral©, Sandimmune©, Gengraf©), have been shown to increase potassium levels in the blood. Therefore, patients should minimize or avoid foods that have high amounts of potassium such as bananas, tomatoes, dried fruit, and low sodium salt. Patients should not take potassium supplements with immunosuppressants.

PRECAUTIONS

Co-existing medical conditions: Patients should tell their healthcare providers if they have any other medical conditions. Immunosuppressants can worsen symptoms of some conditions, including chicken pox or a viral infection of the nerves called shingles. Immunosuppressants may have increased effects if taken in patients with liver disease or kidney disease because the body is slow to break down the drug. Immunosuppressants may be weakened if patients have gastrointestinal problems because the drug may not be absorbed properly.

Interactions: Patients should tell their healthcare providers if they are taking any other drugs (prescription or over-the-counter), herbs, or supplements because they may interact with treatment.

Patients should not eat grapefruit or drink grapefruit juice one hour before taking cyclosporine (Neoral©, Sandimmune©, Gengraf©) because the fruit may break down the drug before it is absorbed into the bloodstream.

The effects of azathioprine (Azasan©, Imuran©) may be stronger in patients who take allopurinol (Aloprim©, Zyloprim©), a medicine used to treat gout. This combination may cause immunosuppressants to weaken the immune system too much, and it may lead to an increase in side effects. Therefore, patients taking these drugs may require lower doses of allopurinol and/or azathioprine.

The effects of cyclosporine (Neoral©, Sandimmune©, Gengraf©) may be stronger when taken with female hormones (estrogens), male hormones (androgens), antifungals such as asketoconazole (Nizoral©), ulcer drugs such ascimetidine (Tagamet©), or erythromycins, which are used to treat infections. These combinations may cause immunosuppressants to weaken the immune system too much, and it may lead to an increase in side effects. Patients may require lower doses of the medications.

If sirolimus (Rapamune©) is prescribed in combination with cyclosporine (Neoral©, Sandimmune©, Gengraf©), it should be taken four hours after cyclosporine. This reduces the risk of side effects.

Immunosuppressants should be used cautiously with other drugs that weaken the immune system, such as corticosteroids (such as prednisone) or anticancer drugs, such as chlorambucil (Leukeran©), cyclophosphamide (Cytoxan©), or mercaptopurine (Purinethol©).

Pregnancy and breastfeeding: Patients should tell their healthcare providers if they may be pregnant or are thinking about becoming pregnant because immunosuppressants may cause serious side effects in the fetus. This may occur if the medication is taken during pregnancy or if the male or female takes the drug during conception.

Patients taking immunosuppressants should not breastfeed their babies. The drugs can pass into the breastmilk and may cause serious side effects in the baby.

Treatment adherence: Patients should take their medications exactly as prescribed by their healthcare providers. Patients should not change the dose or stop taking the medication without first consulting their healthcare providers.

Vaccines: Before receiving vaccines, patients should tell their healthcare providers if they are taking immunosuppressants. In general, vaccines may be less effective in patients who are taking immunosuppressants. Live viral vaccines that contain a live virus, such as small pox or chickenpox, should not be given to patients taking immunosuppressants. This is because live viral vaccines may infect recipients who have weakened immune systems. Patients may even become infected if they come into close contact with a recently vaccinated individual. While this is uncommon, it occurs most often in individuals who have weakened immune systems.

INTEGRATIVE THERAPIES

Unclear or conflicting scientific evidence :

Cordyceps : Cordyceps is a parasitic fungi that is commonly used as a dietary supplement and tonic beverage. Two studies using combination herbal treatments that included cordyceps indicate that these combinations suppressed the immune system in kidney transplant and lupus nephritis patients. However, because these treatments used combination products, the effect of cordyceps cannot be defined. More studies with cordyceps as a single therapy are needed.

Avoid if allergic or hypersensitive to cordyceps, mold, or fungi. Use cautiously with diabetes, bleeding disorders, or prostate conditions. Use cautiously if taking anticoagulants, immunosuppressants, hormonal replacement therapy, or oral contraceptives. Avoid with myelogenous types of cancers. Avoid if pregnant or breastfeeding.

Traditional or theoretical uses, which lack sufficient evidence :

Bupleurum : Bupleurum is an herb that is typically found in East Asia. Bupleurum has long thin leaves that look like fennel. Bupleurum may have immune inhibitory effects. However, there is insufficient available evidence on the safety and efficacy of this treatment in humans. Further research is warranted.

Avoid if allergic or hypersensitive to Bupleurum, snakeroot, cow parsnip, poison hemlock, or Apiaceae or Umbelliferae (carrot) families. Use cautiously if operating motor vehicles or hazardous machinery due to a possible risk of sedation. Use cautiously with diabetes. Saikosaponins, constituents of Bupleurum, have been shown to increase plasma glucose concentrations in rat studies. Use cautiously with high blood pressure, diabetes, or edema due to possibility of adrenal stimulation. Use cautiously if taking anticoagulants due to theoretical inhibition of human platelet activation. Avoid if pregnant or breastfeeding due to insufficient available evidence of safety.

Cascara sagrada : Cascara is obtained from the dried bark of Rhamnus purshianus (Rhamnaceae), which is a medicinal and poisonous plant found in Europe, western Asia, and North America. Cascara may have immunosuppressant activities. However, further research is necessary to determine whether this treatment is safe and effective in humans.

Cascara was formerly U.S. Food and Drug Administration (FDA)-approved as safe and effective, but this designation was removed in 2002 because of lack of supporting evidence. Avoid if allergic or hypersensitive to cascara or the Rhamnaceae family. Use cautiously with anticoagulants (blood thinning) drugs, corticosteroids, diuretics, isoniazid or sulfisoxazole, licorice, and vitamin K. Use cautiously in children due to the risk of electrolyte loss, specifically low levels of potassium. Use cascara cautiously in elderly patients. Avoid using cascara with nausea or vomiting, inflammatory bowel disease, appendicitis, intestinal obstruction, acute intestinal inflammation, Crohn's disease, ulcerative colitis, appendicitis, ulcers, or abdominal pain of unknown origin. Avoid with other laxatives. Avoid if pregnant or breastfeeding. Be aware that prolonged use of cascara may lead to dependence and tolerance.

Dong quai : Dong quai, (Angelica sinensis), also known as Chinese angelica, has been used for thousands of years in traditional Chinese, Korean, and Japanese medicine. It remains one of the most popular plants in Chinese medicine. Although dong quai has been suggested as a possible immunosuppressant, human studies on the safety and efficacy of this treatment are lacking. Further research is necessary.

Although Dong quai is accepted as being safe as a food additive in the United States and Europe, its safety in medicinal doses is unknown. There are no reliable long-term studies of side effects available. Avoid if allergic or hypersensitive to Angelic radix or members of the Aplaceael Umbelliferae family (such as anise, caraway, carrot, celery, dill, or parsley). Avoid prolonged exposure to sunlight or ultraviolet light. Use cautiously with bleeding disorders or if taking drugs that may increase the risk of bleeding (anticoagulants). Use cautiously with diabetes, glucose intolerance, or hormone sensitive conditions (such as breast cancer, uterine cancer, ovarian cancer, or prostate). Do not use before dental or surgical procedures. Avoid if pregnant or breastfeeding.

Glucosamine : Glucosamine is a natural compound that is found in healthy cartilage. Laboratory studies suggest that glucosamine may have immunosuppressant activities, but human evidence is lacking. Further research is necessary before a firm conclusion can be made.

Avoid if allergic or hypersensitive to shellfish or iodine. Some reports suggest a link between glucosamine/chondroitin products and asthma. Use cautiously with diabetes or with a history of bleeding disorders. Avoid if pregnant or breastfeeding.

Horny goat weed : Horny goat weed is an herb that is commonly used in traditional Chinese medicine (TCM). Although laboratory evidence suggests that horny goat weed may act as an immunosuppressant, human studies are lacking. Further research is needed in order to evaluate the safety and efficacy of this treatment in humans.

Avoid if allergic or hypersensitive to horny goat weed (Epimedium grandiflorum), its constituents, or related plants in the Berberidaceae family. Use cautiously with tachyarrhythmia, decreased blood pressure, frequent nosebleeds, musculoskeletal disorders, bipolar disorder, immune function disorders, homocysteine disorders, hypothyroid conditions, or cardiovascular disease. Use cautiously if taking anticoagulants or antiplatelet (blood thinning) medications, anti-hypertensive (blood pressure) medications, antidepressants (MAOIs), interleukins, or cholesterol-lowering medications. Avoid with hormone-sensitive conditions or if taking estrogen or birth control pills. Avoid in patients with fire from yin deficiency (people with too much "yang" or heat, masculinity, and activity, based on Chinese philosophy). Avoid if pregnant or breastfeeding.

Nopal : Traditionally, nopal, or prickly pear, has both food and medicinal uses. According to laboratory research, nopal may have immunosuppressant properties. However, there is insufficient human evidence available on the safety and efficacy of this particular treatment.

Avoid if allergic/hypersensitive to nopal (Opuntia spp.), any of their constituents, or members of the Cactaceae family. Use cautiously if taking medications that alter blood sugar, cholesterol, or blood pressure. Use cautiously with thyroid dysfunction, rhinitis (runny or congested nose), or asthma. Avoid with immunosuppression or impaired liver function. Avoid if pregnant or breastfeeding. The nopal plant should be handled cautiously because it is covered in long, sharp spines and shorter soft-appearing barbs of glochids, which may be painful and difficult to remove once they are imbedded in the skin. It is recommended that oral doses of dried nopal be taken with at least eight ounces (250 milliliters) of water.

Omega-3 fatty acid : Although omega-3 fatty acid has been suggested as a possible immunosuppressant, human evidence is lacking. Additional research in humans is warranted.

Avoid if allergic or hypersensitive to fish, omega-3 fatty acid products that come from fish, nuts, linolenic acid, or omega-3 fatty acid products that come from nuts. Avoid during active bleeding. Use cautiously with bleeding disorders, diabetes, low blood pressure, or drugs, herbs, or supplements that treat any such conditions. Use cautiously before surgery. The Environmental Protection Agency (EPA) recommends that fish intake be limited in pregnant or nursing women to a single six-ounce meal per week and to less than two ounces per week in young children. For farm-raised, imported, or marine fish, the U.S. Food and Drug Administration (FDA) recommends that pregnant or nursing women and young children avoid eating types of fish with higher levels of methylmercury and less than 12 ounces per week of other fish types. Women who might become pregnant are advised to eat seven ounces or less per week of fish with higher levels of methylmercury or up to 14 ounces per week of fish types with about 0.5 parts per million (such as marlin, orange roughy, red snapper, or fresh tuna).

Red yeast rice : Red yeast rice (RYR) is the product of yeast (Monascus purpureus) grown on rice. Laboratory research suggests that RYR may have immunosuppressant properties. However, additional research in humans in needed before a firm conclusion can be made.

Avoid if allergic or hypersensitive to red yeast. Avoid with liver disease. Use cautiously with bleeding disorders. Avoid if pregnant or breastfeeding.

Rehmannia : Traditional Chinese medicine (TCM) has used rehmannia for centuries as an immunosuppressive agent. However, there is insufficient available human evidence on the safety and efficacy of this treatment.

Avoid if allergic or hypersensitive to rehmannia, any of its constituents, or any members of the Scrophulariaceae family. Use cautiously if taking anticoagulants, blood pressure medications, diuretics, or thyroid medication. Use cautiously with diabetes. Use cautiously in children younger than two years of age. Avoid if taking therapeutic immunosuppressants. Avoid with diarrhea and lack of appetite. Avoid if pregnant or breastfeeding.

Vitamin B12 : Although vitamin B12 has been suggested as a possible immunosuppressant, there is not enough available evidence to support this claim.

Avoid vitamin B12 supplements if allergic or hypersensitive to cobalamin, cobalt, or any other product ingredients. Avoid with coronary stents (mesh tube that holds clogged arteries open) or Leber's disease. Use cautiously if undergoing angioplasty. Vitamin B12 is generally considered safe when taken in amounts that are not higher than the recommended dietary allowance (RDA). The highest dose of vitamin B12 that is safe for pregnant women is 2.6 micrograms daily and 2.8 micrograms during breastfeeding. There is not enough scientific data available about the safety of larger amounts of vitamin B12 during pregnancy.

AUTHOR INFORMATION

This information has been edited and peer-reviewed by contributors to the Natural Standard Research Collaboration (www.naturalstandard.com).

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Copyright © 2011 Natural Standard (www.naturalstandard.com)
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