Immunosuppressants (Immunomodulators, Interleukin Receptor Antagonists)

Immunosuppressants or immune suppressants are usually used in conjunction with corticosteroids to block inflammatory reactions and decrease initial damage to cells in cases of organ transplantation and autoimmune diseases. Immunosuppressants include immunomodulators, T- and B-cell suppressors, interleukin receptor antagonists, and monoclonal antibodies (antibodies produced by a single clone of B-cells that react with specific antigens).

Immunosuppresants: Generic and Brand Names

Here is a table of commonly encountered immunosuppressants, their generic names, and brand names:

• Immune Modulators
  • fingolimod (Gilenya)
  • lenalidomide (Revlimid)
  • thalidomide (Thalomid)
• T- and B-Cell Suppressors
  • abatacept (Orencia)
  • azathioprine (Imuran)
  • cyclosporine (Sandimmune)
  • tacrolimus (Prograf)
• Interleukin Receptor Antagonist
  • anakinra (Kineret)
• Monoclonal Antibodies
  • infliximab (Remicade)
  • muromonab-CD3 (Orthoclone OKT3)

Immunomodulators

• Immune modulators block chemicals to suppress the immune system.

Therapeutic Action

The desired and beneficial action of immune modulators is:

• Blocking the release of various cytokines involved in the inflammatory response and activation of lymphocytes, decreasing immune activity.

Indications

Immune modulators are indicated for the following medical conditions:

• Lenalidomide and thalidomide inhibit proinflammatory cytokine secretions and increase anti-inflammatory cytokines from monocytes. Thalidomide is used in the treatment of multiple myeloma and erythema nodosum leprosum.
• Fingolimod inhibits the release of lymphocytes from lymph nodes into the peripheral blood so they cannot migrate to activate immune and inflammatory reactions. It is the first oral agent for the treatment of relapsing forms of multiple sclerosis.

Pharmacokinetics

Here are the characteristic interactions of immune modulators and the body in terms of absorption, distribution, metabolism, and excretion:

Route	Onset	Peak	Duration
PO	Slow	12-16 h	–

Half-life (T1/2)	Metabolism	Excretion
6-9 d	Liver	Urine

Contraindications and Cautions

The following are contraindications and cautions for the use of immunomodulators:

• Pregnancy. Can cause serious fetal harm.

T-and B-Cell Suppressors

• These drugs inhibit the actions of the cell-mediated immunity.

Therapeutic Action

The desired and beneficial action of T- and B-cell suppressors is:

• Not clearly understood. However, it has been shown that they block antibody production by B cells, inhibit suppressor and helper T cells, and modify the release of interleukins and of T-cell growth factor.

Indications

T- and B-cell suppressors are indicated for:

• Prevention and treatment of specific transplant rejection.

Pharmacokinetics

Here are the characteristic interactions of T- and B-cell suppressors and the body in terms of absorption, distribution, metabolism, and excretion:

Route	Onset	Peak	Duration
PO	Varies	3.5 h	–
IV	Rapid	1-2 h	–

Half-life (T1/2)	Metabolism	Excretion
19-27 h	Liver	Bile

Contraindications and Cautions

The following are contraindications and cautions for the use of T- and B-cell suppressors:

• Known allergy to drug and its components. Prevent hypersensitivity reactions.
• Pregnancy and lactation. Potential serious adverse effects on the fetus or neonate.   
• Renal or hepatic impairment. Interfere with metabolism or excretion of the drug.
• Known neoplasms. Potentially could spread with immune system suppression.

Adverse Effects

Use of T- and B-cell suppressors may result to these adverse effects:

• Increased risk for infection and development of neoplasms.
• CNS: headache, tremors
• CV: hypertension
• Respiratory: pulmonary edema
• GI: hepatotoxicity, GI upset, diarrhea
• GU: renal toxicity, renal dysfunction

Interactions

These drugs have drug-drug interactions with:

• Other hepatotoxic and nephrotoxic drugs. Combined toxicity.

Interleukin Receptor Antagonist

• Interleukin receptor antagonists block the activity of the interleukins that are released in an inflammatory or immune response.
• The only available interleukin receptor antagonist is anakinra (Kineret).

Therapeutic Action

The desired and beneficial action of interleukin receptor antagonist is:

• Antagonizing human interleukin-1 receptors, blocking the activity of interleukin-1. Interleukin-1 levels are elevated in response to inflammatory or immune reactions and are thought responsible for the degradation of cartilage that occurs in rheumatoid arthritis.

Indications

Interleukin receptor antagonist is indicated for:

• Reduction of signs and symptoms of moderately to severely active rheumatoid arthritis in patients 18 years of age and older who have not responded to traditional treatment.

Pharmacokinetics

Here are the characteristic interactions of interleukin receptor antagonist and the body in terms of absorption, distribution, metabolism, and excretion:

Route	Onset	Peak	Duration
Subcutaneous	Slow	3-7 h	–

Half-life (T1/2)	Metabolism	Excretion
4-6 h	Tissues	Urine

Contraindications and Cautions

The following are contraindications and cautions for the use of interleukin receptor antagonist:

• Known allergy to E-coli-produced products and to the drug itself. Prevent hypersensitivity reactions.
• Pregnancy and lactation. Drug may cross placenta and enter breast milk.
• Renal impairment, immunosuppression, active infection. Exacerbated by the effects of the drug.

Adverse Effects

Use of interleukin receptor antagonist may result to these adverse effects:

• EENT: sinusitis
• CNS: headache
• Respiratory: upper respiratory tract infections
• GI: nausea, diarrhea
• Skin: injection-site reactions

Interactions

These drugs have drug-drug interactions with:

• Etarnecept (Enbrel). Potential for severe and life-threatening infections.
• Potential for serious infections.

Monoclonal Antibodies

• Monoclonal antibodies attach to specific receptor sites to exhibit their immune suppressor actions.

Therapeutic Action

The desired and beneficial action of monoclonal antibodies is:

• Reacting as an antibody to human T cells, disabling T cells and acting as an immune suppressor.

Indications

Monoclonal antibodies are indicated for:

• Muromonab-CD3 is the first monoclonal antibody approved for use. It is indicated for treatment of acute allograft rejection in those receiving heart or liver transplants.

Pharmacokinetics

Here are the characteristic interactions of monoclonal antibodies and the body in terms of absorption, distribution, metabolism, and excretion:

Route	Onset	Peak	Duration
IV	Minutes	2-7 d	7 d

Half-life (T1/2)	Metabolism	Excretion
47-100 h	Tissues	Urine

Contraindications and Cautions

The following are contraindications and cautions for the use of monoclonal antibodies:

• Known allergy to drugs and to murine products. Prevent hypersensitivity reactions.
• Fluid overload. Can be exacerbated by drugs.
• Pregnancy and lactation. Potential adverse effects to fetus or neonate.
• Previous administration of monoclonal antibody. Serious hypersensitivity reactions can occur with repeat administration.

Adverse Effects

Use of monoclonal antibodies may result to these adverse effects:

• Respiratory: acute pulmonary edema associated with severe fluid retention and cytokine release syndrome (flu-like symptoms that can progress to third-spacing of fluids and shock).
• GI: nausea, diarrhea, vomiting
• Musculoskeletal: myalgia
• Others: fever, chills, malaise, increased susceptibility to infection and cancer
• Eculizumab can lead to intravascular hemolysis with resultant fatigue, pain, dark urine, shortness of breath, and blood clots.

Interactions

These drugs have drug-drug interactions with:

• Other immunosuppressants. Severe immune suppression with increased infections and neoplasms 

Nursing Considerations for Immunosuppressants

Here are important nursing considerations when administering suppressants:

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

• Assess for contraindications or cautions (e.g., history of allergies, pregnancy or lactation, renal and hepatic impairment, history of neoplasms, etc.) to avoid adverse effects.
• Establish baseline physical assessment to monitor for any potential adverse effects.
• Assess for presence of skin lesions to detect early dermatological effects.
• Obtain weight to monitor for fluid retention.
• Monitor temperature to detect any infection.
• Evaluate CNS status to assess CNS effects of the drug.
• Monitor pulse, blood pressure, and perfusion to assess for bleeding effects or cardiovascular effects of the drug.
• Monitor laboratory tests for CBC and liver and renal functions tests to determine the need for possible dose adjustment and to identify changes in bone marrow function.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of these drugs for therapy:

• Acute pain related to CNS, GI and flu-like effects
• Imbalanced nutrition: less than body requirements related to nausea and vomiting
• Anxiety related to diagnosis and drug therapy

Nursing Interventions

These are vital nursing interventions done in patients who are taking immunosuppressants:

• Arrange for laboratory tests before and periodically during therapy, including CBC and differential, to monitor for drug effects and adverse effects.
• Administer drug as indicated; instruct patient and significant other if injections are required to ensure that the drug will be given if the patient is not able to administer it.
• Protect the patient from exposure to infections and maintain strict aseptic technique for any invasive procedures to prevent infections during immunosuppression.
• Arrange for supportive care and comfort measures (e.g., rest, environmental control) to decrease patient discomfort and increase therapeutic compliance.
• Provide patient education about drug effects and warning signs to increase knowledge about drug therapy and to increase compliance with drug.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

• Monitor patient response to therapy (improvement in condition being treated).
• Monitor for adverse effects (e.g., flu-like symptoms, GI upset, increased infections, neoplasms).
• Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
• Monitor patient compliance to drug therapy.

Recommended Resources

Our recommended nursing pharmacology resources and books:

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See Also

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• Nursing Pharmacology – Study Guide for Nurses
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• Pharmacology Nursing Mnemonics & Tips
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• Generic Drug Name Stems Cheat Sheet
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• Common Drugs and Their Antidotes
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• IV Fluids and Solutions Guide & Cheat Sheet
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• Drug Dosage Calculations NCLEX Practice Questions (100+ Items)
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References and Sources

References and sources for this pharmacology guide for Immunosuppressants:

• Karch, A. M., & Karch. (2011). Focus on nursing pharmacology. Wolters Kluwer Health/Lippincott Williams & Wilkins. [Link]
• Katzung, B. G. (2017). Basic and clinical pharmacology. McGraw-Hill Education.
• Lehne, R. A., Moore, L. A., Crosby, L. J., & Hamilton, D. B. (2004). Pharmacology for nursing care.
• Smeltzer, S. C., & Bare, B. G. (1992). Brunner & Suddarth’s textbook of medical-surgical nursing. Philadelphia: JB Lippincott.