Immunosuppressants
IMMUNOSUPPRESSANTS
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Introduction
·
Immunosuppressants are a class of drugs that
inhibit or prevent the activity of the immune system.
· These drugs are primarily used to prevent the rejection of transplanted organs and tissues and to treat autoimmune diseases, where the immune system mistakenly attacks the body’s own tissues.
Classification
- Calcineurin Inhibitors
- Examples: Cyclosporine, Tacrolimus
- Mechanism: Inhibit the enzyme calcineurin, which is essential for T-cell
activation.
- mTOR Inhibitors
- Examples: Sirolimus, Everolimus
- Mechanism: Inhibit the mammalian target of rapamycin (mTOR), which is a key
enzyme in cell proliferation.
- Antiproliferative Agents
- Examples: Azathioprine, Mycophenolate mofetil
- Mechanism: Inhibit the proliferation of immune cells by interfering with DNA
synthesis.
- Corticosteroids
- Examples: Prednisone, Methylprednisolone
- Mechanism: Suppress the immune response by decreasing the production of
inflammatory mediators.
- Monoclonal Antibodies
- Examples: Basiliximab, Rituximab
- Mechanism: Target specific molecules on immune cells, leading to their
depletion or inhibition.
- Other Immunosuppressants
- Examples: Methotrexate, Cyclophosphamide
- Mechanism: Interfere with the immune cell replication or function by various
mechanisms.
Pharmacokinetics
- Absorption: Most immunosuppressants are well absorbed orally, but
bioavailability can vary.
- Distribution: These drugs are distributed throughout the
body, often binding to plasma proteins.
- Metabolism: Many immunosuppressants are metabolized in the liver, primarily
through the cytochrome P450 enzyme system.
- Excretion: The metabolites are usually excreted via the kidneys.
Uses
- Organ Transplantation: To prevent the rejection of transplanted
organs such as kidneys, liver, and heart.
- Autoimmune Diseases: To manage conditions like rheumatoid
arthritis, lupus, and multiple sclerosis.
- Inflammatory Diseases: To treat conditions such as Crohn's disease
and ulcerative colitis.
Adverse Effects
- Increased Risk of Infections: Due to the suppression of the immune system.
- Nephrotoxicity: Particularly with drugs like cyclosporine and
tacrolimus.
- Hypertension: Common with many immunosuppressants.
- Hepatotoxicity: Liver damage may occur with certain drugs.
- Bone Marrow Suppression: Leading to anemia, leukopenia, and
thrombocytopenia.
- Malignancies: Long-term use is associated with an increased
risk of cancer, particularly lymphomas.
Contraindications
- Active Infections: Immunosuppressants should not be used in
patients with uncontrolled infections.
- Pregnancy and Breastfeeding: Some immunosuppressants may be teratogenic or
pass into breast milk.
- Liver or Kidney Disease: Patients with severe hepatic or renal
impairment may require dose adjustments or alternative therapies.
Role of the
Nurse
- Patient Education: Nurses should educate patients on the
importance of adherence to immunosuppressant therapy and the risks of
non-compliance.
- Monitoring: Regular monitoring of blood levels, renal function, liver
function, and signs of infection or adverse effects.
- Administration: Ensure correct dosage and timing,
particularly for drugs with a narrow therapeutic index like cyclosporine.
- Support: Provide psychological support to patients, especially those
undergoing long-term therapy or dealing with the side effects of the
medication.
- Coordination of Care: Collaborate with other healthcare
professionals to ensure comprehensive care, including regular check-ups
and adjustment of medication as needed.
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