Immunosuppressant drugs work by inhibiting immune responses and are primarily used for organ transplantation and autoimmune diseases. The main classes of immunosuppressants are calcineurin inhibitors like cyclosporine and tacrolimus, mTOR inhibitors like sirolimus and everolimus, antiproliferative drugs like azathioprine and methotrexate, glucocorticoids like prednisolone, and biological agents that target proteins like TNF, IL-1, IL-2, CD3, and antibodies. These drugs are associated with side effects like nephrotoxicity, hypertension, infection risk, and bone marrow or liver toxicity that require close monitoring by nurses.

1. IMMUNOSUPPRESSANT DRUGS
----Dr. S.S. HASAN

2. IMMUNOSUPPRESSANTS
Immunosuppressants are drugs which inhibit
cellular/humoral or both types of immune
responses, and have their major use in organ
transplantation and autoimmune diseases.

3. • 1. Calcineurin inhibitors(Specific T-cell inhibitors)
Cyclosporine (Ciclosporin),
Tacrolimus
• 2. m-TOR inhibitors
Sirolimus, Everolimus
• 3. Antiproliferative drugs (Cytotoxic drugs)
Azathioprine, Methotrexate,
Cyclophosphamide, Chlorambucil,
Mycophenolate mofetil (MMF)
• 4. Glucocorticoids
Prednisolone and others

4. • 5. Biological agents
(a) TNF alpha inhibitors: Etanercept,
Infliximab, Adalimumab
(b) IL-1 receptor antagonist:
Anakinra
(c) IL-2 receptor antagonists:
Daclizumab,
Basiliximab
(d) Anti CD-3 antibody:
Muromonab
(e) Polyclonal antibodies:
Antithymocyte antibody (ATG),
Rho (D) immune globulin

7. Calcineurin inhibitors
Therapeutic Uses:
– Organ transplantation (kidney, liver, heart)
either alone or with other
immunosuppressive agents (Corticosteroids).
– Autoimmune disorders (low dose 7.5
mg/kg/d). e.g. endogenous uveitis,
rheumatoid arthritis, active Crohn’s disease,
psoriasis, nephrotic syndrome, severe
corticosteroid-dependent asthma, early type
I diabetes.

8. Adverse Effects
– Nephrotoxicity
– Neurotoxicity
– Hepatotoxicity
– Hirsutism
– Hypersensitivity
– Hypertension
– Hyperkalemia
– Hyperglycemia
– Hyperlipidemia
– Hyperplasia of gum

9. mTOR inhibitor
Therapeutic Uses:
Prophylaxis and therapy of graft
rejection reaction.
e.g. sirolimus eluted stent for coronary
angioplasty.
Sirolimus can be used alone, but is
generally combined with lower dose of
cyclosporine/tacrolimus
and/orcorticosteroids and
mycophenolate mofetil

10. Adverse Effects
• Hyperlipidemia (cholesterol, triglycerides).
• Thrombocytopenia
• Leukopenia
• Hepatotoxicity
• Hypertension
• GIT dysfunction

11. Antiproliferative drugs
(Cytotoxic drugs)
USES
• Acute glomerulonephritis
• Systemic lupus erythematosus
• Rheumatoid arthritis
• Crohn’ s disease
• Severe psoriasis
• Pemphigus
• Myasthenia gravis
• Uveitis
• Chronic active hepatitis

12. Adverse Effects
• Bone marrow depression:
leukopenia, thrombocytopenia.
• Gastrointestinal toxicity.
• Hepatotoxicity.
• Increased risk of infections

13. Glucocorticoids
• They particularly inhibit MHC expression
and activation/proliferation of T
lymphocytes.
• Expression of several IL and other
cytokine genes is regulated by
corticosteroids and production of
adhesion molecules is depressed.

14. USES
The corticosteroids are widely employed as
companion drug to cyclosporine or other
immunosuppressants in various organ
transplants.
 In case graft rejection sets in—large doses of
corticoids i.v. are employed for short periods.
They are used in practically all cases of severe
autoimmune diseases, especially during
exacerbation.

15. • 5. Biological agents
(a) TNF alpha inhibitors: Etanercept,
Infliximab, Adalimumab
(b) IL-1 receptor antagonist:
Anakinra
(c) IL-2 receptor antagonists:
Daclizumab,
Basiliximab
(d) Anti CD-3 antibody:
Muromonab
(e) Polyclonal antibodies:
Antithymocyte antibody (ATG),
Rho (D) immune globulin

16. ROLE OF NURSE
Be careful about sterility of drug administration,
universal precaution and good hand hygiene
Proper nutrition and vitamin supplements.
Oral immunosuppressants should be taken with
food to minimize GI upset.
Oral cyclosporine solution must be mixed in a
glass container
Careful about drug interactions.
Monitor lab reports closely: CBC, Renal and Liver
function tests.