Immunosuppressant drugs | Immunology | First Aid Lectures |Lec31 #drjamillecturers #drjameellectures
Channel: Dr. Jamil Lectures
Date: 21/04/2022

In this lecture we will discuss about Immunosuppressants drugs like cyclosporine,tacrolimus,sirolimus,basiliximab,azathioprine,mycophenolate mofetil,glucocorticoids.

https://youtu.be/CNXO-W0xw-A
https://youtu.be/ft9HRw8NNWY
https://youtu.be/aP06bUvyqCA

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Immunosuppressants
 Agents that block lymphocyte activation and proliferation. Reduce acute transplant rejection by 
suppressing cellular immunity (used as prophylaxis). Frequently combined to achieve greater 
efficacy with  toxicity. Chronic suppression  risk of infection and malignancy.

Cyclosporine Calcineurin inhibitor; 
binds cyclophilin
Blocks T-cell activation 
by preventing IL-2
transcription
Psoriasis, rheumatoid
arthritis
Nephrotoxicity, 
hypertension, 
hyperlipidemia, 
neurotoxicity, gingival 
hyperplasia, hirsutism
Both calcineurin 
inhibitors are 
highly nephrotoxic, 
especially in higher 
doses or in patients 
with decreased renal 
function
Tacrolimus (FK506) Calcineurin inhibitor; 
binds FK506 binding 
protein (FKBP)
Blocks T-cell activation 
by preventing IL-2 
transcription
Similar to cyclosporine, 
 risk of diabetes 
and neurotoxicity; 
no gingival 
hyperplasia orSirolimus (Rapamycin) mTOR inhibitor; binds 
FKBP
Blocks T-cell
activation and B-cell
differentiation by 
preventing response 
to IL-2
Kidney transplant 
rejection prophylaxis 
specifically
Sir Basil’s kidney 
transplant
“PanSirtopenia” 
Azathioprine Antimetabolite 
precursor of 
6-mercaptopurine
Inhibits lymphocyte 
proliferation by 
blocking nucleotide 
synthesis
Rheumatoid arthritis, 
Crohn disease, 
glomerulonephritis, 
other autoimmune 
conditions
Pancytopenia 6-MP degraded by 
xanthine oxidase; 
toxicity  by 
allopurinol
Pronounce “azathiopurine”
Mycophenolate 
Mofetil
Reversibly inhibits 
IMP dehydrogenase, 
preventing purine 
synthesis of B and T 
cells
Lupus nephritis GI upset, 
pancytopenia, 
hypertension, 
hyperglycemia
Less nephrotoxic and 
neurotoxic
Associated with 
invasive CMV 
infection
(pancytopenia), 
insulin resistance, 
hyperlipidemia; 
not nephrotoxic
Kidney “sir-vives.”
Synergistic with 
cyclosporine
Also used in drugeluting stents
Basiliximab Monoclonal antibody; 
blocks IL-2R
Edema, hypertension, 
tremor
Glucocorticoids Inhibit NF-κB


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Suppress both B- and 
T-cell function by 
 transcription of 
many cytokines
Induce T cell apoptosis
Many autoimmune 
and inflammatory 
disorders, adrenal 
insufficiency, asthma, 
CLL, non-Hodgkin 
lymphoma
Cushing syndrome, 
osteoporosis, 
hyperglycemia, 
diabetes, amenorrhea, 
adrenocortical 
atrophy, peptic ulcers, 
psychosis, cataracts, 
avascular necrosis 
(femoral head)
Demargination 
of WBCs causes 
artificial leukocytosis
Adrenal insufficiency 
may develop if drug is 
stopped abruptly after 
chronic use