Pharm 210 Immunosuppressant Drugs
Overview for Exam 2 Preparation with Complete
Solution
Immune System
Immunosuppressant Drugs
• The purpose of the immune system is to distinguish self from non-self and protect the
body from foreign material (antigens).
• There are two types of immunity: humoral immunity and cellular immunity.
o Humoral immunity is mediated by B lymphocytes
o Cellular immunity is mediated by T lymphocytes
• The immune system also participates in hypersensitivity, or anaphylactic reactions
which can be life threatening.
• Responsible for rejection of kidney, liver, and heart transplants.
• Can also sometimes attack itself, causing “autoimmune diseases” or immune-mediated
diseases
• Lines of defense
o First line of defense= mechanical barriers/chemical barriers
o Second line of defense= Inflammatory response/phagocytosis
o Third line of defense= Specific immune responses/natural killer cells
Immunosuppressant drugs:
• Drugs that decrease or prevent an immune response, and hence suppress the immune
system.
• Immunosuppressant’s are used for many immune related disorders, including:
RA, SLE, Crohn’s disease, Multiple sclerosis, Myasthenia gravis, and Psoriasis.
• Used to prevent or treat rejection of transplanted organs.
• Transplant patients are on immunosuppressant therapy for the duration of their
life! (so, their body doesn’t reject the organ)
o Mechanism of action
o they selectively suppress certain T-lymphocyte cell lines; preventing their
involvement in the immune response.
o Results in a pharmacologically immunocompromised state similar to that in a
cancer patient or someone with AIDS.
o Major classes of immunosuppressant drugs used in preventing organ rejection
include:
▪ Glucocorticoids
▪ Calcineurin inhibitors
▪ Antimetabolites ex. Azathioprine; inhibit cell proliferation
▪ Biologics inhibit cytotoxic T killer cell function
, o Corticosteroids = inhibit all stages of T-cell activation (used for induction,
maintenance immunosuppression, and acute rejection)
o Contraindications
o Main contraindication for all immunosuppressants is drug allergy
o Renal or hepatic failure, HTN (“many of these drugs cause a mild HTN),
and concurrent radiation therapy are also relative contraindications
depending on the patient’s condition
o Pregnancy not necessarily but should only be given to pregnant women in
clinically urgent situations
o Patients taking immunosuppressants must avoid live vaccines
o Side effects (Imuran)
o Place patients at high risk for opportunistic infections
o high risk for certain types of cancers, esp. skin cancers
, o nephrotoxicity
o post-transplant DM (“ex. steroids usually increase blood sugar”)
o Contraception and use of immunosuppressant women must use some form of
contraception during TX and for up to 12 weeks after therapy ends
o Review lab results for this group.
o Toxic effects. E.g. renal or liver failure
Name azathioprine (Imuran)
Class Antimetabolite
Route PO or IV
MOA Block metabolism of purines, inhibits the synthesis of T-cell
DNA,RNA, and proteins thereby blocking immune response
Indications Prevention of organ rejection in kidney transplantation;
treatment of Rheumatoid Arthritis (RA)
Interactions
Adverse Effects Leukopenia, thrombocytopenia, Hepatotoxicity
Contraindications
*Bone marrow suppression + lymphoma
*BM suppression – always check on blood counts and monitor V/S during TX.
*If WBC count less than 3000 or platelets less than 100,000 – contact prescriber (most likely D/C)
PowerPoint: Check CBC initially and periodically during treatment due to bone marrow
suppression. You have to protect the client from infection, check for nadir, watch for
bleeding and anemia.
Name tacrolimus (Program)
Class Calcineurin Inhibitor
Route PO + injectable
MOA Inhibits the production and release of IL-2
Indications Prevention of liver, kidney, heart, lung, pancreas, and small
bowel
transplant.
Unlabeled uses include: prevention of rejection of bone
marrow,
pancreas, pancreatic islet cells, and small intestine
transplantation, and severe psoriasis (HARE SAID KNOW
THIS)
Interactions
Adverse Effects Peripheral edema, acne, rash, anaphylaxis SEE TABLE 48-2
Contraindications Avoid grapefruit juice – increased effect
St. John’s wort – decreased effects
PP: lymphoma, hepatic artery thrombosis
Poveda: “Program is also an anti-tumor drug, when immunosuppressed more prone to cancer”
BOOK: Tacrolimus is used to prevent rejection and to treat rejection once it occurs
SG: tacrolimus (group):
• Book: sirolimus (Masamune) is an immunosuppressant drug, similar in structure to
, tacrolimus (Program).
• sirolimus = macro-cyclic immunosuppressive, antifungal, and anti-tumor drug
o levels are increased when taken with high-fat meals
• tacrolimus = used to prevent rejection and treat rejection once it occurs
• both drugs have warnings for potential development of lymphoma and serious
infections, as well as lung dehiscence, hepatic artery thrombosis, and hypersensitivity
reactions, including angioedema
Overview for Exam 2 Preparation with Complete
Solution
Immune System
Immunosuppressant Drugs
• The purpose of the immune system is to distinguish self from non-self and protect the
body from foreign material (antigens).
• There are two types of immunity: humoral immunity and cellular immunity.
o Humoral immunity is mediated by B lymphocytes
o Cellular immunity is mediated by T lymphocytes
• The immune system also participates in hypersensitivity, or anaphylactic reactions
which can be life threatening.
• Responsible for rejection of kidney, liver, and heart transplants.
• Can also sometimes attack itself, causing “autoimmune diseases” or immune-mediated
diseases
• Lines of defense
o First line of defense= mechanical barriers/chemical barriers
o Second line of defense= Inflammatory response/phagocytosis
o Third line of defense= Specific immune responses/natural killer cells
Immunosuppressant drugs:
• Drugs that decrease or prevent an immune response, and hence suppress the immune
system.
• Immunosuppressant’s are used for many immune related disorders, including:
RA, SLE, Crohn’s disease, Multiple sclerosis, Myasthenia gravis, and Psoriasis.
• Used to prevent or treat rejection of transplanted organs.
• Transplant patients are on immunosuppressant therapy for the duration of their
life! (so, their body doesn’t reject the organ)
o Mechanism of action
o they selectively suppress certain T-lymphocyte cell lines; preventing their
involvement in the immune response.
o Results in a pharmacologically immunocompromised state similar to that in a
cancer patient or someone with AIDS.
o Major classes of immunosuppressant drugs used in preventing organ rejection
include:
▪ Glucocorticoids
▪ Calcineurin inhibitors
▪ Antimetabolites ex. Azathioprine; inhibit cell proliferation
▪ Biologics inhibit cytotoxic T killer cell function
, o Corticosteroids = inhibit all stages of T-cell activation (used for induction,
maintenance immunosuppression, and acute rejection)
o Contraindications
o Main contraindication for all immunosuppressants is drug allergy
o Renal or hepatic failure, HTN (“many of these drugs cause a mild HTN),
and concurrent radiation therapy are also relative contraindications
depending on the patient’s condition
o Pregnancy not necessarily but should only be given to pregnant women in
clinically urgent situations
o Patients taking immunosuppressants must avoid live vaccines
o Side effects (Imuran)
o Place patients at high risk for opportunistic infections
o high risk for certain types of cancers, esp. skin cancers
, o nephrotoxicity
o post-transplant DM (“ex. steroids usually increase blood sugar”)
o Contraception and use of immunosuppressant women must use some form of
contraception during TX and for up to 12 weeks after therapy ends
o Review lab results for this group.
o Toxic effects. E.g. renal or liver failure
Name azathioprine (Imuran)
Class Antimetabolite
Route PO or IV
MOA Block metabolism of purines, inhibits the synthesis of T-cell
DNA,RNA, and proteins thereby blocking immune response
Indications Prevention of organ rejection in kidney transplantation;
treatment of Rheumatoid Arthritis (RA)
Interactions
Adverse Effects Leukopenia, thrombocytopenia, Hepatotoxicity
Contraindications
*Bone marrow suppression + lymphoma
*BM suppression – always check on blood counts and monitor V/S during TX.
*If WBC count less than 3000 or platelets less than 100,000 – contact prescriber (most likely D/C)
PowerPoint: Check CBC initially and periodically during treatment due to bone marrow
suppression. You have to protect the client from infection, check for nadir, watch for
bleeding and anemia.
Name tacrolimus (Program)
Class Calcineurin Inhibitor
Route PO + injectable
MOA Inhibits the production and release of IL-2
Indications Prevention of liver, kidney, heart, lung, pancreas, and small
bowel
transplant.
Unlabeled uses include: prevention of rejection of bone
marrow,
pancreas, pancreatic islet cells, and small intestine
transplantation, and severe psoriasis (HARE SAID KNOW
THIS)
Interactions
Adverse Effects Peripheral edema, acne, rash, anaphylaxis SEE TABLE 48-2
Contraindications Avoid grapefruit juice – increased effect
St. John’s wort – decreased effects
PP: lymphoma, hepatic artery thrombosis
Poveda: “Program is also an anti-tumor drug, when immunosuppressed more prone to cancer”
BOOK: Tacrolimus is used to prevent rejection and to treat rejection once it occurs
SG: tacrolimus (group):
• Book: sirolimus (Masamune) is an immunosuppressant drug, similar in structure to
, tacrolimus (Program).
• sirolimus = macro-cyclic immunosuppressive, antifungal, and anti-tumor drug
o levels are increased when taken with high-fat meals
• tacrolimus = used to prevent rejection and treat rejection once it occurs
• both drugs have warnings for potential development of lymphoma and serious
infections, as well as lung dehiscence, hepatic artery thrombosis, and hypersensitivity
reactions, including angioedema
