immuno drugs Flashcards
Cyclophosphamide
Cytotoxic and Antiproliferative Agent (T and B)
pro-drug, needs to be activated by cP450
cell cycle-nonspecific (CCNS) alkylating agent (entire cycle)
tx: anti-cancer agent, sev. rheumatologic conditions
suppressive: infections may happen
* SIGNAL 3*: can inactivate cell cycle
cyclophosphamide SEs: short term
GI: Nausea, vomiting, diarrhea; stomatitis; abdominal discomfort or pain.
Dermatologic: Alopecia (frequent).
Azathioprine [ImuranR]
Cytotoxic and Antiproliferative Agent (T*>B cells)
derivative of 6-mercaptopurine (anti-metabolite)
cell cycle specific: only targets S phase
inhibits adenosine deaminase
kidney transplants
RA
SIGNAL 3
Azathioprine [ImuranR] SEs: short and long term
GI: N/V (12%), diarrhea
- Hematologic: leukopenia or thrombocytopenia, macrocytic anemia, severe bone marrow depression. dose-related
- GU: temporary depression in spermatogenesis and reduction in sperm viability and sperm count
Pregnancy category D (fetal harm)*
may cause serious infections
carcinogen

Methotrexate [RheumatrexR]
Cytotoxic and Antiproliferative Agent (T and B)
inhibits dihydrofolic acid reductase (THF)
cell cycle specific
-targets 2nd phase of imm. response
tx for RA, Crohn’s, malignancy
SIGNAL 3
Methotrexate [RheumatrexR] potential for toxicity from high-dose regimens or delayed excretion is reduced by ??? during the final phase of methotrexate plasma elimination
leucovorin calcium
protects normal cells
Methotrexate [RheumatrexR] SEs
GI: N/V/D, stomatitis *hepatotoxicity *nephrotoxicity *obstructive pulmonary disease (COPD) infections
Cyclosporine [SandimmuneR]
T-Cell Suppressant
comes from a fungus
inhibits SIGNAL 1 by inhib. calcineurin phosphatases
inhib. IL-2–>inhib. T cell activation
suppresses CMI, some humoral immunity,
*reversible inhib.
Cyclosporine [SandimmuneR] may be affected by concomitant use of ???
because it requires ?? for metabolism
HIV protease inhibitors
anticonvulsants
azole antifungals
cytochrome P450 3A enzymes
Cyclosporine [SandimmuneR] SEs
nephrotoxicity (mild–>chronic progressive)
(peritubular cap. congesion, interstitial fibrosis w. tubular atrophy)
HTN
*can cross placenta!: terotgen
Cyclosporine [SandimmuneR] uses
organ transplants (take with corticosteroids, azathioprine)
RA
psoriasis
MYCOPHENOLATE MOFETIL [CellceptR]
T-Cell Suppressant
reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH)–>
inhib guanosine nucleotide synthesis
(affects T and B cells)
SIGNAL 3
MYCOPHENOLATE MOFETIL [CellceptR] SEs
GI
severe neutropenia
use in combo with cyclosporine, corticosteroids
Muromonab-CD3 (Orthoclone OKT3R)
T- cell suppressant
murine monoclonal Ab (IgG2a) blocks TCR (CD3) Ag
block calcineuria–>block IL-2–>block cell cycle/clonal expansion
tox: hypersn to murin products
* SIGNAL 1*
Lymphocyte Immune Globulin (AtgamR)
T-cell suppressant
- SIGNAL 1*
tox: may cause hypersn: prepped from horse IgG
risk for systemic infection
use with antimetabolite/cortster.
don’t use in pregnancy