B.29-immunopharmacology 1 (cytotoxic agents, retinoids) +autoimmune diseases Flashcards
list the cytotoxic agents
cyclophosphamide methotrexate azathioprine, 6-MP (6-mercaptopurine) leflunomide mycophenolic acid
what is cyclophosphamide?
alkylating agent
how are the cytotoxic agents given?
oral or parenteral
except for leflunomide–> only oral
how is leflunomide and teriflunomide given?
oral
what is methotrexate?
anti-metabolite
inhibitor of dihydrofolate reductase
what is the mechanism of azathioprine and 6-MP?
inhibits de-novo purine synthesis
what is the mechanism of mycophenolic acid?
inhibits de novo GTP synthesis
*B and T cells are suppressed
what is the mechanism of leflunomide and teriflunomide?
inhibit de-novo pyrimidine synthesis
which cytotoxic agent requires hepatic P450 activation?
cyclophosphamide
why do we need adequate hydration in methotrexate?
to prevent urinary crystallization
from when is azathioprine effective?
after 12 weeks of starting therapy
indications for cyclophosphamide
hematological malignancies breast and ovarian cancer autoimmune diseases (SLE, GN, vasculitis)
indications for methotrexate
hematological malignancies
CNS and other solid tumors
Autoimmune diseases (RA, psoriasis)
indications for azathioprine and 6-MP
hematological malignancies
autoimmune diseases (SLE,RA)
IBD
indications for mycophenolic acid
solid organ transplantation autoimmune diseases (SLE, GN, myasthenia, psoriasis)
indications for leflunomide, teriflunomide
autoimmune diseases (RA, multiple sclerosis)
side effects for cyclophosphamide
myelosuppression
GI distress
hemorrhagic cystitis
what is given as an antidote for the damage of the bladder from cyclophosphamide?
mesna
SE from methotrexate
myelosuppression
toxic effects on skin and GI mucosa
pulmonary fibrosis (in chronic use)
what reduces the toxic effect of methotrexate?
folinic acid