Rheumatology, NSAIDs, Acetaminophen Flashcards
Rapidly converted to mycophenolic acid which inhibits inosine monophosphate dehydrogenase (an enzyme in the de novo pathway of guanosine triphosphate synthesis GTP)
Supresses both B and T lymphocyte activation
Mycophenolate mofetil
Ind: SLE, Transplants
Mycophenolate toxicity
GI
Myelosupression (neutropenia)
Alkylating agents
Cyclophosphamide
Cisplatin
Antimetabolites
5-FU
Methotrexate
Gemcitabine
6-mercaptopurine
Antitumor antibiotics
Bleomycin
Doxorubicin
Mitomycin
Natural product
Etoposide
Paclitaxel
Vincristine
Alklyating agents form reactive molecular species that alkylate
nucleophilic groups on DNA bases particulary N-7 position of guanine
Nitrogen mustard alkylating agent that alkylates nucleophilic groups ob DNA bases particularly the N-7 position of guanine
Cross-linking of bases, abnormal base pairing, and DNA strand breakage
Used in SLE, leukemia, non-Hodgkin’s, breast, ovarian cancer and neuroblastoma
Cyclophosphamide
Breakdown product of cyclophosphamide by CYP450
Needed for antitumor activity
Acrolein
Cyclophosphamide toxicity
GI distress
Myelosupression
Alopecia
Hemorrhagic cystitis
Cardiac dysfunction
Pulmo toxicity
SIADH
Adverse effect of cyclophosphamide from acrolein formation
Decreased by vigorous hydration and by use of mercaptoethane sulfonate (MESNA)
Hemorrhagic cystitis
First ever targeted biological treatment for SLE
Fully humanized IgG1 gamma monoclonal antibody against soluble B lymphocyte stimulator
Belimumab
Enter the cell and bind to cytosolic receptors that transport it into the nucleus
This complex alters genes expression by binding to GRE (response elements) and tissue specific responses are made possible by protein regulators
Glucocorticoids
Glucocorticoid organ and tissue effect on metabolism
Stimulates gluconeogenesis Blood glucose rise Muscle protein catabolism Increased insulin secretion Lipolysis and lipogenesis stimulation with fat deposition
Glucocorticoid catabolic effect
Muscle protein catabolism
Lymphoid tissue connective tissue fat and skin wasting
Osteoporosis