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
Glucocorticoid immunosupressive effect
Inhibit cell mediated immunologic functions especially those dependent on lymphocytes
Glucocorticoid anti-inflammatory effect
Supressant on inflammatory process
Increase neutrophil
Decrease lymphocyte, eosinophil, basophil, monocyte
Inhibition of leukocyte migration
Induced synthesis of inhibitor of phospholipase A2
Decreased mRNA for COX2
Decreased IL-2 and IL-3
Decreased platelet activating factor
Other glucocorticoid effects
Normal renal excretion of water
CNS behavioral change
Stimulate gastric acid secretion
Decreased resistance to ulcer formation
DMARDs that interfere with activity of T lymphocytes
Immunosupressant used for rheumatoid arthritis
DMARDs
Hydroxychloroquine
Chloroquine
DMARD toxicity
Retinal toxicity Rash GI distress Myopathy Neuropathy
Inhibitot of dihydroorotate dehydrogenase an enzyme involved in de novo pyrimidine synthesis
Used in RA
Leflunomide
Cytotoxic to rapidly dividing immune cells due to inhibition of dihydrofolate reductase
Anticancer, rheumatoid disorders
Methotrexate
Methotrexate toxicity
Nausea Mucosal ulcera Hematoxicity Hepatotoxicity Teratogenecity
Inhibition of microtubule assembly decreases macrophage migration and phagocytosis
Chronic and acute gout
Familial Mediterranean Fever
Colchicine