DMARDs Flashcards
What are the Non-biological DMARDs
MTX Leflunomide Hydroxychloroquine Sulfasalazine Cyclosporine Azathioprine Cyclophosphamide Gold sodium thiomalate Auranofin
What are the Biological DMARDs
Adalimumab
Infliximab
Etanercept
Anakinra
What are used, but not real DMARDs
Glucocorticoids
What is the only purpose of NSAID administration in RA
Sx relief
What is the purpose of DMARD administration
Control Sx and delay disease progression
How long does it take for DMARDs to kick in
6 weeks to 6 months
Some bio in 2wks
What is the DOC for RA
MTX
What does MTX do
Decrease purine synthesis
How do you reduce MTX toxicity
Add Leucovorin or folate
What does Leflunomide do
Arrest cells in G1
Decrease pyrimidine synthesis
Used for UC Tx
Sulfasalazine
What do you give with Hydroxychloroquine
MTX
Sulfasalazine
How does Hydroxychloroquine work
Little gnomes in the blood
What must be done before Hydroxychloroquine administration
Opthalmologic exam
What are the Hydroxychloroquine AE
Hemolysis with G6PD deficiency
Retinal damage
What does MTX do
Inhibit AICAR transformylase
No IMP formation
Adenosine accumulation
What does a high amount of adenosine lead to
Decreased NF-kappaB
What are the MTX AE
Nausea
Ulcers
Hepatotoxicity
Pseudolymphomatous Rxn
When is MTX contraindicated
Pregnancy
What is MTX important in inhibiting in cancer
DHF reductase
How does Leflunomide act
Inhibits Dihydroorotate dehydrogenase
Decreases UMP
Inhibits autoimmune B, T cell prolif
What happens if you mix Leflunomide with MTX
Severe hepatotoxicity
What are the Leflunomide AE
Frequent diarrhea
Alopecia, rash
Myelosuppression
Increased aminotransferase activity
When is Leflunomide contraindicated
Pregnancy
What is the active form of Sulfasalazine
Sulfapyridine
What happens to Sulfasalazine in the colon
Metabolized to Sulfapyridine and 5-ASA
What are the Sulfasalazine AE
Nausea Anorexia Rash Hepatitis Leukopenia SLE
What can happens with Sulfasalazine in G6PD deficiency
Hemolysis
Is Sulfasalazine safe in pregnancy
Yes
What does Cyclosporine do
Inhibits Ag-induced signal transduction in T-cells
How does Cyclosporine work
Complex with Cyclophillin
Prevents NFAT dephos by calcineurin
Decreased IL-2
Main AE of Cyclosporine
Nephrotoxicity
Hirsutism
Gum hyperplasia
What is a purine antimetabolite
Azathioprine
When is Azathioprine administered as a DMARD
Refractory RA
How does Azathioprine work
Converted to 6-MP
Inhibition of de novo purine synth
Suppression of B and T cells
When should you reduce the Azathioprine dose
Pt taking Allopurinol
Inhibition of xanthine oxidase
What are the Azathioprine AE
BM suppression
GI disturbance
Infection/Malignancy
When do you give Cyclophosphamide
Severe RA
How does Cyclophosphamide work
Alkyklating agent crosslinks DNA
No cell replication
What is the main AE of Cyclophosphamide
Hemorrhagic Cystitis
How do you treat the main AE of Cyclophosphamide
Mesna
What are the other Cyclophosphamide AE
BM suppression, Infertility
Infection/Malignancy
Fanconi’s Anemia
What are the Macrophage poisons
Gold sodium thiomalate
Auranofin
How is GST administered
IM
How is Auranofin administered
PO
What do GST and Auranofin do
Suppress phagocytosis and lysosomal activity
What is the fully human IgG1 anti-TNF Ab
Adalimumab
What is the chimeric anti-TNF Ab
Infliximab
What is the recombinant anti-TNF Ab
Etanercept
How do anti-TNF Abs work
Bind TNFalpha and prevent receptor interaction
Downregulation of T-cell and macrophage function
What should be done before anti-TNF Ab Tx
Screening for latent TB
What is the main AE of anti-TNF Ab
Serious infection
What is the Il-1 receptor antagonist
Anakinra
When are Glucocorticoids given in RA
Short term Sx relief until positive DMARD effect is seen
What do Glucocorticoids do
Inhibit PLA2 and COX-2
What are the AE with chronic Glucocorticoid use
Osteoporosis Weight gain Ulcers HTN Hyperglycemia
What do you never give as combinatino therapy
Multiple biological DMARDs
