methotrexate, leflunomide, sulfasalazine, hydroxychloroquine
What are the classical DMARDs? (4)
analog of folic acid; irreversibly inhibits dihydrofolate reductase; inhibiting proliferation and stimulating apoptosis in immune cells
Methotrexate MOA?
b
Which is the first-line DMARD for RA?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
b
Which stimulates the release of adenosine?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
b
Which has the quickest onset of action?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
nausea/mucosal ulcers (BW), elevated liver enzymes(BW), infection
What are AEs of Methotrexate? (3)
a,b
Which have BBW for teratogenicity?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
Hydroxychloroquine, leflunomide, methotrexate, sulfasalazine
Rank these drugs in terms of Half-life. (Longest-Shortest)
Leflunomide, Methotrexate, Hydroxychloroquine, Sulfasalazine.
3 months; 2 years
Methotrexate requires women to be ________ clean before they can become pregnant while Leflunomide requires women to be ________ clean.
a,b
Which has a BBW for hepatotoxicity?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
diarrhea, elevated liver enzymes
Leflunomide AE's? (2)
Cholestyramine
_______ is used to increase the excretion of Leflunomide.
inhibits pyrimidine synthesis; which leads to the inhibition of T-cell proliferation and reduction in B-cell ABs
Leflunomide MOA?
a,d
Which are prodrugs?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
unknown MOA; decreases: T cell response, B-cell proliferation, release of inflammatory cytokines
Sulfasalazine MOA?
d
Which medication has salicylate and sulfa metabolites?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
d
Which can cause urine to turn yellow-orange?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
d
Which med has 30% patient discontinuation?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
N/V, headache, rash, neutropenia
What are the AE's of Sulfasalazine? (4)
c, d
Which is safe in pregnancy?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
c
Which can cause irreversible retinal damage?
a) leflunomide
b) methotrexate
c) hydroxychloroquine
d) sulfasalazine
malaria, lupus
What are the main uses of Hydroxychloroquine? (2)
unknown; interferes with antigen process through suppressed t-cell response through leukocyte chemotaxis
Hydroxychloroquine MOA?
-citinib suffix
What are the tsDMARDs?
small synthetic molecule that disrupts JAK-STAT signaling pathway; inhibiting inflammatory gene transcription
Janus Kinase inhibitors MOA?
serious infections, cancer, increased CV events (thrombosis), death
What are the BBW for JAK-STAT inhibitors? (4)
JAKSTAT inhibitors
You should NEVER combine biologics and __________.
JAKSTATs; TB
Patients that take _______ should be tested for _________.
limited efficacy; high risk of toxicity
Why is Azathioprine not commonly used? (2)
prodrug of 6-mercaptopurine; an antimetabolite that inhibits lymphoid cell proliferation
Azathioprine MOA?
xanthine oxidase; 6-thiouric acid
__________ splits mercaptopurine into _________ causing renal excretion
along with small amounts of parent prodrug and mercaptopurine.
myelosuppression
What is the main AE of Azathioprine?
allopurinol
Which medication would require a dose reduction when used in
combination with Azathioprine?