[PHARM] Anti-Rheumatic Drugs [Wolff] Flashcards
What is a DMARD?
Disease modifying anti-rheumatic drug
Goals of RA therapy?
Stop inflammation
Relieve symtpoms
Prevent joint/organ damage
What are the first line drugs used for RA pain?
NSAIDs
What is the indirect mechanism for immunosuppression for glucocorticoids?
Complex with NF-kappaB and AP1 transcription factors
When are glucocorticoids most useful in treating RA?
Treating FLARES
Alleviates pain and inflammation
What are some of the consequences of high dose glucocorticoids?
- Cushing syndromes
- Upper body obesity
- Buffalo hump
- Acne
- Striae
- Hirsutism
When do you use glucocorticoids?
For a short period while AWAITING A CLINICAL RESPONSE to the slower-acting disease-modifying antirheumatic drug (DMARD)
MOA of methotrexate?
Drug undergoes polyglutamation
It accumulats in cells over time, this blocks AICAR (this blocks purine synthesis)
This causes the anti-inflammatory effects
What is methotrexate used for?
1st line for RA
Acts faster than all other DMARDs
High efficacy, safety and low cost
Toxicities with methotrexate?
Congenital abnormalities
Bone marrow suppression
Hepatic fibrosis
GI ulceration
MOA of hydroxychloroquine
Accumulates in lysosomes
Increases the pH of the lysosomes, makes less effective
This slows the progress of class II MHC molecules
What is unique about the populations that can take hydroxychloroquine?
Anti-malarial
***SAFE IN PREGNANCY
What is the major concerning toxicity with hydroxychloroquine?
Retinal damage
When is sulfasalazine used?
Typically introduced during RA treatment for:
“Triple therapy”
It’s a combination of hydoxychloroquine, methotrexate and sulfasalazine. Typically use triple thearpy before goint to biologics
What is an important thing to remember with biologic DMARDs?
Biologic DMARDs should NEVER BE COMBINED
*you could literally kill your patient
What are some of the benefits of biologic DMARDs?
Faster onset of action
High rate of response
What are some of the downsides to using biologic DMARDs?
More expensive
Increased risk for severe adverse effects
What are the (3) TNF inhibitors?
Etanercept
Infliximab
Adalimumab
What is the best selling drug in the world?
Adalimumab
(Very effective, recombinant FULLY HUMAN anti-TNF mAb)
*Humera
MOA of rituximab?
Antibody targets CD20
Specifically KILLS B CELLS while leaving plasma cells alone
MOA of abatacept?
Prevents CD28 from binding to its counter receptor CD80/CD86
T cell activation inhibitor
MOA of tocilizumab?
Humanized anti-human IL-6 receptor antibody
Competes for both the membrane bound and soluble forms of human IL-6 receptor
MOA of tofacitinib?
JAK3 antagonist
What is unique about the pharmacokinetics of tofacitinib?
ORALLY administered
All the others require injection
MOA of anakinra
IL-1 receptor antagonist
