Musculoskeletal System Pharmacology (NSAIDs, RA) π Flashcards
What are examples of NSAIDs?
Aspirin, ibuprofen, naproxen, diclofenac, celecoxib, etoricoxib
How do NSAIDs help to reduce inflammation?
They inhibit COX-1 or COX-2 enzymes which convert arachidonic acid into prostanoids
Which two of the NSAIDs are the most selective for COX-2?
Celecoxib, etoricoxib
What are the gastrointestinal adverse effects associated with NSAIDs?
Dyspepsia, nausea, peptic ulceration, bleeding and perforation, exacerbation of IBD
Why are NSAIDs contraindicated in CKD and heart failure?
There is a greater reliance on prostaglandins for vasodilation of afferent arteriole and renal perfusion
Why do COX-2 selective NSAIDs have a higher CVD risk compared to COX-1 selective?
COX-2 inhibits the synthesis of PGI2 which is generally protective for the CVS, doesnβt inhibit TXA2 which is generally bad for CVS
What is NSAID protein binding like?
Highly protein bound
What is the name and function of the enzyme methotrexate inhibits?
Dihydrofolate reductase: essential for synthesis of purines and pyrimidines
How often is the dosing for methotrexate?
Taken weekly
What feature of methotrexate should be considered when prescribing to females of reproductive age?
Highly teratogenic and abortifacient
What are ADRs associated with sulfasalazine?
Myelosupression, hepatitis, rash, N+V
Is sulfasalazine safe to use in pregnancy?
Yes, it is safe to use in pregnancy
What type of drug is rituximab?
A monoclonal antibody that depletes B-lymphocytes
Reactivation of what infection is a risk with TNF inhibitor drugs?
Tuberculosis reactivation
What are two examples of TNF inhibitors?
Infliximab, adalimumab