Pharmacology of Rheumatoid Arthritis Flashcards
Front line Disease Modifying Anti-Rheumatic Drug
low dose MTX (MTX-(glu)n)
MOA: inhibits DHF-reductase
MOA of front line DMARD
MTX:
- inhibits DHFR = depleted thymidine/purines, resulting in antiproliferative and immunosuppressive
- inhibits AICAR-TFase, resulting in adenosine accumulation –> anti-inflammatory effects
Bioavailability of MTX
variable absorption - oral or parenteral differs form person to person
Clearance of MTX
kidneys
MTX toxicities (3)
- Hepatotoxicity (do LFTs)
- Pulmonary damage - hypersensitivity
- Myelosuppression
All people receiving MTX should also take ____
folic acid (or folinic acid - leucovorin)
Expect what in 3-6 weeks of MTX withdrawl
RA flare
GC receptor agonists MOA
repress transcription of inflammatory cytokines and COX2 (REPRESS NF-kB TF)
type of GC therapy for acute RA flare
pulse GC therapy
AE of GC therapy for RA
osteoporosis, DIABETOEGENIC
four CS and route
Oral - prednisone
IM - methylprednisolone
Intraarticular - triamcinolone, hexacetonide
Moderate to severe RA tx: TNF inhibitors
Etanercept (receptor decoy - absorbs TNFalpha)
Infliximab - mouse/human (antibody)
Adalimumab - human/human (antibody)
Anti-TNF agents result in increased risk of…
infections - TB and opportunistic infections
IL-1 inhibitor (receptor antagonist)
anakinra
what is a pegylated humanized antibody Fab’ fragment of TNF alpha monoclonal antibody
certolizumab
