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Inflammation Treatment & Anti-Rheumatic Drugs
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What is the generic name for Advil/Motrin?
ibuprofen
Name the NSAIDs using generic names?
Ibuprofen, Naproxen, Diclofenac, Meloxicam, Celecoxib
What is the target for NSAIDs?
COX-1 and COX-2
What is the target family for NSAIDs?
Cyclooxygenase
What is the MOA for NSAIDs?
Reversibly inhibits COX-1/COX-2 → Decreases conversion of arachidonic acid into prostaglandins → Decreases prostaglandins-mediated inflammation, pain, and fever
What is ibuprofen intended use?
Non-selective NSAID
Symptomatic pain/inflammation
What is naproxen intended use?
Longer-acting NSAID
Pain/Inflammation Relief
What is diclofenac intended use?
Pain/Inflammation relief
What is meloxicam intended use?
OA/RA pain & inflammation
Preference to COX-2
What is celecoxib intended use?
OA/RA pain & inflammation
Why is Celebrex a special NSAIDs?
Targets only COX-2
Name the NSAIDs using brand names?
Motrin, Aleve, Voltaren, Mobic, Celebrex
What is the generic name for Aleve?
Naproxen
What is the generic name for Voltaren?
Diclofenac
What is the generic name Mobic?
meloxicam
What is the generic name for Celebrex?
Celecoxib
What is the brand name for acetaminophen?
Tylenol
What is the drug group for acetaminophen?
Non-opioid analgesic/ antipyretic
Name the drugs for Glucocorticoid?
Methylprednisolone and Prednisone
What is the drug target for Glucocorticoid?
Glucocorticoid Receptor (GR)
What is the methylprednisone and prednisone intended use?
Rapid suppression of inflammation
What else is methylprednisolone used for?
Infection risk, osteoporosis, adrenal suppression
What is the MOA for methylprednisolone?
Activates GR → alters gene transcription → Decreases production of inflammatory cytokines/mediators
What is the target family for Glucorticoid?
Intracellular/ nuclear receptor
What is the generic name for Medrol?
methylprednisolone
What is the generic name for Plaquenil?
hydroxychloroquine
What is the generic name for Azulfidine EN-tabs?
Sulfasalazine
What is the generic name for Xeljanz?
tofacitinib
What is the generic name Olumiant?
Baricitinib
What is the generic name for Rinvoq?
Upadacitinib
What does the drug ending in ~citinib?
Janus Kinase Inhibitor (JAK) and DMARD
What is hydroxychloroquine used for?
Rheumatoid Arthritis (RA) and Lupus (SLE)
What is sulfasalazine used for?
Rheumatoid Arthritis (RA) and Ulcerative Colitis
What is tofacitinib used for?
Rheumatoid Arthritis (RA)
What is baricitinib used for?
Rheumatoid Arthritis (RA)
What is upadacitinib used for?
Rheumatoid Arthritis (RA)
What is methotrexate used for?
Rheumatoid Arthritis (RA) and Chemotherapy
What are the DMARDs?
Methotrexate, hydroxychloroquine, and sulfasalazine
What is the drug target for hydroxychloroquine?
Endosomal/lysosomal and TLR signaling
What is the drug target for sulfasalazine?
Multiple inflammatory pathways
What is the MOA for hydroxychloroquine?
Increase lysosomal pH → Affects antigen processing and TLR signaling → Decreases inflammatory cytokines
What is the drug target for methotrexate?
Dihydrofolate reductase (DHFR)
What is the MOA for sulfasalazine?
Prodrug → Decrease inflammatory mediator production
What is the MOA for methotrexate for RA?
Increases adenosine signaling → Inhibits inflammatory pathways → Decreases T-cell activity and inflammation
What are the big AE for methotrexate?
Hepatotoxicity and Bone marrow suppression
What are the big AE for hydroxychloroquine?
Retinal toxicity and GI upset
What are the big AE for sulfasalazine?
Bone marrow suppression, GI upset, and rash
What are the big AE for NSAIDs? (4)
GI irritation, ulcer, bleeding, kidney injury → Decreased renal function
What are the big AE for diclofenac?
Hepatotoxicity + cardiovascular risk
What are the big AE for celecoxib?
CV thrombotic risk but less GI toxicity
What are the AEs for glucorticoids?
Weight gain, fluid retention, hyperglycemia
Name the drugs from the drug family JAK inhibitors?
tofacitinib, baricitinib, and upadacitinib
What is the MOA for JAK inhibitors?
Cytokine binds receptor → JAK activation → STAT phosphorylation → STAT into nucleus → Decreases inflammation transcription
What are the major AE for glucocorticoids?
Respiratory infections, blood clots, MACE
What is aspirin drug class?
NSAID, salicylate anti-platelet
What type of inhibitor is aspirin?
Irreversible competitive inhibitor
What is aspirin intended use?
secondary prevention of cardiovascular/cerebrovascular events; pain; fever