Anti-Inflammatory Drugs Flashcards
Ketorlac
NSAID for IM and IV
Indomethacin
used for patent ductus arteriosus
What is the mechanism of antipyretic NSAID?
dec. PGE2 and inh. IL-1 activity
What is the mechanism of analgesic NSAID?
PGE2 and INF mechanism
What is general pharmacokinetics of NSAIDs?
Weak acids, well absorbed
cyp3A or cyp2C
renal excretion and some biliary excretion that can cause GI damage
Used for acute inflammation and Sx Tx of chronic inflammation
What are general contraindications of NSAIDs?
Allergy
Viral fever in kids (Reye’s Syndrome)»_space; fatal, fatty LV, encephalopathy, hypoglycemia. No jaundice
3rd trimester»_space; could close ductus
What are drug interactions with NSAIDs?
Anti-virals + NSAIDs >> nephrotoxicity >> separate use by 7 days Inhibits Li excretion Additive with opiods GI complications Caffeine is additive
What is Acetominophen?
Analgesic and antipyretic
Destroyed in INF’ed tissue
Inh Cox-3 (a Cox-1 variant in the CNS)»_space; works for H/A
Few side effects in GI, KD, CV
What are chronic inflammatory mediators?
IL-1, 2, 3, GM-CSF, TNF-alpha, IFN, PDGF
What are the 3 categories of anti-chronic inflammation?
Ablation with DMARDs
inh. cytokine and immune cells with GC
Anti-TNF»_space; inh. cytokines
What are Three DMARDs?
MTX
Leflunomide
Sulfasalazine
What is MTX?
What are side effects?
Contraindication?
What is this the first line med for?
DMARD
inh folate metabolism (non toxic at low dose)
GI distress, oral ulcers, hepatotoxicity
Contraindicated: prego, LV/KD problems, DM, obesity
First line med for RA, better used in Crohn’s disease, but also in UC
What is Leflunomide?
S/E?
Contraindications?
Inh pyrimdine synthesis
inh. COX-2 expression
GI distress, oral ulcers, hepatotoxicity
Contraindicated: prego, LV/KD problems, DM, obesity
As effective as MTX for RA but more hepatotoxicity
What is Sulfasalazine?
Combo of Mesalamine and Sulfapyridine
Mes»_space; inh. COX and LOX in gastric mucosa
Sul»_space; free O2 scavenger effective in joints
Not absorbed in ST or SI»_space; used for IBD
More toxic than MTX and Leflunomide
What is the anti-inflammatory mechanisms Glucocorticoids?
inh. INF, edema, scar tissue, and immune response
Lipocortins, PLA2 and lipo-oxygenase inhibitory proteins
Essentiall prevent INF from causing immune response
What is the immunosuppression mechanisms Glucocorticoids?
inh. lymphoid and myeloid lineages
What are S/E of glucocorticoids?
Cushingoid syndrome and other endocrine
Peptic ulcers, hypomania, acute psychosis, depression, fluid retention
What are contraindications of GC?
Peptic ulcer, heart dz, HTN, infexs, DM, psychoses,
hepatic dysfux
What are three Anti-TNF agents?
Infliximab (remicade)
Adalimumab (humira)
Etanercept
What are Infliximab (remicade) and Adalimumab (humira)?
What is different about them?
Both Anti-TNF-alpha mAb
Both use murine Ab
Humira is more human, so has less side effects
What is the significance of Etanercept?
Anti-TNF-alpha mAb
more favored for PAIN
Very expensive
What are indications for
Infliximab (remicade)
Adalimumab (humira)
Etanercept
arthritis (RA, PsA, AS, Juv RA), psoriasis
Infliximab is also indicated for Behcet’s syndrome and Crohn’s
What are contraindications of
Infliximab (remicade)
Adalimumab (humira)
Etanercept
breast feeding, DM, elderly
may cause infections and cancer due to inh. immunity
What are indole and indene acetic acids and indomethacin used for in term 4?
RA, OA, PDA
