STEP1 Pharm Flashcards
Glucocorticoids inhibit
Phospholipase A2
Cortisone, hydrocortisone,
“-sone, -olone”
Glucocorticoids increase ____ which ____
IkB inhibits NF-kB (prevents increase COX-2)
Inhibit COX-2 only
celecoxib
Glucocorticoids increase IkB which inhibits NF-kB which increases COX-2
Inhibit COX1/2
Aspirin (irreversible)
NSAIDS
- Ibuprofen, naproxen, indomethacin
Inhibit 5-Lipoxygense
Zileuton
Inhibit Leukotriene receptor
Montelukast
Zafirlukast
Arachidonic pathway
Membrane phospholipids –> Arachidonic acid [Phosphlipase A2]
Arachidonic acid –> 5-HPETE [5-Lipoxygenase] –> Leukotrienes
Arachidonic acid –> cyclic enoperoxides [COX1/2] –> Prostacyclin (PGI2), Prostglandins (PGE), Thromboxane (TXA)
Acetaminophen MOA
reversibly inhibits cycloxygenase
Not anti-inflammatory
Aspirin MOA
Irreversibly inhibits cycloxygenase
Covalent acetylation
Tinnitus, Acute renal failure, GI bleeding
Celecoxib MOA
COX2 specific
Spares platelet fxn as TXA2 production is dependent on COX-1
Rheumatoid arthritis, osteoarthritis
Leflunomide MOA
Reversibly inhibits dihydroorotate dehydrogenase
Preventing pyrimidine synthesis
Suppress T cell proliferation
RA, psoriatic arthritis
Bisphosphonates
- Examples (4)
- MOA
- Clinical (5)
- AE (3)
Alendronate, ibandronate, risedronate, zoledronate
Pyrophosphate analog, bind hydroxyapatite in bone, inhibiting osteoclast activity
Osteoporosis, hypercalcemia, Paget dises of bone, metastatic bone disease, osteogenesis imperfecta
Epophagitis, osteonecrosis of jaw, atypical stress fracture
Teriparatide MOA
Recombinant PTH analog give SQ daily
Increase osteoblast activity
Osteoporosis
Increase risk of osteosarcoma
Gout drugs (7)
Chronic
1) Allopurinol
2) Febuxostat
3) Pegloticase
4) Probenecid
Acute
5) NSAIDs
6) Glucocorticoids
7) Colchicine
Purine excretion pathway (1,1, 3)
Purines –> hypoxanthine –> xanthine [Xanthine oxidase]
Xanthine –> Plasma uric acid [Xanthine oxidase]
Plasma uric acid –> Urate crystals in joints –> Gout
- -> Tubular reabsorption - -> Urine
Allopurinol MOA
Competitive inhibitor of xanthine oxidase
Decrease conversion to hypoxanthine and xanthine to urate
Febuxostat MOA
Inhibits xanthine oxidase
Inhibits xanthine oxidase
Allopurinol
Febuxostat
Recombinant uricase that catalyzes metabolism of uric acid to allantoin (more water soluble product)
Pegloticase
Probenecid MOA
inhibits reabsorption of uric acid in proximal convoluted tubule
Can precipitate uric acid calculi
Colchicine MOA
Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation
TNF-alpha inhibitors
Etanercept
Infliximab
Adalimumab
Certolizumab
Golimumab
Etanercept MOA
TNF-alpha inhibitor
Fusion protein (receptor for TNF-alpha + IgG Fc) produced by recombinant DNA
eTaNerCEPT interCEPTs TNf
Infliximab
Adalimumab
Certolizumab
Golimumab
TNF-alpha inhibitor
Anti-TNF-alpha monoclonal ab
-sartan
Angiotension receptor blockers
-stigmine
cholinesterase inhibitors
-curium/ -curonium
Non-depolarizing neuromuscular blocking drugs
-glitazone
thiazolidinediones
-dipine
dihydropyridine calcium channel blockers
-azepam
Benzodiazepine
-conazole
antifungal drugs
-caine
local anesthetics
-cycline
tetracycline antibiotics
-navir
protease inhibitors
cholinesterase inhibitors
-stigmine
local anesthetics
-caine
dihydropyridine calcium channel blockers
-dipine
protease inhibitors
-navir
Non-depolarizing neuromuscular blocking drugs
-curium/ -curonium
Angiotension receptor blockers
-sartan
antifungal drugs
-conazole
tetracycline antibiotics
-cycline
Benzodiazepine
-azepam