Anti-Inflammatories Flashcards
Cortisol MOA
Redistribution of neutrophils, lymphocytes monocytes, eosinophil and basophils.
macrophage release of TNFα, IL1, metalloproteinase and plasminogen factor
synthesis of prostaglandins, leukotrienes, thromboxane and histamines from mast cells
COX2 expression
drug with the highest anti-inflammatory activity
Dexmethasone
Contraindications of anti-inflammatory use
Peptic ulcers, hypertension, osteoporosis and heart failure
Adverse effects of anti-inflammatory drugs
Na+ retention and hypertension Hypokalemia Osteoporosis Infections Hyperglycemia, glycosuria, and peptic ulcers
MOA of NSAIDs: Inhibit _____ and _____ , long-term use → many deleterious effects: ___bleeding time, dyspepsia, ________damage and hemorrhage, gastric mucosal erosion, frank ulceration and gastric mucosal necrosis.
COX1, COX2, increased, subepithelial
NSAIDs: ____ blood vessels’ sensitivity to bradykinin and histamine, ___ GFR and may lead to kidney failure
Decreased, decreased
Aspirine MOA, what other three drugs do this
Decreased NADPH oxidase which affects neutrophils oxidative burst, (indomethacin, piroxicam & ibuprofen)
Adverse effects of aspirine
airway hyperactivity, Reye syndrome
long T½ is 20 times more potent than aspirin, directly inhibits leukocyte function and cause less severe adverse effects that aspirin, and is a derivative of _____
Naproxen, Propionic acid, (same as ibuprofen)
Used for anti-inflammation as well as closure of ducts arteriosus
Indomethacin
decreases intracellular concentration of arachidonic acid, used widely in renal stone-associated pain, derivative of_____
diclofenac, acetic acid
, strong analgesic properties, used in post surgical patients, derivative of____
ketorolac, acetic acid
Fenamate derivatives used for primary dysmenorhea, and arthritis
Mefenemate, meclofenamate
A pro-drug
More selective for COX2, less GI disturbances
Nabumetone
As efficacious as aspirin, naproxen and ibuprofen against arthritis and is better tolerated
Piroxicam
devoid of anti inflammatory activity but has a lower toxicity profile, maybe suitable for______, side effects include
Acetaminophen, children, kidney and liver toxicities
More expensive than aspirin or traditional NSAIDs
Similar efficacy in treating osteoarthritis, rheumatoid arthritis, 1 dysmenorrhea but cause less GI side effects than other NSAIDs
Also approved for familial adenomatous polyposis
Higher risk of cardiovascular toxicity (heart attack and stroke) than other NSAIDs
celecoxib
Adalimumab, Etanercept and Infliximab
suppress IL-1, IL-6
risk of lymphoma with use
Anti-TNF-alpha
blocks T-cell activation with subsequent decrease in TNF. It is approved for use in patient with severe resistant rheumatoid arthritis.
abatacept
is a recombinant human anti-CD11a mononclonal antibody approved for adults with sever psoriasis
efalizumab
blocks interaction between IgE and the high affinity Fc receptor. Approved for resistant allergic asthma in adults and adolescents
omilzumab
PLA is stimulated by
TNFalpa and gamma interferon, macrophages, colony stimulating factor, granulocytes