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Questions and Answers
Prostaglandins play a role in maintaining temperature homeostasis.
Prostaglandins play a role in maintaining temperature homeostasis.
True (A)
PGD2 is responsible for the anti-inflammatory effects of some prostaglandins such as PGE1.
PGD2 is responsible for the anti-inflammatory effects of some prostaglandins such as PGE1.
False (B)
PGI2 promotes platelet aggregation.
PGI2 promotes platelet aggregation.
False (B)
PGE2 causes vasodilation and bronchoconstriction.
PGE2 causes vasodilation and bronchoconstriction.
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TXA2 causes vasodilation.
TXA2 causes vasodilation.
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Acidic NSAIDs tend to accumulate in inflamed synovial tissues.
Acidic NSAIDs tend to accumulate in inflamed synovial tissues.
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NSAIDs with lower pKa values tend to have longer half-lives.
NSAIDs with lower pKa values tend to have longer half-lives.
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COX-1 is primarily induced by pro-inflammatory stimuli like LPS, TNFα, IL-2, and IFNγ.
COX-1 is primarily induced by pro-inflammatory stimuli like LPS, TNFα, IL-2, and IFNγ.
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COX-2 is ubiquitously expressed in the body.
COX-2 is ubiquitously expressed in the body.
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Aspirin has a short half-life, which is known to be less than 6 hours.
Aspirin has a short half-life, which is known to be less than 6 hours.
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Naproxen has a short half-life, which is within 6 hours.
Naproxen has a short half-life, which is within 6 hours.
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COX-1 produces PGE2 in vascular endothelium.
COX-1 produces PGE2 in vascular endothelium.
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NSAIDs can increase the risk of bleeding when taken with anticoagulants like warfarin.
NSAIDs can increase the risk of bleeding when taken with anticoagulants like warfarin.
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NSAIDs enhance the effects of anti-hypertensive medications.
NSAIDs enhance the effects of anti-hypertensive medications.
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NSAIDs reduce gastric acid production and provide protection.
NSAIDs reduce gastric acid production and provide protection.
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The risk of GI bleeding is decreased when taking NSAIDs, due to their protective effect on the stomach.
The risk of GI bleeding is decreased when taking NSAIDs, due to their protective effect on the stomach.
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Aspirin is used for platelet inhibition to prevent stroke and myocardial infarction.
Aspirin is used for platelet inhibition to prevent stroke and myocardial infarction.
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Metoclopramide and caffeine decrease the absorption of aspirin.
Metoclopramide and caffeine decrease the absorption of aspirin.
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Sulfasalazine is recommended for the treatment of severe ulcerative colitis.
Sulfasalazine is recommended for the treatment of severe ulcerative colitis.
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Oligospermia, which is a possible side effect of sulfasalazine, is a decrease in sperm count.
Oligospermia, which is a possible side effect of sulfasalazine, is a decrease in sperm count.
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Ibuprofen is contraindicated in patients with a history of gastrointestinal disease.
Ibuprofen is contraindicated in patients with a history of gastrointestinal disease.
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Naproxen is in the proprionic acid class of NSAIDs.
Naproxen is in the proprionic acid class of NSAIDs.
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Oxaprozin demonstrates the least selectivity for COX-2 compared to other NSAIDs.
Oxaprozin demonstrates the least selectivity for COX-2 compared to other NSAIDs.
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Aspirin is indicated for treatment of mild to moderate ulcerative colitis.
Aspirin is indicated for treatment of mild to moderate ulcerative colitis.
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Sulindac is safe to use in patients with renal disease.
Sulindac is safe to use in patients with renal disease.
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Concomitant use of ketorolac and probenecid is recommended.
Concomitant use of ketorolac and probenecid is recommended.
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Aspirin can be used safely with other NSAIDs without concern of interaction.
Aspirin can be used safely with other NSAIDs without concern of interaction.
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Ketorolac is an acetic acid derivative.
Ketorolac is an acetic acid derivative.
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Patients with rheumatoid arthritis are at a lower risk of adverse corneal events after ocular surgeries.
Patients with rheumatoid arthritis are at a lower risk of adverse corneal events after ocular surgeries.
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Elevated liver function tests can occur with the absorption of some NSAIDs.
Elevated liver function tests can occur with the absorption of some NSAIDs.
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Short-term management of acute pain can involve NSAIDs for less than 5 days.
Short-term management of acute pain can involve NSAIDs for less than 5 days.
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Patients with complications like diabetes are not at risk for corneal adverse events.
Patients with complications like diabetes are not at risk for corneal adverse events.
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Acetaminophen is primarily used for analgesia and anti-pyretic purposes.
Acetaminophen is primarily used for analgesia and anti-pyretic purposes.
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The antidote for acetaminophen overdose is ibuprofen.
The antidote for acetaminophen overdose is ibuprofen.
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Coxibs, including Celecoxib and Valdecoxib, are noted for causing severe hepatic reactions.
Coxibs, including Celecoxib and Valdecoxib, are noted for causing severe hepatic reactions.
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Rofecoxib is indicated for treating acute pain in children.
Rofecoxib is indicated for treating acute pain in children.
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Valdecoxib may increase the efficacy of ACE inhibitors.
Valdecoxib may increase the efficacy of ACE inhibitors.
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Patients with renal disease should generally avoid taking Coxibs.
Patients with renal disease should generally avoid taking Coxibs.
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Dyspepsia is a common side effect of Coxibs.
Dyspepsia is a common side effect of Coxibs.
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Hypersensitivity reactions may occur with the use of Coxibs in patients who have allergies to NSAIDs.
Hypersensitivity reactions may occur with the use of Coxibs in patients who have allergies to NSAIDs.
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Etanercept may be administered with or without methotrexate.
Etanercept may be administered with or without methotrexate.
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Anakinra is primarily used to treat psoriatic arthritis.
Anakinra is primarily used to treat psoriatic arthritis.
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Adalimumab has been shown to increase the risk of infections and lymphomas.
Adalimumab has been shown to increase the risk of infections and lymphomas.
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Infliximab should be administered without methotrexate.
Infliximab should be administered without methotrexate.
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Cytokine antagonists can lead to rare conditions such as pancytopenia.
Cytokine antagonists can lead to rare conditions such as pancytopenia.
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Fatigue and nausea are common side effects of all cytokine antagonists.
Fatigue and nausea are common side effects of all cytokine antagonists.
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Patients using Infliximab are at risk of congestive heart failure.
Patients using Infliximab are at risk of congestive heart failure.
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The administration of cytokine antagonists guarantees reduced symptoms in rheumatoid arthritis.
The administration of cytokine antagonists guarantees reduced symptoms in rheumatoid arthritis.
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Study Notes
Anti-Inflammatory Drugs
- Inflammation is partly mediated by prostaglandins produced by the cyclooxygenase pathway.
- NSAIDs inhibit this pathway and act as anti-inflammatory, antipyretic, and analgesic agents.
- NSAIDs are generally non-specific, causing numerous side effects. More specific treatments like COX-2 inhibitors and anti-cytokine agents are being investigated.
Prostaglandins
- All body cells can synthesize prostaglandins.
- Inflammatory stimuli cause arachidonic acid (AA) release from plasma phospholipids by phospholipase A2.
- Cyclooxygenase metabolizes AA into PGH2, which then forms PGD2, PGE2, PGF2α, PGI2, or TXA2 via specific enzymes.
- Prostaglandins have physiologic and pathologic functions:
- Physiologic: temperature regulation, bronchial tone, cytoprotection (gastric and renal mucosa), intestinal motility, myometrial tone, semen viability (some, like PGE1, have anti-inflammatory effects), renin secretion.
- Pathologic: fever, asthma, ulcers, diarrhea, dysmenorrhea, inflammation, bone erosion, and pain (possibly from PGD2).
- Specific inflammatory functions: PGI2 inhibits platelet aggregation, causes vasodilation, and increases vascular permeability (edema); PGE2 causes pain, hyperalgesia, and heat; increases vasodilation and bronchoconstriction; acts synergistically with other inflammatory mediators (like histamine, complement, and LTB4); and TXA2 promotes platelet aggregation, vasoconstriction, and bronchoconstriction.
Cyclooxygenase (COX) Enzymes
- Two forms of COX exist: COX-1 and COX-2.
- Though they catalyze the same reaction, their expression, functions, and properties differ significantly.
- COX-1 is constitutive and found ubiquitously; COX-2 is inducible and found at inflammatory sites.
- COX-1 plays a 'housekeeping' role, maintaining blood flow, vascular homeostasis, renal function, intestinal health, and platelet function.
- COX-2's pro-inflammatory actions include pain, fever, leukocyte proliferation, and inflammation (in macrophages and rheumatoid arthritis joints). It also has mitogenic functions involved in renal genesis and reproduction.
NSAIDs
- Most NSAIDs are polycyclic carboxylic acid derivatives.
- Different types include salicylates (aspirin), acetic acids (indomethacin), propionic acids (ibuprofen), fenamic acids (meclofenamate), enolic acids (piroxicam), and ketones (nabumetone).
- NSAIDs block arachidonic acid access and inhibit COX enzyme pathways for reducing inflammation.
- General effects: analgesia, antipyrexia, anti-inflammation, and anti-thrombotic. COX-2 selective inhibitors avoid effects on COX-1 (which impacts the GI tract and platelets).
NSAID Toxicity
- NSAIDs can affect the gastrointestinal, central nervous system, hepatic, renal, hematologic, and skin systems.
- GI toxicity: NSAIDs can cause gastric irritation, exacerbate peptic ulcers, induce mucosal lesions, suppress gastric acid secretion, maintain gastric mucosal barrier, etc. Specific risk factors include high doses, older age, and concurrent steroid use.
COX-2 Selective Inhibitors
- Coxibs (e.g., celecoxib, valdecoxib) preferentially block COX-2.
- Potential benefits of reduced gastrointestinal side effects.
- Concerns about cardiovascular risk associated with some COX-2 selective inhibitors, particularly rofecoxib (removed from market).
Glucocorticoids
- Glucocorticoids are 21-carbon steroid molecules with various physiologic and metabolic effects. Cortisol (hydrocortisone) is a primary glucocorticoid.
- Activity depends on a hydroxyl group at carbon 11. Glucocorticoid preparations for topical use are already hydroxylated at C-11, bypassing hepatic transformation.
- Varying potency and duration of action are clinically important factors in their use.
Cytokine Antagonists
- Cytokine antagonists (e.g., etanercept, adalimumab, infliximab, anakinra) modulate immune responses and target specific cytokines.
- Used for conditions like rheumatoid arthritis, psoriatic arthritis, and Crohn's disease.
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Description
This quiz explores the mechanisms and effects of anti-inflammatory drugs, particularly NSAIDs and COX-2 inhibitors, on prostaglandin synthesis. It discusses the role of prostaglandins in both physiological and pathological conditions, as well as the pathways involved in inflammation. Test your knowledge on these critical aspects of pharmacology and biochemistry.
