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Flashcards covering key concepts from Anti-Inflammatory, Anti-Arthritic, and Related Agents, including NSAIDs, salicylates, acetaminophen, gold compounds, DMARDs, TNF blockers, and their indications, mechanisms, contraindications, and adverse effects.
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What are the four main actions of salicylates (aspirin) beyond anti-inflammatory effects?
Antipyretic, analgesic, and antiplatelet (inhibits platelet aggregation).
What is the typical dosing range for low-dose aspirin used for antiplatelet protection?
81 mg (often listed as 81 mg); sometimes 325 mg tab for other uses; baby aspirin is 81 mg but not for babies.
What are common contraindications for salicylates?
Allergy to salicylates, NSAIDs, or tartrazine (dye); recent surgery (1 week prior); pregnancy/lactation.
What are potential adverse effects and toxicity signs of salicylates?
GI effects and bleeding; salicylate toxicity can include dizziness, tinnitus, hearing loss, N/V, diarrhea, confusion, tachypnea, hemorrhage, pulmonary edema, seizures, coma.
What is COX-1’s role in the body?
Present in all tissues; protects the stomach lining; maintains Na and water balance in kidneys; involved in clotting; converts arachidonic acid to prostaglandins.
What is COX-2’s role in inflammation?
Active at trauma sites or sites of cellular injury; increases pain and inflammation via prostaglandins.
What is a key effect of COX-2 inhibitors compared to nonselective NSAIDs?
COX-2 inhibitors reduce inflammation with lower GI risk but have higher cardiovascular risk.
What is Celecoxib (Celebrex)?
A COX-2 selective NSAID used for conditions like osteoarthritis and RA; associated with cardiovascular risk; watch for GI side effects.
Name the major categories of NSAIDs.
Propionic acids, Acetic acids, Fenamates, Oxicam derivatives, COX-2 inhibitors (and nonselective NSAIDs).
What is the general mechanism of NSAIDs?
Block COX-1 and COX-2, reducing prostaglandin synthesis to relieve inflammation, pain, and fever.
What are the effects of COX-1 inhibition?
Gastric erosion/ulceration, bleeding tendencies, renal impairment; but protection against MI and stroke in some contexts.
What are the effects of COX-2 inhibition?
Reduction of inflammation, pain, and fever; potential renal impairment; possible increased risk of MI and stroke; may reduce colorectal cancer risk.
List examples of nonselective, semi-selective, and COX-2 selective NSAIDs.
Nonselective: ibuprofen, naproxen, indomethacin, ketorolac, diclofenac; Semi-selective: meloxicam, diclofenac, etodolac, piroxicam, nabumetone, sulindac; COX-2 selective: celecoxib.
What is a known risk associated with COX-2 selective NSAIDs?
Increased risk for cardiovascular events; relatively decreased GI side effects compared with nonselective NSAIDs.
Why was rofecoxib (Vioxx) removed from the market?
Because of increased cardiovascular risk leading to market withdrawal.
What are common NSAID contraindications?
Allergy to NSAIDs or salicylates; celecoxib allergy with sulfonamides; CV dysfunction or hypertension; peptic ulcers/GI bleed; pregnancy/lactation; renal or hepatic disease.
What is acetaminophen (Tylenol) not considered NSAID-wise, and what are its key cautions?
Not an NSAID; analgesic and antipyretic; hepatotoxic at high doses; max daily dose 4000 mg/day; antidote is acetylcysteine; caution with liver disease/alcohol use.
What are acetaminophen dosing guidelines and overdose concerns?
Typically 325–1000 mg every 4–6 hours; maximum 4000 mg/day; overdose is a major risk, especially in children; liver toxicity is the major concern.
What are acetaminophen contraindications and major adverse effects?
Contraindications: hepatic dysfunction, chronic alcoholism. Adverse effects: hepatotoxicity, headache, hemolytic anemia, renal dysfunction, rash, fever.
What are gold compounds used for in anti-arthritic therapy, and how do they work?
Chrysotherapy (gold salts: auranofin, aurolate); gold uptake by macrophages inhibits phagocytosis, reducing lysosomal enzyme release and tissue destruction.
What is a key caution about gold compounds as DMARDs?
Reserved for patients not responding to other treatments; not a repair agent but prevents progression; contraindicated in pregnancy/lactation and several organ dysfunctions.
What are DMARDs and their general purpose?
Disease-Modifying Anti-Rheumatic Drugs; slow or prevent joint damage; some classify gold as DMARD; includes TNF blockers and other agents; adverse effects can be severe.
What are TNF blockers and typical uses?
Adalimumab, certolizumab, etanercept, golimumab, infliximab; used for RA, polyarticular juvenile arthritis, psoriatic arthritis, plaque psoriasis, ankylosing spondylitis.
What are the major contraindications for TNF blockers?
Black box warning for serious infections and lymphoma/cancer risk; avoid in acute infection, cancer, sepsis, TB, hepatitis, myelosuppression, demyelinating disorders; pregnancy; live vaccines; animal product allergy.
What are other DMARDs and their roles?
Methotrexate, cyclophosphamide, abatacept, anakinra, IL-1 receptor antagonist; used alone or in combination; adverse effects can be serious; often used with TNF blockers.
What is the IL-1 receptor antagonist Anakinra’s mechanism?
Blocks IL-1, which is responsible for cartilage degradation in RA.
How do DMARDs compare to NSAIDs in terms of onset and disease progression?
DMARDs have a slow onset but can arrest disease progression and prevent deformities; used in chronic disease. NSAIDs have rapid onset for symptom relief but do not stop disease progression and are used in acute cases.