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Questions and Answers
What is the primary action of COX-2 selective inhibitors?
What is the primary action of COX-2 selective inhibitors?
Which of the following is an effect of aspirin due to its metabolism?
Which of the following is an effect of aspirin due to its metabolism?
What is a significant adverse effect of aspirin related to the gastrointestinal system?
What is a significant adverse effect of aspirin related to the gastrointestinal system?
Which therapeutic use of aspirin is indicated for cardiovascular issues?
Which therapeutic use of aspirin is indicated for cardiovascular issues?
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What is the effect of chronic use of aspirin on cancer incidence?
What is the effect of chronic use of aspirin on cancer incidence?
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Which cytokine is NOT mentioned as being involved in chronic synovial inflammation?
Which cytokine is NOT mentioned as being involved in chronic synovial inflammation?
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What is the primary goal of treatment in rheumatoid arthritis (RA)?
What is the primary goal of treatment in rheumatoid arthritis (RA)?
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Which class of medication does NOT provide disease-modifying effects but only partial pain relief in RA?
Which class of medication does NOT provide disease-modifying effects but only partial pain relief in RA?
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Which of the following is a common analgesic effect of NSAIDs?
Which of the following is a common analgesic effect of NSAIDs?
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What is the mechanism by which NSAIDs exert their antipyretic effects?
What is the mechanism by which NSAIDs exert their antipyretic effects?
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Which is NOT a classification of non-steroidal anti-inflammatory drugs (NSAIDs)?
Which is NOT a classification of non-steroidal anti-inflammatory drugs (NSAIDs)?
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Which type of pain is NSAIDs least effective at relieving?
Which type of pain is NSAIDs least effective at relieving?
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Which of the following symptoms is associated with chronic synovial inflammation?
Which of the following symptoms is associated with chronic synovial inflammation?
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What is a key characteristic of Reye's syndrome?
What is a key characteristic of Reye's syndrome?
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Which symptom is associated with mild salicylate toxication?
Which symptom is associated with mild salicylate toxication?
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What is a major adverse effect of long-term acetaminophen use?
What is a major adverse effect of long-term acetaminophen use?
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Which of the following medications is known for its potent anti-inflammatory effects?
Which of the following medications is known for its potent anti-inflammatory effects?
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What is an important consideration about the use of indomethacin?
What is an important consideration about the use of indomethacin?
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Which condition is ibuprofen primarily indicated for in chronic treatment?
Which condition is ibuprofen primarily indicated for in chronic treatment?
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What is a common adverse effect of long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen?
What is a common adverse effect of long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen?
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Which of the following is NOT considered an adverse effect of indomethacin?
Which of the following is NOT considered an adverse effect of indomethacin?
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Which of the following drugs is considered the 'gold standard' for Disease Modifying Anti-Rheumatic Drug (DMARD) therapy?
Which of the following drugs is considered the 'gold standard' for Disease Modifying Anti-Rheumatic Drug (DMARD) therapy?
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What is a common side effect of Methotrexate when taken within the recommended dosage range?
What is a common side effect of Methotrexate when taken within the recommended dosage range?
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Which of the following statements about Leflunomide is true?
Which of the following statements about Leflunomide is true?
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What potential effect does Hydroxychloroquine have that requires periodic evaluation?
What potential effect does Hydroxychloroquine have that requires periodic evaluation?
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Which statement accurately describes the elimination route and half-life of Leflunomide?
Which statement accurately describes the elimination route and half-life of Leflunomide?
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Study Notes
Rheumatoid Arthritis Management
- Rheumatoid arthritis (RA) is a chronic synovial inflammation.
- RA is an autoimmune disease.
- Cytokine networks (TNF-α, Interleukins - 1, 6, 17) are responsible for inflammation and joint destruction.
- Inflammation damages cartilage and bone.
Inflammation Drives Arthritis
- Inflammation leads to damage to cartilage and bone.
- Images show synovial membrane, cartilage, plasma cells, synovial villi, pannus, erosions, and neutrophils in affected joints.
Disability in Early RA
- Inflammation
- Stiffness
- Swelling
- Soreness
- Warmth
- Fatigue
Rheumatoid Arthritis - Joint Involvement
- Small joints of the hands and feet are affected first, followed by larger joints.
- Metatarsophalangeal joints are shown to be affected.
Treatment Goals in RA
- Reduce or eliminate pain.
- Protect articular structures.
- Control systemic complications.
- Prevent loss of joint function.
- Improve or maintain quality of life.
Treatment for RA
- Nonsteroidal anti-inflammatory drugs (NSAIDs).
- Glucocorticoids.
- Nonbiological disease-modifying antirheumatic drugs (DMARDs).
- Biological DMARDs.
NSAIDs
- Cyclo-oxygenase inhibitors.
- Do not slow disease progression.
- Provide partial relief from pain and stiffness.
- Types of NSAIDs: salicylates, aminophenol derivatives (acetaminophen), pyrazolones, other organic acids.
- Non-selective COX inhibitors: aspirin, diclofenac
- COX-2 selective inhibitors: celecoxib, etoricoxib, meloxicam
NSAID - 1. Antipyretic Effects
- Reduce body temperature in patients with fever.
- No effect on normal body temperature.
- Mechanism: Reduce prostaglandin biosynthesis by inhibiting cyclo-oxygenase.
NSAID - 2. Analgesic Effects
- Effective for mild to moderate dull pain.
- Little effect on colicky or sharp pain.
- Not a narcotic.
- Mechanism: Inhibit prostaglandin biosynthesis.
- Relief from common dull pains (headache, toothache, neuralgia, muscular pain, arthralgia, dysmenorrhea).
NSAID - 3. Anti-inflammatory Effects
- Relieve inflammatory symptoms (pain and swelling).
- Mechanism: Inhibition of prostaglandin synthesis.
Salicylates (e.g., Aspirin)
- Pharmacokinetics: Metabolized in the liver to salicylate and acetic acid by esterases.
- Half-life: 3.5 hours.
- Aspirin rapidly deacetylates to salicylate with anti-inflammatory, analgesic, and antipyretic effects.
- Irreversibly acetylates cyclooxygenase to inhibit enzyme activity.
- Antipyretic potency: Moderate.
- Analgesic effectiveness: Effective on mild to moderate pain.
- Anti-inflammatory effects: Treats rheumatoid and rheumatic arthritis.
- Antiplatelet effects: Inhibits platelet aggregation.
- Side Effects: Increased gastric acid secretion, causes epigastric distress, ulceration, hemorrhage; sodium and water retention causing edema and hyperkalemia;
- Therapeutic Uses: Hyperpyrexia (moderate dose); pain (middle dose); Rheumatic fever and rheumatoid arthritis (high dose); preventing thromboembolism, stroke, and myocardial infarction (small dose).
Adverse Effects of Aspirin
- Gastrointestinal reactions (epigastric distress, nausea, vomiting, gastric ulceration, bleeding).
- Hepatic damage (mild and reversible).
- Prolonged bleeding time.
- Hypersensitivity or allergy.
- Reye's syndrome (seen during viral infections; children are more susceptible)
Acetaminophen (Aminophenol Derivative)
- Inhibits prostaglandin synthesis within the central nervous system (CNS).
- Less effect on peripheral cyclooxygenase.
- Similar antipyretic/analgesic potency as aspirin.
- No anti-inflammatory activity.
- Use: Dull pain and hyperpyrexia, especially in children with viral infections.
- Side effects: Skin rash, drug fever, hypoglycemic coma, renal tubular necrosis, renal failure (long-term use), and acute hepatic necrosis (large doses).
Other Organic Acids (e.g., Indomethacin)
- Anti-inflammatory, analgesic, and antipyretic effects.
- More potent than aspirin as an anti-inflammatory agent.
- Inferior to salicylates at tolerated doses for rheumatoid arthritis.
- Use: Rheumatoid and rheumatic arthritis ; not routinely for analgesia or antipyresis because of toxicity.
- Adverse Effects: 35%-50% of patients report some adverse effects; most are dose-related and include gastrointestinal complaints, CNS effects (frontal headache, dizziness, vertigo, mental confusion), hematologic effects (neutropenia, thrombocytopenia, impaired platelet functions, and rare aplastic anemia),contraindicated in pregnancy/nursing mothers and patients with psychiatric disorders, epilepsy, parkinsonism, renal diseases, and peptic ulcers.
Ibuprofen
- Anti-inflammatory, analgesic, and antipyretic activity.
- Chronic treatment of rheumatoid and osteoarthritis.
- Less intense gastrointestinal effects than aspirin.
Glucocorticoids
- Potent anti-inflammatory drugs.
- Serious adverse effects with long-term use.
- Used to control the disease.
- Indications: As a bridge to effective DMARD therapy; or for systemic complications such as vasculitis.
- Routes: Oral, intra-articular, IM-depot.
DMARDs (Disease-Modifying Anti-Rheumatic Drugs)
- Reduce swelling and inflammation.
- Improve pain.
- Improve function.
- Reduce radiographic progression (erosions).
- Types: Synthetic (nonbiological) and Biological
Synthetic (Nonbiological) DMARDs
- Methotrexate
- Sulphasalazine
- Chloroquine
- Hydroxychloroquine
- Leflunomide
Methotrexate (MTX)
- Dihydrofolate reductase inhibitor, considered the "gold standard" DMARD.
- Dose: 7.5-30 mg weekly.
- Absorption: Variable
- Elimination: Primarily renal.
- Adverse Effects: Hepatotoxicity, bone marrow suppression, dyspepsia, oral ulcers, and pneumonitis.
Sulphasalazine
- Combination of sulphapyridine and 5-aminosalicylic acid.
- Removes toxic free radicals.
- Remission typically in 3-6 months.
- Elimination primarily hepatic.
- Side effects: Dyspepsia, rashes, and bone marrow suppression.
Chloroquine and Hydroxychloroquine
- Mechanism unknown, but anti-inflammatory and immunomodulatory.
- Useful for mild disease.
- Side effects: Irreversible retinal toxicity and corneal deposits.
- Ophthalmologic evaluation every 6 months is recommended.
Leflunomide
- Competitive inhibitor of dihydroorotate dehydrogenase.
- Reduces lymphocyte proliferation.
- Oral administration.
- Half-life: 4-28 days
- Elimination: Hepatic
- Action onset in one month.
- Avoid pregnancy for at least 2 years.
- Side effects: Hepatotoxicity, Bone marrow suppression, Diarrhea, Rashes
Biological DMARDs
- T-cell modulating drug (abatacept).
- B-cell cytotoxic agent (rituximab).
- Anti-IL-6 receptor antibody (tocilizumab).
- TNF-blocking agents (infliximab).
Combination Therapy
RA treatment is often more effective with the use of two or three DMARDs.
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Description
Test your knowledge on rheumatoid arthritis, including its causes, symptoms, and management strategies. This quiz covers the impact of inflammation on joint health and the treatment goals for RA patients. Understand how cytokine networks contribute to this autoimmune disease and assess your grasp of the disease's progression and treatment options.
