NSAIDs, RA & OA Management Flashcards
In order to be considered an NSAID, a drug must be able to…
Decrease inflammation
Relieve mild-moderate pain
Reduce fever
Decrease risk of blood clotting (inhibit platelet aggregation)
Is acetaminophen an NSAID?
NO! It does NOT have anti-inflammatory properties or anticoagulant properties
How do NSAIDs work?
Interfere with synthesis of prostaglandins (increase in the presence of inflammation, pain & fever) by inhibiting the COX enzyme
COX-1 vs COX-2
Cox-1 produces prostaglandins that regulate normal cell activity and maintain cell homeostasis. Beneficial prostaglandin creation
Cox-2 enzyme is produced in injured cells and create harmful prostaglandins
Inhibiting which COX enzyme is the best clinically?
COX-2 - Inhibit COX-2 to decrease pain/inflammation and spare COX-1
Are Aspirin & traditional NSAIDs selective?
No, they are not selective in COX inhibition
Benefits of Aspirin (Acetylsalicyclic acid)
Manage pain in musculoskeletal and joint disorders, s/p surgery pain, prevention of clots, treatment of adult fever, and some cancer prevention (prevent tumor growth)
Side Effects of NSAIDs
Gastrointestinal damage (hemorrhage, ulceration)
Cardiovascular (decreased platelets, increased BP)
Impaired hepatic & kidney function
Aspirin intoxication/poisoning
Reye Syndrome
Inhibition of bone healing
What population will Aspirin cause kidney impairments in?
Those with already impaired kidney function, diabetes mellitus, heart failure or those with decreased body water
Signs of Aspirin Intoxication/Poisoning
Headache, tinnitus, difficulty hearing, confusion, GI distress, and metabolic acidosis
What is Reye syndrome?
Occurs in children/teenagers that take aspirin. Signs include high fever, vomiting, liver dysfunction, increased unresponsiveness, delirium, coma and even death
COX-2 Selective Drugs
Celebrex - Less gastric irritation but increased respiratory tract infections and risk of heart attack/stroke
What is Acetaminophen?
Tylenol
Equal to NSAIDs in terms of pain relief/fever reduction in children/teens
No upper GI irritation
Used for treating non-inflammatory conditions with mild-moderate pain
Used in early stages of OA
Mechanism of Action - Acetaminophen
Inhibit COX enzyme
What is the toxic level of Acetaminophen for the liver?
15 g - Can be fatal
What are the two main goals of RA treatment?
Decrease joint inflammation & stop the progression of the disease
What are the three categories of drugs for RA?
- NSAIDs
- Glucocorticoids
- Disease-Modifying Antirheumatic Drugs (DMARDs)
Glucocorticoids (Corticosteroids)
Provide symptomatic relief by decreasing joint inflammation and pain. Effective anti-inflammatory agents. Early use can decrease joint erosion and slow progression of RA
Example: Prednisone
How are Glucocorticoids administered?
2-3 injections per joint per year
Used for acute flare-ups or exacerbations
Mechanism of Action - Glucocorticoids
Bind to receptor in cytoplasm of certain cells and form glucocorticoid-receptor complex. This complex moves and binds to genes that regulate inflammatory process - Inhibits production of inflammatory substances
Adverse effects of Glucocorticoids
Osteoporosis
Muscle wasting/weakness
HTN
Aggravation of DM
Glaucoma
Cataracts
Increased risk of infection
DMARDs
Slow or halt the progression of RA in early stages
Promote remission before joints become too damaged
Types of DMARDs (5)
- Antimalarials
- Gold Compounds
- Nonbiological DMARDs
- Biological DMARDs (TNF)
- Others
Antimalarials
Non-biological traditional DMARD
Affect immune cell responses
Very safe compared to other DMARDs - Can cause irreversible retinal damage, HA, GI distress though
Example: Hydroxychloroquine
Gold Therapy
Cease progression of RA disease by binding to enzymes in immune cells that suppress ability for autoimmune responses
Side effects: GI distress, oral mucosa irritation, rashes/itchy skin, proteinuria, conjunctivitis, thrombocytopenia, leukopenia
What is Methotrexate used for?
Treatment of cancer and RA
Rapid onset (2-3 weeks)
Side effects: TOXICITY, Gi issues, pulmonary problems, hematological disorders, liver dysfunction, hair loss
Tumor Necrosis Factor Inhibitors
Inhibits the erosion and inflammation of joints
Good for initial stages of RA
Side effects: URI, sepsis, malignancy, liver disease, heart failure, lupus-like disease, demyelinating diseases
TNF inhibitors are contraindicated in…
People who have infections
Which drug is considered the cornerstone drug for RA?
Methotrexate - Other DMARDs are added to this (TNF-a) for optimal benefits
Relationship between RA and Diet
Good - Diets high in fish oil & omega-3 fatty acids
Bad - Diets high in meat & protein
What should the primary focus for OA be?
Nonpharmacological intervention - PT, weight loss, joint replacement
What is the goal of OA drug treatment?
Manage pain & maintain active lifestyle
Types of OA medications
Acetaminophen, NSAIDs, Disease-modifying OA drugs (DMOADs)
What is the first drug of choice for OA?
Acetaminophen
Example of Viscosupplementation for OA
Hyaluronan (Hyaluronic Acid) - 3-5 injections that last 6 mo -1 year
Restore lubricating properties of synovial fluid and limit joint destruction. Improves pain and function as well
Dietary supplements for OA treatment
Glucosamine & Chondroitin Sulfate (supplements)
Protect articular cartilage or reverse joint deterioration
Key ingredients for the production of synovial fluid/cartilage
Rehab Implications for RA
Monitor for skin breakdown and damaged bone, tendon, or muscle - Focus on ROM and strengthening to prevent injury/fractures
Infection control is essential with DMARDs
