Anti-inflammatory Drugs 3 Flashcards by G V

Rheumatoid Arthritis (RA)

Buzzword: Extra-articular involvement
Joints, eyes, heart, lungs

F>M, all over the place, not localized
Symmetrical arthritis 
Synovium first 
Bones get thinner 
Rhematoid factor is + (though not primary diagnostic test)

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RA: Dx

Buzzword: rheumatoid nodules

1 - Early morning stiffness for 1 hour or longer
2 - Simultaneous swelling of 3 or more joints

Always order joint X-ray

Order ESR to look for inflammation, with RA = Elevated ESR

Wrist, PIP, NOT DIP
Elbow, ankle, knee

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RA: Rx

First: NSAIDs or COX2 Inhibitors

If this doesn’t work within 3 months , go to Disease-Modifying Antirheumatic Drugs (DMARDS)

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RA: DMARDs definition

Disease-Modifying Antirheumatic Drugs

Used when NSAIDs or COX2 inhibitors don’t work

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RA: DMARDS - Methotrexate

MOA: Inhibits Dihydrofolate Reductase; cytotoxic to lymphocytes

Adverse effects: Bone marrow suppression, hair loss, mucositis, worsens nodules

*also a cancer drug for chemotherapy

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RA: DMARDS - Hydroxychloroquine

MOA: Stabilizes lysosomes and decreases chemotaxis

Adverse effects: GI distress and visual dysfunction (Cinchonism), and hemolysis from G6PD deficiency)

Also, increased LFTs: increased AST and ALT elevations.

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RA: DMARDS - Sulfasalazine

MOA: ASA inhibits COX2
Sulfapyridine: decrease B cell functions

Adverse: ASA (GI distress), Sulfapyridine: rash, hemolysis, SLE like syndrome

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RA: DMARDS - Corticosteroids

For flaring

MOA: Decreases LTs, IL-2, and PAF (platelet activating factor)

Adverse effects: ACTH depression, susceptibility to infections

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RA: DMARDS - Gold Salts

MOA: Decrease lysosomal and macrophages functions

Adverse effects: stomatitis, rash, bone marrow depression, proteinuria, and nephrotic syndrome

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RA: DMARDS - D-Penicillamine

Suppress T-cell and decreased rheumatoid factor

Adverse effects: aplastic anemia, myasthenia gravis

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RA: DMARDS - Cyclophosphamide

Alkylating agents used in severe cases

Adverse: hemorrhagic cystitis

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RA: DMARDS - Azathioprine

Immunosuppressive in autoimmune disease
MOA: Inhibits purine synthesis

Side effects: bone marrow suppression

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RA: New DMARDs (Biologics) - Infliximab

Monoclonal antibody
MOA: Decreases TNF

Adverse effects: Infusion reactions, infections

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RA: New DMARDs (Biologics) - Etanercept (Enbrel)

A recombinant of TNF receptor
BINDS to TNF (not inhibit; binding decreases effects)

Adverse effect: Hypersensitivity, infections

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RA: New DMARDs (Biologics) - Leflunomide

MOA: Inhibits pyrimidine synthesis, inhibits dihydro-acid dehydrogenase

Adverse effects: apopecia, rash, hepatotoxicity

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RA: New DMARDs (Biologics) - Anakinra

MOA: IL-1 receptor antagonist

Adverse effects: Reaction at injection site, infection

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RA: New DMARDs (Biologics) - Adalimumab (Humira)

Recombinant Monoclonal antibody

BINDS TO TNF

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RA: New DMARDs (Biologics) - Abatacept

Co-stimulation modulator
MOA: Inhibits T-cell activation by binding to cell surface markers (proteins) on leukocytes

Rx of RA

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RA: So, what are the drugs that decrease TNF (not inhibit, but binds and decreases)?

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Infliximab
Etanercept
Adalimumab

Osteoarthritis: Defined

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Buzz word: Increase with age

M=F
Most common form 
New bone formation = osteophytes
Weight bearing joints 
*Stiffness less than 30 minutes in the morning 
Primary most common

Osteoarthritis: Secondary Osteoarthritis

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Anything that affects cartilages (joint deformity)

Osteoarthritis: Dx, Buzzword, Rx

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Dx: X-ray

Buzz word: Unequal loss of joint space

Rx: Exercise, weight loss,

Rx Meds: Tylenol, Ibuprofen, COX-2 inhibitors (celecoxib)

*Osteomyelitis: Defined

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*NOT AN INFLAMMATORY DISEASE

Buzzword: Bacterial infection from Staph Aureus (gram positive –> highly resistant to antibiotics)

Any part of the bone: marrow, cortex, and periosteum

Children: Acute
Adult: Chronic

Do blood cultures detect *Osteomyelitis?

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No, because it doesn’t tell you if bone is involved

Osteomyelitis: 1st Dx Test

1st: X-ray

Osteomyelitis: If X-ray is (+)

Order biopsy Rx IV antibiotics

Osteomyelitis: If X-ray is (-)

Bone scan and If (+) --> biopsy --> Rx and IV antibiotics If (-) --> Not osteomyelitis --> Rx: could be ulcer

Osteomyelitis: Why is dx of bone involvement necessary before rx? Also, antibiotics for Staph aureus

You don't wanna put someone in IV antibiotics for 6 weeks without a diagnosis of osteomyelitis For Staph Aureus: Ox/Clox/Diclox and Naf (IV)

Fibromyalgia: Defined

Buzzword: Labs are normal Short sleeve shirt part --> shoulder, trapezius, and hip girdle Widespread aching and stiffness for longer than 3 months Look for tender points

Fibromyalgia: Rx

Analgesics and antidepressants Cymbalta (duloxetine) --> CNS depressant Lyrica (Pregbalin, more potent than gabapentin) Gabapentin

Polymyalgia Rheumatica: Def, Lab, and Buzzword

Elderly with same presentation as fibromyalgia Lab: Increased ESR Buzzword: Giant Temporal Arteritis (Biopsy)

Polymyalgia Rheumatica: *Tx

Give steroids 15 mg/day and taper *If they come back with severe headache, increase steroids to 40 mg/day. If not, blindness has occurred

Gout:

Crystal induced arthritis Male 10:1 Buzz word: Big toe and elevated serum uric acid Why: Increased UA production: Idiopathic Decreased UA excretion: (renal)

Gout: Lab

Negative birefringence with polarized light If positive: pseudo-gut

Gout: Drugs

1st: NAIDS | Then, Indomethacin, Naproxen, and sulindac

Gout: Acute Gouty Attack Buzzword and MOA

Colchicine Binds to tubulin --> Decreases microtubular polymerization Decreases LTB4 formation (inhibits leukocyte and granulocyte migration)

Acute Gouty Attack: Colchicine Adverse effects

Acute: Diarrhea and GI pain Long term: Mylosuppression, peripheral neuropathy, hematuria and alopecia

Chronic Gouty Arthritis: Goal

To decrease uric acid

Chronic Gouty Arthritis Drugs: Allopurinol

Allopurinol MOA: Inhibits Xanthine Oxidase Suicide substrate: own product inhibiting the enzyme (decreases purine metabolism, which decreases uric acid)

Chronic Gouty Arthritis Drugs: Allopurinol Buzz word and Adverse Effects

Inhibits 6-mercaptopurine metabolism If given with cancer drug, have to lower the dose of cancer drug, else severe liver toxicity Peripheral neuropathy, stone formation, rash, vasculitis

Chronic Gouty Arthritis Drugs: Probenicid MOA and Adverse Effects

MOA: Inhibits proximal tubular reabsorption of urate. Inhibits secretion of acidic drugs: Penicillins Adverse: Higher excreter of urate --> urate crystals in the kidney

Chronic Gouty Arthritis Drugs: Sulfinpyrazone

MOA: Similar to Probenicid Activity is GFR dependent (not good below 30 ml/min) Inhibits platelet aggregation Adverse effects: Gi Distress, rash, nephritic syndrome

Gout New Drug:

Febuxistat

Corticosteroids: MOA at cellular level (4)

1. Inhibit the release of inflammatory mediators 2. Decrease migration of leukocytes 3. Decrease capillary permeability 4. Decrease phagocytosis

Corticosteroids: MOA at the biochemical level (4)

1. Inhibits PLA2 2. Block COX2 expression 3. Decrease platelet activating factor 4. Decrease interleukins (IL-2)

Corticosteroids: Adverse reactions (8)

1. Electrolyte imbalance: edema, HTN 2. Increase infection and decrease wound healing 3. Hyperglycemia due to gluconeogenesis 4. Osteoporosis 5. ACTH suppression: cortical atrophy 6. Iatrogenic Cushing's syndrome 7. Increase glaucoma and cataracts 8. Steroid rage (mental dysfunction)

Anti-inflammatory Drugs 3 Flashcards

(46 cards)