Reumatologic agents Flashcards
1
Q
Systemic corticosteroids
- Prednisone (Deltasone)
- Methylprednisolone
- Prednisolone (Pred Forte)
A
- Anti-inflammatory agents
- MOA: inhibit cytokine production, adhesion, protein activation, inflammatory cell migration and activation (immunosuppressant)
- Asthma indications: Short term (gain control of inadequately controlled asthma); Long term (prevention in severe persistent asthma)
- SHORT TERM ADR: Hyperglycemia, increased appetite, fluid retention, wt gain, mood alteration, HTN, peptic ulcer
- LONG TERM ADR: adrenal axis suppression (HPA), growth suppression, thinning of skin, osteoporosis, HTN, DM, cushing’s syndrome, impaired immune fxn
2
Q
DMARDs
A
DMRDs: Methotrexate; Leflunomide; Hydroxychloroquine; Sulfasalazine; Minocycline
Biologics
- Anti TNF: Adlimumab, certolizumab pegol, etanercept, infliximab, golimumab
- Non TNF: Abatacept, rituximab, tocilizumab
3
Q
Methotrexate (Rheumatrex, Trexall)
- First line for RA (Relieves inflammation, swelling, pain; Prevents dz progression and joint destruction)
A
- Folate analogs; Inhibits Dihydrofolate reductase (DHFR) (DHFR rduces dihydrofolates to tetrahydrofolates for incorporation into purines– adenine and guanine); Interferes w/ DNA synthesis, repair and replication; Greatest response in actively proliferating cells (bone marrow, fetus, oral mucosa, urinary bladder, malignancy)
- MOA in RA not well known
- INDICATIONS: RA, psoriasis, some cancers
- ADR: N/V/D, hair loss, skin rash, abnormal liver enzymes, fatigue, mouth sores, low blood counts (increased risk of infection)
- CONTRAINDICATIONS: PREGNANCY/LACTATION (Male and female); liver dz/ alcoholism; blood dyscrasias
- Hepatic metabolism
- Renal elimination
4
Q
Leflunomide (Arava)
- Reduce s/sx of RA
- Block structural damage
- Improve physical fxn
A
- Pyrimidine synthesis inhibitor (blocks enzyme)
- Anti-inflammatory effects
- Prodrug
- ADR: DIARRHEA/N/stomach pain, indigestion, rash, hair loss, abnormal LFTs/decreased blood cell or platelet counts; rare cough/SOB/lung injury
- CONTRAINDICATION: pregnancy (baseline pregnancy test)
- WARNING: hepatotoxicity (monitor LFTs monthly x 6 months, then q6-8wks)
- Renal, biliary excretion
5
Q
Hydroxychloroquine (Plaquenil)
- RA/ discoid and systemic lupus/ malaria tx and prophylaxis
A
- Antimalarial
- ADR: NAUSEA/DIARRHEA, skin and hair changes, rash
- EYE EFFECTS: rare; bull’s eye maculopathy, cornea deposits (baseline and annual eye exams)
- CONTRAINDICATIONS: retinal or visual fields changes; long term use in kids
6
Q
Sulfasalazine (Azulfide)
- Ulcerative colitis
- Treats pain, swelling and stiffness in RA
- Juvenile RA, ankylosing spondilitis, psoriatic arthritis
A
- Sulfa + salicylate
- Anti-inflammatory and immunomodulatory properties
- ADR: N/abd discomfort, photosensitivity
7
Q
Minocycline (Minocin)
- For mild RA
A
- Tetracycline antibiotic
- Anti-inflammatory properties (decreases PG, metalloproteinases and leukotrienes; increases IL 10)
- ADR: GI, dizziness, rash, photosensitivity
- SLOW onset
8
Q
Biologics (can memorize brand names)
A
AntiTNF
- Adalimumab (Humira)
- Etancercept (Enbrel)
- Infliximab (Remicade)
- Certolizumab pegol (Cimzia)
- Gloimumab (Simponi)– long t1/2
NonTNF
- Abatacept (Orencia)
- Rituximab (Rituxan)
- Tocilizumab (Actemra)
- Ustekinumab (Stelara)
9
Q
AntiTNF drugs
- INCREASED RISK OF INFECTION (require TB prior to initiation– can activate latent TB)
- Adalimumab (Humira)
- Etancercept (Enbrel)
- Infliximab (Remicade)
- Certolizumab pegol (Cimzia)
- Gloimumab (Simponi)
A
- Genetically engineered protines
- Block proinflammatory cytokines (TNF alpha, IL-1/IL-6)
- HF relative contraindication due to increased cardiac mortality
- Can worsen MS or cause MS like sx
- Increased risk of lymphoproliferative cancer
- Used when DMARDs fail to give adequate
- INDICATION: inflammatory conditions (RA, psoriatic arthritis, juvenile arthritis, crohn’s colitis, ankylosing spondylitis and psoriasis); reduce inflammation and stop dz progression; can be used in combo w/ DMARDs
- ADR: infection (URI, sinusitis and pharyngitis), injection site rxn (local rash, itching, burning), infusion-related rxn, HA, abd pain
10
Q
NonTNF
A
- Abatacept (Orencia)
- Rituximab (Rituxan)
- Tocilizumab (Actemra)
- Ustekinumab (Stelara)
11
Q
Abatacept (Orencia)
- Second line for RA, juvenile arthritis after MTX and biologics
A
- Selective T cell costimulation modulator
- Costimulation: immune cells generally require two signals for activation, target cell becomes anergic or apoptotic if only one signal received, anergic cells limit extent of autoimmune dz
- Binds antigenic CD80/86 receptors, blocking interaction w/ T cell CD 28 (prevents stimulation w/ second signal)
- Treats pain, swelling, prolonged joint stiffness
- ADR: HA, URI, nasopharyngitis, N
- CONTRAINDICATION: concomitant use with other biologics (worsen infection)
- Can cause COPD flares
- No increased cancer risk
12
Q
Rituximab (Rituxan)
- Second line RA
A
- Chemo drug
- CD 20 directed cytolytic antibody
- Targets and removes abnormal B cells, decreasing autoimmune response
- INDICATION: non-hodgkins lymphoma, chronic lymphocytic leukemia; wegener’s granulomatosis, microscopic polyangiitis
- ADR: infusion rxn (premedicate w/ prednisone, diphenhydramine); hypotension
- WARNING: tumor lysis syndrome, SJS/TEN, Hep B reactivation, cardiac arrhythmias, renal toxicity, bowel obstruction/perforation
13
Q
Tocilizumab (Actemra)
- RA, Juvenile arthritis
A
- IL-6 receptor antagonist (mediates T cell activation)
- ADR: increased cholesterol; URI, nasopharyngitis, HA, HTN, increased ALT
- WARNING: serious infections, GI perforation, Neutropenia, Live vaccines
14
Q
Ustekinumab (Stelara)
- Psoriasis, Psoriasis arthritis
A
- MOA: selectively targets IL-12 and IL-23
- COMMON ADR: nasopharyngitis, URI, HA, fatigue, arthralgia, N
- Malignancies reported
15
Q
Guidelines Early RA
A
- Start with DMARD monotherapy (MTX preferred)
- then TNF or nonTNF
- then glucocorticoids
- use short term glucocorticoids for flare ups
