Module 8: Unit D Flashcards
Common gluccocoritcoids
prednisone
prednisolone
methylprednisolone
betamethasone
dexamethasone
Indications glucocorticoids
RA
SLE
IBS
Inflammatory disorders
Allergic reactions
Asthma
Dermatological conditions
MOA glucocorticoids
Glucocorticoids produce anti-inflammatory and immunosuppressive effects when administered at pharmacologic doses (vs. physiologic dosage). Glucocorticoids activate receptors within the cellular cytoplasm, forming an active receptor-steroid complex which produces mRNA in the nucleus to code for specific regulatory proteins.
Cautions, contraindications, D2D of glucocorticoids
Contraindicated: systemic fungal infections; patients receiving live virus vaccines (MMR, rotavirus, varicella, FluMist)
Caution: pediatric patients, pregnant or breastfeeding women, HTN, renal impairment, HF, DM, osteoporosis, gastritis, esophagitis, treatment-resistant infection, glaucoma.
Caution: NSAIDs, oral hypoglycemics, insulin, digoxin, potassium-sparing diuretics.
AE and SE of glucocorticoids
Potentially harmful withdrawal symptoms if long-term or high-dose stopped abruptly.
Risk of adrenal suppression
AE: osteoporosis, infection, ↓ wound healing, hyperglycemia, myopathy, fluid and electrolyte imbalance, growth delay, psychological disturbance, cataracts and glaucoma, peptic ulcer disease, iatrogenic Cushing’s disease, ↑ risk of GI bleed, adrenal suppression
Monitoring needed with glucocorticoids
Baseline: V/s, BMI, height, weight, DXA, CBC, CMP, lipids, then one month after starting treatment and every 6 months when stable
Establish baseline, monitor, and identify high risk patients or situations
Eye exams-advise pts. to notify you of any vision changes
Glucose testing - sliding scale or med adjustment at necessary
Conventional synthetic csDMARDs:
methotrexate (Trexall)
leflunomide (Arava)
sulfasalazine (Azulfidine)
hydroxychloroquine (Plaquenil)
Biologic DMARDS
TNF inhibitors
etanercept (Enbrel)
adalimumab (Humira)
infliximab (Remicade)
Targeted synthetic tsDMARDs:
Janus kinase inhibitor
Methotrexate indication
RA, psoriasis, acute lymphoblastic leukemia, polyarticular juvenile idiopathic arthritis
Leflunomide indication
active RA
Indication sulfasalazine
RA, IBS
hydroxychloroquine indication
RA (adjunct to methotrexate)
Methotrexate MOA
folate antagonist which DNA synthesis, repair, and cellular replication in active, proliferative cells. In RA, methotrexate may ↓ activity of B and T lymphocytes leading to immunosuppression.
leflunomide MOA
prodrug converted to metabolite 1 which inhibits T-cell proliferation and ↓ inflammation
Sulfasalazine MOA
Exact MOA unknown. 5-ASA (active component) may attenuate local mediators of the inflammatory response (leukotrienes), May also function as a free radical scavenger or an inhibitor of tumor necrosis factor (TNF)
Hydroxycloroquine MOA
exact MOA unknown; thought to ↓ movement neutrophils, and eosinophils; impairs complement-dependent antigen-antibody reactions
Contraindications DMARDS
Pregnancy, hypersensitivity, dyscrasias, immunodeficiency, liver disease
BBW methotrexate
cause numerous and potentially fatal toxicities of the bone marrow, liver, lungs, and kidneys. Other fatalities have occurred with skin reactions, hemorrhagic enteritis, and GI perforation. Pregnancy. Hypersensitivity.
SE leflunomide
hepatotoxic, SJS, serious infection, diarrhea, alopecia, interstitial lung disease, peripheral neuropathy, teratogen- discontinuation protocol
SE sulfasalazine
GI- nausea, vomiting, anorexia, pain; rash, SJS, pruritus,
SE/Safety hydroxychloroquine
Retinal damage, cardiomyopathy, AV block, BBB, prolonged QT, hypoglycemia, myopathy, neuropathy, worsening of psoriasis, GI distress
TNF-Inhibitors Biologic bDMARDs:
etanercept (Enbrel)
adalimumab (Humira)
infliximab (Remicade)
Indications TNF inhibitors:
etanercept (Enbrel)
adalimumab (Humira)
infliximab (Remicade)
Primarily RA
Also used for inflammatory disorders like psoriatic arthritis, Crohn’s, and ankylosing spondylitis.
MOA: TNF inhibitors:
etanercept (Enbrel)
adalimumab (Humira)
infliximab (Remicade)
Suppresses inflammation by inhibiting TNF by forming a TNF-receptor complex, preventing TNF from binding with natural receptors on cells
TNF inhibitors SE:
etanercept (Enbrel)
adalimumab (Humira)
infliximab (Remicade)
Sepsis, active infection, hypersensitivity
Risk for serious infection, bacterial sepsis, invasive fungal infection, hepatitis B, TB, HF, liver failure, dyscrasias, cancer, neuro concerns
BBW TNF inhibitors
TNFIs: Serious systemic infections and sepsis
infliximab: serious and potentially fatal infections
Janus kinase inhibitors
Targeted synthetic tsDMARDs
tofacitinib (Xeljanz)
baricitinib (Olumiant)
Indications for Janus kinase inhibitors: tofacitinib (Xeljanz)
baricitinib (Olumiant)
Moderate to severe RA not responding to methotrexate
psoriatic arthritis
ulcerative colitis
MOA janus kinase inhibitors: tofacitinib (Xeljanz)
baricitinib (Olumiant)
Reduce immune and inflammatory responses by blocking JAK enzyme signaling and interrupting the STAT pathway
Safety considerations Janus Kinase inhibitors:
tofacitinib (Xeljanz)
baricitinib (Olumiant)
Active infection, hypersensitivity
infection, HA, ↑ cholesterol, gastroenteritis, bone marrow suppression, thrombosis, dysrhythmias, CA,
BBW janus kinase inhibitors:
tofacitinib (Xeljanz)
baricitinib (Olumiant)
serious and potentially fatal infections
