Medications for Inflammation Flashcards
Which type of cells releases histamine?
Mast cells and basophils
What are two major effects of histamine when it is released?
Vasodilation
Increased vascular permeability
What happens when H1 (histamine) receptors are activated?
Causes alertness (bc are in the CNS)
Causes itching and pain
Promotes secretion of mucus in the upper respiratory system
Generally: promotes inflammation –> chemotaxis of eosinophils, neutrophils, increased activity of dendrites
Antihistamines MOA
Selectively antagonize H1 receptors (H1 blockers)
Diphenhydramine MOA
H1 receptor antagonist
Diphenhydramine Class
H1 blocker
Diphenhydramine ADE
Sedation, anticholinergic effects
Paradoxical CNS excitation in children
Diphenhydramine Contraindications
In breast-feeding
Diphenhydramine Warnings/Considerations
Risk-benefit for pregnant people bc it can cross the placenta
Avoid/minimize in older adults
Examples of anticholinergic effects
Dizziness
Drowsiness/sedation
Dry mouth & mucus membranes, eyes
Hypotension
Constipation
Blurry vision
Confusion
What is the first choice drug for the treatment of anaphylaxis?
Epinephrine IM
Epinephrine MOA
vasoconstrictor and bronchodilator
What can antihistamines treat and NOT treat?
Can be given for hives and itching
NOT for bronchospasm, hypotension, or shock
NSAIDs MOA
Inhibit COX, the enzyme that converts arachidonic acid to prostaglandins and related compounds
Immunosuppressants and immunomodulators MOA
Inhibit or limit the immune response more generally
Immunosuppressants vs immunomodulators
Immunosuppressants
- Tamp down the immune system
- Higher risk of infection and cancer
Immunomodulators
- Target a specific cytokine or signaling pathway
- Do not have a risk of infection and cancer
COX-1 vs COX-2
COX-1
- found in almost all tissues
- protects the gastric mucosa, supports renal function, promotes platelet aggregation
- “good COX”
COX-2
- found mainly at sites of tissue injury
- produced in response to cytokines
- mediates inflammation
- present in fever & pain (brain), kidneys, vasodilation
- “bad COX”
Harmful effects in the inhibition of COX-1
Gastric ulceration
Bleeding
Renal impairment
Beneficial effects in the inhibition of COX-1
Protection against myocardial infarction and stroke, 2/2 reduced platelet aggregation
Beneficial effect in the inhibition of COX-2
Suppression of inflammation
Alleviation of pain
Reduction of fever
Protection against colorectal cancer
Harmful effects in the inhibition of COX-2
Renal Impairment
Promotion of MI and stroke (2/2 suppressing vasodilation and production of prostacyclin and not suppressing platelet aggregation)
All NSAIDs can cause:
Renal impairment
Increase risk of bleeding (if COX-1 is inhibited)
Increase GI bleeding tendencies
Increase risk of MI and stroke (except aspirin)
Fetal abnormalities (except low-dose aspirin)
NSAIDs Contraindications
Past 30 weeks of gestation due to the risk of premature closure of the ductus arteriosus
NSAIDs should be avoided in patients with:
Severe renal impairment
Uncontrolled hypertension
Active peptic ulcer disease
Other bleeding tendencies
Sever liver disease (esp if cirrhosis is present)
Aspirin Class
NSAID (1st gen)
Aspirin MOA
Irreversibly inhibits COX (COX-1 > COX-2)
Aspirin ADE
Bleeding, GI bleeding, renal dysfunction, tinnitus, Reyes syndrome (rare brain swelling), hypersensitivity reactions (including anaphylaxis)
Aspirin Contraindications
< 18 y.o.
30+ weeks gestation
Aspirin Warnings/Considerations
Low-dose aspiring can be given to pregnant people to prevent preeclampsia and in certain clotting disorders
Discontinue 7-10 days before surgery
Aspirin Drug interactions
Anticoagulants, glucocorticoids, EtOH, NSAIDS
can cause more bleeding
Ibuprofen Class
NSAID (1st gen)
Ibuprofen MOA
Inhibits COX (COX-1 = COX-2 — 50/50)
Ibuprofen ADE
Bleeding, GI bleeding, renal dysfunction, increased risk of MI/stroke
Ibuprofen Contraindication
30+ weeks gestation
Ibuprofen Warnings/Considerations
Can cause oligohydramnios past 20 weeks gestation
Avoid 20-30 weeks gestation
Discontinue 3 days before surgery
Ibuprofen Interactions
Low-dose aspirin (block COX binding site)
Glucocorticoids
Celecoxib Class
NSAID (2nd gen)
Celecoxib MOA
Selectively inhibits COX-2
Celecoxib ADE
Renal impairment, risk of MI/stroke
Celecoxib Warnings/Considerations
Caution with sulfonamide allergy (“sulfa” allergy)
Can cause oligohydramnios past 20 weeks gestation
Risk-benefit calculation in lactation
Celecoxib Contraindications
Past 30 weeks gestation
Celecoxib Interactions
Warfarin (enhance anticoagulant effects)
COX inhibitors (additive effect)
What do glucocorticoids mimic?
Cortisol
What effects do glucocorticoids cause?
Anti-inflammatory and immunosuppressant effects
Prednisone Class
Glucocorticoid/corticosteroid/steroid
Prednisone MOA
inhibits pro-inflammatory mediator synthesis via gene transcription mechanism
Prednisone Elimination
Is a PRODRUG
Converted via CYP3A4 enzyme
Prednisone Interactions
NSAIDs (GI bleed risk), diabetes medications (bc incr BG)
Prednisone Pregnancy/Lactation Considerations
Conflicting evidence
possible growth suppression, fetal adrenal hypoplasia
Use lowest possible dose for shortest amount of time
Prednisone ADE
Short-term: increased appetite, hyperglycemia, insomnia, delayed wound healing, GI ulcers/bleeding, blood clots
Medium-long-term: osteoporosis, infection, iatrogenic Cushing’s syndrome, adrenal suppression
How is Adrenal Suppression caused?
Long-term glucocorticoid use with abrupt cessation
Prednisone teaching points
Take once-daily doses
Do NOT abruptly discontinue taking
Monitor BG if diabetic
Avoid NSAIDs
Report early signs of infections
Report abdominal pain/bloody or black stools, swelling/edema, muscle weakness, irregular heart rhythms
Wear medical alert bracelet, have emergency supply if being used in long-term therapy
What are DMARDs? What do they do?
Disease-Modifying Antirheumatic Drugs
They modify the underlying disease process, rather than simply treating the resulting inflammation
May suppress immune function
Types: biologic and non-biologic
DMARDs vs. NSAIDs (action, toxicity)
DMARDs are slower acting. and more toxic than NSAIDs
Methotrexate Class
Non-biologic DMARD
Methotrexate MOA
Not entirely understood
Methotrexate Patient teaching point
Onset is 3-6 weeks, takes time to have an effect
Methotrexate Contraindications
Severe liver disease
Pregnancy
Methotrexate ADE
Hepatic fibrosis, bone marrow suppression, GI ulceration
Methotrexate Warnings/Considerations
Decrease dose in renal impairment
Folic acid supplement recommended to minimize hepatic, GI, and hematologic adverse effects
CBC, platelet count, LFTs required q 8-12 weeks
Excreted in breast milk, avoid use
Methotrexate Warnings/Considerations
Decrease dose in renal impairment
Folic acid supplement recommended to minimize hepatic, GI, and hematologic adverse effects
CBC, platelet count, LFTs required q 8-12 weeks
Excreted in breast milk, avoid use
What are monoclonal antibodies?
Biologic DMARDs
antibodies that are identical because they were produced by clones of a single-parent cells
used to treat autoimmune/chronic inflammatory disorders, considerable use in oncology as well
EXPENSIVE
Infliximab Class
Biologic DMARD
Infliximab MOA
TNF-alpha antagonist
Binds both soluble and receptor-bound TNF-alpha –> bound TNF-alpha cannot function nor signal inflammation effects
Infliximab Warning/Considerations
Use concomitant methotrexate, improves efficacy of infliximab
Test for latent TB bc it can activate it! –> continue monitoring for it
Avoid 30+ weeks of gestation
Lactation
Infliximab ADE
BBW: severe infection
Infusion reaction
Infliximab Interactions
Immunosuppressants, immunomodulators (except methotrexate), corticosteroids, (live) vaccines
Thromboxane A2 is synthesized in:
Platelets
_____________ T cells recognize Class I MHC and ____________ T cells recognize Class II MHC
CYTOTOXIC T cells recognize Class I MHC and HELPER T cells recognize Class II MHC.
A blood transfusion reaction is which type of hypersensitivity reaction?
Type II
Your patient has just been prescribed diphenhydramine (Benadryl) for his allergies. Patient teaching should include avoidance of which beverage?
Alcohol
Which statement by the patient with diabetes who has been prescribed prednisone (Deltasone), 10 mg daily x 60 days, requires further teaching by the nurse?
“If I can’t attend my 2-month follow-up appointment, I will just stop taking this medication”.
The mechanism of action of Celecoxib (Celebrex) can be described as:
COX-2 inhibitor
In an allergic reaction, which type of antibody/immunoglobulin binds to mast cells?
IgE
This cell type can release reactive oxygen species (ROS) and proteases that have the potential to damage nearby healthy tissue
Neutrophils
Which med is a prodrug?
Prednisone
Which med requires testing for CBC and platelet count?
Methotrexate
Which med calls for folic acid supplementation?
Methotrexate
Which med causes anticholinergic effects?
Diphenhydramine
Which meds selectively inhibit COX-2?
Celecoxib
Which two meds given together increase one of their efficacy?
Infliximab and Methotrexate
Which med can activate late TB?
Infliximab
NSAIDs on this exam
Aspiring (1st gen)
Celecoxib (2nd gen)
Ibuprofen (1st gen)
DMARDs on this exam
Methotrexate (non-biologic)
Infliximab (biologic)
Which med is contraindicated in people less than 18 y.o.?
Aspirin
Which med can result in Reye’s Syndrome?
Aspirin
