Anti-Inflammatory Flashcards
Prostaglandin
lipid compounds that have hormone-like effects as local mediators
produced in minute quantities by almost all tissues and rapidly metabolized (don’t circulate in blood)
Arachnoid Acid is primary precursor of PLP of membranes
Production of Prostaglandins
Cycooxygenase Pathway
COX 1: gastric production, vascular homeostasis, platelet aggregation, kidney and reproductive function
COX 2: elevated prostaglandin in sites of chronic disease and inflammation
Lipoxygenase Pathway Leukotrienes produced (tx asthma)
Prostaglandin Analogs
bind to membrane receptor and act as local signals with varying functions but play major role in modulating pain, inflammation, and fever
also controls uterine contractions, renal BF, and acid secretion/mucous production in GI tract
Misoprostol
PGE1 Analog ~ used to protect mucosal lining of stomach during chronic use of NSAIDS
decrease incidence of ulcers and constipation by binding to PGE receptors in parietal cells to decrease gastric acid and increase mucous production
AE: induce labor ** , D, Abdominal Pain, HA
- contraindicated in pregnancy
Iloprost
Prostacyclin Analog to increase cGMP causing vasodilation and mainly treats pulmonary HTN
inhalation only (short half life, needs frequent dosing)
AE: flush, HA, dizzy
Latanoprost
PGF analog
binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)
AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation
Travaprost
PGF analog PRODRUG
binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)
AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation
Bimatoprost
endogenous prostamides
binds to prostaglandin FP receptor to increase uveoscleral outflow and DECREASE IOP (tx glaucoma)
AE: blur, increased iris pigmentation, increase pigment and number of lashes, eye redness and irritation
Non-steroidal Anti-inflammatory drugs (NSAIDS)
inhibit COX enzymes which will decrease prostaglandin synthesis (PG etc)
anti-pyretic, anti-inflammatory, and analgesic but ulcers
- PGE: thought to sensitize nerve endings to inflammatory chemical mediators (analgesic)
- PGI: inhibits gastric acid secretion (increases acid)
- PGE/F: stimulate mucous production (decrease protection)
- PGE: increases set point for thermoregulatory center (no fever and resets body temp)
AE: ulcers + serious CV thrombotic events, MI, CVA
Contraindicated in post-op pain for CABG
Aspirin
prototype and ONLY NSAID to irreversibly inactivate COX
Esterases rapidly break down into salicylate
low dose decreases TXA and inhibits aggregation (prolongs bleeding) - DO NOT TAKE W/ anticoagulant
increases alveolar ventilation: elevates CO2 and increased respiration
Avoid in children with viral infections (reye syndrome)
Acetic and Propionic Acids
inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)
Indomethacin
Acetic and Propionic Acid / NSAID
highest incidence for GI issues + may cause ocular AE at large doses/long-term use
Blur, Whorl Keratopathy, Macular pigment changes
Ibuprofen
Acetic and Propionic Acid / NSAID
inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)
Max: 3200 mg/day
Diclofenac
Acetic and Propionic Acid / NSAID
inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)
Naproxen
Acetic and Propionic Acid / NSAID
inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)
Ketorolac
Acetic and Propionic Acid / NSAID
inhibit COX enzymes reversibly and nonspecifically with no effect on leukotrienes (less intense GI effects)
Meloxicam
Oxicams/NSAID
long half life (1x/day dosing)
preferential for COX-2 but nonselective at high doses
- may have lesser AE
Piroxicam
Oxicams/NSAID
long half life (1x/day dosing)
Celecoxib
COX-2 Specific NSAID
theoretically less AE; no inhibition of platelet aggregation and COX-1 still provides GI protection
some of these showed high CV disease and CVA risk
Acetaminophen
Tylenol / not NSAID - NOT ANTI-INFLAMMATORY
max 4g/day
inhibits prostaglandin synthesis (more activity in CNS so ONLY antipyretic and analgesic)
inactivated by chemicals in inflammatory cells/platelets
- poor anti-inflam or anti-platelet action
1st choice for children with viral infections or chicken pox
Metabolite: liver DAMAGE!! main AE
Hydroxychloroquine
also known as Plaquenil
increases pH within inflammatory cells to interfere with antigen processing and decrease CD4
Treat RA, SLE, Anti-malarial
AE: GI, skin rash, Acne + Bull’s Eye Maculopathy
Bull’s Eye Maculopathy
permanent loss of vision
RF: excessive daily dose of hydroxychloroquine by weight, duration of use, concomitant use of Tamoxifen, Retinal Disease
Recommendations:
- Dose: <5mg/kg of weight
- Baseline Screening within 1 year of starting treatment and annual screening after 5 years of use
- – DFE + 10-2 VF + macular OCT
Methotrexate
DMARD: immunosuppressant that inhibits dihydrofolate reductase and impairs DNA synthesis in immune cells
other meds can be added
lower dose than for cancer so less AE
IL-1 and TNF
pro-inflammatory cytokines involved in RA secreted by synovial macrophages to stimulate release of collagenase (decrease collagen!!)
Etanercept
TNF Inhibitor
subcutaneous/IV only
AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers
Adalimumab
TNF Inhibitor
subcutaneous/IV only
AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers
Infliximab
TNF Inhibitor
subcutaneous/IV only
AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers
Golimumab
TNF Inhibitor (treat RA)
subcutaneous/IV only
AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers
Certolizumab
TNF Inhibitor
subcutaneous/IV only
AE: high infection risk, no live vaccines, worsen pre-existing HF, increase risk of lymphoma/cancers
Anakinra
IL-1 Antagonist
do NOT take with TNF inhibitor
Subcutaneous 1x/day
Abatacept
inhibit t-cell activation to treat RA
Tocilizumab
inhibit IL-6 to treat RA
Tofacitinib
regulate immune cell function (oral)
