24. Anti-inflammatories Flashcards
Name 3 prototypes of NSAIDs
- salicylates (Aspirin or ASA)
- propionic acid derivatives (Ibuprofen)
- selective COX-2 inhibitors (Celecoxib)
Name 1 prototype of immune modulators
Infliximab
Name 1 prototype of uric acid biosynthesis inhibitors
Allopurinol
Name 3 chemical mediators released after tissue injury
- histamines
- kinins
- prostaglandins
5 Cardinal Signs of inflammation
- erythema (vasodilation)
- edema (increased membrane permeability)
- heat (vasodilation)
- pain (stretching of pain receptors and chemical mediators)
- loss of function (due to pain and swelling)
enzyme responsible for converting arachidonic acid into prostaglandins
cyclooxygenase (COX)
COX-1 vs COX-2 enzymes
- COX-1: protects stomach lining, decreases fever, promotes clotting
- COX-2: triggers pain and inflammation
What is caused by Aspirin and NSAIDs when they inhibit both COX-1 and COX-2 enzymes?
- inhibit COX-1: loss of stomach lining -> ulcers; prevent clotting
- inhibit COX-2: reduces pain and inflammation
What is the function of 2nd generation NSAIDs?
- inhibit COX-2: reduces pain and inflammation
- does NOT inhibit COX-1: protects stomach lining and promotes clotting
list 4 general uses for anti-inflammatories
- inflammation
- pain
- fever
- anticoagulant (anti-platelet)
How is Aspirin used differently than other NSAIDs?
- used as an anti-platelet in cardiac/CVA patients
T/F: ASA can be taken with other NSAIDs
False; ASA and NSAIDs reduce each others effects
What form does ASA come in?
- enteric-coated pills -> absorbed later in GI system to prevent stomach ulcers
- can come in regular tablets for those who can’t take full pills (can be crushed)
MOA of Aspirin (ASA)
- inhibition of prostaglandin synthesis
- inhibition of hypothalamic heat-regulator
Uses for Aspirin
- reduce pain/inflammation/fever
- inhibit platelet aggregation
- osteoarthritis
- RA
Adverse reactions for Aspirin
- tinnitus
- GI bleed/hemolytic anemia
- agranulocytosis
- thrombocytopenia
- hepatotoxicity
syndrome linked to viral illness in children (ex. chickenpox/influenza) and administration of Aspirin
Reye’s syndrome
Sxs of Reye’s syndrome
- vomiting
- lethargy
- delirium
- coma
How are Ibuprofen and Naproxen different from older NSAIDs?
- stronger than ASA but less GI irritation
- highly protein bound (risk for drug interactions)
MOA of Ibuprofen
- inhibition of prostaglandin synthesis -> relieving pain and inflammation
Uses for Ibuprofen
- reduce inflammatory process
- relieve pain
- reduce fever
- arthritic conditions
Adverse reactions for Ibuprofen
- hearing loss/tinnitus
- anemia (LT)
- neutropenia (LT)
- thrombocytopenia (LT)
- nephrotoxicity (LT)
- anaphylaxis (LT)
1 contraindication for Ibuprofen
CABG (increased risk of another MI due to effect in another area of the clotting system)
What is the only selective COX-2 inhibitor (2nd generation NSAID) and what is it the drug of choice for?
- Celecoxib
- used for severe arthritis
MOA of Celecoxib
- inhibits COX-2 -> inhibits prostaglandin synthesis and inflammation
- does not inhibit COX-1
Uses of Celecoxib
- osteoarthritis
- RA
- moderate/severe pain
- ankylosing spondylitis
Adverse reactions for Celecoxib
- peripheral edema
- bleeding
- HTN
- CVA (LT)
What are DMARDs and what are they used for?
- disease modifying anti-rheumatic drugs
- include immunosuppressives, immunomodulators, and antimalarials
- used to control immune-mediated pain when NSAIDs don’t work
MOA of Infliximab
- binds to TNF and blocks it from attaching to receptors on synovial cell surface
- reduces infiltration of inflammatory cells and delays inflammatory process
Uses for Infliximab
- RA
- psoriatic arthritis
- spondylitis
- ulcerative colitis
- Crohn’s disease
- psoriasis
Adverse reactions for Infliximab
- severe infections
- BP changes
- seizures
- elevated liver enzymes
- Steven-Johnson syndrome
- anemia
Contraindication for Infliximab
heart failure
What should be considered before starting a pt on Infliximab?
- medication is an immune suppressant (can lead to infection)
- review pt’s infection risk
- make sure they are up to date on all immunizations (especially attenuated virus vaccines before starting)
serious disorder (usually dug induced) that causes flu symptoms and a painful rash that spread and blisters on the skin and mucous membranes
Steven-Johnson syndrome (SJS)
more severe form of SJS that causes damage to more than 30% of the skin surface and mucous membranes
toxic epidermal necrolysis (TEN)
What should be done to help during a gout attack?
- increase fluid intake
- avoid foods high in purines (organ meats, liver, gravy, and beer)
MOA of Allopurinol
inhibits final step of uric acid synthesis -> lowers serum uric acid levels
Uses of Allopurinol
- prophylactic for gout
- chronic tophaceous gout
- NOT used for acute gout attack
Adverse reactions for Allopurinol
- hepatic impairment
- angioedema
- hyperglycemia
- hyperlipidemia
Side effects of Aspirin hypersensitivity or overdose
- tinnitus
- dizziness
- bronchospasm
- flushing/sweating
- headache
Pt teaching for Aspirin
- do NOT give ASA to children w/ flu-like sxs (Reye’s)
- take ASA w/ food or fluids (prevents GI distress)
Pt teaching for Ibuprofen
- do NOT take ASA w/ Ibuprofen or other NSAIDs
- pregnant women should not take NSAIDs (may cause congenital defects)
- take NSAIDs w/ food or fluids (prevents GI distress)
Pt teaching for Inflixmab
advise pt not to receive live vaccines while taking Infliximab
Normal therapeutic range of ASA
15-30 mg/dL
