Analgesics Flashcards
What is COX?
cyclooxygenase; a key enzyme responsible for production of lipid based inflammatory mediators
COX is responsible for _____ generation
TXA2 (thromboxane A2)
What are the five cardinal signs of the inflammatory response
- Heat (calor)
- Redness (rubor)
- Swelling (tumour)
- pain (dolor)
- loss of function (function lease)
The inflammatory response is an immediate, protective _____ process characterized by ____, irritation, or injury
pathological; infection
Tissue repair is a _____ inflammatory process
post
Lipocortin is a protein that inhibits _____ activity
phospholipase 2
Steroids act by ____- inhibiting production of end products by causing transcription and translation of lipocortin
indirectly
Class ____ prostaglandins and type ____ leukotrienes apply to inflammation (pro inflammatory)
2; 4
Which leukotrienes enhance histamine effects, bronchoconstrict, constrict coronary arteries and dilate vessels in regions of inflammation
LTC4 and LTD4
____ decrease GI acid secretion and the GI tract, inhibits platelet aggregation, and promotes _____ in the kidneys
PGI2 (prostacyclin)
Which prostaglandin activates matrix metalloproteinases
Platelet activating factor
Which antibiotic inhibits MMP’s
Tetracyclines; degade ECM and allow immune cells to infiltrate to the region.
Omega 3 are good source of ____inflammatory supplement
anti
Type ____ prostaglandins and type ____ leukotriene are actually anti inflammatory
3; 5
What is the first and the last step of the anti-inflammatory pathway
first step: alpha linolenic acid (ALA)
last step: eicosanpentanoic acid
what is the first and the last step for the pro inflammatory pathway
first step: linoleic acid
last step: arachidonic acid
What is a constitutive (housekeeping) enzyme predominantly involved in PG and TXA2 production
COX 1
What is an inducible enzyme; predominantly involved in PG and Prostacyclin production which generates pro inflammatory PGs and O2 radicals.
COX -2; it doesn’t exist unless our body is told to make it.
What are autonomic responses of pain
- tachycardia
- systemic hypertension
- tachypnea
- diaphoresis
- pallor
- nausea
What are some therapeutic relief mechanisms peripherally
block pain mediators, receptor sensitization, and affarent neuronal discharge
what are some central therapeutic relief mechanisms
block pain receptors in the CNS
Bradykinin, norepinenphrine and ____ stimulate pain fibers
histamine
what results when prostaglandins, leukotrienes and substance P sensitize pain fibers
allodynia
what are endogenous analgesics
- endorphins (natural opioids)
2. serotonin
Aspirin and salicylate like agents are ______
NSAIDs
What are NSAID alternatives
Acetaminophen (parecetamol); central acting COX inhibition (pain and fewer); toxicity via hepatoxic metaolite; leading drug of choice for suicide.
Salicylic acid inhibits synthethis of ___enzyme
COX
Which NSAID’s are available as topical preparations
- flurbiprofen
- suprofen
- diclofenac
- ketoralac
____ has the most Cox 1 selectivity and the least Cox 2 selectivity
Ketorolac
ASA and acetaminophen have similar properties except:
Acetaminophen:
- is NOT antiinflammatory
- is NOT a platelet inhibitor
- does NOT irritate the GI
- Is pregnancy category B vs D in ASA
what are ASA adverse effects
- headache
- nausea
- abdominal cramps, bleeding, ulceration
- hemorrhagic diathesis: bleeding time doubles
- tinnitus –> hearing loss
- nephrotoxicity
- respiratory alkalosis –> metabolic acidosis
- acute poisoning by respiratory depression
- non immune low dose hypersensitivity
What is Reyes syndrome associated with
adverse reaction in children taking ASA to reduce fever in viral infections. Peptobismol should be avoided in kids up to 15 yoa. 35% mortality!
Cox 2 selective drugs are the ____GI toxic. Reduced Cox 2 selectivity leads to the ____GI toxicity
least; most
what are NSAID drug interactions?
- NSAIDs
- Steroids
- Anticoagulants
- omega 3 fatty acids
- ginkgo biloba
- intraocular cholinergics
what are NSAID contraindications
- active peptic ulcer
- chronic GIT inflammation
- bleeding disorders
- heavy alcohol use
- NSAD/ASA induced asthma
- Known hypersensitive
- chronic/hepatic/renal disease, diabetes
- hypertension/congestive heart failure
- pregnancy
- corneal denervation, dry eye
What are the different NSAID preparations
- topical
- oral
- local injection
- IV
Age restrictions do not apply to the topical NSAIDs except for which ones?
- Acular LS (Ketorolac) : 3 yrs
2. Ilevro (Nepafenac): 10 yrs
Which topical NSAID is the most prescribed drug?
Ilevro; pro drug that gets activated once it enters anterior chamber; used by most surgeons post op
what are some adverse effects of topical NSAIDs
- burning, stinging
- corneal toxicity, melting
- vitreous detachment
- delayed wound healing
- prolonged bleeding time
6 elevated IOP
you are not supposed to combine NSAIDs with ____
prostaglandins; they are pro inflammatory and NSAIds are antiinflammatory
In contrast to NSAIDs, narcotics dont have a ceiling effect, they induce _____, they are non topical, have no anti inflammatory effects, anti platelet effects, or anti pyretic effecs
meiosis
Key side effect of optiods is that it causes ____ release
histamine
what are other opiod adverse effects
- nausea and vomiting
- miosis
- flushing and itching
- sedation
- constipation
- cough suppression
- respiratory depression
- depedence
