lecture 16 - non-opioid analgesic

Question 1

initiation of inflam

injured cells release alarmins IL-33 which can produce degranulation of resident _ cells

Answer 1

mast cells

Question 2

mast cells release _ that act thru G protein coupled receptors to produce vasodilation and render the capillaries leaky

Answer 2

histamine

binds to H1 receptor and increases intracellular Ca of endothelium cells
Ca increase cause NO increase always

1. NO mediated relaxation of SM causing vasodilation
2. MLCK mediated contraction of the capillary endothelium - leaky

Question 3

the anti-inflammatory properties and pain relief comes from attenuating the production of _

Answer 3

prostaglandins
cause pain sensitization and more inflammtion from Arachidonic acid - part of cell membrane - A2 phospholipase yields 4 different PGs

so we block them

Question 4

NSAIDS block _ enzyme

Answer 4

COX

COX send AA to become PG - NSAIDS stop cox

COX 1 - lining of stomach - side effevt stomach probs - not desirable to inhib

COX 2 - for inflammation

Question 5

pharmacologic intervention to diminsh pain

_ inhib at the periphery

_ inhib of signaling to the CNS

_ inhib of CNS activity

Answer 5

NSAIDS and steroidal anti-inflamm and opioids at the periphery

LA-signaling to the CNS

inhib of CNS activity - opioids

Question 6

_ NSAID
irreversible inhibitor

about 100x better inhib of COX1 than COX2

worst selectivity of commo used pain relivers and NSAIDS

Answer 6

acetylsalicylic acid - aspirin

better at COX 1 - but we don’t want that

Question 7

_ _ _ are reversible inhibitors of COX 1 and COX2

attenuate the production of PG by inhib of COX2

Answer 7

ibuprofen, naproxen, acetaminophen

naproxen is the closest to being selective for COX2

Question 8

therapeutic effects of _

analgesia, antipyretic (fever), antiinflammatory, antithrombotic

Answer 8

acetylsalicyclic acid (aspirin)

all of these effects due to inhib of COX

antithrombsis - low dose

unique effect on thombosis - platelet aggregation is mediated by autocrine production of thromboxane (TXA2) - COX inhibit this production

Question 9

therapeutic effects of _

analgesia, antipyretic (fever), antiinflammatory,

Answer 9

ibuprofen and naproxen

no antithrombotic with these guys

Question 10

therapeutic effects of _

analgesia, antipyretic (fever),

Answer 10

acetaminophen

no antiinflam or antithromosis

Question 11

_ complication
fatty change in liver and edematous encephalopathy following aspirin use, 3-5 days later
children 6mon -15yr
etiology uncertain

preceded by milk upper resp tract infection, varicella, or influenza A or B - managed with aspirin admin at levels that are not ordinarily toxic but causes vomiting, irritability, lethargy and heptamoegly

Answer 11

Reye’s syndrome - asiprin

25% progress to coma , death, or permanent neurological impairments

Question 12

symptoms of _OD
sweling of the eyes, face, lips, tongue, throat
ringing in the ears - loss of hearing

wheezing, hard breathing, fast breathing
fast HR
cold,clammy skin
hives/rash
bring red in stool(black or tarry)
bloody vomit - coffegrounds

Answer 12

aspirin - acetylsalicyclic acid

contraindications:
ulcer - leading to internal bleeding
diabetes - hyper or hypo glycemia
gout - complex effects on plasma Urate levels
hypocoag condiitions - leads to bleeding
youth!

Question 13

Meloxicam - unique NSAID - prescription that is sequestered in synovial fluid

we care why

Answer 13

arthritis

Question 14

are there COX2 selevtive inhibitors

Answer 14

yes just don’t work very well

lumiracoxib

celecoxib

Question 15

Is there value to combo opioid and non-opioid pain relieves

NSAID -There is a ceiling effect for blocking pain

Mild stuff - they work great 

But really strong pain - not good - need to block with opiods 
	Management of pain - combo is effective  Strictly pain - opiods

Answer 15

yes!

NSAIDS have celing effect on pain

opidods - strictly pain