Apex midterm questions and answers
mj mj mj mj
Opioid receptors & their ligands?
mj mj mj mj
Where do opioids work? - ANSWERMu --> endorphins
mj mj mj mj mj mj mj mj
delta --> enk mj mj mj
kappa --> Dyn mj mj mj
PNS & CNS (brain, spinal cord)
mj mj mj mj mj
what drugs work on each step of pain nociception? - ANSWERtransduction -
mj mj mj mj mj mj mj mj mj mj mj
NSAIDs, LA, opioids, antihistamines, steroids
mj mj mj mj mj
transmission - LA mj mj
modulation - nmda, ssri, snri, nxl opioids, alpha 2 agonists, ache inhibitors
mj mj mj mj mj mj mj mj mj mj mj
perception: alpha 2 agonists, GA, opioids mj mj mj mj mj
explain 1st, 2nd, 3rd order neurons in transmission. What spinal tract is
mj mj mj mj mj mj mj mj mj mj mj
transmission in? - ANSWER1st: site --> dorsal horn
mj mj mj mj mj mj mj mj
2nd: DH --> thalamus (cell body in DH)
mj mj mj mj mj mj mj
3rd: thalamus --> cortex (cell body in thalamus)
mj mj mj mj mj mj mj
Spinothalamic
Where is the most important site of modulation? - ANSWERSubstantia gelatinosa in
mj mj mj mj mj mj mj mj mj mj mj
DH rex lam 2 & 3
mj mj mj mj mj mj
Which 2 effects of opioids are NOT impacted by tolerance? - ANSWERMiosis &
mj mj mj mj mj mj mj mj mj mj mj mj
constipation
mj
MoA of opioids? - ANSWER-bind to g protein
mj mj mj mj mj mj mj mj
-↓adenylate cyclase --> ↓camp mj mj mj
-↓ca+ presynaptically, ↑k+ postsynaptically
mj mj mj
Mu receptors effects
mj mj
Delta effects mj
kappa effects - ANSWERmu: bradycardia, miosis, n/v, sphincter of oddi contraction
mj mj mj mj mj mj mj mj mj mj
(↑biliary pressure), euphoria, prolactin rlz, hypothermia, resp depression, pruritis,
mj mj mj mj mj mj mj mj mj
analgesia
mj
delta: analgesia, urinary retention, resp depression, NO CNS, NO MIOSIS
mj mj mj mj mj mj mj mj mj mj
kappa: antishivering, diuresis, resp depression?, dysphoria, hallucinations, delirium,
mj mj mj mj mj mj mj
sedation, NO PRURITIS
mj mj mj
opioid OD - s/s, narcan dose - ANSWER↑ICP, TV, PaCo2
mj mj mj mj mj mj mj mj mj
↓pH, RR mj
,Apex midterm questions and answers
mj mj mj mj
narcan: 1-4mcg/kg (20-40mcg) mj mj
**slowly, sudden ↑SNS --> tachy, pulm edema, arrythmia, death
mj mj mj mj mj mj mj mj
*can also cause n/v
mj mj mj mj
*can do infusion
mj mj
which drugs release histamine? - ANSWERopioids: morphine, meperidine, codeine
mj mj mj mj mj mj mj mj mj
NMB: succs, atra, miva, (NOT PANC)
mj mj mj mj mj
barbs: thiopental (reflex tachy)
mj mj mj
which opioid increase sphincter of oddi pressure the least? - ANSWERmeperidine
mj mj mj mj mj mj mj mj mj mj
which opioids have metabolites? How are opioid metabolites excreted? -
mj mj mj mj mj mj mj mj mj
ANSWERmorphine, meperidine, TRAMADOL & maybe hydromorphone
mj mj mj mj mj mj
(CODEINE??)
mj
morphine - m6g, m3g mj mj mj
*CI in renal pt, elderly
mj mj mj mj mj
mep - normep mj mj mj
*can cause myoclonus, seizures
mj mj mj
renally
how are all opioids metabolized? - ANSWERliver
mj mj mj mj mj mj
which opioid contraindicated for nxl use? - ANSWERremi
mj mj mj mj mj mj mj
*has glycine in constitution, causes skeletal muscle weakness
mj mj mj mj mj mj mj
which opioids are likely to cause chest wall rigidity?
mj mj mj mj mj mj mj mj
tx?
does chest wall rigidity increase icp? FRC? - ANSWERmore potent ones (suf, alf,
mj mj mj mj mj mj mj mj mj mj mj mj
remi, fent)
mj mj mj
paralyze & intubate mj mj mj
↑ICP, ↓FRC mj
how do opioids affect immune function?
mj mj mj mj mj
how do they affect SSEPs?
mj mj mj mj
BP? - ANSWER↓killer t cell, cause inflammation, ↓immunologic fxns
mj mj mj mj mj mj mj mj
do not affect sseps
mj mj mj
do no affect BP, if drop in BP its from histamine.
mj mj mj mj mj mj mj mj mj mj mj
*do not affect contractility.
mj mj mj
what opioid has anticholinergic side effects & inhibits n. conduction?
mj mj mj mj mj mj mj mj mj
which opioid should you not admin with a pt on MAOI - ANSWERMEP &
mj mj mj mj mj mj mj mj mj mj mj mj mj
FENTANYL
mj mj
Mep: stimulate mu & kappa
mj mj mj mj
,Apex midterm questions and answers
mj mj mj mj
causes tachy, mydriasis, dry mouth (xerostomia)
mj mj mj mj mj
mep & fentanyl: has mild MAOI properties
mj mj mj mj mj mj
which opioid has the fastest onset? why? - ANSWERalfentanil
mj mj mj mj mj mj mj mj
*all opioids are weak bases, alfentanil PKA is 6.8
mj mj mj mj mj mj mj mj mj
**↑unionized fxn at phys pH mj mj mj mj mj
**↓Vd
*all other opioids pka > 7.2
mj mj mj mj mj
which opioid is the most ionized/least unionized at phys pH? - ANSWERmep
mj mj mj mj mj mj mj mj mj mj mj
list opioids by potency - ANSWERmeperidine 100mg
mj mj mj mj mj mj
morphine 10mg mj mj
hydromorphone 1.4mg (7x as strong) mj mj mj mj
alfentanil 1000mcg mj
fentanyl 100mcg mj
remi 100mcg mj
sufentanil 10mcg mj
draw context sensitive half time graph of opioids - ANSWER
mj mj mj mj mj mj mj mj mj
list opioid antagonists - ANSWERNaloxone
mj mj mj mj
Naltrexone - can also use for alcohol abuse, long acting
mj mj mj mj mj mj mj mj mj
Nalmefene - longer acting narcan mj mj mj mj
Methylnaltrexone - doesnt cross cns, good for bowel obs mj mj mj mj mj mj mj mj
list partial agonists
mj mj
drawbacks - ANSWERBuprenorphine - analgesia stronger than morphine
mj mj mj mj mj mj mj
butorphanol - analgesia stronger than morphine mj mj mj mj mj
nalbuphine - good for heart disease mj mj mj mj mj
a local anesthetic with a pka (further, closer) to physiological pH will have a faster
mj mj mj mj mj mj mj mj mj mj mj mj mj mj
onset. - ANSWERcloser to.
mj mj mj mj
3 components of local anesthetic molecule and what they determine? - ANSWER1.
mj mj mj mj mj mj mj mj mj mj mj
benzene ring
mj mj mj
*lipophilicity mj
2. intermediate chain
mj mj
*metabolism, allergy mj
*COC or NH-C mj mj
3. tertiary amine
mj mj
*hydrophilicity; accepts proton mj mj
*weak base mj
, Apex midterm questions and answers
mj mj mj mj
metabolism of esters vs amides mj mj mj mj mj
allergy potential esters vs amides - ANSWEResters: pseudocholin
mj mj mj mj mj mj mj mj
amides: liver cyp450 mj mj
esters: PABA preservative allergy
mj mj mj
*cross sensitivitymj mj
amides: methylparaben mj
local anesthetics are weak ____ that are typically more ____ at phys pH
mj mj mj mj mj mj mj mj mj mj mj mj
what part of the LA exerts the anesthetic action? - ANSWERbases; ionized
mj mj mj mj mj mj mj mj mj mj mj
the charged, ionized component
mj mj mj
**except w/ benzocaine mj mj
Order pkas locals - ANSWERamides have lower pka
mj mj mj mj mj mj mj mj
*bupi, levobupi, ropi: 8.1
mj mj mj
*lido, prilo: 7.9
mj mj
*mepi: 7.6 mj
esters higher mj mj
*procaine 8.9 mj
*chloro 8.7 mj
*tetra 8.5 mj
what is the highest pka of the amides?
mj mj mj mj mj mj mj
what is the highest pka of the esters? - ANSWER8.1
mj mj mj mj mj mj mj mj mj
8.9
max doses amides
mj mj
levobupi, bupi, bupi + epi, ropi, lido, mepi etc - ANSWERlevobupi 150mg (2mg/kg)
mj mj mj mj mj mj mj mj mj mj mj mj
bupi 175 (2.5)
mj mj
bupi + epi 200 (3)
mj mj mj mj
ropi 200 (3)
mj mj
lido 300 (4.5)
mj mj
mepi 400 (7)
mj mj
lido + epi 500 (7)
mj mj mj mj
prilo <70kg: 500/>70kg: 600 (8)
mj mj mj mj
max doses esters - ANSWERprocaine 350-600mg (7mg/kg)
mj mj mj mj mj mj
chloroprocaine 800 (11) mj mj
chloroprocaine + epi 1000 (14) mj mj mj mj
Max dose of Exparel (liposomal bupi)
mj mj mj mj mj
mj mj mj mj
Opioid receptors & their ligands?
mj mj mj mj
Where do opioids work? - ANSWERMu --> endorphins
mj mj mj mj mj mj mj mj
delta --> enk mj mj mj
kappa --> Dyn mj mj mj
PNS & CNS (brain, spinal cord)
mj mj mj mj mj
what drugs work on each step of pain nociception? - ANSWERtransduction -
mj mj mj mj mj mj mj mj mj mj mj
NSAIDs, LA, opioids, antihistamines, steroids
mj mj mj mj mj
transmission - LA mj mj
modulation - nmda, ssri, snri, nxl opioids, alpha 2 agonists, ache inhibitors
mj mj mj mj mj mj mj mj mj mj mj
perception: alpha 2 agonists, GA, opioids mj mj mj mj mj
explain 1st, 2nd, 3rd order neurons in transmission. What spinal tract is
mj mj mj mj mj mj mj mj mj mj mj
transmission in? - ANSWER1st: site --> dorsal horn
mj mj mj mj mj mj mj mj
2nd: DH --> thalamus (cell body in DH)
mj mj mj mj mj mj mj
3rd: thalamus --> cortex (cell body in thalamus)
mj mj mj mj mj mj mj
Spinothalamic
Where is the most important site of modulation? - ANSWERSubstantia gelatinosa in
mj mj mj mj mj mj mj mj mj mj mj
DH rex lam 2 & 3
mj mj mj mj mj mj
Which 2 effects of opioids are NOT impacted by tolerance? - ANSWERMiosis &
mj mj mj mj mj mj mj mj mj mj mj mj
constipation
mj
MoA of opioids? - ANSWER-bind to g protein
mj mj mj mj mj mj mj mj
-↓adenylate cyclase --> ↓camp mj mj mj
-↓ca+ presynaptically, ↑k+ postsynaptically
mj mj mj
Mu receptors effects
mj mj
Delta effects mj
kappa effects - ANSWERmu: bradycardia, miosis, n/v, sphincter of oddi contraction
mj mj mj mj mj mj mj mj mj mj
(↑biliary pressure), euphoria, prolactin rlz, hypothermia, resp depression, pruritis,
mj mj mj mj mj mj mj mj mj
analgesia
mj
delta: analgesia, urinary retention, resp depression, NO CNS, NO MIOSIS
mj mj mj mj mj mj mj mj mj mj
kappa: antishivering, diuresis, resp depression?, dysphoria, hallucinations, delirium,
mj mj mj mj mj mj mj
sedation, NO PRURITIS
mj mj mj
opioid OD - s/s, narcan dose - ANSWER↑ICP, TV, PaCo2
mj mj mj mj mj mj mj mj mj
↓pH, RR mj
,Apex midterm questions and answers
mj mj mj mj
narcan: 1-4mcg/kg (20-40mcg) mj mj
**slowly, sudden ↑SNS --> tachy, pulm edema, arrythmia, death
mj mj mj mj mj mj mj mj
*can also cause n/v
mj mj mj mj
*can do infusion
mj mj
which drugs release histamine? - ANSWERopioids: morphine, meperidine, codeine
mj mj mj mj mj mj mj mj mj
NMB: succs, atra, miva, (NOT PANC)
mj mj mj mj mj
barbs: thiopental (reflex tachy)
mj mj mj
which opioid increase sphincter of oddi pressure the least? - ANSWERmeperidine
mj mj mj mj mj mj mj mj mj mj
which opioids have metabolites? How are opioid metabolites excreted? -
mj mj mj mj mj mj mj mj mj
ANSWERmorphine, meperidine, TRAMADOL & maybe hydromorphone
mj mj mj mj mj mj
(CODEINE??)
mj
morphine - m6g, m3g mj mj mj
*CI in renal pt, elderly
mj mj mj mj mj
mep - normep mj mj mj
*can cause myoclonus, seizures
mj mj mj
renally
how are all opioids metabolized? - ANSWERliver
mj mj mj mj mj mj
which opioid contraindicated for nxl use? - ANSWERremi
mj mj mj mj mj mj mj
*has glycine in constitution, causes skeletal muscle weakness
mj mj mj mj mj mj mj
which opioids are likely to cause chest wall rigidity?
mj mj mj mj mj mj mj mj
tx?
does chest wall rigidity increase icp? FRC? - ANSWERmore potent ones (suf, alf,
mj mj mj mj mj mj mj mj mj mj mj mj
remi, fent)
mj mj mj
paralyze & intubate mj mj mj
↑ICP, ↓FRC mj
how do opioids affect immune function?
mj mj mj mj mj
how do they affect SSEPs?
mj mj mj mj
BP? - ANSWER↓killer t cell, cause inflammation, ↓immunologic fxns
mj mj mj mj mj mj mj mj
do not affect sseps
mj mj mj
do no affect BP, if drop in BP its from histamine.
mj mj mj mj mj mj mj mj mj mj mj
*do not affect contractility.
mj mj mj
what opioid has anticholinergic side effects & inhibits n. conduction?
mj mj mj mj mj mj mj mj mj
which opioid should you not admin with a pt on MAOI - ANSWERMEP &
mj mj mj mj mj mj mj mj mj mj mj mj mj
FENTANYL
mj mj
Mep: stimulate mu & kappa
mj mj mj mj
,Apex midterm questions and answers
mj mj mj mj
causes tachy, mydriasis, dry mouth (xerostomia)
mj mj mj mj mj
mep & fentanyl: has mild MAOI properties
mj mj mj mj mj mj
which opioid has the fastest onset? why? - ANSWERalfentanil
mj mj mj mj mj mj mj mj
*all opioids are weak bases, alfentanil PKA is 6.8
mj mj mj mj mj mj mj mj mj
**↑unionized fxn at phys pH mj mj mj mj mj
**↓Vd
*all other opioids pka > 7.2
mj mj mj mj mj
which opioid is the most ionized/least unionized at phys pH? - ANSWERmep
mj mj mj mj mj mj mj mj mj mj mj
list opioids by potency - ANSWERmeperidine 100mg
mj mj mj mj mj mj
morphine 10mg mj mj
hydromorphone 1.4mg (7x as strong) mj mj mj mj
alfentanil 1000mcg mj
fentanyl 100mcg mj
remi 100mcg mj
sufentanil 10mcg mj
draw context sensitive half time graph of opioids - ANSWER
mj mj mj mj mj mj mj mj mj
list opioid antagonists - ANSWERNaloxone
mj mj mj mj
Naltrexone - can also use for alcohol abuse, long acting
mj mj mj mj mj mj mj mj mj
Nalmefene - longer acting narcan mj mj mj mj
Methylnaltrexone - doesnt cross cns, good for bowel obs mj mj mj mj mj mj mj mj
list partial agonists
mj mj
drawbacks - ANSWERBuprenorphine - analgesia stronger than morphine
mj mj mj mj mj mj mj
butorphanol - analgesia stronger than morphine mj mj mj mj mj
nalbuphine - good for heart disease mj mj mj mj mj
a local anesthetic with a pka (further, closer) to physiological pH will have a faster
mj mj mj mj mj mj mj mj mj mj mj mj mj mj
onset. - ANSWERcloser to.
mj mj mj mj
3 components of local anesthetic molecule and what they determine? - ANSWER1.
mj mj mj mj mj mj mj mj mj mj mj
benzene ring
mj mj mj
*lipophilicity mj
2. intermediate chain
mj mj
*metabolism, allergy mj
*COC or NH-C mj mj
3. tertiary amine
mj mj
*hydrophilicity; accepts proton mj mj
*weak base mj
, Apex midterm questions and answers
mj mj mj mj
metabolism of esters vs amides mj mj mj mj mj
allergy potential esters vs amides - ANSWEResters: pseudocholin
mj mj mj mj mj mj mj mj
amides: liver cyp450 mj mj
esters: PABA preservative allergy
mj mj mj
*cross sensitivitymj mj
amides: methylparaben mj
local anesthetics are weak ____ that are typically more ____ at phys pH
mj mj mj mj mj mj mj mj mj mj mj mj
what part of the LA exerts the anesthetic action? - ANSWERbases; ionized
mj mj mj mj mj mj mj mj mj mj mj
the charged, ionized component
mj mj mj
**except w/ benzocaine mj mj
Order pkas locals - ANSWERamides have lower pka
mj mj mj mj mj mj mj mj
*bupi, levobupi, ropi: 8.1
mj mj mj
*lido, prilo: 7.9
mj mj
*mepi: 7.6 mj
esters higher mj mj
*procaine 8.9 mj
*chloro 8.7 mj
*tetra 8.5 mj
what is the highest pka of the amides?
mj mj mj mj mj mj mj
what is the highest pka of the esters? - ANSWER8.1
mj mj mj mj mj mj mj mj mj
8.9
max doses amides
mj mj
levobupi, bupi, bupi + epi, ropi, lido, mepi etc - ANSWERlevobupi 150mg (2mg/kg)
mj mj mj mj mj mj mj mj mj mj mj mj
bupi 175 (2.5)
mj mj
bupi + epi 200 (3)
mj mj mj mj
ropi 200 (3)
mj mj
lido 300 (4.5)
mj mj
mepi 400 (7)
mj mj
lido + epi 500 (7)
mj mj mj mj
prilo <70kg: 500/>70kg: 600 (8)
mj mj mj mj
max doses esters - ANSWERprocaine 350-600mg (7mg/kg)
mj mj mj mj mj mj
chloroprocaine 800 (11) mj mj
chloroprocaine + epi 1000 (14) mj mj mj mj
Max dose of Exparel (liposomal bupi)
mj mj mj mj mj