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48 Cards in this Set

  • Front
  • Back
­ specialized sensory receptor cells that are activated by noxious inputs to peripheral tissues
nocireceptors
inflamation causes which pain
nocireceptor
burning or an electric sensation
neuropathic pain
hypersensitivity to noxious stimuli
hyperalgia
hypersensititvity to an innocuous
allodynia
myelinated and mediate fast, sharp pain
A
unmyelinated and mediate slow burning and dull pain.
C fibers
how many months for neuropathic pain to be established as neuro
6mo
what opioids are for
Analgesic /cough/ diarrhea/ acute pulmonary edema/ air hunger/ opiod overdose
what nsaids are for
Analgesic, Antipyretic, Anti inflammatory, Overdose-variable, Salicylates-CNS excitation,

Acetaminophen-liver toxicity
where are OH groiups on morphine
3 and 6
cns depressant
what can codiene cause in kids?
seizures
codeine CH3 is where
3
order of strength / ease crossing BBB
­ HEROIN> CODEINE> MORPHINE
where is codeine and heroin converted to ...
morphine in LIVER
morphine exreted in .. how?
KIDNEY

GLUCURONIDATION

6-glucuronyl-morphine
3 is inactive

Both 3 and 6 glucuronyl-morphine forms are excreted by the kidney.
morphine binding site
MU
MU does what?
therapeutic and adverse effects of opioids

o Analgesia,
euphoria,
respiratory depression,
miosis,
decreased GI motility,
physical dependence
■ NE and 5-HT on spinal interneurons that inhibit transmission of pain
descending inhibition
pre post nocireceptors act how
■ decrease the action potentials in nociceptive neurons reducing release of glutamate and substance P.
■ decrease the responses of the dorsal horn interneurons by activating K+ channels and hyperpolarizing the interneuron
3d way morphine works
) reduced emotional reaction to pain mediated through the limbic system
why is morphone PCA admin
so pts cant feel IM and "get better now" always used to be ok and wotn have withdrawl
: lacks other opioid activities “Robitussin DM” (may interact with MAOI's)
o Cough suppression: oral; depression of cough reflex centrally
dextromethorphan
to decrease abuse
o Antidiarrheal effect: oral; increases GI muscle tone, delays gastric emptying, reduces peristaltic activity
diphenoxylate
OTC, poorly absorbed, low abuse potential
o Antidiarrheal effect: oral; increases GI muscle tone, delays gastric emptying, reduces peristaltic activity
Loperomide
TOXICITY
PHYS DEPENDANCE worst at 2 days past last dose
­
­ Tolerance
o Remain constipated and miotic
respiraroty depression
.
■ Must ventilate patients, sleepy
­
Nausea vomiting, mess with CTZ zone activate vomit center
­ CNS stimulates SEIZURES on codeine and children
GI reduced motility and constipation. Biliary colic
­ GU – increased tone in bladder sphincter, urinary retention
. Pinpoint pupils
miosis
eyes overdoise of opioid
less potent than morphine, but higher PO bioavailability.
2. Prodrug that must me metabolized to morphine
3. Primary use is antitussive. Second line analgesic, usually combined with an NSAID.
codeine
why is meperidine good in OB
­ Shorter half life, good in OB bc doesn’t prolong labor
meperidine is metabolized to what and where
LIVER
to NORMEPERIDINE
causes what?
­ in liver which has long half life and toxic can cause seizures.

Problem in renally compromised pts
why is meperidine abused by healthcare workers
antimuscarinic effect, no pinpoint pupils
meperidine has fatal reactions with what drugs
MAOIS!!!!
why is meperidine good for pancreatitis
less sphincter of odi contraction
­ 80x more potent then morphine.
­ Anathesia + droperidol
­ Spinal and epidural anathesia
­ Available in patch for severe pain
FENANYL
­ Mixed with acetaminophen
­ Moderate opioid agonist
hydrocodone
­ a semisynthetic opioid derived from thebane
­ ORAL combined with aspirin or Tylenol
­ As effective as morphine
oxycodone
how is oxycodone metabolized
in liver

excretion in KIDNEYS
­ MU recepot agonist
­ Inhibits reuptake of SE and NE – pain transmission
­ Seizures
TRAMADOL
mixed agonists are bettte why
LESS RESPIRATORY DEPRESSION
mixed agonist resistant to nalaxone
buprenorphine
o sublingually effective (lollipops)
o 25-50x more potent than morphine
o partial  agonist.
o Ceiling effect on resp depression and analgesia
o RESISTANT TO NALAXONE tx bc slowly comes off receptor s
o Recently approved for therapy of opioid dependence. Also used for migraines (nasal spray).
buprenirphine
"pure" competitive opioid antagonist
o reverses acute opioid toxicity
o Used IV or IM to reverse acute opioid intoxification
o Complete first pass effect so not useful orally
NALAXONE
NALAXONE admin which wa
IM or IV - short half life
first pass 100%
o Can be ORAL
o LONGER HALF LIFE – 10 hrs
o Useful in smokers and addicts ?
o Heroin effects blocked for 48 hrs
NALTREXONE
antagonist