OPIOID AND NONOPIOID ANALGESIA
EXAM 2 QUESTIONS AND 100%
VERIFIED ANSWERS
•The goal of synthetic manufacture of analgesics was the creation of
potent analgesics that would have (3) - ANSWER high specificity for
receptors, were not addictive, and were free of side effects.
•The first attempt to administer an opium vapour by inhalation was
documented in _____ and first administered IV in 1853. - ANSWER
1778
•In 1803, Sertürner reported the isolation of a pure substance from
opium that he named ___________, after Morpheus, the Greek god of
dreams. - ANSWER morphine
•Opioids exert their effects by mimicking naturally occurring
________________________________ or endorphins. - ANSWER
endogenous opioid peptides
Can narcotics provide a full MAC? - ANSWER No - they do not hold
amnesia properties, so will never be a full anesthetic
•Narcotic is derived from the Greek word narkōtikos, meaning
"__________________," and refers to potent morphine-like analgesics
with the potential to produce stupor, insensibility, and dependence. -
ANSWER benumbing
the 1 benxylisoquinoline derivative (naturally occurring opioids) -
ANSWER papaverine
the 2 thebaine derivatives (naturally occurring opioids) - ANSWER
buprenorphine (Subutex) (if you add naloxone to this it becomes
Suboxone)
oxycodone (oxycontin)
the 1 diphenyheptane (methadones) (synthetic) - ANSWER methadone
the 2 benzomorphans (synthetic) - ANSWER pentazocine (Talwin)
phenazocine
he doesnt have any piperidines (synthetic) listed FYI dudeeee -
ANSWER
the 2 anilinopiperidine (synthetic) - ANSWER meperidine (demerol)
loperamide
the 4 phenylpiperidines (synthetic) - ANSWER alfentanil (alfenta)
fentanyl (sublimaze)
,sufentanil (sufenta)
remifentanil (ultiva)
•The properties of opium are attributable to the 20 different isolated
alkaloids, and the alkaloids are divided chemically into two types:
•_____________________ (from which morphine and codeine are
derived)
•_______________________ (from which papaverine, a nonanalgesic
drug, is derived) - ANSWER Phenanthrene
Benzylisoquinoline
•Modification of the morphine molecule with retention of the
_______________ structure results in the semisynthetic drugs heroin
and hydromorphone. - ANSWER five-ring
•The phenylpiperidines (e.g., fentanyl) and the diphenylheptane
derivatives (e.g., methadone) all have only ______ of the original five
rings of the basic morphine molecular structure. - ANSWER two
Morphine releases _______________ - causes vasodilation --- BUT
doesn't cause as much respiratory depression as hydromorphone -
ANSWER histamine
Hydromorphone doesn't release histamine
•A close relationship exists between the stereochemical structure and
_____________ of opioids, with the levo-isomers being the most potent.
•All opioids, despite the diverse molecular structures, share an
__________________ moiety, which seems to confer analgesic activity.
- ANSWER potency
N-methylpiperidine
•Opioid drugs produce pharmacologic activity by binding to opiate
receptors primarily located in the (4) - ANSWER central nervous
system (CNS)
supraspinal and spinal
, several peripheral sites (vasculature, lung, heart, gastrointestinal, and
immune systems).
•Supraspinal analgesia occurs through activation of opioid receptors in
the ____________________ & _____________ (inhibition of neurons
involved in pain pathways). - ANSWER medulla
midbrain
•Spinal analgesia occurs by activation of ______________ opioid
receptors (decreased _______________ influx and decreased release
of neurotransmitters involved in nociception). - ANSWER presynaptic
calcium
•Clinically, supraspinal and spinal opioid analgesic mechanisms are
_______________. - ANSWER synergistic
•In 1975, three such agonists were identified: enkephalins (_______),
endorphins (____), and dynorphins (___________). - ANSWER Delta
Mu
Kappa
•By the early 1980s, three precursor molecules to these agonists were
identified: proenkephalin, pro-opiomelanocortin, and prodynorphin.
•Since then, an additional precursor, pronociceptin, that results in
nociceptin, has been identified.
•Endomorphins __________(2), which are agonists at mu receptors,
have been identified. - ANSWER 1 and 2
•Receptors activated by opiate drugs respond physiologically to
endogenous opioid peptides; they are therefore __________
_____________ _______________, the receptor family being
designated by the two-letter abbreviation OP - what are they? (3) -
ANSWER opioid peptide receptors
MOP, DOP, KOP
Mu opioid receptor
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