Download Name ______________________________ CH 204, Fall 2014 Assignment 8 – Opioids

Name ______________________________
CH 204, Fall 2014
Assignment 8 – Opioids
Refer to the Julien textbook and class notes as needed.
1) Which of the following opioid drugs is not derived from the Papaver plant?
a.
b.
c.
d.
Thebaine
Naltrexone
Naloxone
Meperidol
2) The naturally occurring opioids can be isolated from the poppy seed pod exudate by:
a.
b.
c.
d.
e.
Extraction into aqueous acid
Extraction into aqueous base
Extraction into water
All of the above
None of the above
3) Heroin is obtained from morphine via what general type of reaction?
a.
b.
c.
d.
Alkylation
Etherification
Esterification
Amide bond formation
4) Heroin is a pro-drug of morphine, metabolized in vivo via two
hydrolysis reactions. Considering the active component of
heroin is morphine, briefly indicate why heroin is two to four
times a more potent drug.
5) Specifically, how can urinalysis distinguish between heroin
and other opioid use, if heroin (as well as codeine) is
metabolized in vivo to the Schedule II painkiller morphine?
6) Which of the following receptors is the target of all clinically used opioid analgesics?
a.
b.
c.
d.
MOP
KOP
DOP
NOP
7) Upon binding of morphine to its receptor, a series of downstream signaling events occur leading to
the opening of K+ channels. Based on the concentration gradient, determine which direction K+ ions
flow. As a result, the affected neurons become:
a. Depolarized
b. Hyperpolarized
c. The resting potential of -70 mV remains unchanged
8) In addition to opening of K+ channels, binding of opioid agonists to their receptors causes inhibition
of what ion to flow through its channels?
a.
b.
c.
d.
Na+
ClMg2+
Ca2+
9) The euphoria associated with opioids is attributed to the downstream effect of increased dopamine
release in the brain’s reward pathway (ventral tegmental area -> nucleus accumbens -> prefrontal
cortex). This occurs through inhibition of which neurotransmitter pathway?
a.
b.
c.
d.
Glutamate
GABA
Serotonin
Norepinephrine
10) Most opioids are metabolized by CYP2D6 and CYP3A4, though up to 20-30% of patients have genetic
differences in their production these enzymes. These patients may be rapid metabolizers, and thus
not experience adequate analgesia. Alternatively, some may have insufficient enzyme levels,
resulting in drug accumulation. Which of the following analgesics is metabolized primarily through
glucuronidation, versus CYP-oxidation, allowing more predictable pharmacokinetics in its use
amongst patient populations?
a.
b.
c.
d.
Oxycodone
Hydromorphone
Methadone
Fentanyl
11) Indicate the most serious acute side effect of opioid overdose,
resulting in numerous fatalities.
12) What drug is used as an antidote for opioid overdose? Note this
for use in emergency situations, not as a long-term opioid
deterrent.
13) Which of the following effects is observed upon opioid withdrawal?
a.
b.
c.
d.
Vasodilation
Decreased blood pressure
Hypothermia
Pupillary dilation
14) Prescription cough syrups may contain the antitussive
codeine phosphate or codeine sulfate. Briefly indicate why
codeine is marketed in these forms versus its free base
form for use in cough syrup.
15) Two of the metabolic pathways that codeine undergoes include CYP2D6-catalyzed dealkylation to
morphine, and UGT-catalyzed glucuronidation to codeine-6-glucuronide. A person who is taking
diphenhydramine while on codeine may have:
a. Increased levels of morphine
b. Decreased levels of morphine
c. No effect on metabolism is expected
16) Recently, Vicodin® and other hydrocodone/acetaminophen products have been reclassified as
Schedule II. One of the risks of overdose of any acetaminophen-containing drug is liver toxicity, due
to the reactive metabolite generated from acetaminophen,
NAPQI. Indicate what antidote may be given to a person who
has overdosed on acetaminophen.
17) Which of the following is the most potent opioid used for pain in humans?
a.
b.
c.
d.
Hydrocodone
Oxycodone
Fentanyl
Etorphine
18) Methadone is a synthetic full-agonist of the mu-opioid
receptor. It has been administered since 1965 as a
substitute for opioid dependency. Indicate an important
pharmacokinetic parameter of methadone that differs
from heroin, facilitating its use in maintenance therapy.
More than one answer is possible.
19) Currently in the United States, more patients receive buprenorphine than methadone for opioid
dependence. Buprenorphine is a Schedule III drug, versus methadone which is Schedule II, so
patients have increased access. Buprenorphine acts at the mu opioid receptor as a:
a.
b.
c.
d.
Full agonist
Partial agonist
Antagonist
Inverse agonist
20) Suboxone® is a combination product of buprenorphine and naloxone (4:1), which is less liable to
abuse. Naloxone acts at the mu opioid receptor as a:
a.
b.
c.
d.
Full agonist
Partial agonist
Antagonist
Inverse agonist