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