PHC 722 Exam 1 (Final Exam) questions
well answered passed
Invention of new drugs - phase 1 - correct answer ✔✔first in human
- 10-100 participants
- usually healthy volunteers (sometimes patients with advanced or rare disease)
- open label
- safety and tolerability
invention of drugs - phase 2 - correct answer ✔✔first in patient
- 50-500 participants
- patient-subjects receiving experimental drug
- randomized and controlled (can be placebo controlled); may be blinded
- efficacy and dose ranging
invention of drugs - phase 3 - correct answer ✔✔multisite trial
- few hundred to a few thousand participants
- patient-subjects receiving experimental drugs
- randomized and controlled (can be placebo-controlled) or uncontrolled, ; may be blinded
- confirm efficacy in larger population
invention of drugs - phase 4 - correct answer ✔✔postmarketing surveillance
- many thousands of participants
- patients in treatment with approved drug
- open label
- adverse events, drug-drug interaction
,Lecture 3 - correct answer ✔✔Opioid Analgesics and Antagonists
opium powder, when dry and powdered, contains... - correct answer ✔✔5-20% morphine and 0.5-2.5%
codeine
two natural alkaloids - correct answer ✔✔codeine and morphine
hydrocodone and oxycodone are metabolized where and to what? - correct answer ✔✔in the body
- hydromorphone
- oxymorphone
natural alkaloids - correct answer ✔✔prototypic
opioid analgesics
- morphine and codeine
semisynthetic drugs - correct answer ✔✔congeners of morphine - similar structure to morphine
- hydrocodone and oxycodone
entirely synthetic drugs - correct answer ✔✔opioid analgesics
- meperidine (pethidine)
- methadone
- pentazocine
- fentanyl (many conjugates)
opioid receptors - correct answer ✔✔mu, kappa, delta
seven membrane spanning alpha helical segments, G protein coupled
,where does the analgesic effect of opioids come from? - correct answer ✔✔from activation of MOR (mu
opioid receptors)
opioid analgesics --> all of it is mediated by mu receptors
primary site of action for opioids - correct answer ✔✔cingulate and insular cortex
- affective motivational (aversive) aspect of pain (discomfort and unpleasantness)
T/F: opioids are effective at spinal cord level and beginning of nociceptive pathway to brain (terminal
ends) - correct answer ✔✔TRUE
morphine mechanism of action - correct answer ✔✔binding to and activation of MOR, which results in
- inhibition of adenylyl cyclase, calcium influx, and neurotransmitter release
- activation of K+ currents
therapeutic effects/indications of morphine - correct answer ✔✔symptomatic relief of pain (highest
efficacy known)
- without influencing its underlying cause (because they block at central level)
- without impeding reflex responses to noxious stimuli (withdrawal reflex)
sedation/perioperative procedures
somnolence/sleeplessness caused by pain or coughing
antitussive (decreased cough reflex; codeine in cough preparations)
antidiarrheal
efficacy and potency of opioids - correct answer ✔✔they all act through mu receptors so their efficacy is
the same, but the potency is different
, strongest blockade of pain transmission - correct answer ✔✔activation of mu opioid receptors
most serious adverse effect of opioids - correct answer ✔✔respiratory depression
adverse effects of opioids - correct answer ✔✔RUNCAPED
respiratory depression (tidal volume and rate; dose dependent; life threatening); orthostatic
hypotension
- depth of breathing is shallow and lower
urinary retention
nausea (central and vestibular components); vomiting (initially, then suppression of emesis)
constipation and gastrointestinal spasm, including biliary tract
analgesic tolerance, physical dependence, psychological dependence-addiction (some patients)
pupillary constriction (miosis; central effect on CN III; no appreciable tolerance)
euphoria (majority) or dysphoria (smaller percentage)
drowsiness
at doses that produce equivalent analgesia... - correct answer ✔✔the incidence of adverse effects is
similar among the opioid agonists
how can morphine be administered? - correct answer ✔✔by virtually any route
well answered passed
Invention of new drugs - phase 1 - correct answer ✔✔first in human
- 10-100 participants
- usually healthy volunteers (sometimes patients with advanced or rare disease)
- open label
- safety and tolerability
invention of drugs - phase 2 - correct answer ✔✔first in patient
- 50-500 participants
- patient-subjects receiving experimental drug
- randomized and controlled (can be placebo controlled); may be blinded
- efficacy and dose ranging
invention of drugs - phase 3 - correct answer ✔✔multisite trial
- few hundred to a few thousand participants
- patient-subjects receiving experimental drugs
- randomized and controlled (can be placebo-controlled) or uncontrolled, ; may be blinded
- confirm efficacy in larger population
invention of drugs - phase 4 - correct answer ✔✔postmarketing surveillance
- many thousands of participants
- patients in treatment with approved drug
- open label
- adverse events, drug-drug interaction
,Lecture 3 - correct answer ✔✔Opioid Analgesics and Antagonists
opium powder, when dry and powdered, contains... - correct answer ✔✔5-20% morphine and 0.5-2.5%
codeine
two natural alkaloids - correct answer ✔✔codeine and morphine
hydrocodone and oxycodone are metabolized where and to what? - correct answer ✔✔in the body
- hydromorphone
- oxymorphone
natural alkaloids - correct answer ✔✔prototypic
opioid analgesics
- morphine and codeine
semisynthetic drugs - correct answer ✔✔congeners of morphine - similar structure to morphine
- hydrocodone and oxycodone
entirely synthetic drugs - correct answer ✔✔opioid analgesics
- meperidine (pethidine)
- methadone
- pentazocine
- fentanyl (many conjugates)
opioid receptors - correct answer ✔✔mu, kappa, delta
seven membrane spanning alpha helical segments, G protein coupled
,where does the analgesic effect of opioids come from? - correct answer ✔✔from activation of MOR (mu
opioid receptors)
opioid analgesics --> all of it is mediated by mu receptors
primary site of action for opioids - correct answer ✔✔cingulate and insular cortex
- affective motivational (aversive) aspect of pain (discomfort and unpleasantness)
T/F: opioids are effective at spinal cord level and beginning of nociceptive pathway to brain (terminal
ends) - correct answer ✔✔TRUE
morphine mechanism of action - correct answer ✔✔binding to and activation of MOR, which results in
- inhibition of adenylyl cyclase, calcium influx, and neurotransmitter release
- activation of K+ currents
therapeutic effects/indications of morphine - correct answer ✔✔symptomatic relief of pain (highest
efficacy known)
- without influencing its underlying cause (because they block at central level)
- without impeding reflex responses to noxious stimuli (withdrawal reflex)
sedation/perioperative procedures
somnolence/sleeplessness caused by pain or coughing
antitussive (decreased cough reflex; codeine in cough preparations)
antidiarrheal
efficacy and potency of opioids - correct answer ✔✔they all act through mu receptors so their efficacy is
the same, but the potency is different
, strongest blockade of pain transmission - correct answer ✔✔activation of mu opioid receptors
most serious adverse effect of opioids - correct answer ✔✔respiratory depression
adverse effects of opioids - correct answer ✔✔RUNCAPED
respiratory depression (tidal volume and rate; dose dependent; life threatening); orthostatic
hypotension
- depth of breathing is shallow and lower
urinary retention
nausea (central and vestibular components); vomiting (initially, then suppression of emesis)
constipation and gastrointestinal spasm, including biliary tract
analgesic tolerance, physical dependence, psychological dependence-addiction (some patients)
pupillary constriction (miosis; central effect on CN III; no appreciable tolerance)
euphoria (majority) or dysphoria (smaller percentage)
drowsiness
at doses that produce equivalent analgesia... - correct answer ✔✔the incidence of adverse effects is
similar among the opioid agonists
how can morphine be administered? - correct answer ✔✔by virtually any route
