Term
| What type of tissue damage causes pain? (stupid question) |
|
Definition
| both actual and potential |
|
|
Term
| What type of pain is caused by tissue damage? |
|
Definition
|
|
Term
| What type of pain is caused by nerve damage? |
|
Definition
|
|
Term
| What type of pain (nociceptive or neuropathic) responds better to opioids? |
|
Definition
|
|
Term
| What two locations on the morphine molecule are important for its metabolism and analgesia? |
|
Definition
|
|
Term
| What happens when you change the 3 or 6 hydroxyl groups of the morphine structure? |
|
Definition
| decreases its metabolism by the liver |
|
|
Term
| How do morphine and naloxone differ in molecular structure? |
|
Definition
|
|
Term
| What is the purpose of thebaine if it is an inactive opioid? |
|
Definition
| thebaine is one of the drugs in the steps to make oxycodone (hydroxylated opioid) |
|
|
Term
| What drug is an intermediate in the production of oxycodone? |
|
Definition
|
|
Term
| How is the structure of heroin different than morphine? |
|
Definition
| it has two CH3 groups. one at 3 and one at 6 |
|
|
Term
| What illegal drug is inactive but can be converted to morphine easily? |
|
Definition
|
|
Term
| What is the difference in structure between codeine and morphine? |
|
Definition
| codeine has a 3 CH3 group that makes it less metabolized and less analgesic than morphine |
|
|
Term
| What is another name for methylmorphine? |
|
Definition
|
|
Term
| What is true of the ADME of opioids? |
|
Definition
absorbed well by all routes
Distributed to all metabolic tissues (less in the brain)
Metabolized by liver (glucoronidation)
polar compound after glucoronidation is excreted |
|
|
Term
| What does the liver do to morphine in metabolizing it? |
|
Definition
| glucoronidation into a polar molecule |
|
|
Term
| What are the nine effects of morphine? |
|
Definition
analgesic (Euphoria)
respiratory depression
miosis
GI depression
Urinary retention
Cardiovascular (orthostatic hypertension)
Sphincter of Oddi contraction
Antitussive
Emesis
|
|
|
Term
| How does morphine cause emesis? |
|
Definition
| it crosses into CTZ center to stimulate nausea/vomit |
|
|
Term
| What effects of morphine can one become tolerant to (2)? |
|
Definition
analgesia
Respiratory depression |
|
|
Term
| What can't an individual become tolerant to with respect to morphine's effects? |
|
Definition
|
|
Term
| What effect of morphine can easily be examined in a patient that you want to check complient of morphine use? |
|
Definition
|
|
Term
| What type of pain is relieved better with morphine? |
|
Definition
|
|
Term
| What does morphine do for more sharp pain? |
|
Definition
| it still reduces it like dull pain but does not totally get rid of it |
|
|
Term
| How does morphine cause analgesia? |
|
Definition
| by euphoria (making one feel well and tranquil) |
|
|
Term
|
Definition
|
|
Term
| How is emesis exacerbated in using morphine? |
|
Definition
|
|
Term
| What is the cardiovascular effect (hypertension) of morphine due to? |
|
Definition
| vasodilation secondary to histamine release |
|
|
Term
| What cardiovascular symptom is experienced with the use of morphine? |
|
Definition
| orthostatic hypertension/fainting |
|
|
Term
| How is the respiratory drive supressed with the use of morphine? |
|
Definition
| the central chemoreceptors lose senstivity causing the respiratory system to respond to peripheral hypoxia at the carotid body instead; therefore the respiratory system will not activate at the higher levels of CO2 and you become acidotic |
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|
Term
| What does the increased CO2 secondary to the decreased respiratory drive cause in addition to acidosis? |
|
Definition
| causes autoregulation in the CNS leading to vasodilation and increased intercranial pressure |
|
|
Term
| What part of breathing is supressed by morphine (voluntary or involuntary)? Why is this important? |
|
Definition
involuntary
this is important because you can reduce the respiratory effects (increased ICP and acidosis) by getting them to voluntary breath off the CO2 |
|
|
Term
| With the use of morphine what can make the respiratory depression worse? |
|
Definition
| others CNS acting drugs (ETOH, benzos, Barbituates) |
|
|
Term
| What type of patient do you not want to give morphine to? |
|
Definition
|
|
Term
| What drug specifically takes advantage of the antitussive effect of morphine by changing the structure of morphine? |
|
Definition
|
|
Term
| What is the use for dextromethorphen? |
|
Definition
| antitussive (cough supressant) |
|
|
Term
| At what location does morphine have its antitussive effect? |
|
Definition
| at the pulmonary receptors |
|
|
Term
| How does morphine cause miosis? |
|
Definition
| stimulating parasympathetic fibers |
|
|
Term
| What three effects are seen in morphine's GI actions? |
|
Definition
increases anal sphincter tone
decreases peristalsis --> diarrhea
decreases awareness to GI stimului |
|
|
Term
| How does morphine effect the bladder? |
|
Definition
| it contracts the detrosor muscle while at the same time contracting the urinary sphincter |
|
|
Term
| How does morphine make biliary colic worse? |
|
Definition
| contraction of the sphincter of oddi |
|
|
Term
| What are the three signs of a morphine overdose? |
|
Definition
pinpoint pupils
coma
depressed respiration |
|
|
Term
| What three receptors does morphine bind to? |
|
Definition
|
|
Term
| How do you treat codeine overdose? |
|
Definition
|
|
Term
| What three general areas of the brain does morphine bind to? |
|
Definition
limbic system
reward system
pain pathway |
|
|
Term
| What is a major difference between the μ and κ receptor effects? |
|
Definition
| μ will have analgesic effects at supraspinal regions and cause euphoria whereas κ will produce dysphoria and just spinal analgesia |
|
|
Term
| What are three endogenous stimuli for the morphine receptors? |
|
Definition
endorphin
enkephalin
dynorphin |
|
|
Term
| Which morphine receptor does not produce any effect? |
|
Definition
|
|
Term
| Where do the opioids have there effects specifically on nerves? |
|
Definition
both presynaptically by increasing G-protein Gi that inhibits Ca influx (primary neuron)
and postsynaptically by hyperpolarizing (secondary neuron) |
|
|
Term
| What do opioids do to secondary neurons? |
|
Definition
| they hyperpolarize them to reduce the transmission |
|
|
Term
| How do opiods effect primary neurons? |
|
Definition
| they active an inhibitory G protein to reduce Ca influx and thus decrease neurotransmitter release from presynaptic neuron |
|
|
Term
| Why does morphine not have very good oral efficacy? |
|
Definition
| because it is greatly reduced by first pass in the liver by glucoronidation |
|
|
Term
| What is heroin converted to first prior to being converted to fully active morphine? |
|
Definition
|
|
Term
| What makes methadone a great drug to begin getting someone off heroin addiction? |
|
Definition
| it is less intense, longer acting, and slower onset |
|
|
Term
| Why don't addicts like to use methadone? |
|
Definition
| because it is oral and psycologically is different |
|
|
Term
| What are the initial signs (w/in hours) of opioid withdrawal? |
|
Definition
|
|
Term
| What are the main signs of opiod withdrawal in 8-16 hours (5)? |
|
Definition
lacrimation
sweating
rhinorrhea
mydriasis
anorexia |
|
|
Term
| What are six signs of opoid withdrawal in 36 hrs? |
|
Definition
muscle twitching
cramps
V/N/D
weakness
chills
increased vital signs (BP, Respiratory rate, temp) |
|
|
Term
| After how many hours do opioid withdrawals symptoms usually peak? |
|
Definition
|
|
Term
| How long does an opioid withdrawal usually last? |
|
Definition
|
|
Term
| What is true of the withdrawal symptoms of opioids versus ETOH or barbituates? |
|
Definition
| it is not life threatening (specifically no seizures) |
|
|
Term
| What makes a particular opioid have a more severe withdrawal? |
|
Definition
the longer the half life the less intense but more prolonged
the shorter the half life (morphine) the more intense |
|
|
Term
| What are the 5 strong opioid agonists in this lecture? |
|
Definition
morphine
fentanyl
heroin
methadone
merperidine |
|
|
Term
| What are the four mild-moderate opioid agonists of this lecture? |
|
Definition
CHOP
codeine
hydrocodone
oxycodone
prropoxyphene |
|
|
Term
| What are the three mixed action opioid drugs discussed in this lecture? |
|
Definition
pentazocine
butorphanol
buprenorphin |
|
|
Term
| What are the two opioid antagonists discussed in this lecture? |
|
Definition
|
|
Term
| What drug offers the same effect as morphine except for the GI, urinary, and biliary effects? |
|
Definition
|
|
Term
| What drug leads to the excitatory syndrome when given in large doses? |
|
Definition
|
|
Term
| If meperidine is given in large doses what can it cause? |
|
Definition
|
|
Term
| What are some (3) clinical characteristics of the excitatory syndrome? |
|
Definition
tremors
hyperreflex
and dilated pupild |
|
|
Term
| A patient comes to you who took a large dose of particular opioid, but she was not sure the name. She is showing signs of tremor, hyperreflex, and dilate pupils (mydriasis). What drug did she probably take? |
|
Definition
|
|
Term
| What type of patients can you not use meperidine for? Why? |
|
Definition
| cannot use meperidine for pain patients that need it for long term b/c it is readily converted to normeperidine by N-demethylation. normeperidine has a very long half life. |
|
|
Term
| What is normeperidine and how is it produced? |
|
Definition
| it is the product of N-demethylation of meperidine |
|
|
Term
| What is true of the potency of fentanyl compared to morphine? |
|
Definition
| it is 80x more potent than morphine |
|
|
Term
|
Definition
|
|
Term
| What protects codeine from fast metabolism? |
|
Definition
|
|
Term
| What gene polymorphism leads to different metabolism of codeine? |
|
Definition
|
|
Term
| What ethnicity has slow metabolism of codeine? |
|
Definition
|
|
Term
| Which type of metabolizers of codeine are at greater risk of overdosing? Ultra rapid metabolism, or slow? |
|
Definition
| ultrarapid becuase it will be converted to morphine faster by CYP2D6 |
|
|
Term
| How does codeine become active? What does it convert to initially? |
|
Definition
| converts to morphine in the liver by CYP2D6 |
|
|
Term
| What age group does not have CYP2D6, what clinical implication does this have? |
|
Definition
| neonates...so dont give codeine to them |
|
|
Term
| How is hydrocodone given always? |
|
Definition
| with another drug (acetaminaphine or ibuprofen) |
|
|
Term
| What is darvon the trade name for? |
|
Definition
|
|
Term
| What opioid drugs have been associated with ototoxicity? |
|
Definition
| some of the mild-moderate opoids most specifically vicodin (hydrocodone+acetaminaphin) |
|
|
Term
| What is pentazocine (what is its activity at receptors)? |
|
Definition
| a weak antagonist of μ and an agonist of κ |
|
|
Term
| What side effect does increased doses of pentazocine not induce when compared to morphine? |
|
Definition
| decreased respiratory drive is not seen with pentazocine |
|
|
Term
| What unique type of patients can you not give pentazocine in due to a side effect? |
|
Definition
| cardiac patients b/c it increases work of the heart |
|
|
Term
| What cardiac effects does pentazocine have? |
|
Definition
|
|
Term
| Due to the fact that pentazocine is a μ antagonist what can it cause if given to a opioid dependent patient? |
|
Definition
| it can cause a withdrawal |
|
|
Term
| What is pentazocine combined with in the oral form and why? |
|
Definition
| it is combined with naloxone (Talwin-NX) to prevent abuse |
|
|
Term
| What is the reason behind given Talwin-NX? |
|
Definition
| In giving oral talwin NX you are given pentazocine with a small does of naloxone. So when you take talwin-NX orally, the naloxone is metabolized by first pass and has not antagonistic effect. However, if you were to abuse the drug and change its form to enable it to be injected, you would not have the benefit of first pass and it would induce a withdrawal symptom |
|
|
Term
| What are two uses for naloxone? |
|
Definition
| it is used for reversal of overdose and used to determine if a suspected individual is abusing opioids (will cause an acute withdrawal syndrome for up to 2 hours in a positive abuser) |
|
|
Term
| What mixed opioid is more potent and longer lasting than morphine? |
|
Definition
|
|
Term
| What is buprenorphine derivied from? |
|
Definition
|
|
Term
| WHat is the difference in administration of naloxone and naltrexone? |
|
Definition
| naltrexone can be administered orally |
|
|
Term
| What is the use of naltrexone? |
|
Definition
| it is great for highly motivated past opioid abusers who are afraid that they may try opioids and dont want to lose all their work in detoxing |
|
|
Term
| Which has a higher length of duration? Naltrexone or Naloxone? |
|
Definition
|
|
Term
|
Definition
|
|
