005 - opiod analgesics Flashcards
Compared to Morphine (in regards to potency), how does Codeine compare (more or less)
Less Potent
Compared to Morphine (in regards to potency), how does Oxymorphine compare (more or less)
More Potent
Most potent narcotic analgesic
Etorphine
Because of Etorphine’s high potency it should be antagonized by……
Diprenorphine (similar structural compound. usually used in large animal)
What would be a more commonly used drug to antagonize Etorphine?
Naloxone (pure antagonist)
Why would you use Codeine orally rather than Morphine?
Goes directly to the liver, making Oral Codeine better due to better bio availability
Morphine is sequestered in what part of the body?
Stomach (making it less bioavailable than Codiene)
Oral or I.V. administration of Morphine is more rapidly metabolized?
Morphine more rapidly metabolized in the gut
Compared to Morphine (in regards to potency), how does Butorphanol compare (more or less)
Butorphanol more potent (4-7 x), but less efficacious. Can be used to reverse morphine induced respiratory depression while still providing some analgesia.
Oxymorphone has more or less respiratory depression?
Less
Name the opioid receptor types?
Mu
Delta
Kappa
Morphine interacts best with which opioid receptor subtype?
Mu
Butorphanol interacts best with which opioid receptor subtype?
Kappa
Opioid D and L isomers: Which one has the best analgesic activity?
L sterioisomer
What is the D isomer of Opioids best used clinically for?
D has more anti-tussant activity
Opioids increase or decrease flux of what in the ion channels?
Open K+ channels
Close Ca++ (prevents neurotransmitter release)
Butorphanol produces more or less resp depression and GI effects than morphine?
Less
Which opioid receptor type causes analgesia?
Mu
Delta
Kappa
Which opioid receptor type causes more respiratory depression?
Mu and Delta
Which opioid receptor type causes more diuresis?
Kappa
Long acting, endogenous receptor opioid made in the brain?
Endorphins (in areas in brain linked to HPA axis and cleaved from proopiomelantocortin)
What is an endogenous opioid that is linked to chronic pain?
Dynorphin
Name as many species that are sedated by Morphine?
Rat, rabbits, dogs, cattle, primates, guinea pigs (NOT MICE)
Morphine causes death by….
Respiratory Depression (but c.v. system is not affected as much. Use respirator)
Name an opioid drug used as an anti-tussant compound and not analgesia
Dextromethrophan
Opioids are synergistically potentiated by which two drug categories
Major Tranquilizers
NSAIDS
Opioids affects on g.i. tract (absorption, motility, etc.)
Spasms of sphincters (defecation and vomitting)
Decrease motility
Increase absorption
Leading to very severe constipation
Duration of naloxane compared to morphine (which is shorter, which is longer)
Naloxone is much shorter
To combat respiratory depression caused by Morphine how often would you have to give naloxone?
Check every 20 minutes (Naloxone has no respiratory depressive effects like some other Narcotic Analgesics)
Name two different drug combinations that are referred to neuroloptic drug (trade name and the generic names)
Fentanyl + Droperidol
Etorphine + Acetylpromazine (zoo medicint)
Does naloxone block the anti-tussant effect of codeine?
No (not caused by an opiate receptor and naloxone is not an opiate antagonist)
Do opiates decrease/increase nuerotransmitter release
decrease
What might you give to a horse in a standing surgery position to prevent the excitation effect of morphine?
preanestethic like xylazine
Name two drug combinations ref to as neuroleptic-analgesic compounds
Fentanyl + Droperidol (more used_
Etorphine + Ace (exotics)
Does Naloxone block the antitussive effect of Codeine?
no
Why use codeine rather than morphine?
Morphine has first-pass metabolism and is trapped in gut; codeine can be given orally
Is diprenorphine more or less analgesic than fentanyl?
less
Is diprenorphine more or less analgesic than butorphanol?
less
Opiates increase or decrease NT release?
decrease
What might you give to a horse to prevent the side affects of morphine (standing surgery)?
Preanesthetic like xylazine
What is one negative effect of pentazocine?
Dysphoric