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26 Cards in this Set
- Front
- Back
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Narcotics in legalistic terms refers to any illegal drug but in pharmalogical terms, narcotic refers to ______ -inducing agents.
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sleep inducing drug = narcotic
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Differentiate between opium, opiate, and opioid.
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Opium- extract of opuim poppy.
Opiate- drug derived from opium (ex. morphine, codeine) Opioids - any drug or peptide that has opiate like effects via binding to opiate receptors. (ex. endogenous opioids). |
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True or False:
The NSAIDs block the mediators of pain but they don’t block the transmission of pain. |
True.
At site of injury, you get mediators of pain. The NSAIDs block the mediators of pain but they don’t block the transmission of pain. Opiods block the excitation of neuron transmission. All of them have the same mechanism! They just differ in their breakdown products and slightly in pharmacokinetics |
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[ NSAIDs / Opioids ] block the excitation of neuron transmission.
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Opioids.
At site of injury, you get mediators of pain. The NSAIDs block the mediators of pain but they don’t block the transmission of pain. Opiods block the excitation of neuron transmission. All of them have the same mechanism! They just differ in their breakdown products and slightly in pharmacokinetics. |
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Why use NSAIDs and opioids in combo?
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NSAID blocks much of the initial stimuli , thus decreasing the amount of opioid you have to administer to block the pain. The two work synergistically. NSAIDs are usually the first treatment for pain.
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Name some of the endogenous opioids. (6)
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Beta-endorphin, met and leu enkephalin, dynorphin, orphanin FQ (anti-analgesic), endomorphins 1 and 2.
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True or False:
Every single clinically used opioid drug can bind to every single opioid receptor. There are NO selective opioid drugs. |
True
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What endogenous ligands preferentially utilize the Mu1 and Mu2 receptors?
A. beta-endorphins B. Dynorphins C. Endomorphins 1 and 2 D. Leu-Enkephalin and Met-Enkephalin E. Orphanin FQ |
A. beta-endorphins
C. Endomorphins 1 and 2 binding to Mu1 produces: **analgesia** , *euphoria* --> dependence |
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What is the effect of agonist binding to:
A. Mu1 B. Mu2 |
A. Mu1 : ***analgesia*** , *euphoria* --> dependence
B. Mu2 : respiratory depression (aka medullary effect), bradycardia. Mu2 effect is what kills in an overdose situation. |
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What endogenous ligands preferentially bind Kappa 1, 2 and 3 receptors?
A. beta-endorphins B. Dynorphins C. Endomorphins 1 and 2 D. Leu-Enkephalin and Met-Enkephalin E. Orphanin FQ |
B. Dynorphins
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What endogenous ligands preferentially bind Delta 1 and 2 receptors?
A. beta-endorphins B. Dynorphins C. Endomorphins 1 and 2 D. Leu-Enkephalin and Met-Enkephalin |
D. Leu-Enkephalin and Met-Enkephalin
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What endogenous ligands preferentially bind Epsilon receptors?
A. beta-endorphins B. Dynorphins C. Endomorphins 1 and 2 D. Leu-Enkephalin and Met-Enkephalin |
A. beta-endorphins
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True or False:
All opioid receptors are G-protein coupled receptors. |
True
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Which opioid agonist is utilized for severe pain and is DOC for pain associated with MI?
A. Codeine B. Fentanyl C. Morphine D. Oxycdone |
C. Morphine
Other drugs used for moderate to severe pain but is NOT a DOC for MI pain are: oxycodone. |
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Morphine is best administered IV, IM, or epidurally. Why?
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Has a high "first pass" effect and thus not given orally.
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Given the following metabolites, list the agent they come from.
A. morphine-6-glucuronide B. normeperidine C. mono-demethyl tramadol D. 6-beta-naltrexol |
A. morphine
B. meperidine (this metab is a proconvulsant and hallucanagen) C. tramadol (active as potent analgesic) D. naltrexone (this metab is a pure opioid antagonist too) |
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Name the three opioid agonists and one opioid antagonist that has an active metabolite.
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Morphine: morphine-6-glucuronide
Meperidine: normeperidine (proconvulsant and hallucinogneic metabolite!) Tramadol : mono-demethyl tramadol (potent analgesic metabolite) Naltrexone: 6-beta-naltrexol |
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Which opioid agonist is 80-100x more potent than morphine?
A. Codeine B. Fentanyl C. Meperidine D. Oxycdone |
B. Fentanyl
A. Codeine (10-12x less) C. Meperidine (8-10x less) D. Oxycdone (not mentioned) |
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What opioid agonist is equally potent to morphine and is orally active with a long onset and long offset?
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Opioid abstinence drug Methadone
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Which of the following was removed from the market due to high toxicity with alcohol consumption due to the acetaminophen inside it?
A. Meperidine B. Pentazocine C. Propoxyphene D. Talwin |
C. Propoxyphene (Darvocet)
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Which opioid agonist is utilized for moderate to severe pain around the clock (not as a PRN drug!)
A. Fentanyl B. Hydrocodone C. Methadone D. Oxycodone E. Tramadol |
D. Oxycodone
Fentanyl is for chronic pain but no mention of severity. Hydrocodone is analgesic and antitussive no mention of severity. |
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Which is not for use in patients immediately after surgery due to the risk of depressed respiration?
A. Codeine B. Fentanyl C. Meperidine D. Oxycdone |
B. Fentanyl
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Pentazocine and buprenorphine are mixed agonist antagonist opioids. What does that mean and what are their effects?
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These are potent analgesics in opioid-naïve patients but precipitate withdrawal in patients that are currently physically dependt on opioids.
Pentazocine: morphine-like: analgesic, respiratory depression ; non-morphine-like: increased HR and BP, increased NE release. Buprenorphine: more potent than morphine orally as an analgesic |
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What opioid related drug would be contrindicated for patinets with MI, epileptic patients, head trauma patients and those with psychoses?
A. Buprenorphine B. Fentanyl C. Oxycodone D. Pentazocine |
D. Pentazocine
Fentanyl shouldn't be given to pts right after surgery. Oxycodone shouldn't be given to those with renal or kidney impairments. |
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Pentazocine and buprenorphine are mixed agonist antagonist opioids. What does that mean and what are their effects?
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These are potent analgesics in opioid-naïve patients but precipitate withdrawal in patients that are currently physically dependt on opioids.
Pentazocine: morphine-like: analgesic, respiratory depression ; non-morphine-like: increased HR and BP, increased NE release. Buprenorphine: more potent than morphine orally as an analgesic |
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What opioid related drug would be contrindicated for patinets with MI, epileptic patients, head trauma patients and those with psychoses?
A. Buprenorphine B. Fentanyl C. Oxycodone D. Pentazocine |
D. Pentazocine
Fentanyl shouldn't be given to pts right after surgery. Oxycodone shouldn't be given to those with renal or kidney impairments. |
