Opioids Flashcards
List the main pharmacological effects of opioids.
Analgesia
Sedation
Excitation
Bradycardia
Respiratory depression
Nausea/vomiting/decreased GI motility
Antitussive?
Urinary/pupillary effects
Describe full agonists and give two examples.
Bind to and activate a receptor with the maximum response that an agonist can elicit at that receptor
Methadone and fentanyl
Describe partial agonists and give an example.
Bind to and activate a receptor but only have partial efficacy, even if they bind to all receptors
Buprenorphine
Give an example of a mixed agonist-antagonist.
Butorphanol
Give an example of an antagonist.
Naloxone
Which type of opioid is most associated with analgesia?
Mu agonists
Full mu agonists provide the most effective analgesia
By what routes can be opioids be administered?
IM
IV
SC
OTM/buccal
Transdermal
Epidural/spinal
Why are opioids not useful when administered orally?
Significant first pass metabolism resulting in poor oral bioavailability
What are the (dis)advantages of IV opioids?
A = rapid onset of action, reliable uptake, painless (regardless of volume)
DA = Need IV access
What are the (dis)advantages of IM opioids?
A = reliable uptake
DA = Painful (large volumes)
What are the (dis)advantages of SC opioids?
A = easy to perform
DA = unreliable uptake
What are the (dis)advantages of OTM opioids?
A = easy to perform
DA = Only certain opioids
What are the (dis)advantages of transdermal opioids?
A = good for chronic use
DA = no licensed products
What are the (dis)advantages of epidural/spinal opioids?
A = very effective analgesia (mostly intra-op)
DA = No licensed products, technically difficult
List some ultra-short-acting (mins) opioids.
Fentanyl
Alfentanil, Sufentanil, Remifentanil