Sedatives Analgesia Part 3 opioids Flashcards
Opioids have what analgesic effect on nociception?
- Perception
- Modulation
- Transduction
What are the 3 types of opioid receptors?
-Mu (u), Kappa (k) and Delta
Where are the locations of opioid receptors?
- Brain: thalamus, limbic system, amygdala, corpus striatum, hypothalamus, pituitary gland
- Spinal cord: Dorsal horn (substantia gelatinosa)
Describe Mu receptors
- Most common and most affected by opioid drugs
- Brain, spinal cord, joint capsules
- Supraspinal analgesia (u1)
- Spinal analgesia (u2)
- Resp. depression (u2)
- Euphoria
- Sedation
- GI motility
- Physical dependence
Describe Kappa (k) receptors
- Weakly affected by opioid drugs
- Brain and spinal cord
- Spinal/supraspinal sedation
- Analgesia/antinociception
- Dysphoria
- GI Motility
Which opioids are full Mu Agonist (affinity and activity)
- Morphine
- Oxymorphone
- Hydromorphone
- Methadone
- Fentanyl
- Remifentanil
Which opioids are full Mu antagonist
-Naloxone
Which opioids are partial Mu agonist (affinity and only partial activity)
-Buprenorphine (ceiling effect)
Which opioids are mixed agonist-antagonist -> K agonist and Mu antagonist (affinity and no activity)
-Butorphanol
Which opioids are considered special opioids
- Tramadol
- Hydrocodone
Which opioids are Schedule II controlled drugs
Most full Mu agonist (morphine, fentanyl) and oral drugs used more in human medicine
Which opioids are Schedule III controlled drugs
Buprenorphine, codine mixed with aspirin or acetaminophen, hydrocodone
Which opioids are Schedule IV controlled drugs
Butorphanol, Tramadol
Which opioids are Schedule V controlled drugs
Cough suppressant (codeine + hydrocodone liquid)
MOA for opioid agonists- What happens during the activation of mu-opioid receptor
- Inhibits presynaptic release of substance P and other excitatory NTs.
- Inhibits post synaptic response to excitatory NTs.
