Opioid Agonists and Antagonists (M3) Flashcards
What are all compounds that work at opiod receptors (agonists, partial agonists, and antagonists) called?
opioid
What are naturally occurring alkaloids (morphine, codeine, thebaine, papaverine) called?
opiates
What are sleep-inducing medications called?
narcotics
What are the three opioid receptor types?
- mu
- delta
- kappa
What are the three families of endogenous opioid peptides?
- endorphins
- enkephalins
- dynorphins
Where can opioids accumulate?
muscle and fat
Where is heroin metabolized?
plasma
What is the mechanism of opioids?
bind G-protein-coupled receptors in brain and spinal cord involved in transmission and modulation of pain
What is the cellular mechanism of opioids?
- close voltage gated Ca2+ channels on presynaptic nerve terminal, reducing NT release
- open K+ channels and hyperpolarize, inhibiting postynaptically
What are the unique functions of mu receptors? 1. What is the relative affinity for the peptides? 2
- sedation, inhibition of resp, slow GI transit, modulate hormone and NT release
- endorphins > enkephalins > dynorphins
What are the unique functions of delta receptors? 1. What is the relative affinity for the peptides? 2
- modulation of hormone ant NT release
2. enkephalins > endorphins > dynorphins
What are the unique functions of kappa receptors? 1. What is the relative affinity for the peptides? 2
- psychotomimetic effects, slowed GI transit
2. dynorphins»_space; endorphins and enkephalins
What peptide do most opioid analgesics act on?
mu receptor
What peptide do most endogenous opioids act on?
delta and kappa
What pathways do opioids act on?
- ascending pain pathways
2. descending (modulatory) pathways
What is it called when with long-term administrtion, opioid analgesics increase the sensation of pain?
hyperalgesia
What is the CNS effect of opioids that relieves sensory pain?
analgesic
What is the CNS effect of opioids that provide a pleasant floating snesation, lessened anxiety and distress, and possible dysphoria?
euphoria
What are the CNS effects of opioids?
- analgesia
- euphoria
- sedation
- respiratory depression
- cough suppression
- miosis
- truncal rigidity
- nausea and vomiting
- varying body temp
What do opioids do to the liver?
decrease renal plasma flow
What do opioids do to the uterus?
prolong labor
What do opioids do to the endocrine systems?
- stimulate ADH, prolactin and somatotropin release
- effects of hypothalamus
- low testosterone
- amenorrhea
What are the associated numbers for the Numeric Rating Scale (NRS)?
- mild: 1-3
- moderate: 4-6
- severe: 7-10
What is the scale for pain that uses the facial expressions of the patient?
Wong-Baker scale