Exam 2 - Opioid agonists Flashcards
Opiates are derived from what plant?
What are were the first three opiates?
Papaver somniferum aka poppy juice
- Morphine
- Codeine
- Papverine
The word narcotic comes from the greek word ____ , which means ____
stupor
has the potential to produce a physical dependance
What 3 drugs are the phenanthrenes?
- Morphine
- Codeine
- Thebaine
What 2 opioids are benzylisoquinolines?
- Papaverine
- Noscapine
What is the general MOA of opiates?
- Act on pre and post synaptic opioid receptors in the CNS
- Presynaptic inhibition of ACh, dopamine, norepinephrine, and substance P
→ Hyper polarization via ↑K+ conductance
→ Ca+ channel inactivation - Decreased neurotransmisson of pain modulators
Where are opioid receptors in the brain?
-Periaqueductal gray (PAG)
- locus ceruleus
- rostral ventral medulla (RVM)
-hypothalamus
Where are opioid receptors located in the spinal cord?
- Interneurons
- Primary afferent neurons in the substantia gelatinosa
Where are opioid receptors outside of the CNS?
- Sensory neurons
- Immune cells
These 2 opioid receptors effects include low abuse potential and miosis?
Mu1 and Kappa
These 2 opioid receptors cause physical dependence and constipation?
Mu2 and Delta
This opioid receptor is the only receptor that does not produce supraspinal analgesia?
Mu2
This opiod receptor causes bradycardia, hypothermia, and urinary retention?
Mu1
This opioid receptor can cause dysphoria and diuresis?
Kappa
Endorphins, morphine, and synthetic opioids are agonists of these receptors?
Mu1 and Mu2
What is the agonist for kappa and delta receptors?
Kappa: Dynorphins
Delta: Enkephalins
These opioid receptors cause depression of ventilation?
Mu2 and delta
What are the CV side effects from opioids?
- Histamine release causing decreased SNS tone in veins = ↓ venous return, CO, and BP
- Bradycardia
- Increased effects with benzos or nitrous
- Cardioprotective from MI
Opiods effect on responsiveness to CO2?
Leads to what?
Decreased
Increases resting PaCO2 (shifts curve right)
Depresses ventilation leading to hypoventilation or apnea if overdosed
What drug can antagonize the ventilatory depression of opiods?
How?
- Physostigmine
- Increases CNS ACh levels - reducing ventilatory effects while maintaing analgesia
These opiods can cause cough suppression:
- Codeine
- Dextromethorphan
The other opioids can cause reflexive coughing pre-induction
Why should you caution opioids in patients with head injuries?
- Can decrease CBF
- Affects wakefulness
- Causes miosis
- Increased PaCO2 can increase ICP
- Damage to the BBB can increase sensitivity to opioids
Can opioids cause myoclonus?
Yes, in large doses
What severe side effect of opioids can be exacerbated by mechanical ventilation?
Treatment?
- Thoracic and abominal muscle rigidity - can lead to difficulty with ventilation/oxygenation
- Tx: muscle relaxant or naloxone
Primarily seen with fentanyl and its derivatives, especially sufentanil
Which opioids cautioned during an ERCP?
Why?
How can this be treated?
- Fentanyl, morphine, and meperidine
- Causes sphincter of Oddi spasms (3 % incidence)
- Tx: Glucagon 2 mg IV, reverses spasm but not analgesia