Anesthesia Pharm II Flashcards
Opioid receptors
mu, delta, and kappa
Opioid mechanism of action
- opioid binds receptor
- Ca2+ channels close
- K+ channels open
- cells hyperpolarize
- transmission blocked
primary effect is a decrease in neurotransmission
Where are opioid receptors located
brain, spinal cord, and peripheral nerves
Common clinical effects of Opioids (8)
- impairs sympathetic compensatory responses
- itching
- depression of ventilation
- increased CO2 increases ICP
- sedation
- biliary spasm
- nausea/vomiting
- urinary retention
Meperidine
(Demerol)
- antispasmodic effect
- renal excretion
- CNS stimulant
- shivering
- serotonin syndrome
- demethylation to normeperidine in the liver
Fentanyl
- renal excretion
- stable hemodynamics
- no amnestic effect
- depression of ventilation
- skeletal muscle rigidity possible
Sufentanil
- renal and biliary excretion
- bradycardia
- skeletal muscle rigidity
Rank in order of duration
morphine, meperidone, fentanyl
fentanyl < meperidone < morphine
Remifentanil
- ester linkage susceptible to hydrolysis
- rapidly titratable
- respiratory depression
- no change in ICP
*must add a longer acting agent to cover post-op pain
Context-Sensitive half-time of Remifentanil
4 minutes
Sufentanil
Fentanyl
Alfentanil
Remifentanil
Rank in order of increasing context-sensitive half time:
Sufentanil, Fentanyl, Alfentanil, Remifentanil
Remifentanil
Sufentanil
Alfentanil
Fentanyl
Codeine
- interindividual variability
- cough supressant
Hydromorphone
(Dilaudid)
- 5x more potent than morphine
- faster onset
- oral dose every 4 hours
- agitiation/restlessness
- dangerous when combind with other sedatives
Oxycodone
moderate to severe pain
high abuse potential
Hydrocodone
high abuse potential
Methadone
- used for chronic pain
- prolonged duration of action
- overdose possible
- used to control withdrawal symptoms
Opioid Agonist-Antagonist
- binds to mu receptors, but produce limited effects
- may antagonize effects of other narcotics
- may produce dysphoric effects
- low abuse potential
- limited respiratory depression
Pentazocine
(Talwin)
combined with naloxone to prevent “powdering”
can develop phyiscal dependence
Suboxone
treats opioid addiction
Naloxone
- nonselective antagonist of all 3 opioid receptors
- treats depression of ventilation
Naltrexone
treats alcoholism
Q24 hour dosing
PCA pumps
(patient-controlled anesthesia)
- Settings
- drug concentration
- loading dose
- lockout interval
- basal rate
Which opioid has a cephalad movement?
Morphine
less lipid soluble compared to fentanyl/sufent
Side effects of Neuraxial Opioids
- itiching
- urinary retention
- nausea/vomiting
- depression of ventilation
*does not appear in breast milk
*may be reversed by naloxone
Masimo Acoustic Monitor
alarm that triggers when patient stops breathing
- 81% sensitive
- do not give to a person at risk of hypoventilation
Withdrawal symptoms
- yawning
- diaphoresis
- lacrimation
- coryza (stuffy nose)
- insomnia
- abdominal cramps
- nausea/vomiting
What can cause an increase of NMB activity?
CO2 retention
- patient can hypoventilate in PACU and become “recurarized”
- Treatment
- increase FIO2
- sit patient up
- assist ventilation
- additional reversal
What can reverse a spasm of the sphincter of Oddi?
naloxone or glucagon (2mg IV)
4 Parts in a Nociceptive system
- transduction
- transmission
- modulation
- perception
What accounts for perception of sensory-discriminative component of peripheral pain stimuli?
forebrain somatosensory cortex
What accounts for the perception of motivational affective components of pain?
Limbic cortex and Thalamus
(3) Primary afferent nocicpetors
A-beta, A-delta, and C fibers
A-alpha fibers
proprioception
myelinated
wide diameter
fastest conduction speed