Opiods Flashcards
how is alfentanil supplied
500 mcg/mL
2mL vial
what are the principal uses of alfentanil
anesthetic induction
maintenance
monitored anesthesia care MAC
what is the MOA of alfentanil
Mu-1(supraspinal)
Mu-2(spinal)
receptor agonism
endogenous opioid ligand ekephalin’s receptor
delta
endogenous opioid ligand endorphin’s receptor
mu
endogenous opioid ligand dynorphin’s receptor
kappa
how do opiods work?
Mu-1(supraspinal)
Mu-2(spinal)
receptor agonism
inhibition of ascending transmission of nociceptive information from the spinal cord dorsal horn
activation of pain control circuits that descend from the midbrain, via rostram ventromedial medulla
to the spinal cord dorsal horn
mu-1 location
supraspinal
mu-2 location
spinal
mu-1 effects
euphoria miosis bradycardia hypothermia urinary retention
mu-2 effects
respiratory depression
constipation
physical dependence
potency order of opioids greatest to least
Sufentanil Remifentanil-Fentanil Alentanil hydromorphone Morphine Meperidine
“Susan/Robert Formed A Happy Monique
MARS least to greatest without fent and hydro”
Vd of alfentanil
0.4-1 L/kg in adults
1/2 life of alfentanil
90-111 minutes
context sensitive 1/2 life
metabolism of alfentanil
hepatic metabolism via CYP-450
Ndealklation
glucuronide formation
peak of alfentanil
1-3 min
onset of alfentanil
60 seconds
duration of alfentanil
20 min
dose dependent
contraindicaions/adverse rxn alfentanil
hypersensitivity
N/V
chest wall rigidity
physiologic effects of alfentanil
CNS depressoin
respiratory depression
protein binding % of alfentanil
92%
how does acidosis/alkalosis affect protein binding?
protein binding increases with alkalosis
decreases with acidosis
Varies purpose:
Incremental injection: alfentanil
5-15 mcg/kg q 5-20 minutes
Max 75 assisted vent required
Continuous Infusion alfentanil
50-75 mcg/kg induction/ maintenance 1-1.5 mcg/kg/min procedure dependent
Induction of Anesthesia: alfentanil
130-245 – maintenance 0.5-1.5 mcg/kg/min *reduce concentration of inhaled agents by 30-50 for first hour
MAC dose alfentanil
3-5 mcg/kg q 5-20 min OR 0.25-1 mcg/kg/min initial dose 3-8 TOTAL dose 3-40
how is sufentanil supplied
50 mcg/mL
100 mcg/2mL
250 mcg/5mL
MOA of sufentanil
Mu-1 and Mu-2 receptor agonism
Binds to opiod receptors throughouts CNS.
Opening K channels- inhibiting Ca++ channels
Increase pain threshold
Alters pain perception
Inhibit ascending pain pathways
Inhibition of catecholamine release- controls sympathetics response to surgical stress (up to 30 mg/kg)
trade name of sufentanil
sufenta
protein binding % of sufentanil
91-93%
1/2 life elimination of sufentanil
2-4 hr
1/2 Context Sensative of sufentanil
25 min 3 hour infusion
40 min 6 hour infusion
metabolism of sufentanil
CYP3A4
liver
small intestine
excretion of sufentanil
urine
first pass uptake of sufentanil- pulmonary %
60
peak of sufentanil
5 min
onset of sufentanil
10 seconds
duration of sufentanil
30-60 minutes
contraindications of sufenanil
chest wall rigidity
hypersensitivity
Premed: sufenta
2-5 mcg