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Opioids part 1

Pharm test 2

Sufentanil: lipid solubility, potency, and onset 1 1 2
Meperidine: lipid solubility, potency, and onset 6 6 5
Morphine: lipid solubility, potency, and onset 5 5 4
Alfentanil: lipid solubility, potency, and onset 4 4 1
Fentanyl: lipid solubility, potency, and onset 3 3 3
Remifentanil: lipid solubility, potency, and onset 2 2 1
bind to specific receptor site to elicit a specific response opioid agonist
opioids are unique in their ability to provide analgesia without loss of ____, _____, or _____ touch, proprioception, consciousness
term used for drugs derived from opium opiate
partially bind to my receptors where they produce limited (partial agonist) responses or no effect (competitive antagonist) opioid agonist-antagonist
fentanly, sufentanil, alfentanil, and remifentanil are examples of semisynthetic opiods
opioids act as agonist at steriospecific opioid receptors at presynaptic and postsynaptic sites in the CNS, spinal cord, brainstem, peripheral tissures
enkephalins, endorphins and dynophins are endogenous peptide opioid receptor ligands
opiods in the ionized state bind most strongly to the ____ receptor site anionic
only ____ forms have agonist activity levrotatory
what are the opioid receptors mu, delta, and kappa
Mu or morphine preferring receptors are principally responsible for _____ and ____ analgesia supraspinal, spinal
receptors are responsible for hypoventilation, bradycardia, and physical dependence Mu²
activation of ___ receptor is speculated to produce analgesia Mu¹
Morphine, Meperidine, Fentanly, Sufentanil, Alfentanil, Remifentanil are what type of agoinst Mu receptor agonist
mu receptor antagonist Naloxone
activation results in inhibition of NT release via N calcium channels results in analgesia, although dyshporia and diuresis may also occur Kappa receptors
High intensity painful stimulation may be resistant to the analgesic effects of____receptors Kappa
Kappa receptor agaonist is the endogenous ligand dynorphins
kappa antagonist receptors include Naloxone, Naoltrexone, Naolmefene
_____receptors modulate Mu receptors delta
____receptors respond to the endogenous ligands know as enkephalins delta
are not blocked by naloxone therefore these receptors are not opioid receptors sigma receptors
this receptor have a high affinity for phencyclidine, may be identical to receptors that bind to ketamine Sigma receptors
the role of the opioid receptors and endorphins is to function as the endogenous pain suppression system
opioid receptors are located in the periaqueductal gray matter of the brainstem, amygdala, corpus striatum and hypothalmus and the substantia gelatinosa of the spinal cord
it is thought that endorphins inhibit the release of _____ NT excitatory
administration of opioids into the epidural and subarachnoid space Neuraxial Opioids
contradictions to epidural anticoagulants➞epidural hematoma=paralysis hold for 7 days
the epidural space has which two meninges dura and arachnoid
epidural administration of a poorly _____ opioid such as morphine will result in a slower onset of action and longer duration of action. lipid soluble
most common location for an epidural is the lumbar spine
spinal cord ends at L-1 vertebrae
the epidural dose is _____ times the subarachnoid dose 5-10
analgesia is specific for ___rather than ____ pain visceral, somatic
neuraxial opiods ____ MAC for volatile anesthetics increase or decrease decrease
The administration of _____ with the opioid will decrease systemic absorption but does not decrese diffusion into the CSF epinephrine
most common side effect of neuraxial opiods is ____ and can be relieved by giving ____ pruritis, naloxone
cephalad migration can be increased by coughing, increase the risk of resp. depress
delayed respiratory depression involves morphine usually occus in____hrs 6-12
with morphine ___ respiratory depression does not occur early
with fentanyl ____ depression occurs and ___ depression of ventilation does not occur early, late
DepoDur (morphine liposomal) provides pain relief before or during surgery for up to ___hrs 48
lumbar epidural only, not for pts <18yrs, no other drug given in epidural space for 48hrs, do not freeze med, and intrathecal admin. has resulted in prolonged resp. depress. DepoDur warnings
Meperidine is a synthetic opioid agonist at ___ and ___ opioid receptors mu, kappa
Analogues of meperidine Fentanyl, Sufentanil, Alfentanil, and remifentanil FARS
has a extremely short duration of action, it is necessary to administer an opioid with a longer duration of action (care must be taken not to stop the infusion) Remifentanil
an opioid receptor antagonist which blocks opioid binding at the mu receptor, derivative of naltrexone Methylnaltrexone Bromide
onset in 30-60min, absorpt. SQ rapid, adverse reactions:GI Methylnaltrexone Bromide
reports of reactivation of herpes virus with epidural morphine has been reported with ______ administration of opioids Neuraxial
produces a analgesia, euphoria, sedation, and a diminished ability to concentrate. morphine
___pain is relieved more effectively by morphine than ___ pain dull, sharp
poor lipid solubility, high ionization at physiologic pH, protein binding, rapid conjugation with aleuronic acid reasons for morphine poor penetration into CSF
since morphine is highly ionized providing a alkalinized state in the blood by hyperventilation will ____ passage into the CSF increase
undergoes significant first pass into the lungs fentanyl
this drugs metabolism principle pathway is conjugation with glucuronic acid in hepatic and extra hepatic sites, especially (kidney), making which pts. at risk for accumulation? morphine renal failure pts taken MAOI can lead to exaggerated effects by the formation of glucuronide metabolites
first 4 day of a neonates,their more sensitive to morphine clearance making them at risk for respiratory depression
patients with reanal failure show higher plasma concentrations reflecting a ___ Vd with morphine smaller
limiting the rate of administration to 5mg per min., maintaining the pt supine, keep pt hydrated are ways to minimizes Histamine release and hypotension from morphine
the combination of an opioid with ____ will result in cardiovascular depression nitrous oxide
all opioids produce a _____ depression of ventilation, due to Mu²receptor effects dose-dependant
opioids may diminish sensitivity to CO2, giving ____, may antagonize respiratory depression but not analgesia physostigime
use opioids with caution in pts with head injuries due to wakefulness, production of miosis, and depression of ventilation with associated increases in ICP if the PaC02 is increased.
cause skeletal muscle rigidity, thoracic and abdominal (diaphragm) opioids
these have induced biliary spasms effects fentanyl, morphine, meperidine, pentazocine
reverses opioid induced biliary spasms glucagon
opioid induced nausea and vomiting are caused by direct stimulation of the chemoreceptor trigger zone in the floor of the fourth ventricle
morphine can increase the tone and peristaltic activity of the ureter, giving an ___ drug such as ___ can reverse these effects anticholinergic atrophine
cause skin flushing morphine
ventilary depression can occur in the ____ as a result of giving opioids to the mother fetus
these drugs exaggerate the effects of some opioids by causings ventilatory depression amphetamines, phenothiazines, MAOI (phenelzine, tranylcypromine), and TCA
_____ and physical dependence with repeated doses of opioids are characteristic of all opioids tolerance
____ tolerance develops between all of the opioids cross
tolerance usually takes ___ weeks 2-3
physical dependence on morphine usually requires __ days, however some degree of physical dependence occurs after __ days 25, 2
yawning, diaporesis, lacrmation, or coryza, insomnia and restlessness are prominent inital symptomes of withdrawal
abdominal cramps, nausea, vomiting, and diarrhea reach their peak in __ hrs and then decline 72
helps prevent withdrawal symptoms clonidine
what is the withdrawal triad miosis, hypoventilation, and coma
what is the treatment for opioid overdose mechanical ventilation, Narcan
Created by: melbacs