Opioids part 1 Word Scramble
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Question | Answer |
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 |
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melbacs
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