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