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Pharm Exam 4 Ch 28

Opioid Analgesics, Antagonists, Nonopioid centrally activing analgesics

QuestionAnswer
Opioid any drug that has actions similar to those of morphine
narcotic analgesic, CNS depressant, capable of causing physical dependence; also to illicit street drugs
endogenous opioid peptides x3 enkephalins, endorphins, dynorphins
endogenous opioid peptides function neurotransmitters, neurohormones, neuromodulators
endogenous opioid peptide found in: CNS, peripheral tissue
opioid receptors x3 mu, kappa, delta
opioid analgesics act by activating which receptor mu;(also weak activation of kappa)(do not interact with delta)
endogenous opioid peptides act through which receptors? mu, kappa, delta
mu receptor activation responses analgesia, respiratory depression, euphoria, sedation
kappa receptor activation responses analgesia, sedation, (may underlie psychotomimetic effects)
classes of drugs that act at opioid receptors pure opioid agonist, agonist-antagonist opioids, pure opioid antagonists
pure opioid agonists 2 subgroups strong opioid agonists-(morphine), moderate to strong opioid agonists-(codeine)
drugs that relieve pain without causing loss of consciousness analgesics
most effective pain relievers available opioids
applies to compounds present in opium opiates
agonist-antagonist opioid effects when: given alone, given with pure opioid alone: produce analgesia, with pure opioid: opioid anagonist (pentazocine [Talwin])
agonist-antagonist opioids x4 pentazocine, nalbuphine, butorphanol, buprenorphine
pure opioid agonist action at mu receptor agonist
pure opioid agonist action at kappa receptor agonist
agonist-antagonist opioid action at mu receptor antagonist (except buprenorphine)
agonist-antagonist opioid action at kappa receptor agonist (except buprenorphine)
pure opioid antagonist action at mu antagonist
pure opioid antagonist action at kappa antagonist
pure opioid antagonist use reversal of respiratory and CNS depression from overdose of opioid agonists (Naloxone)
delta (δ) receptor location brain
delta (δ) receptor activation analgesia, antidepressant, physical dependence
kappa (κ) receptor location brain, spinal cord
kappa (κ) receptor activation spinal analgesia, sedation, miosis (small pupils)
mu (μ) receptor location brain, spinal cord, GI tract
mu (μ) receptor activation supraspinal analgesia, respiratory depression, miosis (small pupils), euphoria, reduced GI motility, physical dependence
strong opioid agonists x4 morphine, fentanyl, remifentanyl, alfentanyl
moderate to strong opioid agonists x3 oxycodone, codeine, hydromorphone
pure opioid antagonists (major) naloxone, naltrexone
morphine source opium (dried juice) of seedpod of poppy plant
site of action for morphine (pain relief) mu receptor
morphine-like drugs mechanism of action (analgesia) mimicking actions of endogenous opioid peptides
Morphine administrations: if patient respirations are below 12 breaths/minutes, what should the nurse do Dose of morphine should be withheld and the prescriber notified
circumstances in which patients are especially sensitive to respiratory depression very young, elderly, pts with respiratory disease,(asthma, emphysema)
A man with asthma is prescribed morphine by the prescriber. As his nurse, what should you do? inpatient: monitor him closely, outpatient: inform him of the risk for respiratory depression (RD) and instructed to notify prescriber if (RD) occurs
morphine promotes analgesia and respiratory depression by: decreasing brain stem respiratory centers
True/False: Morphine is more effective in relieving sharp, intermittent pain False: it is more effective for relieving constant, dull pain
Besides pain relief, morphine can be given for: (2) pre-op sedation and reduction of anxiety
onset of respiratory depression may be delayed for hours when morphine is administered by which route? spinal injection
effects of using morphine with other drugs with CNS-depressant actions Respiratory depression is increased
which drugs should be avoided when using morphine CNS depressants (alcohol, barbituates, benzodiazepines)
morphine adverse effects` euphoria/dysphoria, sedation, miosis, neurotoxicity, itching (IV)
prolonged use of morphine can lead to __________________ (2) tolerance (analgesia, euphoria, sedation, respiratory depression) physical dependence
milligram potency 100 times that of morphine fentanyl
fentanyl indication x3 surgical analgesia, chronic pain control, control of breakthrough pain in pts taking other opioids
parenteral fentanyl use induction and maintenance of surgical anesthesia
transdermal fentanyl use persistent severe pain in pts who are already opioid tolerant
transmucosal fentanyl use breakthrough cancer pain for opioid tolerant pts
intravenous fentanyl-related opioids x2 and use alfentanil, sufentanil, used for induction and maintenance of anesthesia
intravenous opioid with rapid onset and brief duration used for analgesia during surgery and immediate post-op period remifentanil
use in decline because interacts adversely with many drugs and risk of harm from accumulation of toxic metabolite meperidine [Demerol]
used to relieve pain and to treat opioid addiction methadone
great caution should be taken when taking methadone because prolonged QT because increases risk of fatal dysrthythmias
schedule I opioid illegal in US higher lipid solubility than morphine subjective effects produced by metabolites heroin
opioids contraindicated for pts with intracranial pressure because suppressed respirations cause CO2 levels content of blood (raises intracranial pressure)
degree of pain relief achieved safely is much lower than morphine codeine
risk for breast-fed infants of mothers taking codeine severe toxicity
non-pain related indication for codeine cough suppression
most widely prescribed drug in the US hydrocodone
strong opioid agonist removed from US market propoxyphene
difference between physical dependence and addiction abstinence syndrome will occur with abrupt withdrawal continued use of psychoactive substance despite physical, psychologic, or social harm
define abuse drug use inconsistent with medical or social norms
define and describe PCA patient-controlled analgesia; self-administration of parenteral opioids on an "as-needed" basis
advantage of PCA over traditional IM therapy PCA is ideally suited to maintain steady levels of opioids
opioid choice for decreasing pain of myocardial infarction morphine (reduces discomfort and can decrease cardiac work by lowering blood pressure)
what does REMS stand for Risk Evaluation and Mitigation Strategy
REMS purpose to reduce injuries and death from prescription opioids and to reduce abuse
naloxone contraindication supraventricular dyrhythmias
methylnaltrexone use treatment of opioid-induced constipation
Relieve pain by mechanisms largely or completely unrelated to opioid receptors nonopioid centrally acting analgesias (little to no risk of resp. depression, dependence, or abuse)
tramadol contraindications x3 epilepsy patients, those taking CNS depressants, MAO-inhibitors
clonidine indications x2 mech of action hypertension, relief of severe pain; (alpha-2 agonist) blockade of nerve traffic for transmission of pain signals from PNS to brain
clonidine adverse effects severe hypotension, rebound hypertension (from withdrawal), bradycardia
max duration of treatment with meperidine 48 hrs (to avoid toxic metabolite accumulation)
Created by: tmbobe11
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