click below
click below
Normal Size Small Size show me how
Pharm Exam 4 Ch 28
Opioid Analgesics, Antagonists, Nonopioid centrally activing analgesics
Question | Answer |
---|---|
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) |