Opioids - Iszard Flashcards
morphine codeine hydrocodone hydromorphone levorphanol oxycodone oxymorphone buprenorphine nalbuphine butorphanol naloxone heroin
phenanthrenes
pentazocine
diphenoxylate
loperamide
benzomorphans
meperidine
fentanyl
sufentanil
ramifentanil
phenylpiperidines
methodone
propoxyphene
diphenylheptanes
what are the opioid agonists? (9)
morphine hydromorphine meperidine fentanyl codeine oxcodone hydrocodone propoxyphene
what are the mixed agonist/antagonists? (4)
pentazocine
nalbuphine
buprenorphine
butorphanol
what are the opioid antagonists? (2)
naloxone
naltrexone
what are the concerns related to opioid adverse effects?
- CNS depression
- constipation
- hypotension -> use caution in pt w/hypovolemia*
what is the black box warning of opioids?
serious, life-threatening respiratory depression may occur
what are the indications of opioid therapy?
- MI
- sickle cell crisis
- post-op
- trauma
- cancer
- kidney stones
- back pain
- epidural anesthesia
- antitussive
- antidiarrheal (loperamide)
which opioid receptor subtype shows this affinity:
- endorphins > enkephalins > dynomorphins
mu
which opioid receptor subtype shows this affinity:
- enkephalins > endorphins and dynomorphins
delta
which opioid receptor subtype shows this affinity:
- dynomorphins»_space; endorphins and enkephalins
kappa
methadone is a full agonist for which receptor?
mu
naltrexone and nalmefene inhibit which receptor?
mu
buprenorphine is a partial agonist for which receptors?
kappa and delta
naltrexone is a partial agonist for which receptor?
kappa
nalmefene is a partial agonist for which receptor?
kappa
what are the dampening effects of opioids?
- depresses pain sensation (analgesic)
- depresses respiratory and cough centers (antitussive)
what are the stimulant effects of opioids?
- antinociceptive system (analgesic)
- smooth musculature of stomach and bowel (antidiarrheal)
- ureter, bladder, sphincter
- respiratory depression
- nausea/vomiting
- pruritus
- urticaria
- constipation
- urinary retention
- delirium
- sedation
- myoclonus
- seizures
acute adverse effects of opioid use
- hypogonadism
- immunosuppression
- increased feeding
- increased GH secretion
- withdrawal effects
- tolerance/dependence
- abuse/addiction
- hyperalgesia
- impairment while driving
chronic effects of opioid use
what are the minimal effects of opioid use?
- miosis
- constipation
- convulsion
what is the one moderate effect of opioid use?
bradycardia
what are the serious effects of opioid use?
- analgesia
- euphoria
- mental clouding
- sedation
- respiratory depression
- antidiuresis
- nausea/vomiting
- cough suppression
what are the effects of opioid use with sedative-hypnotics?
increased CNS depression, especially respiratory depression
what are the effects of opioid use with antipsychotic agents?
increased sedation
- variable effects on respiratory depression
- accentuation of cardiovascular effects (antimuscarinic and a-blocking actions)
what are the effects of opioids with monoamine oxidase inhibitors?
relative contraindication to all opioid analgesics d/t high incidence of hyper-pyrexic coma
- HTN has also been reported
this drug is an opioid agonist indicated for the management of pain not responsive to non-narcotic analgesics
- contraindicated in pts with bronchial asthma or upper airway obstruction, or respiratory depression
morphine sulfate
warnings: respiratory depression, CNS toxicity, don’t use with CNS depressants (alcohol)
adverse rxns: sedation, lightheadedness, dizziness, nausea, vomiting, constipation
this drug is indicated for treatment of opioid dependence and is preferred for induction
- can be abused in a similar manner to other opioids
- significant respiratory depression and death have occurred, especially when given intravenously in combination with benzodiazepines and other CNS depressants
buprenorphine
what are the drug interactions of buprenorphine?
monitor patients starting or ending CYP34 inhibitors for potential over/under-dosing
- use caution with benzos or other CNS depressants
pure opioid antagonist that competes and displaces opioids at opioid receptor
- used for complete or patial reversal of opioid overdose or opioid depression (respiratory depression)
nalozone
NOTE: causes the release of catecholamines, which may precipitate acute withdrawal or unmask pain in those who regularly take opioids
pure opioid antagonist
- cyclopropyl dervative of oxymorphone similar to naloxone and nalorphine
- acts as competitive antagonist at opioid receptor, showing highest affinity for mu receptors
naltrexone
NOTE: pts who have been treated with naltrexone may respond to lower opioid doses than previously used -> could result in potentially life-threatening opioid intoxication
- may also precipitate symptoms of acute withdrawal in opioid-dependent patients
