Pharm - Opioids Flashcards
name the benzomorphans
- pentazocine
- diphenoxylate
- loperamide
name the phenylpiperidines
- meperidine
- fentanyl
- sufentanil
- ramifentanil
name the diphenylheptanes
- methadone
- propoxyphene
name the opioid agonists
- morphine
- hydromorphine
- methadone
- meperidine
- fentanyl
- codeine
- oxycodone
- hydrocodone
- propoxyphene
name the mixed opioid agonist/antagonist (partial agonists)
- pentazocine
- nalbuphine
- buprenorphine
- butorphanol
name the opioid antagonists
- naloxone
- naltrexone
MOA opioids
bind to opioid receptors in the CNS causing inhibition of ascending nerve pathway, altering the perception of and response to pain and producing generalized CNS depression
compare onset of action between oral and IV opioids
oral: 30 mins
IV: 5-10 mins
compare duration between:
- immediate release
- extended release
- epidural/intrathecal
- suppository
- immediate release: 3-5 hours
- extended release: 8-24 hours
- epidural/intrathecal: up to 24 hours
- suppository: 3-7 hours
3 main adverse effects of opioids
- CNS depression
- constipation
- hypotension
constipation (as an adverse effect of opioid use) is particularly problematic in what patients
what preventative measures can be taken to reduce potential for constipation
patients with unstable angina and patients post-MI
stool softeners, increased fiber
hypotension (as an adverse effect of opioid use) is particularly concerning in what patients
hypovolemic patients, CV disease, circulatory shock, or pts on other drugs that exaggerate hypotensive effects (phenothiazines, general anesthetics)
what is the black box warning for opioids
serious, life-threatening, or fatal respiratory depression may occur
carbon dioxide retension
compare potency of opioids
least: - hydrocodone - oxycodone - methadone - oxymorphone - hydromorphone - butorphanol - buprenorphine - fentanyl most:
other than pain relief indications for opioids, what are some additional indications
- adjunct to general anesthesia
- epidural anesthesia
- palliative care
- antitussive
- antidiarrheal
compare affinities to endogenous opioids peptides for the mu receptor
endorphins > enkaphalins > dynorphins
compare affinities to endogenous opioids peptides for the delta receptor
enkephalins > endorphins and dynorphins
compare affinities to endogenous opioids peptides for the kappa receptor
dynorphins»_space; endorphins and enkaphalins
what receptors does methadone work on
full agonist on mu receptor
what receptors does buprenorphine work on
partial agonist to all receptors
what receptors does naltrexone work on
- antagonist to mu
- partial agonist to kappa
what receptors does nalmefene work on
- agonist to mu
- partial agonist to kappa
what is the only listed drug to work on delta receptors
buprenorphine
describe the stimulant effects of opioids
analgesic: stimulates vagal centers, chemoreceptors, antinociceptive system
antidiarrheal: spastic constipation, works on ureter, bladder
describe the dampening effects of opioids
analgesic: decreased pain sensation and mood alertness
antitussive: decreases respiratory center, cough center, emetic center
list the acute adverse effects of opioid use
- respiratory depression
- N/V
- pruritis
- urticaria
- constipation
- urinary retention
- delirium
- sedation
- myoclonus
- seizures
list the chronic adverse effects of opioid use
- hypogonadism
- immunosuppression
- increased feeding
- increased GH secretion
- withdrawal effects
- tolerance, dependence
- abuse, addiction
- hyperalgesia
- impairment while driving
specific side effects to oxycodone
CNS: hallucinations, confusion, fainting, dizziness
Eyes: swelling, redness
MSK: seizures
Skin: hives, rash
Respiratory: difficulty breathing
what drug-drug interactions can occur with opioids
1) w/ sedatives/hypnotics –> increased CNS depression, particularly respiratory
2) antipsychotics –> increased sedation
3) MOAIs –> hyperpyrexic coma, hTN
indications for morphine sulfate
opioid agonist indicated for management of pain not responsive to non-narcotic analgesics
contraindications to morphine sulfate
bronchial asthma or upper airway obstruction
AEs of morphine sulfate
- respiratory depression
- CNS toxicity
- CNS depression
- sedation
- light-headedness
- dizziness
- N/V
- constipation
indications for buprenorphine
treatment of opioid dependence and is preferred for induction
AEs buprenorphine
- headache
- N/V
- hyperhidrosis
- constipation
- withdrawal
- insomnia
- pain
drug interactions buprenorphine
monitor pts starting or ending CYP3A4 inhibitors or inducers for potential over or under dosing
MOA naloxone
pure opioid antagonist that competes and displaces opioids at opioid receptor site
indications naloxone
for the complete or partial reversal of opioid depression induced by natural and synthetic opioids
also for diagnosis of suspected or known acute opioid overdosage
warnings/precautions naloxone
acute opioid withdrawal: naloxone causes release of catecholamines which may precipitate acute withdrawal or unmask pain
MOA naltrexone
pure opioid antagonist; cyclopropyl derivative of oxymorphone; competitive antagonist at opioid receptor sites with high affinity for mu receptors
indications naltrexone
treatment of alcohol use disorder
blocks effects of exogenously administered opioids
warnings/precautions naltrexone
- accidental opioid OD (pts on naltrexone may respond to lower opioid doses than previously used, so using opioids again could cause OD)
- acute opioid withdrawal
indications loperamide other than pain relief
used to treat diarrhea
