8. Opioids Flashcards
Overdose rates were highest among people aged 25-54, higher in whites, american indian or alaskans than black/ hispanic, men were more likely to die from overdose, the MC drugs involved include oxycodone, hydrocodone, and?
Methadone
All of the following are what chemical class of opioids? morphine codeine hydrocodone hydromorphone levophanol oxycodone oxymorphone buprenorphine nalbuphine naloxone heroin
Phenanthrenes
All of the following are what chemical class of opioids?
pentazocine
diphenoxylate
loperamide
Benzomorphans
All of the following are what chemical class of opioids? Meperidine Fentanyl Sufentanil Famifentanil
Phenylpiperidines
All of the following are what chemical class of opioids? Methadone Prpoxyphene
Diphenylheptanes
All of the following are what functional class of opioids? morphine hydromorphine methadone meperidine fentanyl codeine oxycodone hydrocodone propoxyphene
Complete Opioid Agonists
All of the following are what functional class of opioids? Pentazocine Nalbuphine Buprenorphine Butorphanol
Partial/Mixed opioids agonists
All of the following are what functional class of opioids?
naloxone
naltrexone
Opioid Antagonists
Opioids general mechanism of action is they bind to opioid receptors in the CNS causing inhibition of ascending pain pathways, altering the preception of and response to pain, producing a generalized?
CNS Depression
Onset of action of opioids depends on administration- oral 30 minutes, IV-5-10 minutes. Duration depends on patient and type of medication, immediated release 3-5hrs, ER 8-24 hours, epidural 24 hours, suppository ?
3-7 hours
Side affects associated with opioids include CNS depression, hypotension, consitpation**MC- give preventative stool softener, and has a black box warning for serious life threatening or fatal?
respiratory depression (monitor closely during initiation/ dose escalation)
Compared to morphine, opioids are much more potent, hydrocodone oxycodone are only slightly stronger as compared to what, which is 100X the strength of morphine?
Fentanyl
Opioids are used for pain management in both acute and chronic pain, such as MI, sickle cell crisis, post op procedures, trauma, cancer, kidney stones and even?
Back pain
Opioids are also used as an adjunct to general anesthesia, epidural anesthesia, palliative care, antitussive for cough, and antidiarrheal such as?
Loperamide
Match the opioid receptor with its correct affinity... Endorphins > enkephalins > dynorphins enkephalins > Endorphins > dynorphins Dynorphins >> Endorphins > Enkephalins Delta Kappa Mu
Mu = Endorphins > enkephalins > dynorphins Kappa = Dynorphins >> Endorphins > Enkephalins Delta = enkephalins > Endorphins > dynorphins
A full opioid agonist will fully activate Mu receptor, partial agonists will partial activate all three opioid receptors, and Naltrexone and nalmefene do what?
are antagonists at the Mu receptor however are partial agonists at kappa and delta- used for alcohol and opioid addiction
Stimulant effects of opioids are analgesic at chemoreceptors of area postrema oculomotor center and antinociceptive, other stimulat effects occur include ureter/ bladder/ bladder sphincter as well as smooth m. stomach and bowel causes?
Antidiarrheal or constipation
Dampening effects of opioids at their receptors include pain sensation/mood alertness= analgesic, and it also affects the emetic center (causing N/V) and the respiratory and cough center which leads to its?
antitussive qualities
At increasing rates of a full agonist (methadone) the opioid effect continues to increase exponentially, a partial agonist plateaus after a certain amount, what about an antagonist?
Naloxone** he likes completely blocks opioids and can even throw them off their receptor
There is a safety margin between normal treatment with morphine for pain (decreased perception), but once enough is given- or an overdose, what occurs?
respiratory depression and DEATH
There is a high degree of tolerance that is caused by opioids including analgesia, euphoria/dysphoria, mental cloduing, sedation, respiratory depression, antidiuresis, N/V and?
cough suppression
There are moderate degrees of tolerance that develop to some of the effects of the opioids which include bradycardia, and minimal or no degrees or tolerance to the effects include miosis, convulsions and?
Constipation
Acute* adverse effects of opioid use includes resp depression, N/V, pruritus, urticaria, constipation, urinary retention, delirium, myoclonus, and what else?2
sedation
seizures
Chronic* adverse effects of opioids include hypogandism, immunosuppression, increased feeding, inc. GH secretion, withdrawal, tolerance and dependence, abuse/addiction, and what other 2?
hyperalgesia
impairment while driving
general side effects of opioids include hallucinations, confusion, fainting, dizziness, swelling of tongue/lips, hives, rash, troubled breathing/slowed breathing, seizures, hoarsness, swelling throat, cant swallow, and what in the face and eyes?
Swelling of the face and eyes (as well as swelling in hands feet ankles legs)
Opioids with sedative-hypnotic drugs increases central nervous system depression (**resp depression). Opioid with what causes increased sedation, effects on respiratory depression and accentuation of CV effects?
Antipsychotic agents
Opioids with what inhibitors is a relative contraindication to all opioid analgesics because of the high incidence of hyperpyrexic coma*, hypertension is also seen?
Monoamine Oxidase Inhibitors
What opioid is a pure opioid antagonist that competes and displaces opioids at the opioid receptor sites, used for opioid overdose- complete or partial reversal of opioid depression induced by natural and synthetic opioids?
Naloxone
SE: acute opioid withdrawal due to release of catecholamines which can unmask pain
What is a pure opioid antagonist- a cyclopropyl derivative of oxymorphone similar in structure, it acts as competitive antagonist at opioid receptor sites, with highest affinity for MU?
Naltrexone
Naltrexone is used in treatment of alcohol use disorder, and for the blockade of the effects of exogenously administered opioids.. SE include accidental overdose bc patients who had been treated w naltrexone will have a lower response to opioids, and what other side effect?
acute opioid withdrawal, may precipitate symptoms of acute withdrawal in opioid dependent patients, such as pain, hypertension, sweating, agitation, and irritability
(neonates = shill cry/failure to feed)
What is used to treat diarrhea and can also decrease amount of drainage in patients with ostomies, if overdosed, naloxone is given as an antidote, vital signs must be monitored for recurrence of symptoms of drug overdose for 24 hours?
Loperamide
What is an opioid agonist indicated for the management of pain not responsive to non-narcotic analgesics, contraindicated in people allergic, in bronchial astham or upper airway obstruction, respiratory depression in absence of resuscitiative equipment?
Morphine Sulfate
SE: sedation, lightheadedness, dizziness, N/V, constipation
Morphine Sulfate must be given carfully to avoid dosing errors due to confusion between different concentrations* and between mg/ml, causes resp depression, CNS toxicity, and may increase the risk of?
respiratory depression with other CNS depressants
What is indicated for the treatment of opioid dependence and is preferred for induction ( a withdrawal med), resp depression and death may occur via IV or in combo w benzos/alch?
Buprenorphine
Buprenorphine has side effects including headache, N/V, hyperhidrosis, consitpation, withdrawal, insomnia and pain, and patients must be monitored starting or ending what inhibitors or induces, for potential over and under dosing?
CYP3A4 inhibs/inducers (processed by this)
