Chapter 8: Drugs To Treat Pain - Opioid Analgesics Flashcards
Name a low potency opioid.
Codeine
Name a medium potency opioid.
Morphine
Name an opioid.
- hydrocodone
- oxycodone
Name a extremely high potency opioid.
Fentanyl
Name an illegal opioid.
Heroin
Name an opioid antagonist.
Naloxone
Prescribers should consider opioid therapy only if…
The expected benefits for both pain and function are anticipated to outweigh the risks to the patient
If opioids are used, they should be combined with _______ therapy and _______ _______ therapy, as appropriate.
- nonpharmacologic
- nonopioid pharmacologic therapy
Opioid drugs act by binding to _____ _____, primarily located in the ______, the _______ ______ _____, and the _______ _____.
- opioid receptors
- CNS
- peripheral nervous system
- gastrointestinal tract
Onset of analgesic effect for oral opioids:
45 min
Peak effect of oral opioids usually occurs when?
1-2 hours after administration
Name some symptoms of opioid addiction or opioid use disorder.
- inability to control opioid use
- uncontrollable cravings
- drowsiness
- changes in sleep habits
- weight loss
- frequent flulike symptoms
- decreased libido
- lack of hygiene
- changes in exercise habits
- isolation from family and friends
- stealing from family, friends, or businesses
- new financial difficulties
What is Norco, Lortab, or Vicodin?
Combination of hydrocodone and acetaminophen
What is Percocet?
Oxycodone and acetaminophen
What is vicoprofen?
Hydrocodone and ibuprofen
The extended release (ER) form of all opioids should be used only for ______ _____ and is dosed ….
- chronic pain
- around the clock rather than on an as-needed basis
What is opioid-induced constipation?
Reduction of spontaneous bowel movement from baseline to typically < 3 bowel movements per week after commencing opioid therapy.
What reverses the constipation associated with opioids?
Peripherally Acting Mu-Opioid Receptor Agonists (PAMORA)
What happens when you combine opioids and benzodiazepines or sleep hypnotics?
- significant sedation
- respiratory depression
- coma, death
- should be avoided, especially when driving
What are the 3 primary FDA opioid warnings?
- Risk of addiction, abuse, and misuse.
- Life-threatening respiratory depression.
- Risks from concomitant use with benzodiazepines or other CNS depressants.
What effects does codeine have?
- low-potency opioid analgesic
- antitussive
What is the onset of action, peak effect, duration, bioavailability, and half life of codeine?
- onset of action: 0.5-1 hr
- peak effect: 1-1.5 hr
- duration: 4-6 hr
- bioavailability: 53%
- half life: 3 hr
How is codeine metabolized and excreted?
- hepatic
- urine, feces
What is equianalgesic?
- the standard against which new analgesics are measured
- morphine
What are congeners?
Semisynthetic derivatives
What effect does morphine have?
Medium-potency opioid analgesic
Routes of administration for morphine:
- oral (IR, ER)
- rectal
- IV
- IM
- SQ
What is the onset of action, peak effect, duration, bioavailability, and half-life of morphine?
- onset of action: ~30 min (patient dependent)
- peak effect: 1 hour
- duration: patient dependent
- bioavailability: 17-33% (first pass effect limits oral bioavailability)
- half life: 2-4 hr
How is morphine distributed?
- skeletal muscle, liver, kidneys, lungs, intestinal tract, spleen, and brain
- binds to opioid receptors in the CNS and periphery (eg. GI tract)
How is morphine metabolized and excreted?
- hepatic
- urine and feces
When is morphine indicated?
- for management of pain severe enough to require daily, around-the-clock, long-term opioid treatment
- alternative treatment options are inadequate
Name 2 synthetic derivatives of morphine. They are widely used in combination with _______.
- oxycodone
- hydrocodone
- acetaminophen
Hydrocodone is approximately equipotent to ______, with an onset of action of ______ min, duration of ______ hours, and a serum half life of about ______ hours.
- oxycodone
- 10-30 min
- 4-6 hours
- 4 hours
Fentanyl is ____ times more potent than morphine.
100
Fentanyl is most widely used for….
Intraoperative and periprocedural analgesia
Time to peak analgesic effect after IV administration of fentanyl vs morphine.
- ~ 5 min
- ~ 15 min
What routes of administration are preferred when using fentanyl for chronic pain management?
- poorly absorbed in the GI tract
- transdermal or buccal administration methods preferred
Transdermal fentanyl patches (Duragesic) provide sustained release for _____ hours. However, factors promoting increased absorption such as _______, _____ ______, can lead to overdosage and increased side effects.
- 48-72 hours
- fever, moist heat
The transdermal patch fentanyl is indicated only for what type of patients?
- opioid-tolerant patients
- patients who have been on 60 mg of morphine/day or an equianalgesic dose of another opioid for at least a week
How does Naloxone work?
Binds competitively to opioid receptors but does not produce an analgesic or opioid side-effect response. Used to reverse the toxic effects of opioid agonists.
- can completely or partially reverse opioid depression (including respiratory depression)
How much Naloxone can be administered how often?
2 mg every 2 or 3 minutes
