Opioids Flashcards
What is a classical analgesic receptor?
mu receptor
What are opioids a mix of?
Agonist-antagonist agents
What is an opiate? What are some examples?
Natural agents from opium
Codeine, morphine
What are opioids?
Modifications of natural opiates (synthetics)
What are some examples of mixed opioid agonists?
Buprenorphine
Butorphanol
Pentazocine
Nalbuphine
Are mixed agents frequently or infrequently used?
Little used
What is an exception to the little use of mixed opioid agonist-antagoinsts?
Nalbuphine
Describe nalbuphine
More effective in females
Ceiling effect on respiratory depression
Used in L&D
What are endorphins derived from?
Small endogenous peptide hormones
What do endorphins account for?
Variability of response to pain
List the SEs to opiates/opioids
Nausea Itching Sedation & cognitive impairments Respiratory depression (possibly life-threatening) Meiosis (pinpoint pupils) Decreased GI peristalsis -> constipation
How do we deal with the effects of opioids on the GI tract?
Anticipate and prophylax
Can we expect tolerance to opioid constipation?
No
Review slide 42
Bowel regimens for opioid constipation
What opioids do we use for mild-moderate pain?
Tramadol
Codeine
Hydrocodone
What kind of opioid is tramadol? What is it useful for?
Weak opioid analgesic
Useful for chronic pain
What are the 3 forms of tramadol?
Immediate release
Tramadol 37.5mg/acetaminophen 325 mg
ER tabs
What happens as we increase dosage of tramadol over weeks? What does this mean?
High incidence of NV
Limits use for acute pain
Does tramadol have a single or dual MOA
Dual
What is tramadol useful for?
Neuropathic pain
Is tramadol a controlled substance? If so, why? When did this happen if it did?
Yes
Less abuse potential
2014
What kind of opiate is codeine?
Weak analgesic and antitussive
Relate codeine to ASA
60 mg less effective than 650 mg aspirin
What is codeine metabolized by? What does this metabolize codeine to?
CYP2D6
Morphine
What does CYP2D6 inhibitors do to codeine? Give some examples
Decrease its effect Antiemetic phenothiazines (thorazine, compazine, phenergan) Haloperidol Fluoxetine Paroxetine
What % of the population lack the CYP2D6 enzyme?
10%
What forms does codeine come in?
Codeine (C-II)
Tylenol w/ codeine (C-III)
Guaifenesin w/ codeine (C-V)
How is hydrocodone available PO?
Only available w/ acetaminophen PO
How many mg does hydocodone exist w/in Norco?
325 mg
Give two more examples of hydrocodone PO meds
Lortab
Vicoden
How does hydrocodone relate to codeine?
Better pain relief
Longer duration
What is hydrocodone metabolized by and to what?
CYP2D6
Hydromorphone
What % of unintentional overdoses involve combination products? What is the MC opioid in these combination products?
63%
Hydrocodone
What opioids do we give for moderate to severe pain?
Morphine Hydromorphone Oxycodone Meperidine Methadone Fentanyl