Pain 2 - Oops, All Opioids Flashcards
What are the 3 main opioid receptor subtypes? What does activation of each do?
- mu (µ):
- Analgesia, euphoria, physical dependence, respiratory depression, reduced GI motility ( –> constipation), sedation - delta (ẟ):
- Analgesia, euphoria, physical dependence - kappa (ϰ):
- Analgesia, sedation, ? mood, does NOT contribute to physical dependence
What are the “big 5” opioids?
- Morphine
- Codeine
- Hydromorphone
- Oxycodone
- Fentanyl
What is the MOA of opioids?
Opioid molecules bind to opioid receptors in the central and peripheral nervous system, suppressing neuronal firing from the presynaptic neuron and also inhibition of postsynaptic nerves in some areas, which ultimately alters the transmission and perception of pain
Opioid use in acute pain:
What is the usual oral starting dose and frequency of codeine IR? (tylenol + codeine + caffeine)
15-30mg q4h prn
Opioid use in acute pain:
What is the usual oral starting dose and frequency of hydromorphone IR?
1-2mg q4-6h prn
Opioid use in acute pain:
What is the usual oral starting dose and frequency of morphine IR?
5-10mg q4h prn
What should we be taking into consideration when using opioids in acute pain? (3)
- Lowest dose (should not need >50 MEQ), shortest duration
- Use clinical judgement re: quantity (consider limit to 3-5 days to start)
- Education about adverse effects including toxicity, take home naloxone
What are 3 advantages of opioid use in chronic non-cancer pain? (3)
- Potent analgesic effect
- Fast onset
- Relatively low risk of major organ toxicity
- Renal, hepatic, cardiac
What are the adverse effects of opioid use in chronic non-cancer pain? (7)
- CNS depression
- Falls/fractures
- Constipation
- Apnea
- Hypogonadism
- Opioid-induced hyperalgesia
- Dependence, opioid use disorder
What are some disadvantages (4) to opioid use in chronic non-cancer pain?
- Adverse effects (discussed in another card)
- Risk of diversion
- Tolerance –> withdrawal-mediated pain, escalating dose
- Long term evidence of benefit (>3 months) lacking
Opioid use in osteoarthritis, chronic low back pain, and neuropathic pain. Yay or nay?
Nay. Only unless exhausted all other possible options
When are oral IR opioids used?
Used for acute pain, breakthrough pain, or when initiating someone on chronic therapy
What are the non-oral opioid formulations available? (4)
- Buccal/sublingual
- Suppository
- Transdermal
- Injection
What is the initial dosing for controlled-/extended-release morphine tabs?
How about caps? (both 12h and 24h)
Tab: 10-15mg q12h
Cap (12h): 10mg q12h
Cap (24h): 10mg q24h
What is the inital dosing for oral IR morphine? What is the maximum?
5-10mg q4h prn, maximum 40mg/day
What is the mimumum time interval for dose increase of CR/ER morphine?
How about for IR morphine?
CR/ER: Minimum 2 days. Recommended 14 days
IR: 7 days
Which two opioids are “opiates”?
Morphine and codeine
Morphine is metabolized into two primary compounds (excreted in urine). What are they?
- Morphine-6-glucuronide
- Active analgesic - Morphine-3-glucuronide
- Not active as an analgesic, CNS stimulation
Morphine use should be monitored closely (or avoided) if CrCl <__-__mL/min
20-30
Morphine is the “reference” opioid. Meaning?
Use for conversion factor calculations
The MEQ of codeine is?
0.15
Codeine is a _______. Converted to morphine in the body via CYP___
prodrug; 2D6
What are 2 CIs for codeine?
- ≤12 years old
- ≤ 18 years old post op tonsillectomy and/or adenoidectomy
Codeine antitussive dose is?
≥15mg q4-6h