Opioid Analgesics Flashcards
Three MoA of opioids
- Inhibit the transmission of nociceptive input from the periphery to the spinal cord
- Activate descending inhibitory pathways that modulate transmission in the spinal cord
- Later limbic system activity (pain perception)
What is each Mu receptor primarily responsible for?
Mu1 = analgesia
Mu2 = respiratory depression, Meiosis, reduced gastric motility, sedation, euphoria, pruritus, urinary retention, physical dependence
Which opioid is the most hydrophilic and which is the most lipophilic?
Morphine is the most hydrophilic, Fentanyl is the most lipophilic
Does tolerance develop equally to all opioid effects?
No, GI and Resp continue to be effected long after tolerance to the analgesic effect develops
What is the most serious AE w/opioid therapy?
Respiratory depression
Which opioid is associated with the greatest histamine release?
Morphine (oxycodone and fentanyl cause fewer)
What is the treatment for opioid toxicity?
Naloxone- pure opioid antagonist
Full agonists
Effectiveness is not limited by dose increases…pure agonist: do not antagonize the effects of other full agonists
Partial agonists
Medications have a ceiling analgesic effect whereas the pure agonists do not…meaning greater doses won’t increase analgesic effectiveness, only greater SEs
Partial/mixed agonist
Agonist for some receptors and antagonist for others
Antagonist
No analgesic effect, used to block the effect of opioids
Anti-tussive opioids work by inhibition of the coughing center in the medulla, but don’t cure the irritation, what are the three opioids used for this?
Codeine (MC)
Hydrocodone
Dextromethorphan
Phenanthrene opioids to remember
Morphine Hydromorphone (Dilaudid) Hydrocodone ER Hydrocodone/APAP (Vicodin, Lortab) Levorphanol Oxycodone (OxyContin) Oxycodone/APAP (Percocet) Oxymorphone (Opana) Codeine Codeine/APAP (Tylenol #3) Mixed agonist/antagonist - Buprenorphine - Butorphanol - Nalbuphine Heroin
Strong agonist, slow and erratic oral absorption, enters all body tissues, least lipophilic, crosses placenta…used for pain
Morphine
Two opioids that are metabolized to morphine
Heroin and codeine (so morphine in urine could mean exposure to morphine, heroin, or codeine)
AEs for this opioid: Increase in ICP, so significant caution in severe head injury…N/V, itching, hypotension
Morphine
Metabolite of morphine with better oral absorption, more fat soluble than morphine for moderate to severe pain…ER form is a Risk Evaluation and Mitigation Strategy (REMS) drug that requires provider training every 2 years
Hydromorphone (dilaudid)
Opioid that’s a moderate agonist, metabolized to hydromorphone for moderate to severe pain…there are two combination forms
Hydrocodone ER