Opioids Flashcards
What is the MOA for opioids
Simulate opioid receptors (mu, kappa, and delta) in the CNS
What are the major AEs of the opioid analgesics (general)
Dependence Decreased GI motility Respiratory depression Somnolence Stimulation of CTZ Mood changes Increase in sphincter tone Tolerance Histamine release
Pneumonic: D(D)R. S(S)MITH
Opiod most common AEs and the most severe
MC: drowsiness, nausea, vomiting, contipation, pruritis
Most severe: Decrease respiratory rate
Opioid withdrawal symptoms
Minor: rhinorhhea, lacrimation, excessive yawning, mild irritability, mild N/V
Major: increasing reslessness, tremors, abdominal cramps, anxiety, persistent N/V, increased HR, BP, hot or cold flashes, fever
4 types of opioid and receptor drugs
Agonists (bind to mu receptor; best reponse)
Partial agonists (submax response at the receptor)
Agonist/antagonists (has an analgesia ceiling)
Antagonist (reverse/inhibit effects; good for tx OD/substance abuse)
Moderate pain agents related to Morphine (Phenanthrenes)
Codeine Codeine/APAP (Tylenol #3) Hydrocodone Hydrocodone/APAP (Vicodin) Oxycodone (Oxycontin) Oxycodone/APAP (Percocet)
Moderate pain agents: other opioid agonists
Meperidine (Demerol)
Tramadol (Ultram)
Tramadol/APAP
Tapentadol (Nucynta)
Severe pain agents related to Morphine
Morphine
Hydromorphone (Dilaudid)
Levorphanol
Oxymorphone
Severe pain agents: other opioid agents
Fentanyl (Sublimaze)
Methadone
Mixed mu agonists/antagonists
Butorphanol (Stadol)
Nalbuphine (Nubain)
Pentazocine (Talwin)
Mu partial agonists
Buprenorphine
Mu antagonists
Naloxone (Narcan)
Naltrexone (Depade)
Important info to know about codeine, hydrocodone, and oxycodone
They all metabolize to morphine
CYP2D6 metabolizers have increased risk of toxicity (codeine) or CYP3A4 substrate (hydrocodone, oxycodone)
Important info to know about Meperidine
Metabolite is a direct CNS irritant that can lead to seizures
Only use short term
Do not use with MAOI could lead to hypertensive crisis
Important info about Tramadol
1/3 of actions effect the mu and other 2/3 have actions on NE and seratonin reuptake