Pharm test 2 Flashcards
Efficacy
Maximal response a drug can produce
Potency
Measure of dose required to produce a response
Name strong opioid agonist (high efficacy)
Morphine, methadone, Fentanyl, oxycodone, and heroin
Name partial agonists for opioid
Codeine, hydrocodone, tramadol, tapentadol
Opioids that also have antidepressant
Tramadol and tapentadol
What would you use to treat a opioid addiction as an alternative to methadone
Buprenorphine (partial mu agonist, kappa opioid antagonist) -compete with heroin, so can’t get high because buprenorphine higher affinity -must give sublingual, because inactive if given orally -slow acting
A patient comes in with an opioid overdose what do you use to treat them?
Naloxone ( not orally active ) Antagonist with high affinity, no efficacy
A patient is struggling with alcohol dependence and comes to you for help. What drug can you give them to help?
Naltrexone (Is orally active) Antagonist with high affinity, no efficacy
How does morphine and other related opioids work? Side effects?
Activate the mu opioid receptor Side affects: constipation, respiratory depression, analgesia, sedation
Tolerance of opioids causes want?
Increase dose required to produce desired therapeutic effects
Physical dependence of opioids withdrawl signs?
Muscle aches, insomnia, rhinorrhea, your name, piloerection
Hyperalgesia opiods
Can happen when go off opioids Sensitization of pronociceptive pathways
Heroin pharmakinetics
Opioids: Rapid onset blood brain barrier, short duration ( more hydrophobic form)
Methadone, oral pharmakinetics
Opioids: Slowly absorbed, slowly penetrate. Slowly cleared, so drug accumulation can occur more easily and lead to toxicity. Hard to up titrate
Naloxone, oral pharmakinetics
Prevent abuse of drugs when combine with other drug. Opioids: Rapid metabolized, give with buprenorphine or oxycodone to prevent diversion Can put inside drug so get withdrawl effects if inject (abuse deterrent)
Loperamide, oral pharmakinetics
Opioids: Doesn’t penetrate brain, anti diarrheal ( reduce gut motility)
18-year-old woman with severe hip pain and shoulder pain after hip and shoulder contusions 4 hours after a bicycle accident. No fractures or a head injury. Which opioid would you choose for treatment and why?
oral hydrocodone (opioid use for acute pain)
32-year-old woman with uncontrolled rheumatoid arthritis while on DMARD (disease modifying antirheumatic drug) and severe polyarthralgias, is still experiencing severe pain every 3 to 4 hours after taking moderately high does oxycodone on for more than two weeks. Which opioid would you choose to give this patient?
Oxycodone extended release oral (Chronic pain opioids) -last 3-4 hours but extended release mean release for 12 hours -taking more than 2 weeks mean tolerance build up
35-year-old woman with the right femoral fracture that occurred after a fall injury. He is on buprenorphine/naloxone sublingual and clinic record support good control of her opioid use disorder. You recognize the obvious need for opioid to manage her severe pain prior to admission to orthopedics for urgent surgical internal fixation. Which opioid would you choose?
-Fentanyl IV -Need to treat with something with higher affinity, because she is on buprenorphine which has such a high affinity.
23-year-old male methadone user had a witnessed overdose and was transported to your ED following a bystander administration of Evzio (naloxone hydrochloride injection). He is awake and in acute withdrawal, but while in the ED he becomes increasingly more sedated. Why?
Naloxone is short acting and methadone is long acting, so methadone OD symptoms return after naloxone metabolized -give naloxone IV and wait til methadone clears
46-year-old man with severe pain immediately after surgery for partial colon resection, following ruptured diverticulitis. Nausea and vomiting from post op. Has hypomotility of the gastrointestinal tract in the absence of mechanical bowel obstruction. Which opioid would you choose?
- morphine IV -no addiction problems -oral route won’t work because vomitting -(can’t give fentanyl transdermal because takes to long to clear, get stuck in fat)
How do volatile anesthetics work?
-Decrease effectiveness of excitatory transmission (glutamatergic) -increasing effectiveness inhibitory (GABArrgic) -effect throughout CNS