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Opioids
| Question | Answer |
|---|---|
| What are endogenous opioid peptides? | neurotransmitters or neuromodulators for inhibitory neurons in pathways operating for pain sensation |
| Where do endogenous opiod peptides act? | acts at substance P / glutamate synapses |
| clinical effects of mu receptor mediation? | euphoria, analgesia, physical dependence, respiratory depression |
| clinical effects of kappa receptor mediation? | miosis, analgesia of Talwin (pentazocine), sedation |
| What is the MOA of opioids? | link to Gi proteins → inhibit adenylyl cyclase → ↓cAMP (hyperpolarized cell)→ CA++ entry blocked (can't get in so ↓intracellular Ca+)& K+ channels open (K+ leaves the cell so ↓intracellular K+ → ↓ release of neurotransmitter → ↓nociceptive pain |
| opium derivative agonists? | morphine, codiene, heroin, hydromorphone, oxymorphone, hydrocodone, oxycodone |
| synthetic opioid agonists? | meperidine, methadone, propoxyphine,levorphanol |
| opioid partial agonists? | pentazocine, buprenorphine, butorphanol, nalbuphine |
| opioid antagonists? | naloxone (IV only, Narcan), naltrexone, nalmefine |
| what would happen if a patient being given morphine for pain but who cont'd to c/o of pain was then given pentazocine (Talwin) or buprenorphine (Buprenex)? | pain would get worse because talwin would partially bind receptors preventing morphine from binding with them. |
| Morphine-6-glucuronide | active metabolite of morphine contributes siginificantly to analgesia |
| Morphine-3-glururonide | inactive metabolite of morphine contributes siginificantly to dysphoric side effects |
| Which of the opioids crosses BBB the most significantly? | heroin |
| GI peripheral effects of morphine? | increase pyloric sphincter tone, decreased peristalsis with resultant delayed gastric emptying and constipation AND bile duct spasm d/t increased biliary pressure |
| GU peripheral effects of morphine? | increased bladder sphincter tone with resultant decreased urinary output d/t urinary retention |
| Acute toxic symptoms of morphine overdose? | TRIAD of coma, pinpoint pupils and respiratory depression |
| Morphine effects can be prolonged or exaggerated by? | CNS depressants, phenothiazines (atypical antipsychotics), TCAs, cimetidine |
| What are the cautions to morphine administration? | bronchial asthma (d/t histamine release), emphyzema, liver damage, head injuries (↑cerebral vasodilation, miosis, LOC changes), acute alcohol use (potentiation of effects), previous addiction, convulsive disorders, abdominal pain of unknown origin |
| What is 3,6-diacetylmorphine | heroin |
| difference between codiene & morphine? | codiene has greater oral efficacy d/t low 1st pass hepatic metabolism |
| 54 yo white male who is taking codiene for pain and says its not working, what might you suspect? | lack of cytochrome 2D6 enzyme to metabolize it to morphine |
| -codones are prodrugs and (i.e., oxycodone, hydrocodone) are metabolized to? | corresponding -morphone (i.e., oxymorphone, hydromorphone) |
| differences between meperidine & morphine? | demerol faster onset but shorter duration, meperidine less potent, not antitussive, less constipation and produces less biliary spasm |
| What is normeperidine? | a metabolite of meperidine, a CNS stimulant that can accumulate with repeated or chronic demerol administration can cause convulsions |
| your patient has been receiving demerol q6hrs for the last 4 days, he suddenly begins siezing, what would you give? | diazepam is the only antagonist of normeperidine, a metabolite of demerol that will accumulate with prolonged or chronic dosing |
| demerol is contraindicated with? | MAOIs and SSRIs d/t potential for seratonin syndrome |
| diphenoxylate / atropine | lomotil |
| difference between morphine & methadone? | methadone has greater oral efficacy and extended duration of action, used for suppressing withdrawal from opioids |
| methadone may cause what dysrrhythmia? | torsade de pointes |
| a weak analgesic with strong side effects? | propoxyphene (Darvon) |
| tramadol MOA? | binds to mu receptors and inhibits NE and 5HT reuptake |
| Injection of an opioid antagonist to a person who has physical dependence to an opioid can cause? | withdrawal syndrome |
| Used for moderate/severe pain? | morphine, meperidine, methadone, fentanyl |
| used for mild/moderate pain? | codiene, oxycodone, pentazocine |
| used for obstetrical pain? | meperidine because there is a lesser degree of respiratory depression in fetus and it does not inhibit uterine contraction |
| prototype opioid agaonist to which all other opioids are compared? | morphine |
| Why does morphine tend to cause nausea & vomiting? | direct dtimulation of dopamine receptors in the chemoreceptor trigger zone in the floor of the fourth cerebral ventricle |
| To avoid N&V, what position should your patient be in prior to administration of morphine? | recumbent, N&V are relatively uncommon in recumbent patients suggesting that a vestibular component may contribute to opioid-related N&V. |
| an analogue of fentanyl that is 5 to 10 times more potent? | sufentanil |
| an analogue of fentanyl that is 1/5 to 1/10 as potent and has 1/3 the duration of action but a more rapid onset of action? | alfentanil |
| an opioid agaonist with similar potency to fentanyl, fast "on & off" like alfentanil but has an ester linkage? | remifentanil |
| Your patient is in severe pain what would you give? hydrocodone or propoxyphene? | hydrocodone |
| You have a patient that you're concerned about addiction and abuse of pain medicines but he is having moderate pain, what could you give? | toradol |
| A patient presents with pinpoint pupils, depressed respirations and decreased LOC; what would you suspect? | opioid overdose |
| In an acute opioid overdose what would give you the fastest results? | naloxone IV |
| A patient who is a known heroin addict presents with what appears to be an overdose; why not give him naloxone? | you would percipitate a withdrawal syndrome which could prove to be fatal to this long term opioid addict, it is best to support the patient otherwise (ventilatory and CV if necessary) until the symptoms lessen. |
| Binding of hydrocodone (Hycodan) to Mu opioid receptors results in? | decreased intracellular potassium |
| What is responsible for the flushing , itching, rashes and sweating associated with opioid administration? | histamine release |
| What peripheral effects do NOT develop a tolerence to opioids? | miosis, constipation & seizures |
Created by:
psfisher50
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