Term
| Name 3 strong opioid agonists |
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Definition
| morphine, methadone and fentanyl |
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Term
| How do hydromorphone and oxymorphone compare to morphine? |
|
Definition
| similar efficacy but higher potency |
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Term
|
Definition
| a strong opioid agonist with anticholinergic effects |
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Term
| How do sufentanil, alfentanil and remifentanil compare to fentanyl? |
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Definition
|
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Term
| What are morphine, fentanyl and methadone? They work on which receptors? |
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Definition
| Strong m-receptor agonists, variable affinity for d and k receptors |
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Term
| mu receptors depress ____, k are involved with ____ actions, and d is involved with ______ |
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Definition
| respiratory center, sedative, tolerance |
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Term
| What are the effects of morphine, methadone and fentanyl? |
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Definition
| analgesia, relief of anxiety, sedation, slowed GI transit |
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Term
| Which drug is used in pulmonary edema? |
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Definition
|
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Term
| Are strong opioid agonists susceptible to first pass effect? |
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Definition
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Term
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Definition
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Term
| How do codeine and hydrocodone compare to morphine, in regard to the MOA? |
|
Definition
| less efficacious than morphine, can antagonize strong agonists |
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Term
| what are the effects of codeine and hydrocodone, compared to morphine? |
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Definition
| like strong agonists, with weaker effects |
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Term
| What are the partial agonists used for? |
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Definition
| mild-moderate pain and cough (codeine) |
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Term
| The toxicity of which drugs depends on genetic variation of metabolism? |
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Definition
| partial agonists - codeine and hydrocodone |
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Term
| Name 2 mixed opioid agonist-antagonists |
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Definition
| buprenorphine, nalbuphine |
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Term
|
Definition
| mixed opioid agonist-antagonist |
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Term
|
Definition
| mixed opioid agonist-antagonist |
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Term
| Opioid analgesics are relatively contraindicated in pts with which injuries? |
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Definition
|
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Term
| The active metabolite of codeine is... |
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Definition
|
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Term
| meperidine is metabolized to _____, which can cause ____ at high levels |
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Definition
|
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Term
| opioids _____ synaptic activity |
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Definition
|
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Term
| all 3 major opioids receps are coupled with _______ and activate _____ or inhibit _____ |
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Definition
| G-proteins, PLC, adenylate cyclase |
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Term
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Definition
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Term
| Nausea and vomiting from opioids is caused by... |
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Definition
| activation of chemoreceptor trigger zone |
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Term
| Except ____, opioids cause contraction of biliary tract smooth muscle, which may cause biliary colic or spasm, increased ureteral and bladder sphincter tone, and a reduction in uterine tone. |
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Definition
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Term
| _________ constriction is a characteristic effect of all opioids, except meperidine, which has a muscarinic blocking action. |
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Definition
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Term
| opioids can cause flushing and pruritis, in part through ____ release |
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Definition
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Term
| Which drugs cause release of ADH and prolactin, but inhibit the release of LH? |
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Definition
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Term
| Exaggerated responses to opioid analgesics may occur in pts with... |
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Definition
| adrenal insufficiency or hyperthyroidism |
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Term
| Tolerance to opioid analgesics does not apply to which effects? |
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Definition
|
|
Term
| What kinds of drugs are reported to block opioid tolerance? |
|
Definition
| antagonists of glutamate NMDA recepts and d-receptor antagonists |
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Term
| What is the basis for opioid rotation? |
|
Definition
| cross-tolerance is not complete |
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Term
| Rhinorrhea, lacrimation, chills, gooseflesh, muscle aches, diarrhea, yawning, anxiety and hostility are features of... |
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Definition
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Term
| Important drug interactions occur between opioids and... |
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Definition
| ethanol, sedatives, anesthetics, antipsychotics, tricyclics, antihistamines |
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Term
| Use of certain opioids, like meperidine, together with monoamine oxidase inhibitors increases the risk of... |
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Definition
|
|
Term
| ____ has been implicated in serotonin syndrome when used with SSRIs |
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Definition
|
|
Term
| Describe the MOA of buprenorphine |
|
Definition
| partial m agonist, K antagonist |
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|
Term
| describe the MOA of nalnuphine |
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Definition
|
|
Term
| What are the effects of buprenorphine? |
|
Definition
| like strong agonist, but can antagonize their effects, also reduces craving for alcohol |
|
|
Term
| what are the effects of nalbuphine? |
|
Definition
| like strong agonists, but can antagonize their effects, also reduces craving for alcohol |
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Term
| What are the indications for buprenorphine? |
|
Definition
| moderate pain, some maintenance rehab programs |
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Term
| What are the indications for nalbuphine? |
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Definition
|
|
Term
| Which drugs have a long duration of action - 4-8 hrs, and may precipitate abstinence syndrome? |
|
Definition
| buprenorphine and nalbuphine |
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|
Term
| pentazocine is what kind of drug? How does it compare to the others in this class? |
|
Definition
| Mixed agonist-antagonist, less analgesia |
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Term
| Butorphanol, nalbuphine and pentazocine are ___ agonists with weak antagonist effects at __ and __ recepts |
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Definition
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Term
| Butorphanol may act as a partial agonist or antagonist at the ___ recep |
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Definition
|
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Term
| Which drugs may be resistant to naloxone reversal? |
|
Definition
| buprenorphine and nalbuphine |
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|
Term
| Mixed agonist-antagonist drugs - side/adverse effects? |
|
Definition
| sedation at analgesic doses, dizziness, sweating, nausea, anxiety, hallucinations, nightmares, respiratory depression may be less intense but is not as reliably reversed by naloxone, tolerance and physical dependence are less than pure agonists |
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Term
| Naloxone, nalmefene and naltrexone are... |
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Definition
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Term
| Naloxone, nalmefene and naltrexone have greater affinity for ___ recepts than for the others |
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Definition
|
|
Term
| naloxone and nalmelfene are given... |
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Definition
|
|
Term
| describe the DOA of naloxone |
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Definition
|
|
Term
| Naltrexone has a long half-time, blocking the actions of strong agonists for up to.. |
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Definition
|
|
Term
| Naltrexone decreases the craving for ____ |
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Definition
|
|
Term
| Describe the MOA of dextromethorphan |
|
Definition
| poorly understood, but strong and partial m-agonists are also effective at decreasing cough |
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|
Term
| How long is the DOA of DM? |
|
Definition
|
|
Term
| Nalmefene has a DOA of... |
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Definition
|
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Term
| What are alvimopan and methylnaltrexone? What are they used for? |
|
Definition
| potent m antagonists with poor entry into CNS, may be used to treat severe opioid-induced constipation without precipitating abstinence syndrome |
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Term
|
Definition
| moderate m agonist, strong NET inhibitor |
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Term
| What is tapentadol used for? Toxicity? |
|
Definition
| moderate pain, headache, nausea and vomiting, possible dependence |
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|
Term
| What is the MOA of tramadol? |
|
Definition
| mixed effects - weak m agonist, moderate SERT inhibitor, weak NET inhibitor |
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|
Term
| What is tramadol used for? Tox? |
|
Definition
| moderate pain, adjunct to opioids in chronic pain syndrome. Seizures. |
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