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29 Cards in this Set
- Front
- Back
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metabolites of morphine
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M-3-glucuronide - non-active metabolite that has neuroexcititory activity
M-6-glucuronide - active metabolite |
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mechanism of action in general for opioid analgesics
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inhibit synaptic activity through direct action of opioid receptors and partly through release of endogenous opioid peptides (B-endorphin, enkephalin, dynorphin)
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Differentiate the pre-synaptic and post-synaptic activity of opioids
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pre-synaptic - decrease Ca influx and decrease transmitter release
post-synaptic - increase K conductance to cause hyperpolarization |
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strong opioid agonist (phenanthrene)
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morphine
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partial opioid agonist (phenanthrene)
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codeine
hydrocodone oxycodone |
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strong opioid agonists (phenylpiperidine)
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fentanyl
meperidine |
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strong opioid agonist (phenylheptylamine)
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methadone
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partial opioid agonist (phenylheptylamine)
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propoxyphene
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drugs that are u-agonists as well as NMDA antagonists
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methadone
propoxyphene |
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weak u agonists; inhibits NE and 5-HT transporters
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tramadol
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adverse effect of tramadol
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seizures
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k-receptor agonist with weak u-receptor antagonist activity (mixed agonist-antagonist)
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pentazocine
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opioid associated with use for acute debilitating cough
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codeine
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antagonists at all receptors
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naloxone
naltrexone |
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used for alcohol dependence
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naltrexone
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useful in acute pulmonary edema because of hemodynamic actions and calming effects
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morphine
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used for treatment of opioid overdose, rsult in prompt signs of recovery
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naloxone
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triad of opioid overdose
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pupillary constriction
comatose state respiratory depression |
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two classes of drugs that are dangerous to take with Meperidine
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SSRIs - serotonin syndrome
MAOIs - hyperpyrexic coma |
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important drug interactions with opioid analgesics
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ethanol
sedative-hypnotics anesthetics antipsychotics TCAs antihistamines *all are CNS depressants |
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effects associated with mixed agonist-antagonist, pentazocine
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sedation at analgesic doses
dizziness, sweating, nausea, anxiety, hallucinations |
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very weak opioid agonist, avaiable in combination with acetaminophen
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propoxyphene
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systemic effects of opioids
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analgesia
sedation respiratory depression nausea/vomiting constipation miosis flushing and pruritis increased release of ADH and prolactin with inhibition of LH release |
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opioid receptors and their effects
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u - respiratory depression and physical dependence
k - sedation and reduced gastrointestinal transit d - tolerance |
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what two things does the body not develop tolerance to with respect to opioid use
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constipating effects
miotic actions |
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what drug was the patient taking along with meperidine that developed seizures then a coma
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MAOI - phenelzine
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what drugs are metabolized by the liver and associated with genotypic polymorphisms that are responsible for variations to analgesic response
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codine
hydrocodone oxycodone |
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contraindications for use of strong opioids (morphine)
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1. Addison's disease
2. hypothyroidism 3. head injury 4. biliary tract surgery 5. late stages of labor |
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effects of propoxyphene overdose
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respiratory depression
circulatory collapse pulmonary edema seizures |
