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39 Cards in this Set
- Front
- Back
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oral bioavailability of morphine (low or high)
administration of morphine rate of entering CNS (slow/fast) |
low
IM or IV slowly (compared to heroin or methadone, except in infants) |
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clinical uses of morphine
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post-op
renal colic MI pain for terminal illness (esp CA) |
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contraindications for morphine
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TBI
asthmatics (--> bronchoconstriction and histamine release) pts with decreased resp reserve hypovolemic pts liver or kidney dz |
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which receptor does methadone act on?
low or high bioavailability interaction of methadone with morphine t 1/2 of methadone |
mu
high cross tolerance and dependence 15-40hrs |
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uses of methadone
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similar to morphine
detox of morphineheroin abusers |
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receptors for meperidine
bioavailability metabolism of meperidine |
synthetic mu agonist
50% to normeperidine (causes convulsions) |
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contraindications of meperidine
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NEVER >1 week
NEVER with MAOI |
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which opiate is safe to use in pregnancy?
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meperidine
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what are the advantages to meperidine
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doesn't delay labor
doesn't elevate biliary tract pressure less constipation less miosis |
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metabolism of heroin
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converted to 6 monoacetyl morphine and morphine
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which is more potent: morphine or fentanyl
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fentanyl (100x more potent)
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which are the strong opioid agonists
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heroin
fentanyl morphine meperidine methadone |
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mild-moderate opioid agonists
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oxycodone
propoxyphene codeine tramadol |
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bioavailability of oxycodone
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high; not susceptible to 1st pass inactivation
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effects of propoxyphene
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CNS excitation
delusions hallucinations no eurphoria |
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interesting points about codeine
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10% of whites can't metabolize
commonly used as anti-tussive mild analgesic |
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MOA of tramadol
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centrally acting atypical agonist
weak mu agonist with GABA-ergic, NorE, and 5HT activiites |
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contraindications for tramadol
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SSRI
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examples of mixed agonists-antagonists
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pentazocine
buprenorphine nalbuphine butorphanol |
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pentazocine acts at which opioid receptor
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kappa agonist
mu partial agonist |
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effects of pentazocine at high doses
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dysphoria
anxiety nightmares |
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effects of nalbuphine and butorphanol
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similar to pentazocine
less likely to cause euphoria |
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ceiling effect seen in which drugs
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mixed agonists-antagonists
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receptor buprenorphine acts on
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mu partial agonist
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which drug is marketed as an alternative to methadone for opioid dependence
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buprenorphine
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MOA of dextromethorphan
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doesn't bind mu agonist
binds to receptor tha tmediates cough suppression safest anti-tussive available |
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which opioids are used as anti-tussives
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dextromethorphan
codeine hydrocodone |
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which opioids are used to treat diarrhea
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diphenoxylate
loperamide |
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MOA of diphenoxylate
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diminishes peristaltic reflex
At high doses, systemic my agonist effects are seen |
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what are the anti-diarrheal opioids combined with?
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atropine
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what are the pharmacological activities of opioid antagonists dependent on
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whether endogenous opioids have been released
whether opiate agonists have been been previously administered pharm profile of opiate degree of physical dependence |
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which opiate antagonist has the longest half life?
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naltrexone (14 h) > nalmefene (10 h) > nalaxone (48 min)
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which are the opioid antagonists?
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nalaxone
naltrexone nalmefene |
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which opioids have reduced 1st pass hepatic glucuronidation?
what accounts for this? |
codeine
hydrocodone oxycodone modification on the R1 (off of C3) |
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what do the delta opioid receptors do?
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spinal analgesia
decreaed GI motility |
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what do kapp receptors do?
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mediates analgesia through spinal cord
dysphoria disorientation anxiety |
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what do mu receptors do?
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mediate analgesia through supraspinal mechanisms
respiratory depression miosis euphoria decreased GI motility physical dependence |
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which are the endogenous opioids and which receptors do they selectively activate?
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enkephalins: delta
dynorphins: kappa b-endorphins: mu endomorphins: mu nociceptin: nu |
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where are enkephalins found?
how are they stored? |
adrenal medulla, GI, cortex, spinal cord
co-stored in adrenal medulla granules wiht NorE and Epi |
