Term
| compunds related to those found in opium |
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Definition
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Term
| agents which has funcitonal properties of an opiate |
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Definition
|
|
Term
| what are the endogenous opoid peptides -3 |
|
Definition
enkephalins
endorphins
dynorphins |
|
|
Term
| endogenous opoids do what things-2 |
|
Definition
inhibit transmission from C fibers
reduce dorsal horn nueron exictability/transmission |
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|
Term
| where are opoid receptors located?-2 |
|
Definition
presynaptic C fibers
dorsal horn |
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|
Term
what is the main recptor do the opioids act on-
what is the affinity for the 3 peptides?
where is the recpt located?-3 |
|
Definition
mu (M)
endorphins>enkephalin>dynorphin
brain, spinal cord, peripheral |
|
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Term
| what is the funct of mu opoid recpt-4 |
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Definition
| analegia, inhibit resp, slow GI, hormone rleease |
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Term
| what recptro is invovled in ALL endogenous opoid pepties and most opiates? |
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Definition
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|
Term
the Mu recptor is most important for?
it can also do? |
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Definition
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|
Term
delta recptors have high affinty for?
they inhibit? |
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Definition
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Term
| which recptor is associated wiht sedation and dysophoria |
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Definition
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|
Term
| what is the only recptor associated wiht psychomimetic effects |
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Definition
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|
Term
| which recpt is no longer a opoid recpotr? |
|
Definition
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|
Term
analgeisa by endogenous opoids is mediated by-2
at high doses it inhibits |
|
Definition
spinal and supraspinal
pain perception and affective pain |
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|
Term
| if depednce devlops with endogenous opioids what happens |
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Definition
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|
Term
| endogenous opioids are broken down bby- |
|
Definition
|
|
Term
| what side effects are with endogenous opioids |
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Definition
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|
Term
| MOA of opioids acting on MOR -3 |
|
Definition
reduce pain stimuli
reduce action potential on presynaptic
inhibit postsynaptic (hyperpolar) |
|
|
Term
| opioid recptors are couples to what-2 |
|
Definition
| G rpotein and adenyl cyclase |
|
|
Term
activaiton of opoid receptors decreases -
this leads ot efflux of -1
the result is? |
|
Definition
cAMP
K
hyperpolar, decrease nerve firing |
|
|
Term
| opioid action on nociceptors |
|
Definition
| decrease peripheral nerves |
|
|
Term
opioid action on spinal cord:
binding to presynaptic MOR
" " postsynaptic MOR |
|
Definition
decrease Ca, prevent NT release (Glu)
increase K efflux, hyperpolarization |
|
|
Term
| MOA of opiods on supraspinal |
|
Definition
| decrease dorsal horn excitability |
|
|
Term
| MOA of opioids on limibic system |
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Definition
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|
Term
| which drug is an agonist at ALL opioid recptors |
|
Definition
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|
Term
| what repctor does morphine have highest affinty for? |
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Definition
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|
Term
| which drug is most important for severe pain? |
|
Definition
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|
Term
| morphine reduces what 2 things |
|
Definition
pain perception
affective pain processing |
|
|
Term
morphine isnt good for? -2
which work better? why? |
|
Definition
inflammaotry pain (toothache
headache
NSAIDS; inhibit prostoglandins |
|
|
Term
morphine has potential depednce on what
when is it rare to occur |
|
Definition
euphoria
when used for chronic pain |
|
|
Term
|
Definition
somnolense/sedation
resp depresison
nasuea/vomit
pupillary constict
HPA inhibtion of hormones (prolactin, growth hromone) |
|
|
Term
| miosis (pupil cnstrict) is apparetn in who |
|
Definition
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|
Term
| morphine peripheral ADEs-4 |
|
Definition
GI/ constipaiton
cardiovasc/ orthostatic hypotension
psuedo allergic reaction/histamine release
immune syst |
|
|
Term
| what is the absorption of morphine |
|
Definition
|
|
Term
| what accounts for the analgesic effects of morphine? |
|
Definition
|
|
Term
| what moprhine metabolite contributes to the excitatory effects |
|
Definition
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|
Term
| morphine should be avoided or closely monitoried in who |
|
Definition
| neonates (have immature BBB and immature liver for metab) |
|
|
Term
| why does chronic use of opioid agonist lead to loss of effect? |
|
Definition
| reduced inhibition of cAMP (lose sedation or analgesic) |
|
|
Term
|
Definition
|
|
Term
|
Definition
| have withdrawl symtpoms so person has this state of adaptation |
|
|
Term
| do tolerance nad dependence lead to addiciotn? |
|
Definition
|
|
Term
| look on slide 20 for recptor slecvitity for agents |
|
Definition
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|
Term
| the selective MOR morphine derivatives-3 |
|
Definition
oxycodone
hydrocodone
codeine |
|
|
Term
|
Definition
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|
Term
| which drugs are used for moderate severe pain-2 |
|
Definition
|
|
Term
| which drug is for moderate pain |
|
Definition
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|
Term
| which drug is metab by 2D6 |
|
Definition
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|
Term
| which drug has celing affect of 100 mg (no more analgesia affect) |
|
Definition
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|
Term
piperidine opioids:
modificaiotn on the _ alter slectivity
_ on the side chains contrivbutes to CNS penetraiton an potency |
|
Definition
|
|
Term
| What are the piperidine opioids-5 |
|
Definition
fentanyl
sufentanil
remifentanil
meperidine
methadone |
|
|
Term
| what drug is 100x more potent than morphine |
|
Definition
|
|
Term
| for chronic pain how is fentantly admin |
|
Definition
|
|
Term
| which drug is 1000x more potent than morphine |
|
Definition
|
|
Term
| what is for short surgicla proceuders |
|
Definition
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|
Term
| what drugs cna be used for labor or psot op-2 |
|
Definition
|
|
Term
| meperidine has less what ADe |
|
Definition
|
|
Term
meperidine can cause more what?-4
other side effects? |
|
Definition
CNS exictiaiton, tremor, muscle twitching, seizures;
resp dep, histamine release |
|
|
Term
methadone has no _
so it can be used for-3 |
|
Definition
euphoria
opioid absensce relief, chronic pain, heroin users |
|
|
Term
| which drug has half life of 24 hours |
|
Definition
|
|
Term
| which drug is metab byu 3A4 |
|
Definition
|
|
Term
look on slide 2 for methadone metabolites
look on slide 28 to see the diff recpt afifnity and time it takes for response |
|
Definition
|
|
Term
partial agonist alone have _
what can they do if combined with agonist? |
|
Definition
agonist - just not as potent
antag |
|
|
Term
| what are the partial agonists/antagonists-4 |
|
Definition
pentazocine
nalbuphine
butorphanol
buprenorphine |
|
|
Term
| the partial agonists/antagonists are _ antagonists and _ agonists? |
|
Definition
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|
Term
| agents that work thru KOr are more effective for what gender? |
|
Definition
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|
Term
| which drug cna be used for migraines |
|
Definition
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|
Term
| the partial agonists that can show antagonism if used with full agonist is- |
|
Definition
|
|
Term
| what can be used with fentanyl to antagonize the resp depression without affecting the analgesia efects |
|
Definition
|
|
Term
| buprenorphine has _ half life bc of? |
|
Definition
long
very high affinty for recptors |
|
|
Term
| tramadol is a stonrg/weak MOR antag/agon |
|
Definition
|
|
Term
| tramadol inhibits the re-uptake of-2 |
|
Definition
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|
Term
| opioid antagonist is used for? |
|
Definition
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|
Term
| in absnece of opioid over dose hte antagonists have few effects but can do |
|
Definition
| slight drowsiness and increase hormones/cortisol |
|
|
Term
| what is opioid antagonist-2 |
|
Definition
nalaxone (onlyneed small doses)
naltrexone |
|
|
Term
| in opioid depedent pt the use of opioid anatagonist can cause - |
|
Definition
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|
Term
which opioid antagonist has quick onset/half life?
how is it admin? |
|
Definition
|
|
Term
other analgesic drugs:
NSAIDS/salysilytes-3 |
|
Definition
ibuprofen, apsirin, naproxen
(APAP can be used too) |
|
|
Term
| the other analegeic drug for COX 2 inhibiton |
|
Definition
|
|
Term
| the other alangesic drug for topical use-2 |
|
Definition
|
|
Term
treatment of chronic/neuropathic pain what isnt effective
what have a lot of ADEs if used |
|
Definition
|
|
Term
| what drugs cna be used for neuropathic/chronic pain-5 |
|
Definition
gabapentin, carbamezapine (antiepleipti)
cymbalta, (5Ht, Ne inhibit) imipramine, amitryptiline (TCAs) |
|
|
Term
| slide 36 for the exact MOA of all the analgesics |
|
Definition
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|
