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40 Cards in this Set

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Thre main proteins cleaved to make endogenous opiods
POMC
Proenkephalin
Prodynorphin
Three major biologically active opiods?
Metenkephalin
Leu-enkephalin
Dynorphin A and B
the main receptor subtype of medical relevance
mu
Ion channel effects of opiod receptor activation
increase potasium going out
decrease calcium coming in

net effect, inhibition both pre and post synaptically
Endogenous opiods and PCP
endogenous opiods don't bind to PCP receptor sites!
allodynia
pain cause by previously inocuous stimuli

Prostoglandins sensitize nervers to sensation from stretch, head, chemicals
Drugs that can be combine with opiods to increased efficacy
SSRI b/c serotonin modulates opiod interneurons in the dorsal colum

NSAIDS b/c prostoglandins sensitize nociceptors
Why you don't administer O2 to a patient on morphin
Morphin depresses response to hypercapnia, so high C02 and carotid O2 are main resp drive. Giving pure O2 depresses drive and can cause resp failure
Tx for first dose nausea with morphine
Procholorperazine or chlorpromazine

Patients generally becomes refractory to nauses after initial dose
Morphines effect on autonomin system
Depress sympathetic tone causing vasodilation

May cause orthostasis in normal people or worse in hypovolemic
GI effects of morphine
Acts on nerve plexi and reduce propulsive contraction and increase spasm. Atropine lowers spasm so Atropine + morphine good anti-diarrheal
Tx for actue morphine poisioning
repeat injection of naloxone

Naloxone may precipitate withdrawal if patient is dependent on morphine
withdrawl from opiods vs withdrawls from ehtanol/barbits
morphine withdrawls is less severe
Codeine
Fully absorbed orally unlike morphine (1/5) so is as effect as parenterally
hydromorphone, oxymorphone
like morphine but more potent
oxycodone and hydrocodone
used as antitussive and alagesic mixtures

equal to morphine but better absorbed orally
Heroin
prodrug for morphine that rapidly, rapidly crosses BBB
Leveorphanol
optical isomer is dextromorpha
Meperidine
Demerol

Preferred opiate for OB because it has less constipation, urine retention, fetal resp depression and does not prolong labor
Mechanism of action for Meperidine
Broken to meperidinic acid (analgesia) and normeperidine (excitatory) in the liver
Naloxone with meperidine
Naloxone blocks the analgesic properties of meperidine, but not the excitatory, so it can lead to convulsions
Diphenoxylate
Lomotil

Insoluable so no absorbed. With atropine, works as a good antidiarrheal with no CNS effects
Fentanyl
80 potentcy of morphine
Methadone
Morphine plus

Little higher oral absorbed
Longer half life
Less withdrawl
Propoxyphene
slightly less effective than codeine but less addictive because you get toxic before you get high of codeine
1-acetylmethadol
long lasting opiod in depot form used for treatment of opiate addiction
long lasting opiate in depot form for tx of opiate addiction
1-acetylmethadol
less effective than codein but it has less addictive potential as well
propoxyphene
Pentazocin
kappa agonist, mu antagonist

less respiratory distress than all others

but causes nightmares etc at high doses.

May precpitate withdrawl in morphine addicts
Less respiratory effects than morphine but causes dysphoric effects at high doses
pentazocin
Naloxone vs Naltrexone
Naloxone has no oral availability, naltrexone does with longer effects
dextromethorphan
antitussive with no opiod effects except at very high doses
drug of choice for ob analgesia
meperidine
insoluble opiate used with atropine for diarrhea
diphenoxylate
80x the potency of morphine
fentanyl
opiate of choice for cough
dextromethorphan
tx of autonomic symptoms during opiate withdrawl
clonidine
Which cause more biliary spasm

Codein, Morphine, Meperidine, Methadone
Morphine=Meth>Meperidine>Codein
Duration of action for meperidine vs morphine vs methadone
Methadone>Morphine>Meperidine
Respiratory depression of meperidine vs morphine vs methadone
All have same effect on respiratory depression

Mixed actors like pentazocine have less respiratory depression