Term
| useful analgesias in opiate resistant pain states = |
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Definition
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Term
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Definition
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Term
| opioid Rs are what type of Rs? |
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Definition
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Term
| disadvantages of Mew agonists = |
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Definition
resp depression
constipation
euphoria = drug of abuse |
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Term
| disadvantages of kapa agonists = |
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Definition
diuresis with chronic use
dysphoria (state of unease)
hallucinations
but no resp effects!! :) |
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Term
| delta agonists used as... |
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Definition
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Term
| disadvantage of delta R agonists = |
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Definition
| pronconvulsant (so not in clinical use!) |
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Term
| disadvantages of ORL1 agonists = |
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Definition
impairs learning
impairs locomotion
NO ORL1 targetting drugs yet |
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Term
| advantage of ORL1 agonists = |
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Definition
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Term
| the best opioid drugs target what R? |
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Definition
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Term
| what is imp for morphines activity? |
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Definition
| benzene ring with hydroxyl group |
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Term
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Definition
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Term
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Definition
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Term
| morphine has how many rings in its structure? |
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Definition
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Term
| name an endogenous opioid/endorphin? |
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Definition
| tyrosine (has benzene ring with hydroxyl group like morphine) |
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Term
| activate Gprotein coupled opioid Rs = |
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Definition
| activate Gi/Go = open K+channel, close Ca2+ channel and inhibit AC |
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Term
| opioid Rs all have same GPCR pathway (activating Gi/Go), so how can opioids have diff effects? |
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Definition
| diff opioids effect diff Rs in diff parts of the brain |
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Term
| functional consequences of activating opioid Rs = |
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Definition
1. inhibit neuronal firing (due to incr K+ out of cell)
2. inhibit neurotransmitter release (due to inhibition of Ca2+ entry into cell)
3. Disinhibition - if opioid R inhibits something inhibitory then get excitation (due to removal of inhibitory influence) |
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Term
| opioid Rs actions are always... |
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Definition
| ...inhibitory (but if inhibit an inhibitory influence of something else = excitatory effect!) |
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Term
| desirable effects of opioids = |
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Definition
1. analgesia
2. contipation (to tx severe diarrhoea - but now got better drugs)
3. sedation (gd if tx acute pain)
4. cough supression (nowadays got better drugs to tx this than opioids) |
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Term
| Undesirable effects of opioids = |
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Definition
1. resp depression (less if patient in pain)
2. constipation (with long term tx)
3. nausea & vom (often on 1st admin and then goes away but sometimes get patient that never stops!!)
4. sedation/excitation (not gd for long term pain relief)
5. tolearnce
6. incr. in intracranial press
7. psychological dependance
8. physical dependance
9. euphoria |
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Term
| opoids cause sedation in what sp? |
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Definition
man
dog
monkey
rat
rabbits
birds |
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Term
| opioids cause excitation in what sp? |
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Definition
cats
horses
pigs
cattle
sheep
goats |
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Term
| other effects of opioids = |
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Definition
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Term
| therapeutic uses of opioids = |
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Definition
1. relief of pain
2. tx severe diarrhoea
3. cough supression |
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Term
| inhibitory effect of opioids = |
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Definition
effect s.c. =
pre and post synaptic actions to decr flow of sensory info |
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Term
| excitatory effect of opioids = |
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Definition
suprapinal sites (eg periaquaductal grey matter) =
activate descending pathways to inhibit the s.c. |
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Term
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Definition
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Term
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Definition
dextropropoxyphene
codeine |
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Term
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Definition
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Term
| the gold standard opioid = |
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Definition
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Term
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Definition
| oral slow release tablets - release over 8hrs |
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Term
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Definition
| ...oral bioavailability unlike morphine (probs be moved into vetmed) |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
| other effects of methodone = |
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Definition
| sedative and depressing effects |
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Term
| problems with pethidine = |
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Definition
| short acting, and can supress babys resp in labous so DONT use as pain relief during labour |
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Term
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Definition
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Term
| name an opioid gd for LA's |
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Definition
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Term
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Definition
| potent - easy to overdose, only need small dose (=why gd for LA's) |
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Term
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Definition
| if use have to have someone with you with the antagonist as dangerous if inject yourself |
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Term
|
Definition
| naloxone or Diprenorphine |
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Term
| remifentanyls half life = |
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Definition
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Term
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Definition
| infusion because its so short lasting |
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Term
| buprenorphines effect on mew and kapa Rs = |
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Definition
mew partial agonist (so less resp effects)
kapa antagonist |
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Term
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Definition
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Term
| Naloxone isnt v gd at antagonising morphine, why? |
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Definition
| naloxone is short acting an morphine is long acting |
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Term
| diprenorphine antagonist is potent but its a ... |
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Definition
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Term
| morphine is metabolised by... |
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Definition
| ...glucuronidation in the liver to morphine-3-glucuronide and morphine-6-glucuronide |
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Term
| active morphine metabolite (still got 'OH' group) = |
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Definition
morphine-6-glucuronide
(this is reabsorbed in gut and prolongs morphines action) |
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Term
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Definition
| goes into brain v rapidly and is metabolised to get a hydroxyl group = becomes active and can bind to opioid Rs |
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Term
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Definition
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Term
neuroleptanalgesia:
a) LA Immobilin =
b) SA Immobilin =
c) Hypnorm = |
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Definition
a) ectorphine + ACP
b) ectorphine + methotrimeprazine
c) fentanyl + fluanizone |
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Term
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Definition
| NSAIDs and opioids = give together = incr analgesia and decr side effects of both drugs :) |
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