pain and opioid pharmacology Flashcards
name a naturally occurring opioid
from the opium poppy ->
morphine
codeine (weaker)
name a synthesised opioid
fentanyl - made to have faster onset time
heroin aka. diamorphine
what is the antidote to opioids?
naloxone
what are routes of administration for opioids ?
oral - need x2 as IV (50% bioavaibabilty)
IM
IV -fastest, can use patient controlled analgesia (patient presses button for more from IV)
lollipops
what class drugs are opioids?
class A
how do opioids reduce pain ?
they use the existing pain modulation system
inhibit the release of pain transmitters at spinal cord and midbrain – and modulate pain perception in higher centers – euphoria – changes the emotional perception of pain
Block it with release of endorphins and enkephalins (pleasurable. euphoric hormones)
which pain pathway do opioids act on?
Descending inhibition of pain
are opioids designed for short term or long term pain relief?
designed for short term pain relief
Sustained activation leads to tolerance and addiction through Downregulation of receptors
how soon does opioid withdraw start?
within 24 hours
why are there some side effects of opioids, not to do with pain relief ?
Opioid receptors exist outside the pain system e.g. digestive tract, respiratory control centre
we tend to administer them systemically eg. IV therefore they affect the whole body
list examples of side effects of opioids
Respiratory depression
Sedation
Nausea and vomiting
Constipation
Itching
Immune suppression
Endocrine effects
how is respiratory depression caused by morphine?
Morphine is metabolized to morphine 6 glucuronide which is more potent than morphine and is renally excreted.
With normal renal function this is cleared quickly
In renal failure it will build up and may cause respiratory depression
advice for prescribing opioids
*Before prescribing opioids, discuss with the patient the risks and features of tolerance, dependence, and addiction - use short term courses
Agree a treatment strategy and plan for end of treatment
Warnings have been added to the drug labels and packaging of opioids to support patient awareness
At the end of treatment, taper dosage slowly to reduce the risk of withdrawal effects - may take weeks
why does different dosages of codeine affect people differently?
Codeine is a prodrug - it needs to be metabolised by cytochrome CYP2D6 into morphine to work
CYP2D6 activity varies in patients
should you prescribe codeine for non-cancerous pain?
explain why
no - it loses affect quickly (tolerance builds to pain relief) and is very addictive
what is the WHO pain ladder?
simplistic way to rate pain intensity .
There are 3 rungs to the ladder, corresponding to increasing pain intensity.
The clinician prescribes medications as pain worsens, moving from one rung to the next.
what are the 3 rungs to the pain ladder?
1) anti-inflammatory agents, for mild pain
2) weak opioids, for mild - moderate pain
3) strong opioids for moderate to severe pain
define pain
an unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage.