Pharmacology of analgesics Flashcards
What is the action of NSAIDs?
act at the site of injury
block the synthesis of prostaglandins - which decreases sensitivity of nociceptors
What is the action of local anaesthetics?
supress nerve conduction by blocking/inactivating voltage activated sodium channels
What is the action of opioids?
supress the synaptic transmission of nociceptive signals in the dorsal horn of the spinal cord
What is the action of gabapentin and pregabalin?
target ion channels that are upregulated in nerve damage
What is rung 3 of the WHO analgesic ladder?
strong opioids - morphine (gold standard), oxycodone, heroin, fentanyl, hydromorphone
What is rung 2 of the WHO analgesic ladder?
weak opioids - codeine, tramadol, dextropropoxyphene
What is rung 1 of the WHO analgesic ladder?
NSAIDs or Paracetemol
What are the possible combinations of the WHO analgesic ladder?
3 + 1
2 + 1
NOT 3 + 2 AS THEY ACT ON THE SAME RECEPTORS
What is supraspinal anticociception?
efferent regulation of pain - decending pathway from the brainstem
What are the important regions of the brain that are involved in pain perception and emotion and project to specific brainstem nuclei?
the periaqueductal gray - PAG
locus cereleus - LC
nucleus raphe Magnus - NRM
Where is the PAG found?
midbrain
Where is the LC found?
pons
Where is the NRM found?
medulla
What is the process of supraspinal antinociception?
PAG is excited by electrical stimulation or opioids
activated PAG neurones project into the NRM cause release of 5-HT and enkephalins
The serogenrgic and enkephalinergic neurones projecting into the dorsal horn excite the LC which releases Na
all of these substances inhibit nociceptive transmission in the dorsal horn of the spinal cord
What are enkephalins?
endogenous opioid - occurs naturally