opioids Flashcards
opioids mechanism of aciton
opioids bind to G-protein coupled receptors, causing closing of voltage gated Ca2+ channels on presynaptic nerve terminals to decrease neurotransmitter release and opening of K+ channels which hyperpolarise neurons, reducing neuronal excitability
types of opioid receptors
μ, δ, κ (miu, delta, kappa)
Neuropathic pain (pain from diseases or damage directly to sensory neurons) require ___ doses than nociceptive pain (pain from physical/chemical agents)
higher
elderly require ___ dose to achieve pain relief than younger patients
lower
failure to get partial analgesia with incremental dosing in a patient taking opioids for the first time may indicate that…
pain syndrome is unresponsive to opioid therapy
people with chronic pain may not feel analgesic effects until…
a threshold is reached
types of opioid agonists (the drugs)
morphine, pethidine, fentanyl, methadone, codeine, tramadol
which are the weak opioid agonists
codeine (weak μ and δ agonist)
tramadol (weak μ agonist)
which drug is used as epidural
pethidine
adverse effects of pethidine
dry mouth, blurring of vision
which is a long acting opioid
methadone
which opioids are strong agonists with high maximum analgesic efficacy?
morphine, pethidine, methadone, fentanyl
which opioid is used as an anaesthetic adjuvant? why?
fentanyl as it is short acting
general adverse effects of opioids
- nausea/vomiting, drowsiness, constipation (common)
- miosis (a diagnostic feature of opioid overdose)
- urinary retention
- postural hypotension
- bradycardia
- immunosuppressant effect (long term use)
- respiratory depression (at lethal doses)
adverse effect of morphine
cause histamine release from mast cells leading to urticaria and itching, bronchoconstriction and hypotension due to vasodilation
which group of people do we use morphine with caution in
asthmatics
which receptor is most responsible for both therapeutic and adverse effects?
μ (miu)
therapeutic effects refer to analgesia on the supraspinal, spinal and peripheral level
which receptor is most responsible for dysphoria?
κ (kappa)
what is the effect after prolonged use of opioids?
development of tolerance i.e. less effective after prolonged and frequent use; need a larger dose to achieve same level of analgesia
types of opioid antagonists
naloxone, naltrexone, nalmefene
function of opioid antagonists
treat opioid overdose
which opioid antagonists are short and long acting respectively?
naloxone - short
nalmefene, naltrexone - long
why do we use opioid antagonists with extreme caution
they can precipitate a potentially fatal withdrawal syndrome if too much is given