Pain treatments and opioids Flashcards
Anatagonist at all opioid receptors
Naloxone
Side effects of opioids
Euphoria (mu receptors) Respiratory depression Nausea and vomiting Constipation Tolerance and dependance
Mu action and agonist
Opens K channels
Morphine etc
Delta action and agonsit
Opens K
DPDPE
Kappa actions
Closes Ca channels
ORL-1 action
Opens K channels
Opioid GPCR coupled to
Gi
Inhibits adenylyl cyclase, less cAMP
Heroin
Diamorphine, converted to morhpine in brain, More rapidly uptaken
Morphine uses
Acute and chronic pain.
4 hrs half life
Methadone
used to treat withdrawal from opioids as has less euphoria associated
Fentanyl
Used for acute pain and anathsisia
High potency
Oxycodone
Major drug of abuse in US
Codeine
Used for mild pain.
Has low dependance as no euphoria
Can supress cough
Tramadol
Weak agonist
Used for acute pain
No respiratory depression
Loperamide
u agonist that cannot cross BBB, therefore is used to slow peristalsis in diarrhoea
Chronic pain definition
Pain that persists beyond wound healing, can be musculoskeletal or neuropathic, but also has psychosomatic symptoms
Chronic pain drugs
Tricyclic antidepressants
Gabapentin and pregabalin
Some epiletics
Tricylic antidepressants action
inhibit NA uptake
tricyclic examples
Amitriptyline
Nortriptyline
desipramine
What pain type can nACh agonist help with
Neuropathic
How do nACh agonists exert their effect
presynaptic nACh can modulate GABA to increase inhibition. Antagonists have the opposite effect