CPTP 3.20 - Opiods Flashcards
Name three functions opiotes have on the body?
- Change limbic system (Dopa projections) = control emotions and pleasure
- Block pain messages transmitted by the spinal cord
- Change the brainstem (pons and medulla) - areas that control the ANS
What three things happen with opiod receptor activation?
Inhibition of neuronal firing
Inhibition of neurotransmitter release
Dis-inhibition - removal of inhibitory influence (GABA) = excitation
Name four areas where opiods interact with opiod receptors to elicit therapeutic effects?
Limbic areas
Medulla
Periaquaductal grey
Dorsal horn of spinal cord
Name the three opiod receptors and state their activities?
Mu (μ) - analgesic effects in the brain
Kappa (κ) - analgesic effects in the spinal cord
Delta (δ) - Interact with endogenous enkephalins and mediate CNS effects
What two effects do all the opiod receptors have in common upon activation?
Anti-nocioception
Meiosis (contraction of pupils)
Name three classes of endogenous opiods?
Proopiomelanocortin = B-endorphin (Mu) Proenkephalin = Met-enkephalin and Lue-enkephalin (Delta) Prodynorphin = Dynorphin A and Dynorphin B - Kappa ONLY
Name four opiod (agonist) analgesics?
Morphine
Dimorphine (heroin)
Codiene
Tramadol
Describe how morphine works?
Mu and delta receptor AGONIST
Metabolism by glucoronidation
Describe how tramadol works?
Mu opiod receptor AGONIST
Also inhibits the re-uptake of 5HT and Nor epi
Describe how addiction occurs with opiod analgesics?
Reward = due to tolerance users increase the dosage to obtain the high - As more drug is taken the withdrawal state with dependency increases = Negative Re-inforcement
How does diamorphine work?
Activation of Mu opiod receptor on GABA inter neurone in the ventral tegmental area leading to the inhibition of GABA release = Increased Dopa in the nucleus accumbens