Opioids Flashcards
Where can we find opioids
Opium poppy seed
Codeine (Cough Syrup)
Oxytocin
Pentanol
What is a neurotransmitter that blocks opioid receptors
Naloxone (antagonist) of heroin. Found in narcan ( medication given to people who OD on heroin). Mu receptor antagonist
Buprenorphine- Kappa receptor antagonist
Methadone - partial Kappa agonist
Opioid receptors in brain
Mu
Kappa
Delta
What do endogenous opioids do
A) Open K+ channels presynaptically ( opioid binding to NT ends up in G modulation of receptor opening up K+ resulting in hyperpolarization, decreasing firing)
B) Axonic signaling closes Ca2+ channels( Binding to receptor leads to G modulation closing the Ca2+ channels, this reduces firing of the NT)
C) presynaptic autoreceptors reduce transmitter release ( Endorphin autoreceptor decrease release of cells NT, neuron with NT + opioid bind to NT reducing the post synaptic effect of the drug)
Pain
Early Pain -> first sharp initial pain (ex. burning) carried out by myelinated A delta fibers
Late pain -> symptoms from early plain + plus prolonged pain (burning + throbbing of finger) carried out by unmyelinated C fibers
-Opioid neurons reduce pain by inhibiting pain neurons in spinal cord
PAG (Opioids + Reward)
-Opioid neurons (inhibitory) bind to GABA neurons (inhibitory) which are either binded to NE neurons in the Locus Correlus (LC) or Serotonin neurons in the (Raphe Nuclei) -> opioids inhibit the inhibition of GABA -> serotonin and NE can then go on to inhibit spinal cord pain receptors
What does Morphine do
Morrphine is a Mu angonist. Increases the amount of dopamine in the system
Dopamine reward pathway
VTA -> Nucleus Accumbens -> Ventral Pallidum
GABA -> Mu-> DA/ Kappa -> dopamine release in Ventral Pallidum
Tail of VTA
is Gabaergic and is rich of opioid receptors
Desensitization causes
Tolerance
cAmp in morphine treatment
- opioid receptor activation reduces cAMP
-withdrawl overproduces cAMP
-cAMP is important for addiction because it activates the CREB protein which leads to stronger synapses which changes the gene expression in the brain (Which forms addiction)