Exam review Flashcards
(53 cards)
MOR Specificity
endorphins>enkephalins>dynorphins
DOR specificity
enkephalins
KOR Specificity
dynorphins
key features: structure of opioid receptor
–extracellular and intracellular loops: ligand binding and signaling
-intracellular C terminus including phosphorylation sites
-extracellular N-terminus including glycosylation sites
Opioids ascending pathway
-block release of excitatory NTs by blocking Ca channels
-enhance K channels causing hyperpolarization
-as a result, opioid block the release glutamate and substance P
Opioids in descending pathway
-enhance pain relief by reducing the release of GABA
DOR Opioid receptor
-agonist can have analgesic effect
-serious side effects
KOR opioid receptos
-analgesia
psychotomimetic effects
Opioid Receptor Signaling
1)Agonist binds
2) G protein binds
3) Arrestin recruitment, signaling and internalization
4) recycling or degradation
oxycodone metabolism
-3A4 -noroxycodone
-2D6-oxymorphone
Methadone metabolism
-3A4, 2B6, 2D6
-excreted in urine and bile
Buprenorphine
-partial mu agonist, antagonist
Embeda
morphine + naltrexone
Talwin
Pentazocin+Naloxone
Targiniq
Oxycodone+Naloxone
Simple partial
preserved consciosness
complex partial
impaired consciusness
absence seizure
staring and cessation of ongoing activities
myoclonic seizure
breif shock like contraction
tonic clonic seizure
sustained contraction, relaxation
GABA-B
-metabotropic(G-protein coupled)
-produces slow and prolonged inhibitory signals
Na Channel AEDs
1) Phenytoin
2) Carbamazepine
3) Lamotrigrine
4) Lacosamide
5) Zonisamide
Na fast inactivation
phenytoin and carbamzepine
Na slow inactivation
lacosamide, lamotrigine, valproate, zonisamide