Opioid_Flashcards (1)
What are opioids used to treat?
Moderate to severe pain
What type of receptors are opioid receptors?
Inhibitory GPCR
What is the MOA of opioids?
Activate Gαi → inhibit cells via hyperpolarization, cAMP, inhibit Ca+2 and Na+, activate K+ channels
Who discovered opioid receptors and in what year?
Pert and Snyder, 1973
What is naloxone’s mechanism of action?
Opioid antagonist; blocks opioid effects by binding to receptors
Which endogenous compound binds Mu receptors?
Endorphins
What are the effects of Mu receptor activation?
Analgesia, euphoria, respiratory depression
Which endogenous compound binds Kappa receptors?
Dynorphins
What are the effects of Kappa receptor activation?
Sedation, dysphoria, analgesia, may cause psychosis
Which endogenous compound binds Delta receptors?
Enkephalins
What side effect is associated with Delta receptor agonists?
Seizures
Name two natural opioids.
Morphine, Codeine, Thebaine
Name a semisynthetic opioid.
Heroin
Name two synthetic opioids.
Meperidine, Methadone, Fentanyl, Pentazocine
What is the main indication for morphine?
Analgesia for nociceptive pain