Centrally acting Analgesics Flashcards
Name Morphine Analogues.
Morphine, Heroin, Codeine.
Heroin.
Diamorphine.
Synthetic Derivatives of Morphine?
Methadone, Fentanyl, Pethidine, Pentazocine.
Stuff that act like opoids in the body?
Endorphins, Enkephanlins and Dynorphins.
Types of receptors affected by opoids?
Mu, Delta and Kappa.
How does morphine work?
Two components in action
Spinal - Inhibits dorsal horn pain transmission.
Supraspinal - Sends inhibitory impulses through descending pathways.
Inhibit release of excitatory transmitters from primary afferents.
What happens when a opoid receptor is activated?
Inhibition of Nuerotransmitter release.
Presynaptic - Inactivation of Ca2+ ion channels.
Post synaptic - Increased Potassium conductance (hyperpolarization).
Activation of descending gaba neurones.
Mu receptors.
Gets you high, addicted, sedated and can kill you (respiratory depression).
Kappa receptors
Modest analgesia with no addiction. Feel like shit and sedated.
Delta receptors.
Very small analgesic effect.
Pure Agonists at Mu and Kappa?
Morphine, Methadone, Fentanyl, Codeine.
Pure Antagonist?
Naloxone.
A mixed Agonist-Antagonist?
Buprenorphine.
Partial Agonist?
Pentazocine, Nalbuphine.
Effects of Opoids.
Analgesia, Sedation, Euphoria, Respiratory and Cough depression, Tranquility.
Nausea, Constipation, Low blood pressure, Urticaria and bronchoconstriction - release of histamines.