Pain Therapeutics Flashcards
TPRV1 is a
transient potential receptor subunit - an ion channel pore involved in detecting pain
TPRV1 is activated by
H+ in intersitial fluid
cpsaicin
temperature
In response to acute injury, cells lyse and release
Acid H+, ATP
Induction of COX2 leads to
prostaglandin synthesis
Mediators released in response to trauma include
bradykinin serotonin histamine prostaglandins cytokines
When nociceptors are activated, axons reflexively release
substance P, CGRP
Nociceptor sensitization refers to what in terms of threshold?
reduction
Generally, aspirins and NSAIDs target _______ to _________
COX2 to reduce prostaglandins
The primary transmission of pain at the level of the spinal cord is reliant on
Glutamine and inhibitory filtering responses mediated by glycine and GABAnergic receptors
When a pain neuron comes into the SC __________ is released
Glutamate
Glutamate acts primarily on
AMPA and NMDA receptors
NMDA receptors have _________ threshold and are activated in _____________
high threshold; prolonged pain/stimulus
Activation of the NMDA receptor leads to
displacement of Mg2+ plug, causing the cell to re-model, causing 2’ SC sensitixation
Activation of NMDA receptors and 2’ SC sensitization is responsible for resistance to what class of drugs?
Opiods
Ketamine acts at the __________ channel
NMDA