Analgesics & Opioids (Laprairie Lecture) Flashcards
Agonist binding to Opioid Receptors reduces ____, inhibits inwardly rectifying K+ channels, & __________ the cell.
cGMP; hyperpolarizes
Examples of Endogenous Opioids?
Enkephalin
Dynorphin
Substance P
Endorphin
Which country is the number one producer of Opium plants?
Tasmania
Cleavage of a ______ functional group renders Codeine into Morphine.
methoxy
Phase I metabolism of Codeine, Hydrocodone, Oxycodone & Tramadol are all mediated by what CYP enzyme?
CYP2D6
Phase II conjugative reactions of Morphine, Hydromorphone & Oxymorphone are mediated by what enzyme?
UGT2B7
Aside from proposed CNS-selective COX inhibition, how else does Tylenol elicit pain relief?
1) Anandamide Reuptake Inhibitor (which serves to boost Endocannabinoid levels)
2) TRPV1 Agonist
What CYP enzymes metabolize Tylenol?
CYP2E1, CYP3A4
Phase I metabolism of NSAIDs is conducted by what CYP enzymes?
CYP2C9, CYP2D6
What distinguishes Endogenous Opioids from Exogenous Opioids?
Endogenous = Peptides
Opioids & Cannabinoids both do what same thing to limit pain perception?
Inhibit NT release from Pre-Synaptic Neuron
Of the following Opioid Receptors, which one DOES NOT induce respiratory depression when stimulated?
Mu
Kappa
Delta
Delta
Of the following Opioid Receptors, which one elicits euphoria when stimulated?
Delta
Mu
Kappa
Mu
T or F: There are currently no known Cannabinoid Receptor polymorphisms that affect drug efficacy.
True!
An increasing number of this BP triplet can predict the likelihood of one using Cannabis, as well as the severity of Huntington’s Disease if they were to acquire it.
AAT