Flashcards in Week 1 - General Principles, pharmacodynamics, drug receptors Deck (76)
mechanism of action of anesthesia
not precisely known, primary site- membrane receptors, NOT lipid bilayer
gamma aminobutyric acid
primary mechanism of action for injected and inhaled anesthetics
the processes by which a drug produces one or more measured physiologic responses
biosphere - protein receptor site
1- site of drug binding
2- regulator of pharmacologic response
four additional influences of pharmacologic responses
3- metabolism (biotransformation)
Abs distinctly metabolize excrement.
drug receptors are typically a __ that binds to a __ or endogenous substance
three receptor properties
1- sensitivity (how much drug to elicit effect)
2- selectivity (response to structurally similar drugs)
3- specificity (receptor response is always the same)
drug receptor subunits - 2 points
1- primary regulator of onset/offset response
2- individual genetic variation in receptor proteins may account for variations in response to different drugs among different populations
bonds between drugs and receptors from weakest to strongest
1- Van der Waals
"Vandy hides iconic co-valet parking spots and forces us take the shuttle"
four regulatory protein types
1- cell surface proteins
3- carrier proteins (transporters)
4- ion channels
"cell phones enzymatically carry ion channels"
three drug receptor protein locations
1- within luminal membranes
2- ion channel surfaces
"INSIDE the lumen membrane or ON the ion channel has the best cellular reception"
prototypical Mu receptor agonist first used 5,000 years ago in ancient Samaria
the most frequent receptor site for IV anesthetics, may play significant role in inhalation anesthetic activity (as inhalation agents bind to this receptor)
anesthetics bind to receptors at at least __ points causing a conformational change
anesthetics DO NOT bind by ___
covalent, otherwise your patient would never wake up
drugs also bind to ACCEPTORS like plasma proteins which... (2 points)
1- DO NOT elicit a pharmacologic response
2- reduce the amount of drug available to bind to RECEPTORS
describe a GABA receptor
5 peptide subunits arranged in a ring
"lady GAGA has a 5 carat diamond ring that she got for shooting the new Pepsi/Tide (peptide) commercial"
the two opioid receptors that McCarver emphasized
Mu and Kappa receptors
four types of opioid receptors
delta, kappa, mu, sigma
McCarver stated "sigma" as a receptor, but that has been disproven. It is actually "nociceptin". Contact me if you want the evidence.
two adrenergic receptors
two acetylcholine receptors
two OTHER types of receptors
conversion of one signal to a new signal, a sequence of biochemical reactions
anesthetic signal transduction
G protein coupled receptor (cell surface receptor) ->
cyclic AMP ->
cyclic GMP ->
protein kinases, phosphatases, intracellular actions
"Yo G! You're cyclic a/gmp has two aces!"
drug response equation
drug + receptor -> drug receptor complex -> tissue response
the drug receptor complex is a __ process
selective, only a few drugs may bind to a receptor type to create a response
three variables in tissue response
occupancy theory states that...
but what about population variability...
...the magnitude of a drug's response is proportional to the number of receptors occupied, the more drug = greater tissue response
...the tissue response to a drug can be disproportionate to the number of occupied receptors