Week 1 - General Principles, pharmacodynamics, drug receptors Flashcards Preview

ANPH 500 - Pharmacology - McCarver > Week 1 - General Principles, pharmacodynamics, drug receptors > Flashcards

Flashcards in Week 1 - General Principles, pharmacodynamics, drug receptors Deck (76)
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mechanism of action of anesthesia

not precisely known, primary site- membrane receptors, NOT lipid bilayer

1

GABA

gamma aminobutyric acid

2

primary mechanism of action for injected and inhaled anesthetics

GABA receptors

3

pharmacology

the processes by which a drug produces one or more measured physiologic responses

4

biosphere - protein receptor site
2 functions

1- site of drug binding
2- regulator of pharmacologic response

Bind, regulate

5

four additional influences of pharmacologic responses

1- absorption
2- distribution
3- metabolism (biotransformation)
4- excretion

Abs distinctly metabolize excrement.

6

drug receptors are typically a __ that binds to a __ or endogenous substance

protein
drug

7

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)

8

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

9

bonds between drugs and receptors from weakest to strongest

1- Van der Waals
2- Hydrogen
3- Ionic
4- Covalent
"Vandy hides iconic co-valet parking spots and forces us take the shuttle"

10

four regulatory protein types

1- cell surface proteins
2- enzymes
3- carrier proteins (transporters)
4- ion channels
"cell phones enzymatically carry ion channels"

11

three drug receptor protein locations

1- within luminal membranes
2- ion channel surfaces
3- intracellular
"INSIDE the lumen membrane or ON the ion channel has the best cellular reception"

12

prototypical Mu receptor agonist first used 5,000 years ago in ancient Samaria

morphine

13

the most frequent receptor site for IV anesthetics, may play significant role in inhalation anesthetic activity (as inhalation agents bind to this receptor)

GABA receptor

14

anesthetics bind to receptors at at least __ points causing a conformational change

three

15

anesthetics DO NOT bind by ___

covalent, otherwise your patient would never wake up

16

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

17

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"

18

the two opioid receptors that McCarver emphasized

Mu and Kappa receptors

19

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.

20

two adrenergic receptors

alpha, beta

21

two acetylcholine receptors

nicotinic, muscarinic

22

two OTHER types of receptors

histamine, capsaicin

23

signal transduction

conversion of one signal to a new signal, a sequence of biochemical reactions

24

anesthetic signal transduction

drug ->
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!"

25

drug response equation

drug + receptor -> drug receptor complex -> tissue response

26

the drug receptor complex is a __ process

selective, only a few drugs may bind to a receptor type to create a response

27

three variables in tissue response

1- receptor
2- genetics
3- physiology

28

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

29

mean dose

average of the range of doses to produce a given response