Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

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

Week 1 - General Principles, pharmacodynamics, drug receptors Flashcards

0
Q

GABA

A

gamma aminobutyric acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
1
Q

mechanism of action of anesthesia

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

primary mechanism of action for injected and inhaled anesthetics

A

GABA receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

pharmacology

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

biosphere - protein receptor site

2 functions

A

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

Bind, regulate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

four additional influences of pharmacologic responses

A

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

Abs distinctly metabolize excrement.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

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

A

protein

drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

three receptor properties

A

1- sensitivity (how much drug to elicit effect)
2- selectivity (response to structurally similar drugs)
3- specificity (receptor response is always the same)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

drug receptor subunits - 2 points

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

bonds between drugs and receptors from weakest to strongest

A 
1- Van der Waals
2- Hydrogen
3- Ionic
4- Covalent
"Vandy hides iconic co-valet parking spots and forces us take the shuttle"
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

four regulatory protein types

A 
1- cell surface proteins
2- enzymes
3- carrier proteins (transporters)
4- ion channels
"cell phones enzymatically carry ion channels"
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

three drug receptor protein locations

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

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

A

morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

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

A

GABA receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

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

A

three

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

anesthetics DO NOT bind by ___

A

covalent, otherwise your patient would never wake up

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

drugs also bind to ACCEPTORS like plasma proteins which… (2 points)

A

1- DO NOT elicit a pharmacologic response

2- reduce the amount of drug available to bind to RECEPTORS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

describe a GABA receptor

A

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”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

the two opioid receptors that McCarver emphasized

A

Mu and Kappa receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

four types of opioid receptors

A

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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

two adrenergic receptors

A

alpha, beta

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

two acetylcholine receptors

A

nicotinic, muscarinic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

two OTHER types of receptors

A

histamine, capsaicin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

signal transduction

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

anesthetic signal transduction

A

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!”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

drug response equation

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

the drug receptor complex is a __ process

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

three variables in tissue response

A

1- receptor
2- genetics
3- physiology

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

occupancy theory states that…

but what about population variability…

A

…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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

mean dose

A

average of the range of doses to produce a given response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

median dose

A

the dose on either side of which half of the drug responses occur

31
Q

mode dose

A

the dose representing the greatest percent of responses

32
Q

the mean, median, and mode doses are typically close to each other but …

A

are not the same

33
Q

two types of drug response curves

A

1- graded dose response

2- quantal dose response

34
Q

graded drug response

A

change in response as dose in increased, has a hyperbolic shape

Similar to how your “grade” will change as your “dose” of studying increases

35
Q

quantal drug response

A

provides information on the FREQUENCY which a drug produces a therapeutic response, all or nothing, helps determine ED, TD, LD using dose response curves

36
Q

toxic dose

A

TD50

37
Q

lethal dose

A

LD50

38
Q

therapeutic index

A

LD50/ED50

39
Q

safety margin

A

(LD1 - ED99) / (ED99 x 100)
(the lethal dose for 1% minus the effective dose for 99%) divided by (the effective dose for 99% times 100)
-the greater the therapeutic margin = safer drug

40
Q

therapeutic index

A

the median therapeutic safety margin for a specific effect
LD50 / ED50
volatile inhalation agents have a narrow therapeutic effect
iso at 1.5% end tidal provides anesthesia, 4% causes circulatory collapse

41
Q

median effective dose

A

ED50, the dose where 50% of patients respond as desired, helps to compare drug potency within a drug class

42
Q

when the drug + the receptor combine and form a drug/receptor complex it causes a…

A

fractional tissue response

43
Q

fractional tissue response

A

the desired drug effect, occurs when enough receptors are activated by a drug

44
Q

intrinsic activity

A

the DEGREE of drug/receptor interaction for a given drug and receptor population

Think of Degree antiperspirant, it has “intrinsic activity” that varies for all of its different formulas and for different people.

45
Q

two variables to describe intrinsic activity

A

1- affinity

2- efficacy

46
Q

affinity

A

1- potency
2- used to differentiate between different agonists that activate the same receptor
3- the agonist (drug) that produces a maximal response at the lowest concentration has the greatest affinity or “potency”

47
Q

efficacy

A
  • the ability to produce a desired response by stimulation of a specific receptor
  • the maximum effect that a drug may produce
48
Q

four factors of fractional tissue response time

A

1- delay in delivery of drug to receptors effected by pharmacokinetics or drug elimination
2- time for conformational change of drug receptor
3- receptor up regulation (increased sensitivity to a drug)
4- receptor down regulation (decreased sensitivity to a drug)

49
Q

agonist

A
  • any substance that binds to a specific receptor and triggers a response
  • mimics the action of an endogenous ligand that binds to the same receptor
  • in sufficient concentrations may elicit maximal receptor activation
50
Q

ligand

A
  • molecules that bind to receptors and form a complex to produce a biological response
  • can be endogenous chemicals or exogenously administered
  • example: endogenous insulin vs. lantus
51
Q

pure antagonist

A
  • structurally similar to agonists but bind to the receptor without causing a conformational change and have no efficacy
  • BUT, by occupying the receptor they MAY block an endogenous chemical and produce a physiological response (ie. beta BLOCKERS)
52
Q

competitive antagonists

A
  • possess weak affinity (atropine, esmolol)

- may be displaced by an agonist

53
Q

antagonists have __ affinity for receptors than agonists

A

higher

54
Q

NONcompetitive antagonists

A
  • STRONG affinity for receptors
  • form STRONG covalent bonds
  • NOT displaced by agonists (it was NO competition for the NONcompetitive antagonist to win over the agonist)
  • ex. ASA, phenoxybenzamine
55
Q

partial agonists

A

-activates receptor but cannot produce maximal response (it only PARTIALLY produces a response), thus it has lower efficacy than a full agonist

56
Q

partial agonists may __ block the effect of full agonists

A

partially

57
Q

partial agonists have __ efficacy than full agonists

A

lower

58
Q

inverse agonist

A

drug or endogenous chemical that binds to a receptor and produces the OPPOSITE action of an agonist

59
Q

inverse agonists bind preferentially to __ receptors

A

inactivated

60
Q

for an inverse agonist to work, the receptor must have some base level activity in the __ of any ligand

A

absence

61
Q

an inverse agonist __ the activity __ the basal level

A

decreases, below

62
Q

the efficacy of a full agonist is __

A

100%

63
Q

an inverse agonist has less than __% efficacy

A

0

64
Q

examples of inverse agonists

A

cimetidine, ranitidine, haldol, prazosin, timolol, clozapine, yohimbe

65
Q

physiologic antagonism involves __ agonists binding to __ receptors to create opposing responses and cancel each others effects

A

two, different

example- beta blocker and levophed

66
Q

chemical antagonism is when a drug’s action is __ but no receptor is involved
example__

A

blocked

heparin/protamine, sugammadex/roc

67
Q

receptors are controlled by __ and __ mechanisms

A

regulatory, homeostatic

68
Q

four factors that influence receptor regulation and adaptation

A 
1- synthesis and degradation
2- covalent modification
3- association with regulatory proteins
4- relocation in the cell
"new and old (synthesis and degradation) friends make the strongest bonds (covalent) during the "teens rule" years (regulatory proteins) even after we moved to a new neighborhood (relocation)
69
Q

receptor DOWN regulation is when the __ stimulation of cells by agonists results in __ and is commonly called __

A

continuous, DEsensitization, tolerance

70
Q

receptor UP regulation is when continuous __ administration results in increased number and __ of receptors. Tolerance to __ requires __ doses to counteract the increased number of receptors

A

ANTAgonist, sensitivity, ANTAgonist, larger

71
Q

tolerance is when an __ concentration of drug is required to produce a response and usually results from __ exposure to an agonist

A

increased, chronic

72
Q

five causes of tolerance

A 
1- up and down regulation
2- enzyme induction
3- depleted neurotransmitters
4- protein conformational changes
5- changes in gene expression

“Tolerance is when my up and down enzymes deplete the conforming genes”

73
Q

tachyphylaxis is the __ __ __ __ due to acute drug exposure

A

rapid development of tolerance

74
Q

the “spare receptor concept” states that a __ response can be produced by the activation of only a __ of receptors

A

maximal, fraction

75
Q

THAT’S __ FOLKS

A

ALL

ANPH 500 - Pharmacology - McCarver (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions