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HLSC 222- midterm 1 > pharmacodynamics > Flashcards

pharmacodynamics Flashcards

(51 cards)

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1
Q

Dose- response relationship

A

relationship between size of an administered dose and intensity of response produced

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2
Q

What does graded dose response mean

A

as dose increases, response becomes progressively larger

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3
Q

maximal efficacy

A

largest EFFECT drug can produce
- for the SAME doses, which drug has the LARGER EFFECT

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4
Q

How is maximal efficacy indicated on a dose response curve

A

the height of a curve

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5
Q

what is a problem with high efficacy when treating a patient?

A

it is hard to match the response intensity to patient needs

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6
Q

Relative Potency

A

AMOUNT of drug required to elicit an effect
- how much drug do we need to elicit the same effect

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7
Q

what are 3 points about potency

A

(1) rarely important drug characteristic
(2) Implies nothing about Maximal efficacy
(3) “this drug produces its effect at low doses”

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8
Q

Receptors

A

chemical sites in body that most drugs interact with to produce its effect

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9
Q

Equation for interaction between a drug and receptors

A

D + R <– –> D - R COMPLEX –> RESPONSE

D= drug
R= receptors

binding of a drug is reversible
receptor can only be on or off

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10
Q

what happens when a drug binds to a receptor?

A

mimic or block actions of endogenous regulatory molecules
- increase of decrease activity controlled by receptor

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11
Q

what do drugs do for the body

A

help the body help itself

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12
Q

what are the 4 primary receptor families

A

a) cell- membrane embedded receptor
b) ligand- gated ion channels
c) G protein- coupled receptor systems
d) transcription factors

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13
Q

Cell-membrane embedded receptors

A
  • spans cell membrane
  • ligand-domain located on cell surface
  • enzyme catalytic site located on inside of cell
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14
Q

what happens when a drug binds to cell-membrane embedded receptors?

how quickly does it respond

A

activates enzyme = increase activity

response occurs in seconds

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15
Q

what receptor does insulin use

A

cell-membrane embedded receptors

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16
Q

Ligand- Gated Ion Channel function

how fast does it happen

A

regulate ion flow in and out of cells
- specific to ion

milliseconds

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17
Q

what act through ligand-gated ion channels?

A

several neurotransmitters (acetylcholine and GABA)

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18
Q

G Protein -Coupled Receptor System components

A
  • receptor
  • G protein
  • effector
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19
Q

G Protein- Coupled Receptor System function

how fast

A

drug/endogenous ligand activates receptor which activated G Protein –> activates effector

rapid response

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20
Q

Transcription factors

A

situated on DNA in nucleus
- activated by lipid-soluble ligands

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21
Q

how do transcription factors differ from the other

Study These Flashcards
A

(1) receptors are within cell not on surface
(2) responses from activation are delayed –> because transcription of RNA

22
Q

How fast does transcription factors act

Study These Flashcards
A

hours or days

23
Q

Selectivity

Study These Flashcards
A

only elicit responses for which it is given

24
Q

why is there no such thing as wholly selective drugs

Study These Flashcards
A

all drugs cause side effects

25
what does it mean when a drug is more selective
fewer side effects because the drug reacts with fewer specific receptors for that drug.
26
what are there receptors for
(1) each neurotransmitter (2) each hormone (3) molecules that regulate physiological processes (histamine, prostaglandins, leukotrienes)
27
why is selective drug action possible
due to many types of receptors
28
if a drug only acts with one receptor and regulates one process
drug effect will be limited
29
if drugs interact with several receptors
drug will elicit a drug effect will be wide
30
can a drug selectively turn on single processes of a receptor?
no, if the receptor is activated ALL processes are activated. Ex) opioid receptors modulate pain, but also respiration and bowel motility - morphine for pain will also cause respiratory depression and constipation
31
does selectively guarantee safety
NO EX) botulinum toxin selective for one receptor but causes paralysis of respiratory muscles --> death
32
what are the theories of drug- related interaction
(1) Simple Occupancy Theory (2) Modified Occupancy Theory
33
Simple Occupancy Theory (SOT)
(1) intensity of drug response is proportional to number of receptors occupied by the drug (2) maximal response will occur when all available receptors are occupied
34
What does SOT assume
all receptors are identical with (1) ability to bind to receptor (2) ability to influence receptor function
35
What factors does Modified theory take into account?
Affinity and Intrinsic activity
36
Affinity is it reflected in efficacy or potency?
strength of attraction between drug and receptor potency - high affinity = effective at low doses = very potent
37
Intrinsic Activity is it reflected in efficacy or potency?
ability of a drug to ACTIVATE a receptor Efficacy -high intrinsic activity cause intense receptor activation = high efficacy - intensity of response is still related to number of receptors occupied
38
Antagonists
Drugs block action of endogenous molecules - prevents activation of the receptors by agonist
39
Agonists
Drugs mimic action of endogenous molecules - activate receptor (decreases or increases receptor activity depending on what the endogenous molecules does to the receptor)
40
does agonists have affinity or high intrinsic activity?
BOTH - binds and activates
41
Explain how antagonist response is determined
Determined by how much Agonist is present - if there is no agonist present, administering antagonist has no effect
42
Noncompetitive (insurmountable) Antagonists (NA
bind IRREVERSIBLY - reduce number of receptors available for agonists - reduces TOTAL number of receptors available for - if enough NA is present, agonist effect will be completely blocked
43
Competitive (Surmountable) Antagonists (CA)
REVERSIBLY binds - binding to endogenous molecules or CA is due to which is present in highest conc. - MAX response of agonist is not reduced --> increase amount of agonist required to produce a given intensity of response
44
Partial Agonists
- moderate intrinsic activity - Maximal effect of a partial agonist is lower than that of a full agonist
45
What can happen to a cell that is subject to continuous activation/ inhibition
(1) can change number of receptors on their surface (2) change sensitivity to agonist molecules
45
what happens when a receptor is continually exposed to an agonist
- will become less responsive (desensitized, refractory, or down-regulated) - destruction of receptors
46
What happens to receptors with continuous exposure to antagonist
cell will become more responsive (hypersensitivity, supersensitive, up-regulated) -synthesis of more receptors
47
what are examples of drugs that don't involve receptors?
Antacids: neutralize gastric acidity by chemical reaction stomach acid Antiseptics: precipitating bacterial proteins Saline laxatives: draws water into intestinal lumen via osmotic effect
48
What is ED50
Average Effective Dose The dose at middle frequency distribution standard dose
49
Therapeutic Index (TI)
measure of drugs safety ratio of drugs LD50 to ED50
50
LD50
the dose that is lethal to 50% of animals treated

HLSC 222- midterm 1 (10 decks)

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