Exam 1: Pharmacodynamics Flashcards

1
Q

The study of the effects of drugs and their mechanism of action in the body

A

Pharmacodynamics

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2
Q

Describes what the animal does to the dug

A

Pharmacokinetics

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3
Q

Describes that the drug does to the animal

A

Pharmacocynamics

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4
Q

What are the 3 effects that drugs have after administration

A
  1. Targets for drug action
  2. Drug-receptor interactions
  3. Quantification of drug response
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5
Q

T/F Physical interactions of drugs cause non specific effects

A

T

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6
Q

What are the two forms of biological interaction of drugs?

A
  1. Non receptors

2. Receptors

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7
Q

What are the 3 criteria of non receptor biological interactions

A
  1. Voltage gated ion channels
  2. Enzymes
  3. Carrier proteins
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8
Q

What are the 4 types of Receptors for biological interactions of drugs

A
  1. Ionotropic
  2. GPCR
  3. Kinase-coupled
  4. Nuclear receptors
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9
Q

WHat are 3 examples of Physical interaction of drugs?

A
  1. Osmotic diuretics
  2. Antacids that act by direct neutralization of acid in the GIT
  3. Radioactive Iodine
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10
Q

How do drugs Target ion channels in non receptor interactions?

A

Physically obstructing of ion channels and modulation of opening and closing channels

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11
Q

How do drugs effect enzymes in non receptor interactions?

A

compete for binding to enzymes

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12
Q

Small polar molecules cannot cross the memb. and thus require _____

A

carrier proteins

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13
Q

How do drugs effect carier proteins in non receptor interactions

A

Alter the proteins and remove molecules from their site of action ending their effects

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14
Q

Groups of 4-5 proteins embedded in the cell memb. forming a pore

A

Ligand gated ion channels

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15
Q

What is another term for Ligand gated ion channels

A

Ionotropic

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16
Q

What happens when a drug binds to an ionotropic channel?

A

prevents ions such as Ca and Na from passing through

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17
Q

Receptor that transduces an extracellular signal to an intracellular one

A

GPCR

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18
Q

What is another name for GCPR?

A

7TM or Metabotropic

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19
Q

Which type of receptor is used for fast neurotransmission?

A

Ligand gated ion channels (ionotropic)

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20
Q

Which type of receptor is used for slow secretory and smooth muscle functions

A

GCPR (metabotropic)

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21
Q

What are the 3 G alpha subunits of GPCRs?

A
  1. Gas
  2. Gai
  3. Gaq
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22
Q

WHich G subunit of GPCR is inhibitory

A

Gai

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23
Q

Which G subunit of GPCR is stimulatory

A

Gas

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24
Q

Which G subunit of GPCR is coupled to PLC

A

Gaq

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25
Describe the Gs protein receptor coupled pathway
Couples to adenylate cyclase causing and inc in cAMP, which phosphorylates cellular constituents
26
Describe the Gi protein receptor coupled pathway.
Couples negatively to adenylate cyclase causing an dec in cAMP which closes Ca and K channels
27
Describe the Gq protein receptor coupled pathway
Couples to phospholipase c-beta increasing IP3 which increases Ca release fro sER
28
What are the 2 adrenergic G protein pathways
1. Phosphatidylinositol signal pathway | 2. Cyclic AMP signal pathway
29
In the Phosphatidylinositol signal pathway, alpha 1 couples with ____, and alpha 2 couples with ____.
1. Gq | 2. Gi
30
What is the end result of the pphosphatidylinositol signal pathway?
Ca release from sER and protein kinase C activation
31
In the cAMP signal pathway beta receptors couple with ___
Gs
32
What is the end result of cAMP signal pathway
Activates Protein kinase A
33
What does the cAMP pathway regulate?
1. Cellular metabolism 2. Gene expression 3. Memb. permeability
34
Extracellular receptor that directly activates enzymes
Kinase linked receptors
35
What is the main function of kinase linked receptors?
Phosphorylation and activation of proteins which activates effectors
36
Transcription factor receptors located in the cytoplasm of the cells
Nuclear receptors
37
An inc in the number of receptors and the drug effect
receptor up regulation
38
A Dec. in the number of receptors and their effects
Receptor down regulation
39
T/F receptor down regulation is part of the normal cellular metabolism
T
40
Gradual dec. in responsiveness to a drug when given repeatedly over days to months
Tolerance
41
Acute tolerance developing over a short period of time, sometimes involves depletion of stored mediator
Tachyphylaxis
42
Anything that binds to a recognition site
Ligand
43
What are the 4 types of ligands
1. Agonist 2. Antagonist 3. Inverse agonist 4. Mixed agonist-antagonist
44
Mimics the effect of an endogenous ligand
Agonist
45
binds to receptor but does not cause as much effect as a full agonist, still blocks that receptor from full agonist binding
Partial agonist
46
Binds to the same receptor and prevents an agonist from, inhibits the effects of the receptor
antagonist
47
most common form of antagonism
competitive antagonism
48
T/F competitive antagonism is irreversible
F
49
Binds to the same receptor site and produces the opposite effect as agonist
Inverse agonist
50
Acts as an agonist on one type of receptor and as an antagonist on other types
Mixed agonist-antagonist
51
The conc. of a drug needed to produce the given effect
Potency
52
The maximal effect a drug can have
Efficacy
53
50% of maximal response in vitro
Effective concentration (EC50)
54
Desired effect in 50% of the population
Effective dose (ED50)
55
Dose that causes toxic effect or dose that caused death
Lethal dose (LD50)
56
A ratio used to evaluate the safety ofa drug
Therapeutic index (TI)
57
What does a narrow TI indicate?
the dose required to cause deathis close to the dose required to have a therapeutic effect
58
What does a Wide TI mean?
the dose required to cause death is much higher than the dose required to have a therapeutic effect
59
A more comprehensive and accurate assessment of drug safety
Standard safety margin
60
What is the calculation for standar safety margin
%ssm=LD-ED/ED
61
Ratio between the LD50/ED50
Therapeutic index
62
The larger the theraqeutic index the more _narrow/wide_ the safety of the drug
Wider
63
Time required after drug admin for a response to be observed
Onset off action
64
Length of time the drug has a quantiiable effect
Duration of action
65
Desirable effects of a drug, what we want clinically
Therapeutic effects
66
Unintended effects of a drug, secondary to the use of the drug. can be good or bad or nothing.
Side effects
67
Unintended and undesirable effects of a drug
Adverse effects