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
Q

Describe the Gs protein receptor coupled pathway

A

Couples to adenylate cyclase causing and inc in cAMP, which phosphorylates cellular constituents

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26
Q

Describe the Gi protein receptor coupled pathway.

A

Couples negatively to adenylate cyclase causing an dec in cAMP which closes Ca and K channels

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27
Q

Describe the Gq protein receptor coupled pathway

A

Couples to phospholipase c-beta increasing IP3 which increases Ca release fro sER

28
Q

What are the 2 adrenergic G protein pathways

A
  1. Phosphatidylinositol signal pathway

2. Cyclic AMP signal pathway

29
Q

In the Phosphatidylinositol signal pathway, alpha 1 couples with ____, and alpha 2 couples with ____.

A
  1. Gq

2. Gi

30
Q

What is the end result of the pphosphatidylinositol signal pathway?

A

Ca release from sER and protein kinase C activation

31
Q

In the cAMP signal pathway beta receptors couple with ___

A

Gs

32
Q

What is the end result of cAMP signal pathway

A

Activates Protein kinase A

33
Q

What does the cAMP pathway regulate?

A
  1. Cellular metabolism
  2. Gene expression
  3. Memb. permeability
34
Q

Extracellular receptor that directly activates enzymes

A

Kinase linked receptors

35
Q

What is the main function of kinase linked receptors?

A

Phosphorylation and activation of proteins which activates effectors

36
Q

Transcription factor receptors located in the cytoplasm of the cells

A

Nuclear receptors

37
Q

An inc in the number of receptors and the drug effect

A

receptor up regulation

38
Q

A Dec. in the number of receptors and their effects

A

Receptor down regulation

39
Q

T/F receptor down regulation is part of the normal cellular metabolism

A

T

40
Q

Gradual dec. in responsiveness to a drug when given repeatedly over days to months

A

Tolerance

41
Q

Acute tolerance developing over a short period of time, sometimes involves depletion of stored mediator

A

Tachyphylaxis

42
Q

Anything that binds to a recognition site

A

Ligand

43
Q

What are the 4 types of ligands

A
  1. Agonist
  2. Antagonist
  3. Inverse agonist
  4. Mixed agonist-antagonist
44
Q

Mimics the effect of an endogenous ligand

A

Agonist

45
Q

binds to receptor but does not cause as much effect as a full agonist, still blocks that receptor from full agonist binding

A

Partial agonist

46
Q

Binds to the same receptor and prevents an agonist from, inhibits the effects of the receptor

A

antagonist

47
Q

most common form of antagonism

A

competitive antagonism

48
Q

T/F competitive antagonism is irreversible

A

F

49
Q

Binds to the same receptor site and produces the opposite effect as agonist

A

Inverse agonist

50
Q

Acts as an agonist on one type of receptor and as an antagonist on other types

A

Mixed agonist-antagonist

51
Q

The conc. of a drug needed to produce the given effect

A

Potency

52
Q

The maximal effect a drug can have

A

Efficacy

53
Q

50% of maximal response in vitro

A

Effective concentration (EC50)

54
Q

Desired effect in 50% of the population

A

Effective dose (ED50)

55
Q

Dose that causes toxic effect or dose that caused death

A

Lethal dose (LD50)

56
Q

A ratio used to evaluate the safety ofa drug

A

Therapeutic index (TI)

57
Q

What does a narrow TI indicate?

A

the dose required to cause deathis close to the dose required to have a therapeutic effect

58
Q

What does a Wide TI mean?

A

the dose required to cause death is much higher than the dose required to have a therapeutic effect

59
Q

A more comprehensive and accurate assessment of drug safety

A

Standard safety margin

60
Q

What is the calculation for standar safety margin

A

%ssm=LD-ED/ED

61
Q

Ratio between the LD50/ED50

A

Therapeutic index

62
Q

The larger the theraqeutic index the more narrow/wide the safety of the drug

A

Wider

63
Q

Time required after drug admin for a response to be observed

A

Onset off action

64
Q

Length of time the drug has a quantiiable effect

A

Duration of action

65
Q

Desirable effects of a drug, what we want clinically

A

Therapeutic effects

66
Q

Unintended effects of a drug, secondary to the use of the drug. can be good or bad or nothing.

A

Side effects

67
Q

Unintended and undesirable effects of a drug

A

Adverse effects