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Pharmacodynamics > Kwon Exam 2 > Flashcards

Kwon Exam 2 Flashcards

1
Q

After administration, a drug must be _____ and _____ to its site of action.

A

absorbed; distributed

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2
Q

What part of ‘ADME’ represents systemic circulation?

A

absorption

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3
Q

What part of ‘ADME’ represents equilibration?

A

distribution

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4
Q

Which route of drug administration is the most complex?

A

oral administration

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5
Q

What part of ‘ADME’ does the drug go from the gut into the blood stream?

A

absorption

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6
Q

Drugs may be _____ to inactive (sometimes active) products to aid elimination from the body.

A

metabolized

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7
Q

The drug and its metabolites must be _____ from the body after it has brought about its effects.

A

excreted

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8
Q

What is the difference between heparin and warfarin?

A
  • heparin stays in plasma (central compartment)
  • warfarin is 99% albumin bound
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9
Q

What is the passage of a drug through cell layers into the general circulation?

A

absorption

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10
Q

What is the passage of a drug from the blood through the capillary tubes into extracellular fluid, cells, and tissues?

A

distribution

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11
Q

What is the passage of drugs into hepatic tissues (site of biotransformation)?

A

metabolism

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12
Q

What is the passage of a drug through nephron units in kidney for removal from the body?

A

excretion

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13
Q

What does the drug passage through cell membranes depend on? (hint: 4 things)

A
  • molecular size/shape
  • degree of ionization
  • relative lipid solubility (of ionized + nonionized forms)
  • binding to serum and tissue properties
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14
Q

What determines the kinetic properties of a drug?

A

polarity (water solubility)

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15
Q

What measures the relative affinity of an agent for a polar aqueous medium versus a non polar, oil-like medium? (hint: water soluble versus lipid soluble)

A

partition coefficient

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16
Q

Membranes are lipids and drugs must cross several membrane (lipid) barriers in order to reach their site of action. What is this called?

A

lipid solubility

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17
Q

Why don’t large molecules readily cross membranes?

A

because of their molecular weight

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18
Q

T/F uncharged drugs readily crosses membranes, charged molecules do not.

A

TRUE

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19
Q

The more charged a drug molecule, the more water soluble and the less lipid soluble it is. What is this called?

A

ionization

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20
Q

Many drugs are ____ acids or ____ bases and their charge at any given moment depends on the pH of the medium they are in.

A

weak acids; weak bases

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21
Q

Absorption rate and efficiency is dependent on what?

A

route of administration

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22
Q

Which type of diffusion shows low structural specificity?

A

aqueous (passive) diffusion

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23
Q

Which type of diffusion requires specific carrier proteins and can be inhibited?

A

facilitated diffusion

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24
Q

What are the 4 primary mechanisms for the passage of a drug through cell membranes?

A
  1. aqueous (passive) diffusion
  2. facilitated diffusion
  3. active transport
  4. endocytosis and exocytosis
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25
Q

Which primary mechanism for the passage of drug absorption through cell membranes is spontaneous and bidirectional and cannot be inhibited?

A

aqueous (passive) diffusion

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26
Q

Which primary mechanism for the passage of drug absorption through cell membranes can be saturated and is driven by a concentration gradient (high to low)?

A

facilitated diffusion

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27
Q

Which primary mechanism for the passage of drug absorption through cell membranes can be saturated and is energy dependent requiring ATP that can be inhibited?

A

active transport

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28
Q

Which primary mechanism for the passage of drug absorption through cell membranes is an energy dependent, saturable process? (hint: carries drugs of exceptionally large size >1000)

A

endocytosis and exocytosis

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29
Q

Lizness (linaclotide) is indicated in adults for the treatment of what?

A

irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC)

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30
Q

Drugs must be absorbed from the site of administration unless _____ ______.

A

injected intravenously

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31
Q

Which two routes of administration take effect in 30-60 seconds? (hint: fastest)

A
  • intravenous (#1)
  • intraosseous (#2)
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32
Q

Which two routes of administration take effect in 2-3 minutes? (hint: second fastest)

A
  • endotracheal (#3)
  • inhalation (#4)
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33
Q

Which is the only route of administration that takes effect in 3-5 minutes?

A

sublingual (#5)

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34
Q

Which two routes of administration take effect between 10-30 minutes?

A
  • intramuscular (#6) (10-20 min)
  • subcutaneous (#7) (15-30 minutes)
35
Q

Which route of administration take effect in 5-30 minutes?

A

rectal (#8)

36
Q

Which route of administration takes the longest (30-90 minutes)?

A

ingestion (#9)

37
Q

Which route of administration varies from minutes to hours?

A

transdermal (topical) (#10)

38
Q

What are the 3 types of parenteral injection?

A
  • intravenous (IV)
  • subcutaneous (SC)
  • Intramuscular (IM)
39
Q

Which route of administration is fastest and allows for systemic circulation immediately?

A

intravenous (IV)

40
Q

List several disadvantages of intravenous injection:

A
  • toxic reactions can be seen immediately
  • most dangerous route
  • drug must be in aqueous solution
  • must be performed slowly
  • once injected, drug cannot be removed
41
Q

List several advantages of intravenous injection:

A
  • extremely rapid
  • initial absorption step is by-passed
  • drug levels are more accurately controlled
  • good for irritant drugs
  • suitable for large volumes
42
Q

The rate of parenteral injection is limited by what 3 things?

A
  • area of absorbing capillary membranes
  • solubility of the substance in interstitial fluid
  • large molecules gain access to the circulation (biologics)
43
Q

The ‘time until effect’ that refers to route of administration is based on what?

A

plasma concentration curve

44
Q

Route of administration determines the ____ and ____ of absorption.

A

rate; efficiency

45
Q

The more charged a drug molecule, the ____ water soluble and the ____ lipid soluble it is.

A

more; less

46
Q

Which functional groups are acids?

A
  • carboxylic acids
  • beta-dicarbonyls
  • sulfonamides and sulfonylureas
  • tertrazoles
  • phenols
  • thiols
  • sulfates, phosphates, phosphonates
47
Q

Which functional groups are bases?

A
  • aliphatic and alicyclic amines
  • aromatic amines
  • imines and hydrazines
  • aromatic heterocycles (nitrogen)
48
Q

T/F amides are bases:

A

FALSE amides are neutral !!

49
Q

T/F sulfonamides are acids:

A

TRUE

50
Q

What is an amphoteric molecule?

A

a molecule with acidic + basic groups

51
Q

What is the most abundant protein in blood?

A

serum albumin (lipid binding sites)

52
Q

Ionization of acidic/basic groups affect plasma protein binding and tissue binding, what does this affect?

A

distribution

53
Q

What type of group can be in a benzo ring?

A

amine group

54
Q

An imide is when X is a ___ atom.

A

NITROGEN
(X = N)

55
Q

What functional group has a pKa slightly higher than carboxylic acids (less acidic) and is more lipophilic than carboxylic acids?

A

tetrazoles

56
Q

What type of drug contains a tetrazole in its structure? (hint: not an actual drug name)

A

angiotensin II receptor blockers

57
Q

Is phenol predominantly ionized in blood?

A

no, its unionized

58
Q

What amino acid has a phenolic side chain?

A

tyrosine

59
Q

Which functional group (that was listed in the acid/base powerpoint) is the strongest base?

A

guanidine (pKa = 12-13)

60
Q

The acid/base nature of a drug molecule influences what? (this is long, sorry)

A
  • overall water solubility of drug molecule
  • oral absorption of drug molecule
  • passive reabsorption of drug molecule w/in urinary tract
  • ability of drug molecule to interact w biological target
  • metabolism and elimination of drug molecule
  • ability to form water or lipid-soluble salts
  • suitability of drug molecule for given pharmaceutical formulation and route of administration

SHORTENED VERSION
- water solubility
- oral absorption
- passive reabsorption
- integration w target
- metabolism/elimination
- formation of water/lipid soluble salts
- suitability for formulation/administration

61
Q

What is #1 in the image?

A

peak effect

62
Q

What is #2 in the image?

A

onset of effect

63
Q

What is #3 in the image?

A

lag period

64
Q

What is #4 in the image?

A

duration of action

65
Q

What is #5 in the image?

A

MEC for adverse response

66
Q

What is #6 in the image?

A

therapeutic window

67
Q

What is #7 in the image?

A

MEC for desired response

68
Q

What does “Drug Effect (CP)” in the image refer to?

A

plasma concentration

69
Q

The therapeutic window of a drug is related to what?

A

related to drug effect

70
Q

What functional group is pictured?

A

alkane

71
Q

What functional group is pictured?

A

alkene

72
Q

What functional group is pictured?

A

alkyne

73
Q

What functional group is pictured?

A

benzene ring (phenyl)

74
Q

What functional group is pictured?

A

amine

75
Q

What functional group is pictured?

A

alcohol (hydroxyl group)

76
Q

What functional group is pictured?

A

ether

77
Q

What functional group is pictured?

A

alkyl halide

78
Q

What functional group is pictured?

A

thiol

79
Q

What functional group is pictured?

A

aldehyde

80
Q

What functional group is pictured?

A

ketone

81
Q

What functional group is pictured?

A

ester

82
Q

What functional group is pictured?

A

carboxylic acid

83
Q

What functional group is pictured?

A

amide

Pharmacodynamics (4 decks)

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