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Chem exam 4 > 11/5 > Flashcards

11/5 Flashcards

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1
Q

this is the study of the interactions between a drug and
organism

A

pharmacology

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2
Q

the study of how a drug affects the
organism

A

Pharmacodynamics

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3
Q

the study of how the organism affects the drug

A

Pharmacokinetics

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4
Q

What is included in pharmacodynamics?

A

-Site of Action
-Mechanism of Action
-Receptor Binding
-Postreceptor Effects
-Chemical Interactions

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5
Q

What can affect pharmacodynamics?

A

Disease or Disorder
Age
Drug–Drug interactions

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6
Q

What are the three receptor subtypes?

A

Enzymes
Ion Channels
Membrane receptors

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7
Q

What are the ways that drugs bind due to chemical interactions (4 total)?

A
  • Electrostatic interactions (intermolecular forces)
  • Hydrophobic interactions
  • Covalent bonds
  • Stereospecific interactions (enantiomers)
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8
Q

how well the drug binds to the receptor

A

affinity

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9
Q

how well the drug produces its desired effect

A

efficacy

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10
Q

term used to compare the relative affinity of competing drugs

A

potency

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11
Q

These concepts help us gain a better understanding of how we are going to administer the drug

A

absorption, distribution, metabolism, and excretion of drugs from the body

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12
Q

What is the most common type of intermolecular force with drugs?

A

hydrogen bonding

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13
Q

LD50

A

lethal dosage to kill 50% of the population given that drug - not done on humans

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14
Q

This method of drug administration is other than the intestine

A

parenteral

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15
Q

Examples of parenteral drug administration

A

-intramuscular
-Subcutaneous
-Intravenously
-Inhalation

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16
Q

This determines time to maximal concentration at the receptor to produce peak effect.

A

Absorption rate

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17
Q

This is how much of the administered drug is actually
absorbed. (typically used for oral administration)

A

bioavailability

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18
Q

8 factors effecting bioavailability

A
  • Molecular weight of the drug
  • Drug formulation
  • Drug stability (especially pH sensitivity)
  • First pass metabolism (typically in the liver)
  • Blood flow
  • Gastric emptying (food slows this process)
  • Intestinal motility
  • Drug interactions
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19
Q

This is the effectiveness of the movement of the drug throughout the body

A

distribution

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20
Q

What influences distribution? (6 things)

A
  • Blood
  • Total body water
  • Extracellular fluids
  • Lymphatic fluids
  • Cerebrospinal fluids
  • Protein-binding
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21
Q

What type of properties help determine ability of drug to be
distributed to the desired receptor site.

A

drug solubility

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22
Q

This is the breakdown of drugs into metabolites

A

metabolism

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23
Q

What happens to prodrugs during metabolism?

A

They are converted from inactive form to active form

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24
Q

Cytochrome p450 enzymes like to use this type of reaction to metabolize drugs

A

REDOX reactions

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25
Q

Common metabolism processes

A

REDOX reactions, hydrolysis

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26
Q

What things are metabolized via hydrolysis?

A

esters, amides, and nitriles

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27
Q

What is a downside to metabolism?

A

Has the potential to lead to the formation of toxic metabolites

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28
Q

Main routes for excretion:

A
  • Kidneys (majority of drugs)
  • Feces (unabsorbed drug or metabolites from bile)
  • Lungs (inhaled anesthetic drugs)
  • Sweat (not very common)
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29
Q

Most drugs fail during the _____ phase

A

discovery

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30
Q

___% of all drugs fail in clinical testing

A

90%

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31
Q

Lipinski Rule of 5

A

-describes drug potential for a new chemical entity (NCE)
-Used as a tool to measure a NCE’s potential bioavailability

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32
Q

Ionized drugs are more ___ soluble

A

water

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33
Q

Lipinski rule of 5 with drug development is based on

A

*Hydrogen bond donors (typically amines and alcohols)
* Hydrogen bond acceptors (total number of N, O, and F)
* Molecular weight (MW)
* Calculated Partition Coefficient (cLogP)

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34
Q

Violation of more than one “rule” predicts a NCE is ______

A

non-orally available

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35
Q

We try to limit molecular weight at

A

500

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36
Q

Ratio of the solubility of a drug in oil vs water (so it mirrors the cellular membrane)

A

cLogP

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37
Q

Try to keep the cLogP under __

A

5

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38
Q

We try to limit the amount of hydrogen bond acceptors (N and O) to __ or less

A

10

39
Q

This is where the binding has to occur to elicit a response

A

active site

40
Q

Is it easy for low MW drugs with a low cLogP to cross membranes?

A

Yes

41
Q

Potential drug compounds must have a mix of ________ and
______ groups

A

hydrophilic, lipophilic

42
Q

Structural alerts – certain functional groups that have been linked
to increased toxicity due to their metabolites (5 total) :

A
  • Aromatic anilines
  • Nitroaromatics
  • Aliphatic halides
  • Polycyclic aromatic hydrocarbons
  • Thiophenes
43
Q

Drug efficacy is directly related to ____________

A

the concentration of the drug at
its site of action.

44
Q

True or false Drugs must cross membranes throughout the entirety of ADME

A

true

45
Q

Absorption of drugs into the bloodstream is dependent on the _____ properties of the drug and the ___ at the site of absorption

A

acid/base, pH

46
Q

Why does transport plateau at high drug concentrations?

A

due to limited number of transport proteins available

47
Q

Daltons is shorthand for

A

g/mol

48
Q

Extremely Small Drugs (< 50 Da)

A

Bulk Flow (passive transport)

49
Q

Lipophilic Drugs (50 – 500 Da)

A

Passive transport

50
Q

Lewis acid

A

electron acceptor

51
Q

Lewis base

A

electron donor

52
Q

Bronsted base

A

proton acceptor

53
Q

Anything less than 500 g/mol will diffuse by

A

passive transport

54
Q

Bronsted acid

A

proton donor

55
Q

These acids completely ionize (break apart into ions) when
dissolved in water

A

strong acids

56
Q

Strong acid examples

A

HCl, HBr, HI, HNO3, HClO4, H2SO4

57
Q

These acids partially ionize when dissolved in water

A

weak acids

58
Q

Examples of weak acids

A

HF, H2CO3, H3PO4, organic acids (carboxylic acids, protonated drugs, etc)

59
Q

Strong Acids have ____ conjugate bases

A

weak

60
Q

Weak Acids have _____ conjugate bases

A

strong

61
Q

When we calculate pH we focus on the ____ definition of acid and bases. Why?

A

Bronsted-Lowry, we are looking at the protons

62
Q

Conjugate acid and bases are shown on the ___ side of an equation

A

product

63
Q

Water can act as

A

either an acid or base

How it acts depends on what it is being mixed with

64
Q

Think of acidity as

A

a sliding scale

You can take two acids and they react together, one will react as an acid one as a base because one is more acidic than the other.

65
Q

This is the substance formed by the removal of a proton from an acid

A

conjugate base

66
Q

This is a chemical compound formed when an acid gives a proton to a base

A

conjugate acid

67
Q

When talking about strength of acids we are referring to

A

if it completely ionizes (strong) or not (weak)

68
Q

What does ionize mean?

A

break apart into ions

69
Q

All of the drugs we are dealing with will be

A

a weak acid or weak base

70
Q

These bases completely ionize (break apart into ions) when
dissolved in water

A

strong base

71
Q

What does the double arrow “equilibrium” represent

A

The rate of the forward reaction is equal to the rate of the backwards reaction

72
Q

Strong base examples

A

LiOH, NaOH, KOH, Sr(OH)2, Ca(OH)2, Ba(OH)2

73
Q

These bases partially ionize when dissolved in water

A

weak bases

74
Q

Water is amphoteric, what does this mean?

A

can act as either an acid or a base

74
Q

What is the Water Constant (KW)? (definition)

A

measure of the self ionization of water

75
Q

What is the water constant (#)?

A

1.00 x 10^-14

76
Q

The higher the pH the more ___ something is

A

basic

77
Q

The higher the pOH the more ___ something is

A

acidic

78
Q

The lower the pOH the more ___ something is

A

basic

79
Q

When dealing with a strong acid it produces

A

H3O+

80
Q

When dealing with a strong base it produces

A

OH-

81
Q

When solving for a pH of a base solve for ___ initially then ___

A

pOH, then subtract it from 14 to get pH

82
Q

If you get a pH for a base it should always be

A

> 7.0

83
Q

if you get a pH for an acid it should always be

A

<7.0

84
Q

pH + pOH =

A

14

85
Q

pH of 7 =

A

neutral

86
Q

Acid strength is actually relative and depends on the ability of the
group to _________

A

give up a proton.

87
Q

The larger the KA = the easier it is to ______

A

remove the proton (more acidic)

88
Q

The lower the pKA the more ___ something is

A

acidic

89
Q

Note the pH scale is logarithmic so a change of 1 actually scales to a
change by a _____

A

factor of 10

So when you go to a pH of 6 –> 7 you are actually changing it by a factor of 10

90
Q

If the exponent is negative move your decimal place

A

to the left

91
Q

Calculate the pH of the following solution:
1.50 x 10^-3 M HCl

A

2.82

Steps:
-log [1.50 x 10^-3] = 2.82

92
Q

Calculate the pH of the following solution:
3.51 x 10^-2 M NaOH

A

12.55

Steps:
-log[3.51 x 10^-2] = pOH = 1.45
pH = 14 - 1.45 = 12.55

93
Q

pKA of H2O

A

16

Chem exam 4 (2 decks)

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