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OU PDA > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

What are the agencies responsible for selection of nonproprietary drug names?

A

USAN, AMA, APhA, USP, FDA

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2
Q

Define pharmacore

A

portion of a drug that is responsible for its biological action

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3
Q

Define prototype

A

representative compound of a drug class that is the standard of comparison for other compounds; ex. IBP is a prototype for NSAIDs

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4
Q

What are the characteristics of an effective drug?

A
  • effectively released from its dosage form
  • maintain physical characteristics and long shelf life
  • be appealing (via smell, taste, etc)
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5
Q

Define dosage form

A

final drug product in its final form which includes the active ingredient, excipients and drug delivery system

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6
Q

What are the four categories that dosage form fall under?

A
  • solids
  • liquids
  • semi-solids
  • dispersions
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7
Q

What are the physicochemical characteristics of drugs?

A
  • Physical nature of compound
  • Chemical nature of compound
  • Solubility
  • Acid-base formation
  • Stability
  • Stereochemistry
  • Functional groups
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8
Q

What are two forms of solid compound?

A

Crystalline form & Amorphous form

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9
Q

What are characteristics of the most stable polymorph?

A

highest melting point, lowest solubility, maximum stability

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10
Q

Define solution

A

solute dissolved in a solvent

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11
Q

Define VanderWaal interactions

A

weakest, between nonpolar portion, temperature dependent; important in lipopihlic substances

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12
Q

Define dipole-dipole interactions

A

also known as H bonding, partial ionic character leads to permanent dipole,

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13
Q

Define ionic interactions

A

attraction of oppositely charges atoms, important in inorganic molecules and salts of organic molecules

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14
Q

Define ion-dipole interactions

A

occurs between ion and dipole, important for dissolving organic salts in water, strong attraction is insensitive to temperature and distance

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15
Q

Define dissolution

A

process that controls the availability of a drug at the site of action, whereby a compound goes from a solid to solution in a solvent

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16
Q

Define solubility

A

concentration of a saturated solution of the compound in a given solvent at a given temperature

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17
Q

What is important in monofunctional groups?

A

intermolecular bonding

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18
Q

What is important in polyfunctional groups?

A

intramolecular bonding AND intermolecular bonding

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19
Q

What is lipophilicity important for?

A
  • permeability
  • drug transport
  • binding to plasma proteins
  • accumulation in tissues
  • recognition by receptor
  • specificity
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20
Q

What does the empiric method measure?

A

Estimates how many carbons a functional group can solubilize and water solubility

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21
Q

What is used in the analytical method for predicting solubility?

A

partition coefficient

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22
Q

With reference to the partition coefficient, which phase will the lipophilic drugs be more concentrated in?

A

the n-octanol phase

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23
Q

With respect to the analytical method, what is the value/meaning of LogP?

A

Concentration of drug in octanol / Concentration of drug in water

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24
Q

With respect to the analytical method, what does a positive and negative pi (π) value mean?

A
  • Positive: lipophilic

- Negative: hydrophilic

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25
Q

What does IMHB stand for?

A

intramolecular hydrogen bonding

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26
Q

Does intramolecular hydrogen bonding reduce or increase solubility?

A

reduces

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27
Q

Define water solubility with log P values

A
  • Log P > +0.5 (P > 1) –> water insoluble

- Log P < + 0.5 (P ≤ 1) –> water soluble

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28
Q

Identify undesirable values of log P to be a drug

A
  • Log P < 0 (P < 1) –> too hydrophilic to be a drug

- Log P > 3.5 (P> 3,000) –> too lipophilic to be a drug

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29
Q

What kind of shapes does micelles exist in?

A

spherical and cylindrical

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30
Q

Brönsted-Lowry definition of acids

A

any substance that can donate a proton

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31
Q

Brönsted-Lowry definition of bases

A

any substance that can accept a proton

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32
Q

Strong acid Ka and pKa values

A
  • tend to have high Ka value

- low pKa values

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33
Q

Strength of weak and strong acid’s conjugate base

A
  • strong acid have weak conjugate base

- weak acid has strong conjugate base

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34
Q

Strong base Ka and pKa values

A
  • low Ka value

- high pKa value

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35
Q

What does having a low Ka value mean?

A

favor accepting protons

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36
Q

What does having a high Ka value mean?

A

favor donating protons

37
Q

Why are salts preferred for manufacturing?

A

they are easier to crystallize, more stable, dissolve faster, and easier to handle

38
Q

Different salts of the same pharmacore have (same/different) chemical and biological profiles

A

different

39
Q

Which is more soluble in water? monovalent salts or multivalent salts

A

monovalent salts

40
Q

What are examples of salts of acidic drugs?

A

sodium, potassium, ammonium, calcium, magnesium, zinc and aluminum salts

41
Q

What are examples of salts of basic drugs?

A

hydrochlorides, sulfates, phosphates, gluconates, glucuronates

42
Q

Salts with what are likely water insoluble?

A

complex amines and fatty acids

43
Q

With respect to what they do in the body, how does ionized compounds differ from non-ionized compounds?

A

they undergo absorption, distribution, metabolism, bind to receptors, and undergo elimination

44
Q

Stomach pH

A

1 - 3.5

45
Q

Small intestine pH

A

5.5 - 7.5

46
Q

Lung and blood pH

A

7.4

47
Q

Weak base and solubility

A
  • higher solubility at low pH
  • high solubility and dissolution in the stomach
  • low solubility in the small intestine
48
Q

Weak acid and solubility

A
  • higher solubility at high pH
  • low solubility and dissolution in the stomach
  • high solubility and dissolution in the intestines
49
Q

What are the purposes of buffers?

A
  • control pH
  • minimize degradation
  • improve patient comfort and compliance
  • (sometimes) to improve the efficacy of the drug
50
Q

Acidic buffer is made of what?

A

weak acid and salt

51
Q

Basic buffer is made of what?

A

weak base and salt

52
Q

weak acid + strong base ->

A

gives a weak conjugate base, results in a basic solution

53
Q

weak base + strong acid ->

A

gives a weak conjugate acid, results in an acidic solution

54
Q

For a weak acid, what does it mean when pH > pKa?

A

ionized (A-) > non-ionized (HA)

55
Q

For a weak base, what does it mean when pH < pKa?

A

ionized (BH+) > non-ionized (B)

56
Q

Percent of ionization based on pH and pKa values (pH of solution, pKa of compound)

A
  • if difference between the two is close to 0, then changes in pH cause changes in % ionization
  • if difference is large, there is little change in % ionization
  • if compound is weak acid and solution pH is 4 units less than the pKa, completely unionized
  • if compound is weak base and solution pH is 4 units above the pKa, completely unionized
57
Q

What are two excipients commonly found in IR drugs?

A

disintegrants and surfactants (which increases deaggregation)

58
Q

Which (IR or CR) has better pharmacodynamics?

A

CR; it also has better efficacy

59
Q

What is sustained release?

A

it is CR but dissolution rate is reduced so that dissolution rate = elimination rate ==> Drug in = Drug out

60
Q

Can all drugs be formulated into sustained release?

A

No; it depends on the limitation of the drug’s physicochemical properties

61
Q

Define shelf life

A

Time period of consistent performance of a drug when stored under the recommended conditions

62
Q

What are the accepted levels of degradation?

A

± 10% of the active ingredient

63
Q

What are the properties which to consider when determining a drug’s stability?

A

chemical, microbiological and physical

64
Q

Define chemical stability

A

ability of compound to resist changes in amount of active ingredients with time as a result of hydrolysis, oxidation, and photolysis

65
Q

Define microbiological stability

A

ability of a drug to resist microbial contamination from the environment and/or from patient use

66
Q

Define physical stability

A

ability of a drug to maintain its physical properties over time

67
Q

What are some examples of physical properties (with respect to Dr. You’s lecture notes)?

A

dissolution rate, uniformity, appearance, taste, odor

68
Q

What are the ways in which you can avoid degradation of a drug and maintain its stability?

A

adding buffers, cosolvents, chelating agents, antioxidants, protective film coating; adapted packaging, formulated as pro drugs

69
Q

What are the similarities and differences in enantiomers?

A

similar in physicochemical properties but differ in interactions (ex. binding sites)

70
Q

What are the different types of isomers?

A

optically active, enantiomers, geometric

71
Q

Define enantiomers

A

non-superimposable mirror images of each other

72
Q

What does functional groups determine (with respect to properties of a drug)?

A
  • size
  • solubility
  • acid-base properties
  • stereochemistry
  • reactivity
73
Q

Define bioisoterism

A

Functional groups which have similar spatial and electronic character

74
Q

Define ionic bonds

A

the strongest type of non-covalent bond. This results from the attraction of ions with opposite charge

75
Q

Define ion-dipole bonds

A

results when there is an attraction between an ion and the partial charge of a dipole of the opposite polarity

76
Q

Define dipole-dipole bonds

A

partially positive atom in a dipole is attracted to a partially negative atom in another dipole

77
Q

Define hydrogen bonding

A

dipole-dipole interaction where one of the constituents is a hydrogen attached to a heteroatom

78
Q

Define the hydrophobic effects

A

when water cage surrounding a hydrophobic region is broken and entropy increases

79
Q

Define the charge-transfer complexes

A

lone pair of electrons is “shared” with a neighboring group that has considerable pi character

80
Q

Acidic buffer pH

A

pH < 7

81
Q

Basic buffer pH

A

pH > 7

82
Q

How do can dissolution be increased?

A
  • decrease particle size
  • increase solubility of weak acids/bases
  • decrease concentration in bulk
  • decrease diffusion layer thickness
83
Q

Define chemical isoterism

A

similarity in physicochemical properties of ions, compound, or elements due to the similar electronic structure

84
Q

What happens when replacing a group within a bioisostere?

A

a new compound that retains/enhances/reduces the activity of the parent compound

85
Q

What are the Lipinski’s Rule of Five?

A
  • Not more than 5 hydrogen bond donors
  • Not more than 10 hydrogen bond acceptors
  • A molecular mass not greater than 500 daltons (g/mol)
  • An octanol-water partition coefficient log P not greater than 5
86
Q

What are important functional groups in receptor and enzyme binding?

A

hydroxy, carboxy, amino, ethers, carbonyl groups

87
Q

What are “Privileged Scaffolds”?

A

molecular frameworks that are seemingly capable of serving as ligands for a diverse array of receptors

88
Q

What makes up Phase I in metabolism?

A

oxidation, reduction, hydrolysis

89
Q

What makes up Phase II in metabolism?

A

acetylation, sulfation, glucuronidation, and conjugation with amino acids

OU PDA (8 decks)

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