PRELIM 03 - Basic Considerations of Drug Activity Flashcards

1
Q

A molecule that possesses one or more functional groups positioned in a 3D space on a structural framework

A

Drug molecule

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2
Q

Is the discipline concerned with determining the influence of chemical structure on biological activity

A

Medicinal chemistry

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3
Q

A molecule that possesses the chemical and physical properties that will enable it to become a drug molecule

A

Drug-like molecule

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4
Q

Portion of the molecule that establishes intermolecular interactions with the receptor site (Structural fragments)

A

Bioactive face

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5
Q

Hold the functional group’s atoms of the pharmacophore in a fixed geometric pattern to permit specific receptor interaction (Structural fragments)

A

Molecular baggage

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6
Q

Arrangement of molecules that permits the bioactive face to interact with the receptor (Types of biophores)

A

Pharmacophore

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7
Q

3D arrangement of atoms in a molecule that is responsible for the metabolic properties (Types of biophores)

A

Metabophore

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8
Q

3D arrangement of atoms in a molecule that is responsible for the toxicity eliciting interaction (Types of biophores)

A

Toxicophore

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9
Q

A highly significant physical property that determines the ability to be transported to the site of action

A

Water solubility

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10
Q

Relationship between bioactivity and solubility

A

Directly proportional

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11
Q

Equation used to predict the degree of ionization in a molecule

A

Henderson-Hasselbalch equation

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12
Q

Refers to the ratio of the concentrations of drug in octanol to that in water

A

Partition coefficient

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13
Q

Coefficient that determines the relative solubility of a drug between water and lipids

A

Partition coefficient

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14
Q

A partition coefficient of __________ means that the drug is lipid soluble

A

> 0.01

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15
Q

Refers to the electron density and distribution patterns that help explain a drug’s reactivity

A

Resonance

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16
Q

Refers to the electron-attracting or electron-withdrawing effect that is transmitted through sigma bonds

A

Inductive effect

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17
Q

Electron donating = __________ group

A

Activating

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18
Q

Electron-withdrawing = __________ group

A

Deactivating

19
Q

Refers to the spacing or the distance between the nuclei of atoms in a drug molecule

A

Interatomic distance

20
Q

Are compounds containing the same number and kinds of atoms and the same arrangement of bonds but different 3D structures

A

Stereoisomers

21
Q

Are non-superimposable mirror images (Types of stereoisomers)

A

Enantiomers

22
Q

Include compounds containing double bonds and ring systems (Types of stereoisomers)

A

Diastereomers

23
Q

The portion of drug molecule containing the essential organic functional groups that directly interact with the receptor active site

A

Pharmacophore

24
Q

Promazine is an example of __________ drug

A

Antipsychotic

25
Promethazine is an example of __________ drug
Antihistamine
26
Replacement or modification of functional groups with other groups having similar properties is known as __________ or __________ (IB)
Isosteric replacement/Bioisosteric replacement
27
Are functional groups or molecules that have chemical and physical similarities producing broadly similar biological properties
Bioisosterism
28
Activity is more correlated to chemical properties of a drug (Structural specificity)
Structurally specific
29
Activity is more correlated to physical properties (Structural specificity)
Structurally nonspecific
30
Usually administered in small doses (Structural specificity)
Structurally specific
31
Usually administered in large doses (Structural specificity)
Structurally nonspecific
32
Relative saturation is <0.01 (Structural specificity)
Structurally specific
33
Relative saturation is 0.01-1 (Structural specificity)
Structurally nonspecific
34
If aspirin's pKa is 3.5 at a gastric pH of 2.1, what percentage of the drug would exist in the ionized and unionized form?
% Ionization = 3.83%; % Non-ionization = 96.17%
35
What is the % ionization and non-ionization of phenylpropanolamine at pH 7.4? The pKa is 9.4
% Ionization = 99.01%; % Non-ionization = 0.99%
36
What is the % ionization and non-ionization of amobarbital at pH 7.4? The pKa is 8.0
% Ionization = 79.92%; % Non-ionization = 20.08%
37
Active configuration of epinephrine
R-epinephrine
38
Inactive configuration of epinephrine
S-epinephrine
39
Active configuration of triprolidine
E-triprolidine
40
Inactive configuration of triprolidine
Z-triprolidine
41
Active configuration of ibuprofen
S-ibuprofen
42
Inactive configuration of ibuprofen
R-ibuprofen
43
The potent and toxic configuration of warfarin
S-warfarin
44
Configuration of warfarin with an anticoagulant effect
R-warfarin