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Chemistry Fall '24 > Test 4 - Module 10: Pharmacology Basics > Flashcards

Test 4 - Module 10: Pharmacology Basics Flashcards

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1
Q

Pharmacology is _____.

A. The study of how a drug affects the organism

B. The study of how the organism affects the drug

C. The study of the interactions between a drug and an organism

A

C

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2
Q

Pharmacodynamics is _____

A. The study of how a drug affects the organism

B. The study of how the organism affects the drug

C. the study of the interactions between a drug and an organism

A

A

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3
Q

Pharmacokinetics is _____

A. The study of how a drug affects the organism

B. The study of how the organism affects the drug

C. the study of the interactions between a drug and an organism

A

B

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4
Q

The study of the biochemical, physiological and molecular effects of drugs on the body is ____

A

Pharmacodynamics

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5
Q

When looking at pharmacodynamics what is included? (5)

A
  1. Site of action
  2. Mechanism of action
  3. receptor binding
  4. post receptor effects
  5. chemical interactions
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6
Q

What three things can affect pharmacodynamics

A
  1. age
  2. disease/disorder
  3. drug-drug interactions
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7
Q

What three receptor subtypes are included in pharmacodynamics

A
  1. Enzymes
  2. Ion channels
  3. Membrane receptors
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8
Q

How do drugs bind due to chemical reactions? (4)

A
  1. Electrostatic interactions (intermolecular forces)
  2. Hydrophobic interactions
  3. Covalent bonds
  4. stereospecific interactions (enantiomers)
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9
Q

Why do we avoid covalent bonds with drugs

A

Because it is an intramolecular force. Makes that receptor completely unavailable

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10
Q

What can happen with stereospecific interactions if you have the wrong enantiomers

A

it might not bind, or it might bind and have negative or no effects

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11
Q

Drugs act as a ____ that bind to the receptor

A

ligand

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12
Q

Affinity is ____

A. Term used to compare the relative affinity of competing drugs

B. How well the drug binds to the receptor

C. How well the drug produces its desired effect

A

B

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13
Q

Efficacy is ____

A. Term used to compare the relative affinity of competing drugs

B. How well the drug binds to the receptor

C. How well the drug produces its desired effect

A

C

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14
Q

Potency is ____

A. Term used to compare the relative affinity of competing drugs

B. How well the drug binds to the receptor

C. How well the drug produces its desired effect

A

A

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15
Q

If we have a higher affinity we would be able to do what to the dose?

A

Have a lower dose/not take as much of the drug

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16
Q

What is a competitive antagonists

A

bind reversibly

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17
Q

what is a non-competitive antagonists?

A

Either binds irreversibly or binds to create allosteric effects that diminish an agonists ability to bind to a different receptor

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18
Q

The study of the ADME of drugs from the body

A

Pharmacokinetics

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19
Q

______ effects the ability of the drug to give its desired effect

A

concentration

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20
Q

_____ helps us to better understand:
1. drug administration
2. therapeutic dosing
3. time intervals between drug dosing
4. toxic dosing

A

pharmacokinetics

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21
Q

What determines time to maximal concentration at the receptor to produce peak effect?

A

absorption rate

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22
Q

_____ tells us how much of the administered drug is actually absorbed

A

Bioavailability

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23
Q

What factors affect bioavaliability (8)

A
  1. Drug molecular weight
  2. Drug formulation
  3. Drug stability (esp pH sensitivity)
  4. Drug interactions
  5. Intestinal motility
  6. Gastric emptying (food slows this process)
  7. Blood flow
  8. First pass metabolism (typically in the liver)
24
Q

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

A

distribution

25
Q

Distribution is influenced by what? (6)

A
  1. blood
  2. total body water
  3. ECF
  4. lymphatic fluids
  5. CSF
  6. protein-binding
26
Q

What drug property help determine ability of a drug to be distributed to the desired receptor site?

A

Drug solubility

27
Q

_____ is the breakdown of drugs into metabolites

A

metabolism

28
Q

_____ convert from inactive form to active form

A

prodrug

29
Q

True/false: metabolism typically does not inactivate the drug ahead of excretion

A

false. It DOES typically inactivate ahead of secretion

30
Q

what are common processes of metabolism?

A

Hydrolysis and REDOX

31
Q

esters, amides and nitriles are metabolized via ____

A

hydrolysis

32
Q

If a drug is being broken down with CP450 enzymes in the liver that would be an example of a ______ reaction

A

REDOX

33
Q

What is Lipinski Rule of 5?

A

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

34
Q

How does the lipinski rule of 5 apply to H bond acceptors/donors

A

keep them less than 10

35
Q

Lipinski rule of 5 for molecular weight

A

less than 500

36
Q

Lipinski rule of 5 for calculated partition coefficient (cLogP)

A

less than 5. if it is less than 5 then it can cross membrane easily

37
Q

Violation of ______ “rule” predicts a NCE is non-orally available

A

one or more

38
Q

Structure of an amino acid

A
  1. amine group
  2. carboxcylic acid
  3. side chain (polar, non-polar, acid/base)
39
Q

What part of an amino acid can form an H bond?

A

the polar and acid/base part of the side chain

40
Q

Why do we like H bonds in drugs

A

they increase affinity

41
Q

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

A

hydrophillic and lipophillic

42
Q

What functional groups have been linked to increased toxicity due to their metabolites

A
  1. aromatic anilines
  2. nitroaromatics
  3. aliphatic halides
  4. polycyclic aromatic hydrocarbons
  5. thiophenes
43
Q

What do these functional groups have in common?
1. aromatic anilines
2. nitroaromatics
3. aliphatic halides
4. polycyclic aromatic hydrocarbons
5. thiophenes

A

They have been linked to an increased toxicity due to their metabolites

44
Q

Drug efficacy is directly related to the ______ of the drug at its site of action

A

concentration

45
Q

True/false. Drug concentration must be high enough to elicit the desired effect but not too high to cause negative effects

A

true

46
Q

Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for absorption?

A

when they enter the bloodstream

47
Q

Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for distribution

A

contact with a receptor

48
Q

Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for metabolism

A

when they leave receptor and move to liver

49
Q

Drugs have to cross membranes throughout the entirety of ADME. Where do they cross for excretion

A

passage to kidneys for removal

50
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

51
Q

_____ transport requires no energy while _____ transport requires energy

A

passive; active

52
Q

Active transport: At high drug concentrations, transport _____ due to limited number of transport proteins

A

plateaus

53
Q

true/false. active transport can lead to competition with structurally similar compounds.

A

true

54
Q

Small drugs (<50Da) and lipophilic drugs (50-500 Da) are transported via

A

passive

55
Q

Drugs that have an ionized charge and are (>50 Da) are transported via

A

active

Chemistry Fall '24 (10 decks)

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