Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Chemistry > Module 10: Pharmacology Basics > Flashcards

Module 10: Pharmacology Basics Flashcards

Test 4

You may prefer our related Brainscape-certified flashcards:
Periodic Table flashcards Chemistry 101 flashcards AP® Chemistry flashcards Organic Chemistry 101 flashcards
1
Q

What is the difference between Pharmacology, pharmacodynamics, and pharmacokinetics?

A

Pharmacology: interactions between a drug & organism

pharmacodynamics: how the drug affects the organism

pharmacokinetics: how the organism affects the drug (ADME)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are 3 things that can affect pharmacodynamics?

A
  1. disease/disorder
  2. age
  3. drug interactions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the receptor subtypes? Main one?

A

Enzyme (main)
Ion channel
membrane receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

How do drugs bind to receptors?

A

Intermolecular forces (electrostatic interactions)
Hydrophobic interactions
Covalent bonds (Intramolecular forces)
Sterospecific interactions

SICH of this…

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Covalent bonds are normally _____ therefore we try to avoid them

A

irreversible

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Why are sterospecific interactions important?

A

some receptors are antiomer specific while some allow multiple stereoisomers. some receptors will illicit a negative effect if bound with a different stereoisomer.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Drugs act as a _______

A

ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are 4 drug properties that we look at? Describe them. Do we like for them to be low or high?

A
  1. Affinity: How well the drug binds to the receptor
  2. Specificity: How specific the drug is to that receptor
  3. Efficacy: how well the drug produces desired effects
  4. Potency: compare drugs to see which has a higher affinity/specificity/efficacy
  • We want all of these things to be high
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the 2 types of drugs and their subtypes?

A

Agonist

Antagonist: Competitive & noncompetitive (irreversible)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What does allosteric mean?

A

Outside of active site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What does ADMET stand for?

A

Absorption
Distribution
Metabolism
Excretion
Toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

________ of the drug at the _________ affects the ability of the drug to give its desired effects

A

concentration

active site

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

ADMET refers to Pharmaco_____

A

kinetics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is LD50?

A

Lethal dosing to kill 50% of population in animals

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

T/F: Water has an LD50

A

T

Everything has an LD50

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are 4 things Pharmacokinetics help us understand?

A
  1. Drug administration
  2. therapeutic dosing
  3. time intervals between drug dosing
  4. toxic dosing
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the unit measurement in toxic dosing?

A

mg/kg

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is fentanyl’s LD50?

A

Very low

0.2 mg/kg

This means a very small amount can kill you
The lower the LD50, the easier it is to kill a person with a small dose!!! This is why people wear gloves when there could be a possible exposure to fentanyl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Explain ADME

A

Absorption: getting drug into the body

Distribution: getting the drug to the place where it needs to work (site of action)

Metabolism: Most metabolized in the liver by enzyme P450

Excretion: Leaving the body by means of mostly urine or feces

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What type of reactions are used in the liver for metabolism? What enzyme is used?

A

REDOX

Cytochrome P450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are all the ways a drug can be exreted from the body? What are the 2 most common ways?

A

Urine
Bile
Feces
Sweat
Saliva

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What happens if we dont properly excrete drugs from the body?

A

Toxic build up

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What are the methods of drug administration?

A

Enteral (oral)
Parenteral (non-oral)
–IM
–SQ
–IV
–Inhalation
–Topical

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Which method of drug administration bypasses the 1st pass effect?

A

IV, IM, SQ

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Which method of drug administration is the fastest?

A

IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Which method of drug administration is most effected by the 1st pass effect?

A

PO

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Which method of drug administration are effected by the 1st pass effect?

A

PO
Inhalation

28
Q

________ rate will determine how long it takes to see peak effects

A

absorption

29
Q

What does bioavailability refer to?

A

How much of the administered drug is actually absorbed. Typically in PO & topical

30
Q

Describe what taking a medication on an empty stomach does vs with food

A

W/ food: slows down absorption

w/o food: drug absorbed more rapidly

31
Q

What does ionized mean?

A

Able to dissociate when dissolved in water

32
Q

An ionized drug is ______ soluble in water

A

More

33
Q

T/F: A drug that is less water soluble is more easily distributed through the body

A

F

more water soluble

34
Q

How do you make a drug more water soluble?

A

Adding more polar groups
Ionization of the drug

35
Q

Although making a drug more polar/ionized will help it be distributed through the body more, why dont we want to do this TOO much?

A

having the drug be too polar or too charged will make it harder for it to cross the cell membranes.

36
Q

What happens to drugs and prodrugs in the liver?

A

Prodrugs: actives
drugs: inactives or activated metabolites

37
Q

What are the 2 reactions that take place during metabolism?

A

Hydrolysis
REDOX

38
Q

What helps prevent toxic buildup and promotes the removal of metabolites in the body?

A

Excretion

39
Q

How many years does it take for a drug to make it to market?

A

13 years

40
Q

What are the top 2 reasons why drugs fail during clinical testing? What percentage is it?

A

Pharmacokinetics and lack of efficacy

69%

41
Q

Where do most drugs fail at?

A

Discovery phase

42
Q

How long is the preclinical phase?

A

1 year

43
Q

How long is the discovery phase?

A

4.5 years

44
Q

Describe the Lipinski Rule of 5

A

-Occurs in preclinical

-Want to ensure drug compounds follow these 5 basic rules

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

45
Q

What are the Lipinski’s Rule of 5

A
  1. Less than 10 Hydrogen donors/acceptors
  2. Molecular wt less than 500
  3. Calculated partition coefficient (cLogP) <5
46
Q

What is Calculated partition Coefficient (cLogP)?

A

ratio that measures the solubility of oil vs water
Want to be <5

47
Q

What are hydrogen bond donors?

A

-NH
-OH

48
Q

What are hydrogen bond acceptors?

A

NOF
-N
-O
-F

49
Q

T/F: -NH is both a good hydrogen bond donor & acceptor

A

T

50
Q

Why do we want the hydrogen bond donors/acceptors to be less than 10 in the Lipinski’s Rule of 5?

A

It increases polarity which decreases membrane premeability

51
Q

Describe a hydrogen bond

A

Specialized dipole-dipole interaction
Increases affinity of a drug to a receptor

52
Q

What increases a drug’s affinity to a receptor?

A

Hydrogen bonds

53
Q

What part of an amino acid is able to undergo hydrogen bonding?

A

Side chains

54
Q

Potential drugs must have both _______ and ______ groups

A

Hydrophilic

Lipophilic

55
Q

Which structural groups have been linked to increased toxicity due to their metabolites?

A

Aromatic anilines
Nitroaromatics
Aliphatic halides
Polycyclic armomatic hydrocarbons
Thiophens

56
Q

What does Nitroaromatics metabolize into?

A

Armomatic aniline

57
Q

What happens when you metabolize aliphatic halides?

A

Covalent bonds

58
Q

Polycyclic aromatic hydrocarbons are ________

A

Cancer causing

59
Q

Thiophens oxidize into_______

A

toxic metabolites

60
Q

T/F: Size & charge of the drug effect permeability

A

T

61
Q

What are we going to need if we have a big, charged drug?

A

Active transport protein

62
Q

What are the 2 types of transport? Describe them

A

Active: Requires energy (ATP)
-Across a gradient
-AT high drug concentration, transport plateaus

Passive: high concentration to low concentration
-drug needs to be low wt, and uncharged

63
Q

What is Da?

A

Dalton
Unit of measurement

Grams/Mol

64
Q

What is a small drug? What does this mean?

A

< 501 Dalton

Uses passive transport

65
Q

What functional groups does Hydrolysis include?

A

Esters
Amides
Nitriles

66
Q
A

Chemistry (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions