Lecture 1: Intro to Pharmacology Flashcards

1
Q

How do drugs exert their effects?

A

By binding to receptors in our bodies and triggering a functional change

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

What is Pharmacodynamics?

A

The detailed interaction of drugs at the molecular level. The specific actions of drugs at its receptors

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

What is Pharmacokinetics?

A

All the steps in the body before the drug reaches its target receptor in the body. The distributions and absorption properties of drugs that determine the specific concentration that a receptor will see

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

What is the generic name of Terfenadine?

A

Seldane

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

What target was Terfenadine initially believed to act on?

A

The H1 receptor (the histamine receptor)

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

How was it thought that Terfenadine worked?

A

It was an H1 receptor antagonist so it prevented the activation of H1 receptors by histamine

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

How did Terfenadine actually work?

A

It was metabolized by the liver and converted to fexofenadine which is the actual antagonist of the H1 receptor

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

What is a Prodrug?

A

A compound that is not intrinsically active and is activated by some metabolic step after administration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is a Receptor?

A

The molecular target of a drug

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

Through what process is Terfenadine metabolized?

A

Through “first pass metabolism” in the liver

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

What kind of principles are the principles of a drug being activated or deactivated?

A

These are Pharmacokinetics principles

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

What could happen if Terfenadine is not completely processed by the liver?

A

It could have unintentional effects on the heart

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

How can Terfenadine affect the heart?

A

It can block certain ion channels in the heart that control electrical activity that underlies the heart beat

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

What are Off-Target Effects?

A

When drugs are not perfectly specific for one receptor type and can influence closely related receptors or completely unrelated receptors

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

What are Adverse events?

A

Undesirable drug effects that can vary in severity

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

What are the benefit and harm of drugs summarized with?

A

The “numbers needed to treat” and the “numbers needed to harm”

17
Q

What are adverse events related to on target effects?

A

Undesirable effects related to the drugs mechanism of action that tell you that the drug is working

18
Q

What caused some people to have unprocessed Terfenadine?

A
  • Some substances inhibit the activity of certain liver enzymes involved in drug metabolism (CYP3A4 enzyme)
  • Patients with diminished liver function or who are taking certain antibiotics or antifungals
  • Grapefruit juice is a CYP3A4 inhibitor
19
Q

Why were only some people affected by unprocessed Terfenadine?

A

Some patients also carried mutated versions of the genes encoding ion channel off targets in the heart making them more sensitive to terfenadine

20
Q

What is the solution to the Terfenadine issue?

A

To just administer the metabolite Fexofenadine

21
Q

What is Pharmacogenomics?

A

The genetic background of a patient which can significantly affect how they respond to a drug

22
Q

What is Drug Interactions?

A

When one drug/substance adversely affects the response to another

23
Q

What is Drug Interactions?

A

When one drug/substance adversely affects the response to another