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Flashcards in Module 7 Deck (39)
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1
Q

Study of what the drug does to the body.

A

Pharmacodynamics

2
Q

Study of the biochemical and physiological effects of drugs and the mechanisms by which drugs produce effects.

A

Pharmacodynamics

3
Q

To evaluate the pharmacodynamics of drugs, we look at __________.

A

dose-response curves

4
Q

Dose-response curves are _______, which means that the response increases as the dose increases.

A

monotonic

5
Q

Importantly, dose response curves are not linear, thus we usually look at them as _____________ plots.

A

semi-logarithmic

6
Q

What are the phases of the semi-log dose response curve.

A

Phase 1 - Doses are too low to elicit a clinically relevant response
Phase 2 - the response is graded and nearly linear
Phase 3 - Larger doses do NOT lead to greater responses - larger doses may lead to toxicity.

7
Q

Measure of how effective a drug is at a given dose

A

Efficacy

8
Q

Maximum effect that a drug is capable of achieving

A

maximal efficacy

9
Q

Maximal efficacy is read off the dose response curve by looking at what?

A

Maximum height

10
Q

Healthcare professionals often titrate the dose of a drug. What does this mean?

A

This means they start with a low dose of the drug and slowly increase the dose while monitoring the patient’s response

11
Q

Refers to the amount of drug required to elicit a pharmacological response.

A

potency

12
Q

In order to compare potency, what is necessary?

A

Both drugs MUST produce the same therapeutic effect

13
Q

A more potent drug will require a ______ dose to achieve the desire effect than a less potent drug.

A

smaller

14
Q

Potency is determined by comparing the dose required to produce the half-maximal response - the ____.

A

ED50

15
Q

Most drugs act on ________ _________.

A

cellular macromolecules

16
Q

Give an example of a drug that does not act on cellular targets.

A

Antacids

17
Q

Protein that a drug binds to and produces a measurable response.

A

receptor

18
Q

What are the 4 most important types of receptors?

A

1 - Ligand-gated ion channels
2 - GPCR
3 - Enzyme-linked receptors
4 - Intracellular receptors

19
Q

What is an important example of a ligand-gated ion channel?

A

GABA receptor

20
Q

Describe the action of the GABA receptor.

A

When GABA (NT) binds to the GABA receptor, it causes the opening of a channel that allows the ion chloride to flow into the cell

21
Q

Drugs that are part of the _______ class are able to bind to the GABA receptor and allow chloride to enter the cell.

A

benzodiazepine

22
Q

Activation of the GABA receptor causes _______ and muscle _______ mediated by the increased intracellular chloride.

A

sedation

relaxation

23
Q

Describe the time frame of response for ligand-gated ion channels.

A

Responses to these receptors are very rapid, having a duration of milliseconds

24
Q

Approximately __% of marketed drugs mediate their effects through actions on GPCRs.

A

50

25
Q

What are the three components of GPCRs?

A

Seven transmembrane spanning protein receptor
G-protein with three subunits
Effector molecule

26
Q

Describe the timeframe of activation of GPCRs.

A

Result in a response that lasts from seconds to minutes in duration.

27
Q

What endogenous NTs mediate their effects by binding to GPCRs?

A

NE, serotonin, histamine

28
Q

Describe enzyme-linked receptors.

A

Receptor side is on the outside of the cell membrane

Catalytic side in on the inside

29
Q

Describe the time frame of the response for enzyme-linked receptors.

A

Very rapid - seconds

30
Q

What is an example of an enzyme-linked receptor in the body?

A

Insulin binding to the insulin receptor - causes enzyme-mediated phosphorylation and activation of an intracellular effector (causes increased translocation of glucose transporters to the cell membrane)

31
Q

What is the net effect of insulin binding to its receptor?

A

Increased cellular glucose uptake and utilization

32
Q

Intracellular receptors reside completely inside the cell and are also called __________ _________.

A

transcription receptors

33
Q

In order for ligands to access intracellular receptors, what must they be able to do?

A

Cross the cell membrane by diffusion or via drug transport proteins

34
Q

Binding of the ligand to the intracellular complex causes translocation of this complex to the _______ and binding to ______.

A

nucleus

DNA

35
Q

When the ligand-receptor complex binds to DNA, what occurs?

A

RNA transcription is stimulated, with protein synthesis occurring hours to days later

36
Q

Ligands to intracellular receptors are typically highly ______ _______. What are some endogenous examples?

A

lipid soluble

Steroid molecules such as testosterone and estrogen

37
Q

Drugs that are ________ will bind to only one receptor and therefore will be less likely to produce ______ _______.

A

selective

side effects

38
Q

IF a drug binds to only one receptor, can there be side effects?

A

Yes, the receptor may be located in many different organs.

39
Q

What is the classical view of drug selectivity?

A

Lock and key hypothesis