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Year 1- Principles of Disease (FOM) > Pharmacogenetics > Flashcards

Pharmacogenetics Flashcards

1
Q

Define drug

A

A chemical designed to prevent, diagnose, treat or cure pathology.

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2
Q

What is the outcome of the drug treatment known as?

A

Pharmacological response

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3
Q

When does the pharmacological response occur?

A

When drug molecules interact with target molecules.

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4
Q

The effect of a drug binding to an inhibitor depends on two things- what are they?

A

-Affinity
-Intrinsic efficacy

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5
Q

Explain what is meant by high affinity and high efficacy

A

If a drug binds tightly to a receptor (i.e. has a high affinity), and has the capacity to produce a peak response (high efficacy).

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6
Q

Define residence time

A

The length of time for which the drug-receptor complex persists.

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7
Q

Define polymorphic variation.

A

How receptor responses vary between different people.

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8
Q

Name two factors which can impact receptor expression.

A

Age and disease

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9
Q

Describe the structure of endogenous interaction.

A

Lock and key

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10
Q

Describe the effect of agonists on receptors.

A

Agonists increase proportion of activated receptors

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11
Q

Describe the effect of antagonists on receptors.

A

Antagonists prevent activation

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12
Q

Define pharmacodynamics.

A

The effect of the drug on the body

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13
Q

Define pharmacokinetics.

A

The effect of the body on the drug.

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14
Q

Name the factors which determine whether or not a drug can exert its effects at the receptor.

A

ADME
Absorption
Distribution
Metabolism
Excretion

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15
Q

Name the two factors which determine if the drug gets to the site of action and whether it stays there.

A

Absorption and distribution

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16
Q

Name the two factors which determine if a drug will stay in the body.

A

Metabolism and excretion

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17
Q

Define absorption of drugs.

A

How the drug gets into the body

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18
Q

Define distribution of drugs.

A

How the drugs get around the body.

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19
Q

Define biophase.

A

The effect site of the drug (the physical region in which the drug target is located)

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20
Q

Define bioavailability.

A

The extent and rate at which the drug reaches it site of action

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21
Q

Why can’t we measure the bioavailability?

A

Most of the sites of action are going to be in tissues or on cells - or even in cells so would be too invasive or expensive to measure.

22
Q

Define practical bioavailability.

A

The extent and rate at which the drug reaches the systemic circulation.

23
Q

What is the most efficient way of getting the drug into the plasma?

A

IV

->100% gets into plasma while other routes, like oral etc, have to overcome barriers.

24
Q

Why is there less response when drugs are administrated in alterative ways to IV?

A

Drugs are metabolised before they reach the plasms.

25
Q

Where does most first-class metabolism occur?

A

In the liver.

26
Q

Describe half-life in terms of drugs.

A

The time taken for the concentration of drug in the plasma to fall to half of its current value.

27
Q

If there is a low half-life, how is can plasma concentration be maintained?

A

Regular administrations.

28
Q

What could a high half-life lead to?

A

Toxicity and accumulation.

29
Q

Define therapeutic index.

A

A ratio that compares the blood concentration at which a drug becomes toxic and the concentration at which the drug is effective.

30
Q

Where do the drugs go to after the plasma?

A

Depends on characteristic of the drug but characteristically-

->move from plasma to interstitial fluid
->cells are bathed
->then goes into intracellular fluid.

31
Q

Where are transcellular fluids produced?

A

By epithelial linings of spaces within the body

32
Q

Give some examples of transcellular fluids.

A

Cerebrospinal fluid, peritoneal fluid and the aqueous and vitreous humours in the eye.

33
Q

How do the drugs get from plasma to interstitial fluid?

A

Need to get out of capillary bed
They could either move between the cells of the capillary endothelial cells (filtration) or move into and out of the endothelial cells themselves (transcellular movement).

34
Q

How do drugs get from the interstitial fluid to the intracellular fluid?

A

->Drug must cross cell membrane

35
Q

What are some of the problems drugs face when trying to cross barriers?

A

->Not all endothelium is the same - whether or not the drug moves easily between cells depends on things like the presence of tight junctions (can stop cell movement).
->May have to use transport mechanisms
->May have to dissolve in the lipid bilayer of the membrane,

36
Q

What may effect filtration of drugs?

A

Size of drug
Structure of capillary wall

37
Q

What is important if a drug has to cross a membrane?

A

The lipophilicity of the drug (how easily it diffuses across cell membranes).

38
Q

Are lipid soluble drugs polar or non-polar?

A

Non-polar

39
Q

What could excessive ionisation lead to?

A

The ion becoming trapped

40
Q

If drugs are not lipid soluble, how can they cross the membrane?

A

Via some transport mechanisms
May involve facilitated diffusion, active transport or endocytosis

41
Q

Tissues must have a good supply of what to ensure drugs do their function?

A

Good supply of blood

42
Q

What would make the plasma concentration drop lower than the tissue concentration?

A

Metabolism and excretion

43
Q

What are general anaesthetics primarily metabolised by?

A

Enzymes in the liver

44
Q

What does elimination group together?

A

Metabolism and excretion.

45
Q

What happens to drugs that are not metabolised?

A

They are excreted

46
Q

What is the main principle of metabolism when getting rid of alien molecules or drugs etc?

A

To make the metabolite more polar than the parent compound and thus more easily excreted.

47
Q

Where is the main site of metabolism?

A

Liver

48
Q

What can liver disease increase the likelihood of?

A

Toxicity

49
Q

The health of the kidney as it plays a function in the role of?

A

Excretion as drugs can get excreted in the bile

50
Q

List the different methods of administration.

A

Intravenous: not absorbed
Oral (most common)
Subcutaneous
Intramuscular
Other GI (rectal, sublingual)
Nasal
Inhalation
Transdermal

Year 1- Principles of Disease (FOM) (40 decks)

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