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Year 3 > Molecules Exam 1a > Flashcards

Molecules Exam 1a Flashcards

1
Q

Pharmacology

A

The study of drug action on biological systems. What can we target?

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2
Q

Medicinal Chemistry

A

Design and optimization of drug molecules

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3
Q

Pharmaceutics

A

The science of drug delivery systems

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4
Q

What is a Drug?

A

Any chemical agent (other than food) that causes a physical or emotional change in an individual

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5
Q

Most drugs are less than how many daltons?

A

500

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6
Q

Serendipitous Drug Discovery

A

When your research is looking for something but you end up discovering something else

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7
Q

Why would enhancing a side effect be a good thing?

A

You can alter a drug with a certain side effect, such as increasing urinary output, and alter that drug to be made to increase urinary output (diuretic)

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8
Q

Why is selectivity important?

A

If there is a certain receptor that produces a certain side effect that you want to inhibit, you design the drug to be an antagonist to that receptor.

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9
Q

2 main reasons that drugs fail in clinical phase

A

Safety and efficacy

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10
Q

What is the importance of Gleevec?

A

It is a cancer therapy drug that kills cancer cells but leaves healthy cells intact. Gleevec’s mechanism focuses on a specific protein that does not exist anywhere else in the body.

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11
Q

Gene cloning is done with what kind of proteins?

A

Recombinant

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12
Q

Pharmacokinetic concept

A

When a drug is working to change the amount/concentration of another drug

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13
Q

Pharmacodynamic concept

A

When a drug changes the effect of another drug without changing the amount of drug

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14
Q

Pharmacokinetic definition

A

What the body does to the drug

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15
Q

Pharmacodynamic definition

A

What the drug does to the body

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16
Q

What route of administration is the only route that does not go through the venous side?

A

Inhalation

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17
Q

Absorption

A

When the drug has to go through a barrier before it can enter the bloodstream

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18
Q

When would it be desirable for an oral drug to have minimal absorption?

A

If the drug is treating something in the intestines, then it would be beneficial for the drug to stay there to treat it

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19
Q

Bioavailability

A

The rate and extent to which a drug is absorbed and becomes available at the site of action

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20
Q
A
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21
Q

Fenestrae

A

Windows(opening/pore) in capillaries that drugs can pass through endothelial cells

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22
Q

What organ does not have fenestrae?`

A

Brain capillaries

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23
Q

3 properties that allow molecules to freely diffuse through cell membranes

A

Low molecular weight, high lipid solubility, and uncharged

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24
Q

Does increased lipid solubility increase or decrease absorption?

A

Increase

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25
Q

What do you do to polar functional side groups in order to increase membrane permeability?

A

Remove them. The less polar functional groups, the more lipophilic the drug is and more easily absorbed.

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26
Q

What are prodrugs and why are they important?

A

They are drugs with added esters where polar or ionizable groups are masked with hydrophobic residues. After uptake of the drug, the hydrophobic groups are cleaved enzymatically which leaves the original drug in the bloodstream.

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27
Q

Is an acidic drug better absorbed in an acidic environment or basic environment? Why?

A

Acidic because it will be protonated and made neutral, which will allow it to be absorbed.

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28
Q

Where will amphetamine (pka 10) be best absorbed? Stomach (pH 1) or intestine (pH 8.5)?

A

Intestine because its more basic and deprotonates the drug making it neutral and able to be absorbed.

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29
Q

Why is it beneficial for a drug to not cross a membrane? Think of inhalers.

A

You inhale the drug into your lungs, so you want the drug to be charged so that it stays in the lungs instead of being absorbed.

30
Q

Ion Trapping

A

Drug molecules tend to accumulate where the pH most favors ionization. They get stuck on one side.

31
Q

How would you change the urine pH to increase excretion of acidic drugs like aspirin?

A

You would increase pH to make more basic to make them charged so they are excreted instead of reabsorbed.

32
Q

What is partition coefficient?

A

Can be used to determine where a drug will go in the body

33
Q

Drugs with partition coefficient greater than 1

A

Diffuses through cell membranes easily and is likely to be found in all 3 fluid compartments

34
Q

Drugs with partition coefficient less than 1

A

Fairly water-soluble so they are often unable to cross and require more time to distribute throughout the rest of the body

35
Q

Atenolol is hydrophilic, and propranolol is lipophilic. If a patient is experiencing CNS side effects such as nightmares, which drug is better to use?

A

Atenolol because it is hydrophilic so it is polar so it has a harder time going across the blood-brain barrier to affect the CNS

36
Q

What is an inducer?

A

A drug that increases the rate of another drug’s metabolism which makes the drug excreted more, which lessens its effectiveness

37
Q

What is an inhibitor?

A

A drug that that decreases the rate of another drug’s metabolism which makes it accumulate more, which can lead to toxic levels in the body

38
Q

If clearance is high, is the half-life high or low?

A

Low

39
Q

Zero order kinetics

A

Constant amount per unit time is metabolized

40
Q

First order kinetics

A

Constant faction per unit time is metabolized

41
Q

Why can men metabolize alcohol more than women?

A

Women have almost no alcohol dehydrogenase enzyme which is what breaks down alcohol

42
Q

How does hepatitis affect drug metabolism?

A

Decreases metabolism

43
Q

How does nephritis affect drug excretion?

A

Decreases excretion

44
Q

What does it mean that enzymes are polymorphic?

A

Everyone has different enzymes to break down drugs, no two people are the same

45
Q

Pharmacogenomics

A

Study of how genes affect a person’s response to drugs

46
Q

ADRs

A

Adverse drug responses

47
Q

How can SNPs affect proteins?

A

They can be silent and keep it normal, or they can affect it so that is is low or nonfunctioning

48
Q

What is a normal protein called?

A

Wild type

49
Q

What mutation is a STOP?

A

Nonsense

50
Q

Intermediate metabolizer

A

Slower metabolism than normal, will require a lower dose because it is being broken down slower

51
Q

Poor metabolizer

A

Very low metabolic activity. Even small dose can be toxic because so little drug is being broken down

52
Q

Ultrarapid metabolizer

A

Very fast metabolism, will require higher dose because so much drug is being broken down very quickly

53
Q

When does a prodrug become active

A

After metabolism

54
Q

How does warfarin work?

A

Inhibits VKORC1 which leads to reduced amount of vitamin K available to serve as a cofactor for clotting proteins

55
Q

True or False? Most diseases are polygenic, perhaps requiring more than one target to be addresses.

A

True

56
Q

Biotechnology

A

The manipulation of natural biological processes to benefit society

57
Q

Plasmid

A

Small, circular piece of DNA that not only is separate from the chromosome, but can also replicate independently

58
Q

How can plasmids help us?

A

It is a way to easily get genes into bacteria by inserting gene into plasmid

59
Q

How do we copy and read DNA in biotech?

A

Transformation; insert recombinant plasmid into bacteria to create a transformed protein that does the function you need it to

60
Q

Why is the DNA code universal?

A

All living organisms use the same DNA and read their genes the same way. This is how we are able to use animals to help us

61
Q

How do we cut DNA?

A

Restriction enzymes: They cut DNA at specific places called recognition sites and form sticky ends

62
Q

What is the molecular paste that puts sticky ends back together?

A

DNA ligase: Forms bonds between the sugar and phosphate backbone of the DNA molecule

63
Q

How do you find the gene of interest?

A

Use nucleic acid hybridization

64
Q

Polymerase Chain Reaction (PCR)

A

DNA often needs to be amplified in order to have a large enough amount to study in detail. Uses primers to do this

65
Q

How do we measure DNA size?

A

Agarose gel electrophoresis

66
Q

When working with expression, what material do we use?

A

RNA

67
Q

Gene Therapy

A

Treatment of genetic disease by alteration of the affected person’s genotype, or the genotype of the affected cells

68
Q

What do iPS cells do?

A

Take skin cells and change them into stem cells which are then changed to neurons

69
Q

Transgenic Animal

A

Way to achieve large scale production of therapeutic proteins from animals for use in humans (milk)

70
Q

Gene Knockout

A

Disrupt a gene in the animal and then look at what functions are affected as a result of the loss of the gene

Year 3 (7 decks)

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