The billion dollar pill Flashcards

1
Q

What are agonist drugs?

A

Drugs that stimulate biological responses

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2
Q

What are antagonist drugs?

A

Drugs that inhibit biological responses.

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3
Q

What are the 3 tenets of pharmaceutical science?

A
  1. All drugs must bind to a biological target in order to achieve a desired biological effect.
  2. Magnitude of the response depends on the dose.
  3. Every drug is a potential poison.
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4
Q

What are the general biological targets of a drug?

A
  1. Targets that are overexpressed.
  2. Targets that are underexpressed.
  3. Targets that control a critical process that affects the biology that you are trying to manipulate.
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5
Q

What is the largest class of drug targets?

A

Enzymes.

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6
Q

What are exogenous molecules?

A

Molecules originating from outside the organism

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7
Q

What is pharmacokinetics and pharmacodynamics?

A

pharmacokinetics: study of how the body affects the drug
Pharmacodynamics: study of how the drug affects the body

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8
Q

Where are HER2 receptors overexpressed?

A

on the cell surface of breast tumours

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9
Q

Why are enzymes the largest class of drug targets?

A

because of the presence of the active site, which can be exploited as binding sites for pharmaceutical enzyme inhibitors

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10
Q

How does potency relate to EC50?

A

higher potency = lower EC50

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11
Q

Why is higher potency of a drug sometimes bad?

A

the chance of the drug binding to other targets is higher, causing side effects

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12
Q

What are the 2 ways in which a drug can become a poison?

A
  1. Too much action on the target
  2. Loss of selectivity, where the drug binds to other targets
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13
Q

What is the first step in the process of drug discovery?

A

Identification and validation of a target.

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14
Q

What are the criteria for a good target?

A
  1. The target’s 3D structure is accessible
  2. Effects of altering the target is measurable
  3. It is not evenly distributed throughout the body
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15
Q

What are the criteria during target validation?

A
  1. Is the effect of the target reproducible?
  2. Can the target be modulated?
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16
Q

After identifying a target, how is the drug chosen?

A

Start with a endogenous molecule that is known to bind to the target and go from there

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17
Q

What is an endogenous molecule?

A

A molecule originating from inside the organism

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18
Q

What is a pharmacological assay?

A

An investigative procedure to measure the presence, amount or functional activity of a drug

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19
Q

What are the 4 processes of pharmacokinetics?

A
  1. Absorption
  2. Distribution
  3. Metabolism
  4. Elimination
20
Q

Why might drugs not be absorbed into the bloodstream?

A
  1. poor solubility
  2. degradation prior to absorption
  3. cannot be transported well across the cellular barrier
21
Q

What is paracellular transport?

A

Transport of molecules in between 2 cells

22
Q

How do you use logP to determine hydrophobicity?

A
  1. Negative log P = hydrophilic
  2. Positive log P = hydrophobic
23
Q

Why are some drugs taken with food or milk?

A
  1. They are poorly soluble in water, so the food/milk allows the drug to be absorbed into the bloodstream
  2. To delay the absorption of some drugs
24
Q

What is the bioavailability of a drug administered through IV injection? Why?

A

1
because there is no pre-absorption losses

25
Q

What is the first pass effect?

A

A phenomenon in which a drug gets metabolised at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the blood.

26
Q

Why are some drugs taken before meal?

A
  1. Food may inhibit metabolism of the drug
  2. Speeds up gastric emptying so there’s quicker exposure to the drug
27
Q

What is the most water soluble area of the body?

A

Blood

28
Q

What is the most lipid soluble area of the body?

A

bone marrow

29
Q

What does volume of distribution measure?

A

It approximates how well a drug binds to different tissues

30
Q

What are instances where a drug’s poor oral absorption is a good thing?

A

Poor absorption means the drug will stay in the gut longer, which is good if you want a localised effect in the gut

31
Q

What is the goal of metabolism?

A
  1. To convert a foreign substance into a more water soluble entity so that it can be readily excreted from the system
  2. To convert a substance into something less reactive so that it causes less harm to the system
32
Q

What happens if the metabolism of a drug is too fast or too slow?

A
  1. Too fast: The effect of the drug may be too little
  2. Too slow: The effect of the drug may become toxic
33
Q

What is biotransformation?

A

Chemical modification of the compound made by an organism usually through an enzymatic process

34
Q

What are xenobiotics?

A

Chemicals found in the body which are not normally produced or present within the organism

35
Q

What is bioactivation?

A

Enzymatic conversion of a substance into a reactive species

36
Q

What are the general characteristics of metabolism?

A
  1. It is an enzymatic process
  2. One enzyme can metabolise many subtrates
  3. Targets are mostly xenobiotics
  4. They exhibit genetic differences
37
Q

What are some organs that carry out metabolism?

A
  1. liver
  2. kidneys
  3. gastrointestinal mucosa
  4. skin
  5. lung
38
Q

What is the primary organ for metabolism?

A

Liver

39
Q

How are water soluble substances secreted?

A

Secreted by the kidneys in urine

40
Q

How are fat soluble substances secreted?

A

Secreted by liver into bile and then in faeces

41
Q

What is clearance?

A

It reflects the intrinsic ability of the body to clear the specific drug

42
Q

What is the main organ that eliminates drugs from the body?

A

Kidney

43
Q

What is enterohepatic recirculation and how is it significant?

A
  1. It is the process by which bile gets reabsorbed back into the blood from the small intestine
  2. It prolongs the half life of the drug
44
Q

What is bioavailability?

A

It provides an indication of the proportion of the
administered dose that will be taken into the circulatory system.

45
Q

What are the main categories of toxicity testing?

A
  1. general toxicity
  2. safety pharmacology
  3. developmental and reproductive toxicity
  4. immunotoxicity
  5. phototoxicity
  6. genotoxicity and carcinogenecity
46
Q

What are the limitations of toxicity testing?

A
  1. Many toxicities are hard to pick up from trials
  2. We do not fully understand the mechanism of toxicities
  3. All models are imperfect (computer based, animal models, human studies)