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Medical Pharmacology Exam 1 > Introduction > Flashcards

Introduction Flashcards

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USMLE® Step 1 flashcards
1
Q

Proadifen and cimetidine are significant and related to each other because _. What class of antibiotics have the same effect?

A

They inhibit drug metabolism

Macrolide antibiotics

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2
Q

Ethanol, phenobarbitol and phentoin are drugs that are significant and related to one another because _. What other agric, product has the same effect?

A

The enhance / activate drug metabolism.

DDT

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3
Q

The mechanism of action of probenecid is _

A

It competitively inhibits organic anion transporter

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4
Q

The mechanims of action of cimetidine is _

A

It competitively inhibits organic cation transporter

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5
Q

Endobiotics and xenobiotics differ because _

A

Endobiotics and endogenously produced chemicals while xenobiotics are from exogenous sources

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6
Q

The law that required labeling of all active ingredients was _

A

The pure food and drug act of 1906

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7
Q

The harrison narcotics act of 1914 did what?

A

Restricted the sale of addictive drugs

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8
Q

What were the 2 goals of the food, drug and cosmetic act of 1938?

A
  • Labeling of inactive ingredients

- Documentation of product safety

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9
Q

The Durham-Humphrey amendment to the food and drug act did what?

A

Split drugs into legend (prescription) and non-prescription

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10
Q

What was the amendment to the food, drug and cosmetic act that required documentation of drug efficacy?

A

The Kefauver-Harris amendment

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11
Q

The law that created the DEA, and restricted the manufacture and distribution of controlled substances was _

A

The controlled substances act

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12
Q

Schedule 1 drugs include heroin, marijuana and LSD. These are all drugs described as _

A

Having no medical use

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13
Q

What is the goal of phase 1 studies? Who are the subjects?

A

Establish initial dose and safety

Healthy volunteers

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14
Q

What is the goal of phase 2 studies (2)? Who are the subjects?

A

Establish efficacy in treating disease and effective dose

Potential patients

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15
Q

What is the goal of phase 3 studies? Who are the subjects?

A

Compare versus established treatment protocol

Potential patients

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16
Q

What is an NDA regarding drug development?

A

New drug application, phase 4 which is post market monitoring

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17
Q

What is a category 1 OTC?

A

Both safe and effective

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18
Q

What is a category 2 OTC?

A

Not safe, not effective or both

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19
Q

What is a category 3 OTC?

A

Data on safety or efficacy inconclusive

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20
Q

What law accomplished the following:-

  • Vitamins, minerals, herbals, etc are no longer approved / regulated by FDA
  • No company responsibility for ensuring effectiveness
  • Ensuring safety is manufacturer’s responsibility
A

The dietary supplement health and education act of 1994

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21
Q

What are the 2 sources of technical information about drugs from the manufacturer?

A

Package inserts

Physician’s desk reference

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22
Q

What are the 3 sources of technical information about drugs not from the namufacturer?

A

American hospital formulary service
US Pharmacopeia Dispensing Information
AMA Drug Evaluations

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23
Q

Regarding pharmacology, ADME stands for _. This is related to pharmacokinetics or pharmacodynamics?

A 
Absorption
Distribution
Metabolism 
Elimination 
Pharmacokinetics
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24
Q

Understanding what the body does to a consumed drug is referred to as _

A

Pharmacokinetics

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25
Q

Understanding what a consumed drug does to the body is referred to as _

A

Pharmacodynamics

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26
Q

Enteral administration refers to any administration via _. Three types of enteral administration are _

A

Any thing via GI

Oral, rectal, sublingual

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27
Q

Any drug administration that requires the use of a needle is referred to as _

A

Parenteral administration

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28
Q

What is the difference between topical and transdermal application?

A

The intended site of action. Topical has intended site of action of skin, while transdermal is going through skin to get to intended site of action

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29
Q

How would you have to administer a drug so that it avoids the liver before getting to the right heart, lungs and left heart?

A

Intravenous administration

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30
Q

What is referred to as “complex formation in the GI tract”?

A

This is when drugs are administered orally, they can form new compounds in the GI tract that affect drug absorption e.g. binding calcium, food, etc

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31
Q

What is the first pass effect?

A

This accounts for the fact that many drugs are metabolized by the liver upon their “first pass through”, therefore that has to be accounted for when choosing a route of administration

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32
Q

What is an enteral route of admin that completely bypasses the first pass effect? What enteral route reduces it?

A

Bypasses - sublingual

Reduces - Rectal

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33
Q

What are 2 routes of admin most commonly used for administration of proteins / peptides? What is a consideration with these routes?

A

SubQ or IM

Activities / surroundings can alter absorption (e.g. cold leading to vasoconstriction)

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34
Q

What is a route of administration that has the advantage of very well controlled rate of admin as well as rapid onset of action, and knowing the entire dose enters the blood?

A

IV

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35
Q

If you wanted to administer a very high dose of drug to a specific organ, what is a route of admin to take? What is the danger?

A

Intra-arterial

Hemorrhage

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36
Q

The best way to get a high dose of drug directly into the CNS is via _ admin

A

Intraspinal

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37
Q

An advantage of topical administration regarding side effects is _. Under what conditions might this advantage be moot?

A

Local effects, minimal systemic effects

Use too much drug, then some gets into blood stream, now have systemic effects

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38
Q

The options are arteries, arterioles, capillaries, venules and veins. The majority of drug absorption occurs across _. Why?

A

Capillaries

Have the thinnest walls

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39
Q

Biomembranes can be considered as lipoprotein barriers

containing small pores. What type of transport depends mainly on lipid solubility of the drug in question?

A

Passive diffusion

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40
Q

What is the major difference between active and facilitated diffusion? What is the main similarity?

A

Difference - Active is coupled to an energy source, facilitated is not directly coupled to an energy source
Similarity - Both require the use of channels

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41
Q

Movement of drugs between cells (vs. through cells) refers to what type of transport?

A

Aqueous diffusion

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42
Q

The type of transport that can be used to highly concentrate a drug in a compartment regardless of its concentration gradient is _

A

Active diffusion

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43
Q

What is the major requirement for pinocytosis / exocytosis to work?

A

The molecule has to be large enough to be recognized by the cell

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44
Q

Between the ionized and non-ionized form of a drug, which is more likely to be able to cross a lipid barrier? Which is more likely to be water soluble?

A

Cross barrier - non-ionized

Water soluble - Ionized

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45
Q

pH = pKa + log ([ionized]/[non-ionized]). This represents the equation for acids or for bases?

A

Acids

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46
Q

pH = pKa + log ([non-ionized]/[ionized]). This represents the equation for acids or for bases?

A

Bases

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47
Q

What is the definition of the pKa?

A

The pH at which the ratio of ionized to non-ionized form of a drug is equal to 1

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48
Q

Consider the ionized and the non ionized form of an acid. What is happening to these 2 elements as you increase the pH of a solution?

A

Know that the ionized form of the acid is A-, non ionized is HA. As the pH goes up, more free H+, therefore more free A-, therefore as pH increases, more ionized acid

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49
Q

Consider the ionized and the non ionized form of a base. What is happening to these 2 elements as you increase the pH of a solution?

A

Know that ionized form of the base is BH+. Therefore as pH goes up (more free H+), that means you’ll have more free B. Therefore as pH goes up, less ionized form is present in solution.

50
Q

For thinking about the henderson hassellbach, know that for the equations, it is A- and B. Think that the what makes it an acid is that it is able to donate a proton, while a base is able to accept a proton

A

HA H+ and A-

B and H+ BH+

51
Q

For weak organic acids, what are the 2 functional groups that are able to donate a proton? What is the main functional group of the base that make it able to accept a proton?

A

Acids - COOH and OH (Become COO- and O-)

Base - NH2, (become NH3+)

52
Q

Can you draw the graphical form of the henderson hasselbach equation?

A

See ppt. pg 21

53
Q

What is the pH partition hypothesis?

A

For Weak Organic Acids or Weak Organic Bases, the Non-Ionized, more Lipid-Soluble form crosses biomembranes much more readily than does the Ionized,
more Water-Soluble form*

54
Q

For a lumen pH of 1.4 and a pKa of 3.4, calculate the ratio of ionized to non-ionized aspirin, a weak organic acid

A

pH = pKa + log [i]/[ni]
1.4 = 3.4 + log [i]/[ni]
log [i]/[ni] = 1.4 – 3.4 = –2
[i]/[ni] = 10–2 = 1/100

55
Q

For a plasma pH of 7.4 and a pKa of 3.4, calculate the ratio of ionized to non-ionized aspirin, a weak organic acid

A

pH = pKa + log [i]/[ni]
7.4 = 3.4 + log [i]/[ni]
log [i]/[ni] = 7.4 – 3.4 = 4
[i]/[ni] = 104 = 10000/1

56
Q

Both active transport and facilitated diffusion rely on channels. What is the major difference between the 2?

A

Facilitated diffusion uses no energy, transports substrates from areas of high to low concentration

57
Q

Glucose, some amino acids and ion transporters work by _ type of transport

A

Facilitated diffusion

58
Q

What are the 2 types of active transport transporters mentioned in the notes? What is the major difference regarding their energy source?

A

MDR / MDP - has ATPase activity

SLC - indirect energy source

59
Q

There are 2 examples of active transport receptors provided. Which is most likely to be an antiporter protein?

A

The SLC, it uses existing gradient to transport its substrates

60
Q

Majority of drug transport occurs using what type of transporter?

A

ABC transporters

61
Q

The blood brain barrier is very tight. What is a means which this structure can be circumvented as discussed in this class?

A

Drug transporters

62
Q

Generally speaking, between the SLCs and the ABC type pumps, which is likely to be an influx pump (into cell) and which is likely to be an efflux pump?

A

ABC - efflux, think drug resistance

SLC - Influx pump

63
Q

Diffusion that occurs between cells via channels is called _

A

Aqueous diffusion

64
Q

How do increased gastric emptying time, decreased intestinal transit time and binding to drugs to mucus or food affect absorbtion?

A

Reduce it

65
Q

Where is a drug most likely to accumulate, in a compartment with or without receptors?

A

In a compartment without receptors

66
Q

What role does the presence of drug receptors have on if a drug will accumulate in a compartment?

A

None, its is mainly an issue to transporters / permeability

67
Q

What types of molecules are most likely to accumulate in the brain and adipose tissue?

A

Non-polar drugs

68
Q

If you were to graph the concentration of free drug in plasma of a drug that could bind plasma proteins, at what point will the rate of increase of free drug markedly change?

A

At the point when the plasma proteins are saturated, more drug added to the system will increase plasma concentrations more than before saturation

69
Q

What kind of effects can be observed when 2 drugs compete for binding on plasma proteins?

A

increased biologic effects, metabolism and toxicity

70
Q

Tight junctions that form the blood brain barrier are formed between what type of cell? Selective permeability of the BBB means that _ soluble drugs are more likely to end up in the brain

A

Endothelial cells

Lipid soluble

71
Q

Which is more restrictive, the blood BB or the blood-placenta barrier?

A

BBB

72
Q

What is the difference between a quantal drug response and a graded drug response?

A

Quantal - All or nothing

Graded - A continuous range of possibilities

73
Q

A dose response curve may be plotted of quantal responses, paradoxical as that may seem. What change has to be made to the graph variable for this to be possible?

A

The Y axis that to now plot responders within a POPULATION

74
Q

an ED50 and a TD50 is common to both a graded and quantal dose response curve. Which of the two types of responses can also be used to generate LD50 data?

A

Quantal dose response curve of entire population. Hard to calculate dose that kills 50% of a population of 1 (graded curve)

75
Q

What is the Emax of a dose response curve? For a single drug, what is the main determinant of Emax?

A

The maximal effect that can be elicited in response to a drug
The number of receptors engaged

76
Q

Changes in efficacy are reflected by curves that shift along the _ axis, while changes in potency are reflected by curves that shift along the _ axis

A

Efficacy is Y axis (Think Emax)

Potency is X axis (Think different ED50s)

77
Q

What is a potency ratio?

A

A ratio of the ED50s of 2 drugs

78
Q

What is a therapeutic index?

A

A measure of how far apart the ED and LD 50 curves are

79
Q

Both an agonist and an antagonist bind the receptor. What differentiates them? While an agonist will likely have a sigmodal curve, what is the shape of an antagonist curve?

A

Agonist elicits an effect, while the antagonist has no effect by itself
Flat line

80
Q

What is intrinsic efficacy?

A

The ability of an individual drug to generate a response, regardless of whether it is a full or partial agonist

81
Q

What is an inverse agonist? What condition has to be met for you to observe the effects of an inverse agonist?

A

It is a molecule that is able to reduce receptor activity below basal levels
You need to have some basal receptor activity that the inverse agonist can reduce

82
Q

In terms of Emax and ED50, what effect does a competitive antagonist have on those parameters?

A

A competitive antagonist will change the ED50 (more agonist needed for same effect) but won’t change the Emax since you can outcompete it with enough agonist

83
Q

In terms of Emax and ED50, what effect does a non- competitive antagonist have on those parameters?

A

A non-competitive antagonist will change the Emax (will reduce the max effect) but will not change the ED50

84
Q

In what conditions can a partial agonist be used as an antagonist?

A

When a partial agonist is mixed with an agonist, it will reduce the number of receptors activated to the max, therefore acting as an antagonist

85
Q

Why do the effect of non-competitive antagonists take longer to reverse?

A

They work by covalent binding to the receptor, therefore usually require new receptor synthesis

86
Q

What is a chemical antagonist?

A

An antagonist that exerts its effects by directly modifying the agonist in question, vs by acting at the receptor

87
Q

What is a physiological antagonist?

A

An antagonist that acts at a receptor exerting an opposite effect of the agonist

88
Q

What is the difference between a selective and a specific drug?

A

Selective - can bind many receptors, has a preference

Specific - Interacts with only one receptor subtype

89
Q

What is an idiosyncratic drug response?

A

An unusual / atypical response to the drug, usually occurs in a small subset of the population

90
Q

Arrange in order of increasing severity: Toxic effect, side effect, adverse effect

A

Side effect - minor, undesired
Adverse effect - major, serious medical consequence
Toxic effect - very serious adverse effect

91
Q

What are the 4 basic sources of side effects?

A

Chemical property of drug
Drug acting at multiple receptors
Drug acting at many subtypes of receptors
Drug acting at receptor in unintended tissue

92
Q

What are the 3 mechanism by which drug actions are stopped? Which is responsible for stopping majority of drug actions?

A

Redistribution
Biotransformation (Majority)
Excretion

93
Q

What are the 2 goals of biotransformation reactions?

A

make compounds more hydrophillic

Make compounds less pharmacologically active (usually)

94
Q

What are the functional groups that are either unmasked or introduced in phase 1 reactions?

A

Unmasked - NH2 and SH

Introduced - OH

95
Q

What are the 3 reaction classes for phase 1 reactions? Which is most prevalent?

A

Oxidation (most prevalent)
Reduction
Hydrolysis

96
Q

What are the enzymes responsible for the majority of phase 1 oxidation reactions? What are 2 other names?

A

CYPs
MFOs (mixed function oxidases)
Liver / hepatic oxidases

97
Q

Beyond the CYPs, what other oxidases are important in metabolism?

A

MAO-A and MAO-B

98
Q

What enzymes carry out reduction reactions? What enzymes carry out hydrolysis (2)

A

Reductions - oxidoreductase

Hydrolysis - Plasma and acetyl - cholinesterases

99
Q

Where are you most likely to find acetyl cholinesterase? What type of compound is the substrate for plasma cholinesterase?

A

The synaptic cleft of cholinergic synapses

Ester drugs

100
Q

How many steps / reactions are involved in the Phase 1 reactions? What is the main co-factor of the first reaction?

A

2 reactions

NADPH is required for the first reaction

101
Q

Which reaction in the series of phase 1 reactions is catalyzed by CYPs? What are the 2 flavoproteins usually involved in this reaction?

A

Catalyzes reaction 2

FAD and FMN

102
Q

What is the goal of phase 2 reactions? What are the 4 examples of substrates that can be added during this phase?

A

Add an endogenous polar substance to the substrate

  • glucuronic acid
  • sulfate
  • amino acid
  • glutathione (GSH)
103
Q

WHat are the class of enzymes that catalze the phase 2 reactions? What are the 5 examples provided and which is most common?

A 
Transferases 
Glucuronyl transferase (most common)
Sulfotransferase
COMT
Acetyltransferase 
Glutathione Transferase
104
Q

How many steps are involved in Phase 2 reactions? What step is usually catalyzed by the transferases?

A

2 reactions

Transferases catalyze step 2

105
Q

The first reaction of the phase 2 reactions usually generates a substrate required in subsequent steps. What is this substrate in for the glucuronyl transferases (UGTs)? What about for the sulfotransferases (STs)?

A

UGTs - UDP-alpha-glucuronic acid (UDPGA)

STs - 3 phosphoadenosine-5-phosphosulfate (PAPS)

106
Q

What us the difference between an active metabolite and a reactive metabolite?

A

Active - drug metabolite with more activity than parent compound
Reactive - drug metabolite that is toxic produced from relatively inert precursor

107
Q

What is the only known role of proadifen?

A

It is an inhibitor of drug metabolism

108
Q

What are 3 drugs provided as examples of metabolic enzyme activators? What are 2 other non-drugs with the same effect?

A

Drugs - Ethanol, phenobarbital, phenytoin

Others - Pesticides, DDT

109
Q

How does hepatic disease affect metabolism and duration of action?

A

Decreased metabolism and increased duration of action

110
Q

What are the 4 major routes of administration provided?

A

Kidney
Liver
GI
Lungs

111
Q

What is the primary means for reducing drug concentration in tissues and thus in terminating drug action?

A

Excretion

112
Q

What are the 3 processes involved in drug excretion?

A

Filtration
Passive diffusion
Active secretion

113
Q

What is the main site of filtration? What are 2 limitations?

A

Glomerulus in kidney

Size and binding to protein

114
Q

What are 2 mechanisms to increase filtration?

A

Increase urinary volume

Increase blood flow to the kidneys

115
Q

What can occur to non-ionized lipophillic drugs in the renal tubule?

A

Can be reabsorbed from the tubule lumen into plasma

116
Q

What is the major determinant of whether weak organic acids or bases diffuse across the lumen? What are 2 drugs that can modify this?

A

pH in the various partitions
Ascorbic acid can acidify the lumen
Sodium bicarb can make the lumen more basic

117
Q

What are 2 of the major transporter systems in the renal tubule for transporting ions? What are their substrates (3) and (1)?

A

OAT - acids, glucuronide conjugates, sulfate conjugates (negatively charged)

OCT - bases

118
Q

What is the drug that is known to be a competitive inhibitor of the OAT? What about the OCT?

A

OAT - Probenecid

OCT - Cimetidine

119
Q

Which is able to filter larger substances, the liver or kidneys? What are 3 transporters found in the liver?

A

Kidney filters larger substances

OCTs, MRPs, OATs

120
Q

What is the enterohepatic circulation? What is the source of enzymes that makes this possible?

A

A metabolized drug may become “unmetabolized” as it transverses the GI, allowing its reabsorption
Enteric bacteria

Medical Pharmacology Exam 1 (15 decks)

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