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RUSVM Pharmacology I > Pharm I Exam I > Flashcards

Pharm I Exam I Flashcards

1
Q

What the drug does to the animal is referred to as:

A

Pharmacodynamics

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2
Q

What the animal does to the drug (the movement of drugs within the body) is referred to as:

A

Pharmacokinetics

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3
Q

T/F: IV administration of a drug is characterized by rapid onset and long duration

A

False

IV administration of a drug is characterized by rapid onset and short duration

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4
Q

Acidic drugs ionize in ______ environments

A

Acidic drugs ionize in basic environments

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5
Q

Basic drugs ionize in ______ environments

A

Basic drugs ionize in acidic environments

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6
Q

Does this graph represent a weak acid or a weak base?

A

Weak base

Weak bases are absorbed from an alkaline environment and sequestered in an acid medium

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7
Q

Does this graph represent a weak acid or a weak base?

A

Weak acid

Weak acids are absorbed from an acidic environment and sequestered in an alkaline medium

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8
Q

T/F: Facilitated diffusion is a carrier-mediated transport, moves with a concentration gradient, and requires energy for movement

A

False.

Facilitated diffusion is a carrier-mediated transport, moves with a concentration gradient, but does not require energy for movement

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9
Q

T/F: Active transport is a carrier-mediated transport, moves against a concentration gradient, and requires energy for movement

A

True

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10
Q

Do you care about this dog drawing?

A

No. No you don’t.

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11
Q

What is the rate-limiting barrier for absorption of drugs in the skin?

A

Stratum corneum

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12
Q

Transfer of drugs from the bloodstream to tissues around the body is referred to as:

A

Drug distribution

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13
Q

›Chemical alteration of a drug by different body tissues is referred to as:

A

Drug metabolism

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14
Q

›Most drugs are eliminated via the ________

A

›Most drugs are eliminated via the kidney

if a drug is very lipophilic it will be easily reabsorbed (and thus not eliminated)

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15
Q

›The _______ is the main organ for drug biotransformation

A

›The liver is the main organ for drug biotransformation

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16
Q

What does ADME stand for?

A
  • Absorption
  • Distribution
  • Metabolism
  • Excretion/Elimination
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17
Q

How do drugs get across cell membranes?

A
  • Passive diffusion
  • Facilitated diffusion
  • Active transport
  • Pinocytosis
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18
Q

What does pKa mean?

A

pH at which 50% is ionized and 50% nonionized

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19
Q

What percentage of the body is water?

A
  • ~57% of the body is water
    • 40% of that is intracellular
    • 13% is interstitial fluid
    • 4% is plasma
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20
Q

Weak acids bind to ________; Weak bases bind to _________

A

Weak acids bind to albumin; Weak bases bind to β globulins and glycoproteins

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21
Q

What are the two things that can happen to a drug when it is metabolized?

A

Bio-inactivation or bio-activation

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22
Q

What are Phase I reactions?

A
  • Nonsynthetic - produce more reactive molecules
    • Oxidative reactions
    • Reductive reactions
    • Hydrolytic reactions
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23
Q

Which phase reactions involve cytochrome p450 enzymes?

A

Phase 1

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24
Q

Name the 3 major enzyme inhibitors:

A

cimetidine, chloramphenicol, ketoconazole

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25
Q

What are the 2 main routes of drug excretion?

A

Renal & hepatic (biliary)

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26
Q

What is the primary method of renal excretion?

A

glomerular filtration

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27
Q

How does electric charge affect excretion?

A

›Large, negative charged drugs are repelled by negative charged basal cell membrane protein

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28
Q

How does protein binding affect excretion?

A

Protein-bound drugs can not be filtered, therefore can not be excreted

›Only unbound molecules can be filtered

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29
Q

What is beneficial about active tubular secretion?

A

›Ionized molecules can be transported

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30
Q

What type of drugs can be excreted in bile?

A

›Lipid soluble drugs with MW > 300 and a polar group attached are more easily excreted in the bile

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31
Q

What is enterohepatic recirculation?

A

Conjugates in bile are hydrolyzed in intestine, then the drug is absorbed again. This prolongs the drug’s residence time in body

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32
Q

What type of drugs undergo ion trapping in milk?

A

Weak bases

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33
Q

What is t1/2?

A

Half life – time it takes for drug concentration to decrease by 50% (for first order kinetics drugs)

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34
Q

What is bioavailability?

A

The amount of a drug that gets into systemic circulation

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35
Q

In order for 2 drugs to be bioequivalent, they must have what 3 things in common?

A

AUC, Cmax, Tmax

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36
Q

If you double the dose of a drug, how much longer will it stay in the body?

A

1 more half-life

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37
Q

What is the equation for volume of distribution?

A

Vd = Q/Cp

Q = dose

Cp = plasma drug concentration (mg/mL)

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38
Q

What does it mean if a drug has a large Vd?

A

A large Vd means that the drug is distributed somewhere outside of the bloodstream (usually fat) and is unavailable

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39
Q

What does it mean if a drug has a small Vd?

A

A small Vd means that the drug is not being saturated to all tissues of the body (Vd < 1L)

Drugs that remain mostly in plasma with have a low Vd

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40
Q

What are different types of drug effects?

A

Therapeutic, side effect, adverse effect, toxic effect

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41
Q

A ________ is anything that binds to a recognition site

A

A ligand is anything that binds to a recognition site

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42
Q

What is a pro-drug? Give an example.

A

the ‘drug’ needs to be metabolized to be active

enalapril –> converted to enalaprilat in the liver

43
Q

What is the difference between an ionotropic and metabotropic receptor?

A
  • Ionotropic – binding of the drug prevents/allows ions passing through – fast neurotransmission (nicotinic)
  • Metabotropic – (G-protein receptors) - transduce an extracellular signal to an intracellular one; slow secretory and smooth muscle receptors (muscarinic, Ach, histamine)
44
Q

A(n) ________ mimics the effect of an endogenous ligand

A

An agonist mimics the effect of an endogenous ligand

(can be full, partial, inverse)

45
Q

What is an antagonist?

A

Binds to the receptor but (in theory) does nothing on its own, however it prevents an agonist from binding and thus blocks effects of the receptor

46
Q

What is a mixed agonist-antagonist

A

Acts as an agonist in one type of receptors and as an antagonist on other type of receptors

47
Q

An agent used to enhance renal excretion of weak base drug:

A

ammonium chloride

48
Q

An agent used to enhance renal excretion of weak acid drug:

A

sodium bicarbonate

49
Q

T/F: All ganglionic synapses utilize acetylcholine

A

True

50
Q

_____________ are enzymes that break down acetylcholine and are important in stopping the stimulation of the post- synaptic nerve

A

Cholinesterases are enzymes that break down acetylcholine and are important in stopping the stimulation of the post- synaptic nerve.

They are membrane bound enzymes that bind acetylcholine and break it into choline and acetate which can then be recycled into more acetylcholine.

51
Q

Mean Residence Time, which describes the length of drug persistence in the body, is utilized in which type of compartment model?

A

non-compartment model

52
Q

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An Alkaloid is derived from which of the following?<!--EndFragment-->

  1. Plant
  2. Animal
  3. Bacteria
  4. Fungi
A

Plant

53
Q

All of the following are properties of active transport across biological membranes EXCEPT

  • It requires cellular energy
  • It needs a carrier protein molecule
  • It moves against concentration gradient
  • It is generally specific
  • It is not a saturable process
A

It is not a saturable process

54
Q

Biotransformation of drugs is increased by the following EXCEPT

  • Distribution
  • Lipid solubility
  • Oral administration
  • Enzyme induction
  • Decreasing the dose
A

Distribution

55
Q

Which of the following statements concerning plasma protein binding is true?

  • It is increased in the neonate
  • It increases the volume of distribution
  • Extensive protein-binding (> 80%) increases half-life
  • It increases systemic bioavailability
  • It is an irreversible process
A

Extensive protein-binding (> 80%) increases half-life

56
Q

A competitive pharmacological antagonist is

  • a drug that binds irreversibly with the receptor
  • a drug that has affinity and intrensic activity
  • a drug that can be displaced by the agonist from the receptor
  • a drug that alters the structure of the agonist
  • a drug that has affinity but small efficacy
A

a drug that can be displaced by the agonist from the receptor

57
Q

Which type of drug transport is not concentration dependent?

  • Pinocytosis
  • Simple diffusion
  • Facilitated diffusion
  • Active transport
  • B & C
A

Pinocytosis

58
Q

What is correct regarding the blood-brain barrier?

  • Water soluble drugs cannot cross.
  • It does not require the use of carrier proteins for transportation of drugs.
  • Meningitis decreases the rate of penetration.
  • Lipid soluble drugs cannot penetrate.
  • It is not susceptible in the newborn.
A

What is correct regarding the blood-brain barrier?

  • Water soluble drugs cannot cross.
  • It does not require the use of carrier proteins for transportation of drugs.
  • Meningitis decreases the rate of penetration.
  • Lipid soluble drugs cannot penetrate.
  • It is not susceptible in the newborn.
59
Q

Plasma protein binding:

  • Decreases the half-life of the drug.
  • Generally is not reversible.
  • Acidic drugs bind mainly to glycoproteins and lipoproteins
  • Basic drugs bind mainly to albumin
  • The bound form is inactive, not distributed, metabolized or excreted by glomerular filtration.
A

**The bound form is inactive, not distributed, metabolized or excreted by glomerular filtration. **

60
Q

The doctor orders an IV medication to run over 5 hours. It comes in a 1L bag of 0.9% sodium chloride. The medication contains metoclopramide 6mg/2mL. The drop factor is 15gtts/mL. How many mL/hr should we infuse?

  • 40mL/hr
  • 55mL/hr
  • 180mL/hr
  • 250mL/hr
  • 200mL/hr
A

200mL/hr

61
Q

T/F: Cats are deficient in glucuronyl transferase

A

True

62
Q

T/F: Older animals tend to have reduced cardiac output and hepatic blood flow, which could affect dosage of and response to a drug

A

True

63
Q

T/F: The BBB in younger animals tends to have a lower permeability than in older animals

A

False – Young animals have increased BBB permeability

64
Q

T/F: Idiosyncrasy of a drug is dependent on the dose administered to an animal

A

False – Not dependent on the dose

65
Q

Are NSAIDs an example of weak acid drugs or weak base drugs?

A

Weak acids

66
Q

When one drug reduces the concentration of the other at its site by interfering with ADME process, this is called:

A

Pharmacokinetic antagonism

67
Q

T/F: The higher the lipid solubility of a drug, the faster it crosses cell membranes

A

True

68
Q

Birds lack oxidative enzymes and are the ONLY animals to use ________ as conjugation substance

A

Birds lack oxidative enzymes and are the ONLY animals to use ornithine as conjugation substance

69
Q

The volume of distribution (Vd) of a drug is higher when the drug is:

  • a strong acid
  • a weak acid with a low pka value
  • a weak acid with a high pka value
  • a weak base with a low pka value
  • a weak base with a high pka value
A

a weak base with a low pka value

70
Q

Phenylbutazone, a weak acid/enzyme inducer:

  • is excreted in milk in relatively high concentration
  • its distribution is decreased in systemic acidosis
  • is rapidly excreted in urine in dogs
  • its renal excretion is enhanced by administration of ammonium chloride
  • its renal excretion is enhanced by administration of sodium bicarbonate
A

its renal excretion is enhanced by administration of sodium bicarbonate

71
Q

______ is the plasma concentration of the drug when the maintenance rate of the drug administered is equal to the rate of elimination.

A

Steady-state plasma concentration (Cpss)

72
Q

Diffusion of most drugs across a membrane is mostly dependent upon what?

A

Blood flow

73
Q

___________ is an acute form of tolerance

A

Tachyphylaxis

74
Q

Which route of administration bypasses the absorption process?

A

IV (intravenous)

The “absorption” phase is the time it takes to inject the drug. Usually IV injections are made quickly so that the plasma concentration reaches an almost instantaneous peak and rapidly declines as the drug is distributed to other tissues

75
Q

What is the most important factor involved with drug absorption for oral medications?

A

Surface area of the gut available for absorption

(diseases like gastroenteritis, neoplastic infiltration, or villus atrophy can significantly change the surface area)

76
Q

In cows with mastitis, the usual route of drug administration is _____________

A

In cows with mastitis, the usual route of drug administration is intramammary

77
Q

T/F: Drugs that are not in solution or some sort of emulsion are safe to be given intravenously

A

False!

78
Q

What is the pH of plasma?

A

7.4

79
Q

What is the pH of gastric contents?

A

2

80
Q

T/F: Only the ionized form of a drug can cross cell membranes

A

False.

Only the un-ionized form of a drug can cross the cell membrane. It will diffuse down the concentration gradient to the other side of the membrane where most of it will become ionized (and thus trapped)

81
Q

T/F: P-glycoprotein is an important protein present in cell membranes that pumps foreign substances out of cells. However, it is not present in the BBB

A

False.

P-glycoprotein is an important protein present in cell membranes that pumps forwign substances out of cells. It is present in the BBB

82
Q

Metabolism usually inactivates a drug. The exception to this is:

A

prodrugs

need to be metabolized to become active

83
Q

What is the most common metabolic phase II reaction?

A

glucuronidation

Catalyzed by glucuronyl transferase (except in cats, who lack this enzyme); acetylation of acetyl CoA; and methylation by S adenosyl methionine

84
Q

_________ receptors act to alter gene transcription and thus protein production

A

nuclear receptors act to alter gene transcription and thus protein production

85
Q

The ________ is the concentration at which a drug produces 50% of its maximal effect

A

EC50

This only applies to in vitro preparations.

Just a heads up: EC50 and ED50 are NOT the same thing. ED50 is the dose at which a drug produces a quantal response in 50% of animals

86
Q

The _______ is the dose that kills 50% of animals

A

The LD50 is the dose that kills 50% of animals

87
Q

This is not a question, but just remember that in zero-order kinetics, a certain amount of drug is eliminated per time, regardless of what the drug concentration is. When plotted out, you would get a straight line

A
88
Q

As Vd increases, t1/2 __________

A

As Vd increases, t1/2​ increases

89
Q

As Vd decreases, t1/2​ __________

A

As Vd decreases, t1/2​ decreases

90
Q

As Clearance increases, t1/2​ __________

A

As Clearance increases, t1/2​ decreases

91
Q

As Clearance decreases, t1/2​ __________

A

As Clearance decreases, t1/2​ increases

92
Q

Which of the following agents can be used to enhance renal excretion of aspirin, a weak acidic drug, in cats?

  • atropine
  • ammonium chloride
  • epinephrine
  • sodium bicarbonate
  • methionine
A

sodium bicarbonate

93
Q

T/F: A drug’s volume of distribution (Vd) is a good indication for the ability of drug to diffuse across membranes.

A

True

94
Q

T/F: If the intravenous infusion rate is doubled, the time needed to achieve a steady-state plasma concentration is doubled.

A

False

95
Q

T/F: For most drugs, the half-life (t1/2) depends on the dose of drug administered.

A

False

96
Q

T/F: The MOST common biotransformation reaction is oxidation.

A

True

97
Q

T/F: Facilitated diffusion of drugs is a carrier-mediated transport that requires energy

A

False

does not require energy

98
Q

T/F: Generally, drugs that bind extensively to plasma protein tend to have short half-lives

A

False

99
Q

Which of the following is the rate-limiting step that controls the rate of absorption of a solid drug given orally?

  • a - dissolution
  • b - lipid solubility
  • c - degree of ionization
  • d - stability
A

c - degree of ionization

100
Q

A drug that counters the effect of another drug by binding to different receptors and causing opposing effects is called:

A

noncompetitive antagonist

101
Q

T/F: Urinary acidification increases the excretion rate of NSAIDs such as aspirin

A

False

102
Q

T/F: The volume of distribution (Vd) of a drug can be used to calculate the amount of drug needed to achieve a desired plasma concentration.

A

True

103
Q

A drug with a half-life of 8 hours is administered by continuous intravenous infusion. How long approximately will it take for the drug to reach its desirable steady-state level?

  • 10 hours
  • 20 hours
  • 30 hours
  • 40 hours
A

40 hours

104
Q

Which of the following is a phase I drug-metabolizing reaction?

  • glucuronidation
  • acetylation
  • sulfation
  • hydroxylation
A

hydroxylation

RUSVM Pharmacology I (4 decks)

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