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Pharmacology I > Lecture 2/3 - Pharmacokinetics > Flashcards

Lecture 2/3 - Pharmacokinetics Flashcards

1
Q

What are the two methods of passive transport?

A

Channel mediated + Transporter mediated

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2
Q

What are three major components that go with carrier mediated transport?

A

Structure specific
Competition
Tmax

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3
Q

What are the two methods of carrier mediated methods?

A

Facilitated diffusion + Active transport

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4
Q

What is different about active transport compared to facilitated diffusion?

A

This method needs ATP in order to function

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5
Q

What is transcytosis?

A

Drug molecules + fluids are engulfed by the cell membrane and transported within the cell

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6
Q

What is the pH of most drugs given?

A

Weak acids or Weak bases

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7
Q

What is the most basic process that drugs undergo within the body ? (Hint: decides whether they are absorbed or not)

A

Ionization - phH dependent

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8
Q

What is the purpose of the Henderson-Hasselbach equation?

A

Tells you to what extent the drug is ionized within the body

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9
Q

What is A- form of the acid?

A

Ionized form

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10
Q

What is the HA form of the acid?

A

Unionized form

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11
Q

What is the B form of a base?

A

Unionized form

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12
Q

What is the BH+ form of a base?

A

Ionized form

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13
Q

What occurs to a weak acid within an acidic medium?

A

Less ionized
More lipid soluble
Rapidly absorbed

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14
Q

What occurs with a weak basic drug within basic medium?

A

Less ionized

Rapidly absorbed

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15
Q

What is an example, given in lecture, of an area with low pH?

A

The stomach (~2)

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16
Q

What is an example, given in lecture, of an area in the body with basic tendencies?

A

The intestines

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17
Q

What occurs when a basic drug is within an acid medium? What is this called?

A

Ionized and therefore will accumulate within the area. Known as ion trapping

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18
Q

What is the rule of thumb with both strong acids and bases within the body?

A

Always will be ionized within the body, so they are not lipid soluble meaning they will not undergo passive diffusion

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19
Q

What is the basic understanding of ion trapping?

A

Acids will be stuck in basic environments

Bases will be stuck in acidic environments

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20
Q

How do you make urine more acidic?

A

Ammonium chloride

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21
Q

How do you make urine more basic?

A

Sodium bicarbonate

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22
Q

What happens when you make urine more acidic?

A

Increase the elimination of bases via ion trapping

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23
Q

What happens when you make the urine more basic?

A

Increased elimination of acids, via ion trapping

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24
Q

What are the three types of active transport?

A

Uniport + Symport + Antiport

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25
Q

What is an example of a uniport given in lecture?

A

H+

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26
Q

What is an example of a symport given in lecture?

A

Glucose uptake

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27
Q

What is an example of an antiport given in the lecture?

A

Na/K ATPase

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28
Q

What is P-gp?

A

Permeability glycoprotein

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29
Q

What are two other names for P-gp?

A

MDRI
– or –
ABCBI

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30
Q

What is the function of P-gp?

A

Utilizes ATP to pump out a WIDE variety of drugs across both extra/intracellular membranes

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31
Q

Where is P-gp located?

A

Pretty much everywhere, important to know it is found in the BBB

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32
Q

What is absorption in regards to a drug?

A

Process where drug gains entry into body fluids (normally blood) and moves throughout the organism

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33
Q

What are seven things that tend to affect absorption?

A

Solubilty + Dissolution + Concentration + Blood flow + SA + pH + Contact time

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34
Q

What is bioavailability?

A

Amount of active drug available at the site of action

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35
Q

What four things play a role in bioavailability?

A

Decomposition of drug in intestines
Degree of absorption
Metabolism in wall of gut or liver
Transport of drug back into lumen via P-gp

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36
Q

What is the first pass effect?

A

Initial metabolism of drug, occurs through wall of gut or liver

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37
Q

What is the most common method by which a drug is administered?

A

Per os (by mouth)

38
Q

What is the downside to a slow release formulation?

A

Absorption is irregular and erratic

39
Q

What are the disadvantages to per os method of drug administration?

A 
Destruction of drug due to low pH 
Gastric emptying time 
binding to food 
Metabolism by microbes 
Exposed to liver
40
Q

What does the process of drug distribution entail?

A

Movement of drug from systemic circulation to organs/tissues

41
Q

Where are the three popular sites in the body that drugs accumulate?

A

Fat + Tissues + Bone

42
Q

What affects do storage depots have on the drugs metabolism?

A

decrease plasma levels
– and –
prolong half lives

43
Q

Where are the five sites of exclusion?

A

CSF + Ocular + Endolymph + Fetal + Pleural

44
Q

What two components help define volume of distribution?

A

Plasma concentration of drug at time zero

Intravenous dose

45
Q

What is the standard plasma size of a 70kg dog?

A

3L

46
Q

What is the standard EC compartment size in a 70kg dog?

A

12 L

47
Q

What is the standard Total body water compartment in a 70kg dog?

A

41 L

48
Q

What does a large Vd mean?

A

The drug is either distributed extensively or has bound extensively to peripheral tissues

49
Q

What does a very low Vd mean?

A

Drug is mostly present in the plasma, very high plasma protein binding

50
Q

What are the characteristics of most active drugs?

A 
Lipid soluble 
Unionized at physiological pH 
Strongly bound to plasma proteins 
Not readily excreted by kidneys 
Remain in body for long periods of time
51
Q

What is the most basic thing that happens in phase II reactions?

A

Conjugation

52
Q

What is the most basic way to describe what occurs in a phase I reaction?

A

Modification of the molecule

53
Q

What commonly occurs within the phase I reaction?

A

Lipid soluble parent compound converted to more polar metabolites
Most commonly these are inactive and therefore excreted

54
Q

What does the phase I reaction do to the chemical structure of most drugs?

A

introduce or unmask functional groups (-OH, SH, NH2, etc)

55
Q

What are the two types of phase I reactions?

A

Non-microsomal + Microsomal

56
Q

Is phase I specific to certain compounds?

A

No, enzymes are focused on specific groups/bonds

57
Q

What are five enzymes that are examples of nonmicrosomal metabolism in phase I?

A

Esterases/amidases
Monoamine oxiidases
Alcohol/aldehyde dehydrogenases

58
Q

What is a Phase I microsomal reaction?

A

Drug oxidation via P450 (and other biological variations)

59
Q

How do microsomal reactions differ from non-microsomal Phase I reactions?

A

Induction + Inhibition can occur

60
Q

How is Phase II reactions similar to Phase I?

A

Not compound specific

61
Q

What type of reactions are Phase II reactions?

A

Synthetic

62
Q

What are the results of Phase II reactions?

A

Larger molecular weight
Increased polarity
Decreased biological activity

63
Q

What is the only microsomal Phase II reaction?

A

Glucuronidation (therefore it is inducible)

64
Q

What are the five major types of phase II reactions?

A 
Glucuronidation 
Acetylation 
Glutathione conjugation 
Glycine conjugation 
Sulfation
65
Q

What is the endogenous reactant in glucuronidation?

A

UDP glucuronic acid

66
Q

What is the transferase/location for glucuronidation?

A

UDP-glucuronosyltransferase

Microsomes

67
Q

What is the endogenous reactant for acetylation?

A

Acetyl-Coa

68
Q

What is the transferase/location for Actylation?

A

N-acetyltransferase

Cytosol

69
Q

What is the endogenous reactant for glutathione conjugation?

A

Glutathione (GSH)

70
Q

What is the transferase/location for glutathione conjugation?

A

GSH-S-transferase

Cytosol - Microsomes

71
Q

What is the endogenous reactant for glycine conjugation?

A

Glycine

72
Q

What is the transferase/location for glycine conjugation?

A

Acyl-CoA glycinetransferase

Mitochondria

73
Q

What is the endogenous reactant for sulfation?

A

Phosphoadenosyl phosphosulfate

74
Q

What is the transferase/location for sulfation?

A

Sulfotransferase (cytosol)

75
Q

What is the path for renal excretion of drugs and their metabolites?

A

Glomerular filtration
Active tubular secretion or reabsorption
Passive diffusion across tubular epithelium

76
Q

What does clearance pertain to?

A

The ability of the body to remove the drug

77
Q

What two things does clearance relate?

A

Rate of drug elimination + Plasma concentration

78
Q

What are the two phases of the two-compartment model?

A

Distribution + Elimination

79
Q

Why do you see initial rapid changes in the two compartment model graph?

A

Shows the time it takes for the drug to reach an equilibrium between the central compartment and the plasma space

80
Q

What order is the elimination phase in the two compartment model?

A

First-order, we know this because of it’s linear pattern

81
Q

What is used to get the elimination rate in the two compartment model?

A

K - aka the slope of the linear portion of the graph

82
Q

What on the graph of the two compartment model tells you Co? What does that mean?

A

Where the linear line intercepts the Y-axis, this gives you the plasma concentration of the drug at time zero.

83
Q

What is the most common order of elimination?

A

First-order

84
Q

What does first order elimination mean?

A

constant proportion of the drug is eliminated per unit time

85
Q

Why do you get first order elimination?

A

Elimination system is not saturated by the drug

86
Q

What does half life mean?

A

Time required to change amount of drug in body by one-half

87
Q

What are you assuming when you determine 1/2 life?

A

Body is single compartment
Size = Vd
Drug is distributed equally
Drug in plasma is in equillibrium w/ total volume

88
Q

What is zero order elimination?

A

The elimination system becomes saturated after a high dose of the drug, meaning only a constant amount can be eliminated per unit time

89
Q

What needs to be done to reach steady state with repeated administration?

A

Interval of time it takes to reach SS is equal to five half lives

90
Q

What is a loading dose?

A

Done for immediate therapeutic concentration

91
Q

What follows a loading dose?

A

Maintenance dose

92
Q

What are the three stages of Pharmacokinetics?

A

Absorption + Distribution + Elimination

Pharmacology I (21 decks)

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