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Pcol > Unit 1: Nature of Drug > Flashcards

Unit 1: Nature of Drug Flashcards

1
Q

the science of drug preparation & the
medical uses of drugs

A

Materia medica

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2
Q

Receptors for which no ligand has been discovered & function can only be guessed

A

orphan receptors

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3
Q

short nucleotide chains that can interfere with the readout of genes & the transcription of RNA

A

Antisense Oligonucleotides (ANOs)

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4
Q

Body of knowledge concerned with the action of chemicals on biologic systems, especially by binding to regulatory molecules (receptors) and activating or inhibiting normal body processes

A

pharmacology

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5
Q

Area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans

A

medical pharmacology

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6
Q

Area of pharmacology concerned with the undesirable effects of chemicals on biologic systems

A

toxicology

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7
Q

Relation of the individual’s genetic makeup to his or her response to specific drugs (brought about by the exploration of the human gene)

A

pharmacogenomics

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8
Q

Any substance that brings about a change in biologic function through chemical actions

A

drug

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9
Q

Specific molecule in the biologic system that plays a regulatory role

A

receptor

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10
Q

Explains what the body will do with the drug (how the drug is handled by the patient)

A

pharmacokinetics

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11
Q

4 basic concepts of pharmacokinetics

A

absorption
distribution
metabolism
elimination

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12
Q

Explains what the drug does to the body

A

pharmacodynamics

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13
Q

Involves the follwing concepts: receptor, receptor sites, and inert binding sites

A

pharmacodynamics

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14
Q

T/F:
Drugs can produce effects in the body with or without binding sites.

A

false
Receptors (binding sites) are always required; no binding site = no effect in the body

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15
Q

T/F:
Drugs are made of chemical components similar to the human body: inorganic ions, nonpeptide organic molecules, small peptides and proteins, nucleic acids, lipids, and carbohydrates.

A

true

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16
Q

molecules or substances found in plants or animals, where many are partially or completely synthetic

A

hormones
xenobiotics (foreign substances that enter the body)

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17
Q

3 physical natures of drugs

A

solid (tablets, granules)
liquid (syrup, suspension)
gas (aerosolized anesthetics)

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18
Q

Drugs are given:
a. directly at the intended site of action
b. at a site distant from the intended site of action

A

b. at a site distant from the intended site of action
(ex. For headache, you consume an analgesic (pain reliever) instead of patching it to your head.)

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19
Q

Most drugs have MW between _____ and _____.

A

100
1000

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20
Q

MW for selective binding

A

100 MW
(Small drugs require small receptors therefore it could only accept or adapt certain size of molecules)

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21
Q

MW for traversing to different barriers of the body

A

1000 MW

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22
Q

MW where drugs cannot move within the body and are given at the site of action

A

> 1000 MW

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23
Q

T/F:
The shape of the drug affects the duration of the action as well as the potency of a drug.

A

true

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24
Q

chemical forces or bonds through which the drug interacts with the receptors

A

drug receptor bonds

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25
Q

__________ bonds are more selective bonds

a. stronger
b. weaker

A

b. weaker

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26
Q

Arrange the types of bonds from strongest to weakest:
electrostatic
hydrophobic
covalent

A

covalent > electrostatic > hydrophobic

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27
Q

strongest bond that is irreversible

A

covalent bond

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28
Q

type of bond that is more common but is weaker (e.g. bond between cation and an anion)

A

electrostatic

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29
Q

weakest bond seen in highly soluble drugs

A

hydrophobic bonds

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30
Q

Give the pharmacodynamic sequence where the receptor makes the effects (no effector molecule)

A

Drug (D) + receptor-effector (R) → drug-receptor-effector complex → effect

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31
Q

Give the pharmacodynamic sequence where the drug receptor complex produces an intracellular effector, and it is this intracellular effector that mediates an action of the drug

A

D + R → drug-receptor complex → effector molecule → effect

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32
Q

Give the pharmacodynamic sequence where the drug receptor complex activates a coupling molecule or enzyme inside

A

D + R → D-R complex → activation of coupling molecule → effector molecule → effect

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33
Q

Inhibition of metabolism of endogenous activator → _________ (increased, decreased) activator action on an effector molecule → increased effect

A

increased

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34
Q

T/F:
Some of the receptor pool must exist in Ra (active) form, and this can occur in the absence of the agonist.

A

true
(constitutive activity; may produce same physiologic effect as agonist-induced activity)

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35
Q

Antagonist action can be overcome by increasing the dosage of ________.

A

agonist

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36
Q

binds to and activate the receptor

A

agonist

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37
Q

Activates receptor-effector system to the maximum extent (Ra-D pool) {activated form}

A

full agonist

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38
Q

Binds to the same receptors and activate them in the same way but do not evoke as great a response

A

partial agonist

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39
Q

Binds to a site on the receptor molecule separate from the agonist binding site

A

allosteric modulators

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40
Q

T/F:
Allosteric modulators modifies receptor activity by blocking agonist activity

A

false
(does not block agonist activity, binds to another site)

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41
Q

T/F:
Allosteric modulators are noncompetitive and may increase or decrease response to agonist

A

true

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42
Q

Drug has a stronger affinity for the Ri pool (nonfunctional form)

A

inverse agonist

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43
Q

Inverse agonist ___________ constitutive activity

a. increases
b. decreases

A

decreases

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44
Q

T/F:
Inverse agonist results in effects that are almost the same with the effects
produced by conventional agonists

A

false
opposite effects

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45
Q

Several other binding sites in the
receptors and for other chemicals that bind to the receptors

A

allosteric site

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46
Q

binds to a receptor, competes with and prevent binding by other molecules

A

antagonist (competitive inhibitor)

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47
Q

inactive precursor that must be administered and converted to the active drug by biologic process inside the body

A

prodrug

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48
Q

Movement of drug molecules into and within the biologic environment

A

permeation

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49
Q

type of permeation:
for water-soluble drugs

A

Aqueous Diffusion

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50
Q

type of permeation for membranes of capillaries with small water-filled pores

A

Aqueous Diffusion

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51
Q

Aqueous Diffusion

a. active process, governed by Fick’s law
b. active process, not governed by Fick’s law
c. passive process, governed by Fick’s law
d. passive process, not governed by Fick’s law

A

c. passive process, governed by Fick’s law

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52
Q

equation for Fick’s Law of Diffusion

A

Flux (moles/ unit time) = C1 - C2 * (Permeability coefficient / thickness) * area

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53
Q

type of permeation:
movement of molecules through membranes and other lipid structures

A

lipid diffusion

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54
Q

type of permeation:
Most important factor for drug permeation

A

lipid diffusion

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55
Q

Lipid Diffusion

a. active process, governed by Fick’s law
b. active process, not governed by Fick’s law
c. passive process, governed by Fick’s law
d. passive process, not governed by Fick’s law

A

c. passive process, governed by Fick’s law

56
Q

type of permeation:
Drugs transported across barriers by mechanisms that carry similar endogenous substances

A

Transport by Special Carriers

57
Q

T/F:
Transport by Special Carriers is capacity-limited and is governed by Fick’s law.

A

false
capacity-limited but not governed by Fick’s law

58
Q

2 types of Transport by Special Carriers

A

active transport
facilitated diffusion

59
Q

needs energy, against a concentration gradient

a. active transport
b. facilitated diffusion

A

a. active transport

60
Q

no energy required, downhill

a. active transport
b. facilitated diffusion

A

b. facilitated diffusion

61
Q

type of permeation:
Binding to specialized components (receptors) on cell membranes

A

endocytosis

62
Q

type of permeation:
Internalization by infolding of the area of the membrane and contents of the vesicle are subsequently released into the cytoplasm

A

endocytosis

63
Q

type of permeation:
Permits very large or very lipid-insoluble chemicals to enter the cell

A

endocytosis

64
Q

type of permeation:
for B12 with intrinsic factor and Iron with transferrin (large chemicals)

A

endocytosis

65
Q

type of permeation:
Expulsion of membrane-encapsulated material from the cell (intracellular content)

A

exocytosis

66
Q

type of permeation:
for neurotransmitters

A

exocytosis

67
Q

Predicts the movement of molecules across a barrier

A

Fick’s Law of Diffusion

68
Q

According to Fick’s Law of Diffusion, drug absorption is:
_________ (faster, slower) in organs with LARGER surface areas
_________ (faster, slower) in organs with SMALLER surface areas

A

FASTER in organs with LARGER surface areas

SLOWER in organs with SMALLER surface areas

69
Q

According to Fick’s Law of Diffusion, drug absorption is:
_________ (faster, slower) from organs with THICK membrane barriers
_________ (faster, slower) from organs with THIN membrane barriers

A

SLOWER from organs with THICK membrane barriers

FASTER from organs with THIN membrane barriers

70
Q

Rate of absorption:
stomach ___ small intestine
(< or >)

A

<
(small intestine: larger surface area)

71
Q

Rate of absorption:
lungs ___ skin
(< or >)

A

> (lungs: thinner membrane barrier)

72
Q

In Fick’s law, this refers to the measure of the mobility of the drug in medium of the diffusion path

A

permeability coefficient

73
Q

↑ Rate of diffusion: ____ concentration gradient

A

↑

74
Q

↑ Rate of diffusion: ____ surface area

A

↑

75
Q

↑ Rate of diffusion: ____ permeability coefficient

A

↑

76
Q

↑ Rate of diffusion: ____ thickness

A

↓

77
Q

↑ Lipid solubility: _____ charge

A

↓

78
Q

_________ solubility of a drug is a function of the electrostatic charge (degree of ionization, polarity) of the molecule

a. aqeous
b. lipid

A

aqeous

79
Q

__________ molecules are attracted to charged drug molecules forming an aqueous shell around them

a. water
b. lipid

A

water

80
Q

T/F:
Many drugs are strong bases or strong acids

A

false
weak acids/ bases

81
Q

_____ of the medium determines the fraction of molecules charged (ionized) versus uncharged (nonionized)

A

pH

82
Q

T/F:
Weak bases/acids can be charged or
uncharged, ionized or non-ionized depending on the pH where they are located

A

true

83
Q

In lipid diffusion, fraction of molecules in the ionized state can be predicted by means of?

A

H-H equation

84
Q

Protonated weak base:

a. water-soluble
b. lipid-soluble

A

a. water-soluble

85
Q

Protonated weak acid:

a. water-soluble
b. lipid-soluble

A

b. lipid-soluble

86
Q

Deprotonated weak acid:

a. water-soluble
b. lipid-soluble

A

a. water-soluble

87
Q

Clinically important when it is necessary to estimate or alter the partition of drugs between compartments of different pH

A

Henderson-Hasselbach Equation

88
Q

Amount drug of absorbed into the systemic circulation to that amount of drug administered

A

bioavailability

89
Q

Route of administration:
Maximum convenience

A

oral (swallowed)

90
Q

Oral route:
Absorption may be _______ (faster, slower) and ________ (more, less) complete

A

slower
less

91
Q

Some drugs have ______ bioavailability when given orally

a. high
b. low

A

low

92
Q

Route of administration:
Subject to first-pass effect

A

oral (swallowed)
(significant amount of the agent is metabolized in the gut wall, portal circulation, and liver before it reaches the systemic circulation)

93
Q

Route of administration:
Bioavailability by definition is 100% (gold standard)

A

Intravenously (IV)/ parenteral

94
Q

Intravenously (IV)/ parenteral:
Instantaneous and ________ (complete, incomplete) absorption

A

complete

95
Q

T/F:
Drugs taken intravenously are potentially more dangerous.

A

true
(high blood levels reached if administration is too rapid)

96
Q

Intramuscular (IM):
Because of the large amount of blood vessels in the muscles, absorption is often ______ (faster, slower) and ______ (more, less) complete than oral.

A

faster
more

97
Q

T/F:
Drugs administered intramuscularly should be limited to less than 5mL into each buttock.

A

false
(Can be administered through large volumes (>5ml into each buttock) if the drug is not irritating)

98
Q

Enumerate the routes of administration where first-pass effect is avoided

A

intramuscular
subcutaneous
transdermal
rectal/ suppository (partial avoidance)

99
Q

Heparin can be given by this route as it does not cause hematoma in the muscle

a. intramuscular
b. subcutaneous

A

subcutaneous

100
Q

Heparin cannot be given by this route as it causes bleeding in the muscle

a. intramuscular
b. subcutaneous

A

intramuscular

101
Q

Rate of absorption:
intramuscular ____ subcutaneous

A

>

102
Q

Route of administration:
in the pouch between gums and
cheeks

A

buccal route

103
Q

Route of administration:
under the tongue; offers the same features as the buccal route

A

sublingual route

104
Q

T/F:
Suppositories tend to migrate upward in the rectum where absorption is partially into the portal circulation.

A

true

105
Q

Ideal route of administration for larger amounts of unpleasant drugs

A

rectal (suppository)
(may cause significant irritation)

106
Q

Route of administration:
For respiratory diseases; delivery closest to the target tissue

A

inhalation

107
Q

Inhalation results into ______ (faster, slower) absorption because of the thin alveolar surface area

A

faster

108
Q

Route of administration:
Application to the skin or mucous membrane of the eye (eyedrops), nose, throat, airway, or vagina (vaginal suppositories) for local effect

A

topical

109
Q

T/F:
For topical administration, rate of absorption varies with the area of
application and drug’s formulation.

A

true

110
Q

For topical administration, absorption is ______ (faster, slower) compared to other routes

A

slower
(because it still would have to traverse the tissues)

111
Q

Route of administration:
Application to the skin for systemic effect

A

transdermal

112
Q

For topical administration, absorption is very ______ (fast, slow)

A

slow

113
Q

Influences absorption from intramuscular, subcutaneous, and in shock

A

blood flow

114
Q

High blood flow maintains a _____ (high, low) drug depot-to-blood concentration gradient.

A

high

115
Q

Major determinant of the rate of absorption (Fick’s law)

A

concentration

116
Q

determines the concentration gradient
between blood and the organ

A

size of the organ

117
Q

Important determinant of the rate of uptake

A

blood flow

118
Q

Enumerate well-perfused organs, where blood flow is good

A
  1. Brain
  2. Heart, Kidneys
  3. Splanchnic organs - responsible for indigestion during times of stress
119
Q

If the drug is very soluble in cells, concentration in the perivascular space will be _______ (higher, lower)

A

lower
(diffusion from the vessel into the extravascular tissue will be facilitated)

120
Q

Binding of drugs to macromolecules in the blood or tissue compartment will tend to ________ (increase, decrease) the drug’s concentration in that compartment.

A

increase

121
Q

A parameter in pharmacokinetics

A

Apparent volume of distribution (Vd)

122
Q

3 types of drug metabolism

A
  1. Action of many drugs is terminated before they are excreted (converted to metabolite before excreted)
  2. Prodrugs (inactive, metabolized to be active)
  3. Drugs not modified by the body (eliminated as metabolite)
123
Q

For most drugs, excretion is by way of the ____________

A

kidneys (except anesthetic gases-lungs)

124
Q

T/F:
For drugs with active metabolites (ex: diazepam), elimination of the parent molecule by metabolism is not synonymous with termination of action.

A

true

125
Q

For drugs that are not metabolized (not metabolized = not water soluble), __________ is the mode of elimination.

A

excretion
(through the bile)

126
Q

most common process of elimination followed by most drugs

A

first order elimination

127
Q

In first order, rate of elimination is ____________ to drug concentration.

a. proportionate
b. inversely proportionate

A

a. proportionate
(The higher the concentration, the greater the amount eliminated per unit time.)

128
Q

In first order elimination, concentration of such drug in the blood will decrease by ____% for every half-life until amount of drug is negligible.

A

50

129
Q

Rate of elimination is constant regardless of drug concentration

A

zero order elimination

130
Q

type of elimination that occurs with drugs that saturate their elimination of mechanism at concentrations of clinical interest

A

zero order elimination

131
Q

Identify the transporter:
norepinephrine reuptake from synapse

A

NET (Norepinephrine Transporter)

132
Q

Identify the transporter:
serotonin reuptake from synapse

A

SERT (Serotonin Transporter)

133
Q

Identify the transporter:
transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings

A

VMAT (Vesicular Monoamine Transporter)

134
Q

Identify the transporter:
transport of many xenobiotics out of cells

A

MDR1 (Multidrug Resistance Protein 1)

135
Q

Identify the transporter:
leukotriene secretion

A

MRP1 (Multidrug Resistance-Associated Protein 1)

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