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Pharm 1 > Lecture 1 > Flashcards

Lecture 1 Flashcards

0
Q

Substances which can affect the biological system.

A

Drugs

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1
Q

The study of drugs and their action on the body.

A

Pharmacology

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2
Q

The branch of pharmacology dealing with reactions between drugs and living systems.

A

Pharmacodynamics

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3
Q

The mathematical description of the processes through which a drug is handled once introduced into the body.

A

Pharmacokinetics

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4
Q

What a drug does to the body is ______.

A

Pharmacodynamics

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5
Q

What 3 characteristics of drugs are not capable of absorbing past a membrane?

A

Large molecules
Ionized drugs
Hydrophilic

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6
Q

What the body does to the drug is ______.

A

Pharmacokinetics

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7
Q

The study of how drug poison cells, critters, and/or ecosystems.

A

Toxicology

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8
Q

5 phases of pharmacokinetics:

A 
Liberation
Absorption
Distribution 
Metabolism 
Elimination/Excretion
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9
Q

This is the process of the drug being freed from its carrier tablet, capsule, etc.

A

Liberation

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10
Q

Liberation is also known as ______.

A

Disintegration

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11
Q

The nature and characteristics of how a drug moves from its site of administration into usually the critter’s plasma is called ______.

A

Absorption

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12
Q

The dissemination of a drug throughout the “compartments” of a critter’s body, such as plasma, issues, or organs.

A

Distribution

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13
Q

Major vehicle for distribution is the _______.

A

Bloodstream

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14
Q

What 4 things affect absorption?

A

Drug solubility
Dosage form
Administration route
pH

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15
Q

What 3 characteristics of drugs are capable of absorbing past a membrane?

A

Small drug molecule
Nonionized drug
Lipophilic

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16
Q

What 3 things may affect distribution?

A

Blood flow
Fat or water solubility
Protein binding

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17
Q

_____ is affected by renal blood flow and kidney functions.

A

Elimination

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18
Q

The biotransformation of a drug into other (secondary) compounds.

A

Metabolism

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19
Q

Metabolism is frequently a tasked performed by which organ?

A

Liver

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20
Q

After the drug has been absorbed and distributed, the body works to break it down via metabolism into several components called ______.

A

Metabolites

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21
Q

The liver is the major organ for metabolism via drug oxidation by the _________ system.

A

Cytochrome P-450 enzyme

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22
Q

What does the Cytochrome P-450 enzyme system do?

A

Induce (increase) or inhibit (decrease) metabolic activity

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23
Q

What explains why people who frequently drink alcohol become more tolerant to it?

A

Enzyme induction by the P-450 Enzyme System

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24
Q

_____ is affected by liver function and enzymes.

A

Metabolism

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25
Q

The fetal liver contains _____ of the drug metabolism capacity of the adult liver therefore metabolism is _____ at birth.

A

1/3

Reduced

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26
Q

Aging alone accounts for a reduction of _____ of liver mass.

A

20-30%

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27
Q

______ is affected by protein binding, blood flow, and fat or water solubility.

A

Distribution

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28
Q

The processes that remove a drug from an organism.

A

Elimination/excretion

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29
Q

For each drug a certain percentage is converted from the original compound into some intermediate metabolite is called _______.

A

First pass effect

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30
Q

After the first past effect the drug then passes into the systemic circulation as either the ______ or as a ______.

A

Chemically intact drug

Metabolite

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31
Q

Why are oral doses higher than IV doses?

A

First pass effect

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32
Q

3 types of drug interactions:

A

Additive interactions
Synergistic interactions
Potentiation

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33
Q

The summation of the effects of two (or more) groups given together is equal to each of them given separately but at the same time are called ______ interactions

A

Additive

1+1=2

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34
Q

Two categories of drug administration

A

Enteral

Parenteral

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35
Q

If a drug isn’t excreted fast enough it _____ in the body.

A

Bio-accumulates

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36
Q

Acidic drugs get trapped as anions in _____ urine.

A

Alkaline

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37
Q

One drug (which has no direct effect) increases the response of the other drug, which normally has a lesser effect is called a ______ interaction.

A

Potentiation

1+0=3

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38
Q

Oral, sublingual, and buccal routes are called _____ administration.

A

Enteral

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39
Q

IV, intra-arterial, IM, SQ, inhalation, topical, IO, transdermal, and intrathecal/intraventricular routes are called ______ administration.

A

Parenteral

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40
Q

What 5 ways are drugs usually excreted?

A 
Urine
Feces
Pulmonary 
Skin
Hair
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41
Q

Basic drugs get trapped as cations in ____ urine.

A

Acidic

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42
Q

Rectal route is considered ______ administration.

A

can be both enteral and parenteral

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43
Q

A _____ (IV) dose gives a regulated, consistent dose over time, causing a steady state in drug concentration.

A

Continuous infusion

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44
Q

_____ diffusion is described by Fick’s Law.

A

Aqueous

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45
Q

An _______ (IV) has peaks and troughs in drug concentration.

A

Intermittent dose

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46
Q

____ drugs (like warfarin) have a lower pK.

A

Acidic

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47
Q

_____ drugs get trapped as anions in alkaline urine.

A

Acidic

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48
Q

The use of pharmaceuticals or medical devices for an (FDA) unapproved age group, unapproved dosages, unapproved form of administration, or unapproved indication is called ______ n

A

Off label

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49
Q

______ are immune-mediated and induce a hypersensitivity reaction.

A

Drug allergies

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50
Q

_____ diffusion allows the drug to move from an area of high concentration to low concentration.

A

Passive

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51
Q

______ diffusion is used for “large” molecules and can be “saturated”.

A

Facilitated

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52
Q

Basic drugs (like neo) have a ____ pK.

A

Higher (>7.00)

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53
Q

Type of movement of drugs across barriers that doesn’t require energy.

A

Diffusion (passive and facilitated)

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54
Q

______ is the engulfment of large drugs by a cell in a membrane-lined vesicle.

A

Endocytosis/exocytosis

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55
Q

_____ is affected by drug solubility, dosage form, administration route, and pH.

A

Absorption

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56
Q

_______ type of movement that can move drugs against a concentration gradient, can be saturated, and requires energy (ATP).

A

Active transport

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57
Q

Endocytosis/exocytosis requires _____ and _____.

A

Energy and cells

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58
Q

Acidic drugs (like warfarin) have a ____ pK.

A

Lower (<7.0)

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59
Q

The Fick Equation

A

Thickness of diffusion interface surface

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60
Q

2 types of passive diffusion

A

Aqueous diffusion

Lipid diffusion

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61
Q

Basic drugs get trapped as _____ in acidic urine.

A

Cations

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62
Q

Aqueous diffusion is described by ______.

A

Fick’s Law

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63
Q

Heparin/protamine is an example of ____ antagonism.

A

Chemical

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64
Q

_____ bind to a receptor and prevent binding of other molecules/drugs. They often have little or no inherent response.

A

Antagonists

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65
Q

All drug allergies are considered ______.

A

Adverse drug reactions (ADR’s)

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66
Q

An _____ drug has an intrinsic activity of 0.

A

Antagonistic

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67
Q

Are all ADR’s considered drug allergies?

A

No

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68
Q

The summation of each individual drug’s activity exceeds the dum of the two individuals are called ______ interactions.

A

Synergistic

1+1=3

69
Q

Acidic drugs get trapped as ____ in alkaline urine.

A

Anions

70
Q

____ drugs (like neo) have a higher pK.

A

Basic

71
Q

_____ drugs tend to be protonated and non-polar at a low pH and non-protonated and polar at high pH.

A

Acidic

72
Q

_____ drugs tend to be non-protonated and non-polar at a high pH and protonated and polar at low pH.

A

Alkaline

73
Q

_____ = the extent to which a drug acts at one specific receptor site.

A

Drug selectivity

74
Q

______ is a macromolecule or the component of a cell or organism that interacts with a drug and initiates the chain of biochemical events leading to the drugs observed effects.

A

Receptor

75
Q

When a drug binds to a receptor, three things may happen:

A

An ion channel can be opened or closed

Biochemical messengers activated

Normal cellular functions turned off or on

76
Q

Many drugs are available in _____ mixtures, which contain two different isomers.

A

Racemic

77
Q

An ____ has the exact same elemental components but the molecular arrangement is different. Each one can have different pharmacologic activity.

A

Isomer

78
Q

_____ are compared by the EC50.

A

Potencies

79
Q

Low of mass action applies to drug-receptor interactions in what 4 ways?

A

1) Pharmacological effects are reversible because the drug-receptors complex is reversible.
2) Pharmacological effects are proportional to the number of receptors occupied.
3) Pharmacological effects plateau because they are limited by the total number of receptors.
4) Drug effects are proportional to the doses.

80
Q

_____ bind to and activate a receptor which directly or indirectly brings about an effect.

A

Agonists

81
Q

Agonists _____ the receptor.

A

Activates

82
Q

_____ = measure of a drug’s effectiveness of causing a response (efficacy).

A

Intrinsic activity

83
Q

“Spare Receptor” Concept

1) ____ response can be achieved by an agonist even if only a fraction of the receptors are occupied.
2) ____ of the cell to an agonist concentration depends on affinity of receptors for the drug and total receptor concentration.

A

Maximal

Sensitivity

84
Q

Effect-Concentration Curves are the _____ curved.

A

Dose-response

85
Q

Dexamethasone/insulin and lisinopril/epinephrine are examples of ______ antagonism.

A

Physiologic

86
Q

Potencies are compared by the ____.

A

EC50

87
Q

Example of chemical antagonism

A

Heparin/protramine

88
Q

4 types of receptors:

A

Regulatory proteins
Enzymes
Transport proteins
Structural proteins

89
Q

Three aspects of drug-receptor function:

A

1) Receptors determine the nature and characteristics of the “Drug Concentration-Effect Curve”
2) Receptors function as regulatory proteins and part of chemical signaling mechanisms that provide target for drugs.
3) Receptors determine the therapeutic and toxic effects of drugs.

90
Q

4 transmembrane signaling mechanisms:

A

Ligand-gated ion channels
G protein-coupled receptors
Enzyme-linked receptors
Intracellular receptors

91
Q

The higher the pK, the more ____ it is.

A

Basic

92
Q

_____ = the amount of drug necessary to produce an effect of a given magnitude.

A

Potency

93
Q

An antagonistic drug has an intrinsic activity of ____.

A

0

94
Q

_____ = (1) one drug molecule interacts with many receptors and (2) the activated receptors can persist for longer than the original drug ligand/receptor complex existed

A

Signal amplification

95
Q

____ = increased amount of drug is needed to produce the same effect.

A

Tolerance

96
Q

______ = long-term exposure of a drug to cells or tissues makes those tissues less responsive over time.

A

Desensitization

97
Q

Differences in potency can be overcome ____.

A

Giving more drug

98
Q

Why is absorption in the intestine more efficient in the stomach?

A

The intestines receive more bloodflow and have a higher surface area due to microvilli.

99
Q

____ = the ability of a drug to elicit a response when it interacts with are receptor.

A

Efficacy

100
Q

Which is generally more important…potency or efficacy?

A

Efficacy

101
Q

Think of fentanyl being more potent than morphine and both are more efficacious for pain than aspirin.

A

Just an example

102
Q

Formula for therapeutic index

A

ED50

103
Q

_____ = occurs over a longer period than desensitization (hours to days to weeks) and the receptors are internalized and eliminated.

A

Down-regulation

104
Q

Amount of drug required to produce 50% of the maximal effect.

A

EC50

105
Q

The effects of down-regulation are _____-lasting.

A

Longer

106
Q

_____ drugs get trapped as cations in acidic urine.

A

Basic

107
Q

We can “trap” acidic or basic drugs in the renal tubules for increased excretion by making them ______.

A

More polar

108
Q

_____ = the ratio of the drug doses that produces a specified toxic effect in 50% of the population vs. the dose that produces a specified therapeutic effect in 50% of the population.

A

Therapeutic Index

111
Q

For drugs administered IV, absorption is not a factor, and the initial phase (from immediately after a administration through the rapid fall in concentration) represents the ____ phase.

A

Distribution

112
Q

______ is the transfer of a drug from the site of administration to the bloodstream.

A

Absorption

113
Q

____ is a measure of the strength of the interaction of a compound with a proton.

A

pK

115
Q

______ is achieved when the permeable form of a drug achieves equal concentration in all body water spaces

A

Distribution equilibrium

116
Q

_____ drugs do not Leslie penetrate cell membrane and must pass through slit junctions.

A

Hydrophilic

117
Q

The _____receives much more bloodflow in the stomach, so absorption is favored here.

A

Intestines

118
Q

What administration route has minimized absorption during shock?

A

SQ because blood flow to cutaneous tissues is reduced.

119
Q

What upset does food have a drug absorption in the stomach?

A

The presence of food in the stomach both dilutes the drug in slows gastric emptying, therefore absorption is slower.

120
Q

_____ “pumps” drugs out of the cells and is also associated with multi drug resistance.

A

P-glycoprotein

121
Q

What happens in areas of high expression of P-glycoprotein?

A

Drug absorption is reduced

122
Q

Determining bioavailability is important for calculating drug Jessicas for _____ routes of administration.

A

Non-IV

123
Q

By availability is determined by comparing plasma levels of a drug after particular route of administration with levels achieved by ____ route of an administration

A

IV

124
Q

Vd is a useful for pharmacokinetic parameter for calculating the ______ dose of a drug.

A

Loading

125
Q

When a drug is a door from the G.I. tract, it enters the ____ before entering systemic circulation.

A

Portal circulation

126
Q

If a drug is rapidly metabolized in the ____ or ____ during this initial passage, the amount of unchanged drug entering the system and is decreased.

A

Liver

Gut wall

127
Q

The lower the pK, the more ____ it is.

A

Acidic

128
Q

First pass metabolism by the intestine or liver limits of the _____ of many oral medications

A

Efficacy

129
Q

Why is nitroglycerin primarily administered via the sublingual and transdermal route?

A

More than 90% is cleared during first-pass metabolism.

130
Q

What must be necessary (regarding solubility) for a drug to be readily absorbed?

A

It must be largely lipophilic, yet have some solubility in aqueous solutions.

131
Q

What makes drug formulations bioequivalent?

A

If they have comparable bioavailability and similar times to achieve peak blood concentrations.

132
Q

To drug formulation are therapeutically equivalent if they are _____ with similar clinical and safety profiles.

A

Pharmaceutically equivalent

Meaning same distance form, same after the gradient, same route of administration

133
Q

Metabolism leads to production of products with increased polarity, which allows the drug to be ______.

A

Eliminated

134
Q

Are all drugs that are bioequivalent considered therapeutically equivalent?

A

No

135
Q

The distribution of a drug from the plasma to the interstitium depends on: (5)

A 
CO and local blood flow
Capillary permeability
Tissue volume 
Degree of binding of the drug to plasma and tissue proteins
Solubility of drug
136
Q

_____ is the process by which a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and the tissues.

A

Drug distribution

137
Q

____-soluble drugs rarely penetrate the CNS because they dissolve in the endothelial cell membrane.

A

Lipid

138
Q

Ionized or polar

A

______ drugs generally fail to enter the CNS because they cannot pass through the endothelial cells that have no split junctions

139
Q

____ drugs readily move across most biological membranes because they dissolve in the lipid membrane and penetrate the entire cell surface.

A

Lipophilic

140
Q

Value of distribution is calculated by dividing _____ by _____.

A

Dose that gets to systemic circulation
—————————————————
Plasma concentration at time zero

141
Q

What are the three functional a distinct compartment of body water?

A

Plasma
Extracellular
Total body water

142
Q

Once a drug enters the body, it has the potential to do distribute into ____ or become _____.

A

Any of the 3 compartments of water

Sequestered in a cellular site

143
Q

If a drug has a high molecular weight or is extensively protein-bound, it is too large to pass through the slit junction of the capillaries and, thus, is effectively trapped within the _____ compartment.

As a result it has a ____ Vd.

A

Plasma (vascular)

Low

144
Q

Is a drug has a low molecular weight but is hydrophilic, it can pass through the endothelial slit junctions of the capillaries into the interstitial fluid, but cannot move across the lipid membranes to enter the intracellular fluid, therefore is in the ______ compartment.

A

Extracellular fluid

145
Q

If I drive has a low molecular weight and is lipophilic, we can move into the interstitium through the slick junctions and also pass through the cell membrane into the intracellular fluid, therefore is in the ______ compartment.

A

Total body water

146
Q

T/F

A drug rarely associates exclusively with only one of the water compartments of the body

A

True

147
Q

______ means that a constant fraction of the drug is eliminated per unit of time.

A

First-order

148
Q

When is time zero?

A

Time of IV bolus

149
Q

The fact that drug clearance is usually a ____ process allows calculation of Vd.

A

First-order

150
Q

If a drug has a barge Vd, most of the drug is in the _____ space and is unavailable to the _____.

A

Extraplasmic

Excretory organs

151
Q

Any factor that increases _____ can increase the half-life and extend the duration of action of the drug.

A

Vd

152
Q

What should you consider if a drug has an explicitly large Vd?

A

Sequestration of the drug in some tissues or compartments.

153
Q

What’s a drug inches the body, the process of _____ begins.

A

Elimination

154
Q

Three major routes of elimination:

A

Hepatic metabolism
Biliary elimination
Urinary elimination

155
Q

Zero-order kinetics are also known as ______ kinetics.

A

Non-linear

156
Q

Give an example of three drugs that use zero order kinetics.

A

ASA
Ethanol
Phenytoin

157
Q

The inside is saturated by a high free drug concentration, and the rate of metabolism remains the same overtime, this is called _____ kinetics.

A

Zero-order

158
Q

Describe metabolism and elimination of a drug with zero-order kinetics.

A

Constant amount of the drug is metabolized per unit of time.

The rate of elimination is constant and does not depend on the drug concentration.

159
Q

The kidneys cannot efficiently eliminate ____ drugs, which are reabsorbed into the distal convoluted tubules. Due to this, these drugs are first metabolized into more _____ substances in the _____

A

Lipophilic

Polar

Liver

160
Q

Cytochrome P450 complexes system is also called ______.

A

Microsomal mixed-function oxidases

161
Q

Cytochrome P450, is the superfamily of heme-containing isozymes that are located in most cells, but primarily in the ____ and ____.

A

Liver

GI tract

162
Q

Drugs must be sufficiently ____ to be eliminated from the body.

A

Polar

163
Q

Drugs that are not absorbed after oral administration or drugs that are secreted directly into the intestines or into the bile are eliminated in the ______.

A

Feces

164
Q

The sole determinant of the rate that a drug achieves steady-state is the _____ of the drug.

A

Half-life

165
Q

I dread reaches steady-state in about blank half lives.

A

4-5

166
Q

Using smaller doses at shorter intervals reduces the amplitude of fluctuation and drug concentration, however does not affect ______.

A

Steady-state concentration

167
Q

What is the goal of drug therapy?

A

To achieve and maintain concentration within a therapeutic response window while minimizing toxicity and/or side effects

168
Q

What 2 rates are important to achieve a given concentration?

A

Rate of administration

Rate of elimination

169
Q

What are two disadvantages of loading doses?

A

Increased risk of toxicity

A longer time for plasma concentrations of fall if excess levels occur.

170
Q

_____ leads to production of products with increased polarity, which allows the drug to be eliminated.

A

Metabolism

171
Q

_______ is a useful for pharmacokinetic parameter for calculating the loading dose of a drug.

A

Vd

172
Q

The major factor influencing the distribution of lipophilic drugs is _____.

A

Blood flow to the area

Pharm 1 (6 decks)

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