Chapter 1 Flashcards

1
Q

how do we define drugs traditionally

A

substance that alters physiology of the body

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2
Q

is vit c a drug?

A

if consumed in bit form not if in orange

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3
Q

what is a psychoactive drug

A

Substances that impact the nervous system to alter a person’s mood, per-ceptions, or level of consciousness (as caffeine does) are often referred to as psychoactive drugs.

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4
Q

Substances that impact the nervous system to alter a person’s mood, per-ceptions, or level of consciousness (as caffeine does) are often referred to as …

A

psychoactive drugs

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5
Q

when gas is inhaled in the workplace what do we refer to it as

A

enviro toxin

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6
Q

Pharmaceutical drugs have at least three names what are they

A

chemical, trade name and generic name

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7
Q

7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1, 4-benzodiazepin-2-one what can a chemist tell by this name

A

how the molecule is made up (joints of the drug molecule)

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8
Q

are chemical drug names always the same

A

the same drug will have different chemical names if different conventions are used.

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9
Q

how was the generic name made up initially

A

combining parts of the chemical name

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10
Q

what is the trade name

A

different formulations of the same drug (the drug in different states)

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11
Q

what is the street name for MDMA

A

ecstacy

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12
Q

All of modern science uses the … system and drug doses are nearly always stated in …

A

metric, milligrams

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13
Q

A milligram is … of a gram

A

1/1,000

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14
Q

what effects a drugs effects on the body? the amount fo the drug?

A

no the concentration = mg per kg

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15
Q

why are drug studies not always accurate

A

because Dif metabolisms = Dif concentrations of drug in the body = higher dose in animals

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16
Q

what is a dose–effect curve (DEC) or a dose–response curve (DRC)?

A

a graph that administers Dif dosages of drug (from so low you can hardly tell to so high nothing more is happening)

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17
Q

T: The range should include a dose so low that there is no detectable effect, a dose so high that increases in dose have no further effect, and a number of doses in between

A

dose–effect curve (DEC)

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18
Q

a small change in … doses will have a large effect

A

low not high

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19
Q

???scale on the horizontal axis is graduated loga-rithmically allows a wide range of doses to be reported and permits greater precision at the low end of the dosage range.

A

?

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20
Q

what’s on the vertical axis?

A

a continuous measure or a binary measure

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21
Q

Binary drug effects are handled by …

A

working with

groups of subjects.

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22
Q

4 types of names? do you know the difference?

A

trade name, street name, generic name and chemical name

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23
Q

what are 2 common ways of describing dosage response curves?

A

LD and ED50

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24
Q

what is ED50?

A

the median effective dose (effecting in 50% of populous)

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25
Q

what is LD?

A

median lethal dose

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26
Q

what is the LD1

A

dose that kills 1% of populous

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27
Q

what is ED99

A

effective in 99% of subjects

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28
Q

what is the ED 50 in a DRC with a continuous measure?

A

??refers to the dose that produces an effect that is 50% of the drug’s maximally effective dose.

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29
Q

what is ideal LD and ED levels

A

ones that the ED is very far from the LD

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30
Q

how do we describe the safety of a drug

A

The therapeutic index (TI; also known as the therapeutic ratio) is sometimes used to describe the safety of a drug.

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31
Q

how do we measure TI

A

ratio of ED to LD

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32
Q

do you want high or low TI

A

high

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33
Q

Drug safety may also be described as a ratio of the ….

A

ED99 and the LD1.

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34
Q

how do we describe the extent of a drugs effects

A

potency or efficacy (effectiveness)

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35
Q

When you are comparing two drugs that have the same effect, …. refers to differences in the ED50 of the drugs.

A

potencY

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36
Q

what is potency

A

the difference between the ED50 of the drugs

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37
Q

which drug is more potent ? higher or lower Ed50

A

lower

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38
Q

what does it mean to say a drug is 10x as potent

A

the nature and extent of the effect of LSA would be the same as that of LSD if you increased the dose of LSA by a factor of 10

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39
Q

… refers to a drug’s ability to produce a maximum, biologically functional response at its molecu-lar target,

A

Effectiveness

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40
Q

what is effectiveness of a drug

A

ability to produce max biological function at molecule target regardless of dose

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41
Q

why can’t you compare the potency of aspirin and morphine?

A

because at ED50 morphine is much more effective, they may both produce effects at the same ED50 and be equally potent but the extent of the effects are incomparable

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42
Q

what is antagonism in drug talk?

A

when one drug hinders the effects of another when mixed

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43
Q

how do you find out if 2 drugs are antagonistic ?

A

plotting two DRCs: one for the drug alone, and a second for the drug in the presence of the other drug

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44
Q

If the DRC for the first drug is ….) by adding the new drug, this result indicates antagonism between the drugs.

A

shifted to the right (i.e., the ED50 increases) ???

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45
Q

If adding the new drug shifts the DRC to the left (i.e.,

the ED50 decreases), the drugs are said to have an …

A

additive effect

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46
Q

what does an additive effect look like for DRC

A

shift to left

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47
Q

If, together, drugs have an effect that is greater than might be expected simply by combining their individual effects, a …, or …., exists.

A

superadditive effect, potentiation

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48
Q

if one drug has no effect alone but increases the effect of a second drug, what is happening

A

potentiation is clearly occurring.

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49
Q

drug interaction is defined in terms

of changes in …—shifts in the DRC indicated by changes in the ED50.

A

potency`

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50
Q

drug interaction can be defined in therms of ….. the ED50 may not change, but the maximum effect may increase or decrease`

A

effectiveness

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51
Q

what is a primary and a side effect

A

the effect for which a drug is taken the primary or main effect and any other effect, harmful or otherwise, is a side effect.

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52
Q

is there a clear distinction between main and side effects

A

the distinction between main and side effects is a matter of intention

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53
Q

the potential for a drug to be abused is a side effect

A

t

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54
Q

The study of how a drug moves around the body is called …

A

pharmacokinetics

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55
Q

what are the 3 processes of pharmokinetics

A

absorption, distribution and elimination

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56
Q

do drugs effect the whole body

A

no only sites of action

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57
Q

what happens if a drug does not reach its site of action

A

nothing happens

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58
Q

why Dif routes of administration

A

not only whether it gets to its site of action, but also how fast it gets there and how much of it gets there.

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59
Q

T: not only whether it gets to its site of action, but also how fast it gets there and how much of it gets there.

A

bioavailability

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60
Q

Getting drugs into the body can be accomplished by taking advantage of the body’s natu-ral mechanisms for taking substances inside itself (such as …), or the drug can be artificially placed under the skin by means of …

A

digestion, breathing, or absorption through mucous mem-branes

injection.

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61
Q

what is a parenteral route

A

administration involve injection through the skin into various parts of the body, using a hollow needle and syringe.

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62
Q

what does a drug have to be before it can be parenteral

A

liquid

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63
Q

what is this liquid called that powder is added to

A

vehicle

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64
Q

what liquid is most common vehicle

A

saline to match body to avoid irritating tissues

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65
Q

what is its not water soluble?

A

Dif vehicle

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66
Q

and the drug and vehicle are then injected to form a small ….

A

bubble, or bolus

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67
Q

4 common parental routes?

A

(a) subcutaneous, (b) intramuscular, (c) intra-peritoneal, and (d) intravenous.

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68
Q

the drug is injected to form a bolus just under the skin or cutaneous tissue.:T

A

subcutaneous

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69
Q

where is the subcutanous area in humans

A

usually done under the skin of the arm or thigh, but the hand or wrist is sometimes used to self-administer recreational drugs

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70
Q

usually done under the skin of the arm or thigh, but the hand or wrist is sometimes used to self-administer recreational drugs :T

A

skin popping

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71
Q

In the intramuscular (i.m.) route, the needle is inserted into …

A

a muscle, and a bolus is left there. (absorbed through muscle capillaries

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72
Q

where is intramuscular usually inserted

A

arm or bum

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73
Q

why no intramuscular in rats

A

muscle must be large

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74
Q

T:the needle is inserted directly into the peritoneal cavity

A

intraperitoneal route

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75
Q

what is the peritoneal cavity

A

contains visceral organs

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76
Q

what are 3 visceral organs

A

sleep, liver, intestines (through stomach only for animals)

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77
Q

what is the intravenous route

A

into bloodstream through vein

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78
Q

what is street name for intravenous route

A

mainlining

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79
Q

where does tourniquet go if elbow infection site

A

above elbow because veins carry blood to the heart

80
Q

problem with intravenous IV

A

view can collapse if used to often

81
Q

problem. with intravenous for rec drugs

A

may contain insoluble contaminants that get get lodged in eyes and lungs

82
Q

a permanently implanted tube called a :T

A

catheter.

83
Q

In … injections, for exam-ple, the needle is inserted into the nervous system between the base of the skull and the first vertebra. goes into CBS fluid then straight to nervous system

A

intrathecal

84
Q

A drug may also reach the CSF through an intra-… injection directly into one of the brain’s ventricles, which are chambers filled with CSF

A

cerebroventricular

85
Q

… injections may be used in which a drug is administered directly into brain tissue. These forms of drug administration are often done through a ….

A

intracerebra

cannula

86
Q

what is a cannula

A

Cannulae are often attached to the skull using dental cement and can remain permanently implanted.

87
Q

which method has the drugs impact you fastest

A

Generally, the volume of blood flow is greater to the peritoneal cavity than to the muscles, and it is greater to the muscles than under the skin. As a result, next to an i.v. injection, absorption is fastest from an i.p. injection and is slowest from an s.c. injection.

88
Q

…2 can speed absorption from i.m. and s.c. sites because such factors increase blood flow to muscles and skin.

A

Heat and exercise

89
Q

To be absorbed into the bloodstream, a drug must pass

through the walls of the …

A

capillaries.

90
Q

why is the single cell wall of the capillary nessasy for drug absorption

A

can pass freely through pores of cap through diffusion

91
Q

why is i.m injections faster then s.c

A

Areas that are serviced by many capillaries will absorb

drugs faster than areas that have few capillaries.muscles have more cap

92
Q

how long does it take i.v injection to circulate around body

A

The body has about 6 liters of blood, and the heart pumps these 6 liters once a minute, so the drug in most i.v. injections is distrib-uted around the body within a minute after injection

93
Q

why use a depot injection and what is it

A

the drug is dissolved in a high concentration in a viscous oil (often sesame oil) which is then injected into a muscle, usually in the buttock. if won’t comply to take antipsychotic drugs

94
Q

how long does depot injection last?

A

4 weeks

95
Q

what does a drug need to be for depot injection

A

highly lipid soluble

96
Q

why is inhalation so effective in speed of drug effect

A

When drugs in the form of gases, aerosols, or fine mists are inhaled, they are very quickly absorbed through the capil-lary walls and enter the bloodstream to circulate around the body

97
Q

where does blood go after heart

A

straight to lungs then after removing CO2 straight back to heart after absorbing o2 then from heart to brain (skips liver = fast effects

98
Q

why are gases preferable to intravenous for controlling drug concentration?

A

the drug passes out of the blood into the air and is exhaled so that the concentration of the gas in the blood reflects the concentration in the gas that is breathed

99
Q

3 drugs that are usually smoked?

A

Tobacco, opium, and marijuana

100
Q

Dif between smoke and gas inhalation?

A

The major difference between smoke and gases is that the drug in the smoke particles will not revaporize after it is dissolved in the blood and, consequently, cannot be exhaled= must be eliminated a different way

101
Q

cons of smoke inhalation?

A

damage to lungs effecting ability to absorb o2 and remove co2

102
Q

when most substances burn in air, … gas is given off. … is a very toxic gas because it blocks the ability of the blood to carry oxygen.

A

carbon monoxide

103
Q

how do vapours compare?

A

no carbon monoxide but same absorption method as smoke = can’t control level exhaled

104
Q

what is the sniffing route called

A

intranasal administration or insufflation

105
Q

what happens with intranasal ?

A

absorbed in nasal cavity and some down to lungs and digestive tract

106
Q

how is drug absorbed during oral ingestion

A

through digestive system

107
Q

what if put in mouth and not swallowed

A

absorbed through the buccal membranes, or mucous membranes of the mouth, not the gastrointestinal tract.

108
Q

when would you want to use a suppository

A

when patient unconscious or vommitting

109
Q
The gastrointestinal tract may also be entered via its
other end (... administration).
A

intrarectal

110
Q

with oral administration where is drug getting absorbed

A

Drugs that are soluble in gastric fluids and resistant to destruction by digestive enzymes may be absorbed from the stomach, but absorption is most efficient in the intestines

111
Q

what determines the rate a swallowed drug is absorbed

A

the speed with which it gets through the stomach to the intestines.

112
Q

does eating food slow or speed absorption

A

slow

113
Q

what are membranes made up

A

lipid bilayer and proteins

114
Q

is the head or the tail hydrophilic

A

head= loves water

115
Q

what determines if a drug will get through the intestine tissue layer

A

the extent to which a drug can get through the lining of the intestine to the blood will depend on its ability to dissolve in lipids.

116
Q

… drug molecules easily diffuse through membranes.

A

lipophilic

117
Q

Different drugs have different degrees of lipid solubility that are usually expressed in terms of the …

A

olive oil partition coefficient.

118
Q

olive oil partition coefficient: how is this found

A

drug put in solution half oil half water then separated and lipid soluble drugs will have higher concentration of drug in oil

119
Q

what happens if a drug is electrically charged ions (to its solubility

A

when a molecule of a drug carries an electric charge, it loses its ability to dissolve in lipids.

120
Q

what is Kpa

A

the ph where half of the drugs molecules become ionized

121
Q

Most drugs are either weak acids or weak bases. what does this mean

A

???

122
Q

what do we need to find out if a drug will be ionized in a certain Ph

A

need to know if its acid or base and its Kpa

123
Q

the percentage of nonionized drug is all that is absorbed t or f

A

f the percentage of nonionized molecules determines the number of molecules available for absorption at any period of time and, therefore, determines the rate of absorption

124
Q

If 50% of the molecules are not ionized, absorption will be …, but if 3% are not ionized, absorption will be …

A

rapid, much slower.

125
Q

in transdermal admin what is hardest layer for drug to penetrate

A

epidermis due to keratin

126
Q

what must drug be for transdermal admin

A

lipid soluble no water passed through epidermis

127
Q

how does the patch work

A

transdermal patch separates the drug from the skin by a special membrane that limits the rate of absorp-tion

128
Q

T: Even though most drugs get transported widely around the body by the blood, they tend to become concentrated in particular places and segregated from others.

A

distribution

129
Q

what does fat do to a drug

A

acts like a sponge absorbs it and has no effect

130
Q

where do lipid soluble drugs end up

A

in body fat around nervous system

131
Q

what effects distribution of drugs

A

ion, lipid soluability, active passive trans, placental barrier, protein binding

132
Q

when do bases and acids ionized

A

when in opposite solution

133
Q

how does a ph difference of 1 effect drug concentration

A

10 time more concentrated on one side of the membrane compared to the other

134
Q

how does a ph difference of 2 effect drug concentration

A

100 times

135
Q

what causes the blood brain barrier

A

special cells in the central nervous system that wrap themselves around the capillar-ies and block the pores through which substances nor-mally diffuse

136
Q

what substances can and can’t get passed blood brain bilayer

A

non lipid soulble can’t except for in some areas

137
Q

the area …. of the medulla oblongata contains specialized cells that play an important role in detecting impurities or toxins in the blood and elicits vomiting in an attempt to rid the body of these substances

A

postrema

138
Q

the … organ in the brain plays an important role in detecting hormone levels in the blood, especially those hormones involved in regulating the bal-ance of bodily fluids

A

subfornical

139
Q

Mechanisms such as ion pumps, which maintain electrical potentials of nerve cells, are examples of ….

A

active transport systems.`

140
Q

what happens if Some drug molecules become bound (attached) to these protein molecules

A

never reach active site or act as depositers as blood concentration of drug declines

141
Q

There is a proportional relationship between the ratio of bound:unbound drug molecules and the drug’s lipid solu-bility (lipophilicity). what is this relationship

A

More lipophilic drugs tend to have a higher percentage of their molecules bound to blood pro-teins

142
Q

can most active drugs be transported to the fetus

A

yes (high lipid sol = easier crossing)

143
Q

Drug concentration in the blood of the fetus usually reaches 75% to 100% of that of the mother within … of administration

A

5 minutes

144
Q

Small amounts of many drugs are eliminated in …3, but the major job of elimination is done by the …2

A

sweat, saliva, and feces

liver and the kidneys

145
Q

what does the liver do

A

molecules are modified to form new substances useful to the body and where toxic molecules are changed into less harmful substances to be filtered out of the blood by the kidneys

146
Q

how does the liver do it!?

A

enzymes

147
Q

enzyme is a …., a substance that controls a certain chemical reaction

A

catalyst

148
Q

how does the body control chemical reactions

A

The body controls chemical reactions by con-trolling the amount of enzyme available

149
Q

other than liver where else are enzymes located

A

blood and brain or, as we will soon see, in the digestive tract

150
Q

Most enzymes end in the suffix …

A

ase

151
Q

what is metabolism

A

This process of biotransformation or the restructuring of molecules to rid them from the body

152
Q

T: products of metabolism

A

metabolites

153
Q

Where drugs are concerned, the metabolic process is sometimes called …

A

detoxification (although metabolites aren’t always less toxic )

154
Q

metabolites are usually

more likely to ionize. why is this important to the kidneys

A

because ionized molecules cannot be reabsorbed into the blood through the nephron wall and, consequently, can be excreted more easily

155
Q

what is first pass metabolism

A

Drugs that are absorbed into the bloodstream from the digestive system reach the liver before arriving at the heart.

156
Q

which routes are not subject to first pass

A

nasal, anal or absorbed in mouth

157
Q

what is the kidneys main job

A

to maintain water salt balances

158
Q

what else do the kidneys do

A

take bad stuff from blood and excrete it

the kidneys can also excrete molecules of unwanted substances, the by-products of metabolism by liver enzymes

159
Q

what it the functional unit of the kidney

A

the nephron

160
Q

what is at both side of the nephron (and inside it)

A

Bowmans capsule, glomerulus

tube that goes to bladder

161
Q

what goes through Bowmans capsule what stays

A

through= fluid

red and white cells in blood stays

162
Q

The kidney works not by filtering impurities out but

by…

A

filtering everything out of the blood and then allowing selective reabsorption of what is required

163
Q

what 2 mi=olecules are excreted inn urine

A

Unless they are reabsorbed by special transport systems, ionized or non-lipid-soluble substances will be excreted.

164
Q

pH influences the degree of …

A

ionization which influences reabsorption

165
Q

do acid or base go to blood or unine

A
urine = base
blood = acid
166
Q

how does the amount of the drug influence metabolism in the liver

A

lower dose= slower meta

167
Q

what does the curve that plots the level of drug metabolizing look like

A

asymotote

168
Q

HOW DO WE DESCRIBE THE WAY DRUGS ARE EXCRETED

A

with the half life

169
Q

what does half life mean

A

Every 30 minutes, the body gets rid of half of the drug circulating in the blood, so the half-life of the drug in this example is 30 minutes

170
Q

what is first-order elimination kinetics

A

the way drugs eliminate with the half life principle

171
Q

what drug does not abide by half life

A

alcohol is eliminated at a constant rate

172
Q

what is name for the way alc is eliminated

A

Xero order elimination kinetics

173
Q

what are 6 reasons for variation in drug metabolisms

A

age, gender, species, past experience with drugs, and genetics.

174
Q

Levels of a given enzyme can be … by previous exposure to a specific drug that uses that enzyme or some other enzyme system. This process, known as ….,

A

increased

enzyme induction

175
Q

what does enzyme induction lead to

A

metabolic tolerance

176
Q

what do heavy drinkers have a lot of

A

enzyme alc dehydronase = faster metabolism

177
Q

When two drugs that use the same enzyme are introduced into the body at the same time, what will happen

A

the metabolism of each will be depressed because both will be competing for the enzyme

178
Q

CAN THE the activity of an enzyme can be blocked by another drug

A

yes

179
Q

disulfiram blocks acetaldehyde. what will happen

A

person will get sick from buildup of acetaldehyde which is toxic

180
Q

how does drinking grapefruit juice alter drug consumption

A

blocks drug enzyme and can significantly increase blood levels of those drugs. As a result, people should avoid drinking grapefruit juice if they are taking any of a number of medi-cations.

181
Q

how does age influence drugging

A

Enzyme systems are not fully functional at birth and may take time to develop completely.= metabolize differently

182
Q

how does theophylline found in tea influence babies vs adults dif

A

the liver of a newborn human first converts the-ophylline to caffeine and then metabolizes caffeine very slowly. In adults, theophylline is metabolized directly without this intermediate stage

183
Q

why do old people have to lower drug use

A

less effective liver function

184
Q

why is drug more dangerous for baby after cord is cut

A

While the child’s circula-tory system is connected to the mother, the mother’s liver can metabolize the drug. But if the baby is born and the umbilical cord is cut before all the drug is broken down, the drug remains in the infant’s body and is dependent solely on the baby’s immature liver for metabolism, a pro-cess that may take many days.

185
Q

how do we plot drugs effects

A

time course (the drug effect is usually represented on the vertical axis, and time on the horizontal axis).

186
Q

how does the rate of excretion differ

A

always stays same

187
Q

how does absorption differ

A

depends of route of admin (shape of half life

188
Q

more intense subjective experience, greater reinforcement, and an increased capacity for addiction : what route?

A

intravenous

189
Q

If the function of a drug depends on maintaining constant blood levels, as with antibiotics, … is pre-ferred. If it is necessary to achieve very high levels for brief periods, the drug is best given ….

A

oral administration

intravenously.

190
Q

T: too high a level, there will be an increase in unwanted side effects and no increase in the therapeutic effect. If the drug falls below a certain level, it will not have a therapeutic effect at all.

A

therepudic window

191
Q

what is the therepudic window

A

too high a level, there will be an increase in unwanted side effects and no increase in the therapeutic effect. If the drug falls below a certain level, it will not have a therapeutic effect at all.

192
Q

how can you stay in the therepudic window

A

a drug must be taken at the correct dose at regular intervals

193
Q

lithium carbonate, which is prescribed to people with bipolar disorder what’s the problem with this drug

A

absorbed and excreted rapidly = narrow therepudic window

194
Q

does tolerance increase at the same rate for all drugs

A

no

195
Q

Tolerance to the toxic effects of morphine builds .., moving the curve for the effective dose closer to the curve for the toxic dose, increasing the risk of overdose and narrowing the therapeutic window

A

more slowly