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NPP > Chapter 1: Principles of Pharmacology > Flashcards

Chapter 1: Principles of Pharmacology Flashcards

1
Q

Neuropharmacology:

A

drug-induced changes in functioning of cells in the nervous system

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2
Q

Psychopharmacology:

A

drug-induced changes that alter mood, thinking, and behavior

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3
Q

Pharmacology:

A

study of actions of drug and their effects on a living organism

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4
Q

Drug action:

A

molecular changes produced by a drug when it binds to a target site or receptor

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5
Q

Molecular changes alter physiological or psychological functions, called …

A

drug effects

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6
Q

Therapeutic side effects:

A

drug-receptor interaction produces desired physical/behavioral changes

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7
Q

Side effects vs therapeutic effects?

A

side effects are everything else that doesn’t include the molecular binding interaction

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8
Q

T/F: Therapeutic side effects and side effects can change.

A

yes depending on the desired outcome

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9
Q

What shows the possibility of medications changing their therapeutic and side effects because of the desired outcome?

A

amphetamine-like drugs

can be used to prevent narcolepsy (produce primary side effect of anorexia)

OR

can be used as a weight loss supplement (produce insomnia and hyperactivity as side effects)

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10
Q

T/F: There are “good” and “bad” drugs.

A

false; it’s character is determined by the way it’s procured

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11
Q

Specific drug effects: […] and […] of a drug with a target site in a living […].

A

physical; biochemical interactions; tissue

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12
Q

Nonspecific drug effects:

A

effects not based on the chemical activity of a drug-receptor interaction but on certain unique characteristics

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13
Q

What are those unique characteristics involved in nonspecific drug effects?

A

neurochemical states existing within an individual:

mood, expectations, perceptions, attitudes

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14
Q

What is an example of nonspecific drug effects?

A

ethyl alcohol; self administered on the same person– they can experience lightheartedness one day and depressed on another

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15
Q

What factors influence the outcome of a drug (5)?

A
  1. individual’s background (drug taking experience)
  2. present mood
  3. expectations of a drug effect
  4. perceptions of the drug-taking situation
  5. attitude toward the person administering the drug

etc

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16
Q

Placebo:

A

a pharmacologically inert compound

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17
Q

T/F: Placebos are fake pills.

A

no; in some cases these placebos can hold the same therapeutic effects

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18
Q

Belief in a drug may have […] despite the […].

A

real physiological effect; lack of chemical activity

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19
Q

Physiological effects that can occur with belief in a drug:

A
  1. altered gastric secretion
  2. blood vessel dilation
  3. hormonal changes

and so forth

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20
Q

What are the 3 possible explanations for the placebo effect?

A
  1. Pavlovian conditioning (cues in the environment)
  2. conscious, explicit explanation of outcomes
  3. social learning
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21
Q

What’s more important than the dosage of the drug?

A

bioavailability

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22
Q

Bioavailability:

A

amount of drug in the blood that is free to bind at specific target sites to elicit drug action

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23
Q

Pharmacokinetic components are at work […].

A

simultaneously

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24
Q

List the PK components/factors:

A
  1. routes of administration
  2. absorption and distribution
  3. binding
  4. inactivation
  5. excretion
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25
Q

Absorption/distribution sites = […].

Target site = […].

Inactivation storage depot sites = […].

A

membranes of organs

neuron receptor

bone and fat

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26
Q

Depot binding:

A

drug binding to plasma proteins

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27
Q

How are drugs eliminated? What exactly is released?

A

biotransformation (metabolism)

metabolites are excreted

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28
Q

Inactivation can influence both the […] and the […] of drug effects.

A

intensity; duration

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29
Q

What are the two major methods of administration? What is involved?

A
  1. enteral– uses the GI tract

2. parenteral– include those that do not use the alimentary canal

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30
Q

The enteral method could administer through the […] or […].

A

oral cavity; rectal

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31
Q

Parenteral administration includes…

A

injection, pulmonary, and topical

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32
Q

Safest and easiest route of administration:

A

oral (PO)

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33
Q

What is the criteria for PO:

A
  1. dissolve in stomach fluids
  2. pass through stomach walls to blood capillaries
  3. resistant to destruction by stomach acid and enzymes
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34
Q

What medication is (at the moment) unable to be taken PO? Why?

A

insulin

it is destroyed by stomach acid and enzymes

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35
Q

Absorption:

A

movement of the drug from the site of drug administration to the blood circulation

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36
Q

When are drugs fully absorbed from the stomach?

A

when they reach the small intestine

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37
Q

What are some factors that influence the rate of absorption (3)?

A
  1. fatty food slows down the stomach
  2. amount of food consumed
  3. level of physical activity

etc…

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38
Q

First-pass metabolism (definition):

A

an evolutionary beneficial function to prevent the passage of harmful chemicals and toxins before passed on to other tissues/organs

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39
Q

What is the biggest ownfall to taking PO?

A

extensive metabolism may occur (more than 90%) reducing their bioavailability

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40
Q

Rectal administration is dependent on the […].

A

placement

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41
Q

If a suppository is placed on the lower end of the rectum…

A

it may avoid some first-pass metabolism

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42
Q

Deep placement of a suppository…

A

means drug is absorbed by veins that drain into the portal vein

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43
Q

For rectal administration, the bioavailability is […].

A

hard to predict

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44
Q

Intravenous is the […] and […] method.

A

most rapid; accurate

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45
Q

What are the dangers of IV?

A

quick onset leaves little time for corrective measure incase of overdose and allergies

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46
Q

Compared to IV, IM injection provides the advantage of…

A

slower and more even absorption over a period of time

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47
Q

Time of IM absorption:

A

10- 30 minutes

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48
Q

What can slow down the rate of IM?

A
  1. second drug that constricts blood vessels

2. suspension

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49
Q

Intraperitoneal injection (IP):

A

rarely used in humans but most common route for laboratory animals

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50
Q

Subcutaneous (SC) administration: the drug is […].

A

injected just under the skin

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51
Q

Use of a pellet or delivery device for SC […] the rate of absorption. Rubbing the area, and dilating the blood vessels on the other hand, […].

A

slows down; increases the rate

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52
Q

Why is inhalation fast-absorbing?

A

the area of pulmonary absorbing surfaces are large and filled with capillaries

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53
Q

Inhalation: The effect of the brain is […] because blood from […] travels only a short distance back to the […] before quickly heading to the brain via […]. which carries O2 generated blood to the […].

A

very rapid (seconds); the capillaries of the lungs; heart; carotid artery; head and neck

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54
Q

Inherent dangers of the inhalant drugs:

A

irritation of the nasal passages and damage to the lungs caused by small particles

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55
Q

Topical application of drugs to […] provide […].

A

mucous membranes; local effects

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56
Q

Some topically administered drugs can be readily absorbed into circulation. This is known as…

A

sublingual administration

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57
Q

Sublingual administration advantages:

A
  1. skips first metabolism
  2. quickly absorbs to capillaries and circulates
  3. not broken down by stomach acid/enzymes
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58
Q

Intranasal has what type of spread/effect?

A

local and sometimes widespread (more effective than oral)

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59
Q

What are the two advantages of intranasal administration?

A
  1. avoids first-pass liver metabolism (fast than oral)

2. bypasses the BBB and access the CSF and in between neurons

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60
Q

Transdermal through skin patches provides […] and […] at a preprogrammed rate.

A

controlled; sustained

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61
Q

Drugs with high lipid solubility move through cell membranes by […].

A

passive diffusion

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62
Q

The larger the difference in concentration of each side of a plasma membrane ([…]), the more […] is diffusion.

A

concentration gradient; rapid

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63
Q

Lipid solubility increases […] (2).

A
  1. ABSORPTION of drug into the blood

2. PASSAGE determines how readily a drug will pass the lipid barriers to enter the brain

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64
Q

Bioactivation is a […]; a substance that is dependent on […] to convert a(n) […] drug to a(n) […] one.

A

prodrug; metabolic reactions; inactive; active

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65
Q

What are the two factors that influence the extent of ionization?

A
  1. relative acidity/alkalinity (pH)

2. intrinsic property of the molecule (pKa)

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66
Q

The pKa of a drug represents the […] of the aqueous solution in which that drug would be […] ionized and […] nonionized.

A

pH; 50%; 50%

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67
Q

Drugs that are weak acids ionize more readily in…

A

an alkaline environment

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68
Q

Drugs that are weak acids become less ionized in…

A

an acidic environment

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69
Q

Ionization: A weak acid in the stomach compared to the intestine.

A

stomach– nonionized form; lack of electric charge means lipid soluble and readily absorbed to blood

intestine– pH is more basic in comparison; ionization increases and absorption is reduced

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70
Q

Intestine absorption advantages (2)

A
  1. greater surface area

2. slower movement of material

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71
Q

Drug redistribution: distribution of the drug from […] to […] in the body.

A

it’s target site; other areas/tissues

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72
Q

BBB purpose:

A

blood plasma that supplies brain cells with essentials and carries away waste products

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73
Q

CSF:

A

fluid that fills the subarachnoid space around the brain and spinal cord, ventricles, and canals

74
Q

CSF is manufactured by cells of the […], which line the cerebral […].

A

choroid plexus; ventricles

75
Q

BBB:

A

separation between brain capillaries and the brain/CSF

76
Q

What is the principal component of the BBB?

A

distinct morphology of brain capillaries

77
Q

Because the job of blood vessels is to […] to cells while […], the walls of typical capillaries are made up of […].

A

deliver nutrients; eliminating waste; endothelial cells

78
Q

Intercellular clefts:

A

small gaps in endothelial cells that allow small molecular passage

79
Q

Fenestrations:

A

larger openings in endothelial cells that allow large molecular passage

80
Q

Pinocytotic vesicles:

A

envelop and transport larger molecules through the capillary wall

81
Q

How are intercellular clefts opened and closed?

A

by adjoining the endothelial cells and forming tight junctions

82
Q

Surrounding brain capillaries are numerous glial feet– extensions of glial cells called…

A

astrocytes or astroglia

83
Q

What is the significant purpose of astrocytes?

A

contribute to both postnatal formation and maintenance of the BBB

84
Q

T/F: The BBB is impermeable.

A

false the BBB is selectively permeable (lipid-soluble passes)

85
Q

Area postrema, or […], is a […] in the brainstem that respond to […] in the blood and induces […].

A

chemical trigger zone; cluster of cells; toxins; vomiting

86
Q

Teratogens:

A

agents that induce developmental abnormalities in the fetus

87
Q

When is a child most susceptible to damaging effects during pregnancy? Why?

A

first trimester

around this time the fetus is developing organs

88
Q

Drug depots are also known as…

A

silent receptors

89
Q

What are drug depots?

A

inactive sites where drug binding occurs and no measurable biological effect is initiated

90
Q

Most notable silent receptor:

A

albumin (plasma protein)

91
Q

Any drug bound to depots cannot reach […], nor can they be […] by the […].

A

active sites; metabolized; liver

92
Q

T/F: Drug binding to drug depots is reversible?

A

true; when the blood level drops these unbind and circulate through the plasma

93
Q

Rapid binding to depots before reaching target tissue causes:

A

slower onset and reduced effects

94
Q

Depot binding: Explain the individual differences in amount of binding and how it might alter the dosages prescribed.

A

high– less free drug so some people seem to need higher doses

low– more free drug, so these individuals are more sensitive

95
Q

Competition among drugs for depot-binding sites:

A

higher than expected blood levels of the displaced drug, causing greater side effects and possibly toxicity

96
Q

**Unmetabolized bound drug:

A

drug remaining in the body for prolonged action

97
Q

Redistribution of drug to less vascularized tissues and inactive sites:

A

termination of drug action

98
Q

A steady-state plasma level is when the desired blood concentration of drug is achieved. How is this done?

A

absorption and distribution phase is equal to the metabolism and excretion phase

99
Q

First-order kinetics:

A

drugs are cleared though an exponential (half life) decline

100
Q

Zero-order kinetics:

A

drug molecules are cleared at a constant rate (no matter dosage)

101
Q

What is the prime example of zero-order clearance?

A

ethanol

although this can switch to first-order when biotransformation occurs at high levels of alcohol (toxication)

102
Q

Drug metabolism is the greatest in which organ?

A

liver

103
Q

List the 2 types of biotransformations:

A
  1. phase one

2. phase two

104
Q

What occurs during phase one of biotransformation?

A

NONSYNTHETIC MODIFICATION of the drug molecule by oxidation, reduction, or hydrolysis

105
Q

For phase one, what is the common modification of the drug?

A

oxidation

106
Q

What occurs during phase two of biotransformation?

A

SYNTHETIC MODIFICATION reactions that require the combination (conjugation) of the drug with small molecules

107
Q

List some of the small molecules that conjugate with phase 2 synthetic biotransformation (3):

Side Note: these small molecules are essential for converting/excreting these foreign substances (xenobiotics) out of the body.

A

glucuronide**
sulfate
methyl groups

**most common

108
Q

The two phases of drug biotransformation ultimately produce one or two […] which are […]. so they can be excreted more readily than their […].

A

inactive metabolite; water-soluble; parent drug

109
Q

After biotransformation of metabolites, what are the two paths for excretion?

A
  1. filtered out by kidneys

2. excreted into bile and eliminated with feces

110
Q

Microsomal enzymes:

A

liver enzymes primarily responsible for metabolizing psychoactive drugs

111
Q

Factors that influence an individual’s ability of drug metabolism (4):

A
  1. enzyme induction (increase of enzyme availability after stimulus)
  2. enzyme inhibition (decrease of enzyme availability after stimulus)
  3. drug competition
  4. individual differences in age, gender, genetics
112
Q

Repeatedly used psychoactive drugs cause an increase in what effect.

A

TOLERANCE: enzyme induction within the liver; the repeated stimulus will allow more enzymes to be available

113
Q

Increased number of enzyme molecules not only cause drugs to […] their own rate of […] by two-to threefold, but also can […] the rate of […] of all other drugs.

A

speed up; biotransformation; increase; metabolism

114
Q

Increased rate of biotransformation and increased number of enzymes leads to…

A

tolerance

115
Q

Enzyme inhibition can lead to…

Why?

A

toxicity

reduces metabolism of other drugs metabolized by the same enzyme

116
Q

MAOIs (antidepressants) can turn […] potentially life-threatening because of […].

A

normal foods; enzyme inhibition

117
Q

What food significantly inhibits biotransformation?

A

grapefruit juice

118
Q

Drug competition occurs for drugs that share […]. This can cause an […] of either drug […] of the second, causing potentially toxic levels.

A

a metabolic system; elevated concentration; reduces the metabolic rate

119
Q

Genetic polymorphisms:

A

genetic variations amoung individuals that produces multiple forms of a given protein

120
Q

What is an example of genetic polymorphisms (2)?

A
  1. acetylation: treat TB and subsequently found to relieve depression
  2. Asian groups and enzyme to break down alcohol
121
Q

What is the most important route of elimination?

A

urine through the kidneys

122
Q

Ionization of drugs reduces […] because it makes drugs less […].

A

absorption; lipid-soluble

123
Q

PD is the study of the […] and […] interaction of drug molecules with target tissue that is responsible for the ultimate effects of a drug.

A

physiological; biochemical

124
Q

Receptors can be known as…

A

protein molecules located on the cell surface or within cells

125
Q

Receptors are the […] of action of biologically active agents such as […], hormones, […] (all referred to as […]).

A

initial sites; neurotransmitters, hormones, and drugs; ligands

126
Q

A ligand is defined as any molecule that…

A

binds to a receptor with some selectivity

127
Q

List CNS stimulates:

A

amphetamine, cocaine, nicotine

128
Q

List CNS depressants:

A

barbiturates and alcohol

129
Q

List hallucinogens:

A

mescaline, LSD, psilocybin (shrooms)

130
Q

List psychotherapeutics:

A

prozac and throazine

131
Q

A receptor can be coupled either with…

A

an ion channel or with a G protein

132
Q

List the two types of receptors:

A
  1. EXTRACELLULAR those on the surface of the cell

2. INTRACELLULAR those within the target cell (cytoplasm or nucleus)

133
Q

Hormonal binding usually occurs […].

A

intracellularly (receptor is located within the target cell)

134
Q

Receptor agonists:

A

has best chemical “fit” (highest affinity); attaches readily to the receptor, and produces a significant biological effect

135
Q

Receptor antagonists:

A

also fit receptors but produces no cellular effect (low efficacy)

136
Q

Partial agonists:

A

ligands that bind to the agonist recognition site but trigger a response that is lower than that of a full agonist at the receptor

137
Q

Inverse agonists:

A

initiate a biological action that is opposite to that produced by an agonist, and also antagonize the effects of other agonists

138
Q

Long-term regulation is called […] when receptor numbers […] and […] when receptors are reduced.

A

up-regulation; increase; down-regulation

139
Q

Dose-response curve:

A

describe the extent of effect (response) produced by a given drug concentration (dose)

140
Q

Potency:

A

absolute amount of drug necessary to produce a specific effect

141
Q

On the dose-response curve, the position of the curves on the x-axis indicates […] and reflects the […].

A

potency; affinity

142
Q

Non-competitive antagonists are drugs that […] the effects of agonists.

A

reduce

143
Q

Physiological antagonism involves…

A

two drugs interact and reduce the effectiveness of both

144
Q

Potentiation refers to the situation in which the…

A

combination of two drugs produces effects that are greater than the sum of their individual effects (additive effects)

145
Q

Cross-tolerance:

A

development of tolerance to one drug can diminishing the effect

146
Q

List the following:

drug that induces tolerance rapidly

drug that requires weeks of tolerance

drug that doesn’t cause significant tolerance

A

LSD

barbiturates

antipsychotics

147
Q

T/F: Tolerance is reversible

A

yes when drug use stops

148
Q

Acute tolerance:

A

tolerance develops during just a single administration

149
Q

Example of acute tolerance:

A

alcohol

150
Q

Drug disposition tolerance or […] occurs when repeated use of a drug […] the amount of that drug that is available at the […].

A

metabolic tolerance; reduces; target tissue

151
Q

T/F: Drugs are capable of liver microsomal enzyme induction.

A

true

152
Q

When does pharmacodynamic tolerance occur?

A

changes in nerve cell function compensate for continued presence of the drug

153
Q

Why does the withdraw syndrome occur?

A

chronic drug user stops abruptly and and the mechanism remains functioning and causes a rebound

154
Q

The occurrence of the withdrawal or abstinence syndrome is the hallmark of …

A

physical dependence

155
Q

Behavioral tolerance (also known as […]) is seen when tolerance occurs in the same […] in which the drug was […].

A

environment; administered

156
Q

What can behavioral tolerance explain with overdoses?

A

chronic users may not be as tolerant to the drug in a different location, environmental cues can contribute to overdoses occurrences

157
Q

State-dependent learning: concept that is closely related to […]. Tasks learned under the influence of a psychoactive drug may subsequently be performed […] in the drugged state.

A

behavioral tolerance; better

158
Q

Sensitization is sometimes called […].

A

reverse tolerance

159
Q

Sensitization:

A

is the enhancement of particular drug effects after repeated administration of the same dose of the drug

160
Q

Pharmacogenetics:

A

study of the genetic basis for variability in drug response among individuals

161
Q

What is the goal of pharmacogenetics?

A

identify genetic factors that confer susceptibility to specific side effects, or predict therapeutic response

personalized medicine

162
Q

Should there be any alteration to the following dosage:

intermediary metabolizer; with one normal allele and one inactive polymorphism

A

slightly reduced dosage for plasma concentration

163
Q

Should there be any alteration to the following dosage:

patient with two highly functional genes (extensive metabolizers)

A

administered a somewhat high than normal dosage to ensure therapeutic effectiveness

164
Q

Should there be any alteration to the following dosage:

ultrarapid metabolizer (have additional high-functioning polymorphisms)

A

higher dosage to reach adequate plasma concentration for effective treatment

165
Q

Knowing genetic variation in metabolizing enzymes is beneficial to…

A

help individuals predict the bioavailability of a given drug so modifications produce optimum therapeutic concentrations

166
Q

Hormonal binding alters cell function by…

A

triggering changes in gene expression

167
Q

Efficacy:

A

capacity to initiate a biological action

168
Q

Competitive antagonists:

A

drugs that compete with agonists to bind receptors but do not initiate intracellular effects, reducing effect of the agonist

169
Q

Competitive antagonists can be replaced by…

A

an excess of agonist

170
Q

What are the three ways that noncompetitive antagonists reduce the effect of agonists:

A
  1. binding to the receptor at a site other than the agonist binding
  2. disturbing the cell membrane supporting the receptor
  3. interfering with cell processes that were initiated by the agonist
171
Q

Ways drugs act as agonists in the brain (2):

A
  1. enhancing synaptic function by increasing neurotransmitter synthesis or release
  2. prolonging action of the neurotransmitter within the synapse
172
Q

Ligand-receptor binding is […].

A

temporary

173
Q

Ligand binding causes change in receptor […] that […] a series of events in the cell.

A

shape; initiates

174
Q

Receptor proteins have a […]; the number and […] or receptors can also change.

A

lifespan; sensitivity

175
Q

Upregulation:

A

number of receptors increases

176
Q

Downregulation:

A

number of receptors is reduced in response to absence of ligands or chronic activation

177
Q

Comparing […] of different drugs shows differences in potency.

A

ED50

178
Q

TD50 (50% toxic dose):

A

dose at which 50% of the population experiences a toxic effect

179
Q

Therapeutic index (TI) =

A

TD50/ED50

180
Q

What are examples of pharmacodynamic tolerance:

A
  1. receptor down regulation

2. receptor up-regulation

181
Q

Operant conditioning may also play a part in […] tolerance

A

behavioral

182
Q

The cytochrome […] have many polymorphisms that affect drug levels.

A

P450 enzyme family

NPP (9 decks)

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