module 1 Flashcards

1
Q

pharmacology can be defined as

A

the science of drugs, there uses effects and mechanisms

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2
Q

historical influences on modern pharmacology

A

discoveries of ancient civilization , the roles of poison and the influence of religion

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3
Q

380 BCE

A

Pupil of Aristotle wrote book that included opium

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4
Q

1803 in germany,

A

Serturner, a pharmacist isolated crystals of morphine from opium and discovered its pain relief capability

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5
Q

opium contains

A

10% morphine and 0.5% codeine and was given the name from from morpheus god of dreams

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6
Q

earliest recorded drug experiments

A

China in 2700 BCE in which ma Huang was used to treat flus and cough. –> today ephedrine has been isolated from the ma Huang plant to treat asthma

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7
Q

ancient Egypt and drugs

A

ebers papyrus in 1550 BCE was used as a medical textbook

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8
Q

Curare is

A

plant derived drug in South America that was used as a poison to hunt animals. Causes paralysis of muscles and eventual death my respiratory paralysis

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9
Q

in modern medicine curare was used as

A

anesthetists in surgery

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10
Q

what is ergot ?

A

a poisonous fungus found on the head of rye and is found in abundance during wet seasons

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11
Q

ergot effect on nervous system

A

mental frenzy , hallucination and convulsions

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12
Q

ergot effect on cardiovascular system

A

can cause constriction of blood vessels , limiting blood supply to fingers and toes and limbs which will eventually become black and die off

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13
Q

ergot and reproductive system

A

can cause violent contractions of the uterus , was sometimes used for labour

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14
Q

ergotamine

A

a compound derived from ergot and is useful in treating migraines through contstriction of blood vessels

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15
Q

ergonovine

A

compound of ergot that is used to hasten birth as to force uterine contractions. can also be used to stop bleeding after birth

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16
Q

religion and drugs

A

ancient societies healers were doctors and priests , plants were used to alter state of conciusness to be able to talk to the gods
ex) Peyote in Mexico, has LSDA properties

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17
Q

A drug can be defined as

A

substance received by a biological system that is not received for nutritive purposes and will influence the biological functions on an organism - chemicals , biological agents and herbal products are all considered drugs

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18
Q

drugs that act on the brain

A

alter the normal signalling ex) LSD

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19
Q

How was LSD discovered

A

Albert hofman who worked for Swiss pharmaceutical firm , synthesized LSD and chemical structure was similar to ergotamine and ergonovine

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20
Q

LSD contribution to pharmacology

A

certain mental illness might be due to production of potent substances in the brain and produce psychiatric disturbances

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21
Q

1900’s what drug came out ?

A

organoarsenicals designed by Paul ehrlich which would bind to parasites and cured syphilis

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22
Q

1930s drug discovery

A

sulpha drugs which were the first synthetic drugs to treat bacterial infections

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23
Q

antibiotic refers to

A

specifically to chemical substances produced by microorganism and not synthetic compounds

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24
Q

drug discovery in 1940s

A

Fleming discovered the first antibiotic known as penicillin and was used for gram positive disease

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25
Q

drug discovery in the 1950s’

A

Waksman discovered discovered streptomycin antibiotic which was a turning point of tuberculosis and gram negative bacterial disease

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26
Q

what are the 5 key steps of drug discovery ?

A

basic research/ drug discovery, preclinical trials , clinical trials, health Canada review , post market surveillance and phase IV clinical trial

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27
Q

what is the first stage in basic research

A

identification of the target, where a receptor is identified

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28
Q

step 2 in basic research

A

studying the target, in which a lead compound is identified and enters into more testing to look at safety and efficacy

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29
Q

pharmacological studies of new drugs are used to

A

determine the detailed mechanism of action of the new drug

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30
Q

toxicology studies of new drug entail,

A

the possible risk or harm of new drug , acute toxicity and chronic toxicity are looked at

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31
Q

if company wants to test new drug on people what 3 things need to fist take place

A

1) investigation - submission to highly qualified scientists who will approve admission
2) methodology, of the proposed clinical trial in humans
3) proof of safety- must be shown to be safe with several animal models and be submitted to the health products and food branch

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32
Q

what are phase 1 clinical trials

A

carefully evaluate absorption, distribution and elimination and adverse effects of new drug - efficacy is not assessed however tolerability is looked at with 20- 80 volunteers

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33
Q

phase 2 clinical trial

A

trying to determine if the drug is effective in a limited number of people ( 100- 500). drug safety is carefully looked at

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34
Q

phase 3 clinical trial

A

also known as randomized control trials and are the main studies used for marketing of drug

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35
Q

number of participants and phase 3 trial and duration

A

test drug in larger number of people( 1000+) and range from months to years

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36
Q

goals of phase 3 trial

A

to determine how safe and effective the drug is compared to no treatment ( placebo)

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37
Q

location and cost of phase 3 trials

A

are considered multicenter and take place in many cities and can cost from 1 million to 50 million

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38
Q

what are the 3 larger stages of phase 3 clinical trials

A

1- determining enrolment prior to the study
2-allocating participants to treatment groups
3-monitoring and analyzing results

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39
Q

the target population includes

A

group of patients for who the drug is intended ex) drug to treat hypertension , adults who have been clinically diagnosed with it would be target population

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40
Q

study population is

A

subset of the target population , 2 factors that influence this is inclusion/ expulsion criteria and consent

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41
Q

why are comorbities often included ?

A

to be representative of target population

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42
Q

obtaining consent means that

A

document which outlines purpose of study , the procedures that will be used and possible risks and benefits

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43
Q

what is meant by double blind design

A

neither investigator or participant is aware of treatment assignment group
- bias can occur otherwise

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44
Q

what is randomization ?

A

when patients are assigned to either treatment group or to control group in a random fashion

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45
Q

why is randomization used

A

ensures that confounding variables ( known and unknown ) are distributed equally between the 2 groups - and also removes possible bias in assigning patients to groups

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46
Q

placebo is

A

identical to experimental drug but does not contain the active ingredient , there is often placebo effect when taking drugs in which symptoms get better

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47
Q

Gold standard drug is known as

A

accepted by the medical community as the best available treatment for the given condition

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48
Q

when analyzing results what3 things need to be considered ?

A

compliance, quality of life and statistics

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49
Q

patient compliance refers to ?

A

how often the participant took the drug

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50
Q

what is meant by bioequivelant ?

A

both generic and brand name drugs will contain the same active ingredient and give similar blood levels

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51
Q

what is a receptor ?

A

molecule or complex of molecules located outside or inside the cell that has regulatory or functional role in the organism

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52
Q

receptors are bound to and activated by

A

endogenous ligands which are substances found in the body like hormones and neurotransmitters

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53
Q

location of receptors will determine

A

where the drug will act and whether the response that results from the drug - receptor interaction is beneficial or detrimental

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54
Q

how does opioid receptors location result in different effects ?

A

when they bind to receptors in the brain , causes pain relief , when they bind to receptors in stomach, causes constipation

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55
Q

other drug targets include

A

chemical reactions and physical chemical forces

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56
Q

chemical reactions include ?

A

when antacid neutralizes the stomach through aid base neutralization

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57
Q

how does cholestyramine work ?( physical chemical force )

A

binds to bile acids in GI tract preventing their reabsorption and increasing the elimination of bile salts that are used to make cholesterol

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58
Q

agonists are known as

A

drugs that bind to stimulate a receptor

59
Q

antagonists are known as

A

bind to receptor but block response of receptor –> will not activate receptor

60
Q

most drugs will

A

mimic the action or block the endogenous ligand at a receptor

61
Q

dose response relationship

A

pharmaocologcial effect will increase in proportion to the dose

62
Q

problem with the alcohol and cannabis study

A

there was a wide discrepancy between the doses of cannabis and liquor

63
Q

what things should be asked when comparing alcohol and cannabis ?

A

quantity, frequency of use, user demographic, environmental factors

64
Q

low dose and drug response

A

very little response will be observed and little receptors will be activated

65
Q

threshold and drug response

A

more receptors activation until a desired response is seen - a certain number of receptors are needed to see a response

66
Q

therapeutic doses

A

once threshold is reached , small increases in dose will result in large increase in response

67
Q

maximal effects

A

once maximal effect has been reached, there will be no difference in the therapeutic response seen

68
Q

dose response curve

A

representation of how much drug you need in the body to see a specific effect

69
Q

Y axis

A

effect of drug iron Y axis and plotted on a linear scale

70
Q

receptor threshold

A

region of the curve , where threshold has been reached and dose of the drug is directly proportional to the response

71
Q

X axis

A

dose of the drug is on this axis and is plotted on a log scale

72
Q

ED 50

A

dose of the drug that will result in 50% of the maximal effect- also be interpreted as the dose that is effective in 50% of pop

73
Q

Efficacy

A

maximum pharmacological response that can produced by a specific drug

74
Q

Potency

A

dose of drug that is required to produce a certain magnitude , usually 50% of the maximal response

75
Q

therapeutic range is referred to as

A

a dose that keeps the blood concentration of a drug above the minimum concentration that produces the desirable effect but below the toxic response

76
Q

What is pharmokinetics ?

A

movement of a drug into and throughout he body and then leaving the body

77
Q

what are the 3 route of drug administration ?

A

topical ,enteral and parenteral

78
Q

what happens after administration ?

A

absorption, distribution, metabolism and excretion (ADME) which will determine the concentration in the blood

79
Q

topical administration

A

drugs that are directly applied directly to the body ( on the skin, through the skin or inhalation )

80
Q

enteral administration refers to

A

through the GI tract either directly through the mouth or an artificial opening ( mouth, rectum or sublingual or buccal * under tongue

81
Q

Parenteral refers to administration through

A

bypasses the GI tract includes intravenous , intramuscular or subcutaneous

82
Q

drugs absorbed through the skin can produce

A

a systemic effect which could be toxicity other parts of the body

83
Q

what is transdermal drug delivery?

A

application of drug from the skin to be absorbed into the general circulation ( nicotine patch )- bypasses the enzymes of stomach

84
Q

inhalation can have

A

local and systemic effects and can be advantageous because a smaller amount is often needed to see systemic effect which reduces the chances of toxicity

85
Q

Enteral administration enter the blood through

A

The GI tract which then brings it to the liver, which decreases the amount of active drug–> known as the first pass effect

86
Q

mouth administration

A

most convenient and least expensive and is the most common way drugs are administered

87
Q

rectum administration

A

systemic or local effect, less invasive route for those in comatose and digestive enzymes in the stomach are bypassed

88
Q

disadvantage of mouth administration

A

variable absorption for patients

89
Q

disadvantage of rectum administration

A

limited number of medications are available and absorption is slow and incomplete

90
Q

sublingual and buccal administration advantages

A

enzymes in the stomach and liver are bypassed

91
Q

disadvantages of sublingual and buccal administration

A

not all drugs are adequately absorbed from, drug may be swallowed in which it behaves as if taken orally

92
Q

Parenteral administration route

A

injected into the body and enter blood stream directly

93
Q

intravenous administration

A

immediate effects, can be used for drugs that are poorly absorbed however has the highest risk of drug reactions as it is irreversible and free of fever producing substances

94
Q

intramuscular administration

A

drug injected into deep muscle where the volume f drug is limited to 2-3 mm

95
Q

subcutaneous administration

A

drug is injected into deepest layer of skin, allows for the timing of release of drug to be controlled

96
Q

bioavailability :

A

fraction of administered dose that reaches systematic circulation ( blood) in active form , intravenous is 100% bioavailable

97
Q

what is absorption ?

A

movement of drug from the site of administration into the blood

98
Q

Distribution ?

A

the movement of a drug from the blood to the site of action and tissues

99
Q

If the concentration of the drug in the blood drops below concentration at any of the sites what will happen ?

A

drug from the site will move to the blood to try and maintain the equilibrium –> distribution sites and blood concentrations are always in equilibrium

100
Q

what is metabolism ?

A

aka biotransformation , is the conversion of a drug to a different chemical compound in order to eliminate it –> products are known as metabolites

101
Q

where do most biotransformations take place and why ?

A

In the liver,( also can happen in the intestines, lungs and skin) a drug must be water soluble to be eliminated by the kidneys

102
Q

P450

A

enzymes that are capable of biotransforming drugs, found in most tissues ( lots in liver)

103
Q

biotransformation is divided into 2 phases:

A

1 and 2

104
Q

phase 1 biotransformation

A

purpose is to add or unmask a functional group on the drug to prepare it for the addition of a large water soluble molecule in phase 2

105
Q

phase 2 biotransformation

A

add a large water soluble moiety (molecule ) that is usually sulphate or glucronic acid making it water soluble for the kidney

106
Q

When taking multiple drugs, what could happen with metabolism

A

drugs will compete for the same enzyme (p450) which could reduce biotransformation and cause toxic effects

107
Q

drug excretion is classified as :

A

moving the drug and metabolites out of the body

108
Q

kidney and drug excretion

A

majority of drugs are eliminated by the kidney , water soluble drugs ill be excreted in urine , lipid soluble drugs go back into the blood

109
Q

Gi tract and excretion

A

some drugs are excreted in the form of feces after gone through the liver biotransformation

110
Q

Excretion and the lungs

A

drugs that are volatile or in a gaseous form, can be excreted in this way ( alcohol and anethsetics )

111
Q

Breast milk and excretion

A

a minor way that drugs are excreted however can effect nursing women and exposing toxic levels of drug to baby

112
Q

saliva and sweat and excretion

A

presence of drugs can be found here, commonly found with the misuse of certain drugs

113
Q

half life of drug =

A

the time that the kidney and the liver need to remove half of the drug from the body , can be used to administer therapeutic doses and make sure that there is enough in circulation in blood

114
Q

2 ways that drugs get out of body=

A

biotransformation and excretion

115
Q

what are the 5 stages the drug goes through after administration

A

absorption from the site, distribution to the site of action, target interaction, metabolism and excretion

116
Q

variation in drug response includes

A

genetic factors, environmental factors, disease states, altered physiological states , presence of other drugs

117
Q

genetic variability and drugs ?

A

way in which the boy eliminates the drug and way in which it binds to receptors , biotransformation can vary ( fast vs slow )

118
Q

environmental factors ?

A

exposure to certain chemicals can increase liver enzymes –> chronic alcohol consumption will increase enzymes

119
Q

disease states and metabolism

A

liver disease= slower metabolism of drugs , and kidney and cvd disease

120
Q

elderly will see what type of effects with drugs

A

will have slower acting metabolism due tor educed kidney function and will see increased drug action especially on CNS

121
Q

adverse drug reaction is defined as

A

any effect produced by a drug that is not its intended effect

122
Q

extension of therapeutic effect

A

when there is too much of the drug in the blood ( overdose )

123
Q

unrelated to the main action of the drug

A

side effects that are unrelated to the intended pharmacological effect

124
Q

allergic reaction

A

adverse effect mediated by the immune system

125
Q

withdrawal and addiction

A

unwanted physiological or psychological effects of the drug

126
Q

teratogenesis

A

when drug produces defects in the fetus

127
Q

adverse biotransformation reaction

A

conversion to a chemically reactive metabolite that can bind to tissue and cause damage

128
Q

why is predicting adverse drug reactions hard ?

A

= may only occur after prolonged periods of use , may be also be very rare , may not be detectable in animals ,certain drugs may have adverse effect at specific times ( during pregnancy )

129
Q

Therapeutic index

A

tells you how safe a drug is , compared does for therapeutic effect vs dose where toxic effect are seen, lower the index, the more toxic

130
Q

therapeutic index formula =

A

TD50( toxic dose 50- dose that is toxic in 50% of pop

/ effective dose 50- dose that is effective in 50 % of pop

131
Q

what is a drug to drug interaction ?

A

one drug changes the pharmacological effect of the second drug

132
Q

absorption and drug to drug interactions

A

absorption can be decreased by increasing intestinal movements, and limiting interaction with the intestine wall

133
Q

how is metabolism effected by drug interactions ?

A

a drug can block the inactivation of a second drug in the liver , increasing blood level and effect of 2nd drug

134
Q

how is excretion effected by drug interactions ?

A

a drug can facilitate the excretion of a second drug by the kidney decreasing the blood levels and effect of second drug

135
Q

what is the problem with tyramine found in cheese ?

A

capable of raising blood pressure and is broken down in the liver by MAO–> problem for people taking MAO inhibitors , tyramine will not be broken down and blood pressure effects will be intensified

136
Q

what is the problem with grapefruit ?

A

inhibits drug metabolizing enzymes in the GI tract , meaning a greater amount of the drug can be absorbed which could possibly lead to overdose

137
Q

the limbic system contains

A

dopaminergic reward centres in the brain that also integrates memory , reward and emotion ( with hypothamulus controls emotion and behaviour

138
Q

cerebral cortex ( cerebrum)

A

largest part of brain - sensory, motor, coordination , vision , , judgement , speech ,consciousness

139
Q

the neuron

A

generates electrical signals and is the functional unit of brain - neuroplasticity = new connections
neurogenesis = new neurons

140
Q

cell body / soma

A

contains the neurotransmitters and is the largest part of neuron and has the nucleus

141
Q

dendrites :

A

receiving antennae for incoming signals

142
Q

axons

A

single fibre that extends from the cell body and ends at synapse , carries electrical pulses to other neurons

143
Q

the synapse

A

junction between 2 neurons

144
Q

synaptic transmission

A

aka neurotransmission , chemical in nature , substance that is quickly released that activates next neuron