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Pharm > Midterm 1 > Flashcards

Midterm 1 Flashcards

1
Q

UDP-glucuronosyltransferases (UGTs)

localized, what does it do, why?

A

Phase 2 Metabolism
In smooth ER
Transfers glucuronic acid (sugar) to drug
Makes them more polar –> to excrete

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2
Q

Sulfotransferases (SULTs)

A

Phase 2 Metabolism
Cytosolic
Transfer sulfate group to hydroxyl group
Make them more polar –> to excrete

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3
Q

Glutathione S Transferases (GSTs)

A

Phase 2 Metabolism
Cytosolic
Transfer glutathione to drug
Makes toxic drugs not toxic

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4
Q

N-acetyltransferases (NATs)

A

Phase 2 Metabolism
Cytosolic
Transfer acetyl group to drug
Subject to genetic polymorphisms

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5
Q

Thiopurine Methyltransferase (TPMT)

A

Phase 2 Metabolism
Cytoslic
Transfer methyl group to drug
Subject to genetic polymorphisms

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6
Q

What does cytochrome P450 do? What is another name?

A

CYPs
Phase 1 metabolism - can be less, more or equally active
oxidizes drugs - can make them

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7
Q

CYP2C9 - phase 1 or 2 SNP? explain

A

Phase 1 SNP
Metabolizes anticoagulant drug warfarin
SNP causes decreased activity in enzyme
Patients with this SNP should receive a lower dose of warfarin or they may experience extensive bleeding

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8
Q

CYP2D6 - phase 1 or 2 SNP? explain

A 
Phase 1 SNP
Metabolizes codeine to morphine (more potent analgesic)
Polymorphisms result in 4 phenotypes:
- ultra rapid 
- extensive (normal)
- intermediate
- poor
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9
Q

UGT1A1 - phase 1 or 2 SNP? explain

A

phase 1 SNP - UGT family
Glucoronidates anti-cancer compound SN38
Polymorphisms decrease activity
Increased risk of diarrhea and bone marrow suppression

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10
Q

NAT2 - phase 1 or 2 SNP? explain

A

Phase 2 SNP
Acetylates the drug isoniazid, caffeine and cancer chemicals
SNP can either cause rapid or slow acetylators
Slow acetylators = isoniazid toxicity and high risk of cancer

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11
Q

First Order Kinetics

A

More enzyme than drug
Metabolism directly proportional to concentration of free drug
Constant fraction of drug metabolized/time

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12
Q

Zero Order Kinetics

A

More drug than enzyme
Metabolism is constant over time
Constant amount of drug metabolized/time

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13
Q

Drugs eliminated in the bile include:

A
  1. high molecular weight
  2. amphipathic
  3. glucuronidated
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14
Q

If a drug is amphipathic which transporter transports it into the bile?

A

P glycoprotein

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15
Q

If a drug is glucuronidated which transporter transports it into the bile?

A

MRP2

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16
Q

What transporter transports drugs into breast milk?

A

BCRP

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17
Q

Drugs excreted in the breast milk are:

A
  1. low protein binding
  2. low molecular weight
  3. high lipophilicity
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18
Q

The most important parameters determining drug disposition in humans are?

A

Clearance
Volume of distribution
Elimination half life
Bioavailability

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19
Q

Drug concentrations are usually measured in __

A

plasma

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20
Q

What is the formula for dosing rate?

A

Dosing rate = plasma concentration x clearance

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21
Q

What is the formula for half life?

A

T1/2 = (0.693 x Vd) / clearance

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22
Q

Why is knowing a drugs clearance important?

A

to know dosing rate

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23
Q

Why is knowing a drugs half life important?

A

for knowing how long it takes to reach steady state and how long it takes for drug levels to decline once it has stopped being administered

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24
Q

When the SAME dose of a drug is administered repeatedly, it takes about ___ half lives to reach steady state

A

5 half life to reach steady state

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25
Q

If the dose of a drug remains constant, the time to reach steady state is (dependent or independent) of the size of the dose

A

independent
e.g. it will take the same time for a 3 mg dose of x and a 1mg dose of x to reach steady state (however, the 3 mg dose will have a high steady state concentration)

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26
Q

What is loading dose used for? What is the formula?

A

If the drug has a long half life - to decrease the time it takes to reach steady state

Loading dose = target drug plasma concentration x Vd

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27
Q

How long does it take for most of a drug to be eliminated from the body? How long does it take for every molecule to be eliminated?

A

Most = 5 half lifes

Every molecule = 9 half lives (important for allergic reaction)

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28
Q

How do we evaluate pharmacodynamics?

A

dose-response curves

these are MONOTONIC and NOT linear

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29
Q

What is efficacy?

A

How effective a drug is at a given dose

the maximal height

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30
Q

What is potency?

A

the amount of a drug required to elicit a pharmacological response

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31
Q

Does high potency mean a drug is more effective?

A

no

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32
Q

How is potency determined?

A

comparing the dose require to produce half maximal response (ED50)

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33
Q

Is a low ED50 or high ED50 more potent?

A

low ED50

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34
Q

What is an important example of a ligand gated ion channel?

A

GABA receptor
GABA (neurotransmitter) binds to GABA receptor it opens channel to let chloride ion into cell
Benzodiazepine drugs bind to GABA receptor too!
Causes sedation and muscle relaxation

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35
Q

Is the response to ligand gated ion channels fast or slow?

A

fast - milliseconds

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36
Q

G protein coupled receptors (GPCRs) have what three components?

A
  1. 7 transmembrane protein receptor
  2. g protein with three subunits
  3. effector molecule (i.e. enzyme)
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37
Q

Are the responses to GPCRs fast or slow?

A

seconds to minutes

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38
Q

Examples of GPCRs endogenous neurotransmitters

A

norepinephrine
seretonin
HISTAMINE

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39
Q

Structure of enzyme linked receptors?

A

span the membrane
ligand binding domain on outside
enzyme catalytic site on inside

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40
Q

Are the responses to enzyme linked receptors slow or fast?

A

fast - seconds

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41
Q

Example of an enzyme linked receptor?

A

Insulin
binding of insulin to insulin receptor causes enzyme mediated phosphorylation of the effector to activate it which then causes increased glucose uptake into the cell

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42
Q

Another name for intracellular receptors?

A

transcription factors

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43
Q

How does an intracellular receptor work?

A

Ligand must be able to cross cell membrane
Ligand binds and causes translocation to nucleus and binding to DNA
When ligand/receptor complex binds to DNA, transcription begins

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44
Q

Are intracellular receptors fast or slow?

A

relatively slow - takes hours/days to make proteins

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45
Q

Example ligands for intracellular receptors?

A

estrogen and testosterone - lipid soluble

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46
Q

If drugs only bind to one receptor how can they still have side effects?

A

If there are types of those receptors in different tissues (ex. brain vs intestine)

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47
Q

Drugs with a high affinity have __ ____

A

high potency

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48
Q

Drugs with high intrinsic activity have __ ___

A

high efficacy

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49
Q

Agonists have both _ and _

A

affinity and intrinsic activity

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50
Q

Agonists can ___ a physiological response

A

increase or decrease

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51
Q

Low dose of dopamine binds to ___. And causes __

A

dopamine receptor

Causes: renal artery dilation - increase BF

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52
Q

Moderate dose of dopamine binds to ___

A

B1 adrenergic receptor

Increase CO

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53
Q

High dose of dopamine binds to ___. And causes __

A

Alpha adrenergic receptor

Causes: renal artery constriction - decrease BF

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54
Q

Antagonists have __

A

have affinity but NO intrinsic activity because

they bind but not activate receptors

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55
Q

Would an antagonist do anything if there was no agonist present?

A

NO! - agonist must be present

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56
Q

Partial agonists have ___

A

affinity but very little intrinsic activity

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57
Q

What are the three types of drug tolerance?

A

1) desensitization - less receptors on surface
2) metabolic tolerance - induction of metabolizing enzyme
3) tachyphylaxis - rapid decrease in drug response

58
Q

Continuous exposure to antagonist can cause?

A

receptor upregulation - hypersensitivity to drug

59
Q

Phase 2 clinical trials determine what?

A

dose response

60
Q

Where is the ED50 on a frequency distribution curve?

A

at the peak

61
Q

What is ED50? What is its relevance?

A

the dose required to produce a response in 50% of the population

often used as initial dose for therapy IF the drug has a wide therapeutic range

62
Q

What is the formula for therapeutic index?

A

TI = TD50/ED50

or

TI = LD50/ED50

63
Q

Are drugs with a high or low therapeutic index considered safe?

A

high TI = safe

64
Q

How do doctors adjust drug dose for obese people?

A

body surface area (BSA)
normal BSA for adult = 1.73m2

dosed as mg/1.73m2

65
Q

List three gender differences in response to drugs

A

Females are slower at metabolizing alcohol
Opioids are more effective in women
Drugs used to treat irregular heart beat cause prolongation of QT interval in women - leading to fatal cardiac dysrhythmia

66
Q

People with kidney disease experience…

A

Decreased drug excretion
This causes increase in half life
Hepatic and intestinal drug metabolism is also decreased
Net effect: increased bioavailability and decreased excretion

67
Q

People with liver disease experience…

A

Decreased hepatic drug metabolism

Half life increased in drugs

68
Q

Examples of environmental factors affecting drugs

A

Cigarette smoke induces enzymes = drug less effective
Alcohol can make drugs toxic
Exercise improves action of insulin
Pesticides can induce CYPs - decrease response to drugs

69
Q

What drug classes cause allergic reactions?

A

Penicillins
Sulfonamides
NSAIDs

70
Q

Idiosyncratic Reaction

A

Occur rarely and unpredictably in the population
Related to genetic polymorphisms
Mostly occur in metabolizing enzymes and transport proteins

71
Q

6-mercaptopurine is metabolized by___

A

TMPT

72
Q

CYP2C9 polymorphism

A

Decreased metabolism

73
Q

CYP2D6 polymorphism

A

People are poor metabolizers and do not experience pain relief when they take codeine (prodrug)

74
Q

TMPT polymorphism

A

Decreased activity of TMPT causes life threatening bone marrow suppression when drugs metabolized by TMPT are given

75
Q

OATP1B1 what is it? polymorphism

A

Uptake transporter in the liver
Polymorphism causes decreased function
Increase in plasma drug concentration
Myopathy in patients taking statin drugs

76
Q

G6PDH what is it? polymorphism

A

Enzyme important in red blood cell metabolism
Polymorphism causes deficiency leading to red blood cell hemolysis following treatment with analgesics (aspirin) or anti-malarial drugs

77
Q

Diethylstilbestrol

A

Drug used to prevent spontaneous abortion during high risk pregnancies
Years later determined to cause vaginal or uterine cancer in female offspring

78
Q

How are drugs tested for their potential as a mutagen?

A

Ames test - ability of compound to cause mutation in specialized strains of bacteria

79
Q

Mutagenic

A

Able to change DNA

80
Q

Teratogens

A

Produce birth defects (physical, behavioral, etc) or impair fertility

81
Q

When do gross malformations usually occur when exposed to a teratogen?

A

1st trimester

82
Q

When exposed to teratogens in the second and third trimester what is disrupted?

A 
function
NOT gross anatomy
83
Q

When is transfer of drugs across the placenta the greatest?

A

third trimester

surface area of placenta increases

84
Q

What category drug is safest from pregnancy?

A

category A
(A, B, C, D, X)
X - the potential risks outweigh benefits

85
Q

The most important organ specific toxicity is observed in the __ and ___

A

liver and heart

86
Q

What is the most common reason for a drug to be removed from the market?

A

hepatotoxicity

87
Q

Signs of liver toxicity

A

Jaundice, dark urine, light coloured stool, nausea and vomiting

88
Q

What else should be performed for patients taking hepatotoxic drugs?

A

Liver function tests to measure blood levels of AST (aspartate aminotransferase) and ALT (alanine aminotransferase)

These SHOULD be in low concentration

89
Q

Who is at risk for liver disease?

A

Alcoholics

90
Q

What does the QT interval represent on an ECG?

A

the time it takes for the ventricles to repolarize

91
Q

Prolongation of the QT interval is a risk factor for development of ___. Which is a __

A

Torsades de Pointes

A life threatening form of ventricular arrhythmia

92
Q

Drugs that prolong the QT interval should be used with caution in patients predisposed to arrhythmias including:

A 
Elderly
Bradycardia patients
Heart failure patients
Low potassium
Congenital QT prolongation
Women at higher risk than men b/c normal interval is longer
93
Q

Classes of drugs that have consequences with rapid withdrawl

A

Opiates - anorexia, irritability, nausea, weakness
Benzodiazepines - anxiety, insomnia, tremors, paranoia
Beta blockers - rebound hypertension, chest pain, heart attack

94
Q

What are the most common cause of adverse drug reactions?

A

Medication errors

95
Q

What is it called when a medication error is caused by a health care professional?

A

Iatrogenic error

96
Q

5 Categories of Medication Errors

A
  1. Prescribing
  2. Dispensing
  3. Administration
  4. Patient education
  5. Patient
97
Q

Plendil
Nicoderm
Flomax
Dioval

A

Pletal
Nitrodrem
Volmax
Diovan

98
Q

Medication errors can be caused by __ and __

A

Similar drug naming

Abbreviation

99
Q

IU is misinterpreted as ___. Write __ instead

A

IV

write units

100
Q

q.d is misinterpreted as ___. Write __ instead

A

qid

write every day

101
Q

q.o.d is misinterpreted as ___. Write __ instead

A

qd or qid

write every other day

102
Q

trailing zero is misinterpreted as ___. Write __ instead

A

e.g. 1.0 misinterpreted as 10

do NOT use trailing zeros for doses expressed in whole units

103
Q

missing leading zero is misinterpreted as ___. Write __ instead

A

e.g. 0.5 misinterpreted as 5

use zero before dose when less than whole unit

104
Q

MgSO4 is misinterpreted as ___. Write __ instead

A

morphine sulfate

write magnesium sulfat

105
Q

MSMSO4 is misinterpreted as ___. Write __ instead

A

magnesium sulfate

write morphine sulfate

106
Q

Most common type of drug drug interaction are those affecting ___

A

pharmacokinetics (ADME)

107
Q

The average 65 year old take __ medications a day

A

7

108
Q

When drugs interact there are 3 possible outcomes:

A

Increased effect
Decreased effect
New effect

109
Q

Increased drug effects can be __ or __

A

increase in therapeutic

increase in adverse effect

110
Q

Example of an increased therapeutic effect

A

Ampicillin - antibiotic rapidly inactivated by enzymes

Sulbactam - inhibitor of enzymes inactivating ampicillin

111
Q

Example of an increased adverse effect

A

Warfarin - anticoagulant (blood thinner)
Aspirin - analgesic (also blood thinner)

Together - bleeding with potentially life threatening side effect

112
Q

Decreased drug effects can be __ or ___

A

Decrease therapeutic

Decrease adverse effect

113
Q

Example of decreased therapeutic effect

A

Clopidogrel - anticoagulant prodrug activated by CYP2C19

Omeprazole - drug used to treat ulcers - inhibits CYP2C19

Together clopidogrel is not activated - insufficient coagulation

114
Q

Example of decreased adverse effect

A

Morphine - analgesic used for pain - overdose = coma, respiratory depression

Naloxone - competitive antagonist

115
Q

Example of new effect

A

Disulfiram - drug used to treat chronic alcoholism
Alcohol metabolized to acetylaldehyde (hangover stuff) to acetic acid
Disulfiram inhibits metabolism of acetylaldehyde

When you mix disulfiram and alcohol - severe hangover symptoms

116
Q

4 Types of Drug Interactions

A

Direct Physical
Pharmacokinetic
Pharmacodynamic (affect receptor binding)
Combined Toxicity

117
Q

What is the most common direct interaction? What happens?

A

Two IV solutions are mixed

A precipitate forms

118
Q

What drug is particularly bad for direct interactions?

A

Diazepam

Never mix with another drug

119
Q

Example of direct interaction

A

Sodium bicarbonate followed by calcium gluconate - precipitate forms

120
Q

Types of pharmacokinetic interaction

A

Absorption - altered pH, chelation/binding, altered BF, gut motility, vomiting, drugs that kill intestinal bacteria
Distribution - altered pH, protein binding
Metabolism - CYP induction, CYP inhibition
Excretion - altered blood flow, altered pH, tubular secretion

121
Q

Example of altered pH affecting absorption

A

Antacids - increase gastric pH - increasing absorption of drugs that are weak bases in stomach

Also, enteric coated tablets dissolve prematurely in stomach

122
Q

What is chelation/binding?

A

Drugs bind to other drugs to form insoluble complex that cannot be absorbed

123
Q

Example of chelation/binding

A

Bile acid sequestrants (drug) bind intestinal bile acids to prevent absorption in the intestine and be excreted in feces

E.g. cholestryamine - sequestrant

124
Q

Example of altered blood flow affecting absorption

A

Local anesthetic + epinephrine

Epinephrine causes vasoconstriction which decreases absorption and allows the anesthetic to stay at the injection site

125
Q

Example of altered gut motility affecting absorption

A

Laxatives increase gut motility (to treat constipation)
Increased gut motility = decreased absorption

Opiates decrease gut motility - AKA morphine

126
Q

How does vomiting affect absorption?

A

Vomiting = decrease absorption
If vomiting occurs 20-30 minutes after taking a medication - absorption incomplete

Health care practitioners have to decide whether to re-administer
If it was in the intestine before vomiting another dose could be toxic

127
Q

Example of drugs that kill intestinal bacteria affecting absorption

A

Antibiotic drugs kill intestinal bacteria which decreased their ability to deconjugate phase II drug metabolites (enteroheptatic recyling) for reabsorption

Result: decreased absorption = decreased plasma concentration

128
Q

Examples of altered pH affecting distribution

A

Sodium bicarbonate = increased pH
Ammonium chloride = decreased pH

During aspirin overdose (weak acid), sodium bicarbonate can be given to make blood ph higher. This draws aspirin out of cell and trapping it for excretion

129
Q

Examples of protein binding affecting distribution

A

If two drugs bind to the same site on a protein, the drug with the lower affinity will become free

Result: increased therapeutic effect, increased toxicity or increased excretion

increases free concentration NOT plasma concentration

130
Q

Induction is delayed and take ___ days to occur. Once the inducer is stopped it takes __ days before the CYP enzyme levels return to normal

A

2-10 days to start

7-10 days to stop

131
Q

Examples of CYP inducers include:

A 
Cigarette/marijuana smoke (one joint = 5-10 cigs)
Rifampin - induces CYP3A4
Phenobarbital - induces many CYPs
BBQ food - induces CYP1A2
Alcohol - induces CYP2E1
132
Q

CYP inhibition results in __. However, prodrugs (will/will not) be activated.

A

increased drug plasma concentrations

will not

133
Q

Examples of CYP inhibitors include:

A 
Antibiotics - inhibit CYP3A4
HIV protease inhibitors - inhibit CYP3A4
Omeprazole - inhibit CYP2C19
SSRIs - inhibits CYP2D6
Fluvoxamine - inhibits CYP142
Grapefruit juice - injibits CYP3A4
134
Q

Examples of altered blood flow affecting excretion

A

NSAIDs decreased blood flow = decreased excretion

Beta blockers also decrease blood flow

135
Q

Example of altered pH affecting excretion

A

If someone overdoses on amphetamine (weak base) the filtrate can be acidified with ammonium chloride causing it amphetamine to move into tubules and be trapped for excretion

136
Q

Example of tubular secretion affecting excretion

A

Probenecid inhibits transporter responsible for moving penicillin from blood into lumen - decreasing excretion and increasing blood concentrations

137
Q

Two types of pharmacodynamic interactions

A
  1. Interaction that occurs at same receptor

2. Interaction that occurs at separate sites (morphine and diazepam for CNS depression)

138
Q

Example of combined toxicity

A

Acetaminophen and alcohol - both are hepatotoxic

139
Q

Example of a food-drug interaction

A

Patients taking monoamine oxidase (MAO) inhibitors for depression must avoid food with tyramine (aged cheese, yeast, red wine, sauerkraut, cured meat and soy sauce
MAO inhibitors inhibit breakdown of tyramine
Tyramine causes increased release or norepinephrine which results in a potentially fatal hypertensive crisis

140
Q

Symptoms of hypertensive crisis

A

tachycardia, severe hypertension, headache, nausea and vomiting

Pharm (8 decks)

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