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Winter 2016 > D&D Unit 1 > Flashcards

D&D Unit 1 Flashcards

1
Q

With enteral drug delivery (rectal), _________% of the dose will bypass the _________

A

50

Liver

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2
Q

Paraenteral drugs (sublingual or buccal) are absorbed into the _________

A

Superior vena cava

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3
Q

The best particle size for lung inhalation is _________ where particles are deposited in the _________

A

1-5 uM
Small airways

exhaled
>10uM -> deposited in oropharynx -> side effects

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4
Q

Henderson-Hasselbach equation

A

pH-pKa = log[ (non-protonated A- or B)/protonated Ha or BH+)]

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5
Q

Ion trapping means _________ drugs are trapped in _________ solutions (and also reverse)

A

Acidic/Basic
vs
Basic/Acidic

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6
Q

Acidic drugs bind to _________ and basic drugs bind to _________

A

Albumin

Alpha-1 acid glycoprotein

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7
Q

A drug binding to a protein _________ concentration of free drug, _________ metabolic degradation/excretion rate, _________ volume of distribution, _________ ability to enter CNS

A

Decreases all

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8
Q

Equation for absolute bioavailability fraction

A

area under curve any route (usually oral) /area under curve IV

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9
Q

What is the volume of distribution?

A

Volume of body fluid into which the drug distributes after admnistration

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10
Q

Equation for loading dose

A

Cp * Vd

peak concentration * volume of distribution

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11
Q

Equation for peak concentration

A

Dose /Vd

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12
Q

Equation for calcuating volume of distribution

A

dose/plasma concentration

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13
Q

Equation for backcalculating dose

A

plasma concentration * Vd

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14
Q

Calculating drug concentration in plasma

A

dose/Vd

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15
Q

A low volume of distribution means most of the drug is in the _________

A

Plasma, vs in other fluids

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16
Q

Drug metabolism produces a more _________ form of the drug

A

Water soluble

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17
Q

Milk is more _________ than plasma (pH)

A

Acidic, so basic things tend to be in it

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18
Q

_________ content of milk increases during the feeding period

A

Fat

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19
Q

Protein binding _________ drug concentration in milk

A

Decreases

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20
Q

Drug clearance equation

A

Vd * Ke

Volume of distribution * fraction of drug eliminated per unit time

MD*Cp/tau
Maintenance dose * peak concentration / dosing interval (hour)

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21
Q

What is clearance?

A

Volume of plasma completely cleared of a drug in a given period of time, mostly due to kidney excretion and drug metabolism

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22
Q

Maintenance dose equation

A

MD/tau = clearance * Cp

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23
Q

What is the elimination rate constant?

A

The fraction of a drug leaving the body per unit time via all elimination processes. It lets us calculate the amount of drug remaining.

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24
Q

What does first-order kinetics mean in terms of pharmacokinetics?

A

Rate of elimination is proportional to plasma concentration

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25
Q

What does zero-order kinetics mean in terms of pharmacokinetics?

A

The rate of elimination is independent of the amount of drug in the body and is constant.

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26
Q

What is potency?

A

Concentration or dose required to produce 50% of a drug’s maximal effect

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27
Q

What is EC50?

A

“Effective Concentration 50”

The drug concentration that gives half-maximal response

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28
Q

What is ED50?

A

“Effective Dose 50”

The drug dose that gives half-maximal response

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29
Q

What is drug efficacy?

A

Maximum response achievable from a drug

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30
Q

Therapeutic index equation

A

lethal dose for 50% of people / ED50

Higher is better
It is a unitless factor

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31
Q

Standard drug safety margin equation

A

100*(LD1/ED99)

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32
Q

Many drugs are metabolized through actions of membrane-bound enzymes of the SER called _________

A

CYP450

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33
Q

A phase 1 drug metabolism reaction renders the molecule more _________

A

Water soluble

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34
Q

A phase II drug metabolism reaction is when a the molecule is rendered highly polar so that it can be _________

A

Excreted (via urine)

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35
Q

The process by which drug metabolites in the liver are secreted into bile, stored in the gallbladder, delivered to the intestine via the bile duct, hydrolyzed by bacterial enzymes back to the parent drug and undergo reabsorption from the gut is _________

A

Enterohaptic recycling

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36
Q

Drug receptor theory assumes that binding is _________ and response is _________ to receptors

A

Reversible

Proportional

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37
Q

Pharmacokinetic factors affecting drug dose (4)

A

Absorption
Distribution
Metabolism
Excretion

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38
Q

Drug distribution can be of clinical consequence if the displaced drug has a _________, is started in _________, _________ is small, or _________ to a drug occurs more rapidly than _________

A 
Narrow therapeutic index
High doses
Volume of distribution
Response
Redistribution
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39
Q

Pharmacodynamic factors affecting drug dose (3)

A

Antagonistic Synergistic/additive therapeutic
Synergistic/additive side effects
Indirect pharmacodynamics (a drug indirectly affects another drug)

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40
Q

2 ways to induce emesis

A

Ipecac

Apomorphine (not commonly used anymore though)

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41
Q

Contraindications of emetic agents (4)

A

Lack of gag reflex (b/c comatose) -> risk of aspiration
Ingestion of corrosive poisons
Ingestion of CNS stimulant -> risk of seizures
Ingestion of petroleum distillate -> risk of pneumonitis, pregnancy category C

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42
Q

4 ways to prevent drug absorption

A

Emesis
Gastric lavage
Chemical adsorption (activated charcoal)
Osmotic catharthics (decrease time in digestive tract)

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43
Q

Gastric lavage is introduction of _________ and removal with a _________

A

Saline

Nasogastric tube

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44
Q

The combination of gastric lavage and emesis removes _________% of oral poisons

A

30

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45
Q

Apomorphine is a _________ agonist and produces _________ by stimulation of _________

A

Dopamine
Emesis
Chemoreceptor trigger zone

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46
Q

4 osmotic catharthics are

A

Sorbitol 70%
Magnesium citrate or sulfate
Sodium sulfate
Polyethylene glycol

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47
Q

Contraindications for magnesium citrate or sulfate (osmotic catharthics) are (2)

A

Renal disease

Poisonings with nephrotoxins

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48
Q

4 ways to enhance elimination with toxin ingestion are

A

Extracorporeal removal
Enhanced metabolism
Enhanced renal excretion (now questionable)
Chelation of heavy metals

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49
Q

2 ways extracorporeal elimination can be done to remove toxins

A

Dialysis

Hemoperfusion (blood pumped through a column of absorbent material)

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50
Q

Dialysis is best for removal of drugs with a _________ volume of distribution

A

Small

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51
Q

2 ways to enhance renal excretion of a toxin

A

Forced diuresis

Block reabsorption

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52
Q

70-80% of acetaminophen is conjugated with _________ in adults and _________ in children

A

Glucuronic acid

Sulfate

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53
Q

Hepatocellular injury occurs with acetaminophen overdose from excessive formation of _________

A

Ac*

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54
Q

Alcohol dehydrogenase can be inhibited by _________ (drug)

A

Fomepizole or ethanol (competitive inhibition)

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55
Q

Ethylene glycol is metabolized by _________ to form _________, which causes _________ damage

A

Alcohol dehydrogenase
Oxalic acid
Renal

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56
Q

Methanol is metabolized by _________ to form _________, which causes _________ damage

A

Alcohol dehydrogenase
Formic acid
Retinal

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57
Q

What is the structure of peptidoglycan?

A

A polymer with repeating units of 2 hexose sugars (N-acetylglucosamine, N-acetylmuramic acid)

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58
Q

Where does peptidoglycan localize?

A

Bacterial cell walls

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59
Q

Bacterial capsules enhance virulence by _________

A

Enabling phagocytosis resistance

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60
Q

Peritrichous means flagella are distributed _________

A

All over the surface

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61
Q

Gram-positive bacteria have a _________ peptidoglycan layer than gram-negative bacteria

A

Thicker

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62
Q

What are the 4 phases of bacterial growth?

A

Lag
Exponential
Stationary
Death

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63
Q

Heterotrophic bacteria get carbon from _________

A

Organic sources

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64
Q

Autotrophic bacteria get carbon from _________

A

Carbon dioxide

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65
Q

_________ bacteria are deficient in at least 1 biosynthetic pathway and require addition of energy and nutrients

A

Fastidious

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66
Q

Obligate intracellular bacteria need to grow in _________

A

Eukaryotic cells

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67
Q

_________ pathogens cause disease in normal hosts and _________ pathogens cause disease in compromised hosts

A

Frank

Opportunistic

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68
Q

Aggressins are microbial products that _________ the host

A

Damage

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69
Q

Impedins are microbial products that _________ the host

A

Block defenses of

70
Q

What is bacterial transformation?

A

Uptake of genetic material

71
Q

What is bacterial transduction?

A

Transfer of genetic material by a virus

72
Q

The major organ of drug metabolism is the _________

A

Liver

73
Q

The major organ of drug excretion is the _________

A

Kidney

74
Q

What is the difference between extension effects and side effects?

A

Extension effects at supra-therapeutic doses

Side effects at therapeutic doses

75
Q

Size comparison between drugs that diffuse via aqueous or lipid diffusion

A

Lipid diffusion drugs are larger

76
Q

What 2 things determine equivalency of oral drug products for FDA approval?

A

Rate, estimated by peak concentration
Extent (bioavailability)

They must be similar

77
Q

Food _________ oral drug absorption

A

Delays

78
Q

In pharmacokinetics, tau is the _________

A

Dosing interval

79
Q

What is bioavailability?

A

% of dose reaching systemic circulation

80
Q

Absorption from the GI tract is primarily via _________

A

Lipid diffusion

81
Q

The plasma/blood volume is

A

3-5 L

82
Q

The extracellular water volume is

A

12-15L

83
Q

The total body water is

A

42 L

84
Q

What is the difference between pharmacokinetics and pharmacodynamics?

A

Pharmacokinetics is what the body does to the drug

Pharmacodynamics is what the drug does to the body

85
Q

What are the 4 things drugs are for?

A

Prevention
Diagnosis
Treatment
Cure

of specific diseases

86
Q

What 5 things does a prescription provide?

A 
Drug
Dose
Route
Frequency
Duration
87
Q

Drug lipid solubility is estimated by the ____________

A

Oil-water partition coefficient. A higher proportion in the oil phase is more lipid soluble.

88
Q

Bioavailability (F) for IV drug administration is ____________

A

100%

89
Q

Bioavailability (F) for oral drug administration is ____________

A

0-100%

90
Q

The rate of onset for various drug administration methods ranked

A

Inhalation > IV > intramuscular > subcutaneous > oral

91
Q

Under what condition should you not switch between different versions of the same drug?

A

Narrow therapeutic window

92
Q

What two conditions must be met for bioavailability?

A

Rate and extent of absorption

93
Q

What are effectors in relation to drugs?

A

Effectors are the components of the biologic system that accomplishes the biologic effect after being activated by the receptor

94
Q

What does receptor theory allow us to do?

A

Allows us to make dose-response curves and quantify relationship between drug dose and effect

95
Q

Most drugs are ________ agonists

A

full (vs. partial)

96
Q

Is potency of efficacy more important clinically?

A

Efficacy, because we care mostly about the end result

97
Q

Is the maximal efficacy of an agonist changed when an competitive agonist is added?

A

No. Just higher doses are needed.

98
Q

Substrates for CYP450 must be ________ -soluble

A

Lipid

99
Q

Isozyme CYP nomenclature, for example CYP1A2

A 
CYP = human origin
1 = isoform family
A = subfamily
2 = individual gene product
100
Q

What is enzyme induction?

A

When a drug induces/enhances enzyme expression - so more enzyme is produced

101
Q

Is the free drug filtered by the glomeruli?

A

No. Only the protein-bound

102
Q

What is the normal glomerular filtration rate?

A

120 ml/min

103
Q

Where does active tubular secretion of drugs happen?

A

In the proximal tubule

104
Q

What sorts of compounds (drugs) are cleared by active tubular secretion?

A

Stronger acids and bases

105
Q

3 common phase 1 biotransformations

A

Oxidation
Reduction
Hydrolysis

106
Q

5 common phase II biotransformation

A

Glucuronidation
Acetylation
Glytathione/glycine/sulfate conjugation

107
Q

What is the cofactor for CYP450?

A

NADPH

108
Q

The therapeutic index compares ________ in the population and the standard safety margin compares ________ in the population

A

Midpoints

Extremes

109
Q

FDA categories for drug use in pregnancy

A

ABCDX

A = no risk
X = contraindicated
110
Q

What is the difference between federal vs. state drug regulation

A

Federal government controls what drugs

State government controls who prescribes drugs

111
Q

What are the 4 drug regulatory categories distinguished by? (3)

A

Whether or not they are evaluated for efficacy or safety prior to use in patients

Available by prescription or direct purchase

Potential for abuse

112
Q

A phase I trial tests ________

A

If a drug is safe

113
Q

A phase II trial tests ________

A

If a drug works in patients

114
Q

A phase III trial tests ________

A

If a drug works in a double blind study

115
Q

A ________ application is submitted to the FDA if animal studies are promising

A

Investigational new drug

116
Q

If phase III trials or promising, a ________ application is checked out by the FDA

A

New Drug

117
Q

An ________ can be submitted to the FDA for generic drugs rather than clinical trials and only ________ standards must be met

A

Abbreviated New Drug Application

Bioequivalence

118
Q

A phase IV clinical trial is ________

A

Marketing surveillance aka submitting reports of adverse effects

119
Q

What 2 drug categories should you not switch between brands?

A

Levothyroxine

Anti-epileptic drugs

120
Q

The 3 types of drug equivalency categories

A

Pharmaceutical equivalence
Bioequivalence
Therapeutic equivalence

121
Q

What is the difference between vitamins/minerals/amino acids and herbal meds?

A

The drug part is not known for most herbal medications unlike the other stuff, which has safe dosage ranges and sometimes daily allowances

122
Q

For new dietary supplement ingredients (after 1994), what must the manufacturer do?

A

Provide reasonable evidence it is safe for human use

123
Q

What FDA requirements are there for health claims?

A

Evaluation and authorization

124
Q

What RDA requirements are there for structure/function claims?

A

Nothing except the disclaimer

125
Q

What are the 3 things drugs are evaluated for on the schedule system?

A

Medical usefulness
Abuse potential
Risk for dependence (physical, psychological)

126
Q

What drugs can go through endothelial call gap junctions?

A

Free drugs, charged and uncharged

Not protein-bound drugs

127
Q

Inputs from the body for Phase I oxidation reactions

A

Oxygen

NADPH

128
Q

Why are phase II reactions more likely to saturate?

A

Because metabolites are more scarce, so you run out faster.

1st order -> 0 order kinetics

129
Q

Chronic alcoholics are fast _________ metabolizers

A

CYP2E1

130
Q

_________ is a CYP450 genetic polymorphism that metabolizes codeine

A

CYP2DG makes codein more active (into morpheine)

131
Q

Alcohol dehydrogenase is a phase _________ reaction

A

I

132
Q

Glucaronyl transferase is a phase _________ conjugation enzyme

A

II

133
Q

How do you tell by drug nomenclature is a pain drug is an amide?

A

-caine means they are local anasthetics and work on sodium channels

Amides have an extra I in the prefix

134
Q

How long does it take for drug induction to occur?

A

2-3 days and max effects are 7-10 days

Same time frame for effects to dissapate

135
Q

Phase I enzymes are _________ prone to inhibition than phase II enzyme

A

More

136
Q

How does Rifampin affect oral contraceptive metabolism?

A

Increases clearance due to induction

137
Q

How does erythromycin affect lipitor metabolism?

A

Decreases clearance due to inhibition

138
Q

2 phases of the log concentration vs time graph for IV drug input

A

Distribution

Elimination

139
Q

How to calculate fold fluctuation in multiple drug boluses

A

2^x where x=# half-lives that occur in the dosage interval

140
Q

What are the 2 types of dose response curves?

A

Graded - measure amt of response

Quantal - measure % of people responding

141
Q

FDA drug-labelling rules for specific populations - what are the 3 populations of note?

A

Pregnancy
Lactation
Females and Males of Reproductive Potential

142
Q

2 methods of pharmacodynamic drug-drug interactions

A

Drugs have same target
Drugs enhance/antagonize the other drug’s effector system

No changes in plasma concentration!

143
Q

Glomerular filtration is decreased by _________ and increased by _________

A

Nephrotoxic drugs

Displacement from plasma proteins

144
Q

Tubular secretion is decreased by _________

A

Competition for active transport like penicillin

145
Q

Tubular reabsorption is increased for _________ drugs and decreased for _________

A

Weak bases

Weak acids

146
Q

Tubular reabsorption increases by _________

A

Increased urine pH

147
Q

What 4 things are needed to demonstrate pharmaceutical equivalence?

A

Active ingredients
Dosage formulation
Route of administration
Strength/concentration

148
Q

Do generics need to demonstrates therapeutic equivalence?

A

No. It is assumed if they are pharmaceutically equivalent and bioequivalent

149
Q

When is it advisable (in terms of drug properties) to avoid switching between drugs?

A

Narrow therapeutic index
Zero order pharmacokinetics
Poor bioavailability

150
Q

Contraindication for sodium sulfate osmotic cathartic

A

Congestive heart failure
Hypertension
b/c will cause systemic Na+ absorption, leading to edema

151
Q

What drug is used to correct metabolic acidosis?

A

NaHCO3

152
Q

How does acetaminophen toxicity happen?

A

Saturation of phase II pathways so more goes by phase I

Increases formation of phase I hepatotoxic metabolite

153
Q

What drug is used for management of acetaminophen intoxication?

A

N-acetylcysteine
A precursor for glutathione synthesis
Inactivates the hepatotoxic metabolite

154
Q

3 classes of drugs limited to prescription use

A

Controlled substances (habit-forming)
Not safe w/o supervision
Limited to prescription only under an NDA

155
Q

Generalized scheme of drug action

A

Drug binds to receptor
Signal transduction via effectors
Amplification
Physiological effect

156
Q

Without an agonist, what are the effects of antagonists?

A

No effects

157
Q

What are rules in a patient getting a schedule II drug in terms of prescriptions (3)?

A

In ink in prescriber’s handwriting
Cannot be telephoned to a pharmacist
Cannot be refilled

158
Q

ac on a prescription means _________

A

Before meals

159
Q

bid on a prescription means _________

A

Twice a day

160
Q

hs on a prescription means _________

A

At bedtime

161
Q

pc on a prescription means _________

A

After meals

162
Q

prn on a prescription means _________

A

When needed

163
Q

qam on a prescription means _________

A

Every morning

164
Q

tid on a prescription means _________

A

3x/day

165
Q

a on a prescription means _________

A

Before

166
Q

c on a prescription means _________

A

With

167
Q

gtt on a prescription means _________

A

drop

168
Q

p on a prescription means _________

A

after

169
Q

qs on a prescription means _________

A

Sufficient quantity

170
Q

s on a prescription means _________

A

without

171
Q

Sig on a prescription means _________

A

label

172
Q

_________ is a CYP450 genetic polymorphism that metabolizes acetominophen to Ac*

A

CYP2E1

Winter 2016 (8 decks)

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