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Winter 2016 > D&D Unit 1 > Flashcards

D&D Unit 1 Flashcards

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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
What does zero-order kinetics mean in terms of pharmacokinetics?
The rate of elimination is independent of the amount of drug in the body and is constant.
26
What is potency?
Concentration or dose required to produce 50% of a drug's maximal effect
27
What is EC50?
"Effective Concentration 50" | The drug concentration that gives half-maximal response
28
What is ED50?
"Effective Dose 50" | The drug dose that gives half-maximal response
29
What is drug efficacy?
Maximum response achievable from a drug
30
Therapeutic index equation
lethal dose for 50% of people / ED50 Higher is better It is a unitless factor
31
Standard drug safety margin equation
100*(LD1/ED99)
32
Many drugs are metabolized through actions of membrane-bound enzymes of the SER called _________
CYP450
33
A phase 1 drug metabolism reaction renders the molecule more _________
Water soluble
34
A phase II drug metabolism reaction is when a the molecule is rendered highly polar so that it can be _________
Excreted (via urine)
35
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 _________
Enterohaptic recycling
36
Drug receptor theory assumes that binding is _________ and response is _________ to receptors
Reversible | Proportional
37
Pharmacokinetic factors affecting drug dose (4)
Absorption Distribution Metabolism Excretion
38
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 _________
``` Narrow therapeutic index High doses Volume of distribution Response Redistribution ```
39
Pharmacodynamic factors affecting drug dose (3)
Antagonistic Synergistic/additive therapeutic Synergistic/additive side effects Indirect pharmacodynamics (a drug indirectly affects another drug)
40
2 ways to induce emesis
Ipecac | Apomorphine (not commonly used anymore though)
41
Contraindications of emetic agents (4)
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
42
4 ways to prevent drug absorption
Emesis Gastric lavage Chemical adsorption (activated charcoal) Osmotic catharthics (decrease time in digestive tract)
43
Gastric lavage is introduction of _________ and removal with a _________
Saline | Nasogastric tube
44
The combination of gastric lavage and emesis removes _________% of oral poisons
30
45
Apomorphine is a _________ agonist and produces _________ by stimulation of _________
Dopamine Emesis Chemoreceptor trigger zone
46
4 osmotic catharthics are
Sorbitol 70% Magnesium citrate or sulfate Sodium sulfate Polyethylene glycol
47
Contraindications for magnesium citrate or sulfate (osmotic catharthics) are (2)
Renal disease | Poisonings with nephrotoxins
48
4 ways to enhance elimination with toxin ingestion are
Extracorporeal removal Enhanced metabolism Enhanced renal excretion (now questionable) Chelation of heavy metals
49
2 ways extracorporeal elimination can be done to remove toxins
Dialysis | Hemoperfusion (blood pumped through a column of absorbent material)
50
Dialysis is best for removal of drugs with a _________ volume of distribution
Small
51
2 ways to enhance renal excretion of a toxin
Forced diuresis | Block reabsorption
52
70-80% of acetaminophen is conjugated with _________ in adults and _________ in children
Glucuronic acid | Sulfate
53
Hepatocellular injury occurs with acetaminophen overdose from excessive formation of _________
Ac*
54
Alcohol dehydrogenase can be inhibited by _________ (drug)
Fomepizole or ethanol (competitive inhibition)
55
Ethylene glycol is metabolized by _________ to form _________, which causes _________ damage
Alcohol dehydrogenase Oxalic acid Renal
56
Methanol is metabolized by _________ to form _________, which causes _________ damage
Alcohol dehydrogenase Formic acid Retinal
57
What is the structure of peptidoglycan?
A polymer with repeating units of 2 hexose sugars (N-acetylglucosamine, N-acetylmuramic acid)
58
Where does peptidoglycan localize?
Bacterial cell walls
59
Bacterial capsules enhance virulence by _________
Enabling phagocytosis resistance
60
Peritrichous means flagella are distributed _________
All over the surface
61
Gram-positive bacteria have a _________ peptidoglycan layer than gram-negative bacteria
Thicker
62
What are the 4 phases of bacterial growth?
Lag Exponential Stationary Death
63
Heterotrophic bacteria get carbon from _________
Organic sources
64
Autotrophic bacteria get carbon from _________
Carbon dioxide
65
_________ bacteria are deficient in at least 1 biosynthetic pathway and require addition of energy and nutrients
Fastidious
66
Obligate intracellular bacteria need to grow in _________
Eukaryotic cells
67
_________ pathogens cause disease in normal hosts and _________ pathogens cause disease in compromised hosts
Frank | Opportunistic
68
Aggressins are microbial products that _________ the host
Damage
69
Impedins are microbial products that _________ the host
Block defenses of
70
What is bacterial transformation?
Uptake of genetic material
71
What is bacterial transduction?
Transfer of genetic material by a virus
72
The major organ of drug metabolism is the _________
Liver
73
The major organ of drug excretion is the _________
Kidney
74
What is the difference between extension effects and side effects?
Extension effects at supra-therapeutic doses Side effects at therapeutic doses
75
Size comparison between drugs that diffuse via aqueous or lipid diffusion
Lipid diffusion drugs are larger
76
What 2 things determine equivalency of oral drug products for FDA approval?
Rate, estimated by peak concentration Extent (bioavailability) They must be similar
77
Food _________ oral drug absorption
Delays
78
In pharmacokinetics, tau is the _________
Dosing interval
79
What is bioavailability?
% of dose reaching systemic circulation
80
Absorption from the GI tract is primarily via _________
Lipid diffusion
81
The plasma/blood volume is
3-5 L
82
The extracellular water volume is
12-15L
83
The total body water is
42 L
84
What is the difference between pharmacokinetics and pharmacodynamics?
Pharmacokinetics is what the body does to the drug Pharmacodynamics is what the drug does to the body
85
What are the 4 things drugs are for?
Prevention Diagnosis Treatment Cure of specific diseases
86
What 5 things does a prescription provide?
``` Drug Dose Route Frequency Duration ```
87
Drug lipid solubility is estimated by the ____________
Oil-water partition coefficient. A higher proportion in the oil phase is more lipid soluble.
88
Bioavailability (F) for IV drug administration is ____________
100%
89
Bioavailability (F) for oral drug administration is ____________
0-100%
90
The rate of onset for various drug administration methods ranked
Inhalation > IV > intramuscular > subcutaneous > oral
91
Under what condition should you not switch between different versions of the same drug?
Narrow therapeutic window
92
What two conditions must be met for bioavailability?
Rate and extent of absorption
93
What are effectors in relation to drugs?
Effectors are the components of the biologic system that accomplishes the biologic effect after being activated by the receptor
94
What does receptor theory allow us to do?
Allows us to make dose-response curves and quantify relationship between drug dose and effect
95
Most drugs are ________ agonists
full (vs. partial)
96
Is potency of efficacy more important clinically?
Efficacy, because we care mostly about the end result
97
Is the maximal efficacy of an agonist changed when an competitive agonist is added?
No. Just higher doses are needed.
98
Substrates for CYP450 must be ________ -soluble
Lipid
99
Isozyme CYP nomenclature, for example CYP1A2
``` CYP = human origin 1 = isoform family A = subfamily 2 = individual gene product ```
100
What is enzyme induction?
When a drug induces/enhances enzyme expression - so more enzyme is produced
101
Is the free drug filtered by the glomeruli?
No. Only the protein-bound
102
What is the normal glomerular filtration rate?
120 ml/min
103
Where does active tubular secretion of drugs happen?
In the proximal tubule
104
What sorts of compounds (drugs) are cleared by active tubular secretion?
Stronger acids and bases
105
3 common phase 1 biotransformations
Oxidation Reduction Hydrolysis
106
5 common phase II biotransformation
Glucuronidation Acetylation Glytathione/glycine/sulfate conjugation
107
What is the cofactor for CYP450?
NADPH
108
The therapeutic index compares ________ in the population and the standard safety margin compares ________ in the population
Midpoints | Extremes
109
FDA categories for drug use in pregnancy
ABCDX ``` A = no risk X = contraindicated ```
110
What is the difference between federal vs. state drug regulation
Federal government controls what drugs | State government controls who prescribes drugs
111
What are the 4 drug regulatory categories distinguished by? (3)
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
A phase I trial tests ________
If a drug is safe
113
A phase II trial tests ________
If a drug works in patients
114
A phase III trial tests ________
If a drug works in a double blind study
115
A ________ application is submitted to the FDA if animal studies are promising
Investigational new drug
116
If phase III trials or promising, a ________ application is checked out by the FDA
New Drug
117
An ________ can be submitted to the FDA for generic drugs rather than clinical trials and only ________ standards must be met
Abbreviated New Drug Application Bioequivalence
118
A phase IV clinical trial is ________
Marketing surveillance aka submitting reports of adverse effects
119
What 2 drug categories should you not switch between brands?
Levothyroxine | Anti-epileptic drugs
120
The 3 types of drug equivalency categories
Pharmaceutical equivalence Bioequivalence Therapeutic equivalence
121
What is the difference between vitamins/minerals/amino acids and herbal meds?
The drug part is not known for most herbal medications unlike the other stuff, which has safe dosage ranges and sometimes daily allowances
122
For new dietary supplement ingredients (after 1994), what must the manufacturer do?
Provide reasonable evidence it is safe for human use
123
What FDA requirements are there for health claims?
Evaluation and authorization
124
What RDA requirements are there for structure/function claims?
Nothing except the disclaimer
125
What are the 3 things drugs are evaluated for on the schedule system?
Medical usefulness Abuse potential Risk for dependence (physical, psychological)
126
What drugs can go through endothelial call gap junctions?
Free drugs, charged and uncharged | Not protein-bound drugs
127
Inputs from the body for Phase I oxidation reactions
Oxygen | NADPH
128
Why are phase II reactions more likely to saturate?
Because metabolites are more scarce, so you run out faster. | 1st order -> 0 order kinetics
129
Chronic alcoholics are fast _________ metabolizers
CYP2E1
130
_________ is a CYP450 genetic polymorphism that metabolizes codeine
CYP2DG makes codein more active (into morpheine)
131
Alcohol dehydrogenase is a phase _________ reaction
I
132
Glucaronyl transferase is a phase _________ conjugation enzyme
II
133
How do you tell by drug nomenclature is a pain drug is an amide?
-caine means they are local anasthetics and work on sodium channels Amides have an extra I in the prefix
134
How long does it take for drug induction to occur?
2-3 days and max effects are 7-10 days Same time frame for effects to dissapate
135
Phase I enzymes are _________ prone to inhibition than phase II enzyme
More
136
How does Rifampin affect oral contraceptive metabolism?
Increases clearance due to induction
137
How does erythromycin affect lipitor metabolism?
Decreases clearance due to inhibition
138
2 phases of the log concentration vs time graph for IV drug input
Distribution | Elimination
139
How to calculate fold fluctuation in multiple drug boluses
2^x where x=# half-lives that occur in the dosage interval
140
What are the 2 types of dose response curves?
Graded - measure amt of response | Quantal - measure % of people responding
141
FDA drug-labelling rules for specific populations - what are the 3 populations of note?
Pregnancy Lactation Females and Males of Reproductive Potential
142
2 methods of pharmacodynamic drug-drug interactions
Drugs have same target Drugs enhance/antagonize the other drug's effector system No changes in plasma concentration!
143
Glomerular filtration is decreased by _________ and increased by _________
Nephrotoxic drugs Displacement from plasma proteins
144
Tubular secretion is decreased by _________
Competition for active transport like penicillin
145
Tubular reabsorption is increased for _________ drugs and decreased for _________
Weak bases Weak acids
146
Tubular reabsorption increases by _________
Increased urine pH
147
What 4 things are needed to demonstrate pharmaceutical equivalence?
Active ingredients Dosage formulation Route of administration Strength/concentration
148
Do generics need to demonstrates therapeutic equivalence?
No. It is assumed if they are pharmaceutically equivalent and bioequivalent
149
When is it advisable (in terms of drug properties) to avoid switching between drugs?
Narrow therapeutic index Zero order pharmacokinetics Poor bioavailability
150
Contraindication for sodium sulfate osmotic cathartic
Congestive heart failure Hypertension b/c will cause systemic Na+ absorption, leading to edema
151
What drug is used to correct metabolic acidosis?
NaHCO3
152
How does acetaminophen toxicity happen?
Saturation of phase II pathways so more goes by phase I Increases formation of phase I hepatotoxic metabolite
153
What drug is used for management of acetaminophen intoxication?
N-acetylcysteine A precursor for glutathione synthesis Inactivates the hepatotoxic metabolite
154
3 classes of drugs limited to prescription use
Controlled substances (habit-forming) Not safe w/o supervision Limited to prescription only under an NDA
155
Generalized scheme of drug action
Drug binds to receptor Signal transduction via effectors Amplification Physiological effect
156
Without an agonist, what are the effects of antagonists?
No effects
157
What are rules in a patient getting a schedule II drug in terms of prescriptions (3)?
In ink in prescriber's handwriting Cannot be telephoned to a pharmacist Cannot be refilled
158
ac on a prescription means _________
Before meals
159
bid on a prescription means _________
Twice a day
160
hs on a prescription means _________
At bedtime
161
pc on a prescription means _________
After meals
162
prn on a prescription means _________
When needed
163
qam on a prescription means _________
Every morning
164
tid on a prescription means _________
3x/day
165
a on a prescription means _________
Before
166
c on a prescription means _________
With
167
gtt on a prescription means _________
drop
168
p on a prescription means _________
after
169
qs on a prescription means _________
Sufficient quantity
170
s on a prescription means _________
without
171
Sig on a prescription means _________
label
172
_________ is a CYP450 genetic polymorphism that metabolizes acetominophen to Ac*
CYP2E1

Winter 2016 (8 decks)

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