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N596 Adv Pharm APN > Wk 1-2: Pharmacokinetics, Pharmacodynamics, Pharmacogenomics > Flashcards

Wk 1-2: Pharmacokinetics, Pharmacodynamics, Pharmacogenomics Flashcards

1
Q

Affinity

A

Affinity: The attraction between a drug and a receptor.

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2
Q

Allosteric site:

A

Allosteric site: A binding site for substrates not active in initiating a response; a substrate that binds to an allosteric site may induce a conformational change in the structure of the active site, rendering it more or less susceptible to response from a substrate.

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3
Q

Bioavailability (F):

A

Bioavailability (F): The fraction or percentage of a drug that reaches the systemic circulation.

F = quantity of drug reaching systemic circulation / quantity of drug administered

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4
Q

Biotransformation:

A

Biotransformation: Metabolism or degradation of a drug from an active form to an inactive form.

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5
Q

Chirality:

A

Chirality: Special configuration or shape of a drug; most drugs exist in two shapes.

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6
Q

Clearance:

A

Clearance: Removal of a drug from the plasma or organs.

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7
Q

Downregulation:

A

Downregulation: Decreased availability of drug receptors.

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8
Q

Enantiomer (also called isomer)

A

Enantiomer (also called isomer): A mirror-image spatial arrangement, or shape, of a drug that suits it for binding with a drug receptor.

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9
Q

Enterohepatic recirculation:

A

Enterohepatic recirculation: The process by which a drug excreted in the bile flows into the gastrointestinal tract, where it is reabsorbed and returned to the general circulation.

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10
Q

First-pass effect:

A

First-pass effect: The phenomenon by which a drug first passes through the liver where it may be degraded before distribution to the tissues.

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11
Q

Half-life (t1⁄2):

A

Half-life (t1⁄2): The time required for half of a total drug amount to be eliminated from the body.

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12
Q

Hepatic extraction ratio:

A

Hepatic extraction ratio: A comparison of the percentage of drug extracted and the percentage of drug remaining active after metabolism in the liver.

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13
Q

Ligand:

A

Ligand: Any chemical, endogenous or exogenous, that interacts with a receptor.

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14
Q

Pharmacodynamics:

A

Pharmacodynamics: Processes through which drugs affect the body.

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15
Q

Pharmacokinetics:

A

Pharmacokinetics: Processes through which the body affects drugs.

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16
Q

Prodrug:

A

Prodrug: A drug that is transformed from an inactive parent drug into an active metabolite; in effect, a precursor to the active drug.

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17
Q

Receptor:

A

Receptor: The site of drug action.

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18
Q

Second messenger:

A

Second messenger: A chemical produced intracellularly in response to a receptor signal; this second messenger initiates a change in the intracellular response.

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19
Q

Therapeutic window:

A

Therapeutic window: The range of drug concentration in the blood between a minimally effective level and a toxic level.

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20
Q

Threshold:

A

Threshold: The level below which a drug exerts little to no therapeutic effect and above which a drug produces a therapeutic effect at the site of action.

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21
Q

Upregulation:

A

Upregulation: Increased availability of receptors.

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22
Q

Volume of distribution (Vd):

A

Volume of distribution (Vd): The extent of distribution of a drug in the body.

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23
Q

High hepatic extraction ratio = ___ oral bioavailability

A

High hepatic extraction ratio = low oral bioavailability

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24
Q

Low hepatic extraction ratio = ___ oral bioavailability

A

Low hepatic extraction ratio = high oral bioavailability

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25
Q

Drugs w/ low hepatic extraction ratio <30%

A 
Barbiturates
diazepam
warfarin
theophylline
tolbutamide
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26
Q

Drugs w/ high hepatic extraction ratio >70% include…

A

lidocaine
meperidine
imipramine

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27
Q

Apparent Volume of Distribution

A

Vd = Amt in body / Plasma drug concentration

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28
Q

Name a drug that is not metabolized at all

A

gentamicin (Garamycin)

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29
Q

Prodrug allopurinol metabolizes into

A

oxypurinol

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30
Q

Prodrug codeine metabolizes into

A

morphine

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31
Q

Prodrug enalapril metabolizes into

A

enalaprilat

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32
Q

Prodrug prednisone metabolizes into

A

Prednisolone

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33
Q

Prodrug valacyclovir metabolizes into

A

Acyclovir

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34
Q

first-order kinetics

A

the actual amount of drug eliminated is proportional to the concentration of the drug (the more drug there is, the faster it is eliminated). This applies to most drugs

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35
Q

zero-order kinetics

A

Fixed amounts of drugs, rather than a fractional proportion, are eliminated at a constant rate
Example: alcohol
This can be dangerous

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36
Q

Pharmacodynamics refers to:

A

the set of processes by which drugs produce specific biochemical or physiologic changes in the body

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37
Q

Four types of receptors:

A

gated ion channels
transmembranous receptors
G protein– coupled receptors (GPCR)
intracellular receptors

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38
Q

Foods with tyramine (fermented cheese, wine…) should not be taken with _____ to avoid _______.

A

MAOIs, hypertensive crisis

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39
Q

Pharmacogenomics

A

Role of genetic variation in drug response

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40
Q

Genetics may account for ___ to ___ % of variability in drug disposition and effects.

A

20 to 95%

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41
Q

Adverse Drug Related Events account for (% admissions, total deaths)…

A

3 to 10% of hospital admissions and prolonged hospital stays, and 100,000 deaths annually

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42
Q

___% DNA accounts for individual differences/variances in drug metabolism and response

A

0.1%

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43
Q

Allele:

A

any of the alternative forms of a gene occurring at a specific location on specific chromosome

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44
Q

Genotype:

A

internally coded, inheritable info in the organism; combination of 2 alleles at single locus

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45
Q

Phenotype:

A

a measurable trait or characteristic

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46
Q

SNP: Single nucleotide polymorphism…

A

Variation in a DNA sequence the occurs when single nucleotide (Adenine, Thymine, Cytosine, Guanine) differs among members of a population.

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47
Q

Polymorphisms

A

DNA variants that occur within a specific population at a frequency rate higher than 1%

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48
Q

The focus of pharmacogenomics are…

A

…SNPs/Polymorphisms

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49
Q

Substrate:

A

A drug that binds to and is metabolized by an enzyme

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50
Q

Enzyme:

A

catalysts that cause oxidation, reduction or hydrolysis of drug

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51
Q

Enzyme Inducer:

A

molecule (drug) that speeds up the production of an enzyme

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52
Q

Enzyme Inhibitor:

A

molecule (drug) that slows down or inhibits the production of an enzyme

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53
Q

Inducer/Inhibitor can include

A

…the drug itself, a second drug, food (grapefruit juice, kale)…

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54
Q

Genetic variants effect proteins how?

A

Genetic variants translate into functional changes in proteins

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55
Q

More than ___ families of drug metabolizing enzymes in humans

A

30

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56
Q

Pt without pseudocholinesterase will be unable to break down _______ and could face complications of _______ including ________ as a result.

A

succinylcholine, prolonged paralysis and apnea

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57
Q

Common efflux protein

A

P-glycoprotein

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58
Q

Transport proteins like P-glycoprotein are thought to be ______ against toxins in food, etc

A

Protective

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59
Q

P-gp controls ATP-dependent _____ _____ of ______

A

cellular efflux of substrates, anticancer drugs, immunosuppressive drugs, and other meds

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60
Q

A LOW expression of gene for P-gp will result in…

A

…higher drug levels. Less P-gp = more drug in circulation.

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61
Q

P-gp associated with lower ___ drug concentrations

A

HIV

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62
Q

Protease inhibitors for HIV (indinavir, nelfinavir, etc…) have ___ bioavailability due to P-glycoprotein

A

Variable or low

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63
Q

Pt’s with low expression of P-gp have ______ plasma concentrations of HIV antivirals

A

2-5 times

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64
Q

P-gp is expressed in these places:

A

GI tract, CNS

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65
Q

___% of drugs marketed in US metabolized by cytochrome 450 / CYP450

A

70%

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66
Q

CYP450 inhibited by these types of foods

A

Grapefruit juice, charred foods, kale / cruciferous vegetables

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67
Q

CYP450 highest levels in this organ _____ but also found in this organ ____

A

liver, GI tract

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68
Q

P-gp is found in ______ and also in ____ and _____

A

intestine (transfers back to intestine), also in liver and kidney (transfers to bile and urine)

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69
Q

The drug ______ INHIBITS intestinal P-gp and renal P-gp, leading to ____ levels of digoxin

A

Quinidine; increases ABSORPTION of digoxin in intestine, and decreases ELIMINATION of digoxin at kidney

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70
Q

The antibiotic drug ________ has this effect on P-gp, and digoxin.

A

Rifampin induces intestinal P-gp, decreases digoxin absorption, lowering serum concentrations

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71
Q

Alcohol can _______ CYP enzymes leading to ____ serum levels of drug

A

inhibit, increase …(hypoglycemia in pt’s taking insulin

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72
Q

Metronidazole inhibits enzyme ______, which increases ____ and leads to ______-like reaction

A

inhibits aldehyde dihydrogenase
elevates acetaldehyde
causes disulfiram-like reaction (flushing, h/a, n/v, hypotension, blurred vision)

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73
Q

SMOKING can _______ CYP enzymes leading to ________ metabolism and _______ levels of certain drugs

A

Smoking can increase CYP metabolism leading to decreased levels of diazepam, propooxyphene, chlorpromazine, amitryptaline, theophylline…

74
Q

Warfarin is metabolized mainly by CYP___

75
Q

Warfarin tends to be poorly metabolized by ______ due to ________ of CYP2C19

A

Asians, due to poor expression of CYP2C19

76
Q

Variant alleles of CYP2C9 occur in ____% of white population, affecting warfarin metabolism

77
Q

Warfarin response is also impacted by gene ______

A

VKORC1, which encodes synthesis of vit K

78
Q

Lecture slide shows that average required warfarin dose is highest for this population; lowest for this population

A

Highest doses for African-American; lowest doses for Asian-American

79
Q

Clopidogrel is this type of drug ______ which when metabolized by CYP____ results in its active metabolite

A

prodrug, CYP2C19

80
Q

Deficiency of CYP2C19 among clopidogrel patients can result in recurrent ______, and are most commonly seen among _______ (50%) and then _______ (33%)

A

….higher rates of recurrent CV events, Asians, African Americans

81
Q

CYP2C19*1 is the “wild type” which means ______

A

Normal enzyme activity

82
Q

CYP2C19*2 is predominantly carried by _______ and are considered ________, and when on Plavix, they face higher rates of _______

A

Asians, poor-metabolizers, higher recurrent rates of CV events

83
Q

Warfarin works when _______ inhibits VKORC1 which encodes synthesis of ______

A

S-warfarin

vitamin K

84
Q

S-warfarin is metabolized by _____

85
Q

Mutations to CYP2C9 can lead to ______ in warfarin patients (CYP2C92, CYP2C93)

A

Bleeding, due to decreased metabolism of S-warfarin, higher serum levels of S-warfarin, subsequent lower levels of VKORC1, and decreased production of vit K and decreased coagulation activity.

86
Q

VKORC1 mutation known as “________” can lead to ______ and thus require lower doses of _______; common among _______

A

VKORC1 “A haptotype” inactivating mutation can lead to less VKORC1 and thus require lower doses of warfarin; common among _______

87
Q

Codeine is a _______ and requires ______ to convert to active form _____

A

Prodrug, requires CYP2D6 to convert to morphine

88
Q

CYP2D6 poor metabolizers can lead to _______ effect of codeine and ultra-rapid metabolizers can lead to ______ effect from taking codeine leading to symptoms related to ______

A

CYP2D6 poor metabolizers can lead to poor pain relief effects of codeine (since poor metabolism to morphine), and ultra-rapid metabolizers can lead to toxic effect from taking codeine due to rapid increase in morphine levels - respiratory depression / apnea

89
Q

Cough and cold medications are not recommended for use in children younger than ____.
Opioids (codeine etc) not recommended in children younger than ______.

A

18 years
6 years
warning for use of tramadol for tonsillectomy etc for ages 12-16.

90
Q

Anti-depressant treatments are successful in ____ (fraction) of patients, which can be related to ______ status of patients

A

2/3 patients, metabolizer status

91
Q

Poor-metabolizers of anti-depressants can have this electrolyte imbalance.

A

Hyponatremia, related to SSRs and tricyclic antidepressants

92
Q

Poor metabolizer may have _______ level of drug in system, with potential _______ problems

A

higher, toxicity

93
Q

Ultra-metabolizer may have _____ level of drug in system, and may be ______ to achieve therapeutic drug levels

A

lower; unable

94
Q

This drug _____ can interfere with Tamoxifen (BRCA cancer med) leading to cancer recurrence

A

Paxil (SSRI)

95
Q

New drug applications are required to be screened for KCNH2 blocking activity, which can lead to ________.

A

QTc-prolongation

96
Q

Variations to ________ receptors may lead to ________ effects of albuterol and beta-blockers like metoprolol

A

beta-adrenergic receptors; pronounced effects, or no effect at all

97
Q

Antidepressants of this type have more pharmacogenomic problems and drug response issues

A

tricyclic antidepressants (e.g. noritriptaline) vs SSRI

98
Q

Swedish and Middle-Eastern patients tend to be _________ metabolizers of CYP_____

A

Swedish and Middle-Eastern patients tend to be ultra-metabolizers of CYP2D6.

99
Q

SNF on gene TCL1A can cause side effects of patients taking ______ including symptoms of _______; implication is _______

A

Tamoxifen; joint pain, stiffness, myalgias, decreased bone density; decreased medication adherence

100
Q

Metformin can result in _____ side effects if pt has certain gene

A

GI side effects

101
Q

Therapeutic drug monitoring is common among the ___

A

narrow therapeutic drugs, like aminoglycosides (gentamicin, other -mycin drugs)

102
Q

Enteric coating medications dissolve in:

103
Q

Rectal drugs are limited by ____ but have less _____ effect than oral drugs

A

erratic absorption, less hepatic first-pass effect than oral

104
Q

Sublingual, buccal meds bypass ___ and have ____ onset

A

first-pass

rapid

105
Q

IV meds have toxicity related to

A

peak concentrations

106
Q

Inhalation meds have ____ onset

107
Q

Topical meds offer the benefit of ______

A

less systemic exposure

108
Q

Fick’s Law predicts

A

how well a drug will passively diffuse across a membrane

109
Q

Passive diffusion is most common, and is facilitated by

A

larger surface area
larger concentration gradient
higher permeability
lower membrane thickness

110
Q

P-glycoprotein is an example of ____

A

carrier mediated, active transport

111
Q

Non-ionized > less polar are…

A

more lipid soluble > crosses membrane

112
Q

Ionized > more polar are…

A

less lipid soluble > does not cross membrane

113
Q

Drug trapping: Weak base: ionized form predominates in

A

acidic environments (stomach)

114
Q

Drug trapping: Weak acid: ionized form predominates in

A

basic environments (urine)

115
Q

P-gp is an efflux transporter also known as

A

MDR1, ABCB1

116
Q

P-gp is ______ for substrate

A

nonselective

117
Q

P-gp serves a protective function such as

A

protecting fetus, blood brain barrier, etc

118
Q

P-gp is found here:

A

tumor, intestine, blood brain barrier, kidney, placenta…

119
Q

P-gp is inhibited by many drugs including:

A

Amiodarone, captopril, carvedilol, ketoconazole, quinidine, verapamil, grapefruit juice

120
Q

P-gp is induced by…

A

St Johns Wort
Tipranavir/ritonavir (HIV med)
Phenytoin
Carbamazepine

121
Q

Basic / alkaline drugs are absorbed in the…

A

…duodenum (alkaline environment, remain non-ionized, and able to pass membrane into portal circulation)

122
Q

Acidic drugs are absorbed in the…

A

…stomach (acidic environment, remain non-ionized, and able to pass membrane into portal circulaton)

123
Q

P-gp is inhibited by…

A

…grapefruit juice, cyclosporine, verapamil, amiodarone

124
Q

Distribution is

A

drug movement from systemic circulation to tissues

125
Q

Which organ has the highest normalized blood flow?

A

Kidneys (3333 ml/min/kg)

126
Q

Drug binding proteins include

A

albumin

alpha1-acid glycoprotein

127
Q

Plasma protein binding remains ______

128
Q

Vd =

A

Amt drug in body / drug concentration (plasma)

129
Q

Smaller Vd will remain in _____

A

Vascular compartment (more hydrophilic, large molecule, high PPB…. aspirin

130
Q

Larger Vd will remain

A

outside of plasma compartment (More lipophilic, small molecule, low PPB) …fluoxetine

131
Q

Elimination =

A

removal of drug from body, includes metabolism and excretion

132
Q

Purpose of metabolism:

A

To facilitate excretion

133
Q

Metabolism phases: Phase 1 and 2

A 
Phase 1 (makes molecule polar, oxidation, hydrolysis
Phase 2 (conjugation (glucuronide)
134
Q

CYP450 uses this type of metabolism:

A

Phase 1 (oxidation, more polar/H2O soluble molecule)

135
Q

Enzyme is a

136
Q

Metabolites can be active, such as metabolites of

137
Q

Metabolites can be toxic, such as with

A

hepatotoxic acetaminophen metabolite

138
Q

Pro-drugs are metabolized into their active form such as:

A

Fosphenytoin, capecitabine, enalopril, codeine

139
Q

CYP450 constitute _____% of drug metabolism

140
Q

CYP INDUCERS include

A

Barbituates, rifampin, anti-seizure meds, dexamethasone, phenytoin, St Johns Wort, char-grilled meat, cigarette smoke

141
Q

CYP INHIBITORS include

A

Grapefruit juice, antiretrovirals, -azoles, SSRIs, PPIs, CCBs, -mycins

142
Q

A person who takes codeine who has a duplicate allele of CYP2D6 will be ____ and have ______ effect

A

ultra-metabolizer, increased morphine level

143
Q

Phenobarbitol is acidic, therefore administering sodium bicarb will ________

A

alkalinize the urine and trap the drug to excrete it in case of an overdose

144
Q

Alcohol follows _______ kinetics

A

Zero-order (constant amount over time)

145
Q

Half-life equation

A

Half-life = 0.693 x Vd / Cl

146
Q

Half life is prolonged by:

A

increase in Vd, OR by decrease in rate of clearance

147
Q

Zero-order elimination drugs have no true…

148
Q

Zero-order elimination drugs can have dangerous…

A

accumulation

149
Q

Zero-order drugs include…

A

alcohol, phenytoin

150
Q

After about 5 half-lives, _____

A

97% of drug is eliminated

151
Q

Steady-state =

A

equilibrium (rate in = rate out)

152
Q

Endogenous ligands are

A

…ligands produced in the body (not drugs).

153
Q

Intrinsic activity of a drug is…

A

…ability of a drug to activate a receptor

154
Q

ACEI utilize this kind of receptor

155
Q

These drugs use intracellular receptors…

A

sex hormones, steroids

156
Q

These drugs use circulating protein receptors…

A

…anticoagulants

157
Q

Irreversible inhibitor example

A

Omeprazole (PPIs)

158
Q

Allosteric interactions

A

Drug attaches to binding site OTHER than the active site to change conformational form of receptor, changing effect (increasing or decreasing)

159
Q

Benzodiazepines are blocked by _____ which is a ______

A

Flumazenil, competitive antagonist, can reverse the binding of benzodiazepines

160
Q

cAMP and cGMP and Ca++ are…

A

…second messenger molecules in the transduction pathway that cause cellular response

161
Q

PDE5 inhibitors (sildenafil, etc) work at _____ level

A

second messenger, increasing cGMP response

162
Q

Quantal Dose-Effect Curve

A

Measures how a population responds to a drug

163
Q

________ Index = TD50 / ED50

A

Therapeutic Index = TD50 / ED50 (median toxic dose / median effective dose)

164
Q

On-target toxicity

A

Intended receptor (improper dose, same receptor but wrong tissue); these are “class effects”

165
Q

Off-target toxicity

A

Unintended target; enantiomers; binds different receptors; immune-related effects; binds different receptor sub-type

166
Q

Tachyphylaxis =

167
Q

PK related toxicity involves

A

CYP450, transporters, PPB related

168
Q

PD related toxicity

A

Method of action interaction (PDE5 inhibitor + NTG)

169
Q

Most frequent reason for drug withdrawal in US

A

hepatotoxicity

170
Q

Hepatic function impairment marker

171
Q

Hepatocellular injury markers

A

AST, ALT, ALP

172
Q

Renal injury marker

A

Creatinine (drugs: NSAIDS, gentamicin)

173
Q

Pulmonary toxicity can be caused by…

A

amiodarone

174
Q

Gentamicin has a narrow therapeutic index and requires _______ monitoring, specifically ____ and ____ monitoring. It causes ______ toxicity.

A

Therapeutic Drug Monitoring
Peak (toxicity >10-12mcg/mL)
Trough (>2mcg/mL)
Renal toxicity

175
Q

NSAIDs can cause _______ toxicity

176
Q

Narrow therapeutic drugs include

A 
warfarin
digoxin
gentamicin
lithium
phenytoin
carbamazepine
Cytotoxic drugs (including anti-epileptic and chemotherapy drugs)
177
Q

Drug distribution to various compartments (compartment / molecule type)

A

Total body water: small, hydrophilic (ethanol)
Extracellular water: Larger, hydrophilic (mannitol)
Blood plasma: Large, plasma-bound, ionized (heparin)
Adipose tissue: Lipophilic (diazepam)
Bone / teeth: Certain ions (fluoride, strontium)

178
Q

Higher Vd typically means ______ half-life due to ______ availability to organs of elimination

A

longer

decreased

179
Q

Vd and compartments:
Plasma compartment:
Extracellular fluid:
Total body water:

A

Plasma compartment:
Low Vd [4L/70kg] (large, protein bound)
heparin

Extracellular fluid:
Medium Vd [20% body wt] (small, hydrophilic) Aminoglycoside abx

Total body water:
High Vd [60% body wt, 42L/70kg] (small, lipophilic) ETHANOL, ASPIRIN

180
Q

Quinidine is metabolized by receptor ______ but works through noncompetitive inhibition to block receptor ________

A

CYP3A4

CYP2D6

N596 Adv Pharm APN (5 decks)

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