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PDA Block 1 > Block 1 Bolded Terms > Flashcards

Block 1 Bolded Terms Flashcards

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1
Q

Receptor

A

Any macromolecular component in an organism that binds a drug/ligand

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2
Q

Affinity

A

The substance’s ability to form a complex with a receptor. In other words, how strong the ligand and receptor bind

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3
Q

Ligand

A

A molecule that binds to a receptor (a drug)

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4
Q

KD

A

The dissociation equilibrium constant

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5
Q

Rt

A

The total number of receptors bound (bound [LR] + free [R])

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6
Q

Agonist

A

A substance that mimics the regulatory effects of the endogenous signaling compound

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7
Q

Antagonist

A

A substance that binds to the receptor without regulatory effect

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8
Q

Partial agonist

A

Partial agonists may act as agonists when no full agonist is around or they may act as antagonists if a full agonist is present - A partial agonist may have higher affinity for a receptor than a full agonist, but it can never produce Emax

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9
Q

Intrinsic Activity

A

The ability of a ligand to produce a cellular effect after it has bound to a receptor

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10
Q

Spare Receptors

A

The relationships between the amount of ligand bound and the effect on the cell is not linear but rather a rectangular hyperbola in most systems because very small amounts of receptor occupancy produce large effects because there are spare receptors available

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11
Q

EC50

A

The ligand concentration at which the effect is 50% Emax

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12
Q

Potency

A

The relationship between the amount of drug administered and its effect, the less drug needed to produce an effect, the more potent the drug

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13
Q

Maximal efficacy

A

The maximum effect of a particular drug on the patient

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14
Q

ED50

A

The dose of drug that is effective in 50% of the population - ED50 tells how potent a drug. A lower ED50 indicates that the drug is more potent and less is necessary to produce the desired effect

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15
Q

TD50

A

Toxic dose in 50% of people

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16
Q

LD50

A

Lethal dose in 50% of people

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17
Q

Therapeutic Index

A

TD50:ED50 ratio. Ideally this is a large number to ensure if the patient takes too much drug it will be less likely that they will suffer toxic consequences

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18
Q

Log-normal distribution

A

Represents most drug effects. The curve shows the number of people in the population that respond to a given dose of the drug

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19
Q

Hyporeactive

A

Patients who did not respond until the dosage of the drug was very high

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20
Q

Hyperreactive

A

Patients who responded with very little drug dosage

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21
Q

Hypersensitivity

A

People that have an allergic or inflammatory response to the drug

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22
Q

Bioavailability

A

Fraction of a drug administered that reaches the systemic circulation

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23
Q

First pass effect

A

The amount of drug metabolized or excreted on its first pass through the liver before it reaches the systemic circulation - Reduces bioavailability

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24
Q

Bioequivalence

A

Two preparations that have:

  • Same drug (active ingredients)
  • Same route of administration
  • Same amount of drug
  • Same rate of entry into the circulation
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25
Redistribution
Drug action is terminated because the drug redistributes from its site of action into other tissues
26
Therapeutic window
The concentration of a drug in the body that is high enough to produce the desired effect with a minimum of toxicity
27
Volume of distribution (Vd)
A measure of the apparent space in the body available to contain the drug
28
Clearance
Rate of elimination/concentration
29
Rate of elimination
Directly proportional to drug concentration. As the concentration increases, the elimination increases proportionally so the clearance stays the same
30
Half life
The time required to decrease the concentration of the drug by one half
31
Loading dose
A larger dose of the drug that allows for therapeutic levels to be achieved immediately
32
Maintenance dose
Dose of the drug needed to maintain the drug concentration within the therapeutic window; balance clearance
33
Pro-drug
Drugs that are inactive as given and subsequently metabolized into their active forms
34
Phase I Metabolism
Small change in the makeup of a drug including: oxidation, reduction, dealkylation, or hydrolysis reactions. They often introduce or reveal a functional group
35
Phase II metabolism
A large change in the makeup of the drug; conjugation of the drug or drug metabolite to an endogenous substrate molecule
36
Cytochrome P450
Hemeproteins that are major catalysts of Phase I biotransformation reactions
37
Monooxygenase
Enzyme that catalyzes the addition of oxygen to substrate (Part of P450 catalytic cycle
38
P450 Reductase
Single isoform of P450 reductase in all cell types but many different isoforms of cytochrome p450
39
CYP3A
Handles 50% of drugs - Inhibited by grapefruit juice
40
CYP2D6
Handles 25% of drugs
41
CYP2C9
15% of drugs
42
CYP2C19
≦5%
43
CYP1A2
≦5%
44
CYP2E1
≦5%
45
Flavin-containing monooxygenase
Flavoprotein localized in smooth endoplasmic reticulum that catalyze monooxygenation reactions, primarily of soft nucleophiles (Requires NADPH, O2 and Substrate)
46
UDP-Glucuronosyl Transferase
Located on endoplasmic reticulum - Adds glucuronic acid to substrate in Phase II metabolism
47
Glucuronidation
Process of adding UDP-glucoronic acid to substrate - Conjugation Capacity: High - Abundance of raw materials for conjugation: High
48
N-Acetyltransferase (NAT)
Replaces -OH or -NH2 with an acetyl group on substrate
49
Acetylation
Process of adding Acetyl-CoA to substrate - - Conjugation Capacity: Variable - Abundance of Raw Materials for Conjugation: Variable
50
Sulfotransferase (SULT)
Replaces -OH or -NH2 with 3'-phophoadenosine-5'-phosphosulfate group (PAPS)
51
Sulfation
Processing of adding PAPS to substrate - Conjugation Capacity: Low - Abundance of Raw Materials for Conjugation: Low
52
Glutathione S-Transferase (GST)
Detoxify xenobiotics by catalyzing the nucleophilic attack by GSH on electrophilic carbon, sulfur, or nitrogen atoms of said nonpolar xenobiotic substrates
53
Glutathione Conjugation
High energy intermediate is the drug itself: arene oxides, epoxides, etc... - Conjugation Capacity: Low - Abundance of Raw Materials for Conjugation: Low
54
Enzyme Induction
Exposure to some drugs and environmental chemicals can markedly upregulate enzyme amount and/or activity - usually transcriptional increases (increase or decrease drug effects)
55
Enzyme Inhibition
Drug or environmental chemical may inhibit the metabolism of several drugs (Competitive vs. Non-competitive)
56
Acetaminophen
Has interplay of multiple phase II reactions (SULT, UGT, GST), phase I reaction, CYP2E1 induction
57
Pharmacogenetics
Genetic factors that alter an individual's response to a drug
58
Genotype
An individual's composition at the gene level; the specific genes they have
59
Phenotype
An individual's expression of their genotype
60
Genetic Polymorphism
Mendelian trait that exists in the population in at least two phenotypes neither of which is rare
61
Single nucleotide polymorphism
A change in one single base pair in the DNA sequence that differs form the "wild type" or predominant sequence
62
Halotype
A cluster of SNPs that occur together in an individual
63
Haplotype
Refers to closely linked genetic markers on a chromosome that tend to be inherited together
64
Autosomal co-Dominance
Each allele contributes to phenotype
65
Autosomal Recessive
Wild-type allele has predominant effect; it takes two recessive alleles to see the effect
66
Autosomal Dominant
A single allele predominates over the presence of other possible alleles
67
X-linked inheritance
Genes inherited on X chromosome; all males will express these traits
68
Homozygous
Have two identical alleles
69
Heterozygous
Have 2 different alleles
70
N-Acetyltransferase-2 polymorphism
Responsible for metabolism of anti-tuberculosis drug izoniazid - Genetic differences in NAT-2 explain "fast" versus "slow" acetylators (autosomal recessive)
71
CYP2D6 polymorphism
First identified from those that suffered severe hypotension following administration of the anti-hypertensive debrisoquiine - poor metabolizer variants - also handles antidepressants
72
CYP2C19
``` Poor metabolizer phenotype Affects several important classes of drugs - Anti-convulsants - Proton pump inhibitors - Anti-platelet drugs - Anti-depressants - Anti-cancer - Hormones ```
73
CYP2C9
Poor metabolizer phenotype ( *2 and *3 variants) | Several substrates including some drugs with a narrow therapeutic window (warfarin cleared almost entirely by CYP2C9)
74
Vitamin K receptor (VKORC1) polymorphism
Subunit of the vitamin K epoxide reductase complex - inhibited by warfarin A clade - Haplotypes H1 and H2 require lower warfarin doses and associated with lower expressoin of VKORC1 B clade - Haplotypes H7, H8, H9 require higher warfarin doses and associated with higher expression of VKORC1
75
Pseudocholinesterase polymorphism
Variant response to succinylcholine, a depolarizing muscle relaxant - due to reduced activity variants of pseudocholinesterase (30-90% decrease in cholinesterase activity)
76
TPMT polymorphism
Presents as increased risk for life threatening bone marrow suppression in patients treated with thiopurine drugs due to variants with decreased activity of thiopurine methyltransferase
77
P-Glycoprotein (Pgp) polymorphism
ATP binding protein that effluxes drugs from the gastrointestinal mucosa - polymorphisms result in increased net uptake of the cardiac glycoside, digoxin

PDA Block 1 (13 decks)

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