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Pharmacology Unit 1 > Pharmaco - Dynamic, Kinetics, & Genomics > Flashcards

Pharmaco - Dynamic, Kinetics, & Genomics Flashcards

(67 cards)

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1
Q

What drugs do to the body

A

Pharmacodynamics

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2
Q

What the body does to drugs:
Absorption
Distribution
Metabolism
Excretion

A

Pharmacokinetics

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3
Q

Specialized target that binds a drug or endogenous ligand and mediates the pharmacologic action

A

Drug Receptor

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4
Q

Nomenclature used when a drug is bound to a receptor.
Initial Phase: drug receptor interaction
Complex phase: biological response

A

Drug Receptor Complex

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5
Q

Occurs when all drug receptors are bound. No further complex & no further increase in response

A

Saturation

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6
Q

Compound that binds to the receptor and stimulates the biological response.
* Usually mimics the response of an endogenous ligand.
* Magnitude of the response depends on how many drug receptor complexes are formed.

A

Agonist

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7
Q

Blocks or reverses the effects of agonists.
- No effect on their own. Can be competitive or non-competitive.

A

Antagonist

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8
Q

Produces a biologic response but not 100% (even at high doses).
- Occupies all receptors but doesn’t activate ligand binding site.
- Opens ion channels differently or incompletely
- Can act as an antagonist if given with full antagonist.

A

Partial Agonist

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9
Q

Competes with agonists for the receptor site
- increase concentration = increased odds of winning the receptor site

A

Competitive Antagonists

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10
Q

Permanently bind with receptor sites and prevent activation by agonists.
- reduces maximal response an agonist can produce.
- cannot be overcome by increase the concentration of the agonist. (the agonist can bind there all it wants; it will still do no good)

A

Noncompetitive Antagonists

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11
Q

Substance that binds to a receptor and causes it to do the opposite of what the naturally occurring transmitter does.
- makes receptors tilt towards the inactive state
or
- decreases the amount of time receptors are open

A

Inverse Agonist

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12
Q

Maximal amount of response a drug can produce

A

Efficacy

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13
Q

Measure of the dose required to produce a response

A

Potency

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14
Q

Measure of drug safety

A

Therapeutic Index

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15
Q

How do you calculate the Therapeutic Index?

A

Lethal Dose₅₀/Effective Dose₅₀

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16
Q

Is a drug safer if the Therapeutic Index is larger or smaller?

A

Larger = Safer

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17
Q

Dose that kills half the population

A

Lethal Dose₅₀

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18
Q

Dose at which half the population responds

A

Effective Dose₅₀

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19
Q

At what number is the Therapeutic Index considered to be narrow?

A

< 2

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20
Q

When two drugs with the opposite effects are given together

A

Functional Antagonism

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21
Q

When an antagonist is administered with an agonist
- Narcan blocking the effects of Heroin.

A

Competitive Antagonism

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22
Q

Diminished response to a drug over time
- receptor desensitization
- receptor down regulation

A

Tolerance

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23
Q

Enhanced response to a drug (super-sensitivity)
- receptor up-regulation = increasing the number of receptors on a cell’s surface

A

Hyperactivity

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24
Q

When the body quickly develops a reduced response to the drug, requires higher doses for the same effect

A

Tachyphylaxis

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25
Enhancement of one drug by another which has no effect on its own - clavulanic acids potentiates amoxicillin (Augmentin)
Potentiation
26
Occurs when the effects of two drugs together is greater than the effect of either drug by itself - Trimethoprim + Sulfamethoxazole (Bactrim)
Synergism
27
Dose related adverse effects of a drug
Toxicity
28
Movement of the drug from the site it was administered into the body
Absorption
29
Amount of drug that is absorbed after oral administration vs. the amount of drug that is absorbed after IV administration
Bioavailability (f)
30
Bioavailability Equation
AUCₒᵣₐₗ / AUCᵢᵥ = f
31
Bioavailability of drugs given IV
f = 1 (100%) because they do not undergo first pass.
32
Driven by a concentration gradient - no carrier and non-saturable - used by most lipid soluble and uncharged drugs
Simple Diffusion
33
Are most drugs polar or non-polar?
Non-polar
34
Carrier mediated and driven by concentration gradient. - Competition by similar molecules and therefore saturable. - NO ATP NEEDED
Facilitated Diffusion
35
Do drugs absorb faster if dissolved in aqueous or oily solutions?
Aqueous
36
Do drugs absorb faster if they have a smaller or larger molecular size?
Smaller Molecular Size
37
Do drugs absorb faster if they have a smaller or larger particle size?
Smaller Particle Size
38
- Most drugs are weak acids or bases - only the nonionized (non-polar form) of the drug can cross the membrane. - Ratio of ionized vs. nonionized is determined at the site of absorption and by the drug's pKa.
Degree of Ionization
39
Likes Dissolve Likes
Acidic drugs = nonionized in acidic medium Basic drugs = nonionized in basic medium
40
Tablet, liquid, capsule, injection, etc. can affect the rate and extent of absorption - liquids given orally are absorbed more rapidly than tabs or caps
Route & Dosage Form
41
Some drugs cannot be absorbed in the GI tract so they must be given IV due to their chemical nature. What drug is an example of this?
Heparin
42
Non-active components of drugs can change absorption - Metoprolol tartrate (IR) vs Metoprolol succinate (ER)
Formulation
43
How does concentration affect absorption?
Higher concentration is absorbed faster
44
How does Area of Absorptive Surface affect absorption?
Larger surface area = faster absorption (intestine > stomach)
45
How does vascularity affect absorption?
Faster absorption in areas with more blood flow (muscle > subcutaneous tissue > stomach)
46
How does pH affect drug absorption?
acidic pH favors acidic drug absorption basic pH favors basic drug absorption
47
How might the presence of other substances affect absorption?
Foods or drugs may interact to alter the rate of absorption
48
How does GI motility affect absorption?
More contact time = more absorption (diarrhea = poor absorption)
49
How does the integrity of the absorptive surface affect absorption?
Edema = decreased absorption Skin thickness can affect topical absorption
50
Initial metabolism in the liver of a drug absorbed from the GI tract before the drugs reaches systemic circulation through the bloodstream (this decreases bioavailability of drugs)
First Pass Effect
51
Initially inactive drugs that exert no pharmacology effects until they are metabolized
Prodrugs
52
Process by which an absorbed drug moves from the site of absorption to other area in the body
Drug Distribution
53
Binding to Plasma Proteins
- mostly albumin - reversible, saturable, subject to competition - SEQUESTERS DRUGS IN THE BLOOD, slows their transfer into tissues, and prolongs their duration of action (Warfarin and Diazepam)
54
Binding to Tissue Proteins
- some drugs accumulate in certain tissues (Benzodiazepines accumulate in fat)
55
Highly perfused organs reach higher concentrations of drug than poorly perfused
Vascularity
56
Other Distribution Factors
Age Gender Body Fat
57
The process of converting a drug into another chemical called a metabolite (biotransformation)
Drug Metabolism
58
What is the major metabolizing organ of the body?
Liver
59
What are the minor metabolizing organs of the body?
GI Tract Lungs Kidneys Skin
60
How does metabolism affect most drugs?
Usually metabolism makes a molecule more water soluble (hydrophilic) to enhance its removal from the body (excretion) as most molecules are lipid soluble and thus normally are hard for the body to excrete
61
These reactions frequently involve the Cytochrome P-450 Enzymes. - Introduces or unmasks a polar functional group to increase renal elimination
Liver Metabolism: Phase I
62
MAKES IT MORE POLAR TO INCREASE RENAL ELIMINATION - reactions are conjugations (united). - combine glucuronic acid, sulfuric acid, acetic acid, or an amino acid with the drug
Liver Metabolism: Phase II
63
Removal of drugs from the body, either unchanged or as metabolites
Drug Elimination
64
What organ eliminates most drugs from the body?
Kidneys
65
Drugs secreted into the bile, then reabsorbed in the small intestine. A fraction is then excreted into the bile, some enters systemic circulation once again. - Prolongs the amount of time the drug is in the body
Enterohepatic Recycling
66
Inherited variation in the DNA sequence (mutation)
Polymorphism
67
Variation in a single base pair within the DNA
Single Nucleotide Polymorphism (SNP)

Pharmacology Unit 1 (5 decks)

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