Block 3 Flashcards

(72 cards)

1
Q

Where are oral drugs mostly absorbed? and why?

A

Upper part of small intestine because it is rich and blood and has a lot of surface area

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2
Q

What is the rate limiting step of absorption?

A

The drug dissolving

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3
Q

T/F: When bound to proteins, drugs are inactive

A

True

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4
Q

Potentiation

A

When there is drug competition and if a drug is being booted from being bound to protein, more drug is free, so more drug is able to be processed, potentially causing toxicity.

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5
Q

Half life

A

Time required for the body to clear half of the drug

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6
Q

Eliminate rate constant

A

The speed at which a drug or substance is removed from the body through various processesT

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7
Q

Total body clearance

A

Rate of drug eliminate from the body by ALL routes (renal + non-renal)

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8
Q

Zero-order kinetics

A

Elimination is constant regardless of the concentration, leading to a linear decrease in drug level over time. Graph is LINEAR.

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9
Q

First-order kinetics

A

Rate of elimination is proportional to the concentration, resulting in a constant percentage reduction per unit of time. Graph is LOGARITHMIC.

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10
Q

Elimination rate constant (Kel)

A

The speed at which a drug or substance is removed from the body the body through various processes –> gradient/slope of the curve

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11
Q

Half-life

A

Time required for the body to clear half of the drug

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12
Q

How many half lives before a drug is almost completely eliminated from the body?

A

5-6 half lives

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13
Q

Extraction ratio

A

Measure that indicates the fraction of a drug that is removed from the bloodstream by an organ while passing through

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14
Q

Pharmacodynamics

A

The study of how drugs interact with the body at a molecular and cellular level to produce their therapeutic effects

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15
Q

Drug action

A

The mechanisms by which a drug acts to produce effects in a patient

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16
Q

Drug effect

A

The tangible consequence of the drug’s action

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17
Q

Agonist

A

Substance that activates or stimulates a receptor in the body, mimicking the effects of a naturally occurring compound

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18
Q

Antagonist

A

Substance that blocks or inhibits the action of a receptor

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19
Q

Inverse Agonist

A

Substance that not only blocks the activation of a receptor but also produces an opposite or “negative” response compared to the receptor’s natural state
///
A drug that acts on the same receptor as an agonist and produces an opposite effect (opposes through the same pathway)

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20
Q

Mixed agonist-antagonist

A

Substance that can act as both an agonist and an antagonist, depending on the specific receptor or tissue it interacts with (binds to more than 1 receptor)

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21
Q

Full agonist

A

Compound that binds to a receptor and activates it to its maximum potential, does NOT reach a ceiling and you can keep upping the concentration indefinitely due to there being spare receptors (can give as much of a drug as you want and keep increasing the concentration)

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22
Q

Partial agonist

A

Compound that binds to a receptor and only activates it partially, it reaches a ceiling effect

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23
Q

Competitive antagonist

A

Competes with agonists for binding to the same receptor, reducing the receptor’s activation by agonists, and its effects can be overcome by increasing agonist concentration, restoring normal receptor activity

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24
Q

Non-competative antagonism

A

The opposite of competitive antagonists, irreversible reaction and is NOT dose dependent (no matter how many agonists you give this will still work as an antagonist)

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25
Physiological Antagonist
A drug that counters the effect of another drug by binding to a different receptor and causing an opposite effect (opposes through a different pathway)
26
EC50
The concentration of a drug needed to produce 50% of a response. Most potent drug is the one with the lowest EC50
27
Drug specificity
How precisely a drug interacts with a particular target or receptor in the bodyD
28
Drug selectivity
The degree to which a drug acts on a given site as well as other sites dependent on the concentration range
29
Drug therapy
Achieving the maximum benefit (drug effect) with minimum risk of toxic effect
30
Steady state
The plasma concentration of a drug when the maintenance rate of drug administration is equal to the rate of elimination. When the rate of drug intake equals the rate of drug elimination
31
Reaching a steady state concentration is dependent on the drug's ____ and ____
Half life and volume distribution
32
Loading dose
Giving a higher amount of drug at once to get to the steady state sooner
33
T/F: Increasing the rate you administer a drug will affect how fast it reaches the steady state
False: Will not affect how fast it reaches steady state. Only an increase in DOSE can achieve this
34
Vd < 1 L/kg
Low distribution, mostly confined in bloodstream
35
Vd = 1 L/kg
Moderate distribution to tissues
36
Vd > 1 L/kg
Largely distributed to tissues
37
Summation
Occurs when 2+ drugs with similar pharmacological actions are taken together, and their combined effects is equal to the sum of their individual effects
38
Potentiation
Occurs when one drug enhances the effect of another drug when they are taken together, and the combined effect is greater than the sum of the individual effects
39
Synergism
Occurs when 2+ drugs are taken together and have a combined effect that is significantly greater than the sum of their individual effects
40
Antagonism
Occurs when 2+ drugs taken together produce a reduced effect compared to what would be expected based on their individual effects, can occur due to blockage or counteracting one another
41
Pre-approval process
Prior to getting approved by the FDA
42
Two kinds of trials in the pre-approval process
Control trials: Textbook experimental trial where you have a control group and experimental group. Filed trials: Real world experiments outside of a clinical setting, but still not approved.
43
Post-approval process
After getting approval by the FDA, there is an ongoing process of pharmicovigilance. This is when you would catch certain things that wouldn't be apparent in control field/trials (you have a bigger pool of test subjects)
44
Side effects
ANY unintended effect of a drug (good or bad, just not expected). Happens at doses normally used. Related to how pharmacological properties of the drug
45
Adverse drug reactions
BAD unintended effect of a drug. Happens at doses normally used. Not related to the pharmacological properties. Ie: a dog having an allergic reaction to an antibiotic
46
Type A adverse drug reaction
Predictable Exaggeration of pharmacological action Can be altered by drug concentration Is reversible
47
Type B adverse drug reaction
Idiosyncratic (not always related to the drug). Can be referred to as hypersensitivity reactions but not always the case. Not dependent on the dose you give Dependent on the individual animal.
48
Adverse drug experience
ANY adverse effect associated with the use of new animal drug (including if it is not related to the drug and if it is not sued according to the label)
49
Therapeutic Dose
The dose that we want to give in order for the drug to work as it should
50
Minimal therapeutic dose
The least amount of drug you can give that would still be effective
51
Maximal therapeutic dose
The largest amount of drug you can give before it reaches a toxic threshold
52
Therapeutic range
The range between minimal and maximal therapeutic dose that would be effective
53
Effective dose fifty (ED50)
Dose that would cause therapeutic effect in 50% of animals
54
Effective dose ninety-nine (ED99)
Dose that would cause therapeutic effect in 99% of animals
55
Toxic dose
Produce adverse effects
56
Lethal dose
Dose that can cause death
57
Lethal dose fifty (LD50)
Causes death in 50% of population
58
Lethal dose one (LD1)
Causes death in 1% of population
59
Therapeutic window
Range of plasma concentration that patients need to be within to have clinical effects without reaching toxic thresholds
60
Therapeutic index
Ratio between the dose that is effective for 50% of patients (ED50) and toxic for 50% of patients (TD50)
61
Margin of safety
Ratio between the dose of drug that is effective to 99% of the population and lethal to 1% of the population
62
Rate limiting step for oral absorption
Dissolution of a substance
63
T/F: the presence of connective tissue will decrease absorption
True
64
First-Pass Effect
Drugs absorbed from GIT and distribute first to the --> LIVER for metabolism. Some drugs will be metabolized before DISTRIBUTION to other tissues. Drugs with high first-pass metabolism have less distribution.
65
T/F Plasma protein binding prolongs the half life of the drug
True
66
Redistribution of drugs
The movement of drugs from the tissues back to the bloodstream, and sometimes to other tissues
67
Metabolism of drugs
The chemical modification of the drug molecule by the cells of the animal.
68
Cytochrome P450
A hemeprotein that plays a key role in the metabolism of drugs and other xenobiotics
69
Potency
Concentration of drug required to achieve a given effect
70
Tolerance
Gradual decrease in responsiveness to a drug when given repeatedly over days to months. Need for increasing the dose over time.
71
Tachyphylaxis
Acute form of tolerance. Higher drug doses are not likely going to increase drug effects. Depletion of a chemical that is necessary for pharmacological action or receptor phosphorylation
72