Block 3 Flashcards

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
Q

Physiological Antagonist

A

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)

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26
Q

EC50

A

The concentration of a drug needed to produce 50% of a response.
Most potent drug is the one with the lowest EC50

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27
Q

Drug specificity

A

How precisely a drug interacts with a particular target or receptor in the bodyD

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28
Q

Drug selectivity

A

The degree to which a drug acts on a given site as well as other sites dependent on the concentration range

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29
Q

Drug therapy

A

Achieving the maximum benefit (drug effect) with minimum risk of toxic effect

30
Q

Steady state

A

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
Q

Reaching a steady state concentration is dependent on the drug’s ____ and ____

A

Half life and volume distribution

32
Q

Loading dose

A

Giving a higher amount of drug at once to get to the steady state sooner

33
Q

T/F: Increasing the rate you administer a drug will affect how fast it reaches the steady state

A

False: Will not affect how fast it reaches steady state. Only an increase in DOSE can achieve this

34
Q

Vd < 1 L/kg

A

Low distribution, mostly confined in bloodstream

35
Q

Vd = 1 L/kg

A

Moderate distribution to tissues

36
Q

Vd > 1 L/kg

A

Largely distributed to tissues

37
Q

Summation

A

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
Q

Potentiation

A

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
Q

Synergism

A

Occurs when 2+ drugs are taken together and have a combined effect that is significantly greater than the sum of their individual effects

40
Q

Antagonism

A

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
Q

Pre-approval process

A

Prior to getting approved by the FDA

42
Q

Two kinds of trials in the pre-approval process

A

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
Q

Post-approval process

A

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
Q

Side effects

A

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
Q

Adverse drug reactions

A

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
Q

Type A adverse drug reaction

A

Predictable
Exaggeration of pharmacological action
Can be altered by drug concentration
Is reversible

47
Q

Type B adverse drug reaction

A

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
Q

Adverse drug experience

A

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
Q

Therapeutic Dose

A

The dose that we want to give in order for the drug to work as it should

50
Q

Minimal therapeutic dose

A

The least amount of drug you can give that would still be effective

51
Q

Maximal therapeutic dose

A

The largest amount of drug you can give before it reaches a toxic threshold

52
Q

Therapeutic range

A

The range between minimal and maximal therapeutic dose that would be effective

53
Q

Effective dose fifty (ED50)

A

Dose that would cause therapeutic effect in 50% of animals

54
Q

Effective dose ninety-nine (ED99)

A

Dose that would cause therapeutic effect in 99% of animals

55
Q

Toxic dose

A

Produce adverse effects

56
Q

Lethal dose

A

Dose that can cause death

57
Q

Lethal dose fifty (LD50)

A

Causes death in 50% of population

58
Q

Lethal dose one (LD1)

A

Causes death in 1% of population

59
Q

Therapeutic window

A

Range of plasma concentration that patients need to be within to have clinical effects without reaching toxic thresholds

60
Q

Therapeutic index

A

Ratio between the dose that is effective for 50% of patients (ED50) and toxic for 50% of patients (TD50)

61
Q

Margin of safety

A

Ratio between the dose of drug that is effective to 99% of the population and lethal to 1% of the population

62
Q

Rate limiting step for oral absorption

A

Dissolution of a substance

63
Q

T/F: the presence of connective tissue will decrease absorption

A

True

64
Q

First-Pass Effect

A

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
Q

T/F Plasma protein binding prolongs the half life of the drug

A

True

66
Q

Redistribution of drugs

A

The movement of drugs from the tissues back to the bloodstream, and sometimes to other tissues

67
Q

Metabolism of drugs

A

The chemical modification of the drug molecule by the cells of the animal.

68
Q

Cytochrome P450

A

A hemeprotein that plays a key role in the metabolism of drugs and other xenobiotics

69
Q

Potency

A

Concentration of drug required to achieve a given effect

70
Q

Tolerance

A

Gradual decrease in responsiveness to a drug when given repeatedly over days to months. Need for increasing the dose over time.

71
Q

Tachyphylaxis

A

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
Q
A