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DPT710A: Pharmacology > Pharm Final: Intro and Pharmokinectics > Flashcards

Pharm Final: Intro and Pharmokinectics Flashcards

1
Q

‘pril’

A

Ace Inhibitors (Ramipril)

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2
Q

‘sartan’

A

Angiotensin Receptor Blockers

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3
Q

‘pine’

A

Calcium Channel Blockers

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4
Q

‘olol’

A

Beta Blockers

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5
Q

What is a dose?

A

amount of drug administered in a given formulation

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6
Q

The response of a drug is essentially proportional to the ___ but not always a linear relationship.

A

of receptors occupied by the drug

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7
Q

A drugs response is affected by what two factors involving the receptor?

A

affinity and receptor signal transmission

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8
Q

The curve of a Dose Response Curve represents __ (2)

A
  1. the dosage over which the drug is effective

2. peak effect/response that can be expected

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9
Q

T/F: Dose response curves can be applied to the population.

A

False: only for a single individual or homogenous population

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10
Q

What is a threshold dose?

A

where response begins and increases in magnitude until a response plateau is reached.

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11
Q

What is a ceiling effect?

A

Maximal Efficacy. The point at which there is no further response (even if dosage continues to be increased)

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12
Q

Define potency?

A

Threshold dose that produces a given response.

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13
Q

A high potency means ___ of the compounds is required to produce a given response

A

less

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14
Q

Define Efficacy?

A

dose ranges of which the drug has desired effect

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15
Q

as dose increases, magnitude of response ___

A

increases

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16
Q

Define First Pass Effect

A

Metabolism/destruction of drug molecule in liver before reaching its site of action

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17
Q

Are enteral or paraenteral subject to the first pass effect?

A

Enteral (oral) medications are subject to the first pass effect.

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18
Q

Why are paraenteral medications not subject to the first pass effect?

A

Paraenteral (oral, sublingual, rectal) medications bypass GI system and takes a more direct route to target site.

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19
Q

Define Bioavailability

A

% of drug administered that reaches the bloodstream

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20
Q

If the Bioavailability of a drug is 10% and 100mg are administered, what does this mean?

A

10mg of the drug make it to the blood stream

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21
Q

What is the Bioavailability of a drug that is injected?

A

100%

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22
Q

What does Bioavailability depend on?

A
  • Route of administration
  • Drugs ability to cross membrane barriers
  • Extent of first pass mechanism
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23
Q

How do you calculate Volume of Distribution?

A

Vd = amount of drug administered / concentration of drug is plasma

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24
Q

If Vd = total amount of body H2O –>

A

uniform body distribution

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25
Q

If Vd > total body H2O –>

A

drug is being concentrated in tissues

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26
Q

If Vd

A

drug is being retained in bloodstream

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27
Q

What does distribution of a drug mean?

A

drug is moving throughout the body

28
Q

What 4 things does volume of distribution depend on?

A
  1. Tissue Permeability
  2. Blood Flow
  3. Plasma Protein Binding
  4. Subcellular Protein Binding
29
Q

How does tissue permeability effect distribution?

A
  • highly lipid soluble molecules cross membranes more easily
  • solubility concerns
  • membrane permeability
30
Q

How does blood flow effect distribution?

A

blood stream carries drugs to highly perfused organs; can be affected by disease

  • Negative venule pressure pulls drug from tissues back into blood
  • Positive arteriole pressure draws drug via blood into tissue spaces
31
Q

How does plasma protein binding effect distribution?

A

reversible bonds; bound portion of drug doesn’t have a therapeutic effect and is not eliminated

  • drug that is bound to plasma protein cannot leave the blood to distribute into tissues (inactive)
  • drug that is unbound (free) may distribute from blood to tissues (active)
32
Q

How does subcellular protein binding effect distribution?

A

drug gets trapped within the cell (usually in the lysosome)

-ex. anti-depressants

33
Q

Inject 100mg of a drug into an unknown volume and stir. If we draw 1.0ml and find that there is 2.0mg/ml, what is our volume of distribution?

A

100mg / 2.0mg/ml =

50ml

34
Q

Where are drugs primarily metabolized? Where else are they metabolized?

A

Primarily in Liver

-Also occurs in lungs, kidneys, GI, and skin

35
Q

What are 3 main factors that affect drug metabolism?

A
  1. Tissue/organ damage
  2. metabolic inhibitors
  3. enzyme induction
36
Q

What is Competitive Inhibition of metabolism?

A

inhibition of the enzyme that metabolizes drug B by drug A

-decreases metabolism of drug B

37
Q

What is Irreversible inhibition of metabolism?

A

inhibition of the enzyme that metabolizes drug B by drug A via covalent binding
-decreases metabolism of drug B

38
Q

What is Induction of metabolism?

A

induction of the enzyme that metabolizes drug B by drug A

-increases metabolism of drug B by increasing the enzyme quantity

39
Q

What is Biotransformation?

A

aka Metabolism

-chemical altering of a drug to a metabolite via enzymes to deactivate that drug

40
Q

What are the three ways that drugs can be eliminated?

A
  1. Biotransformation (metabolism)
  2. Excretion
  3. Combination of Biotransformation and Excretion
41
Q

What are cellular mechanisms for Biotransformation? (4)

A
  1. Oxidation
  2. Reduction
  3. Hydrolysis
  4. Conjugation
42
Q

What are the 3 factors affecting metabolism?

A
  1. Tissue/organ damage
  2. Metabolic inhibitors (competitive and irreversible)
  3. Enzyme induction
43
Q

How does Oxidation cause biotransformation?

A

usual method via endoplasmic smooth reticulum via enzymes; (+) O2 (-)H; Phase I reaction

44
Q

How does Reduction cause biotransformation?

A

(-)O2 (+)H; happens in cell via cytoplasm via enzymes; Phase I reaction

45
Q

How does Hydrolysis cause biotransformation?

A

original compound is broken into separate parts via enzymes; Phase I reaction

46
Q

How does Conjugation cause biotransformation

A

Drug or metabolite bi-produce of one of other mechisms is couples into an endogenous substance via enzymes or endoplasmic reticulum and in cytoplasm; Phase II reaction

47
Q

What exactly is excretion in elimination?

A

eliminating active form of a drug

48
Q

Where does excretion occur?

A

at kidneys

49
Q

What factors affect excretion? (2)

A
  1. Reabsorption

2. Polarity of metabolite

50
Q

T/F: Polar (ionized) drugs tend to be excreted, while non-polar drugs tend to be reabsorbed into the body.

A

True

51
Q

How is Clearance defined?

A

ability of organs to clear a drug; -dependent on organs ability to extract drug from plasma and perfusion

52
Q

What three factors affect Clearance?

A
  1. Blood flow to Organ (Q)
  2. Extraction Ratio - fraction of drug removed from the plasma as it passes through the organ (Ci-Co)
  3. Concentration
53
Q

What is Half-Life?

A

duration of activity of the compound in the body; amount of time required for 50% of the drug remaining in the body to be eliminated

54
Q

What is half-life a function of?

A

both clearance and volume of distribution

55
Q

T/F: Clearance is measured in mL/min because it is measuring drug being removed from a specific volume of blood.

A

False - this is not a good physical description of what is happening

56
Q

What are the two forms of dosing schedules?

A
  1. Continuous Administration

2. Interval Administration

57
Q

What is being done in Continuous Administration dosing schedule?

A

matching the rate of administration with the rate of drug elimination (clearance) once the desired plasma concentration is achieved

58
Q

What is being done in an Interval Administration dosing schedule?

A

dosage is adjusted to provide an average plasma concentration over the dosing period

59
Q

The dosage interval (time in hours) will affect ___ needed to maintain same relative plasma concentration.

A

size of dosage

60
Q

Drug Administration: Oral

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Oral
-Advantages: Easy, safe, convenient

  • Disadvantages: Limited or erratic absorption of some drugs; chance of first pass inactivation in liver
  • Example: Analgesics; sedative-hypnotics; many others
61
Q

Drug Administration: Sublingual

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Oral
-Advantages: Rapid onset; not subject to first pass inactivation.

  • Disadvantages: Drug must be easily absorbed from oral mucosa
  • Example: Nitroglycerin
62
Q

Drug Administration: Rectal

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Rectal
-Advantages: Alternative to Oral Route; local effect on rectal tissues

  • Disadvantages: Poor or incomplete absorption; hance of rectal irritation
  • Example: Laxatives; suppository forms of other drugs
63
Q

Drug Administration: Inhalation

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Inhalation
-Advantages: Rapid onset; direct application for respiratory disorders; large surface area for systemic absorption

  • Disadvantages: chance of tissue irritation; patient compliance sometimes a problem
  • Example: General Anesthetics; anti-asthmatic agents
64
Q

Drug Administration: Injection

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Injection
-Advantages: Provides more direct administration to target tissues; rapid onset

  • Disadvantages: Chance of infection if sterility is not maintained
  • Example: Insulin; antibiotics; anti-cancer drugs; narcotic analgesics
65
Q

Drug Administration: Topical

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Topical
-Advantages: Local effects on surface of skin

  • Disadvantages: Only effective in treating outer layers of the skin
  • Example: Antibiotic ointments; creams used to treat minor skin irritation and injury
66
Q

Drug Administration: Transdermal

  • Advantages:
  • Disadvantages:
  • Example:
A

Drug Administration: Transdermal
-Advantages: Introduces drug into body without breaking the skin; can provide steady, prolonged delivery via medicated patch

  • Disadvantages: drug must be able to pass through dermal layers in tact (don’t use heat on fentanyl patch)
  • Example: Nitroglycerin; motion sickness medications; durgs used with phonophoresis and iontophoresis

DPT710A: Pharmacology (8 decks)

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