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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
If Vd > total body H2O -->
drug is being concentrated in tissues
26
If Vd
drug is being retained in bloodstream
27
What does distribution of a drug mean?
drug is moving throughout the body
28
What 4 things does volume of distribution depend on?
1. Tissue Permeability 2. Blood Flow 3. Plasma Protein Binding 4. Subcellular Protein Binding
29
How does tissue permeability effect distribution?
- highly lipid soluble molecules cross membranes more easily - solubility concerns - membrane permeability
30
How does blood flow effect distribution?
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
How does plasma protein binding effect distribution?
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
How does subcellular protein binding effect distribution?
drug gets trapped within the cell (usually in the lysosome) | -ex. anti-depressants
33
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?
100mg / 2.0mg/ml = 50ml
34
Where are drugs primarily metabolized? Where else are they metabolized?
Primarily in Liver | -Also occurs in lungs, kidneys, GI, and skin
35
What are 3 main factors that affect drug metabolism?
1. Tissue/organ damage 2. metabolic inhibitors 3. enzyme induction
36
What is Competitive Inhibition of metabolism?
inhibition of the enzyme that metabolizes drug B by drug A | -decreases metabolism of drug B
37
What is Irreversible inhibition of metabolism?
inhibition of the enzyme that metabolizes drug B by drug A via covalent binding -decreases metabolism of drug B
38
What is Induction of metabolism?
induction of the enzyme that metabolizes drug B by drug A | -increases metabolism of drug B by increasing the enzyme quantity
39
What is Biotransformation?
aka Metabolism | -chemical altering of a drug to a metabolite via enzymes to deactivate that drug
40
What are the three ways that drugs can be eliminated?
1. Biotransformation (metabolism) 2. Excretion 3. Combination of Biotransformation and Excretion
41
What are cellular mechanisms for Biotransformation? (4)
1. Oxidation 2. Reduction 3. Hydrolysis 4. Conjugation
42
What are the 3 factors affecting metabolism?
1. Tissue/organ damage 2. Metabolic inhibitors (competitive and irreversible) 3. Enzyme induction
43
How does Oxidation cause biotransformation?
usual method via endoplasmic smooth reticulum via enzymes; (+) O2 (-)H; Phase I reaction
44
How does Reduction cause biotransformation?
(-)O2 (+)H; happens in cell via cytoplasm via enzymes; Phase I reaction
45
How does Hydrolysis cause biotransformation?
original compound is broken into separate parts via enzymes; Phase I reaction
46
How does Conjugation cause biotransformation
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
What exactly is excretion in elimination?
eliminating active form of a drug
48
Where does excretion occur?
at kidneys
49
What factors affect excretion? (2)
1. Reabsorption | 2. Polarity of metabolite
50
T/F: Polar (ionized) drugs tend to be excreted, while non-polar drugs tend to be reabsorbed into the body.
True
51
How is Clearance defined?
ability of organs to clear a drug; -dependent on organs ability to extract drug from plasma and perfusion
52
What three factors affect Clearance?
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
What is Half-Life?
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
What is half-life a function of?
both clearance and volume of distribution
55
T/F: Clearance is measured in mL/min because it is measuring drug being removed from a specific volume of blood.
False - this is not a good physical description of what is happening
56
What are the two forms of dosing schedules?
1. Continuous Administration | 2. Interval Administration
57
What is being done in Continuous Administration dosing schedule?
matching the rate of administration with the rate of drug elimination (clearance) once the desired plasma concentration is achieved
58
What is being done in an Interval Administration dosing schedule?
dosage is adjusted to provide an average plasma concentration over the dosing period
59
The dosage interval (time in hours) will affect ___ needed to maintain same relative plasma concentration.
size of dosage
60
Drug Administration: Oral - Advantages: - Disadvantages: - Example:
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
Drug Administration: Sublingual - Advantages: - Disadvantages: - Example:
Drug Administration: Oral -Advantages: Rapid onset; not subject to first pass inactivation. - Disadvantages: Drug must be easily absorbed from oral mucosa - Example: Nitroglycerin
62
Drug Administration: Rectal - Advantages: - Disadvantages: - Example:
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
Drug Administration: Inhalation - Advantages: - Disadvantages: - Example:
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
Drug Administration: Injection - Advantages: - Disadvantages: - Example:
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
Drug Administration: Topical - Advantages: - Disadvantages: - Example:
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
Drug Administration: Transdermal - Advantages: - Disadvantages: - Example:
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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