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Disease and Defense- Pharm > Drug Absorption > Flashcards

Drug Absorption Flashcards

1
Q

The effect of any given dose of drug on the Cp of that drug will depend on the ______ and _____ of drug from the site of administration to the blood.

A

rate (time to peak); extent (bioavailability) of transfer

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1
Q

When would the rectal route be chosen?

A

when pt is vomiting, uncon, post-surgery, GI irritation, or uncooperative

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1
Q

What is the bioavailability of subcutaneous administration?

A

very high- almost that of IV

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2
Q

Knowledge of _____ allows for dosage adjustments when the drug is given by different routes of administration.

A

drug bioavailability

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3
Q

What is the bioavailability of IV administration?

A

100%

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3
Q

If the inhaled particle size is < 0.5 μM, the drug is _____, leading to _____.

A

exhaled, no effect

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3
Q

The topical route is a localized application via _____ for treating local conditions.

A

skin or mucous membranes

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4
Q

A generic drug formulation is said to be bioequivalent to a brand name drug formulation if the ____ and _____ of absorption are similar to the brand name.

A

rate and extent

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5
Q

Drugs with a _____ are typically administered via IV.

A

narrow therapeutic index

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6
Q

What are the 2 most important factors to consider when choosing a route of administration?

A

1) bioavailability 2) relative rates of onset

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6
Q

What is the bioavailability of IM administration?

A

very high- almost that of IV

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7
Q

The transdermal route of administration is for ______.

A

systemic use

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8
Q

Why is the rate of absorption so fast in the inhaled route?

A

large surface area and blood flow in pulmonary tissue

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9
Q

What is the equation for F?

A

F = AUC (route) / AUC (IV)

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9
Q

How rapid is the onset of action of the oral route?

A

slow

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10
Q

Why are IV and inhaled drugs so addicting?

A

because their rate of action is so fast

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11
Q

How is the lipid solubility estimated?

A

oil:water partition coefficient

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12
Q

What is the bioavailability of the buccal/sublingual route?

A

high

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13
Q

What administration type has the second slowest time to peak?

A

subcutanous

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15
Q

The effect of any given dose of drug on the plasma concentration of that drug (Cp) will depend on the rate (time to peak) and extent (bioavailability) of transfer of drug from _______.

A

the site of administration to the blood

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16
Q

Name 2 routes for local effects.

A

1) inhalation (if targeting the lungs) 2) topical

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17
Q

In the _____ route, approximately 50% of dose will bypass the liver, thus first pass metabolism is less than for the oral route.

A

rectal

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18
Q

In the rectal route, approximately ____% of dose will bypass the liver, thus first pass metabolism is ____ than for the oral route.

A

50; less

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19
Q

What administration type has the slowest time to peak?

A

oral

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21
Where is the concentration gradient created?
at the site of administration
22
What is the pKa of a sulfate group?
1
22
What is the onset speed of rectal administration?
slow
22
Sublingual/buccal drugs are typically _____ and \_\_\_\_\_.
lipid soluble; potent
22
Which route is the most hazardous?
IV
23
After absorption from oral mucosa, venous drainage from the mouth is to the \_\_\_\_\_\_, protecting the drug from rapid hepatic first-pass metabolism (faster onset of action).
superior vena cava
24
Because of the extremely large surface area of the intestine relative to the stomach, the rate of absorption of a drug from the intestine will be ______ than that from the stomach.
greater
24
After absorption from oral mucosa, venous drainage from the mouth is to the superior vena cava, protecting the drug from rapid _______ (faster onset of action).
hepatic first-pass metabolism
24
If the inhaled particle size is 1-5 μM, the drug is \_\_\_\_\_\_, leading to \_\_\_\_\_\_.
deposited in small airways; a therapeutic effect
26
How can the rate of absorption via the oral route be changed?
increase by using liquids or rapidly disintegrating tablets; decrease with enteric coated tablets or sustained release
28
Name 4 factors that affect drug membrane passage.
1) molecular size 2) lipid solubility 3) degree of ionization 4) concentration gradient
29
What is the rate of onset of the buccal/sublingual route?
within minutes
30
If the drug is placed _____ the gastrointestinal tract it is called enteral; if it's _____ the GI tract, it's called parenteral.
within; outside
31
Increased GI motility will increase ______ by allowing drug to reach the small intestine faster.
speed of emptying and absorption speed
32
If the inhaled particle size is _____ μM, the drug is exhaled, leading to no effect.
\< 0.5
33
IM injections in ______ exhibit slower, more sustained absorption.
depot forms in oil or suspended in other vehicles
33
If the inhaled particle size is ____ μM, the drug is deposited in small airways, leading to a therapeutic effect.
1-5
34
Most drug absorption from GI tract occurs via \_\_\_\_\_, thereby favoring absorption when the drug is in the non-ionized and more lipophilic form.
passive diffusion
35
What is the most important mechanism of diffusion for the majority of drugs with a mw of 500-800?
lipid diffusion
35
The period of drug absorption can be altered intentionally in _____ administration.
subcutaneous
36
The _____ route is a localized application via skin or mucous membranes for treating local conditions.
topical
37
What is the rate of action for IV administration?
fastest of all
38
What administration type has the second fastest time to peak?
IM
40
What affects the degree of ionization?
tissue pH
41
What is the bioavailability of inhalation administration?
very high- almost that of IV
43
\_\_\_\_\_ delays absorption of most drugs by delaying gastric emptying.
Food
45
Most drug absorption from GI tract occurs via passive diffusion, thereby favoring absorption when the drug is in the _____ and more ______ form.
non-ionized; lipophilic
47
What affects the value of F?
1) survival of drug in GI environment 2) ability to cross GI membrane 3) drug metabolism in the gut wall or liver (4. patient compliance)
48
Lipid diffusion is favored if the drug has \_\_\_\_\_.
a high lipid:water partition coefficient
48
Because of the _____ of the intestine relative to the stomach, the rate of absorption of a drug from the intestine will be greater than that from the stomach.
extremely large surface area
49
Food delays absorption of most drugs by \_\_\_\_\_.
delaying gastric emptying
50
IM injections in depot forms in oil or suspended in other vehicles exhibit ______ absorption.
slower, more sustained
51
What is the rate of action for inhalation administration?
very fast (less than 5 min)
53
If the drug is placed within the gastrointestinal tract it is called \_\_\_\_\_; if it's the GI tract, it's called \_\_\_\_\_\_.
enteral; parenteral
55
What is the bioavailability of an oral drug?
varies between 0-100%
56
In \_\_\_\_\_\_, the drug must be potent, able to permeate skin, nonsensitizing, and nonirritating.
transdermal administration
57
\_\_\_\_\_\_ will increase speed of emptying and absorption speed by allowing drug to reach the small intestine faster.
Increased GI motility
58
Drugs with a narrow therapeutic index are typically administered via \_\_\_\_.
IV
59
Why is IV administration more dangerous than inhalation?
a higher dose can be given
60
What does the degree of ionization effect?
lipid solubility
62
Which drugs use endocytosis to enter the cell?
vitamin B12 and iron
63
What is the bioavailability of the rectal route?
variable, but usually greater than oral
64
In the rectal route, approximately 50% of dose will bypass the \_\_\_\_, thus first pass metabolism is less than for the _____ route.
liver; oral route
65
Which drugs use carrier-mediated diffusion?
xenobiotics, P-glycoproteins
66
How is bioavailability determined?
compare the area under the curve of a dose via any administration to the same drug given via IV
67
Enteral routes of administration include ____ while parenteral routes include \_\_\_\_\_\_\_.
oral and rectal; all others
69
Information on rate of absorption is generally estimated as the _____ or \_\_\_\_\_.
peak Cp; time to attain peak Cp plasma levels
70
The effect _______ on the plasma concentration of that drug (Cp) will depend on the rate (time to peak) and extent (bioavailability) of transfer of drug from the site of administration to the blood.
of any given dose of drug
70
Knowledge of drug bioavailability allows for _____ when the drug is given by different routes of administration
dosage adjustments
71
In transdermal administration, the drug must be \_\_\_\_, \_\_\_\_\_\_, \_\_\_\_\_\_, and \_\_\_\_\_\_\_.
potent, able to permeate skin, nonsensitizing, nonirritating
73
Why does F = 100% in IV administrations?
no absorption step involved
74
Does the transdermal route of administration bypass first clearance?
yes
75
After absorption from the \_\_\_\_\_\_, venous drainage from the mouth is to the superior vena cava, protecting the drug from rapid hepatic first-pass metabolism (faster onset of action).
oral mucosa
76
If the inhaled particle size is \> 10 μM, the drug is \_\_\_\_\_, leading to \_\_\_\_\_\_.
deposited in the oropharynx; side effects
78
What is the rate of action for subcutaneous administration?
slower, constant
79
What is the rate of action for IM administration?
fast
80
If the inhaled particle size is ____ μM, the drug is deposited in the oropharynx, leading to side effects.
\> 10
82
What are some disadvantages of controlled-release preparations?
variability in systemic levels; dose toxicity
83
Drugs with a mw of 100-200 generally transport via \_\_\_\_.
aqueous diffusion
84
Subcutaneous administration can only be used for _____ drugs, and the ____ of the dose is limited.
non-irritating; volume
85
What does F stand for?
bioavailability
86
Name 4 routes of administration, other than IV, that use systemic drug action and F nearly = 100%.
1) intramuscular (IM) 2) Subcutaneous (SC) 3) inhaled 4) sublingual
87
\_\_\_\_\_ routes of administration include oral and rectal while ______ routes encompass all others.
Enteral; parenteral
88
What are some disadvantages to IM administration?
pain, tissue necrosis, microbial contamination
89
What does F equal in an IV administration?
100%
90
What administration type has the fastest time to peak?
IV and inhalational

Disease and Defense- Pharm (12 decks)

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