Drug Absorption/Biotransformation? Flashcards

0
Q

Pharmacokinetics

A

examines the movement of a drug over time through the body

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1
Q

Pharmacodynamics

A

mechanisms of drug action are the processes of Pharmacodynamics

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2
Q

Bioavailability

A

% of dose that gets into body

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3
Q

Bioequivalence

A

similarity between two formulations of same drug

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4
Q

Speed of drug onset

A

how long it takes the drug to begin working

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5
Q

Dosing interval

A

how often the drug should be given

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6
Q

site of action

A

whether the drug stays local or acts systemically

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7
Q

what is drug absorption?

A

the movement of drug molecules across biological barriers (mostly layers of cells) from the site of administration to the blood stream

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8
Q

What affects drug absorption?

A

rate of release of drug from pharmaceutical preparation
membrane permeability of drug
surface area in contact with drug
blood flow to site of absorption
destruction of drug at or near site of absorption

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9
Q

what determines rate of release of drug from pharmaceutical preparation?

A
Dosage form 
additives (excipients) 
manufacturing parameters 
delayed release preparations 
sustained release preparations
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10
Q

Dosage form

A

solutions - no delay, immediate response
capsules & tablets - delay (dissolution) followed by rapid release
creams, ointments & suppositories - no delay, but slow release

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11
Q

Additives (excipients)

A

decrease rate of dissolution - binders, lubricants, coating agents
increase rate of dissolution - disintegrants
Variable effects on rate of dissolution - diluents, coloring agents, flavoring agents

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12
Q

Manufacturing parameters

A

tablet compression - hard tablets dissolve more slowly
tablet shape - round tablets dissolve more slowly
tablet size - large tablets dissolve more slowly

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13
Q

Delayed release preparations

A

enteric coating - dissolve in intestines, not stomach

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14
Q

sustained release preparations

A

Reservoir diffusion products - drug diffuses from pill core through membrane shell
Matrix diffusion products - diffuses through matrix in which it is embedded
Matrix dissolution products - released as matrix dissolves
osmotic tablets - pumped out of tablet by osmotic forces
Ion-exchange products - bound to resin exchanges with endogenous ions

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15
Q

Lipophilicity

A

increases membrane permeability
presence of aliphatic and aromatic structures
absence of polar groups

16
Q

Ionization

A

decreases membrane permeability
weak acids in intestines are mostly ionized (intestinal pH ranges from 6.6 to 7.5)
weak bases in stomach are mostly ionized (stomach pH ranges from 1 to 2)

17
Q

Henderson-Hasselbach equation

A

pH = pKa + [nonprotonated species/protonated species]
For acids: pH = pKa + log [A-]/[HA]
For bases: pH = pKa + log [B]/[BH+]

18
Q

when pH is less than pKa,

A

the protonated forms HA and BH+ predominate

19
Q

when pH is greater than pKa, the

A

deprotonated forms A- and B predominate

20
Q

when pH = pKa then

A
HA = A- 
BH+ = B
21
Q

What parts of the anatomy have a low surface area?

A

eyes, nasal, buccal cavity, rectum, stomach large intestines

22
Q

High surface area anatomy

A

small intestines and lungs

23
Q

Low blood flow areas of the body

A

eyes, stomach, large intestines, rectum, subcutaneous tissue

24
Q

High blood flow areas of the body

A

small intestines, lungs, muscle, buccal cavity, nasal cavity

25
Q

what determines whether a drug is destroyed at or near site of administration?

A

Liver - hepatic enzymes (first pass effect)
colon - intestinal microflora
stomach - digestive enzymes and acids

26
Q

Considering types of administration what is most safe to least safe?

A

highest safety is Oral -> SC -> IM -> IV

27
Q

Routes of administration that would be highly bioavailable to least?

A

IV is the highest, IM = SC > oral

28
Q

Onset of action of routes of administration

A

fastest is IV > IM > SC > oral

29
Q

Most interaction with food to least?

A

Oral > IV = IM = SC

30
Q

Highest volume of drug required to least

A

Oral = IV > IM > SC

31
Q

Availability of sustained release dosage forms

A

Highest with IM > oral > SC > IV

32
Q

Tolerance to “funky” vehicles

A

Highest with Oral = IM = SC > IV

33
Q

Sublingual administration

A

rapid absorption that bypasses liver

34
Q

Rectal

A

great for patient that is vomiting or cannot (will not) swallow medication