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Pharmacology > AMDE > Flashcards

AMDE Flashcards

1
Q

How a drug moves from its site of

administration into the bloodstream

A

Absorption

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2
Q

Movement of the drug between blood and

tissues

A

Distribution

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3
Q

Conversion of drugs into more hydrophilic

metabolites

A

Metabolism

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4
Q

Removal of drugs and/or metabolites from

the body

A

Excretion

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5
Q

Where does the majority of the absorption into blood stream from GI tract occur?

A

Small intestine

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6
Q

If the molecule is larger, it will absorb more or less?

A

Less movement

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7
Q

Do ionized or non-ionized molecules move better?

A

Non-ionized

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8
Q

Does increased lipid solubility increase or decrease movement?

A

Increase movement

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9
Q

Does increased protein binding increase or decrease movement/

A

Decreases movement

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10
Q

To pass through lipid membranes, drugs

have to be ________

A

non-ionized (aka: uncharged)

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11
Q

To be water soluble, drugs need to be

_________

A

ionized (aka: charged)

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12
Q

Most drugs are either ____ acids or _____ bases

A

Weak acids or weak bases

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13
Q

What is the protonation and ionization of an acid drug in an acidic ph?

A

non-ionized; protonated

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14
Q

What is the protonation and ionization of an acid drug in an basic ph?

A

Ionized, deprotonated

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15
Q

What is the protonation and ionization of an basic drug in an acidic ph?

A

Ionized, protonated

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16
Q

What is the protonation and ionization of an basic drug in an basic ph?

A

Non-ionized; deprotonated

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17
Q

_____ are non-ionized (fat soluble)
when protonated, ionized (water soluble) when
deprotonated

A

Acids

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18
Q

_____ are non-ionized when deprotonated,

ionized when protonated

A

Bases

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19
Q

The ___ is the pH at which there are
equal amounts of protonated and
nonprotonated

A

pKa

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20
Q

 pH __ pKa  Protonated equals non-

protonated

A

pH=pKa

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21
Q

 pH __ pKa  Protonated form predominates

A

 pH < pKa

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22
Q

 pH ___ pKa  Non-protonated form predominates

A

 pH > pKa

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23
Q

Only the ________ form of a drug can

readily cross the lipid membrane

A

non-ionized

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24
Q 
Ion Trapping
 Because ionized 
molecules (drugs) 
can’t cross the 
membrane, can 
effectively trap them 
and enhance 
excretion
 Principle is very 
useful in toxicology 
cases
A

Ion Trapping

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25
Q

Typically the ____ form of the drug is lipid soluble meaning it readily absorbs into bloodstream

A

Non-ionized

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26
Q

Will a more acidic or basic local anesthetic get absorbed in an abcess better?

A

Acidic

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27
Q

According to Fick’s law, what 2 things are proportional to the rate of absorption?

A

Concentration of drug

Surface Area

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28
Q

 Movement of a drug from its site of administration into the central compartment
 Process of dissolution and diffusion
 Bioavailability more important

A

Absorption

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29
Q

 Fraction of drug that reaches the systemic
circulation intact
 IV = 100%
 Affected by route of administration

A

Bioavailability (F)

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30
Q

 Fraction of drug in blood that is irreversibly

removed during one pass through the liver

A

Hepatic extraction ratio

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31
Q

 Extent to which a drug is removed by the liver
during its first pass in the portal blood through
the liver to systemic circulation

A

First pass clearance

32
Q

Drugs with low hepatic extraction will have

___ first pass clearance

A

low first pass clearance

33
Q 
\_\_\_\_ extraction
 Low first pass 
clearance
 Change in hepatic 
enzymes won’t have 
significant effect on 
first pass clearance
- Increased drug in bloodstream
A

Low extraction

34
Q 
\_\_\_\_\_ extraction
 High first pass 
clearance
 Changes in enzyme 
function will have large 
effect on first pass 
effect
- Decreased drug in bloodstream
A

High extraction

35
Q

_____ route of administration:

Hits digestive system before going to bloodstream

A

Enteral

36
Q

_____ route of administration:

-Bypasses digestive tract: Decreases first pass effect

A

Parenteral route

37
Q 
\_\_\_\_\_ administration
ADVANTAGES
 Most common route
 Safest
 Easiest
 Most economical
DISADVANTAGES
 Limited absorption
 Emetogenic potential
 Subject to first pass
 Absorption may be 
affected by food or other 
drugs
 Irregularities in 
absorption or propulsion
A

Enteral administration

38
Q 
\_\_\_\_\_\_ Administration
ADVANTAGES
 Not subject to first pass
 Most rapid onset
 Ability to titrate
 Doesn’t require cooperation
DISADVANTAGES
 Greater patient discomfort
 Requires additional training 
to administer
 Concern for bacterial 
contamination
 Injection-associated risks
 Extravasation
 Intra-arterial injection
 Limb loss
A

Parenteral Administration

39
Q 
\_\_\_\_\_ Administration
 Absorption governed by:
 Surface area for absorption
 Blood flow to site of absorption
 Dosage form administered
 Ionization status (lipo- vs. hydrophilic)
 Concentration at site of absorption
A

Oral Administration

40
Q 
 Drugs destroyed by 
gastric secretions, low 
pH, or that cause 
gastric irritation
 Risk of bezoar 
formation
 Delayed Release
A

 Enteric coating

41
Q

F = 100%● Immediate onset, Bypasses GI absorption

● Best for emergencies

A

►Intravenous (IV):

42
Q

75-100%● Irritating drugs given this route
● Not as rapid response as IV
● Depot preparations (sustained release) ie., suspensions, ethylene glycol,
peanut oil- all slow down absorption.

A

►Intramuscular (IM):

43
Q

: 75-100%● Slower absorption than IV or IM
● Little risk of intravascular injection
● Examples: Insulin, Mechanical pumps, heparin (DVT prophylaxis)

A

►Subcutaneous (SQ)

44
Q

:● Small amounts of drug

● Tuberculosis skin test, Local anesthetics

A

► Intradermal (ID)

45
Q

5-100%● Almost as rapid as IV. (Method of abuse)● Delivered directly to lung (good selectivity)- minimal systemic side-effects.
● Gases, aerosols of solutions & powders -good for respiratory conditions.

A

► Inhalation:

46
Q

: 5-100%● Vasopressin for tx of diabetes insipidus, calcitonin (osteoporosis).
● Method of drug abuse.

A

► Intranasal

47
Q

● Subarachnoid space of spinal cord – into CSF (Lumbar puncture- Baclofen
in MS, regional anesthetic in delivery, morphine drip)

A

Intrathecal/Epidural:

48
Q

Skin, oral mucosa, sublingual, rectal (avoids 50% of 1st pass metab)
● When local effect is desired-but can provide systemic effects.
● Sublingual (100%), rectal (50%) bypasses liver- good bioavailability.
● Transdermal Controlled Release- Scopolamine, nitroglycerin, nicotine,
estrogens (BCP), fentanyl.

A

Topical:

49
Q

Perio specific uses: doxycycline(Atridox); minocycline(Arestin)

A

Subgingival:

50
Q 
 The administered drug leaves the blood 
stream and enters other “compartments”
 Dependent upon:
 Cardiac output
 Capillary permeability
 Blood flow
A

Distribution

51
Q

What are the 3 things that distribution is dependent on?

A

Cardiac output
Capillary permeability
Blood flow

52
Q

The the heart, liver, kidney, adipose tissue, and brain; rank the amount of blood flow from most to least?

A 
Kidney
Liver
Heart
Brain
Adipose tissue
53
Q

____ compartment

 Well perfused organs and tissues (heart, blood, liver, brain, kidney). Drug equilibrates rapidly.

A

 Central

54
Q

_____ compartment

 Less well perfused organs/tissues (adipose, skeletal muscle, etc.)

A

 Peripheral

55
Q

______ compartments

 CSF, CNS, pericardial fluid, bronchial secretions, middle ear

A

 Special compartments

56
Q

What protein binds acidic drugs?

A

Albumin

57
Q

What protein binds basic drugs?

A

Alpha-glycoprotein

58
Q

 Distribution of a drug that moves From site of action into other
tissues or sites

A

 Redistribution

59
Q 
 Lipid solubility
 Clinical effects
 Efflux transporters
 Inflammatory 
processes
A

Blood brain barrier

60
Q 
 Volume of fluid in which a drug would 
need to be dissolved to have the same 
concentration in plasma.  Doesn’t 
represent “real” volume
 Relationship between dose and resulting 
Cp
A

Volume of Distribution (Vd)

61
Q

 Lipophilic drugs tend to have a ___ Vd

A

larger

62
Q

Protein bound drugs have ____ Vd

A

lower

63
Q 
 Removal
 Either metabolized/biotransformed and 
eliminated or excreted unchanged
 Must be water-soluble to be removed
 Lipid solubility good for absorption and 
distribution, bad for excretion
 Process of biotransformation
 Converts drugs into polar metabolites
 Lipophilic into hydrophilic
 Liver does the heavy lifting
 P-450
A

Metabolized

64
Q

What organ does the majority of metabolism?

A

Liver

65
Q

What cytochrome system does the majority of metabolism in liver, kidneys, and intestines?

A

P-450

66
Q

Phase ___ of metabolism
 Catabolic
 Exposes functional group on parent compound
 Usually results in loss of pharmacologic activity
 Activation of prodrugs

A

Phase 1

67
Q

IF there is a drug inhibitor that inhibits drug binding to enzyme, is there an increased or decreased drug response?

A

Increased drug response

68
Q

IF there is a drug inducer that induces drug binding to enzyme, is there an increased or decreased drug response?

A

Decreases drug response

69
Q 
Phase \_\_\_ of metabolism
 Occurs after functional groups are exposed
 Anabolic: adds water soluble molecules to 
structure
 Much less interpatient variability
 Major reactions
 Glucuronidation 
 Glutathione conjugation
 Sulfate conjugation
 Acetylation
A

Phase II

70
Q

 Removal of unchanged drug
 Kidney, lung, feces – primary routes
 Polar compounds > lipid soluble
compounds

A

Excretion

71
Q

During excretion, is the lipid or water soluble more prevalent?

A

Water soluble

72
Q 
 3 processes
 Glomerular filtration
 Active tubular secretion
 Passive tubular reabsorption
 Dependent upon renal function Only unbound drug filtered Non-ionized weak acids and bases passively reabsorbed Alkaline urine “traps” ionized, acidic molecules, increases excretion
A

Excretion

73
Q

Unabsorbed orally administered meds; the metabolites are excreted in the ____

A

Bile

74
Q

_______ is main factor that determines rate of passive transport

A

Lipid solubility

75
Q

Only _____ drugs can diffuse across lipid membrane

A

uncharged

Pharmacology (12 decks)

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