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Intro to Pharmacology > Intermolecular interactions - Part 2 - and Pharmacokinetics > Flashcards

Intermolecular interactions - Part 2 - and Pharmacokinetics Flashcards

1
Q

What is a pharmacophore?

A

A collection of functional groups that interact with a specific target that give a similar biological effect.

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2
Q

Heroine and morphine both have similar structures yet, heroine is stronger. Why?

A

Heroine has two methoxy groups rather than Hydrogen groups and is thus more non-polar and can be absorbed better.

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3
Q

What are the purposes of any therapeutic agent?

A

To attain desirable conditions (curing, preventing, or maintaining)

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4
Q

What is compliance in medicine?

A

the degree to which a patient correctly follows medical advice.

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5
Q

What are the different causes of non-compliance in patients?

A 
Time of administration
Frequency of administration
Route of administration
Multiple drugs
Age
Patient conditions
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6
Q

Describe how time of administration may hinder patient compliance.

A

ex: have to take every two hours - hard to do

goes hand in hand with frequency of administration

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7
Q

How does ease of administration affect compliance?

A

The easiest way to raise serum concentration of the drug is through IV, but need trained person to do.
So, in most case enteral route is preferred.

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8
Q

How do multiple drugs affect compliance?

A

In the past, needed to take separate drugs for each symptom.
Now, can buy tylenol to treat all symptoms at once.
More convenient.

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9
Q

The kinetics portion of pharmacokinetics refers to what?

A

Variation in drug concentration with time.

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10
Q

What is pharmacokinetics concerned with?

A

The variation in the drug concentration over time as a result of absorption, distribution, metabolism, excretion

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11
Q

What is pharmacokinetics?

A

Study of the fates of drugs in the body or what the body does to the drug.

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12
Q

What is the acronym for pharmacokinetics?

A

ADME

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13
Q

What rates/routes does pharmacokinetics concerned with?

A

Route of administration, rate and extent of absorption, distribution rate (particularly to site of action) and rate of elimination.

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14
Q

When are ADME studies carried out?

A

During R and D.

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15
Q

What does it mean when a drug lacks efficacy?

A

Means a drug is less effective at producing the desired biological effect when compared to a drug currently on the market.

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16
Q

What is absorption (of a drug)?

A

The process of incorporation of a drug into the bloodstream; or
the movement of a drug from its site of administration into the central compartment.

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17
Q

What route of administration does not require absorption?

A

IV - directly placed into the bloodstream

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18
Q

The central compartment generally refers to what?

A

The bloodstream

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19
Q

For enteral administration, where does absorption occur?

Ingestion?

A

Absorption through the GI tract, via the digestive system.

Oral ingestion.

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20
Q

For enteral administration:

Drugs move across a ______ of ______ ______ into the bloodstream.

A

number of membrane barriers

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21
Q

What are the three different types of capillaries?

A

Continuous
Fenestrated
Sinusoid/discontinuous

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22
Q

Where are continuous capillaries found?

A

Fat, muscle, NS

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23
Q

Where are fenestrated capillaries found?

A

Intestinal villi
endocrine glands
Kidney glomeruli

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24
Q

Where are discontinuous/sinusoid capillaries located?

A

Liver, bone marrow, spleen

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25
Q

What are the two subtypes of continuous capillaries?

A

1 - Those with numerous transport vesicles

2 - Those with few vesicles

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26
Q

Where is the first subtype (i.e. those with numerous vesicles) of continuous capillaries found?

A

Primarily found in skeletal muscle, finger, gonads, skin

27
Q

What is the route of administration for the first subtype (i.e. those with numerous vesicles) of continuous capillaries?

A

intramuscular

topical

28
Q

Where is the second subtype (i.e. those with few vesicles) of continuous capillaries found?

A

Primarily found in the CNS

These capillaries are a consituent of the BBB

29
Q

What is the route of administration for the second subtype (i.e. those with few vesicles) of continuous capillaries?

A

Lumbar epidural injection

30
Q

Describe fenestrated capillaries.

Where are they found?

A

Capillaries with many fenestration - windows.
These allow small molecules and limited amounts of protein to diffuse.

Found in the endocrine glands, intestines, pancreas, and glomeruli of kidney.

31
Q

What is the route of administration for fenestated capillaries?

A

Oral - enteral

32
Q

Which capillary type relates most to Lipinski’s rule of 5?

A

Fenestrated capillaries

allow drugs less than 500 Da to pass through more efficiently; particularly for oral drugs.

33
Q

Describe sinusoidal capillaries.

A

A special type of fenestrated capillaries that have larger openings (30-40um in diameter) in the endothelium.

34
Q

What do sinusoidal capillaries allow to pass through?

A

Red and white blood cells and various serum proteins.

35
Q

How are red and white blood cells and various serum proteins aided in passing through discontinuous capillaries?

A

Using a process that is aided by a discontinuous basal lamina.

36
Q

What is the route of administration for discontinuous capillaries?

A

Intraosseus injection - into bone marrow

37
Q

The lipids of the lipid bilayer are of what type?

A

Phospholipids

38
Q

What are the proteins found in lipid bilayers?

A

Peripheral and integral membrane proteins

39
Q

Passive diffusion occurs for what compounds?

A

Water and lipid soluble
Water soluble through channels
lipid soluble through the lipid bilayer

40
Q

______ diffusion is the most common way of absorption.

A

passive

41
Q

What are the different modes of absorption?

A 
passive diffusion
facilitated transport
active transport
ion pair transport
vesicle formations
42
Q

Passive diffusion:
The most _____ and _____ route of drug transfer across membrane
- The rate of absorption is _________ to the _______ of the drug (in the _________ form)
- affected by _________ and membrane penetration

A

important, common
proportional, concentration, unionized
lipophilicity

43
Q

All drugs/compounds contain chemical _______ ______ which act as either weak acids or bases.

A

functional groups

44
Q

What is Fick’s law of diffusion, in equation form?

A

dM/dt = D*A(Ch-Cl)/X

dM/dt - rate of diffusion
D = diffusion coefficient
A - SA
X - membrane thickness
Ch-Cl - concentration difference
45
Q

The diffusion coefficient is affected by what?

A

A drugs molecular weight and P value

46
Q

An increase in SA causes what to absorption?

An increase in membrane thickness?

A

increased absorption

decreased absorption

47
Q

The greater the difference in concentration between compartments, the ______ passive diffusion will occur.

A

faster

48
Q

The drug absorption from the GI tract is dependent on the _______ of the drug present in the gut.

A

amount

49
Q

The rate of diffusion of a drug is related to what?

A

The concentration given to us

50
Q

Facilitated diffusion is still a _______ process.

A

passive

51
Q

Describe facilitated diffusion.

A

Transport using carriers located on the cell membrane.
Follows a concentration gradient
Limited by the number of carriers.

52
Q

B12 is used to treat what?

What route does it use?

A

Cyanide poisoning

IV

53
Q

Active transport:
Use natural mechanisms to transport ______, amino acids, into the _________
- has ______ carrier proteins called - ________
- uses ____ ________
- _______ number of transporters per cell
- can transport _______ the concentration gradient

A 
glucose, cytoplasm
specific - transporter
ATP hydrolysis
limited
against
54
Q

What type of drugs would use active transport?

A

Drugs with structural features similar to cellular metabolites that use active transport.

55
Q

What are the different types of active transporters?

A

Uniporter - carrier has one specific direction for that molecule
Symporter - both same way
Antiporter - one molecule exchanged for another

56
Q

How does 5-fluorouracil get into the body, most likely?

A

Uracil is a nucleic acid.

This drug shares structural similarities and thus uses active transport

57
Q

What is an example of a transporter using ion pair transport?

A

Na+/K+ ATPase

58
Q

What types of drugs use ion pair transport?

A

Drugs as organic anion or cation.

59
Q

Compare passive and active membrane transport.

A

Passive:

  • No ATP hydrolysis to aid transport
  • Follows Ficks Law of diffusion (high concentration compartment to low concentration)

Active

  • Requires ATP hydrolysis
  • can go against the concentration gradient
  • Transporter/carrier required
60
Q

What is pinocytosis?

A

Invagination of part of the cell membrane, resulting in vacuoles.

61
Q

What types of drugs would use vesicle formations?

A

Hormone related drugs (ex: insulin)

62
Q

What drug and bodily factors affecting drug absorption?

A

Drug properties

  • pH
  • P value

Other:

  • Blood flow
  • Surface area
  • contact time
63
Q

For enteric drug delivery, how else can drug absorption be affected?

A

Absorption can be reduced by the presence of food in the gut.
- can affect gut pH (ex: orange juice/coffee)

  • plasma proteins can bind to drugs and increase the rate of passive absorption
    • maintain concentration gradient of free drug
64
Q

What is done when some drugs are irritating?

A

Take with meals to reduce adverse effects.

Intro to Pharmacology (23 decks)

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