Distribution Flashcards

1
Q

refers to the reversible transfer of drug from one location to another within the body.

A

Distribution

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Factors Affecting Distribution (5)

A
  1. Regional blood flow
  2. Capillary permeability
  3. Physicochemical properties of the drug
  4. Protein binding
  5. Volume of distribution
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Regional blood flow
(Rate of distribution)
- Give 4 highly perfused organ that increases the drug distribution

A

Brain
Heart
Liver
Kidney

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Regional blood flow
(Rate of distribution)
Give 3 slow perfused organ that decreases the drug distribution

A

Fat
Tissue
Skin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

(Factor) It is the ability to pass through capillary and enter to tissues

A

Capillary permeability (volume of blood )

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are the 2 junction types or capillary permeability

A

Discontinuous
Continuous

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

junction type of capillary permeability that:
—- has spaces in between
—- easily pass through

A

Discontinuous

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Ex. Organ that has discontinuous type

A

Liver
—— fast distribution (1st factor)
—— easily pass through (2nd factor)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Ex. Organ that has discontinuous type

A

Liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Ex. Organ that has continuous type

A

Brain (BBB - walls of capillary)
—— fast distribution (factor 1)
—— not easily pass through (factor 2)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

junction type of capillary permeability that:
—- w/o spaces in between
—- do not easily pass through

A

Continuous

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Ex. Of drugs that passes through continuous type

A

LUNA - passes through BBB
Super lipophilic

Ex. 1st gen. Antihistamines
Effect: sedative

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the 2 factors under physicochemical properties of drug.

A

Molecular weight
Solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Physicochemical factors (molecular weight)
- give ex. Of VERY large molecule (upto 2000kDa)
- it stays at_____

A

Dextran
- Plasma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Physicochemical factors (molecular weight)
- give ex. Of large molecule (5-30 kDa)
- it stays at_____

A

Heparin
- extracellular space

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Why High MW - X Pass through cell membrane ?

A

Because of large structure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

(Solubility)
Hydrophilic, ionized drug stays at_____

A

Extracellular fluid(space)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

(Solubility)
Lipophilic compounds is readily diffuse into_____

A

Tissues

19
Q

Extremely lipid soluble compounds accumulate in the _______

A

adipose tissue

20
Q

(Factor) Indicator of the extent of drug distribution into body fluids and tissues
• Relates the amount of drug in the body to the measured concentration in the plasma
𝑉𝑜𝑙𝑢𝑚𝑒 𝑜𝑓 𝑑𝑖𝑠𝑡𝑟𝑖𝑏𝑢𝑡𝑖𝑜𝑛 (𝑉d ) = 𝑎𝑚𝑜𝑢𝑛𝑡 𝑜𝑓 𝑑𝑟𝑢𝑔 /𝑝𝑙𝑎𝑠𝑚𝑎 𝑐𝑜𝑛𝑐𝑒𝑛𝑡𝑟𝑎𝑡𝑖𝑜𝑛 (𝐶”)
• Important for the calculation of loading dose

total amount of administered drug would have to occupy (if it were uniformly distributed), to provide the same concentration as it currently is in blood plasma.

A

Volume of Distribution or apparent volume of distribution

21
Q

Correlation of Vd with body fluids
• Total body fluids =___% of BW (males); ____% of BW (females)

Intracellular fluids = ____% of BW o Extracellular fluids =____% of BW

■ Interstitial compartment =___% BW ■ Intravascularcompartment=__%BW

A

TBF male: 60%
TBF female: 50-55%

ICF: 40%
EXF: 20%

ISC: 15%
IVC: 5%

22
Q

Volume of Distribution of Warfarin

A

8

23
Q

Volume of Distribution of Gentamicin

A

18

24
Q

Volume of Distribution of Digoxin

A

440

25
Q

Volume of Distribution of Diazepam

A

80

26
Q

Volume of Distribution of Diazepam

A

80

27
Q

Volume of Distribution of Nortriptyline

A

1700

28
Q

Volume of Distribution of Chloroquine

A

> 15000

29
Q

SIGNIFICANCE of determining drug__________:
• Provides slow release form of a drug (repository, resulting to extended effect)
• Limit access to certain body compartments
• Can make the drug prone to drug-drug interaction

A

Protein binding

30
Q

(3) SIGNIFICANCE of determining drug protein binding:

A

1.Provides slow release form of a drug (repository, resulting to extended effect)
2.Limit access to certain body compartments
3.Can make the drug prone to drug-drug interaction

31
Q

Protein binding of Gentamicin

A

3

32
Q

Protein binding of Gentamicin

A

3

33
Q

Protein binding of Digoxin

A

25

34
Q

Protein binding of Vancomycin

A

30

35
Q

Protein binding of Lidocaine

A

51

36
Q

Protein binding of phenytoin

A

89

37
Q

Protein binding of warfarin

A

99

38
Q

2 types of plasma protein

A

Albumin
Alpha 1 acid glycoprotein

39
Q

Types of plasma protein that bind to drug w/ neutral and acidic pH ( low pH)

A

Albumin

40
Q

Give 3 example of drug with neutral pH

A

Chloramphenicol
Dexamethasone
Diazepam

41
Q

Give 4 example of drug with acidic/weak acid

A

Barbiturates
Penicillins
Salicylates (Aspirin)
Gentamicin

42
Q

Types of plasma protein that bind to weak bases

A

Alpha 1 acid glycoprotein

43
Q

Give 3 example of drug with weak base

A

Lidocaine (Xylocaine)
Saquinavir
Propranolol

44
Q

Significance of determining drug protein binding

A

Protein displacement