Drug Disposition - Lecture 2 Flashcards

1
Q

What are the fates of drug in the body?

A

Absorption
Distribution
Metabolism
Excretion

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2
Q

What two process combine together to create the process of Drug Elimination?

A

Metabolism and Excretion

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3
Q

What is absorption of a drug dependent upon?

A

Solubility
Chemical Stability
Lipid to water partition coefficient

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4
Q

What quality must a drug have to be soluble to a cell?

A

It must have a degree of lipid solubility

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5
Q

What affects the rate at which a drug is absorbed?

A

The Lipid to water partition coefficient

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6
Q

What does a high Lipid to water partition coefficient mean?

A

Easily soluble with cells and can be absorbed

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7
Q

What does a low Lipid to water partition coefficient mean?

A

Not easily soluble in a cell. Difficulty being absorbed

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8
Q

What does Ka represent ?

A

The ratio of the drug that has been ionised

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9
Q

What does pKa show?

A

pH at which 50% of drug is ionised and 50% unionised

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10
Q

Is an acidic drug more ionised in an acidic environment or a basic environment?

A

Basic

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11
Q

Is an basic drug more ionised in an acidic environment or a basic environment?

A

Acidic

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12
Q

What is Systemic Availability?

A

Systsemic Availability = Amount in Systemic Circulation/Amount absorbed

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13
Q

What is first-pass or presystemic metabolism?

A

This is were a drug once absorbed can be inactivated by enzymes in the gut wall and the liver before reaching the systemic circulation

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14
Q

What are the routes of drug adminisation?

A
Oral
Inhalation
Buccal
Sublingual 
Transdermal
Subcutaneous 
Rectal
Intramuscular
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15
Q

What are the advantages of the Oral route administration?

A
  • Convenient
  • Non-sterile route
  • Good absorption for most

drugs

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16
Q

What are the disadvantages of Oral route administration?

A
  • First pass metabolism
  • Variable absorption
  • GI irritation
17
Q

What is the Buccal route/Sublingual route of administration?

A

Under the tongue

18
Q

What are the advantages of Buccal administration?

A
  • By passes the portal system and avoids first pass metabolism
  • Avoids gastric acid
19
Q

What are the disadvantages of Buccal administration?

A
  • Few sub-lingual drugs
20
Q

What are the advantages of Rectral administraiton?

A
  • Avoids First pass metabolism

- Used for nocturnal administration

21
Q

What are the disadvantages of Rectal administration?

A

-Aesthetically unacceptable

22
Q

What are the advantages of Intravenous administration?

A

Rapid onset

Continuous infusion

23
Q

What are the disadvantages of Intravenous administration?

A

Sterile preparation required

Risk of sepsis or embolism

High drug levels at the heart

24
Q

What are the advantages of Intramuscular administration?

A

Rapid onset of lipid soluble drugs

Slow prolonged release

25
Q

What are the disadvantages of Intramuscular administration?

A

Painful

Tissue damage with some drugs

26
Q

What are the two forms a drug can exist in when in a fluid compartment?

A

Bound forms

Free forms (Only free drugs are able to move compartments)

27
Q

In terms of charge, what type of drug can move readily by diffusion?

A

Unionised drugs

28
Q

What are the fluid filled compartments of the body?

A
Plasma water
Interstitial water
Intracellular water
Transcelluar water 
Fat
29
Q

What does Transcellular water consist of?

A

Cerebral Spinal Fluid
Synvoial fluid
Fluid in the eye

30
Q

How is Volume of Distribution indicate?

A

Vd(Volume) = Dose(Mass)
———————-
Plasma Concentration

31
Q

What is the Volume of Distribution?

A

Volume of Distribution is the apparent volume in which a drug is dissolved?

32
Q

What does a Vd<5 L imply?

A

Implies the drug is retained within the vascular compartment

33
Q

What does Vd < 15L imply?

A

Suggests that the drug is restricted to the extracellular fluid

34
Q

What does a Vd > 15 L

A

Indicates distribution throughout the total body