CB - Pharmacokinetics Flashcards

1
Q

What is pharmacodynamics, and what does it involve?

A

Effect of the drug in the body

  • D→R interactions
  • Processes specific to each class of drug
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is pharmacokinetics, and what does it involve?

A

Effect of the body on drug delivery to site of action

  • Generally the same for most drugs (ADME) irrespective of their therapeutic activity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Why is understanding pharmacokinetics important in drug use? (7)

A
  1. Time of onset of action
  2. Intensity and duration of effect
  3. Accumulation
  4. Inter-individual differences
  5. Intra-individual differences
  6. Drug interactions
  7. Inter-species differences
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the 4 key pharmacokinetic processes?

A
  1. ABSORPTION
  2. DISTRIBUTION
  3. METABOLISM
  4. EXCRETION
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Where do drugs go? (5)

A
  • Body tissues (Peripheral compartment)
  • Liver
  • Kidneys
  • Lungs
  • Site of action → Effect
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How can you measure the therapeutic effect of a drug? (4)

A
  1. Take blood samples
  2. Extract plasma
  3. Use drug concentration in the plasma
  4. Correlate that to the therapeutic effect
    (Generally a linear relationship)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the different routes of drug administration? (4)

A

Intravenous dose → GENERAL CIRCULATION

Oral dose → LIVER → Metabolism, Bile

Intramuscular dose → BODY TISSUES

Inhaled dose → LUNGS → Excretion

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

What is involved in absorption of a drug?

A

Processes that take place between the site of administration and the site of measurement

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

How do different drugs cross the membrane for absorption? (3)

A

MEMBRANE PORES – Low molecular weights (<200Da) or small ions (Li+)

DIFFUSION THROUGH MEMBRANE – Lipid soluble molecules

CARRIER MEDIATED – The drug must resemble a natural ligand or substrate

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

What are 5 factors affecting absorption?

A

1) LIPID SOLUBILITY

  • Rapid absorption from gut
  • Slow absorption from intra-muscular

2) IONISATION

  • Poor absorption for ionic drugs (from gut)
  • pH partitioning

3) FORMULATION

  • May limit rate of absorption
  • May limit extent of absorption

4) GASTRO-INTESTINAL FUNCTION

  • May limit rate of delivery to site of absorption
  • May limit time available for absorption

5) FIRST-PASS METABOLISM

  • May limit extent of absorption
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are ionisable properties of drug acids?

A

Weak acids

  • Ionised at high pH

Strong acid

  • Have a pKa of less than 3

Very strong acids (pKa 1-2)

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

What are ionisable properties of drug bases?

A

Weak bases

  • Ionised at low pH

Strong bases

  • Have a pKa of more than 10

Very strong bases (pKa >10)

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