CB - Pharmacokinetics Flashcards
What is pharmacodynamics, and what does it involve?
Effect of the drug in the body
- D→R interactions
- Processes specific to each class of drug
What is pharmacokinetics, and what does it involve?
Effect of the body on drug delivery to site of action
- Generally the same for most drugs (ADME) irrespective of their therapeutic activity
Why is understanding pharmacokinetics important in drug use? (7)
- Time of onset of action
- Intensity and duration of effect
- Accumulation
- Inter-individual differences
- Intra-individual differences
- Drug interactions
- Inter-species differences
What are the 4 key pharmacokinetic processes?
- ABSORPTION
- DISTRIBUTION
- METABOLISM
- EXCRETION
Where do drugs go? (5)
- Body tissues (Peripheral compartment)
- Liver
- Kidneys
- Lungs
- Site of action → Effect
How can you measure the therapeutic effect of a drug? (4)
- Take blood samples
- Extract plasma
- Use drug concentration in the plasma
- Correlate that to the therapeutic effect
(Generally a linear relationship)
What are the different routes of drug administration? (4)
Intravenous dose → GENERAL CIRCULATION
Oral dose → LIVER → Metabolism, Bile
Intramuscular dose → BODY TISSUES
Inhaled dose → LUNGS → Excretion
What is involved in absorption of a drug?
Processes that take place between the site of administration and the site of measurement
How do different drugs cross the membrane for absorption? (3)
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
What are 5 factors affecting absorption?
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
What are ionisable properties of drug acids?
Weak acids
- Ionised at high pH
Strong acid
- Have a pKa of less than 3
Very strong acids (pKa 1-2)
- Poorly absorbed
What are ionisable properties of drug bases?
Weak bases
- Ionised at low pH
Strong bases
- Have a pKa of more than 10
Very strong bases (pKa >10)
- Poorly absorbed